Copyright 1978-2006 Lexi-Comp, Inc. All rights reserved.
(For additional information see "Abatacept: Patient drug information")
U.S. BRAND NAMES — Orencia®
PHARMACOLOGIC CATEGORY Antirheumatic, Disease Modifying
DOSING: ADULTS — Rheumatoid arthritis: I.V.: Dosing is according to body weight. Repeat dose at 2 weeks and 4 weeks after initial dose, and every 4 weeks thereafter: <60>100 kg: 1000 mg
DOSING: ELDERLY — Refer to adult dosing. Due to potential for higher rates of infections and malignancies, use caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]: 250 mg
DOSAGE FORMS: CONCISE Injection, powder for reconstitution [preservative free]: Orencia®: 250 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over 30 minutes. Administer through a 0.2-1.2 micron low protein-binding. filter
COMPATIBILITY — Stable in NS.
USE — Treatment of rheumatoid arthritis not responsive to other disease-modifying antirheumatic drugs (DMARD); may be used as monotherapy or in combination with other DMARDs (not in combination with TNF-blocking agents)
ADVERSE REACTIONS SIGNIFICANT — Note: Percentages not always reported; COPD patients experienced a higher frequency of COPD-related adverse reactions (COPD exacerbation, cough, dyspnea, pneumonia, rhonchi)
>10%: Central nervous system: Headache (18%) Gastrointestinal: Nausea Respiratory: Nasopharyngitis (12%), upper respiratory tract infection Miscellaneous: Infection
1% to 10%: Cardiovascular: Hypertension (7%) Central nervous system: Dizziness (9%) Dermatologic: Rash (4%) Gastrointestinal: Dyspepsia (6%) Genitourinary: Urinary tract infection (6%) Neuromuscular & skeletal: Back pain (7%), limb pain (3%) Respiratory: Cough (8%), bronchitis, pneumonia, rhinitis, sinusitis Miscellaneous: Infusion-related reactions (9%), herpes simplex, influenza
<1% (Limited to important or life-threatening): Anaphylaxis, anaphylactoid reactions, cellulitis, diverticulitis, dyspnea, flushing, hypersensitivity, hypotension, lung cancer, lymphoma, pruritus, pyelonephritis, urticaria, wheezing
CONTRAINDICATIONS — Hypersensitivity to abatacept or any component of the formulation; concurrent use with tumor necrosis factor (TNF) blocking agents (eg, adalimumab, etanercept, infliximab)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: May cause hypersensitivity, anaphylaxis, or anaphylactoid reactions; medication for the treatment of hypersensitivity reactions should be available for immediate use. Infections: Caution should be exercised when considering the use in patients with a history of new/recurrent infections, with conditions that predispose them to infections, or with chronic, latent, or localized infections. Patients who develop a new infection while undergoing treatment should be monitored closely. If a patient develops a serious infection, therapy should be discontinued. Malignancy: Use may affect defenses against malignancies; impact on the development and course of malignancies is not fully defined. As compared to the general population, an increased risk of lymphoma has been noted in clinical trials; however, rheumatoid arthritis has been previously associated with an increased rate of lymphoma.
Disease-related concerns: COPD: Use caution with chronic obstructive pulmonary disease (COPD), higher incidences of adverse effects (COPD exacerbation, cough, rhonchi, dyspnea) have been observed; monitor closely.
Concurrent drug therapy issues: Anakinra: The manufacturer does not recommend concurrent use with anakinra. TNF-blocking agents: Patients receiving therapy in combination with TNF-blocking agents had higher rates of infections (including serious infections) than patients on TNF-blocking agents alone.
Special populations: Pediatrics: Safety and efficacy have not been established in children. Tuberculosis-positive patients: Safety has not been established in tuberculosis-positive patients; screen patients for latent tuberculosis infection prior to initiating therapy.
Other warnings/precautions: Immunizations: Patients should be brought up to date with all immunizations before initiating therapy. Live vaccines should not be given concurrently; there is no data available concerning secondary transmission of live vaccines in patients receiving therapy.
DRUG INTERACTIONS TNF-blocking agents: Concurrent use with abatacept may increase risk of infections; contraindicated.
Vaccines, live: Concomitant use has not be studied; currently recommended not to administer live vaccines during or for 3 months after the completion of abatacept treatment.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Due to the potential risk for development of autoimmune disease in the fetus, use during pregnancy only if clearly needed.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential for adverse reactions and possible effects on the developing immune system, breast-feeding is not recommended.
PRICING — (data from drugstore.com)Injection (reconstituted) (Orencia) 250 mg (1): $498.99
MONITORING PARAMETERS — Signs and symptoms of infection
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Doses up to 50 mg/kg have been tolerated. In the event of an overdose, monitor for signs and symptoms of adverse reactions; treatment should be symptom-directed and supportive.
MECHANISM OF ACTION — Selective costimulation modulator; inhibits T-cell (T-lymphocyte) activation by binding to CD80 and CD86 on antigen presenting cells (APC), thus blocking the required CD28 interaction between APCs and T cells. Activated T lymphocytes are found in the synovium of rheumatoid arthritis patients.
PHARMACODYNAMICS / KINETICS Distribution: Vss: 0.02-0.13 L/kg
Half-life elimination: 8-25 days
PATIENT INFORMATION — This drug can only be administered by infusion. Do not have any vaccinations while using this medication without consulting prescriber first. You will be more prone to infection. Avoid crowds and wash your hands frequently. Report infections (local or in your whole body) to prescriber immediately. You will need an overall health assessment prior to each treatment to ensure that you do not have an active infection. You may experience headache or dizziness (use caution when driving) or nausea (small frequent meals or sucking lozenges may help).
(For additional information see "Abatacept: Patient drug information")
Wednesday, January 16, 2008
Abatacept: Drug information
Copyright 1978-2006 Lexi-Comp, Inc. All rights reserved.
(For additional information see "Abatacept: Patient drug information")
U.S. BRAND NAMES — Orencia®
PHARMACOLOGIC CATEGORY Antirheumatic, Disease Modifying
DOSING: ADULTS — Rheumatoid arthritis: I.V.: Dosing is according to body weight. Repeat dose at 2 weeks and 4 weeks after initial dose, and every 4 weeks thereafter: <60>100 kg: 1000 mg
DOSING: ELDERLY — Refer to adult dosing. Due to potential for higher rates of infections and malignancies, use caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]: 250 mg
DOSAGE FORMS: CONCISE Injection, powder for reconstitution [preservative free]: Orencia®: 250 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over 30 minutes. Administer through a 0.2-1.2 micron low protein-binding. filter
COMPATIBILITY — Stable in NS.
USE — Treatment of rheumatoid arthritis not responsive to other disease-modifying antirheumatic drugs (DMARD); may be used as monotherapy or in combination with other DMARDs (not in combination with TNF-blocking agents)
ADVERSE REACTIONS SIGNIFICANT — Note: Percentages not always reported; COPD patients experienced a higher frequency of COPD-related adverse reactions (COPD exacerbation, cough, dyspnea, pneumonia, rhonchi)
>10%: Central nervous system: Headache (18%) Gastrointestinal: Nausea Respiratory: Nasopharyngitis (12%), upper respiratory tract infection Miscellaneous: Infection
1% to 10%: Cardiovascular: Hypertension (7%) Central nervous system: Dizziness (9%) Dermatologic: Rash (4%) Gastrointestinal: Dyspepsia (6%) Genitourinary: Urinary tract infection (6%) Neuromuscular & skeletal: Back pain (7%), limb pain (3%) Respiratory: Cough (8%), bronchitis, pneumonia, rhinitis, sinusitis Miscellaneous: Infusion-related reactions (9%), herpes simplex, influenza
<1% (Limited to important or life-threatening): Anaphylaxis, anaphylactoid reactions, cellulitis, diverticulitis, dyspnea, flushing, hypersensitivity, hypotension, lung cancer, lymphoma, pruritus, pyelonephritis, urticaria, wheezing
CONTRAINDICATIONS — Hypersensitivity to abatacept or any component of the formulation; concurrent use with tumor necrosis factor (TNF) blocking agents (eg, adalimumab, etanercept, infliximab)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: May cause hypersensitivity, anaphylaxis, or anaphylactoid reactions; medication for the treatment of hypersensitivity reactions should be available for immediate use. Infections: Caution should be exercised when considering the use in patients with a history of new/recurrent infections, with conditions that predispose them to infections, or with chronic, latent, or localized infections. Patients who develop a new infection while undergoing treatment should be monitored closely. If a patient develops a serious infection, therapy should be discontinued. Malignancy: Use may affect defenses against malignancies; impact on the development and course of malignancies is not fully defined. As compared to the general population, an increased risk of lymphoma has been noted in clinical trials; however, rheumatoid arthritis has been previously associated with an increased rate of lymphoma.
Disease-related concerns: COPD: Use caution with chronic obstructive pulmonary disease (COPD), higher incidences of adverse effects (COPD exacerbation, cough, rhonchi, dyspnea) have been observed; monitor closely.
Concurrent drug therapy issues: Anakinra: The manufacturer does not recommend concurrent use with anakinra. TNF-blocking agents: Patients receiving therapy in combination with TNF-blocking agents had higher rates of infections (including serious infections) than patients on TNF-blocking agents alone.
Special populations: Pediatrics: Safety and efficacy have not been established in children. Tuberculosis-positive patients: Safety has not been established in tuberculosis-positive patients; screen patients for latent tuberculosis infection prior to initiating therapy.
Other warnings/precautions: Immunizations: Patients should be brought up to date with all immunizations before initiating therapy. Live vaccines should not be given concurrently; there is no data available concerning secondary transmission of live vaccines in patients receiving therapy.
DRUG INTERACTIONS TNF-blocking agents: Concurrent use with abatacept may increase risk of infections; contraindicated.
Vaccines, live: Concomitant use has not be studied; currently recommended not to administer live vaccines during or for 3 months after the completion of abatacept treatment.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Due to the potential risk for development of autoimmune disease in the fetus, use during pregnancy only if clearly needed.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential for adverse reactions and possible effects on the developing immune system, breast-feeding is not recommended.
PRICING — (data from drugstore.com)Injection (reconstituted) (Orencia) 250 mg (1): $498.99
MONITORING PARAMETERS — Signs and symptoms of infection
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Doses up to 50 mg/kg have been tolerated. In the event of an overdose, monitor for signs and symptoms of adverse reactions; treatment should be symptom-directed and supportive.
MECHANISM OF ACTION — Selective costimulation modulator; inhibits T-cell (T-lymphocyte) activation by binding to CD80 and CD86 on antigen presenting cells (APC), thus blocking the required CD28 interaction between APCs and T cells. Activated T lymphocytes are found in the synovium of rheumatoid arthritis patients.
PHARMACODYNAMICS / KINETICS Distribution: Vss: 0.02-0.13 L/kg
Half-life elimination: 8-25 days
PATIENT INFORMATION — This drug can only be administered by infusion. Do not have any vaccinations while using this medication without consulting prescriber first. You will be more prone to infection. Avoid crowds and wash your hands frequently. Report infections (local or in your whole body) to prescriber immediately. You will need an overall health assessment prior to each treatment to ensure that you do not have an active infection. You may experience headache or dizziness (use caution when driving) or nausea (small frequent meals or sucking lozenges may help).
(For additional information see "Abatacept: Patient drug information")
(For additional information see "Abatacept: Patient drug information")
U.S. BRAND NAMES — Orencia®
PHARMACOLOGIC CATEGORY Antirheumatic, Disease Modifying
DOSING: ADULTS — Rheumatoid arthritis: I.V.: Dosing is according to body weight. Repeat dose at 2 weeks and 4 weeks after initial dose, and every 4 weeks thereafter: <60>100 kg: 1000 mg
DOSING: ELDERLY — Refer to adult dosing. Due to potential for higher rates of infections and malignancies, use caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]: 250 mg
DOSAGE FORMS: CONCISE Injection, powder for reconstitution [preservative free]: Orencia®: 250 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Infuse over 30 minutes. Administer through a 0.2-1.2 micron low protein-binding. filter
COMPATIBILITY — Stable in NS.
USE — Treatment of rheumatoid arthritis not responsive to other disease-modifying antirheumatic drugs (DMARD); may be used as monotherapy or in combination with other DMARDs (not in combination with TNF-blocking agents)
ADVERSE REACTIONS SIGNIFICANT — Note: Percentages not always reported; COPD patients experienced a higher frequency of COPD-related adverse reactions (COPD exacerbation, cough, dyspnea, pneumonia, rhonchi)
>10%: Central nervous system: Headache (18%) Gastrointestinal: Nausea Respiratory: Nasopharyngitis (12%), upper respiratory tract infection Miscellaneous: Infection
1% to 10%: Cardiovascular: Hypertension (7%) Central nervous system: Dizziness (9%) Dermatologic: Rash (4%) Gastrointestinal: Dyspepsia (6%) Genitourinary: Urinary tract infection (6%) Neuromuscular & skeletal: Back pain (7%), limb pain (3%) Respiratory: Cough (8%), bronchitis, pneumonia, rhinitis, sinusitis Miscellaneous: Infusion-related reactions (9%), herpes simplex, influenza
<1% (Limited to important or life-threatening): Anaphylaxis, anaphylactoid reactions, cellulitis, diverticulitis, dyspnea, flushing, hypersensitivity, hypotension, lung cancer, lymphoma, pruritus, pyelonephritis, urticaria, wheezing
CONTRAINDICATIONS — Hypersensitivity to abatacept or any component of the formulation; concurrent use with tumor necrosis factor (TNF) blocking agents (eg, adalimumab, etanercept, infliximab)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Anaphylaxis/hypersensitivity reactions: May cause hypersensitivity, anaphylaxis, or anaphylactoid reactions; medication for the treatment of hypersensitivity reactions should be available for immediate use. Infections: Caution should be exercised when considering the use in patients with a history of new/recurrent infections, with conditions that predispose them to infections, or with chronic, latent, or localized infections. Patients who develop a new infection while undergoing treatment should be monitored closely. If a patient develops a serious infection, therapy should be discontinued. Malignancy: Use may affect defenses against malignancies; impact on the development and course of malignancies is not fully defined. As compared to the general population, an increased risk of lymphoma has been noted in clinical trials; however, rheumatoid arthritis has been previously associated with an increased rate of lymphoma.
Disease-related concerns: COPD: Use caution with chronic obstructive pulmonary disease (COPD), higher incidences of adverse effects (COPD exacerbation, cough, rhonchi, dyspnea) have been observed; monitor closely.
Concurrent drug therapy issues: Anakinra: The manufacturer does not recommend concurrent use with anakinra. TNF-blocking agents: Patients receiving therapy in combination with TNF-blocking agents had higher rates of infections (including serious infections) than patients on TNF-blocking agents alone.
Special populations: Pediatrics: Safety and efficacy have not been established in children. Tuberculosis-positive patients: Safety has not been established in tuberculosis-positive patients; screen patients for latent tuberculosis infection prior to initiating therapy.
Other warnings/precautions: Immunizations: Patients should be brought up to date with all immunizations before initiating therapy. Live vaccines should not be given concurrently; there is no data available concerning secondary transmission of live vaccines in patients receiving therapy.
DRUG INTERACTIONS TNF-blocking agents: Concurrent use with abatacept may increase risk of infections; contraindicated.
Vaccines, live: Concomitant use has not be studied; currently recommended not to administer live vaccines during or for 3 months after the completion of abatacept treatment.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Due to the potential risk for development of autoimmune disease in the fetus, use during pregnancy only if clearly needed.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential for adverse reactions and possible effects on the developing immune system, breast-feeding is not recommended.
PRICING — (data from drugstore.com)Injection (reconstituted) (Orencia) 250 mg (1): $498.99
MONITORING PARAMETERS — Signs and symptoms of infection
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Doses up to 50 mg/kg have been tolerated. In the event of an overdose, monitor for signs and symptoms of adverse reactions; treatment should be symptom-directed and supportive.
MECHANISM OF ACTION — Selective costimulation modulator; inhibits T-cell (T-lymphocyte) activation by binding to CD80 and CD86 on antigen presenting cells (APC), thus blocking the required CD28 interaction between APCs and T cells. Activated T lymphocytes are found in the synovium of rheumatoid arthritis patients.
PHARMACODYNAMICS / KINETICS Distribution: Vss: 0.02-0.13 L/kg
Half-life elimination: 8-25 days
PATIENT INFORMATION — This drug can only be administered by infusion. Do not have any vaccinations while using this medication without consulting prescriber first. You will be more prone to infection. Avoid crowds and wash your hands frequently. Report infections (local or in your whole body) to prescriber immediately. You will need an overall health assessment prior to each treatment to ensure that you do not have an active infection. You may experience headache or dizziness (use caution when driving) or nausea (small frequent meals or sucking lozenges may help).
(For additional information see "Abatacept: Patient drug information")
Abarelix: Drug information
Copyright 1978-2006 Lexi-Comp, Inc. All rights reserved.
U.S. BRAND NAMES — Plenaxis™ [DSC]
PHARMACOLOGIC CATEGORY Gonadotropin Releasing Hormone Antagonist
DOSING: ADULTS — Male prostate cancer: I.M.: 100 mg administered on days 1, 15, 29 (week 4), then every 4 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product.
Injection, powder for reconstitution [preservative free]: 113 mg [provides 100 mg/2 mL depot suspension when reconstituted; packaged with diluent and syringe] [DSC]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer intramuscularly (to the buttock).
USE — Palliative treatment of advanced prostate cancer; treatment is limited to men who are not candidates for LHRH therapy, refuse surgical castration, and have one or more of the following complications due to metastases or local encroachment: 1) risk of neurological compromise, 2) ureteral or bladder outlet obstruction, or 3) severe bone pain (persisting despite narcotic analgesia)
ADVERSE REACTIONS SIGNIFICANT >10%: Cardiovascular: Hot flushes (79%), peripheral edema (15%) Central nervous system: Sleep disturbance (44%), pain (31%), dizziness (12%), headache (12%) Endocrine & metabolic: Breast enlargement (30%), nipple discharge/tenderness (20%) Gastrointestinal: Constipation (15%), diarrhea (11%) Neuromuscular & skeletal: Back pain (17%) Respiratory: Upper respiratory infection (12%)
1% to 10%: Central nervous system: Fatigue (10%) Endocrine & metabolic: Serum triglycerides increased (10%) Gastrointestinal: Nausea (10%) Genitourinary: Dysuria (10%), micturition frequency (10%), urinary retention (10%), urinary tract infection (10%) Hepatic: Transaminases increased (2% to 8%) Miscellaneous: Allergic reactions (urticaria, pruritus, syncope, hypotension); risk increases with prolonged treatment
CONTRAINDICATIONS — Hypersensitivity to abarelix or any component of the formulation
WARNINGS / PRECAUTIONS Box warnings: Allergic reactions: See "Concerns related to adverse effects" below. Diminished efficacy: See "Other warnings/precautions" below. Plenaxis™ Plus Program: See "Other warnings/precautions" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Allergic reactions: [U.S. Boxed Warning]: Has been associated with immediate-onset allergic reactions; may occur with initial dose and risk increases with duration of treatment. Observe for signs/symptoms of allergic reactions (which may include hypotension and/or syncope) for at least 30 minutes following each injection. Decreased bone mineral density: Extended treatment may result in a decrease in bone mineral density. QT prolongation: May cause prolongation of the QT interval; consider risk:benefit in patients with baseline QTc values >450 msec or patients receiving concurrent medications which prolong the QTc interval (class Ia and class III antiarrhythmics).
Other warnings/precautions: Diminished efficacy: [U.S. Boxed Warning]: Efficacy may diminish during prolonged treatment, particularly in patients weighing >225 pounds; monitor serum testosterone levels to identify treatment failures. Monitoring: Monitor transaminase levels and hepatic function during therapy. Plenaxis™ Plus Program: [U.S. Boxed Warning]: May only be prescribed by physicians enrolled in the Plenaxis™ Plus Program.
RESTRICTIONS — Abarelix is not distributed through retail pharmacies. Prior to its discontinuation, prescribing and distribution of abarelix was limited to physicians and hospital pharmacies participating in the Plenaxis™ PLUS program. Additional information may be obtained by calling 1-877-772-3247 or 1-866-753-2947.
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
QTc-prolonging agents: Additive QTc prolongation may occur. Life-threatening ventricular arrhythmias may result. Example drugs include class Ia and class III antiarrhythmics, cisapride, selected quinolones, erythromycin, pimozide, mesoridazine, and thioridazine.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Not indicated for use in women; may cause fetal harm if administered to a pregnant woman.
LACTATION — Excretion in breast milk unknown/not indicated in women
BREAST-FEEDING CONSIDERATIONS — Not indicated for use in women
MONITORING PARAMETERS — Signs/symptoms of allergic reaction (for at least 30 minutes after each injection). Obtain transaminase levels at baseline and periodically during treatment. Serum testosterone (to identify treatment failure) just prior to abarelix administration, beginning on day 29 and every 8 weeks thereafter. PSA and bone mineral density may be monitored as needed.
REFERENCE RANGE — Efficacy may be monitored by suppression of serum testosterone <50 ng/dL
TOXICOLOGY / OVERDOSE COMPREHENSIVE — No experience in overdose. Treatment is symptomatic and supportive.
MECHANISM OF ACTION — Competes with naturally-occurring GnRH for binding on receptors of the pituitary. Suppresses LH and FSH, resulting in decreased testosterone.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 4040 L (+/- 1607)
Metabolism: Hepatic, via peptide hydrolysis
Half-life elimination: 13 days
Time to peak, serum: 3 days (following I.M. administration)
Excretion: Urine (13% as unchanged drug)
U.S. BRAND NAMES — Plenaxis™ [DSC]
PHARMACOLOGIC CATEGORY Gonadotropin Releasing Hormone Antagonist
DOSING: ADULTS — Male prostate cancer: I.M.: 100 mg administered on days 1, 15, 29 (week 4), then every 4 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product.
Injection, powder for reconstitution [preservative free]: 113 mg [provides 100 mg/2 mL depot suspension when reconstituted; packaged with diluent and syringe] [DSC]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer intramuscularly (to the buttock).
USE — Palliative treatment of advanced prostate cancer; treatment is limited to men who are not candidates for LHRH therapy, refuse surgical castration, and have one or more of the following complications due to metastases or local encroachment: 1) risk of neurological compromise, 2) ureteral or bladder outlet obstruction, or 3) severe bone pain (persisting despite narcotic analgesia)
ADVERSE REACTIONS SIGNIFICANT >10%: Cardiovascular: Hot flushes (79%), peripheral edema (15%) Central nervous system: Sleep disturbance (44%), pain (31%), dizziness (12%), headache (12%) Endocrine & metabolic: Breast enlargement (30%), nipple discharge/tenderness (20%) Gastrointestinal: Constipation (15%), diarrhea (11%) Neuromuscular & skeletal: Back pain (17%) Respiratory: Upper respiratory infection (12%)
1% to 10%: Central nervous system: Fatigue (10%) Endocrine & metabolic: Serum triglycerides increased (10%) Gastrointestinal: Nausea (10%) Genitourinary: Dysuria (10%), micturition frequency (10%), urinary retention (10%), urinary tract infection (10%) Hepatic: Transaminases increased (2% to 8%) Miscellaneous: Allergic reactions (urticaria, pruritus, syncope, hypotension); risk increases with prolonged treatment
CONTRAINDICATIONS — Hypersensitivity to abarelix or any component of the formulation
WARNINGS / PRECAUTIONS Box warnings: Allergic reactions: See "Concerns related to adverse effects" below. Diminished efficacy: See "Other warnings/precautions" below. Plenaxis™ Plus Program: See "Other warnings/precautions" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Allergic reactions: [U.S. Boxed Warning]: Has been associated with immediate-onset allergic reactions; may occur with initial dose and risk increases with duration of treatment. Observe for signs/symptoms of allergic reactions (which may include hypotension and/or syncope) for at least 30 minutes following each injection. Decreased bone mineral density: Extended treatment may result in a decrease in bone mineral density. QT prolongation: May cause prolongation of the QT interval; consider risk:benefit in patients with baseline QTc values >450 msec or patients receiving concurrent medications which prolong the QTc interval (class Ia and class III antiarrhythmics).
Other warnings/precautions: Diminished efficacy: [U.S. Boxed Warning]: Efficacy may diminish during prolonged treatment, particularly in patients weighing >225 pounds; monitor serum testosterone levels to identify treatment failures. Monitoring: Monitor transaminase levels and hepatic function during therapy. Plenaxis™ Plus Program: [U.S. Boxed Warning]: May only be prescribed by physicians enrolled in the Plenaxis™ Plus Program.
RESTRICTIONS — Abarelix is not distributed through retail pharmacies. Prior to its discontinuation, prescribing and distribution of abarelix was limited to physicians and hospital pharmacies participating in the Plenaxis™ PLUS program. Additional information may be obtained by calling 1-877-772-3247 or 1-866-753-2947.
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
QTc-prolonging agents: Additive QTc prolongation may occur. Life-threatening ventricular arrhythmias may result. Example drugs include class Ia and class III antiarrhythmics, cisapride, selected quinolones, erythromycin, pimozide, mesoridazine, and thioridazine.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Not indicated for use in women; may cause fetal harm if administered to a pregnant woman.
LACTATION — Excretion in breast milk unknown/not indicated in women
BREAST-FEEDING CONSIDERATIONS — Not indicated for use in women
MONITORING PARAMETERS — Signs/symptoms of allergic reaction (for at least 30 minutes after each injection). Obtain transaminase levels at baseline and periodically during treatment. Serum testosterone (to identify treatment failure) just prior to abarelix administration, beginning on day 29 and every 8 weeks thereafter. PSA and bone mineral density may be monitored as needed.
REFERENCE RANGE — Efficacy may be monitored by suppression of serum testosterone <50 ng/dL
TOXICOLOGY / OVERDOSE COMPREHENSIVE — No experience in overdose. Treatment is symptomatic and supportive.
MECHANISM OF ACTION — Competes with naturally-occurring GnRH for binding on receptors of the pituitary. Suppresses LH and FSH, resulting in decreased testosterone.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 4040 L (+/- 1607)
Metabolism: Hepatic, via peptide hydrolysis
Half-life elimination: 13 days
Time to peak, serum: 3 days (following I.M. administration)
Excretion: Urine (13% as unchanged drug)
Abarelix: Drug information
Copyright 1978-2006 Lexi-Comp, Inc. All rights reserved.
U.S. BRAND NAMES — Plenaxis™ [DSC]
PHARMACOLOGIC CATEGORY Gonadotropin Releasing Hormone Antagonist
DOSING: ADULTS — Male prostate cancer: I.M.: 100 mg administered on days 1, 15, 29 (week 4), then every 4 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product.
Injection, powder for reconstitution [preservative free]: 113 mg [provides 100 mg/2 mL depot suspension when reconstituted; packaged with diluent and syringe] [DSC]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer intramuscularly (to the buttock).
USE — Palliative treatment of advanced prostate cancer; treatment is limited to men who are not candidates for LHRH therapy, refuse surgical castration, and have one or more of the following complications due to metastases or local encroachment: 1) risk of neurological compromise, 2) ureteral or bladder outlet obstruction, or 3) severe bone pain (persisting despite narcotic analgesia)
ADVERSE REACTIONS SIGNIFICANT >10%: Cardiovascular: Hot flushes (79%), peripheral edema (15%) Central nervous system: Sleep disturbance (44%), pain (31%), dizziness (12%), headache (12%) Endocrine & metabolic: Breast enlargement (30%), nipple discharge/tenderness (20%) Gastrointestinal: Constipation (15%), diarrhea (11%) Neuromuscular & skeletal: Back pain (17%) Respiratory: Upper respiratory infection (12%)
1% to 10%: Central nervous system: Fatigue (10%) Endocrine & metabolic: Serum triglycerides increased (10%) Gastrointestinal: Nausea (10%) Genitourinary: Dysuria (10%), micturition frequency (10%), urinary retention (10%), urinary tract infection (10%) Hepatic: Transaminases increased (2% to 8%) Miscellaneous: Allergic reactions (urticaria, pruritus, syncope, hypotension); risk increases with prolonged treatment
CONTRAINDICATIONS — Hypersensitivity to abarelix or any component of the formulation
WARNINGS / PRECAUTIONS Box warnings: Allergic reactions: See "Concerns related to adverse effects" below. Diminished efficacy: See "Other warnings/precautions" below. Plenaxis™ Plus Program: See "Other warnings/precautions" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Allergic reactions: [U.S. Boxed Warning]: Has been associated with immediate-onset allergic reactions; may occur with initial dose and risk increases with duration of treatment. Observe for signs/symptoms of allergic reactions (which may include hypotension and/or syncope) for at least 30 minutes following each injection. Decreased bone mineral density: Extended treatment may result in a decrease in bone mineral density. QT prolongation: May cause prolongation of the QT interval; consider risk:benefit in patients with baseline QTc values >450 msec or patients receiving concurrent medications which prolong the QTc interval (class Ia and class III antiarrhythmics).
Other warnings/precautions: Diminished efficacy: [U.S. Boxed Warning]: Efficacy may diminish during prolonged treatment, particularly in patients weighing >225 pounds; monitor serum testosterone levels to identify treatment failures. Monitoring: Monitor transaminase levels and hepatic function during therapy. Plenaxis™ Plus Program: [U.S. Boxed Warning]: May only be prescribed by physicians enrolled in the Plenaxis™ Plus Program.
RESTRICTIONS — Abarelix is not distributed through retail pharmacies. Prior to its discontinuation, prescribing and distribution of abarelix was limited to physicians and hospital pharmacies participating in the Plenaxis™ PLUS program. Additional information may be obtained by calling 1-877-772-3247 or 1-866-753-2947.
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
QTc-prolonging agents: Additive QTc prolongation may occur. Life-threatening ventricular arrhythmias may result. Example drugs include class Ia and class III antiarrhythmics, cisapride, selected quinolones, erythromycin, pimozide, mesoridazine, and thioridazine.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Not indicated for use in women; may cause fetal harm if administered to a pregnant woman.
LACTATION — Excretion in breast milk unknown/not indicated in women
BREAST-FEEDING CONSIDERATIONS — Not indicated for use in women
MONITORING PARAMETERS — Signs/symptoms of allergic reaction (for at least 30 minutes after each injection). Obtain transaminase levels at baseline and periodically during treatment. Serum testosterone (to identify treatment failure) just prior to abarelix administration, beginning on day 29 and every 8 weeks thereafter. PSA and bone mineral density may be monitored as needed.
REFERENCE RANGE — Efficacy may be monitored by suppression of serum testosterone <50 ng/dL
TOXICOLOGY / OVERDOSE COMPREHENSIVE — No experience in overdose. Treatment is symptomatic and supportive.
MECHANISM OF ACTION — Competes with naturally-occurring GnRH for binding on receptors of the pituitary. Suppresses LH and FSH, resulting in decreased testosterone.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 4040 L (+/- 1607)
Metabolism: Hepatic, via peptide hydrolysis
Half-life elimination: 13 days
Time to peak, serum: 3 days (following I.M. administration)
Excretion: Urine (13% as unchanged drug)
U.S. BRAND NAMES — Plenaxis™ [DSC]
PHARMACOLOGIC CATEGORY Gonadotropin Releasing Hormone Antagonist
DOSING: ADULTS — Male prostate cancer: I.M.: 100 mg administered on days 1, 15, 29 (week 4), then every 4 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product.
Injection, powder for reconstitution [preservative free]: 113 mg [provides 100 mg/2 mL depot suspension when reconstituted; packaged with diluent and syringe] [DSC]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer intramuscularly (to the buttock).
USE — Palliative treatment of advanced prostate cancer; treatment is limited to men who are not candidates for LHRH therapy, refuse surgical castration, and have one or more of the following complications due to metastases or local encroachment: 1) risk of neurological compromise, 2) ureteral or bladder outlet obstruction, or 3) severe bone pain (persisting despite narcotic analgesia)
ADVERSE REACTIONS SIGNIFICANT >10%: Cardiovascular: Hot flushes (79%), peripheral edema (15%) Central nervous system: Sleep disturbance (44%), pain (31%), dizziness (12%), headache (12%) Endocrine & metabolic: Breast enlargement (30%), nipple discharge/tenderness (20%) Gastrointestinal: Constipation (15%), diarrhea (11%) Neuromuscular & skeletal: Back pain (17%) Respiratory: Upper respiratory infection (12%)
1% to 10%: Central nervous system: Fatigue (10%) Endocrine & metabolic: Serum triglycerides increased (10%) Gastrointestinal: Nausea (10%) Genitourinary: Dysuria (10%), micturition frequency (10%), urinary retention (10%), urinary tract infection (10%) Hepatic: Transaminases increased (2% to 8%) Miscellaneous: Allergic reactions (urticaria, pruritus, syncope, hypotension); risk increases with prolonged treatment
CONTRAINDICATIONS — Hypersensitivity to abarelix or any component of the formulation
WARNINGS / PRECAUTIONS Box warnings: Allergic reactions: See "Concerns related to adverse effects" below. Diminished efficacy: See "Other warnings/precautions" below. Plenaxis™ Plus Program: See "Other warnings/precautions" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Allergic reactions: [U.S. Boxed Warning]: Has been associated with immediate-onset allergic reactions; may occur with initial dose and risk increases with duration of treatment. Observe for signs/symptoms of allergic reactions (which may include hypotension and/or syncope) for at least 30 minutes following each injection. Decreased bone mineral density: Extended treatment may result in a decrease in bone mineral density. QT prolongation: May cause prolongation of the QT interval; consider risk:benefit in patients with baseline QTc values >450 msec or patients receiving concurrent medications which prolong the QTc interval (class Ia and class III antiarrhythmics).
Other warnings/precautions: Diminished efficacy: [U.S. Boxed Warning]: Efficacy may diminish during prolonged treatment, particularly in patients weighing >225 pounds; monitor serum testosterone levels to identify treatment failures. Monitoring: Monitor transaminase levels and hepatic function during therapy. Plenaxis™ Plus Program: [U.S. Boxed Warning]: May only be prescribed by physicians enrolled in the Plenaxis™ Plus Program.
RESTRICTIONS — Abarelix is not distributed through retail pharmacies. Prior to its discontinuation, prescribing and distribution of abarelix was limited to physicians and hospital pharmacies participating in the Plenaxis™ PLUS program. Additional information may be obtained by calling 1-877-772-3247 or 1-866-753-2947.
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
QTc-prolonging agents: Additive QTc prolongation may occur. Life-threatening ventricular arrhythmias may result. Example drugs include class Ia and class III antiarrhythmics, cisapride, selected quinolones, erythromycin, pimozide, mesoridazine, and thioridazine.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Not indicated for use in women; may cause fetal harm if administered to a pregnant woman.
LACTATION — Excretion in breast milk unknown/not indicated in women
BREAST-FEEDING CONSIDERATIONS — Not indicated for use in women
MONITORING PARAMETERS — Signs/symptoms of allergic reaction (for at least 30 minutes after each injection). Obtain transaminase levels at baseline and periodically during treatment. Serum testosterone (to identify treatment failure) just prior to abarelix administration, beginning on day 29 and every 8 weeks thereafter. PSA and bone mineral density may be monitored as needed.
REFERENCE RANGE — Efficacy may be monitored by suppression of serum testosterone <50 ng/dL
TOXICOLOGY / OVERDOSE COMPREHENSIVE — No experience in overdose. Treatment is symptomatic and supportive.
MECHANISM OF ACTION — Competes with naturally-occurring GnRH for binding on receptors of the pituitary. Suppresses LH and FSH, resulting in decreased testosterone.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 4040 L (+/- 1607)
Metabolism: Hepatic, via peptide hydrolysis
Half-life elimination: 13 days
Time to peak, serum: 3 days (following I.M. administration)
Excretion: Urine (13% as unchanged drug)
Abacavir, lamivudine, and zidovudine: Drug information
(For additional information see "Abacavir, lamivudine, and zidovudine: Patient drug information" and see "Abacavir, lamivudine, and zidovudine: Pediatric drug information")
U.S. BRAND NAMES — Trizivir®
PHARMACOLOGIC CATEGORY Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleoside)
DOSING: ADULTS — HIV treatment: Oral: 1 tablet twice daily. Note: Not recommended for patients <40 kg.
DOSING: PEDIATRIC — HIV treatment: Adolescents: Refer to adult dosing (not recommended for patients <40 kg).
(For additional information see "Abacavir, lamivudine, and zidovudine: Pediatric drug information")
DOSING: ELDERLY — Use with caution.
DOSING: RENAL IMPAIRMENT — Clcr 50 mL/minute: Avoid use.
DOSING: HEPATIC IMPAIRMENT — Use contraindicated.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: Trizivir®: Abacavir 300 mg, lamivudine 150 mg, and zidovudine 300 mg
DOSAGE FORMS: CONCISE Tablet: Trizivir®: Abacavir 300 mg, lamivudine 150 mg, and zidovudine 300 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer without regard to food or water.
USE — Treatment of HIV infection (either alone or in combination with other antiretroviral agents) in patients whose regimen would otherwise contain the components of Trizivir®
ADVERSE REACTIONS SIGNIFICANT — Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Trizivir®). If Trizivir® is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or if hypersensitivity cannot be ruled out.
The following information is based on CNA3005 study data concerning effects noted in patients receiving abacavir, lamivudine, and zidovudine. See individual agents for additional information.
>10%: Central nervous system: Headache (13%), malaise (12%), fatigue (12%) Gastrointestinal: Nausea (19%)
1% to 10%: Central nervous system: Fever/chills (6%), depression (6%), anxiety (5%) Dermatologic: Rash (5%) Endocrine & metabolic: Triglycerides increased (2% grade 3-4) Gastrointestinal: Nausea and vomiting (10%), diarrhea (7%), amylase increased (2%) Hematologic: Neutropenia (5%) Hepatic: ALT increased (6%) Neuromuscular & skeletal: CPK increased (7%) Otic: Ear infection (5%) Respiratory: Nose/throat infection (5%) Miscellaneous: Hypersensitivity (2% to 9% based on abacavir component), viral infection (5%)
Other (frequency unknown): Pancreatitis, GGT increased, fat redistribution, immune reconstitution syndrome
CONTRAINDICATIONS — Hypersensitivity to abacavir, lamivudine, zidovudine, or any component of the formulation; hepatic impairment. Do not rechallenge patients who have experienced hypersensitivity to abacavir.
WARNINGS / PRECAUTIONS Box warnings: Chronic hepatitis B: See "Disease-related concerns" below. Hematologic toxicity: See "Concerns related to adverse effects" below. HIV: Appropriate use: See "Disease-related concerns" below. Hypersensitivity reactions: See "Concerns related to adverse effects" below. Lactic acidosis/hepatomegaly: See "Concerns related to adverse effects" below. Myopathy: See "Concerns related to adverse effects" below.
Concerns related to adverse effects: Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance). Hematologic toxicity: [U.S. Boxed Warning]: Zidovudine has been associated with hematologic toxicities (eg, neutropenia, anemia); use with caution in patients with bone marrow compromise. Hypersensitivity reactions: [U.S. Boxed Warning]: Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Trizivir®). Patients exhibiting symptoms of fever, skin rash, fatigue, respiratory symptoms (eg, pharyngitis, dyspnea, cough) and/or GI symptoms (eg, abdominal pain, nausea, vomiting, diarrhea) should discontinue therapy immediately and call for medical attention. Trizivir® should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible. Trizivir® SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. Fatal hypersensitivity reactions have occurred following the reintroduction of abacavir in patients whose therapy was interrupted (eg, interruption in drug supply, temporary discontinuation while treating other conditions). Reactions occurred within hours. In some cases, signs of hypersensitivity may have been previously present, but attributed to other medical conditions (eg, acute onset respiratory diseases, gastroenteritis, reactions to other medications). If Trizivir® is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out. To report these events on Trizivir® hypersensitivity, a registry has been established (1-800-270-0425). Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection; further evaluation and treatment may be required. Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis). Myopathy: [U.S. Boxed Warning]: Prolonged use of zidovudine has been associated with symptomatic myopathy and myositis.
Disease-related concerns: Chronic hepatitis B: [U.S. Boxed Warning]: Exacerbation of hepatitis B has been reported with discontinuation of lamivudine in coinfected HIV/HBV patients; monitor hepatic function closely for several months after discontinuing Trizivir® in coinfected patients. HIV: Appropriate use: [U.S. Boxed Warning]: This combination should only be used as part of a multidrug regimen for which the individual components are indicated. Renal impairment: Trizivir®, as a fixed-dose combination tablet, should not be used in patients with Clcr 50 mL/minute.
Concurrent drug therapy issues: Interferon alfa: Use with caution in combination with interferon alfa with or without ribavirin in HIV/HBV coinfected patients; monitor closely for hepatic decompensation, anemia, or neutropenia; dose reduction or discontinuation of interferon and/or ribavirin may be required if toxicity evident.
Special populations: Adults <40 kg: Trizivir®, as a fixed-dose combination tablet, should not be used in patients <40 kg or those requiring dosage adjustment. Pediatrics: Trizivir®, as a fixed-dose combination tablet, should not be used in children.
RESTRICTIONS — An FDA-approved medication guide and warning card (summarizing symptoms of hypersensitivity) must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS — See individual agents.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — See individual agents.
LACTATION — See individual agents.
BREAST-FEEDING CONSIDERATIONS — See individual agents.
DIETARY CONSIDERATIONS — May be taken without regard to food or water.
PRICING — (data from drugstore.com)Tablets (Trizivir) 300-150-300 mg (60): $1154.51
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms of overdose with zidovudine include nausea, vomiting, headache, dizziness, drowsiness, lethargy, confusion, and hematologic changes. Myocardial degeneration has been documented in animals during long-term high-dose toxicology studies; clinical relevance is unknown. Treatment is symptom-directed and supportive. Peritoneal dialysis and hemodialysis have little to no effect on the removal of the components of Trizivir®.
MECHANISM OF ACTION — The combination of abacavir, lamivudine, and zidovudine is believed to act synergistically to inhibit reverse transcriptase via DNA chain termination after incorporation of the nucleoside analogue as well as to delay the emergence of mutations conferring resistance.
PHARMACODYNAMICS / KINETICS — Bioavailability studies of Trizivir® show no difference in AUC or Cmax when compared to abacavir, lamivudine, and zidovudine given together as individual agents. See individual agents.
Abacavir, lamivudine, and zidovudine: Drug information
(For additional information see "Abacavir, lamivudine, and zidovudine: Patient drug information" and see "Abacavir, lamivudine, and zidovudine: Pediatric drug information")
U.S. BRAND NAMES — Trizivir®
PHARMACOLOGIC CATEGORY Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleoside)
DOSING: ADULTS — HIV treatment: Oral: 1 tablet twice daily. Note: Not recommended for patients <40 kg.
DOSING: PEDIATRIC — HIV treatment: Adolescents: Refer to adult dosing (not recommended for patients <40 kg).
(For additional information see "Abacavir, lamivudine, and zidovudine: Pediatric drug information")
DOSING: ELDERLY — Use with caution.
DOSING: RENAL IMPAIRMENT — Clcr 50 mL/minute: Avoid use.
DOSING: HEPATIC IMPAIRMENT — Use contraindicated.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: Trizivir®: Abacavir 300 mg, lamivudine 150 mg, and zidovudine 300 mg
DOSAGE FORMS: CONCISE Tablet: Trizivir®: Abacavir 300 mg, lamivudine 150 mg, and zidovudine 300 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer without regard to food or water.
USE — Treatment of HIV infection (either alone or in combination with other antiretroviral agents) in patients whose regimen would otherwise contain the components of Trizivir®
ADVERSE REACTIONS SIGNIFICANT — Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Trizivir®). If Trizivir® is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or if hypersensitivity cannot be ruled out.
The following information is based on CNA3005 study data concerning effects noted in patients receiving abacavir, lamivudine, and zidovudine. See individual agents for additional information.
>10%: Central nervous system: Headache (13%), malaise (12%), fatigue (12%) Gastrointestinal: Nausea (19%)
1% to 10%: Central nervous system: Fever/chills (6%), depression (6%), anxiety (5%) Dermatologic: Rash (5%) Endocrine & metabolic: Triglycerides increased (2% grade 3-4) Gastrointestinal: Nausea and vomiting (10%), diarrhea (7%), amylase increased (2%) Hematologic: Neutropenia (5%) Hepatic: ALT increased (6%) Neuromuscular & skeletal: CPK increased (7%) Otic: Ear infection (5%) Respiratory: Nose/throat infection (5%) Miscellaneous: Hypersensitivity (2% to 9% based on abacavir component), viral infection (5%)
Other (frequency unknown): Pancreatitis, GGT increased, fat redistribution, immune reconstitution syndrome
CONTRAINDICATIONS — Hypersensitivity to abacavir, lamivudine, zidovudine, or any component of the formulation; hepatic impairment. Do not rechallenge patients who have experienced hypersensitivity to abacavir.
WARNINGS / PRECAUTIONS Box warnings: Chronic hepatitis B: See "Disease-related concerns" below. Hematologic toxicity: See "Concerns related to adverse effects" below. HIV: Appropriate use: See "Disease-related concerns" below. Hypersensitivity reactions: See "Concerns related to adverse effects" below. Lactic acidosis/hepatomegaly: See "Concerns related to adverse effects" below. Myopathy: See "Concerns related to adverse effects" below.
Concerns related to adverse effects: Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance). Hematologic toxicity: [U.S. Boxed Warning]: Zidovudine has been associated with hematologic toxicities (eg, neutropenia, anemia); use with caution in patients with bone marrow compromise. Hypersensitivity reactions: [U.S. Boxed Warning]: Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Trizivir®). Patients exhibiting symptoms of fever, skin rash, fatigue, respiratory symptoms (eg, pharyngitis, dyspnea, cough) and/or GI symptoms (eg, abdominal pain, nausea, vomiting, diarrhea) should discontinue therapy immediately and call for medical attention. Trizivir® should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible. Trizivir® SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. Fatal hypersensitivity reactions have occurred following the reintroduction of abacavir in patients whose therapy was interrupted (eg, interruption in drug supply, temporary discontinuation while treating other conditions). Reactions occurred within hours. In some cases, signs of hypersensitivity may have been previously present, but attributed to other medical conditions (eg, acute onset respiratory diseases, gastroenteritis, reactions to other medications). If Trizivir® is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out. To report these events on Trizivir® hypersensitivity, a registry has been established (1-800-270-0425). Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection; further evaluation and treatment may be required. Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis). Myopathy: [U.S. Boxed Warning]: Prolonged use of zidovudine has been associated with symptomatic myopathy and myositis.
Disease-related concerns: Chronic hepatitis B: [U.S. Boxed Warning]: Exacerbation of hepatitis B has been reported with discontinuation of lamivudine in coinfected HIV/HBV patients; monitor hepatic function closely for several months after discontinuing Trizivir® in coinfected patients. HIV: Appropriate use: [U.S. Boxed Warning]: This combination should only be used as part of a multidrug regimen for which the individual components are indicated. Renal impairment: Trizivir®, as a fixed-dose combination tablet, should not be used in patients with Clcr 50 mL/minute.
Concurrent drug therapy issues: Interferon alfa: Use with caution in combination with interferon alfa with or without ribavirin in HIV/HBV coinfected patients; monitor closely for hepatic decompensation, anemia, or neutropenia; dose reduction or discontinuation of interferon and/or ribavirin may be required if toxicity evident.
Special populations: Adults <40 kg: Trizivir®, as a fixed-dose combination tablet, should not be used in patients <40 kg or those requiring dosage adjustment. Pediatrics: Trizivir®, as a fixed-dose combination tablet, should not be used in children.
RESTRICTIONS — An FDA-approved medication guide and warning card (summarizing symptoms of hypersensitivity) must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS — See individual agents.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — See individual agents.
LACTATION — See individual agents.
BREAST-FEEDING CONSIDERATIONS — See individual agents.
DIETARY CONSIDERATIONS — May be taken without regard to food or water.
PRICING — (data from drugstore.com)Tablets (Trizivir) 300-150-300 mg (60): $1154.51
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms of overdose with zidovudine include nausea, vomiting, headache, dizziness, drowsiness, lethargy, confusion, and hematologic changes. Myocardial degeneration has been documented in animals during long-term high-dose toxicology studies; clinical relevance is unknown. Treatment is symptom-directed and supportive. Peritoneal dialysis and hemodialysis have little to no effect on the removal of the components of Trizivir®.
MECHANISM OF ACTION — The combination of abacavir, lamivudine, and zidovudine is believed to act synergistically to inhibit reverse transcriptase via DNA chain termination after incorporation of the nucleoside analogue as well as to delay the emergence of mutations conferring resistance.
PHARMACODYNAMICS / KINETICS — Bioavailability studies of Trizivir® show no difference in AUC or Cmax when compared to abacavir, lamivudine, and zidovudine given together as individual agents. See individual agents.
Abacavir and lamivudine: Drug information
Copyright 1978-2006 Lexi-Comp, Inc. All rights reserved.
(For additional information see "Abacavir and lamivudine: Patient drug information" and see "Abacavir and lamivudine: Pediatric drug information")
U.S. BRAND NAMES — Epzicom™
PHARMACOLOGIC CATEGORY Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleoside)
DOSING: ADULTS — HIV: Oral: One tablet (abacavir 600 mg and lamivudine 300 mg) once daily
DOSING: RENAL IMPAIRMENT — Clcr <50 mL/minute: Use not recommended
DOSING: HEPATIC IMPAIRMENT — Use contraindicated.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: Epzicom™: Abacavir 600 mg and lamivudine 300 mg
DOSAGE FORMS: CONCISE Tablet: Epzicom™: Abacavir 600 mg and lamivudine 300 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered with or without food.
USE — Treatment of HIV infections in combination with other antiretroviral agents
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
Postmarketing and/or case reports: Alopecia, anaphylaxis, anemia, aplastic anemia, breath sounds abnormal, CPK increased, erythema multiforme, fat redistribution, hepatic steatosis, hepatitis B exacerbation, hyperglycemia, hypersensitivity reaction, lactic acidosis, lymphadenopathy, muscle weakness, pancreatitis, paresthesia, peripheral neuropathy, rhabdomyolysis, seizure, splenomegaly, Stevens-Johnson syndrome, stomatitis, urticaria, weakness, wheezing
CONTRAINDICATIONS — Hypersensitivity to abacavir, lamivudine, or any component of the formulation; hepatic impairment. Do not rechallenge patients who have experienced hypersensitivity to abacavir.
WARNINGS / PRECAUTIONS Box warnings: Chronic hepatitis B: . HIV: Appropriate use: . Hypersensitivity reactions: . Lactic acidosis/hepatomegaly: .
Concerns related to adverse effects: Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance). Hypersensitivity reactions: [U.S. Boxed Warning]: Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Epzicom™). Patients exhibiting symptoms of fever, skin rash, fatigue, respiratory symptoms (eg, pharyngitis, dyspnea, cough) and/or GI symptoms (eg, abdominal pain, nausea, vomiting, diarrhea) should discontinue therapy immediately and call for medical attention. Epzicom™ should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible. Epzicom™ SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. Fatal hypersensitivity reactions have occurred following the reintroduction of abacavir in patients whose therapy was interrupted (eg, interruption in drug supply, temporary discontinuation while treating other conditions). Reactions occurred within hours. In some cases, signs of hypersensitivity may have been previously present, but attributed to other medical conditions (eg, acute onset respiratory diseases, gastroenteritis, reactions to other medications). If Epzicom™ is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out. To report these events on Epzicom™ hypersensitivity, a registry has been established (1-800-270-0425). Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection; further evaluation and treatment may be required. Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).
Disease-related concerns: Chronic hepatitis B: [U.S. Boxed Warning]: Following discontinuation of lamivudine, severe acute exacerbations of hepatitis B in patients coinfected with HBV and HIV have been reported. Monitor patients closely for several months following discontinuation of therapy for chronic hepatitis B; clinical exacerbations may occur. HIV: Appropriate use: [U.S. Boxed Warning]: This combination should only be used as part of a multidrug regimen for which the individual components are indicated. Renal impairment: Due to fixed dose of combination product, use is not recommended with renal impairment (Clcr <50 mL/minute).
Concurrent drug therapy issues: Interferon alfa: Use with caution in combination with interferon alfa with or without ribavirin in HIV/HBV coinfected patients; monitor closely for hepatic decompensation, anemia, or neutropenia; dose reduction or discontinuation of interferon and/or ribavirin may be required if toxicity evident.
Special populations: Pediatrics: Due to fixed dose of combination product, use is not recommended in children.
RESTRICTIONS — An FDA-approved medication guide and warning card (summarizing symptoms of hypersensitivity) must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS See individual agents.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — See individual agents.
LACTATION — See individual agents.
BREAST-FEEDING CONSIDERATIONS — HIV-infected mothers are discouraged from breast-feeding to decrease potential transmission of HIV. See individual agents.
DIETARY CONSIDERATIONS — May be taken with or without food.
PRICING — (data from drugstore.com)Tablets (Epzicom) 600-300 mg (30): $790.34
MONITORING PARAMETERS — Amylase, bilirubin, liver enzymes, hematologic parameters, viral load, and CD4 count
TOXICOLOGY / OVERDOSE COMPREHENSIVE — See individual agents.
CANADIAN BRAND NAMES — Kivexa™
INTERNATIONAL BRAND NAMES — Kivexa (AR, AT, BE, BG, CA, CH, CL, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IT, NL, NO, PT, RU, SE, TR)
MECHANISM OF ACTION — Nucleoside reverse transcriptase inhibitor combination.
Abacavir is a guanosine analogue which is phosphorylated to carbovir triphosphate which interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Lamivudine is a cytosine analog. After lamivudine is triphosphorylated, the principle mode of action is inhibition of HIV reverse transcription via viral DNA chain termination; inhibits RNA-dependent DNA polymerase activities of reverse transcriptase.
PHARMACODYNAMICS / KINETICS — See individual agents.
(For additional information see "Abacavir and lamivudine: Patient drug information" and see "Abacavir and lamivudine: Pediatric drug information")
U.S. BRAND NAMES — Epzicom™
PHARMACOLOGIC CATEGORY Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleoside)
DOSING: ADULTS — HIV: Oral: One tablet (abacavir 600 mg and lamivudine 300 mg) once daily
DOSING: RENAL IMPAIRMENT — Clcr <50 mL/minute: Use not recommended
DOSING: HEPATIC IMPAIRMENT — Use contraindicated.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: Epzicom™: Abacavir 600 mg and lamivudine 300 mg
DOSAGE FORMS: CONCISE Tablet: Epzicom™: Abacavir 600 mg and lamivudine 300 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered with or without food.
USE — Treatment of HIV infections in combination with other antiretroviral agents
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
Postmarketing and/or case reports: Alopecia, anaphylaxis, anemia, aplastic anemia, breath sounds abnormal, CPK increased, erythema multiforme, fat redistribution, hepatic steatosis, hepatitis B exacerbation, hyperglycemia, hypersensitivity reaction, lactic acidosis, lymphadenopathy, muscle weakness, pancreatitis, paresthesia, peripheral neuropathy, rhabdomyolysis, seizure, splenomegaly, Stevens-Johnson syndrome, stomatitis, urticaria, weakness, wheezing
CONTRAINDICATIONS — Hypersensitivity to abacavir, lamivudine, or any component of the formulation; hepatic impairment. Do not rechallenge patients who have experienced hypersensitivity to abacavir.
WARNINGS / PRECAUTIONS Box warnings: Chronic hepatitis B: . HIV: Appropriate use: . Hypersensitivity reactions: . Lactic acidosis/hepatomegaly: .
Concerns related to adverse effects: Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance). Hypersensitivity reactions: [U.S. Boxed Warning]: Fatal hypersensitivity reactions have occurred in patients taking abacavir (in Epzicom™). Patients exhibiting symptoms of fever, skin rash, fatigue, respiratory symptoms (eg, pharyngitis, dyspnea, cough) and/or GI symptoms (eg, abdominal pain, nausea, vomiting, diarrhea) should discontinue therapy immediately and call for medical attention. Epzicom™ should be permanently discontinued if hypersensitivity cannot be ruled out, even when other diagnoses are possible. Epzicom™ SHOULD NOT be restarted because more severe symptoms may occur within hours, including LIFE-THREATENING HYPOTENSION AND DEATH. Fatal hypersensitivity reactions have occurred following the reintroduction of abacavir in patients whose therapy was interrupted (eg, interruption in drug supply, temporary discontinuation while treating other conditions). Reactions occurred within hours. In some cases, signs of hypersensitivity may have been previously present, but attributed to other medical conditions (eg, acute onset respiratory diseases, gastroenteritis, reactions to other medications). If Epzicom™ is to be restarted following an interruption in therapy, first evaluate the patient for previously unsuspected symptoms of hypersensitivity. Do not restart if hypersensitivity is suspected or cannot be ruled out. To report these events on Epzicom™ hypersensitivity, a registry has been established (1-800-270-0425). Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection; further evaluation and treatment may be required. Lactic acidosis/hepatomegaly: [U.S Boxed Warning]: Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues, including fatal cases; use with caution in patients with risk factors for liver disease (risk may be increased with female gender, obesity, pregnancy or prolonged exposure) and suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (transaminase elevation may/may not accompany hepatomegaly and steatosis).
Disease-related concerns: Chronic hepatitis B: [U.S. Boxed Warning]: Following discontinuation of lamivudine, severe acute exacerbations of hepatitis B in patients coinfected with HBV and HIV have been reported. Monitor patients closely for several months following discontinuation of therapy for chronic hepatitis B; clinical exacerbations may occur. HIV: Appropriate use: [U.S. Boxed Warning]: This combination should only be used as part of a multidrug regimen for which the individual components are indicated. Renal impairment: Due to fixed dose of combination product, use is not recommended with renal impairment (Clcr <50 mL/minute).
Concurrent drug therapy issues: Interferon alfa: Use with caution in combination with interferon alfa with or without ribavirin in HIV/HBV coinfected patients; monitor closely for hepatic decompensation, anemia, or neutropenia; dose reduction or discontinuation of interferon and/or ribavirin may be required if toxicity evident.
Special populations: Pediatrics: Due to fixed dose of combination product, use is not recommended in children.
RESTRICTIONS — An FDA-approved medication guide and warning card (summarizing symptoms of hypersensitivity) must be distributed when dispensing an outpatient prescription (new or refill) where this medication is to be used without direct supervision of a healthcare provider. Medication guides are available at http://www.fda.gov/cder/Offices/ODS/medication_guides.htm.
DRUG INTERACTIONS See individual agents.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — See individual agents.
LACTATION — See individual agents.
BREAST-FEEDING CONSIDERATIONS — HIV-infected mothers are discouraged from breast-feeding to decrease potential transmission of HIV. See individual agents.
DIETARY CONSIDERATIONS — May be taken with or without food.
PRICING — (data from drugstore.com)Tablets (Epzicom) 600-300 mg (30): $790.34
MONITORING PARAMETERS — Amylase, bilirubin, liver enzymes, hematologic parameters, viral load, and CD4 count
TOXICOLOGY / OVERDOSE COMPREHENSIVE — See individual agents.
CANADIAN BRAND NAMES — Kivexa™
INTERNATIONAL BRAND NAMES — Kivexa (AR, AT, BE, BG, CA, CH, CL, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IT, NL, NO, PT, RU, SE, TR)
MECHANISM OF ACTION — Nucleoside reverse transcriptase inhibitor combination.
Abacavir is a guanosine analogue which is phosphorylated to carbovir triphosphate which interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Lamivudine is a cytosine analog. After lamivudine is triphosphorylated, the principle mode of action is inhibition of HIV reverse transcription via viral DNA chain termination; inhibits RNA-dependent DNA polymerase activities of reverse transcriptase.
PHARMACODYNAMICS / KINETICS — See individual agents.
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