MEDICATION SAFETY ISSUES
International issues:
Aliskiren may be confused with Aliseum which is a brand name for diazepam in Italy
U.S. BRAND NAMES — Tekturna®
PHARMACOLOGIC CATEGORY
Renin Inhibitor
DOSING: ADULTS — Hypertension: Initial: 150 mg once daily; may increase to 300 mg once daily (maximum: 300 mg/day). Note: Prior to initiation, correct hypovolemia and/or closely monitor volume status in patients on concurrent diuretics during treatment initiation.
DOSING: PEDIATRIC — Children <18 years: Dosage not established.
DOSING: ELDERLY — Refer to adult dosing. No initial dosage adjustment required.
DOSING: RENAL IMPAIRMENT
Mild-to-moderate impairment [GFR >30 mL/minute and/or Scr <1.7 mg/dL (women); Scr <2 mg/dL (men)]: No dose adjustment required
Severe impairment [GFR<30>1.7 mg/dL (women); Scr >2 mg/dL (men)]: Use caution; not studied in severe renal impairment
DOSING: HEPATIC IMPAIRMENT — No dosage adjustment required.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet:
Tekturna®: 150 mg, 300 mg
DOSAGE FORMS: CONCISE
Tablet:
Tekturna®: 150 mg, 300 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer at the same time daily; may take with or without a meal, but consistent administration with regards to meals is recommended. Avoid taking with high-fat meals.
USE — Treatment of hypertension, alone or in combination with other antihypertensive agents
USE - UNLABELED / INVESTIGATIONAL — Treatment of persistent proteinuria in patients with type 2 diabetes mellitus, hypertension, and nephropathy despite administration of optimized recommended renoprotective therapy (eg, angiotensin II receptor blocker)
ADVERSE REACTIONS SIGNIFICANT
1% to 10%:
Central nervous system: Dizziness (2%)
Dermatologic: Rash (1%)
Endocrine & metabolic: Hyperkalemia (monotherapy ≤ 1%; concurrent with ACE inhibitor in patients with diabetes 6%)
Gastrointestinal: Diarrhea (1% to 2%)
Hematologic: Creatine kinase increased (>300%: 1%)
Renal: BUN increased (≤ 7%), serum creatinine increased (≤ 7%)
Respiratory: Cough (1%)
<1% (Limited to important or life-threatening): Abdominal pain, anemia, angina, angioedema, dyspepsia, gastroesophageal reflux, gout, hypotension (severe), myositis, renal stone formation, rhabdomyolysis, seizure, uric acid increased
CONTRAINDICATIONS
U.S. labeling: There are no contraindications listed in manufacturer's labeling.
Canada labeling: Hypersensitivity to aliskiren or any component of the formulation
WARNINGS / PRECAUTIONS
Boxed warnings: Pregnancy: See "Special populations" below.
Concerns related to adverse effects: Angioedema: Since the effect of aliskiren on bradykinin levels is unknown, the risk of kinin-mediated etiologies of angioedema occurring is also unknown. Use caution in any patient with a history of angioedema (of any etiology) as angioedema has been observed (rarely) with aliskiren use. Discontinue immediately following any signs and symptoms of angioedema. Prolonged frequent monitoring may be required especially if tongue, glottis, or larynx are involved as they are associated with airway obstruction. Patients with a history of airway surgery may have a higher risk of airway obstruction. Aggressive early and appropriate management is critical. Hyperkalemia: May occur (rarely) during monotherapy; risk may increase in patients with predisposing factors (eg, renal dysfunction, diabetes mellitus or concomitant use with ACE inhibitors, potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts). Hypotension: During the initiation of therapy, symptomatic hypotension may occur (rarely), particularly in patients with an activated renin-angiotensin system (ie, volume or salt-depleted patients)
Disease-related concerns: Renal impairment: Use with caution in patients with severe renal impairment; not studied in patients with severe renal impairment [GFR <30>1.7 mg/dL (women); Scr >2 mg/dL (men)], history of dialysis, nephrotic syndrome, or renovascular hypertension. Use with caution or avoid in patients with deteriorating renal function or renal artery stenosis (bilateral or unilateral).
Concurrent drug therapy issues: High potential for interactions: Use caution in patients taking strong inhibitors of P-glycoprotein (eg, cyclosporine).
Special populations: Pediatrics: Safety and efficacy have not been established in children. Pregnancy: [U.S. Boxed Warning]: Based on human data, drugs that act on the angiotensin system can cause injury and death to the developing fetus when used in the second and third trimesters. Aliskiren should be discontinued as soon as possible once pregnancy is detected.
METABOLISM / TRANSPORT EFFECTS — Substrate of CYP3A4 (minor)
DRUG INTERACTIONS
Amifostine: Antihypertensives may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, antihypertensive medications should be withheld for 24 hours prior to amifostine administration. If antihypertensive therapy can not be withheld, amifostine should not be administered. Risk D: Consider therapy modification
Antihypertensives: May enhance the hypotensive effect of other Antihypertensives. Risk C: Monitor therapy
Atorvastatin: May increase the serum concentration of Aliskiren. Risk C: Monitor therapy
CycloSPORINE: May increase the serum concentration of Aliskiren. Risk X: Avoid combination
Diazoxide: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Furosemide: Aliskiren may decrease the serum concentration of Furosemide. Risk C: Monitor therapy
Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Ketoconazole: May increase the serum concentration of Aliskiren. Risk C: Monitor therapy
MAO Inhibitors: May enhance the hypotensive effect of Antihypertensives. MAO Inhibitors may enhance the orthostatic effect of Antihypertensives. Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Pentoxifylline: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-Glycoprotein Inhibitors: May increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
RiTUXimab: Antihypertensives may enhance the hypotensive effect of RiTUXimab. Risk D: Consider therapy modification
Yohimbine: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: High-fat meals decrease absorption.
PREGNANCY RISK FACTOR — C (show table) (1st trimester); D (2nd and 3rd trimesters)
PREGNANCY IMPLICATIONS — Medications which act on the renin-angiotensin system are reported to have the following fetal/neonatal effects: Hypotension, neonatal skull hypoplasia, anuria, renal failure, and death; oligohydramnios is also reported. These effects are reported to occur with exposure during the second and third trimesters. There are no adequate and well-controlled studies in pregnant women. [U.S. Boxed Warning]: Based on human data, drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus when used in the second and third trimesters. Aliskiren should be discontinued as soon as possible once pregnancy is detected.
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — May be taken with or without food; however, a high-fat meal reduces absorption
PRICING — (data from drugstore.com)
Tablets (Tekturna)
150 mg (30): $82.38
300 mg (30): $101.80
MONITORING PARAMETERS — Blood pressure; serum potassium, BUN, serum creatinine
CANADIAN BRAND NAMES — Rasilez®
INTERNATIONAL BRAND NAMES — Enviage (EE); Rasilez (BE, CH, CZ, DE, DK, EE, GB, ID, IE, IL, NO, PE, PH, SE); Tekturna (EE)
MECHANISM OF ACTION — Aliskerin is a direct renin inhibitor, resulting in blockade of the conversion of angiotensinogen to angiotensin I. Angiotensin I suppression decreases the formation of angiotensin II (Ang II), a potent blood pressure-elevating peptide (via direct vasoconstriction, aldosterone release, and sodium retention). Ang II also functions within the Renin-Angiotensin-Aldosterone System (RAAS) as a negative inhibitory feedback mediator within the renal parenchyma to suppress the further release of renin. Thus, reductions in Ang II levels suppress this feedback loop, leading to further increased plasma renin concentrations (PRC) and subsequent activity (PRA). This disinhibition effect can be potentially problematic for ACE inhibitor and ARB therapy, as increased PRA could partially overcome the pharmacologic inhibition of the RAAS. As aliskiren is a direct inhibitor of renin activity, blunting of PRA despite the increased PRC (from loss of the negative feedback) may be clinically advantageous. The effect of aliskiren on bradykinin levels is unknown.
PHARMACODYNAMICS / KINETICS
Onset of action: Maximum antihypertensive effect: Within 2 weeks
Absorption: Poor; absorption decreased by high-fat meal. Aliskiren is a substrate of P-glycoprotein; concurrent use of P-glycoprotein inhibitors may increase absorption.
Metabolism: Extent of metabolism unknown; in vitro studies indicate metabolism via CYP3A4
Bioavailability: ~3%
Half-life elimination: ~24 hours (range: 16-32 hours)
Time to peak, plasma: 1-3 hours
Excretion: Urine (~25% of absorbed dose excreted unchanged in urine); feces (unchanged via biliary excretion)
Sunday, May 30, 2010
Alglucosidase alfa
MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Alglucosidase alfa may be confused with agalsidase alfa, agalsidase beta, alglucerase
SPECIAL ALERTS
Myozyme® Shortage - January 2009
Inventory levels of Myozyme® (alglucosidase alfa) are low because of increased global demand. Increased production is planned once regulatory agencies throughout the world approve a larger scale manufacturing process. In the U.S., the Food and Drug Administration (FDA) is expected to respond by the end of February. In the meantime, recommended guidelines have been developed to help with clinical decisions during this temporary period of supply constraint. Pediatric dosing regimens will be maintained. However, to continue providing therapy to adult patients, adult regimens will be adjusted by increasing the dosing interval. Children with newly-diagnosed disease may begin therapy, but no new adults will be enrolled in the Myozyme® Temporary Access Program (MTAP). Any physician who feels their patient is in urgent need of therapy may contact Genzyme Medical Information at (800) 745-4447, option 2.
Additional information may be found at:
http://www.myozyme.com/pdf/MTAP_Supply_Update_January%202009.pdf
http://www.myozyme.com/MTAP/mtap_pt.asp
U.S. BRAND NAMES — Myozyme®
PHARMACOLOGIC CATEGORY
Enzyme
DOSING: PEDIATRIC — Replacement therapy for Pompe disease (infantile onset): Children 1 month to 3.5 years (at first infusion): I.V.: 20 mg/kg over ~4 hours every 2 weeks
(For additional information see "Alglucosidase alfa: Pediatric drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg [contains mannitol 210 mg; polysorbate 80; derived from Chinese hamster ovary cells]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over ~4 hours; initiate at 1 mg/kg/hour. If tolerated, increase by 2 mg/kg/hour every 30 minutes to a maximum rate of 7 mg/kg/hour. Decrease rate or temporarily hold for infusion reactions. Infuse through a low protein-binding, 0.2 micron in-line filter.
COMPATIBILITY — Stable in NS; do not infuse with other products.
USE — Replacement therapy for Pompe disease (infantile onset)
ADVERSE REACTIONS SIGNIFICANT
>20%:
Cardiovascular: Tachycardia (23%), bradycardia (21%), flushing (21%)
Central nervous system: Fever (92%), pain (postprocedural: 26%)
Dermatologic: Rash (54%), diaper dermatitis (36%), urticaria (21%)
Gastrointestinal: Diarrhea (62%), vomiting (49%), gastroenteritis (41%), oral candidiasis (31%), gastroesophageal reflux (26%), constipation (23%)
Hematologic: Anemia (31%)
Local: Catheter-related infections (28%)
Otic: Otitis media (33% to 44%)
Respiratory: Cough (46%), pneumonia (46%), upper respiratory tract infection (44%), oxygen saturation decreased (41%), pharyngitis (36%), respiratory distress (33%), respiratory failure (31%), rhinorrhea (28%), bronchiolitis (23%), nasopharyngitis (23%), tachypnea (23%)
Miscellaneous: Antibodies to alglucosidase alfa (89%; may affect efficacy), infusion reaction (51%)
Frequency not reported and/or case reports: Abdominal pain, agitation, anaphylactic reactions, bronchospasm, cardiac arrest, cardiorespiratory failure, chest discomfort/pain, conjunctivitis, cyanosis, erythema, face edema, facial erythema, fatigue, fluid overload, headache, hyperhidrosis, hypersensitivity, hyper-/hypotension, irritability, lacrimation increased, livedo reticularis, malaise, muscle spasm, nausea, pallor, periorbital edema, peripheral edema, pruritus, respiratory syncytial virus infection, restlessness, retching, rhinitis, rigors, skin lesions (ulcerative/necrotizing), tremor, wheezing
CONTRAINDICATIONS — There are no contraindications listed in the manufacturer's labeling.
WARNINGS / PRECAUTIONS
Boxed warnings: Anaphylaxis/hypersensitivity reactions: See "Concerns related to adverse effects" below. Cardiovascular disease: See "Disease-related concerns" below. Respiratory disease: See "Disease-related concerns" below.
Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: [U.S. Boxed Warning]: Severe hypersensitivity reactions, including anaphylactic reactions and anaphylactic shock have been reported during and within 3 hours after infusion. Immediate medical support should be readily available. Immune-mediated reactions: Severe immune-mediated reactions (eg, ulcerative and necrotizing skin lesions, type-III immune complex-mediated reactions, inflammatory arthropathy) have occurred up to 3 years after initiation of therapy; monitor for development. Infusion reactions: Infusion-related reactions are common; discontinue immediately for severe hypersensitivity or anaphylactic reaction; mild-to-moderate reactions may be managed by reducing the infusion rate and/or administering antihistamines and/or antipyretics. Appropriate medical support for the management of infusion reactions should be readily available. Use caution with subsequent infusions; infusion reactions have occurred despite premedication with antihistamines, antipyretics, and/or steroids. Patients with acute underlying illness are at greater risk for infusion reactions, including cardiorespiratory failure.
Disease-related concerns: Cardiovascular disease: [U.S. Boxed Warning]: Use with caution in patients with compromised cardiac function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted. Cardiorespiratory failure has been observed in patients with cardiac hypertrophy up to 72 hours after infusion; arrhythmias have also been observed in patients with cardiac hypertrophy. Pompe disease: Safety and efficacy have not been established in juvenile-onset and adult-onset Pompe disease. Patients with Pompe disease are at increased risk for infusion-related cardiorespiratory failure (possibly due to fluid overload); monitor closely during infusion. Respiratory disease: [U.S. Boxed Warning]: Use with caution in patients with compromised respiratory function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted.
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.pomperegistry.com or 1-800-745-4447).
DRUG INTERACTIONS — There are no known significant interactions.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Animal studies have not demonstrated teratogenicity or fertility impairment. There are no adequate and well-controlled studies in pregnant women. A registry has been established for Pompe patients; women of childbearing potential are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447).
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — A registry has been established for Pompe patients; women who are nursing are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447)
MONITORING PARAMETERS — Liver enzymes (baseline and periodically; elevation may be due to disease process); vital signs during and following infusion; volume overload
The manufacturer recommends monitoring for IgG antibody formation every 3 months. No commercial tests are available; however, sampling kits can be obtained by contacting Genzyme Corporation at 1-800-745-4447.
INTERNATIONAL BRAND NAMES — Myozyme (AT, BE, BG, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, NL, NO, PT, RU, SE, TR, TW)
MECHANISM OF ACTION — Alglucosidase alfa is a recombinant form of the enzyme acid alpha-glucosidase (GAA), which is required for glycogen cleavage. Due to an inherited GAA deficiency, glycogen accumulates in the tissues of patients with Pompe disease, leading to progressive muscle weakness. In infantile-onset Pompe disease, glycogen accumulates in cardiac and skeletal muscles and hepatic tissue, leading to cardiomyopathy and respiratory failure. Juvenile- and adult-onset Pompe disease are limited to glycogen accumulation in skeletal muscle, leading to respiratory failure. Alglucosidase alfa binds to mannose-6-phosphate receptors on the cell surface, becomes internalized and transported to lysosomes resulting in increased enzymatic activity and glycogen cleavage.
PHARMACODYNAMICS / KINETICS
Distribution: Vss: 80-147 mL/kg
Half-life elimination: 2-3 hours
Sound-alike/look-alike issues:
Alglucosidase alfa may be confused with agalsidase alfa, agalsidase beta, alglucerase
SPECIAL ALERTS
Myozyme® Shortage - January 2009
Inventory levels of Myozyme® (alglucosidase alfa) are low because of increased global demand. Increased production is planned once regulatory agencies throughout the world approve a larger scale manufacturing process. In the U.S., the Food and Drug Administration (FDA) is expected to respond by the end of February. In the meantime, recommended guidelines have been developed to help with clinical decisions during this temporary period of supply constraint. Pediatric dosing regimens will be maintained. However, to continue providing therapy to adult patients, adult regimens will be adjusted by increasing the dosing interval. Children with newly-diagnosed disease may begin therapy, but no new adults will be enrolled in the Myozyme® Temporary Access Program (MTAP). Any physician who feels their patient is in urgent need of therapy may contact Genzyme Medical Information at (800) 745-4447, option 2.
Additional information may be found at:
http://www.myozyme.com/pdf/MTAP_Supply_Update_January%202009.pdf
http://www.myozyme.com/MTAP/mtap_pt.asp
U.S. BRAND NAMES — Myozyme®
PHARMACOLOGIC CATEGORY
Enzyme
DOSING: PEDIATRIC — Replacement therapy for Pompe disease (infantile onset): Children 1 month to 3.5 years (at first infusion): I.V.: 20 mg/kg over ~4 hours every 2 weeks
(For additional information see "Alglucosidase alfa: Pediatric drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg [contains mannitol 210 mg; polysorbate 80; derived from Chinese hamster ovary cells]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over ~4 hours; initiate at 1 mg/kg/hour. If tolerated, increase by 2 mg/kg/hour every 30 minutes to a maximum rate of 7 mg/kg/hour. Decrease rate or temporarily hold for infusion reactions. Infuse through a low protein-binding, 0.2 micron in-line filter.
COMPATIBILITY — Stable in NS; do not infuse with other products.
USE — Replacement therapy for Pompe disease (infantile onset)
ADVERSE REACTIONS SIGNIFICANT
>20%:
Cardiovascular: Tachycardia (23%), bradycardia (21%), flushing (21%)
Central nervous system: Fever (92%), pain (postprocedural: 26%)
Dermatologic: Rash (54%), diaper dermatitis (36%), urticaria (21%)
Gastrointestinal: Diarrhea (62%), vomiting (49%), gastroenteritis (41%), oral candidiasis (31%), gastroesophageal reflux (26%), constipation (23%)
Hematologic: Anemia (31%)
Local: Catheter-related infections (28%)
Otic: Otitis media (33% to 44%)
Respiratory: Cough (46%), pneumonia (46%), upper respiratory tract infection (44%), oxygen saturation decreased (41%), pharyngitis (36%), respiratory distress (33%), respiratory failure (31%), rhinorrhea (28%), bronchiolitis (23%), nasopharyngitis (23%), tachypnea (23%)
Miscellaneous: Antibodies to alglucosidase alfa (89%; may affect efficacy), infusion reaction (51%)
Frequency not reported and/or case reports: Abdominal pain, agitation, anaphylactic reactions, bronchospasm, cardiac arrest, cardiorespiratory failure, chest discomfort/pain, conjunctivitis, cyanosis, erythema, face edema, facial erythema, fatigue, fluid overload, headache, hyperhidrosis, hypersensitivity, hyper-/hypotension, irritability, lacrimation increased, livedo reticularis, malaise, muscle spasm, nausea, pallor, periorbital edema, peripheral edema, pruritus, respiratory syncytial virus infection, restlessness, retching, rhinitis, rigors, skin lesions (ulcerative/necrotizing), tremor, wheezing
CONTRAINDICATIONS — There are no contraindications listed in the manufacturer's labeling.
WARNINGS / PRECAUTIONS
Boxed warnings: Anaphylaxis/hypersensitivity reactions: See "Concerns related to adverse effects" below. Cardiovascular disease: See "Disease-related concerns" below. Respiratory disease: See "Disease-related concerns" below.
Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: [U.S. Boxed Warning]: Severe hypersensitivity reactions, including anaphylactic reactions and anaphylactic shock have been reported during and within 3 hours after infusion. Immediate medical support should be readily available. Immune-mediated reactions: Severe immune-mediated reactions (eg, ulcerative and necrotizing skin lesions, type-III immune complex-mediated reactions, inflammatory arthropathy) have occurred up to 3 years after initiation of therapy; monitor for development. Infusion reactions: Infusion-related reactions are common; discontinue immediately for severe hypersensitivity or anaphylactic reaction; mild-to-moderate reactions may be managed by reducing the infusion rate and/or administering antihistamines and/or antipyretics. Appropriate medical support for the management of infusion reactions should be readily available. Use caution with subsequent infusions; infusion reactions have occurred despite premedication with antihistamines, antipyretics, and/or steroids. Patients with acute underlying illness are at greater risk for infusion reactions, including cardiorespiratory failure.
Disease-related concerns: Cardiovascular disease: [U.S. Boxed Warning]: Use with caution in patients with compromised cardiac function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted. Cardiorespiratory failure has been observed in patients with cardiac hypertrophy up to 72 hours after infusion; arrhythmias have also been observed in patients with cardiac hypertrophy. Pompe disease: Safety and efficacy have not been established in juvenile-onset and adult-onset Pompe disease. Patients with Pompe disease are at increased risk for infusion-related cardiorespiratory failure (possibly due to fluid overload); monitor closely during infusion. Respiratory disease: [U.S. Boxed Warning]: Use with caution in patients with compromised respiratory function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted.
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.pomperegistry.com or 1-800-745-4447).
DRUG INTERACTIONS — There are no known significant interactions.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Animal studies have not demonstrated teratogenicity or fertility impairment. There are no adequate and well-controlled studies in pregnant women. A registry has been established for Pompe patients; women of childbearing potential are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447).
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — A registry has been established for Pompe patients; women who are nursing are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447)
MONITORING PARAMETERS — Liver enzymes (baseline and periodically; elevation may be due to disease process); vital signs during and following infusion; volume overload
The manufacturer recommends monitoring for IgG antibody formation every 3 months. No commercial tests are available; however, sampling kits can be obtained by contacting Genzyme Corporation at 1-800-745-4447.
INTERNATIONAL BRAND NAMES — Myozyme (AT, BE, BG, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, NL, NO, PT, RU, SE, TR, TW)
MECHANISM OF ACTION — Alglucosidase alfa is a recombinant form of the enzyme acid alpha-glucosidase (GAA), which is required for glycogen cleavage. Due to an inherited GAA deficiency, glycogen accumulates in the tissues of patients with Pompe disease, leading to progressive muscle weakness. In infantile-onset Pompe disease, glycogen accumulates in cardiac and skeletal muscles and hepatic tissue, leading to cardiomyopathy and respiratory failure. Juvenile- and adult-onset Pompe disease are limited to glycogen accumulation in skeletal muscle, leading to respiratory failure. Alglucosidase alfa binds to mannose-6-phosphate receptors on the cell surface, becomes internalized and transported to lysosomes resulting in increased enzymatic activity and glycogen cleavage.
PHARMACODYNAMICS / KINETICS
Distribution: Vss: 80-147 mL/kg
Half-life elimination: 2-3 hours
Alglucosidase alfa
MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Alglucosidase alfa may be confused with agalsidase alfa, agalsidase beta, alglucerase
SPECIAL ALERTS
Myozyme® Shortage - January 2009
Inventory levels of Myozyme® (alglucosidase alfa) are low because of increased global demand. Increased production is planned once regulatory agencies throughout the world approve a larger scale manufacturing process. In the U.S., the Food and Drug Administration (FDA) is expected to respond by the end of February. In the meantime, recommended guidelines have been developed to help with clinical decisions during this temporary period of supply constraint. Pediatric dosing regimens will be maintained. However, to continue providing therapy to adult patients, adult regimens will be adjusted by increasing the dosing interval. Children with newly-diagnosed disease may begin therapy, but no new adults will be enrolled in the Myozyme® Temporary Access Program (MTAP). Any physician who feels their patient is in urgent need of therapy may contact Genzyme Medical Information at (800) 745-4447, option 2.
Additional information may be found at:
http://www.myozyme.com/pdf/MTAP_Supply_Update_January%202009.pdf
http://www.myozyme.com/MTAP/mtap_pt.asp
U.S. BRAND NAMES — Myozyme®
PHARMACOLOGIC CATEGORY
Enzyme
DOSING: PEDIATRIC — Replacement therapy for Pompe disease (infantile onset): Children 1 month to 3.5 years (at first infusion): I.V.: 20 mg/kg over ~4 hours every 2 weeks
(For additional information see "Alglucosidase alfa: Pediatric drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg [contains mannitol 210 mg; polysorbate 80; derived from Chinese hamster ovary cells]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over ~4 hours; initiate at 1 mg/kg/hour. If tolerated, increase by 2 mg/kg/hour every 30 minutes to a maximum rate of 7 mg/kg/hour. Decrease rate or temporarily hold for infusion reactions. Infuse through a low protein-binding, 0.2 micron in-line filter.
COMPATIBILITY — Stable in NS; do not infuse with other products.
USE — Replacement therapy for Pompe disease (infantile onset)
ADVERSE REACTIONS SIGNIFICANT
>20%:
Cardiovascular: Tachycardia (23%), bradycardia (21%), flushing (21%)
Central nervous system: Fever (92%), pain (postprocedural: 26%)
Dermatologic: Rash (54%), diaper dermatitis (36%), urticaria (21%)
Gastrointestinal: Diarrhea (62%), vomiting (49%), gastroenteritis (41%), oral candidiasis (31%), gastroesophageal reflux (26%), constipation (23%)
Hematologic: Anemia (31%)
Local: Catheter-related infections (28%)
Otic: Otitis media (33% to 44%)
Respiratory: Cough (46%), pneumonia (46%), upper respiratory tract infection (44%), oxygen saturation decreased (41%), pharyngitis (36%), respiratory distress (33%), respiratory failure (31%), rhinorrhea (28%), bronchiolitis (23%), nasopharyngitis (23%), tachypnea (23%)
Miscellaneous: Antibodies to alglucosidase alfa (89%; may affect efficacy), infusion reaction (51%)
Frequency not reported and/or case reports: Abdominal pain, agitation, anaphylactic reactions, bronchospasm, cardiac arrest, cardiorespiratory failure, chest discomfort/pain, conjunctivitis, cyanosis, erythema, face edema, facial erythema, fatigue, fluid overload, headache, hyperhidrosis, hypersensitivity, hyper-/hypotension, irritability, lacrimation increased, livedo reticularis, malaise, muscle spasm, nausea, pallor, periorbital edema, peripheral edema, pruritus, respiratory syncytial virus infection, restlessness, retching, rhinitis, rigors, skin lesions (ulcerative/necrotizing), tremor, wheezing
CONTRAINDICATIONS — There are no contraindications listed in the manufacturer's labeling.
WARNINGS / PRECAUTIONS
Boxed warnings: Anaphylaxis/hypersensitivity reactions: See "Concerns related to adverse effects" below. Cardiovascular disease: See "Disease-related concerns" below. Respiratory disease: See "Disease-related concerns" below.
Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: [U.S. Boxed Warning]: Severe hypersensitivity reactions, including anaphylactic reactions and anaphylactic shock have been reported during and within 3 hours after infusion. Immediate medical support should be readily available. Immune-mediated reactions: Severe immune-mediated reactions (eg, ulcerative and necrotizing skin lesions, type-III immune complex-mediated reactions, inflammatory arthropathy) have occurred up to 3 years after initiation of therapy; monitor for development. Infusion reactions: Infusion-related reactions are common; discontinue immediately for severe hypersensitivity or anaphylactic reaction; mild-to-moderate reactions may be managed by reducing the infusion rate and/or administering antihistamines and/or antipyretics. Appropriate medical support for the management of infusion reactions should be readily available. Use caution with subsequent infusions; infusion reactions have occurred despite premedication with antihistamines, antipyretics, and/or steroids. Patients with acute underlying illness are at greater risk for infusion reactions, including cardiorespiratory failure.
Disease-related concerns: Cardiovascular disease: [U.S. Boxed Warning]: Use with caution in patients with compromised cardiac function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted. Cardiorespiratory failure has been observed in patients with cardiac hypertrophy up to 72 hours after infusion; arrhythmias have also been observed in patients with cardiac hypertrophy. Pompe disease: Safety and efficacy have not been established in juvenile-onset and adult-onset Pompe disease. Patients with Pompe disease are at increased risk for infusion-related cardiorespiratory failure (possibly due to fluid overload); monitor closely during infusion. Respiratory disease: [U.S. Boxed Warning]: Use with caution in patients with compromised respiratory function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted.
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.pomperegistry.com or 1-800-745-4447).
DRUG INTERACTIONS — There are no known significant interactions.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Animal studies have not demonstrated teratogenicity or fertility impairment. There are no adequate and well-controlled studies in pregnant women. A registry has been established for Pompe patients; women of childbearing potential are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447).
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — A registry has been established for Pompe patients; women who are nursing are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447)
MONITORING PARAMETERS — Liver enzymes (baseline and periodically; elevation may be due to disease process); vital signs during and following infusion; volume overload
The manufacturer recommends monitoring for IgG antibody formation every 3 months. No commercial tests are available; however, sampling kits can be obtained by contacting Genzyme Corporation at 1-800-745-4447.
INTERNATIONAL BRAND NAMES — Myozyme (AT, BE, BG, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, NL, NO, PT, RU, SE, TR, TW)
MECHANISM OF ACTION — Alglucosidase alfa is a recombinant form of the enzyme acid alpha-glucosidase (GAA), which is required for glycogen cleavage. Due to an inherited GAA deficiency, glycogen accumulates in the tissues of patients with Pompe disease, leading to progressive muscle weakness. In infantile-onset Pompe disease, glycogen accumulates in cardiac and skeletal muscles and hepatic tissue, leading to cardiomyopathy and respiratory failure. Juvenile- and adult-onset Pompe disease are limited to glycogen accumulation in skeletal muscle, leading to respiratory failure. Alglucosidase alfa binds to mannose-6-phosphate receptors on the cell surface, becomes internalized and transported to lysosomes resulting in increased enzymatic activity and glycogen cleavage.
PHARMACODYNAMICS / KINETICS
Distribution: Vss: 80-147 mL/kg
Half-life elimination: 2-3 hours
Sound-alike/look-alike issues:
Alglucosidase alfa may be confused with agalsidase alfa, agalsidase beta, alglucerase
SPECIAL ALERTS
Myozyme® Shortage - January 2009
Inventory levels of Myozyme® (alglucosidase alfa) are low because of increased global demand. Increased production is planned once regulatory agencies throughout the world approve a larger scale manufacturing process. In the U.S., the Food and Drug Administration (FDA) is expected to respond by the end of February. In the meantime, recommended guidelines have been developed to help with clinical decisions during this temporary period of supply constraint. Pediatric dosing regimens will be maintained. However, to continue providing therapy to adult patients, adult regimens will be adjusted by increasing the dosing interval. Children with newly-diagnosed disease may begin therapy, but no new adults will be enrolled in the Myozyme® Temporary Access Program (MTAP). Any physician who feels their patient is in urgent need of therapy may contact Genzyme Medical Information at (800) 745-4447, option 2.
Additional information may be found at:
http://www.myozyme.com/pdf/MTAP_Supply_Update_January%202009.pdf
http://www.myozyme.com/MTAP/mtap_pt.asp
U.S. BRAND NAMES — Myozyme®
PHARMACOLOGIC CATEGORY
Enzyme
DOSING: PEDIATRIC — Replacement therapy for Pompe disease (infantile onset): Children 1 month to 3.5 years (at first infusion): I.V.: 20 mg/kg over ~4 hours every 2 weeks
(For additional information see "Alglucosidase alfa: Pediatric drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg [contains mannitol 210 mg; polysorbate 80; derived from Chinese hamster ovary cells]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Myozyme®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over ~4 hours; initiate at 1 mg/kg/hour. If tolerated, increase by 2 mg/kg/hour every 30 minutes to a maximum rate of 7 mg/kg/hour. Decrease rate or temporarily hold for infusion reactions. Infuse through a low protein-binding, 0.2 micron in-line filter.
COMPATIBILITY — Stable in NS; do not infuse with other products.
USE — Replacement therapy for Pompe disease (infantile onset)
ADVERSE REACTIONS SIGNIFICANT
>20%:
Cardiovascular: Tachycardia (23%), bradycardia (21%), flushing (21%)
Central nervous system: Fever (92%), pain (postprocedural: 26%)
Dermatologic: Rash (54%), diaper dermatitis (36%), urticaria (21%)
Gastrointestinal: Diarrhea (62%), vomiting (49%), gastroenteritis (41%), oral candidiasis (31%), gastroesophageal reflux (26%), constipation (23%)
Hematologic: Anemia (31%)
Local: Catheter-related infections (28%)
Otic: Otitis media (33% to 44%)
Respiratory: Cough (46%), pneumonia (46%), upper respiratory tract infection (44%), oxygen saturation decreased (41%), pharyngitis (36%), respiratory distress (33%), respiratory failure (31%), rhinorrhea (28%), bronchiolitis (23%), nasopharyngitis (23%), tachypnea (23%)
Miscellaneous: Antibodies to alglucosidase alfa (89%; may affect efficacy), infusion reaction (51%)
Frequency not reported and/or case reports: Abdominal pain, agitation, anaphylactic reactions, bronchospasm, cardiac arrest, cardiorespiratory failure, chest discomfort/pain, conjunctivitis, cyanosis, erythema, face edema, facial erythema, fatigue, fluid overload, headache, hyperhidrosis, hypersensitivity, hyper-/hypotension, irritability, lacrimation increased, livedo reticularis, malaise, muscle spasm, nausea, pallor, periorbital edema, peripheral edema, pruritus, respiratory syncytial virus infection, restlessness, retching, rhinitis, rigors, skin lesions (ulcerative/necrotizing), tremor, wheezing
CONTRAINDICATIONS — There are no contraindications listed in the manufacturer's labeling.
WARNINGS / PRECAUTIONS
Boxed warnings: Anaphylaxis/hypersensitivity reactions: See "Concerns related to adverse effects" below. Cardiovascular disease: See "Disease-related concerns" below. Respiratory disease: See "Disease-related concerns" below.
Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: [U.S. Boxed Warning]: Severe hypersensitivity reactions, including anaphylactic reactions and anaphylactic shock have been reported during and within 3 hours after infusion. Immediate medical support should be readily available. Immune-mediated reactions: Severe immune-mediated reactions (eg, ulcerative and necrotizing skin lesions, type-III immune complex-mediated reactions, inflammatory arthropathy) have occurred up to 3 years after initiation of therapy; monitor for development. Infusion reactions: Infusion-related reactions are common; discontinue immediately for severe hypersensitivity or anaphylactic reaction; mild-to-moderate reactions may be managed by reducing the infusion rate and/or administering antihistamines and/or antipyretics. Appropriate medical support for the management of infusion reactions should be readily available. Use caution with subsequent infusions; infusion reactions have occurred despite premedication with antihistamines, antipyretics, and/or steroids. Patients with acute underlying illness are at greater risk for infusion reactions, including cardiorespiratory failure.
Disease-related concerns: Cardiovascular disease: [U.S. Boxed Warning]: Use with caution in patients with compromised cardiac function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted. Cardiorespiratory failure has been observed in patients with cardiac hypertrophy up to 72 hours after infusion; arrhythmias have also been observed in patients with cardiac hypertrophy. Pompe disease: Safety and efficacy have not been established in juvenile-onset and adult-onset Pompe disease. Patients with Pompe disease are at increased risk for infusion-related cardiorespiratory failure (possibly due to fluid overload); monitor closely during infusion. Respiratory disease: [U.S. Boxed Warning]: Use with caution in patients with compromised respiratory function; risk of acute cardiorespiratory failure secondary to infusion-related reactions may be increased. Additional monitoring is warranted.
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.pomperegistry.com or 1-800-745-4447).
DRUG INTERACTIONS — There are no known significant interactions.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Animal studies have not demonstrated teratogenicity or fertility impairment. There are no adequate and well-controlled studies in pregnant women. A registry has been established for Pompe patients; women of childbearing potential are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447).
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — A registry has been established for Pompe patients; women who are nursing are encouraged to enroll in the registry (www.pomperegistry.com or 1-800-745-4447)
MONITORING PARAMETERS — Liver enzymes (baseline and periodically; elevation may be due to disease process); vital signs during and following infusion; volume overload
The manufacturer recommends monitoring for IgG antibody formation every 3 months. No commercial tests are available; however, sampling kits can be obtained by contacting Genzyme Corporation at 1-800-745-4447.
INTERNATIONAL BRAND NAMES — Myozyme (AT, BE, BG, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, NL, NO, PT, RU, SE, TR, TW)
MECHANISM OF ACTION — Alglucosidase alfa is a recombinant form of the enzyme acid alpha-glucosidase (GAA), which is required for glycogen cleavage. Due to an inherited GAA deficiency, glycogen accumulates in the tissues of patients with Pompe disease, leading to progressive muscle weakness. In infantile-onset Pompe disease, glycogen accumulates in cardiac and skeletal muscles and hepatic tissue, leading to cardiomyopathy and respiratory failure. Juvenile- and adult-onset Pompe disease are limited to glycogen accumulation in skeletal muscle, leading to respiratory failure. Alglucosidase alfa binds to mannose-6-phosphate receptors on the cell surface, becomes internalized and transported to lysosomes resulting in increased enzymatic activity and glycogen cleavage.
PHARMACODYNAMICS / KINETICS
Distribution: Vss: 80-147 mL/kg
Half-life elimination: 2-3 hours
Basiliximab
U.S. BRAND NAMES — Simulect®
PHARMACOLOGIC CATEGORY
Monoclonal Antibody
DOSING: ADULTS — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
Renal transplantation: I.V.: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation. The second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss).
DOSING: PEDIATRIC — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
(For additional information see "Basiliximab: Pediatric drug information")
Renal transplantation: I.V.:
Children <35 kg: 10 mg within 2 hours prior to transplant surgery, followed by a second 10 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Children ≥ 35 kg: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No specific dosing adjustment is recommended.
DOSING: HEPATIC IMPAIRMENT — No specific dosing adjustment is recommended.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For intravenous administration only. Infuse as a bolus or I.V. infusion over 20-30 minutes. (Bolus dosing is associated with nausea, vomiting, and local pain at the injection site.)
USE — Prophylaxis of acute organ rejection in renal transplantation
ADVERSE REACTIONS SIGNIFICANT — Administration of basiliximab did not appear to increase the incidence or severity of adverse effects in clinical trials. Adverse events were reported in 96% of both the placebo and basiliximab groups.
>10%:
Cardiovascular: Hypertension, peripheral edema
Central nervous system: Fever, headache, insomnia, pain
Dermatologic: Acne, wound complications
Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyper-/hypokalemia, hyperuricemia, hypophosphatemia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting
Genitourinary: Urinary tract infection
Hematologic: Anemia
Neuromuscular & skeletal: Tremor
Respiratory: Dyspnea, infection (upper respiratory)
Miscellaneous: Viral infection
3% to 10%:
Cardiovascular: Abnormal heart sounds, angina pectoris, arrhythmia, atrial fibrillation, cardiac failure, chest pain, generalized edema, hypotension, tachycardia
Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise, neuropathy, rigors
Dermatologic: Cyst, hypertrichosis, pruritus, rash, skin disorder, skin ulceration
Endocrine & metabolic: Acidosis, dehydration, diabetes mellitus, fluid overload, hyper-/hypocalcemia, hyperlipidemia, hypertriglyceridemia, hypoglycemia, hypomagnesemia, hyponatremia
Gastrointestinal: Abdomen enlarged, esophagitis, flatulence, gastroenteritis, GI hemorrhage, gingival hyperplasia, melena, moniliasis, stomatitis (including ulcerative), weight gain
Genitourinary: Albuminuria, bladder disorder, dysuria, genital edema, hematuria, impotence, oliguria, renal function abnormal, renal tubular necrosis, ureteral disorder, urinary frequency, urinary retention
Hematologic: Hematoma, hemorrhage, leukopenia, polycythemia, purpura, thrombocytopenia, thrombosis
Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, cramps, fracture, hernia, leg pain, myalgia, paresthesia, weakness
Ocular: Abnormal vision, cataract, conjunctivitis
Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, sinusitis, rhinitis
Miscellaneous: Accidental trauma, facial edema, glucocorticoids increased, herpes infection, sepsis
Postmarketing and/or case reports: Capillary leak syndrome, cytokine release syndrome; severe hypersensitivity reactions, including anaphylaxis, have been reported (symptoms may include hypotension, tachycardia, cardiac failure, dyspnea, bronchospasm, pulmonary edema, urticaria, rash, pruritus, sneezing, and respiratory failure)
CONTRAINDICATIONS — Hypersensitivity to basiliximab, murine proteins, or any component of the formulation
WARNINGS / PRECAUTIONS
Boxed warnings: Experienced physician: See "Other warnings/precautions" below.
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Severe hypersensitivity reactions, occurring within 24 hours, have been reported. Reactions, including anaphylaxis, have occurred both with the initial exposure and/or following re-exposure after several months; use caution during re-exposure to a subsequent course of therapy in a patient who has previously received basiliximab. Discontinue the drug permanently if a reaction occurs. Medications for the treatment of hypersensitivity reactions should be available for immediate use. Human antimurine antibodies (HAMA): Treatment may result in the development of HAMA; however, limited evidence suggesting the use of muromonab-CD3 or other murine products is not precluded. Lymphoproliferative disorders: The incidence of lymphoproliferative disorders may be increased by immunosuppressive therapy. Opportunistic infections: The incidence opportunistic infections may be increased by immunosuppressive therapy.
Other warnings/precautions: Appropriate use: To be used as a component of immunosuppressive regimen which includes cyclosporine and corticosteroids. Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of a physician experienced in immunosuppression therapy.
DRUG INTERACTIONS
Abciximab: May enhance the potential for allergic or hypersensitivity reactions to Monoclonal Antibodies. Also may cause thrombocytopenia or diminished therapeutic effects. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemic Agents. Risk C: Monitor therapy
Hypoglycemic Agents: May enhance the adverse/toxic effect of other Hypoglycemic Agents. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Vaccinial infections may develop. Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Echinacea may diminish the therapeutic effect of basiliximab. Avoid hypoglycemic herbs, including alfalfa, bilberry, bitter melon, burdock, celery, damiana, fenugreek, garcinia, garlic, ginger, ginseng, gymnema, marshmallow, and stinging nettle (may enhance the hypoglycemic effect of basiliximab).
PREGNANCY RISK FACTOR — B (show table) (manufacturer)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. IL-2 receptors play an important role in the development of the immune system. Use in pregnant women only when benefit exceeds potential risk to the fetus. Women of childbearing potential should use effective contraceptive measures before beginning treatment and for 4 months after completion of therapy with this agent.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — It is not known whether basiliximab is excreted in human milk. Because many immunoglobulins are secreted in milk and the potential for serious adverse reactions exists, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
MONITORING PARAMETERS — Signs and symptoms of acute rejection
CANADIAN BRAND NAMES — Simulect®
INTERNATIONAL BRAND NAMES — Simulect (AR, AT, AU, BE, BG, BR, CH, CL, CN, CO, CZ, DE, DK, EC, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, KP, MX, MY, NL, NO, PE, PH, PK, PL, PT, PY, RU, SE, SG, TH, TR, TW, UY, VE)
MECHANISM OF ACTION — Chimeric (murine/human) monoclonal antibody which blocks the alpha-chain of the interleukin-2 (IL-2) receptor complex; this receptor is expressed on activated T lymphocytes and is a critical pathway for activating cell-mediated allograft rejection
PHARMACODYNAMICS / KINETICS
Duration: Mean: 36 days (determined by IL-2R alpha saturation)
Distribution: Mean: Vd: Children 1-11 years: 4.8 +/- 2.1 L; Adolescents 12-16 years: 7.8 +/- 5.1 L; Adults: 8.6 +/- 4.1 L
Half-life elimination: Children 1-11 years: 9.5 days; Adolescents 12-16 years: 9.1 days; Adults: Mean: 7.2 days
Excretion: Clearance: Children 1-11 years: 17 mL/hour; Adolescents 12-16 years: 31 mL/hour; Adults: Mean: 41 mL/hour
PHARMACOLOGIC CATEGORY
Monoclonal Antibody
DOSING: ADULTS — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
Renal transplantation: I.V.: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation. The second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss).
DOSING: PEDIATRIC — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
(For additional information see "Basiliximab: Pediatric drug information")
Renal transplantation: I.V.:
Children <35 kg: 10 mg within 2 hours prior to transplant surgery, followed by a second 10 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Children ≥ 35 kg: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No specific dosing adjustment is recommended.
DOSING: HEPATIC IMPAIRMENT — No specific dosing adjustment is recommended.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For intravenous administration only. Infuse as a bolus or I.V. infusion over 20-30 minutes. (Bolus dosing is associated with nausea, vomiting, and local pain at the injection site.)
USE — Prophylaxis of acute organ rejection in renal transplantation
ADVERSE REACTIONS SIGNIFICANT — Administration of basiliximab did not appear to increase the incidence or severity of adverse effects in clinical trials. Adverse events were reported in 96% of both the placebo and basiliximab groups.
>10%:
Cardiovascular: Hypertension, peripheral edema
Central nervous system: Fever, headache, insomnia, pain
Dermatologic: Acne, wound complications
Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyper-/hypokalemia, hyperuricemia, hypophosphatemia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting
Genitourinary: Urinary tract infection
Hematologic: Anemia
Neuromuscular & skeletal: Tremor
Respiratory: Dyspnea, infection (upper respiratory)
Miscellaneous: Viral infection
3% to 10%:
Cardiovascular: Abnormal heart sounds, angina pectoris, arrhythmia, atrial fibrillation, cardiac failure, chest pain, generalized edema, hypotension, tachycardia
Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise, neuropathy, rigors
Dermatologic: Cyst, hypertrichosis, pruritus, rash, skin disorder, skin ulceration
Endocrine & metabolic: Acidosis, dehydration, diabetes mellitus, fluid overload, hyper-/hypocalcemia, hyperlipidemia, hypertriglyceridemia, hypoglycemia, hypomagnesemia, hyponatremia
Gastrointestinal: Abdomen enlarged, esophagitis, flatulence, gastroenteritis, GI hemorrhage, gingival hyperplasia, melena, moniliasis, stomatitis (including ulcerative), weight gain
Genitourinary: Albuminuria, bladder disorder, dysuria, genital edema, hematuria, impotence, oliguria, renal function abnormal, renal tubular necrosis, ureteral disorder, urinary frequency, urinary retention
Hematologic: Hematoma, hemorrhage, leukopenia, polycythemia, purpura, thrombocytopenia, thrombosis
Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, cramps, fracture, hernia, leg pain, myalgia, paresthesia, weakness
Ocular: Abnormal vision, cataract, conjunctivitis
Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, sinusitis, rhinitis
Miscellaneous: Accidental trauma, facial edema, glucocorticoids increased, herpes infection, sepsis
Postmarketing and/or case reports: Capillary leak syndrome, cytokine release syndrome; severe hypersensitivity reactions, including anaphylaxis, have been reported (symptoms may include hypotension, tachycardia, cardiac failure, dyspnea, bronchospasm, pulmonary edema, urticaria, rash, pruritus, sneezing, and respiratory failure)
CONTRAINDICATIONS — Hypersensitivity to basiliximab, murine proteins, or any component of the formulation
WARNINGS / PRECAUTIONS
Boxed warnings: Experienced physician: See "Other warnings/precautions" below.
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Severe hypersensitivity reactions, occurring within 24 hours, have been reported. Reactions, including anaphylaxis, have occurred both with the initial exposure and/or following re-exposure after several months; use caution during re-exposure to a subsequent course of therapy in a patient who has previously received basiliximab. Discontinue the drug permanently if a reaction occurs. Medications for the treatment of hypersensitivity reactions should be available for immediate use. Human antimurine antibodies (HAMA): Treatment may result in the development of HAMA; however, limited evidence suggesting the use of muromonab-CD3 or other murine products is not precluded. Lymphoproliferative disorders: The incidence of lymphoproliferative disorders may be increased by immunosuppressive therapy. Opportunistic infections: The incidence opportunistic infections may be increased by immunosuppressive therapy.
Other warnings/precautions: Appropriate use: To be used as a component of immunosuppressive regimen which includes cyclosporine and corticosteroids. Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of a physician experienced in immunosuppression therapy.
DRUG INTERACTIONS
Abciximab: May enhance the potential for allergic or hypersensitivity reactions to Monoclonal Antibodies. Also may cause thrombocytopenia or diminished therapeutic effects. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemic Agents. Risk C: Monitor therapy
Hypoglycemic Agents: May enhance the adverse/toxic effect of other Hypoglycemic Agents. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Vaccinial infections may develop. Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Echinacea may diminish the therapeutic effect of basiliximab. Avoid hypoglycemic herbs, including alfalfa, bilberry, bitter melon, burdock, celery, damiana, fenugreek, garcinia, garlic, ginger, ginseng, gymnema, marshmallow, and stinging nettle (may enhance the hypoglycemic effect of basiliximab).
PREGNANCY RISK FACTOR — B (show table) (manufacturer)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. IL-2 receptors play an important role in the development of the immune system. Use in pregnant women only when benefit exceeds potential risk to the fetus. Women of childbearing potential should use effective contraceptive measures before beginning treatment and for 4 months after completion of therapy with this agent.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — It is not known whether basiliximab is excreted in human milk. Because many immunoglobulins are secreted in milk and the potential for serious adverse reactions exists, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
MONITORING PARAMETERS — Signs and symptoms of acute rejection
CANADIAN BRAND NAMES — Simulect®
INTERNATIONAL BRAND NAMES — Simulect (AR, AT, AU, BE, BG, BR, CH, CL, CN, CO, CZ, DE, DK, EC, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, KP, MX, MY, NL, NO, PE, PH, PK, PL, PT, PY, RU, SE, SG, TH, TR, TW, UY, VE)
MECHANISM OF ACTION — Chimeric (murine/human) monoclonal antibody which blocks the alpha-chain of the interleukin-2 (IL-2) receptor complex; this receptor is expressed on activated T lymphocytes and is a critical pathway for activating cell-mediated allograft rejection
PHARMACODYNAMICS / KINETICS
Duration: Mean: 36 days (determined by IL-2R alpha saturation)
Distribution: Mean: Vd: Children 1-11 years: 4.8 +/- 2.1 L; Adolescents 12-16 years: 7.8 +/- 5.1 L; Adults: 8.6 +/- 4.1 L
Half-life elimination: Children 1-11 years: 9.5 days; Adolescents 12-16 years: 9.1 days; Adults: Mean: 7.2 days
Excretion: Clearance: Children 1-11 years: 17 mL/hour; Adolescents 12-16 years: 31 mL/hour; Adults: Mean: 41 mL/hour
Basiliximab
U.S. BRAND NAMES — Simulect®
PHARMACOLOGIC CATEGORY
Monoclonal Antibody
DOSING: ADULTS — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
Renal transplantation: I.V.: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation. The second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss).
DOSING: PEDIATRIC — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
(For additional information see "Basiliximab: Pediatric drug information")
Renal transplantation: I.V.:
Children <35 kg: 10 mg within 2 hours prior to transplant surgery, followed by a second 10 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Children ≥ 35 kg: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No specific dosing adjustment is recommended.
DOSING: HEPATIC IMPAIRMENT — No specific dosing adjustment is recommended.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For intravenous administration only. Infuse as a bolus or I.V. infusion over 20-30 minutes. (Bolus dosing is associated with nausea, vomiting, and local pain at the injection site.)
USE — Prophylaxis of acute organ rejection in renal transplantation
ADVERSE REACTIONS SIGNIFICANT — Administration of basiliximab did not appear to increase the incidence or severity of adverse effects in clinical trials. Adverse events were reported in 96% of both the placebo and basiliximab groups.
>10%:
Cardiovascular: Hypertension, peripheral edema
Central nervous system: Fever, headache, insomnia, pain
Dermatologic: Acne, wound complications
Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyper-/hypokalemia, hyperuricemia, hypophosphatemia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting
Genitourinary: Urinary tract infection
Hematologic: Anemia
Neuromuscular & skeletal: Tremor
Respiratory: Dyspnea, infection (upper respiratory)
Miscellaneous: Viral infection
3% to 10%:
Cardiovascular: Abnormal heart sounds, angina pectoris, arrhythmia, atrial fibrillation, cardiac failure, chest pain, generalized edema, hypotension, tachycardia
Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise, neuropathy, rigors
Dermatologic: Cyst, hypertrichosis, pruritus, rash, skin disorder, skin ulceration
Endocrine & metabolic: Acidosis, dehydration, diabetes mellitus, fluid overload, hyper-/hypocalcemia, hyperlipidemia, hypertriglyceridemia, hypoglycemia, hypomagnesemia, hyponatremia
Gastrointestinal: Abdomen enlarged, esophagitis, flatulence, gastroenteritis, GI hemorrhage, gingival hyperplasia, melena, moniliasis, stomatitis (including ulcerative), weight gain
Genitourinary: Albuminuria, bladder disorder, dysuria, genital edema, hematuria, impotence, oliguria, renal function abnormal, renal tubular necrosis, ureteral disorder, urinary frequency, urinary retention
Hematologic: Hematoma, hemorrhage, leukopenia, polycythemia, purpura, thrombocytopenia, thrombosis
Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, cramps, fracture, hernia, leg pain, myalgia, paresthesia, weakness
Ocular: Abnormal vision, cataract, conjunctivitis
Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, sinusitis, rhinitis
Miscellaneous: Accidental trauma, facial edema, glucocorticoids increased, herpes infection, sepsis
Postmarketing and/or case reports: Capillary leak syndrome, cytokine release syndrome; severe hypersensitivity reactions, including anaphylaxis, have been reported (symptoms may include hypotension, tachycardia, cardiac failure, dyspnea, bronchospasm, pulmonary edema, urticaria, rash, pruritus, sneezing, and respiratory failure)
CONTRAINDICATIONS — Hypersensitivity to basiliximab, murine proteins, or any component of the formulation
WARNINGS / PRECAUTIONS
Boxed warnings: Experienced physician: See "Other warnings/precautions" below.
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Severe hypersensitivity reactions, occurring within 24 hours, have been reported. Reactions, including anaphylaxis, have occurred both with the initial exposure and/or following re-exposure after several months; use caution during re-exposure to a subsequent course of therapy in a patient who has previously received basiliximab. Discontinue the drug permanently if a reaction occurs. Medications for the treatment of hypersensitivity reactions should be available for immediate use. Human antimurine antibodies (HAMA): Treatment may result in the development of HAMA; however, limited evidence suggesting the use of muromonab-CD3 or other murine products is not precluded. Lymphoproliferative disorders: The incidence of lymphoproliferative disorders may be increased by immunosuppressive therapy. Opportunistic infections: The incidence opportunistic infections may be increased by immunosuppressive therapy.
Other warnings/precautions: Appropriate use: To be used as a component of immunosuppressive regimen which includes cyclosporine and corticosteroids. Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of a physician experienced in immunosuppression therapy.
DRUG INTERACTIONS
Abciximab: May enhance the potential for allergic or hypersensitivity reactions to Monoclonal Antibodies. Also may cause thrombocytopenia or diminished therapeutic effects. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemic Agents. Risk C: Monitor therapy
Hypoglycemic Agents: May enhance the adverse/toxic effect of other Hypoglycemic Agents. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Vaccinial infections may develop. Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Echinacea may diminish the therapeutic effect of basiliximab. Avoid hypoglycemic herbs, including alfalfa, bilberry, bitter melon, burdock, celery, damiana, fenugreek, garcinia, garlic, ginger, ginseng, gymnema, marshmallow, and stinging nettle (may enhance the hypoglycemic effect of basiliximab).
PREGNANCY RISK FACTOR — B (show table) (manufacturer)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. IL-2 receptors play an important role in the development of the immune system. Use in pregnant women only when benefit exceeds potential risk to the fetus. Women of childbearing potential should use effective contraceptive measures before beginning treatment and for 4 months after completion of therapy with this agent.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — It is not known whether basiliximab is excreted in human milk. Because many immunoglobulins are secreted in milk and the potential for serious adverse reactions exists, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
MONITORING PARAMETERS — Signs and symptoms of acute rejection
CANADIAN BRAND NAMES — Simulect®
INTERNATIONAL BRAND NAMES — Simulect (AR, AT, AU, BE, BG, BR, CH, CL, CN, CO, CZ, DE, DK, EC, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, KP, MX, MY, NL, NO, PE, PH, PK, PL, PT, PY, RU, SE, SG, TH, TR, TW, UY, VE)
MECHANISM OF ACTION — Chimeric (murine/human) monoclonal antibody which blocks the alpha-chain of the interleukin-2 (IL-2) receptor complex; this receptor is expressed on activated T lymphocytes and is a critical pathway for activating cell-mediated allograft rejection
PHARMACODYNAMICS / KINETICS
Duration: Mean: 36 days (determined by IL-2R alpha saturation)
Distribution: Mean: Vd: Children 1-11 years: 4.8 +/- 2.1 L; Adolescents 12-16 years: 7.8 +/- 5.1 L; Adults: 8.6 +/- 4.1 L
Half-life elimination: Children 1-11 years: 9.5 days; Adolescents 12-16 years: 9.1 days; Adults: Mean: 7.2 days
Excretion: Clearance: Children 1-11 years: 17 mL/hour; Adolescents 12-16 years: 31 mL/hour; Adults: Mean: 41 mL/hour
PHARMACOLOGIC CATEGORY
Monoclonal Antibody
DOSING: ADULTS — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
Renal transplantation: I.V.: 20 mg within 2 hours prior to transplant surgery, followed by a second 20 mg dose 4 days after transplantation. The second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss).
DOSING: PEDIATRIC — Note: Patients previously administered basiliximab should only be re-exposed to a subsequent course of therapy with extreme caution.
(For additional information see "Basiliximab: Pediatric drug information")
Renal transplantation: I.V.:
Children <35 kg: 10 mg within 2 hours prior to transplant surgery, followed by a second 10 mg dose 4 days after transplantation; the second dose should be withheld if complications occur (including severe hypersensitivity reactions or graft loss)
Children ≥ 35 kg: Refer to adult dosing
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No specific dosing adjustment is recommended.
DOSING: HEPATIC IMPAIRMENT — No specific dosing adjustment is recommended.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution [preservative free]:
Simulect®: 10 mg, 20 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For intravenous administration only. Infuse as a bolus or I.V. infusion over 20-30 minutes. (Bolus dosing is associated with nausea, vomiting, and local pain at the injection site.)
USE — Prophylaxis of acute organ rejection in renal transplantation
ADVERSE REACTIONS SIGNIFICANT — Administration of basiliximab did not appear to increase the incidence or severity of adverse effects in clinical trials. Adverse events were reported in 96% of both the placebo and basiliximab groups.
>10%:
Cardiovascular: Hypertension, peripheral edema
Central nervous system: Fever, headache, insomnia, pain
Dermatologic: Acne, wound complications
Endocrine & metabolic: Hypercholesterolemia, hyperglycemia, hyper-/hypokalemia, hyperuricemia, hypophosphatemia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting
Genitourinary: Urinary tract infection
Hematologic: Anemia
Neuromuscular & skeletal: Tremor
Respiratory: Dyspnea, infection (upper respiratory)
Miscellaneous: Viral infection
3% to 10%:
Cardiovascular: Abnormal heart sounds, angina pectoris, arrhythmia, atrial fibrillation, cardiac failure, chest pain, generalized edema, hypotension, tachycardia
Central nervous system: Agitation, anxiety, depression, dizziness, fatigue, hypoesthesia, malaise, neuropathy, rigors
Dermatologic: Cyst, hypertrichosis, pruritus, rash, skin disorder, skin ulceration
Endocrine & metabolic: Acidosis, dehydration, diabetes mellitus, fluid overload, hyper-/hypocalcemia, hyperlipidemia, hypertriglyceridemia, hypoglycemia, hypomagnesemia, hyponatremia
Gastrointestinal: Abdomen enlarged, esophagitis, flatulence, gastroenteritis, GI hemorrhage, gingival hyperplasia, melena, moniliasis, stomatitis (including ulcerative), weight gain
Genitourinary: Albuminuria, bladder disorder, dysuria, genital edema, hematuria, impotence, oliguria, renal function abnormal, renal tubular necrosis, ureteral disorder, urinary frequency, urinary retention
Hematologic: Hematoma, hemorrhage, leukopenia, polycythemia, purpura, thrombocytopenia, thrombosis
Neuromuscular & skeletal: Arthralgia, arthropathy, back pain, cramps, fracture, hernia, leg pain, myalgia, paresthesia, weakness
Ocular: Abnormal vision, cataract, conjunctivitis
Respiratory: Bronchitis, bronchospasm, cough, pharyngitis, pneumonia, pulmonary edema, sinusitis, rhinitis
Miscellaneous: Accidental trauma, facial edema, glucocorticoids increased, herpes infection, sepsis
Postmarketing and/or case reports: Capillary leak syndrome, cytokine release syndrome; severe hypersensitivity reactions, including anaphylaxis, have been reported (symptoms may include hypotension, tachycardia, cardiac failure, dyspnea, bronchospasm, pulmonary edema, urticaria, rash, pruritus, sneezing, and respiratory failure)
CONTRAINDICATIONS — Hypersensitivity to basiliximab, murine proteins, or any component of the formulation
WARNINGS / PRECAUTIONS
Boxed warnings: Experienced physician: See "Other warnings/precautions" below.
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Severe hypersensitivity reactions, occurring within 24 hours, have been reported. Reactions, including anaphylaxis, have occurred both with the initial exposure and/or following re-exposure after several months; use caution during re-exposure to a subsequent course of therapy in a patient who has previously received basiliximab. Discontinue the drug permanently if a reaction occurs. Medications for the treatment of hypersensitivity reactions should be available for immediate use. Human antimurine antibodies (HAMA): Treatment may result in the development of HAMA; however, limited evidence suggesting the use of muromonab-CD3 or other murine products is not precluded. Lymphoproliferative disorders: The incidence of lymphoproliferative disorders may be increased by immunosuppressive therapy. Opportunistic infections: The incidence opportunistic infections may be increased by immunosuppressive therapy.
Other warnings/precautions: Appropriate use: To be used as a component of immunosuppressive regimen which includes cyclosporine and corticosteroids. Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of a physician experienced in immunosuppression therapy.
DRUG INTERACTIONS
Abciximab: May enhance the potential for allergic or hypersensitivity reactions to Monoclonal Antibodies. Also may cause thrombocytopenia or diminished therapeutic effects. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemic Agents. Risk C: Monitor therapy
Hypoglycemic Agents: May enhance the adverse/toxic effect of other Hypoglycemic Agents. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Vaccinial infections may develop. Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Echinacea may diminish the therapeutic effect of basiliximab. Avoid hypoglycemic herbs, including alfalfa, bilberry, bitter melon, burdock, celery, damiana, fenugreek, garcinia, garlic, ginger, ginseng, gymnema, marshmallow, and stinging nettle (may enhance the hypoglycemic effect of basiliximab).
PREGNANCY RISK FACTOR — B (show table) (manufacturer)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. IL-2 receptors play an important role in the development of the immune system. Use in pregnant women only when benefit exceeds potential risk to the fetus. Women of childbearing potential should use effective contraceptive measures before beginning treatment and for 4 months after completion of therapy with this agent.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — It is not known whether basiliximab is excreted in human milk. Because many immunoglobulins are secreted in milk and the potential for serious adverse reactions exists, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
MONITORING PARAMETERS — Signs and symptoms of acute rejection
CANADIAN BRAND NAMES — Simulect®
INTERNATIONAL BRAND NAMES — Simulect (AR, AT, AU, BE, BG, BR, CH, CL, CN, CO, CZ, DE, DK, EC, ES, FI, FR, GB, GR, HK, HN, IE, IL, IT, KP, MX, MY, NL, NO, PE, PH, PK, PL, PT, PY, RU, SE, SG, TH, TR, TW, UY, VE)
MECHANISM OF ACTION — Chimeric (murine/human) monoclonal antibody which blocks the alpha-chain of the interleukin-2 (IL-2) receptor complex; this receptor is expressed on activated T lymphocytes and is a critical pathway for activating cell-mediated allograft rejection
PHARMACODYNAMICS / KINETICS
Duration: Mean: 36 days (determined by IL-2R alpha saturation)
Distribution: Mean: Vd: Children 1-11 years: 4.8 +/- 2.1 L; Adolescents 12-16 years: 7.8 +/- 5.1 L; Adults: 8.6 +/- 4.1 L
Half-life elimination: Children 1-11 years: 9.5 days; Adolescents 12-16 years: 9.1 days; Adults: Mean: 7.2 days
Excretion: Clearance: Children 1-11 years: 17 mL/hour; Adolescents 12-16 years: 31 mL/hour; Adults: Mean: 41 mL/hour
Barium
U.S. BRAND NAMES — Anatrast; Bar-Test; Baricon™ ; Baro-Cat®; Barobag®; Barosperse®; CheeTah®; E-Z-Cat®; E-Z-Cat® Dry; E-Z-Disk™ ; Enhancer; Entero Vu™ ; Entrobar®; EntroEase®; Esopho-Cat®; HD 200® Plus; Intropaste; Liqui-Coat HD®; Liquid Barosperse®; Medebar® Plus; Prepcat; Readi-Cat®; Readi-Cat® 2; Tomocat®; Tomocat® 1000; Tonojug; Tonopaque; Varibar® Honey; Varibar® Nectar; Varibar® Pudding; Varibar® Thin Honey; Varibar® Thin Liquid; VoLumen™
PHARMACOLOGIC CATEGORY
Radiopaque Agents
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, oral, as sulfate:
Esopho-Cat®: 3% w/w (30 g) [contains sodium benzoate; vanilla flavor]
Paste, oral, as sulfate:
Varibar® Pudding: 40% w/v (230 mL) [target viscosity 5000 CPS; contains sodium benzoate; vanilla flavor]
Powder for suspension, oral, as sulfate:
Baricon™ : 98% w/w (340 g) [lemon-vanilla flavor]
Enhancer: 98% w/w (312 g) [lemon-vanilla flavor]
E-Z-Cat® Dry: 2% w/w (23 g) [provides 450 mL 2% w/w suspension after mixing; orange vanilla flavor]
HD 200® Plus: 98% w/w (312 g) [strawberry flavor]
Tonopaque: 95% w/w (180 g) [cherry flavor]
Varibar® Thin Liquid: 40% w/v (148 g) [provides 40% w/v suspension after mixing; target viscosity 4 CPS; apple flavor]
Powder for suspension, oral/rectal, as sulfate:
Barosperse®: 95% w/w (225 g, 900 g) [vanilla flavor]
Tonojug: 95% w/w (1200 g) [cherry flavor]
Powder for suspension, rectal, as sulfate:
Barobag®: 97% w/w (340 g, 454 g) [packaged as an enema kit]
Suspension, oral, as sulfate:
Entero Vu™ : 24% w/v (600 mL) [contains sodium benzoate; blueberry flavor]
EntroEase®: 13% w/v (600 mL) [contains sodium benzoate; marshmallow flavor]
E-Z-Cat®: 4.9% w/v (255 mL) [orange flavor]
Liqui-Coat HD®: 210% w/v (150 mL) [contains sodium benzoate; vanilla-raspberry flavor]
Readi-Cat® 2: 2.1% w/v ( 250 mL) [contains benzoic acid and sodium benzoate; banana smoothie flavor]; (450 mL) [contains benzoic acid and sodium benzoate; apple smoothie, banana smoothie, and berry smoothie flavors]
Varibar® Honey: 40% w/v (250 mL) [target viscosity 3000 CPS; contains sodium benzoate; apple flavor]
Varibar® Nectar: 40% w/v (240 mL) [target viscosity 300 CPS; contains sodium benzoate; apple flavor]
Varibar® Thin Honey: 40% w/v (250 mL) [target viscosity 1500 CPS; contains sodium benzoate; apple flavor]
VoLumen™ : 0.1% w/v (450 mL) [contains benzoic acid, sodium benzoate; blueberry flavor]
Suspension, oral/rectal, as sulfate:
Baro-Cat®: 1.5% w/v (300 mL, 900 mL) [banana-pineapple flavor]
CheeTah®: 2.2% w/w (450 mL, 900 mL) [contains sodium benzoate; butterscotch vanilla flavor]
Liquid Barosperse®: 60% w/v (355 mL) [vanilla flavor]
Prepcat: 1.5% w/v (450 mL) [strawberry flavor]
Readi-Cat®: 1.3% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor; also supplied as a Cat-Pak with enema tubing]
Readi-Cat® 2: 2.1% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor]
Tomocat®: 5% w/v (145 mL) [concentrate to make a 1.5% solution; strawberry flavor]
Tomocat® 1000: 5% w/v (225 mL) [concentrate; strawberry flavor]
Suspension paste, rectal:
Anatrast: 100% w/v (500 g) [suspension paste; packaged with enema tips]
Intropaste: 70% w/v (454 g) [raspberry flavor]
Suspension, rectal, as sulfate:
Entrobar®: 50% w/v (500 mL) [packaged in administration kit]
Medebar® Plus: 100% w/v (1900 mL)
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
DOSAGE FORMS: CONCISE
Cream, oral:
Esopho-Cat®: 3% w/w
Paste, oral:
Varibar® Pudding: 40% w/v
Powder for suspension, oral:
Baricon™ , Enhancer, HD 200® Plus: 98% w/w
E-Z-Cat® Dry: 2% w/w
Tonopaque: 95% w/w
Varibar® Thin Liquid: 40% w/v
Powder for suspension, oral/rectal:
Barosperse®, Tonojug: 95% w/w
Powder for suspension, rectal:
Barobag®: 97% w/w
Suspension, oral:
Entero Vu™ : 24% w/v
EntroEase®: 13% w/v
E-Z-Cat®: 4.9% w/v
Liqui-Coat HD®: 210% w/v
Readi-Cat® 2: 2.1% w/v
Varibar® Honey, Varibar® Nectar, Varibar® Thin Honey: 40% w/v
VoLumen™ : 0.1% w/v
Suspension, oral/rectal:
Baro-Cat®, Prepcat: 1.5% w/v
CheeTah®: 2.2% w/w
Liquid Barosperse®: 60% w/v
Readi-Cat®: 1.3% w/v
Readi-Cat® 2: 2.1% w/v
Tomocat®, Tomocat® 1000: 5% w/v
Suspension, paste:
Anatrast: 100% w/v
Intropaste: 70% w/v
Suspension, rectal:
Entrobar®: 50% w/v
Medebar® Plus: 100% w/v
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Diagnostic aid for computed tomography or x-ray examinations of the GI tract
CONTRAINDICATIONS — Hypersensitivity to barium or any component of the formulation; known or suspected obstruction of the colon, known or suspected GI tract perforation, suspected tracheoesophageal fistula, obstructing lesions of small intestine, pyloric stenosis
Specific agents may also be contraindicated with inflammation or neoplastic lesions of the rectum, recent rectal biopsy; use in infants with swallowing disorders; newborns with complete duodenal or jejunal obstruction with suspected distal small bowel or colon obstruction; very small preterm infants and young babies requiring small volumes of contrast media; infants and young children with possible leakage from GI tract (eg, necrotizing enterocolitis, unexplained pneumoperitoneum, gasless abdomen, bowel or esophageal perforation, postoperative anastomosea)
PREGNANCY IMPLICATIONS — Safety and efficacy for use during pregnancy have not been established. In general, elective radiography of the abdomen is avoided during pregnancy unless essential for diagnosis.
BREAST-FEEDING CONSIDERATIONS — Barium sulfate is not systemically absorbed.
INTERNATIONAL BRAND NAMES — Barium Sulfuricum (PL); Falibaryt (PL); Micropaque (PL); Microtrast (PL); Prontobario (PL)
PHARMACOLOGIC CATEGORY
Radiopaque Agents
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, oral, as sulfate:
Esopho-Cat®: 3% w/w (30 g) [contains sodium benzoate; vanilla flavor]
Paste, oral, as sulfate:
Varibar® Pudding: 40% w/v (230 mL) [target viscosity 5000 CPS; contains sodium benzoate; vanilla flavor]
Powder for suspension, oral, as sulfate:
Baricon™ : 98% w/w (340 g) [lemon-vanilla flavor]
Enhancer: 98% w/w (312 g) [lemon-vanilla flavor]
E-Z-Cat® Dry: 2% w/w (23 g) [provides 450 mL 2% w/w suspension after mixing; orange vanilla flavor]
HD 200® Plus: 98% w/w (312 g) [strawberry flavor]
Tonopaque: 95% w/w (180 g) [cherry flavor]
Varibar® Thin Liquid: 40% w/v (148 g) [provides 40% w/v suspension after mixing; target viscosity 4 CPS; apple flavor]
Powder for suspension, oral/rectal, as sulfate:
Barosperse®: 95% w/w (225 g, 900 g) [vanilla flavor]
Tonojug: 95% w/w (1200 g) [cherry flavor]
Powder for suspension, rectal, as sulfate:
Barobag®: 97% w/w (340 g, 454 g) [packaged as an enema kit]
Suspension, oral, as sulfate:
Entero Vu™ : 24% w/v (600 mL) [contains sodium benzoate; blueberry flavor]
EntroEase®: 13% w/v (600 mL) [contains sodium benzoate; marshmallow flavor]
E-Z-Cat®: 4.9% w/v (255 mL) [orange flavor]
Liqui-Coat HD®: 210% w/v (150 mL) [contains sodium benzoate; vanilla-raspberry flavor]
Readi-Cat® 2: 2.1% w/v ( 250 mL) [contains benzoic acid and sodium benzoate; banana smoothie flavor]; (450 mL) [contains benzoic acid and sodium benzoate; apple smoothie, banana smoothie, and berry smoothie flavors]
Varibar® Honey: 40% w/v (250 mL) [target viscosity 3000 CPS; contains sodium benzoate; apple flavor]
Varibar® Nectar: 40% w/v (240 mL) [target viscosity 300 CPS; contains sodium benzoate; apple flavor]
Varibar® Thin Honey: 40% w/v (250 mL) [target viscosity 1500 CPS; contains sodium benzoate; apple flavor]
VoLumen™ : 0.1% w/v (450 mL) [contains benzoic acid, sodium benzoate; blueberry flavor]
Suspension, oral/rectal, as sulfate:
Baro-Cat®: 1.5% w/v (300 mL, 900 mL) [banana-pineapple flavor]
CheeTah®: 2.2% w/w (450 mL, 900 mL) [contains sodium benzoate; butterscotch vanilla flavor]
Liquid Barosperse®: 60% w/v (355 mL) [vanilla flavor]
Prepcat: 1.5% w/v (450 mL) [strawberry flavor]
Readi-Cat®: 1.3% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor; also supplied as a Cat-Pak with enema tubing]
Readi-Cat® 2: 2.1% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor]
Tomocat®: 5% w/v (145 mL) [concentrate to make a 1.5% solution; strawberry flavor]
Tomocat® 1000: 5% w/v (225 mL) [concentrate; strawberry flavor]
Suspension paste, rectal:
Anatrast: 100% w/v (500 g) [suspension paste; packaged with enema tips]
Intropaste: 70% w/v (454 g) [raspberry flavor]
Suspension, rectal, as sulfate:
Entrobar®: 50% w/v (500 mL) [packaged in administration kit]
Medebar® Plus: 100% w/v (1900 mL)
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
DOSAGE FORMS: CONCISE
Cream, oral:
Esopho-Cat®: 3% w/w
Paste, oral:
Varibar® Pudding: 40% w/v
Powder for suspension, oral:
Baricon™ , Enhancer, HD 200® Plus: 98% w/w
E-Z-Cat® Dry: 2% w/w
Tonopaque: 95% w/w
Varibar® Thin Liquid: 40% w/v
Powder for suspension, oral/rectal:
Barosperse®, Tonojug: 95% w/w
Powder for suspension, rectal:
Barobag®: 97% w/w
Suspension, oral:
Entero Vu™ : 24% w/v
EntroEase®: 13% w/v
E-Z-Cat®: 4.9% w/v
Liqui-Coat HD®: 210% w/v
Readi-Cat® 2: 2.1% w/v
Varibar® Honey, Varibar® Nectar, Varibar® Thin Honey: 40% w/v
VoLumen™ : 0.1% w/v
Suspension, oral/rectal:
Baro-Cat®, Prepcat: 1.5% w/v
CheeTah®: 2.2% w/w
Liquid Barosperse®: 60% w/v
Readi-Cat®: 1.3% w/v
Readi-Cat® 2: 2.1% w/v
Tomocat®, Tomocat® 1000: 5% w/v
Suspension, paste:
Anatrast: 100% w/v
Intropaste: 70% w/v
Suspension, rectal:
Entrobar®: 50% w/v
Medebar® Plus: 100% w/v
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Diagnostic aid for computed tomography or x-ray examinations of the GI tract
CONTRAINDICATIONS — Hypersensitivity to barium or any component of the formulation; known or suspected obstruction of the colon, known or suspected GI tract perforation, suspected tracheoesophageal fistula, obstructing lesions of small intestine, pyloric stenosis
Specific agents may also be contraindicated with inflammation or neoplastic lesions of the rectum, recent rectal biopsy; use in infants with swallowing disorders; newborns with complete duodenal or jejunal obstruction with suspected distal small bowel or colon obstruction; very small preterm infants and young babies requiring small volumes of contrast media; infants and young children with possible leakage from GI tract (eg, necrotizing enterocolitis, unexplained pneumoperitoneum, gasless abdomen, bowel or esophageal perforation, postoperative anastomosea)
PREGNANCY IMPLICATIONS — Safety and efficacy for use during pregnancy have not been established. In general, elective radiography of the abdomen is avoided during pregnancy unless essential for diagnosis.
BREAST-FEEDING CONSIDERATIONS — Barium sulfate is not systemically absorbed.
INTERNATIONAL BRAND NAMES — Barium Sulfuricum (PL); Falibaryt (PL); Micropaque (PL); Microtrast (PL); Prontobario (PL)
Barium
U.S. BRAND NAMES — Anatrast; Bar-Test; Baricon™ ; Baro-Cat®; Barobag®; Barosperse®; CheeTah®; E-Z-Cat®; E-Z-Cat® Dry; E-Z-Disk™ ; Enhancer; Entero Vu™ ; Entrobar®; EntroEase®; Esopho-Cat®; HD 200® Plus; Intropaste; Liqui-Coat HD®; Liquid Barosperse®; Medebar® Plus; Prepcat; Readi-Cat®; Readi-Cat® 2; Tomocat®; Tomocat® 1000; Tonojug; Tonopaque; Varibar® Honey; Varibar® Nectar; Varibar® Pudding; Varibar® Thin Honey; Varibar® Thin Liquid; VoLumen™
PHARMACOLOGIC CATEGORY
Radiopaque Agents
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, oral, as sulfate:
Esopho-Cat®: 3% w/w (30 g) [contains sodium benzoate; vanilla flavor]
Paste, oral, as sulfate:
Varibar® Pudding: 40% w/v (230 mL) [target viscosity 5000 CPS; contains sodium benzoate; vanilla flavor]
Powder for suspension, oral, as sulfate:
Baricon™ : 98% w/w (340 g) [lemon-vanilla flavor]
Enhancer: 98% w/w (312 g) [lemon-vanilla flavor]
E-Z-Cat® Dry: 2% w/w (23 g) [provides 450 mL 2% w/w suspension after mixing; orange vanilla flavor]
HD 200® Plus: 98% w/w (312 g) [strawberry flavor]
Tonopaque: 95% w/w (180 g) [cherry flavor]
Varibar® Thin Liquid: 40% w/v (148 g) [provides 40% w/v suspension after mixing; target viscosity 4 CPS; apple flavor]
Powder for suspension, oral/rectal, as sulfate:
Barosperse®: 95% w/w (225 g, 900 g) [vanilla flavor]
Tonojug: 95% w/w (1200 g) [cherry flavor]
Powder for suspension, rectal, as sulfate:
Barobag®: 97% w/w (340 g, 454 g) [packaged as an enema kit]
Suspension, oral, as sulfate:
Entero Vu™ : 24% w/v (600 mL) [contains sodium benzoate; blueberry flavor]
EntroEase®: 13% w/v (600 mL) [contains sodium benzoate; marshmallow flavor]
E-Z-Cat®: 4.9% w/v (255 mL) [orange flavor]
Liqui-Coat HD®: 210% w/v (150 mL) [contains sodium benzoate; vanilla-raspberry flavor]
Readi-Cat® 2: 2.1% w/v ( 250 mL) [contains benzoic acid and sodium benzoate; banana smoothie flavor]; (450 mL) [contains benzoic acid and sodium benzoate; apple smoothie, banana smoothie, and berry smoothie flavors]
Varibar® Honey: 40% w/v (250 mL) [target viscosity 3000 CPS; contains sodium benzoate; apple flavor]
Varibar® Nectar: 40% w/v (240 mL) [target viscosity 300 CPS; contains sodium benzoate; apple flavor]
Varibar® Thin Honey: 40% w/v (250 mL) [target viscosity 1500 CPS; contains sodium benzoate; apple flavor]
VoLumen™ : 0.1% w/v (450 mL) [contains benzoic acid, sodium benzoate; blueberry flavor]
Suspension, oral/rectal, as sulfate:
Baro-Cat®: 1.5% w/v (300 mL, 900 mL) [banana-pineapple flavor]
CheeTah®: 2.2% w/w (450 mL, 900 mL) [contains sodium benzoate; butterscotch vanilla flavor]
Liquid Barosperse®: 60% w/v (355 mL) [vanilla flavor]
Prepcat: 1.5% w/v (450 mL) [strawberry flavor]
Readi-Cat®: 1.3% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor; also supplied as a Cat-Pak with enema tubing]
Readi-Cat® 2: 2.1% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor]
Tomocat®: 5% w/v (145 mL) [concentrate to make a 1.5% solution; strawberry flavor]
Tomocat® 1000: 5% w/v (225 mL) [concentrate; strawberry flavor]
Suspension paste, rectal:
Anatrast: 100% w/v (500 g) [suspension paste; packaged with enema tips]
Intropaste: 70% w/v (454 g) [raspberry flavor]
Suspension, rectal, as sulfate:
Entrobar®: 50% w/v (500 mL) [packaged in administration kit]
Medebar® Plus: 100% w/v (1900 mL)
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
DOSAGE FORMS: CONCISE
Cream, oral:
Esopho-Cat®: 3% w/w
Paste, oral:
Varibar® Pudding: 40% w/v
Powder for suspension, oral:
Baricon™ , Enhancer, HD 200® Plus: 98% w/w
E-Z-Cat® Dry: 2% w/w
Tonopaque: 95% w/w
Varibar® Thin Liquid: 40% w/v
Powder for suspension, oral/rectal:
Barosperse®, Tonojug: 95% w/w
Powder for suspension, rectal:
Barobag®: 97% w/w
Suspension, oral:
Entero Vu™ : 24% w/v
EntroEase®: 13% w/v
E-Z-Cat®: 4.9% w/v
Liqui-Coat HD®: 210% w/v
Readi-Cat® 2: 2.1% w/v
Varibar® Honey, Varibar® Nectar, Varibar® Thin Honey: 40% w/v
VoLumen™ : 0.1% w/v
Suspension, oral/rectal:
Baro-Cat®, Prepcat: 1.5% w/v
CheeTah®: 2.2% w/w
Liquid Barosperse®: 60% w/v
Readi-Cat®: 1.3% w/v
Readi-Cat® 2: 2.1% w/v
Tomocat®, Tomocat® 1000: 5% w/v
Suspension, paste:
Anatrast: 100% w/v
Intropaste: 70% w/v
Suspension, rectal:
Entrobar®: 50% w/v
Medebar® Plus: 100% w/v
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Diagnostic aid for computed tomography or x-ray examinations of the GI tract
CONTRAINDICATIONS — Hypersensitivity to barium or any component of the formulation; known or suspected obstruction of the colon, known or suspected GI tract perforation, suspected tracheoesophageal fistula, obstructing lesions of small intestine, pyloric stenosis
Specific agents may also be contraindicated with inflammation or neoplastic lesions of the rectum, recent rectal biopsy; use in infants with swallowing disorders; newborns with complete duodenal or jejunal obstruction with suspected distal small bowel or colon obstruction; very small preterm infants and young babies requiring small volumes of contrast media; infants and young children with possible leakage from GI tract (eg, necrotizing enterocolitis, unexplained pneumoperitoneum, gasless abdomen, bowel or esophageal perforation, postoperative anastomosea)
PREGNANCY IMPLICATIONS — Safety and efficacy for use during pregnancy have not been established. In general, elective radiography of the abdomen is avoided during pregnancy unless essential for diagnosis.
BREAST-FEEDING CONSIDERATIONS — Barium sulfate is not systemically absorbed.
INTERNATIONAL BRAND NAMES — Barium Sulfuricum (PL); Falibaryt (PL); Micropaque (PL); Microtrast (PL); Prontobario (PL)
PHARMACOLOGIC CATEGORY
Radiopaque Agents
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Cream, oral, as sulfate:
Esopho-Cat®: 3% w/w (30 g) [contains sodium benzoate; vanilla flavor]
Paste, oral, as sulfate:
Varibar® Pudding: 40% w/v (230 mL) [target viscosity 5000 CPS; contains sodium benzoate; vanilla flavor]
Powder for suspension, oral, as sulfate:
Baricon™ : 98% w/w (340 g) [lemon-vanilla flavor]
Enhancer: 98% w/w (312 g) [lemon-vanilla flavor]
E-Z-Cat® Dry: 2% w/w (23 g) [provides 450 mL 2% w/w suspension after mixing; orange vanilla flavor]
HD 200® Plus: 98% w/w (312 g) [strawberry flavor]
Tonopaque: 95% w/w (180 g) [cherry flavor]
Varibar® Thin Liquid: 40% w/v (148 g) [provides 40% w/v suspension after mixing; target viscosity 4 CPS; apple flavor]
Powder for suspension, oral/rectal, as sulfate:
Barosperse®: 95% w/w (225 g, 900 g) [vanilla flavor]
Tonojug: 95% w/w (1200 g) [cherry flavor]
Powder for suspension, rectal, as sulfate:
Barobag®: 97% w/w (340 g, 454 g) [packaged as an enema kit]
Suspension, oral, as sulfate:
Entero Vu™ : 24% w/v (600 mL) [contains sodium benzoate; blueberry flavor]
EntroEase®: 13% w/v (600 mL) [contains sodium benzoate; marshmallow flavor]
E-Z-Cat®: 4.9% w/v (255 mL) [orange flavor]
Liqui-Coat HD®: 210% w/v (150 mL) [contains sodium benzoate; vanilla-raspberry flavor]
Readi-Cat® 2: 2.1% w/v ( 250 mL) [contains benzoic acid and sodium benzoate; banana smoothie flavor]; (450 mL) [contains benzoic acid and sodium benzoate; apple smoothie, banana smoothie, and berry smoothie flavors]
Varibar® Honey: 40% w/v (250 mL) [target viscosity 3000 CPS; contains sodium benzoate; apple flavor]
Varibar® Nectar: 40% w/v (240 mL) [target viscosity 300 CPS; contains sodium benzoate; apple flavor]
Varibar® Thin Honey: 40% w/v (250 mL) [target viscosity 1500 CPS; contains sodium benzoate; apple flavor]
VoLumen™ : 0.1% w/v (450 mL) [contains benzoic acid, sodium benzoate; blueberry flavor]
Suspension, oral/rectal, as sulfate:
Baro-Cat®: 1.5% w/v (300 mL, 900 mL) [banana-pineapple flavor]
CheeTah®: 2.2% w/w (450 mL, 900 mL) [contains sodium benzoate; butterscotch vanilla flavor]
Liquid Barosperse®: 60% w/v (355 mL) [vanilla flavor]
Prepcat: 1.5% w/v (450 mL) [strawberry flavor]
Readi-Cat®: 1.3% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor; also supplied as a Cat-Pak with enema tubing]
Readi-Cat® 2: 2.1% w/v (450 mL, 900 mL, 1900 mL) [contains sodium benzoate; orange vanilla flavor]
Tomocat®: 5% w/v (145 mL) [concentrate to make a 1.5% solution; strawberry flavor]
Tomocat® 1000: 5% w/v (225 mL) [concentrate; strawberry flavor]
Suspension paste, rectal:
Anatrast: 100% w/v (500 g) [suspension paste; packaged with enema tips]
Intropaste: 70% w/v (454 g) [raspberry flavor]
Suspension, rectal, as sulfate:
Entrobar®: 50% w/v (500 mL) [packaged in administration kit]
Medebar® Plus: 100% w/v (1900 mL)
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
DOSAGE FORMS: CONCISE
Cream, oral:
Esopho-Cat®: 3% w/w
Paste, oral:
Varibar® Pudding: 40% w/v
Powder for suspension, oral:
Baricon™ , Enhancer, HD 200® Plus: 98% w/w
E-Z-Cat® Dry: 2% w/w
Tonopaque: 95% w/w
Varibar® Thin Liquid: 40% w/v
Powder for suspension, oral/rectal:
Barosperse®, Tonojug: 95% w/w
Powder for suspension, rectal:
Barobag®: 97% w/w
Suspension, oral:
Entero Vu™ : 24% w/v
EntroEase®: 13% w/v
E-Z-Cat®: 4.9% w/v
Liqui-Coat HD®: 210% w/v
Readi-Cat® 2: 2.1% w/v
Varibar® Honey, Varibar® Nectar, Varibar® Thin Honey: 40% w/v
VoLumen™ : 0.1% w/v
Suspension, oral/rectal:
Baro-Cat®, Prepcat: 1.5% w/v
CheeTah®: 2.2% w/w
Liquid Barosperse®: 60% w/v
Readi-Cat®: 1.3% w/v
Readi-Cat® 2: 2.1% w/v
Tomocat®, Tomocat® 1000: 5% w/v
Suspension, paste:
Anatrast: 100% w/v
Intropaste: 70% w/v
Suspension, rectal:
Entrobar®: 50% w/v
Medebar® Plus: 100% w/v
Tablet, oral, as sulfate:
Bar-Test, E-Z-Disk™ : 648 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Diagnostic aid for computed tomography or x-ray examinations of the GI tract
CONTRAINDICATIONS — Hypersensitivity to barium or any component of the formulation; known or suspected obstruction of the colon, known or suspected GI tract perforation, suspected tracheoesophageal fistula, obstructing lesions of small intestine, pyloric stenosis
Specific agents may also be contraindicated with inflammation or neoplastic lesions of the rectum, recent rectal biopsy; use in infants with swallowing disorders; newborns with complete duodenal or jejunal obstruction with suspected distal small bowel or colon obstruction; very small preterm infants and young babies requiring small volumes of contrast media; infants and young children with possible leakage from GI tract (eg, necrotizing enterocolitis, unexplained pneumoperitoneum, gasless abdomen, bowel or esophageal perforation, postoperative anastomosea)
PREGNANCY IMPLICATIONS — Safety and efficacy for use during pregnancy have not been established. In general, elective radiography of the abdomen is avoided during pregnancy unless essential for diagnosis.
BREAST-FEEDING CONSIDERATIONS — Barium sulfate is not systemically absorbed.
INTERNATIONAL BRAND NAMES — Barium Sulfuricum (PL); Falibaryt (PL); Micropaque (PL); Microtrast (PL); Prontobario (PL)
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