U.S. BRAND NAMES — Feiba VH
PHARMACOLOGIC CATEGORY
Activated Prothrombin Complex Concentrate (aPCC)
Antihemophilic Agent
Blood Product Derivative
DOSING: ADULTS — Control of bleeding: I.V.:
General dosing guidelines: 50-100 units/kg (maximum 200 units/kg)
Joint hemorrhage: 50 units/kg every 12 hours; may increase to 100 units/kg; continue until signs of clinical improvement occur
Mucous membrane bleeding: 50 units/kg every 6 hours; may increase to 100 units/kg (maximum: 2 administrations/day or 200 units/kg/day)
Soft tissue hemorrhage: 100 units/kg every 12 hours (maximum: 200 units/kg/day)
Other severe hemorrhage: 100 units/kg every 12 hours; may be used every 6 hours if needed; continue until clinical improvement
DOSING: PEDIATRIC — Refer to adult dosing.
(For additional information see "Activated prothrombin complex concentrates (factor VIII inhibitor bypassing activity): Pediatric drug information")
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL; packaging contains natural rubber latex]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Maximum infusion rate: 2 units/kg/minute. Following reconstitution, complete infusion within 3 hours.
USE — Hemophilia A & B patients with inhibitors who are to undergo surgery or those who are bleeding
USE - UNLABELED / INVESTIGATIONAL — Nonhemophiliac patients with acquired inhibitors with titers >5 Bethesda units (BU) to factors VIII, XI, and XII
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Blood pressure changes, chest pain, MI, pulse rate changes, thromboembolism
Dermatologic: Rash, urticaria
Hematologic: DIC, fibrin decreased, fibrin split products increased, platelets decreased, PT increased, PTT increased
Respiratory: Cough, respiratory distress
Miscellaneous: Allergic reaction, anamnestic response
CONTRAINDICATIONS — Patients with normal coagulation mechanism
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Thrombotic events: Observe closely for signs and symptoms of intravascular coagulation or thrombosis. High doses have been associated with thrombotic complications, including MI and DIC; single doses should not exceed 100 units/kg and daily doses should not exceed 200 units/kg. Use with caution when administering to patients with liver disease, postoperatively, neonates, or patients at risk of thromboembolic phenomena, disseminated intravascular coagulation or patients with signs of fibrinolysis due to the potential risk of thromboembolic complications.
Disease-related concerns: Hepatic impairment: Use with extreme caution in patients with hepatic impairment.
Dosage form specific issues: Factor VIII: Product contains minute amounts of factor VIII which may cause an anamnestic response. Human plasma: Product of human plasma; may potentially contain infectious agents which could transmit disease. Screening of donors, as well as testing and/or inactivation or removal of certain viruses, reduces the risk. Infections thought to be transmitted by this product should be reported to the manufacturer. Latex: Product packaging may contain natural rubber latex.
Other warnings/precautions: Appropriate use: Should only be used to control bleeding in patients with inhibitors resulting from coagulation factor deficiencies. Tests used to control improvement, such as aPTT, whole blood clotting time (WBCT), and thromboelastography (TEG), do not correlate with clinical efficacy. Dosing to normalize these values may result in DIC.
DRUG INTERACTIONS
Antifibrinolytic Agents: May enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Contains sodium 8 mg/mL
MONITORING PARAMETERS — Monitor for control of bleeding; signs and symptoms of DIC (blood pressure changes, pulse rate changes, chest pain/cough, fibrinogen decreased, platelet count decreased, fibrin-fibrinogen degradation products, significantly-prolonged thrombin time, PT, or partial thromboplastin time); hypotension; have epinephrine ready to treat hypersensitivity reactions. Note: Tests used to control efficacy such as aPTT, WBCT, and TEG do not correlate with clinical improvement. Dosing to normalize these values may result in DIC.
CANADIAN BRAND NAMES — Feiba VH Immuno
Tuesday, May 18, 2010
ctivated prothrombin complex concentrates
U.S. BRAND NAMES — Feiba VH
PHARMACOLOGIC CATEGORY
Activated Prothrombin Complex Concentrate (aPCC)
Antihemophilic Agent
Blood Product Derivative
DOSING: ADULTS — Control of bleeding: I.V.:
General dosing guidelines: 50-100 units/kg (maximum 200 units/kg)
Joint hemorrhage: 50 units/kg every 12 hours; may increase to 100 units/kg; continue until signs of clinical improvement occur
Mucous membrane bleeding: 50 units/kg every 6 hours; may increase to 100 units/kg (maximum: 2 administrations/day or 200 units/kg/day)
Soft tissue hemorrhage: 100 units/kg every 12 hours (maximum: 200 units/kg/day)
Other severe hemorrhage: 100 units/kg every 12 hours; may be used every 6 hours if needed; continue until clinical improvement
DOSING: PEDIATRIC — Refer to adult dosing.
(For additional information see "Activated prothrombin complex concentrates (factor VIII inhibitor bypassing activity): Pediatric drug information")
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL; packaging contains natural rubber latex]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Maximum infusion rate: 2 units/kg/minute. Following reconstitution, complete infusion within 3 hours.
USE — Hemophilia A & B patients with inhibitors who are to undergo surgery or those who are bleeding
USE - UNLABELED / INVESTIGATIONAL — Nonhemophiliac patients with acquired inhibitors with titers >5 Bethesda units (BU) to factors VIII, XI, and XII
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Blood pressure changes, chest pain, MI, pulse rate changes, thromboembolism
Dermatologic: Rash, urticaria
Hematologic: DIC, fibrin decreased, fibrin split products increased, platelets decreased, PT increased, PTT increased
Respiratory: Cough, respiratory distress
Miscellaneous: Allergic reaction, anamnestic response
CONTRAINDICATIONS — Patients with normal coagulation mechanism
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Thrombotic events: Observe closely for signs and symptoms of intravascular coagulation or thrombosis. High doses have been associated with thrombotic complications, including MI and DIC; single doses should not exceed 100 units/kg and daily doses should not exceed 200 units/kg. Use with caution when administering to patients with liver disease, postoperatively, neonates, or patients at risk of thromboembolic phenomena, disseminated intravascular coagulation or patients with signs of fibrinolysis due to the potential risk of thromboembolic complications.
Disease-related concerns: Hepatic impairment: Use with extreme caution in patients with hepatic impairment.
Dosage form specific issues: Factor VIII: Product contains minute amounts of factor VIII which may cause an anamnestic response. Human plasma: Product of human plasma; may potentially contain infectious agents which could transmit disease. Screening of donors, as well as testing and/or inactivation or removal of certain viruses, reduces the risk. Infections thought to be transmitted by this product should be reported to the manufacturer. Latex: Product packaging may contain natural rubber latex.
Other warnings/precautions: Appropriate use: Should only be used to control bleeding in patients with inhibitors resulting from coagulation factor deficiencies. Tests used to control improvement, such as aPTT, whole blood clotting time (WBCT), and thromboelastography (TEG), do not correlate with clinical efficacy. Dosing to normalize these values may result in DIC.
DRUG INTERACTIONS
Antifibrinolytic Agents: May enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Contains sodium 8 mg/mL
MONITORING PARAMETERS — Monitor for control of bleeding; signs and symptoms of DIC (blood pressure changes, pulse rate changes, chest pain/cough, fibrinogen decreased, platelet count decreased, fibrin-fibrinogen degradation products, significantly-prolonged thrombin time, PT, or partial thromboplastin time); hypotension; have epinephrine ready to treat hypersensitivity reactions. Note: Tests used to control efficacy such as aPTT, WBCT, and TEG do not correlate with clinical improvement. Dosing to normalize these values may result in DIC.
CANADIAN BRAND NAMES — Feiba VH Immuno
PHARMACOLOGIC CATEGORY
Activated Prothrombin Complex Concentrate (aPCC)
Antihemophilic Agent
Blood Product Derivative
DOSING: ADULTS — Control of bleeding: I.V.:
General dosing guidelines: 50-100 units/kg (maximum 200 units/kg)
Joint hemorrhage: 50 units/kg every 12 hours; may increase to 100 units/kg; continue until signs of clinical improvement occur
Mucous membrane bleeding: 50 units/kg every 6 hours; may increase to 100 units/kg (maximum: 2 administrations/day or 200 units/kg/day)
Soft tissue hemorrhage: 100 units/kg every 12 hours (maximum: 200 units/kg/day)
Other severe hemorrhage: 100 units/kg every 12 hours; may be used every 6 hours if needed; continue until clinical improvement
DOSING: PEDIATRIC — Refer to adult dosing.
(For additional information see "Activated prothrombin complex concentrates (factor VIII inhibitor bypassing activity): Pediatric drug information")
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL; packaging contains natural rubber latex]
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution:
Feiba VH: Each bottle is labeled with Immuno units of factor VIII [heparin free; contains sodium 8 mg/mL]
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Maximum infusion rate: 2 units/kg/minute. Following reconstitution, complete infusion within 3 hours.
USE — Hemophilia A & B patients with inhibitors who are to undergo surgery or those who are bleeding
USE - UNLABELED / INVESTIGATIONAL — Nonhemophiliac patients with acquired inhibitors with titers >5 Bethesda units (BU) to factors VIII, XI, and XII
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Blood pressure changes, chest pain, MI, pulse rate changes, thromboembolism
Dermatologic: Rash, urticaria
Hematologic: DIC, fibrin decreased, fibrin split products increased, platelets decreased, PT increased, PTT increased
Respiratory: Cough, respiratory distress
Miscellaneous: Allergic reaction, anamnestic response
CONTRAINDICATIONS — Patients with normal coagulation mechanism
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Thrombotic events: Observe closely for signs and symptoms of intravascular coagulation or thrombosis. High doses have been associated with thrombotic complications, including MI and DIC; single doses should not exceed 100 units/kg and daily doses should not exceed 200 units/kg. Use with caution when administering to patients with liver disease, postoperatively, neonates, or patients at risk of thromboembolic phenomena, disseminated intravascular coagulation or patients with signs of fibrinolysis due to the potential risk of thromboembolic complications.
Disease-related concerns: Hepatic impairment: Use with extreme caution in patients with hepatic impairment.
Dosage form specific issues: Factor VIII: Product contains minute amounts of factor VIII which may cause an anamnestic response. Human plasma: Product of human plasma; may potentially contain infectious agents which could transmit disease. Screening of donors, as well as testing and/or inactivation or removal of certain viruses, reduces the risk. Infections thought to be transmitted by this product should be reported to the manufacturer. Latex: Product packaging may contain natural rubber latex.
Other warnings/precautions: Appropriate use: Should only be used to control bleeding in patients with inhibitors resulting from coagulation factor deficiencies. Tests used to control improvement, such as aPTT, whole blood clotting time (WBCT), and thromboelastography (TEG), do not correlate with clinical efficacy. Dosing to normalize these values may result in DIC.
DRUG INTERACTIONS
Antifibrinolytic Agents: May enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex. Risk X: Avoid combination
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Contains sodium 8 mg/mL
MONITORING PARAMETERS — Monitor for control of bleeding; signs and symptoms of DIC (blood pressure changes, pulse rate changes, chest pain/cough, fibrinogen decreased, platelet count decreased, fibrin-fibrinogen degradation products, significantly-prolonged thrombin time, PT, or partial thromboplastin time); hypotension; have epinephrine ready to treat hypersensitivity reactions. Note: Tests used to control efficacy such as aPTT, WBCT, and TEG do not correlate with clinical improvement. Dosing to normalize these values may result in DIC.
CANADIAN BRAND NAMES — Feiba VH Immuno
Activated charcoal
U.S. BRAND NAMES — Actidose-Aqua® [OTC]; Actidose® with Sorbitol [OTC]; Char-Caps [OTC]; CharcoAid® G [OTC]; Charcoal Plus® DS [OTC]; CharcoCaps® [OTC]; EZ-Char™ [OTC]; Kerr Insta-Char® [OTC]; Requa® Activated Charcoal [OTC]
PHARMACOLOGIC CATEGORY
Antidote
DOSING: ADULTS
Acute poisoning:
Oral: 25-100 g as a single dose; if multiple doses are needed, additional doses may be given as 12.5 g/hour or equivalent (eg, 25 g every 2 hours)
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day)
Dietary supplement: Oral: 500-520 mg after meals; may repeat in 2 hours if needed (maximum: 10 g/day)
DOSING: PEDIATRIC
(For additional information see "Activated charcoal: Pediatric drug information")
Acute poisoning: Oral:
Children:
<1 year: 0.5-1 g/kg (10-25 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
1-12 years: 0.5-1 g/kg (25-50 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
>12 years: Refer to adult dosing.
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day).
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Char-Caps, CharcoCaps®: 260 mg
Pellets, for suspension:
EZ-Char™ : 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G: 15 g
Suspension:
Actidose-Aqua®: 15 g (72 mL); 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; unflavored or packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Suspension [with sorbitol]:
Actidose® with Sorbitol: 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Tablet:
Requa® Activated Charcoal: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS: 250 mg
DOSAGE FORMS: CONCISE
Capsule:
Char-Caps [OTC], CharcoCaps® [OTC]: 260 mg
Pellets, for suspension:
EZ-Char™ [OTC]: 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G [OTC]: 15 g
Suspension:
Actidose-Aqua® [OTC]: 15 g, 25 g, 50 g
Kerr Insta-Char® [OTC]: 25 g, 50 g
Suspension [with sorbitol]:
Actidose® with Sorbitol [OTC], Kerr Insta-Char® [OTC]: 25 g, 50 g
Tablet:
Requa® Activated Charcoal [OTC]: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS [OTC]: 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Powder
ADMINISTRATION — Flavoring agents (eg, chocolate, concentrated fruit juice) or thickening agents (eg, bentonite, carboxymethylcellulose) can enhance charcoal's palatability. If treatment includes ipecac syrup, induce vomiting prior to administration of charcoal. Often given with a laxative or cathartic; check for presence of bowel sounds before administration. I.V. antiemetics may be required to reduce the risk of vomiting during multiple-dose therapy with charcoal.
USE — Emergency treatment in poisoning by drugs and chemicals; aids the elimination of certain drugs and improves decontamination of excessive ingestions of sustained-release products or in the presence of bezoars; repetitive doses have proven useful to enhance the elimination of certain drugs (eg, carbamazepine, dapsone, phenobarbital, quinine, or theophylline); repetitive doses for gastric dialysis in uremia to adsorb various waste products; dietary supplement (digestive aid)
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Endocrine & metabolic: Hypernatremia, hypokalemia, and hypermagnesemia may occur with coadministration of cathartics
Gastrointestinal: Vomiting (incidence may increase with sorbitol), diarrhea (with sorbitol), constipation, swelling of abdomen, bowel obstruction, appendicitis
Respiratory: Aspiration (both gastric contents and charcoal)
Miscellaneous: Fecal discoloration (black)
CONTRAINDICATIONS — Hypersensitivity to charcoal or any component of the formulation; intestinal obstruction; GI tract not anatomically intact; patients at risk of hemorrhage or GI perforation; patients with an unprotected airway (eg, CNS depression without intubation); if use would increase risk and severity of aspiration
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Vomiting: Charcoal may cause vomiting; avoid use in hydrocarbon and caustic ingestions.
Disease-related concerns: Decreased peristalsis: Use with caution in patients with decreased peristalsis.
Concurrent drug therapy issues: Ipecac: When using ipecac with charcoal, ensure ipecac-induced vomiting has ceased prior to administering charcoal. Cathartics (eg, sorbitol, mannitol, magnesium sulfate): Coadministration of a cathartic is not recommended secondary to lack of compelling evidence and the increased morbidity associated with their use. If charcoal is administered with a cathartic, avoid excessive fluid and electrolyte losses, especially in children <1 year of age.
Special populations: Pediatrics: Charcoal with sorbitol not recommended in children <1 year of age.
Dosage form specific issues: Propylene glycol: Commercial charcoal products may contain propylene glycol.
Other warnings/precautions: Appropriate use: Not effective for cyanide, mineral acids, caustic alkalis, organic solvents, iron, ethanol, methanol, or lithium poisoning Efficacy: Most effective when administered within 30-60 minutes of ingestion.
DRUG INTERACTIONS
Leflunomide: Charcoal, Activated may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to charcoal when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Do not mix with milk, ice cream, sherbet, or marmalade (may reduce charcoal's effectiveness).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Does not enter breast milk/compatible
CANADIAN BRAND NAMES — Charcadole®; Charcadole® TFS; Charcadole®, Aqueous
INTERNATIONAL BRAND NAMES — Bekarbon (ID); Ca-R-Bon (TH); Carbo Medicinalis (PL); Carbomix (FR, SE); Carbon Natural (UY); Carbosorb (NZ); Carbosorb S (NZ); Carbosorb X (AU); Carbosorb XS (AU); Carbotural (MX); Charcodote (GB, HK, KP); Charcotrace (AU); Deltacarbon (TH); Mamograf (AR); Norit (IL); RCOL (IN); Ultracarbon (SG)
MECHANISM OF ACTION — Adsorbs toxic substances or irritants, thus inhibiting GI absorption; adsorbs intestinal gas; the addition of sorbitol results in hyperosmotic laxative action causing catharsis
PHARMACODYNAMICS / KINETICS — Excretion: Feces (as charcoal)
PATIENT INFORMATION — Charcoal causes the stools to turn black. Do not use prior to calling a poison control center or a prescriber
PHARMACOLOGIC CATEGORY
Antidote
DOSING: ADULTS
Acute poisoning:
Oral: 25-100 g as a single dose; if multiple doses are needed, additional doses may be given as 12.5 g/hour or equivalent (eg, 25 g every 2 hours)
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day)
Dietary supplement: Oral: 500-520 mg after meals; may repeat in 2 hours if needed (maximum: 10 g/day)
DOSING: PEDIATRIC
(For additional information see "Activated charcoal: Pediatric drug information")
Acute poisoning: Oral:
Children:
<1 year: 0.5-1 g/kg (10-25 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
1-12 years: 0.5-1 g/kg (25-50 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
>12 years: Refer to adult dosing.
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day).
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Char-Caps, CharcoCaps®: 260 mg
Pellets, for suspension:
EZ-Char™ : 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G: 15 g
Suspension:
Actidose-Aqua®: 15 g (72 mL); 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; unflavored or packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Suspension [with sorbitol]:
Actidose® with Sorbitol: 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Tablet:
Requa® Activated Charcoal: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS: 250 mg
DOSAGE FORMS: CONCISE
Capsule:
Char-Caps [OTC], CharcoCaps® [OTC]: 260 mg
Pellets, for suspension:
EZ-Char™ [OTC]: 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G [OTC]: 15 g
Suspension:
Actidose-Aqua® [OTC]: 15 g, 25 g, 50 g
Kerr Insta-Char® [OTC]: 25 g, 50 g
Suspension [with sorbitol]:
Actidose® with Sorbitol [OTC], Kerr Insta-Char® [OTC]: 25 g, 50 g
Tablet:
Requa® Activated Charcoal [OTC]: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS [OTC]: 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Powder
ADMINISTRATION — Flavoring agents (eg, chocolate, concentrated fruit juice) or thickening agents (eg, bentonite, carboxymethylcellulose) can enhance charcoal's palatability. If treatment includes ipecac syrup, induce vomiting prior to administration of charcoal. Often given with a laxative or cathartic; check for presence of bowel sounds before administration. I.V. antiemetics may be required to reduce the risk of vomiting during multiple-dose therapy with charcoal.
USE — Emergency treatment in poisoning by drugs and chemicals; aids the elimination of certain drugs and improves decontamination of excessive ingestions of sustained-release products or in the presence of bezoars; repetitive doses have proven useful to enhance the elimination of certain drugs (eg, carbamazepine, dapsone, phenobarbital, quinine, or theophylline); repetitive doses for gastric dialysis in uremia to adsorb various waste products; dietary supplement (digestive aid)
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Endocrine & metabolic: Hypernatremia, hypokalemia, and hypermagnesemia may occur with coadministration of cathartics
Gastrointestinal: Vomiting (incidence may increase with sorbitol), diarrhea (with sorbitol), constipation, swelling of abdomen, bowel obstruction, appendicitis
Respiratory: Aspiration (both gastric contents and charcoal)
Miscellaneous: Fecal discoloration (black)
CONTRAINDICATIONS — Hypersensitivity to charcoal or any component of the formulation; intestinal obstruction; GI tract not anatomically intact; patients at risk of hemorrhage or GI perforation; patients with an unprotected airway (eg, CNS depression without intubation); if use would increase risk and severity of aspiration
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Vomiting: Charcoal may cause vomiting; avoid use in hydrocarbon and caustic ingestions.
Disease-related concerns: Decreased peristalsis: Use with caution in patients with decreased peristalsis.
Concurrent drug therapy issues: Ipecac: When using ipecac with charcoal, ensure ipecac-induced vomiting has ceased prior to administering charcoal. Cathartics (eg, sorbitol, mannitol, magnesium sulfate): Coadministration of a cathartic is not recommended secondary to lack of compelling evidence and the increased morbidity associated with their use. If charcoal is administered with a cathartic, avoid excessive fluid and electrolyte losses, especially in children <1 year of age.
Special populations: Pediatrics: Charcoal with sorbitol not recommended in children <1 year of age.
Dosage form specific issues: Propylene glycol: Commercial charcoal products may contain propylene glycol.
Other warnings/precautions: Appropriate use: Not effective for cyanide, mineral acids, caustic alkalis, organic solvents, iron, ethanol, methanol, or lithium poisoning Efficacy: Most effective when administered within 30-60 minutes of ingestion.
DRUG INTERACTIONS
Leflunomide: Charcoal, Activated may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to charcoal when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Do not mix with milk, ice cream, sherbet, or marmalade (may reduce charcoal's effectiveness).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Does not enter breast milk/compatible
CANADIAN BRAND NAMES — Charcadole®; Charcadole® TFS; Charcadole®, Aqueous
INTERNATIONAL BRAND NAMES — Bekarbon (ID); Ca-R-Bon (TH); Carbo Medicinalis (PL); Carbomix (FR, SE); Carbon Natural (UY); Carbosorb (NZ); Carbosorb S (NZ); Carbosorb X (AU); Carbosorb XS (AU); Carbotural (MX); Charcodote (GB, HK, KP); Charcotrace (AU); Deltacarbon (TH); Mamograf (AR); Norit (IL); RCOL (IN); Ultracarbon (SG)
MECHANISM OF ACTION — Adsorbs toxic substances or irritants, thus inhibiting GI absorption; adsorbs intestinal gas; the addition of sorbitol results in hyperosmotic laxative action causing catharsis
PHARMACODYNAMICS / KINETICS — Excretion: Feces (as charcoal)
PATIENT INFORMATION — Charcoal causes the stools to turn black. Do not use prior to calling a poison control center or a prescriber
Acrivastine and pseudoephedrine
U.S. BRAND NAMES — Semprex®-D
PHARMACOLOGIC CATEGORY
Alpha/Beta Agonist
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT
>10%: Central nervous system: Drowsiness, headache
1% to 10%:
Cardiovascular: Tachycardia, palpitation
Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue
Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea
Genitourinary: Dysuria
Neuromuscular & skeletal: Weakness
Respiratory: Pharyngitis, cough increased
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr ≤ 48 mL/minute)
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease); contraindicated with severe disease. Diabetes: Use with caution in patients with diabetes mellitus. Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or glaucoma. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer). Renal impairment: Use with caution in patients with renal impairment; contraindicated if Clcr ≤ 48 mL/minute. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Pediatrics: Safety and efficacy have not been established in children <12 years of age.
DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Antacids: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Aluminum Hydroxide. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
Bromocriptine: Alpha-/Beta-Agonists may enhance the adverse/toxic effect of Bromocriptine. Including increased blood pressure, ventricular arrhythmias, and seizure. Risk C: Monitor therapy
Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Carbonic Anhydrase Inhibitors: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Brinzolamide; Dorzolamide. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
MAO Inhibitors: May enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Risk D: Consider therapy modification
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)
Capsules (Semprex-D)
8-60 mg (30): $62.39
INTERNATIONAL BRAND NAMES — Duact (DK, FI)
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS
Pseudoephedrine: See Pseudoephedrine.
Acrivastine:
Metabolism: Minimally hepatic
Time to peak: ~1.1 hours
Excretion: Urine (84%); feces (13%)
PHARMACOLOGIC CATEGORY
Alpha/Beta Agonist
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT
>10%: Central nervous system: Drowsiness, headache
1% to 10%:
Cardiovascular: Tachycardia, palpitation
Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue
Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea
Genitourinary: Dysuria
Neuromuscular & skeletal: Weakness
Respiratory: Pharyngitis, cough increased
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr ≤ 48 mL/minute)
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease); contraindicated with severe disease. Diabetes: Use with caution in patients with diabetes mellitus. Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or glaucoma. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer). Renal impairment: Use with caution in patients with renal impairment; contraindicated if Clcr ≤ 48 mL/minute. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Pediatrics: Safety and efficacy have not been established in children <12 years of age.
DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Antacids: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Aluminum Hydroxide. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
Bromocriptine: Alpha-/Beta-Agonists may enhance the adverse/toxic effect of Bromocriptine. Including increased blood pressure, ventricular arrhythmias, and seizure. Risk C: Monitor therapy
Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Carbonic Anhydrase Inhibitors: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Brinzolamide; Dorzolamide. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
MAO Inhibitors: May enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Risk D: Consider therapy modification
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)
Capsules (Semprex-D)
8-60 mg (30): $62.39
INTERNATIONAL BRAND NAMES — Duact (DK, FI)
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS
Pseudoephedrine: See Pseudoephedrine.
Acrivastine:
Metabolism: Minimally hepatic
Time to peak: ~1.1 hours
Excretion: Urine (84%); feces (13%)
Activated charcoal
U.S. BRAND NAMES — Actidose-Aqua® [OTC]; Actidose® with Sorbitol [OTC]; Char-Caps [OTC]; CharcoAid® G [OTC]; Charcoal Plus® DS [OTC]; CharcoCaps® [OTC]; EZ-Char™ [OTC]; Kerr Insta-Char® [OTC]; Requa® Activated Charcoal [OTC]
PHARMACOLOGIC CATEGORY
Antidote
DOSING: ADULTS
Acute poisoning:
Oral: 25-100 g as a single dose; if multiple doses are needed, additional doses may be given as 12.5 g/hour or equivalent (eg, 25 g every 2 hours)
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day)
Dietary supplement: Oral: 500-520 mg after meals; may repeat in 2 hours if needed (maximum: 10 g/day)
DOSING: PEDIATRIC
(For additional information see "Activated charcoal: Pediatric drug information")
Acute poisoning: Oral:
Children:
<1 year: 0.5-1 g/kg (10-25 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
1-12 years: 0.5-1 g/kg (25-50 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
>12 years: Refer to adult dosing.
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day).
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Char-Caps, CharcoCaps®: 260 mg
Pellets, for suspension:
EZ-Char™ : 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G: 15 g
Suspension:
Actidose-Aqua®: 15 g (72 mL); 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; unflavored or packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Suspension [with sorbitol]:
Actidose® with Sorbitol: 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Tablet:
Requa® Activated Charcoal: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS: 250 mg
DOSAGE FORMS: CONCISE
Capsule:
Char-Caps [OTC], CharcoCaps® [OTC]: 260 mg
Pellets, for suspension:
EZ-Char™ [OTC]: 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G [OTC]: 15 g
Suspension:
Actidose-Aqua® [OTC]: 15 g, 25 g, 50 g
Kerr Insta-Char® [OTC]: 25 g, 50 g
Suspension [with sorbitol]:
Actidose® with Sorbitol [OTC], Kerr Insta-Char® [OTC]: 25 g, 50 g
Tablet:
Requa® Activated Charcoal [OTC]: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS [OTC]: 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Powder
ADMINISTRATION — Flavoring agents (eg, chocolate, concentrated fruit juice) or thickening agents (eg, bentonite, carboxymethylcellulose) can enhance charcoal's palatability. If treatment includes ipecac syrup, induce vomiting prior to administration of charcoal. Often given with a laxative or cathartic; check for presence of bowel sounds before administration. I.V. antiemetics may be required to reduce the risk of vomiting during multiple-dose therapy with charcoal.
USE — Emergency treatment in poisoning by drugs and chemicals; aids the elimination of certain drugs and improves decontamination of excessive ingestions of sustained-release products or in the presence of bezoars; repetitive doses have proven useful to enhance the elimination of certain drugs (eg, carbamazepine, dapsone, phenobarbital, quinine, or theophylline); repetitive doses for gastric dialysis in uremia to adsorb various waste products; dietary supplement (digestive aid)
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Endocrine & metabolic: Hypernatremia, hypokalemia, and hypermagnesemia may occur with coadministration of cathartics
Gastrointestinal: Vomiting (incidence may increase with sorbitol), diarrhea (with sorbitol), constipation, swelling of abdomen, bowel obstruction, appendicitis
Respiratory: Aspiration (both gastric contents and charcoal)
Miscellaneous: Fecal discoloration (black)
CONTRAINDICATIONS — Hypersensitivity to charcoal or any component of the formulation; intestinal obstruction; GI tract not anatomically intact; patients at risk of hemorrhage or GI perforation; patients with an unprotected airway (eg, CNS depression without intubation); if use would increase risk and severity of aspiration
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Vomiting: Charcoal may cause vomiting; avoid use in hydrocarbon and caustic ingestions.
Disease-related concerns: Decreased peristalsis: Use with caution in patients with decreased peristalsis.
Concurrent drug therapy issues: Ipecac: When using ipecac with charcoal, ensure ipecac-induced vomiting has ceased prior to administering charcoal. Cathartics (eg, sorbitol, mannitol, magnesium sulfate): Coadministration of a cathartic is not recommended secondary to lack of compelling evidence and the increased morbidity associated with their use. If charcoal is administered with a cathartic, avoid excessive fluid and electrolyte losses, especially in children <1 year of age.
Special populations: Pediatrics: Charcoal with sorbitol not recommended in children <1 year of age.
Dosage form specific issues: Propylene glycol: Commercial charcoal products may contain propylene glycol.
Other warnings/precautions: Appropriate use: Not effective for cyanide, mineral acids, caustic alkalis, organic solvents, iron, ethanol, methanol, or lithium poisoning Efficacy: Most effective when administered within 30-60 minutes of ingestion.
DRUG INTERACTIONS
Leflunomide: Charcoal, Activated may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to charcoal when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Do not mix with milk, ice cream, sherbet, or marmalade (may reduce charcoal's effectiveness).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Does not enter breast milk/compatible
CANADIAN BRAND NAMES — Charcadole®; Charcadole® TFS; Charcadole®, Aqueous
INTERNATIONAL BRAND NAMES — Bekarbon (ID); Ca-R-Bon (TH); Carbo Medicinalis (PL); Carbomix (FR, SE); Carbon Natural (UY); Carbosorb (NZ); Carbosorb S (NZ); Carbosorb X (AU); Carbosorb XS (AU); Carbotural (MX); Charcodote (GB, HK, KP); Charcotrace (AU); Deltacarbon (TH); Mamograf (AR); Norit (IL); RCOL (IN); Ultracarbon (SG)
MECHANISM OF ACTION — Adsorbs toxic substances or irritants, thus inhibiting GI absorption; adsorbs intestinal gas; the addition of sorbitol results in hyperosmotic laxative action causing catharsis
PHARMACODYNAMICS / KINETICS — Excretion: Feces (as charcoal)
PATIENT INFORMATION — Charcoal causes the stools to turn black. Do not use prior to calling a poison control center or a prescriber
PHARMACOLOGIC CATEGORY
Antidote
DOSING: ADULTS
Acute poisoning:
Oral: 25-100 g as a single dose; if multiple doses are needed, additional doses may be given as 12.5 g/hour or equivalent (eg, 25 g every 2 hours)
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day)
Dietary supplement: Oral: 500-520 mg after meals; may repeat in 2 hours if needed (maximum: 10 g/day)
DOSING: PEDIATRIC
(For additional information see "Activated charcoal: Pediatric drug information")
Acute poisoning: Oral:
Children:
<1 year: 0.5-1 g/kg (10-25 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
1-12 years: 0.5-1 g/kg (25-50 g) as a single dose; if multiple doses are needed, give as 0.25 g/kg/hour or equivalent (eg, 0.5 g/kg every 2 hours)
>12 years: Refer to adult dosing.
Note: ~10 g of activated charcoal for each 1 g of toxin is considered adequate; this may require multiple doses. If sorbitol is also used, sorbitol dose should not exceed 1.5 g/kg. When using multiple doses of charcoal, sorbitol should be given with every other dose (not to exceed 2 doses/day).
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Char-Caps, CharcoCaps®: 260 mg
Pellets, for suspension:
EZ-Char™ : 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G: 15 g
Suspension:
Actidose-Aqua®: 15 g (72 mL); 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; unflavored or packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Suspension [with sorbitol]:
Actidose® with Sorbitol: 25 g (120 mL); 50 g (240 mL)
Kerr Insta-Char®: 25 g (120 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]; 50 g (240 mL) [contains sodium benzoate; packaged with cherry flavor (cherry flavor contains propylene glycol and sodium benzoate)]
Tablet:
Requa® Activated Charcoal: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS: 250 mg
DOSAGE FORMS: CONCISE
Capsule:
Char-Caps [OTC], CharcoCaps® [OTC]: 260 mg
Pellets, for suspension:
EZ-Char™ [OTC]: 25 g
Powder for suspension: 30 g, 240 g
CharcoAid® G [OTC]: 15 g
Suspension:
Actidose-Aqua® [OTC]: 15 g, 25 g, 50 g
Kerr Insta-Char® [OTC]: 25 g, 50 g
Suspension [with sorbitol]:
Actidose® with Sorbitol [OTC], Kerr Insta-Char® [OTC]: 25 g, 50 g
Tablet:
Requa® Activated Charcoal [OTC]: 250 mg
Tablet, enteric coated:
Charcoal Plus® DS [OTC]: 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Powder
ADMINISTRATION — Flavoring agents (eg, chocolate, concentrated fruit juice) or thickening agents (eg, bentonite, carboxymethylcellulose) can enhance charcoal's palatability. If treatment includes ipecac syrup, induce vomiting prior to administration of charcoal. Often given with a laxative or cathartic; check for presence of bowel sounds before administration. I.V. antiemetics may be required to reduce the risk of vomiting during multiple-dose therapy with charcoal.
USE — Emergency treatment in poisoning by drugs and chemicals; aids the elimination of certain drugs and improves decontamination of excessive ingestions of sustained-release products or in the presence of bezoars; repetitive doses have proven useful to enhance the elimination of certain drugs (eg, carbamazepine, dapsone, phenobarbital, quinine, or theophylline); repetitive doses for gastric dialysis in uremia to adsorb various waste products; dietary supplement (digestive aid)
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Endocrine & metabolic: Hypernatremia, hypokalemia, and hypermagnesemia may occur with coadministration of cathartics
Gastrointestinal: Vomiting (incidence may increase with sorbitol), diarrhea (with sorbitol), constipation, swelling of abdomen, bowel obstruction, appendicitis
Respiratory: Aspiration (both gastric contents and charcoal)
Miscellaneous: Fecal discoloration (black)
CONTRAINDICATIONS — Hypersensitivity to charcoal or any component of the formulation; intestinal obstruction; GI tract not anatomically intact; patients at risk of hemorrhage or GI perforation; patients with an unprotected airway (eg, CNS depression without intubation); if use would increase risk and severity of aspiration
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Vomiting: Charcoal may cause vomiting; avoid use in hydrocarbon and caustic ingestions.
Disease-related concerns: Decreased peristalsis: Use with caution in patients with decreased peristalsis.
Concurrent drug therapy issues: Ipecac: When using ipecac with charcoal, ensure ipecac-induced vomiting has ceased prior to administering charcoal. Cathartics (eg, sorbitol, mannitol, magnesium sulfate): Coadministration of a cathartic is not recommended secondary to lack of compelling evidence and the increased morbidity associated with their use. If charcoal is administered with a cathartic, avoid excessive fluid and electrolyte losses, especially in children <1 year of age.
Special populations: Pediatrics: Charcoal with sorbitol not recommended in children <1 year of age.
Dosage form specific issues: Propylene glycol: Commercial charcoal products may contain propylene glycol.
Other warnings/precautions: Appropriate use: Not effective for cyanide, mineral acids, caustic alkalis, organic solvents, iron, ethanol, methanol, or lithium poisoning Efficacy: Most effective when administered within 30-60 minutes of ingestion.
DRUG INTERACTIONS
Leflunomide: Charcoal, Activated may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to charcoal when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Do not mix with milk, ice cream, sherbet, or marmalade (may reduce charcoal's effectiveness).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Does not enter breast milk/compatible
CANADIAN BRAND NAMES — Charcadole®; Charcadole® TFS; Charcadole®, Aqueous
INTERNATIONAL BRAND NAMES — Bekarbon (ID); Ca-R-Bon (TH); Carbo Medicinalis (PL); Carbomix (FR, SE); Carbon Natural (UY); Carbosorb (NZ); Carbosorb S (NZ); Carbosorb X (AU); Carbosorb XS (AU); Carbotural (MX); Charcodote (GB, HK, KP); Charcotrace (AU); Deltacarbon (TH); Mamograf (AR); Norit (IL); RCOL (IN); Ultracarbon (SG)
MECHANISM OF ACTION — Adsorbs toxic substances or irritants, thus inhibiting GI absorption; adsorbs intestinal gas; the addition of sorbitol results in hyperosmotic laxative action causing catharsis
PHARMACODYNAMICS / KINETICS — Excretion: Feces (as charcoal)
PATIENT INFORMATION — Charcoal causes the stools to turn black. Do not use prior to calling a poison control center or a prescriber
Acrivastine and pseudoephedrine
U.S. BRAND NAMES — Semprex®-D
PHARMACOLOGIC CATEGORY
Alpha/Beta Agonist
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT
>10%: Central nervous system: Drowsiness, headache
1% to 10%:
Cardiovascular: Tachycardia, palpitation
Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue
Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea
Genitourinary: Dysuria
Neuromuscular & skeletal: Weakness
Respiratory: Pharyngitis, cough increased
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr ≤ 48 mL/minute)
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease); contraindicated with severe disease. Diabetes: Use with caution in patients with diabetes mellitus. Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or glaucoma. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer). Renal impairment: Use with caution in patients with renal impairment; contraindicated if Clcr ≤ 48 mL/minute. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Pediatrics: Safety and efficacy have not been established in children <12 years of age.
DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Antacids: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Aluminum Hydroxide. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
Bromocriptine: Alpha-/Beta-Agonists may enhance the adverse/toxic effect of Bromocriptine. Including increased blood pressure, ventricular arrhythmias, and seizure. Risk C: Monitor therapy
Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Carbonic Anhydrase Inhibitors: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Brinzolamide; Dorzolamide. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
MAO Inhibitors: May enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Risk D: Consider therapy modification
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)
Capsules (Semprex-D)
8-60 mg (30): $62.39
INTERNATIONAL BRAND NAMES — Duact (DK, FI)
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS
Pseudoephedrine: See Pseudoephedrine.
Acrivastine:
Metabolism: Minimally hepatic
Time to peak: ~1.1 hours
Excretion: Urine (84%); feces (13%)
PHARMACOLOGIC CATEGORY
Alpha/Beta Agonist
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation
DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Do not use.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg
DOSAGE FORMS: CONCISE
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies
ADVERSE REACTIONS SIGNIFICANT
>10%: Central nervous system: Drowsiness, headache
1% to 10%:
Cardiovascular: Tachycardia, palpitation
Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue
Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea
Genitourinary: Dysuria
Neuromuscular & skeletal: Weakness
Respiratory: Pharyngitis, cough increased
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr ≤ 48 mL/minute)
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease); contraindicated with severe disease. Diabetes: Use with caution in patients with diabetes mellitus. Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or glaucoma. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer). Renal impairment: Use with caution in patients with renal impairment; contraindicated if Clcr ≤ 48 mL/minute. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Pediatrics: Safety and efficacy have not been established in children <12 years of age.
DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Antacids: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Aluminum Hydroxide. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
Bromocriptine: Alpha-/Beta-Agonists may enhance the adverse/toxic effect of Bromocriptine. Including increased blood pressure, ventricular arrhythmias, and seizure. Risk C: Monitor therapy
Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Carbonic Anhydrase Inhibitors: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Brinzolamide; Dorzolamide. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
MAO Inhibitors: May enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Risk D: Consider therapy modification
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)
PREGNANCY RISK FACTOR — B (show table)
LACTATION — Enters breast milk/contraindicated
PRICING — (data from drugstore.com)
Capsules (Semprex-D)
8-60 mg (30): $62.39
INTERNATIONAL BRAND NAMES — Duact (DK, FI)
MECHANISM OF ACTION — Refer to Pseudoephedrine; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells
PHARMACODYNAMICS / KINETICS
Pseudoephedrine: See Pseudoephedrine.
Acrivastine:
Metabolism: Minimally hepatic
Time to peak: ~1.1 hours
Excretion: Urine (84%); feces (13%)
Acitretin
U.S. BRAND NAMES — Soriatane® CK Convenience Kit™
PHARMACOLOGIC CATEGORY
Retinoid-Like Compound
DOSING: ADULTS
Psoriasis: Oral: Individualization of dosage is required to achieve maximum therapeutic response while minimizing side effects
Initial therapy: Therapy should be initiated at 25-50 mg/day, given as a single dose with the main meal
Maintenance: Doses of 25-50 mg/day may be given after initial response to treatment; the maintenance dose should be based on clinical efficacy and tolerability
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Soriatane® CK Convenience Kit™ : 10 mg, 25 mg [packaged with VersaFoam-EF™ ]
DOSAGE FORMS: CONCISE
Capsule:
Soriatane® CK Convenience Kit™ : 10 mg, 25 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of severe psoriasis
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Hyperesthesia (10% to 25%)
Dermatologic: Cheilitis (>75%), alopecia (50% to 75%), skin peeling (50% to 75%), dry skin (25% to 50%), nail disorder (25% to 50%), pruritus (25% to 50%), erythematous rash (10% to 25%), skin atrophy (10% to 25%), sticky skin (10% to 25%), paronychia (10% to 25%)
Endocrine & metabolic: Hypercholesterolemia (25% to 50%), hypertriglyceridemia (50% to 75%), HDL decreased (25% to 50%), phosphorus increased (10% to 25%), potassium increased (10% to 25%), sodium increased (10% to 25%), magnesium increased/decreased (10% to 25%), fasting blood sugar increased (25% to 50%), fasting blood sugar decreased (10% to 25%)
Gastrointestinal: Xerostomia (10% to 25%)
Hematologic: Reticulocytes increased (25% to 50%), hematocrit decreased (10% to 25%), hemoglobin decreased (10% to 25%), WBC increased/decreased (10% to 25%), haptoglobin increased (10% to 25%), neutrophils increased (10% to 25%)
Hepatic: Liver function tests increased (25% to 50%), alkaline phosphatase increased (10% to 25%), direct bilirubin increased (10% to 25%), GGTP increased (10% to 25%)
Neuromuscular & skeletal: Paresthesia (10% to 25%), arthralgia (10% to 25%), rigors (10% to 25%), CPK increased (25% to 50%), spinal hyperostosis progression (10% to 25%)
Ocular: Xerophthalmia (10% to 25%),
Renal: Uric acid increased (10% to 25%), acetonuria (10% to 25%), hematuria (10% to 25%), RBC in urine (10% to 25%)
Respiratory: Rhinitis (25% to 50%), epistaxis (10% to 25%)
1% to 10%:
Cardiovascular: Flushing, edema
Central nervous system: Headache, pain, depression, insomnia, somnolence, fatigue
Dermatologic: Skin odor, hair texture change, bullous eruption, dermatitis, diaphoresis increased, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, ulcers, fissures, sunburn
Endocrine & metabolic: Hot flashes, potassium decreased, phosphorus decreased, sodium decreased, calcium increased or decreased, chloride increased or decreased
Gastrointestinal: Gingival bleeding, gingivitis, saliva increased, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, taste disturbance, anorexia, appetite increased, tongue disorder
Hepatic: Total bilirubin increased
Neuromuscular & skeletal: Arthritis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis, Bell's palsy
Ocular: Blurred vision, blepharitis, conjunctivitis, night blindness, photophobia, corneal epithelial abnormality, eye pain, eyebrow or eyelash loss, diplopia, cataract
Otic: Earache, tinnitus
Renal: BUN increased, creatinine increased, glycosuria, proteinuria
Respiratory: Sinusitis
<1% (Limited to important or life-threatening): Anxiety, bleeding time increased, chest pain, cirrhosis, conjunctival hemorrhage, constipation, corneal ulceration, cyanosis, deafness, diplopia, dizziness, dyspepsia, dysphonia, dysuria, eczema, esophagitis, fever, furunculosis, gastritis, glossitis, gum hyperplasia, hair discoloration, healing impaired, hemorrhage, hepatic dysfunction, hepatitis, hyperkeratosis, hypertrichosis, hypoesthesia, intermittent claudication, itchy eyes, jaundice, leukorrhea, malaise, melena, MI, moniliasis, myopathy, nervousness, neuritis, pancreatitis, papilledema, peripheral ischemia, photosensitivity, pseudotumor cerebri, scleroderma, skin fragility or thinning, spinal hyperostosis (new lesion), stroke, taste loss, tendonitis, thromboembolism
CONTRAINDICATIONS — Hypersensitivity to acitretin, other retinoids, or any component of the formulation; patients who are pregnant or intend on becoming pregnant; ethanol ingestion; severe hepatic or renal dysfunction; chronically-elevated blood lipid levels; concomitant use with methotrexate or tetracyclines
Acitretin is contraindicated in females of childbearing potential unless all of the following conditions apply.
1) Patient has severe psoriasis unresponsive to other therapy or if clinical condition contraindicates other treatments.
2) Patient must have two negative urine or serum pregnancy tests prior to therapy.
3) Patient must have pregnancy test repeated monthly during therapy. After discontinuation of therapy, a pregnancy test must be repeated every 3 months for at least 3 years.
4) Patient must commit to using two effective forms of birth control starting 1 month prior to acitretin treatment and for 3 years after discontinuation. Prescriber must counsel patient about contraception every month during therapy and every 3 months following discontinuation for at least 3 years.
5) Patient is reliable in understanding and carrying out instructions.
6) Patient has received, and acknowledged, understanding of a careful oral and printed explanation of the hazards of fetal exposure to acitretin and the risk of possible contraception failure; this explanation may include showing a line drawing to the patient of an infant with the characteristic external deformities resulting from retinoid exposure during pregnancy. Patient must sign an agreement/informed consent document stating that she understands these risks and that she should not consume ethanol during therapy or for 2 months after discontinuation.
7) All patients (male and female) should not donate blood during and for 3 years following treatment with acitretin.
WARNINGS / PRECAUTIONS
Boxed warnings: Blood donation: See "Other warnings/precautions" below. Ethanol use: See "Concurrent drug therapy issues" below. Hepatotoxicity: See "Concerns related to adverse effects" below. Medication guide: See "Other warnings/precautions" below. Pregnancy/Do Your P.A.R.T. program: See "Special populations" below.
Concerns related to adverse effects: Depression: Depression, including thoughts of self-harm have been reported; use with caution in patients with a history of mental illness. Hepatotoxicity: [U.S. Boxed Warning]: Changes in transaminases occur in up to1/3of patients. Monitor for hepatotoxicity; discontinue if significant elevations of liver enzymes occur. Use with caution in patients at risk of hypertriglyceridemias. Hyperostosis: Patients receiving long-term treatment should be periodically examined for bony abnormalities; if occur risk vs. benefit of therapy should be considered. Lipid effects: Lipid changes including, increased triglycerides, increased cholesterol, and decreased HDL are common (up to 66%); increased triglycerides may lead to pancreatitis. Photosensitivity: May be photosensitizing; minimize sun or other UV exposure to treated areas. Pseudotumor cerebri: Rarely associated with pseudotumor cerebri. Visual disturbances: May cause a decrease in night vision or decreased tolerance to contact lenses; discontinue if visual changes occur.
Concurrent drug therapy issues: Ethanol use: [U.S. Boxed Warning]: All patients (male and female) should abstain from ethanol or ethanol-containing products during therapy and for 2 months after discontinuation. Tetracyclines: Pseudotumor cerebri (benign intracranial hypertension) has been reported with use of tetracyclines and acitretin independently; concomitant use is contraindicated.
Special populations: Pediatrics: Safety and efficacy have not been established in children; growth potential may be affected. Pregnancy/Do Your P.A.R.T. program: [U.S. Boxed Warning]: Not for use by women who are pregnant or want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. The Do Your P.A.R.T. (Pregnancy Prevention Actively Required During and After Treatment) program explains teratogenic risks and requirements expected of females of childbearing potential to prevent pregnancies from occurring during use and 3 years following discontinuation; this should be used to educate patients and healthcare providers.
Other warnings/precautions: Blood donation: [U.S. Boxed Warning]: All patients should be advised not to donate blood during therapy or for 3 years following completion of therapy. Medication guide: [U.S. Boxed Warning]: All patients must be provided with a medication guide each time acitretin is dispensed. Female patients must also sign an informed consent prior to therapy.
DRUG INTERACTIONS
Alcohol (Ethyl): May enhance the teratogenic effect of Acitretin. Risk X: Avoid combination
Contraceptive (Progestins): Acitretin may diminish the therapeutic effect of Contraceptive (Progestins). Contraceptive failure is possible. Risk X: Avoid combination
Methotrexate: Acitretin may enhance the hepatotoxic effect of Methotrexate. Risk X: Avoid combination
Oral Contraceptive (Estrogens): Retinoic Acid Derivatives may diminish the therapeutic effect of Oral Contraceptive (Estrogens). Two forms of contraception are recommended in females of child-bearing potential during retinoic acid derivative therapy. Risk C: Monitor therapy
Oral Contraceptive (Progestins): Retinoic Acid Derivatives may diminish the therapeutic effect of Oral Contraceptive (Progestins). Two forms of contraception are recommended in females of child-bearing potential during retinoic acid derivative therapy. Risk C: Monitor therapy
Tetracycline Derivatives: May enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Risk X: Avoid combination
Vitamin A: Retinoic Acid Derivatives may enhance the adverse/toxic effect of Vitamin A. Risk X: Avoid combination
Vitamin A: May enhance the adverse/toxic effect of Retinoid-like Compounds. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Use leads to formation of etretinate, a teratogenic metabolite with a prolonged half-life; concomitant use of ethanol or ethanol-containing products is contraindicated.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Acitretin is teratogenic in humans. Severe birth defects have been reported when conception occurred during treatment or after therapy was complete. [U.S. Boxed Warning]: Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. In addition, because ethanol forms a teratogenic metabolite and would increase the duration of teratogenic potential, ethanol should not be consumed during treatment or for 2 months after discontinuation. Limited amounts of acitretin are found in seminal fluid; although it appears this poses little risk to a fetus, the actual risk of teratogenicity is not known. Any pregnancy which occurs during treatment, or within 3 years after treatment is discontinued, should be reported to the manufacturer at 1-888-500-3376 or to the FDA at 1-800-FDA-1088.
LACTATION — Enters breast milk/not recommended
BREAST-FEEDING CONSIDERATIONS — Acitretin should not be given prior to or during nursing due to the potential for adverse effects in the nursing infant.
DIETARY CONSIDERATIONS — Administer with food. Avoid ingestion of additional sources of exogenous vitamin A (in excess of RDA); use of ethanol and ethanol-containing products is contraindicated.
MONITORING PARAMETERS — Lipid profile (baseline and at 1- to 2-week intervals for 4-8 weeks); liver function tests (baseline, and at 1- to 2-week intervals until stable, then as clinically indicated); blood glucose in patients with diabetes; bone abnormalities (with long-term use)
CANADIAN BRAND NAMES — Soriatane®
INTERNATIONAL BRAND NAMES — Acetec (IN); Neo-Tigason (TH); Neotigason (AR, AT, AU, BB, BE, BF, BG, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CZ, DE, DK, EC, EE, EG, ET, FI, GB, GH, GM, GN, GR, GY, HN, IE, IL, IT, JM, KE, KP, LR, MA, ML, MR, MU, MW, MX, NE, NG, NL, NO, PE, PH, PL, PT, PY, SC, SD, SE, SL, SN, SR, TN, TT, TW, TZ, UG, UY, VE, ZA, ZM, ZW); Soriatane (FR)
PHARMACODYNAMICS / KINETICS — Etretinate has been detected in serum for up to 3 years following therapy, possibly due to storage in adipose tissue.
Onset of action: May take 2-3 months for full effect; improvement may be seen within 8 weeks.
Absorption: Oral: ~72% absorbed when given with food
Protein binding: >99% bound, primarily to albumin
Metabolism: Metabolized to cis-acitretin; both compounds are further metabolized. Concomitant ethanol use leads to the formation of etretinate (active).
Half-life elimination: Acitretin: 49 hours (range: 33-96); cis-acitretin: 63 hours (range: 28-157); etretinate: 120 days (range: 84-168 days)
Excretion: Feces (34% to 54%); urine (16% to 53%)
PATIENT INFORMATION — Take with food. Do not drink alcohol during therapy and for 2 months after discontinuation. Use contraception for 1 month before, during, and for 3 years after discontinuation. You may not be able to tolerate contact lenses during treatment. Do not donate blood during treatment and for 3 years after discontinuation (male and female patients). Avoid exposure to sunlight. Wear protective clothing and sunscreens. Avoid use of other vitamin A products. Females: Use two effective forms of birth control. If you have had your tubes tied, then use an additional form of birth control. If you become pregnant, contact your prescriber immediately.
PHARMACOLOGIC CATEGORY
Retinoid-Like Compound
DOSING: ADULTS
Psoriasis: Oral: Individualization of dosage is required to achieve maximum therapeutic response while minimizing side effects
Initial therapy: Therapy should be initiated at 25-50 mg/day, given as a single dose with the main meal
Maintenance: Doses of 25-50 mg/day may be given after initial response to treatment; the maintenance dose should be based on clinical efficacy and tolerability
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule:
Soriatane® CK Convenience Kit™ : 10 mg, 25 mg [packaged with VersaFoam-EF™ ]
DOSAGE FORMS: CONCISE
Capsule:
Soriatane® CK Convenience Kit™ : 10 mg, 25 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of severe psoriasis
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Hyperesthesia (10% to 25%)
Dermatologic: Cheilitis (>75%), alopecia (50% to 75%), skin peeling (50% to 75%), dry skin (25% to 50%), nail disorder (25% to 50%), pruritus (25% to 50%), erythematous rash (10% to 25%), skin atrophy (10% to 25%), sticky skin (10% to 25%), paronychia (10% to 25%)
Endocrine & metabolic: Hypercholesterolemia (25% to 50%), hypertriglyceridemia (50% to 75%), HDL decreased (25% to 50%), phosphorus increased (10% to 25%), potassium increased (10% to 25%), sodium increased (10% to 25%), magnesium increased/decreased (10% to 25%), fasting blood sugar increased (25% to 50%), fasting blood sugar decreased (10% to 25%)
Gastrointestinal: Xerostomia (10% to 25%)
Hematologic: Reticulocytes increased (25% to 50%), hematocrit decreased (10% to 25%), hemoglobin decreased (10% to 25%), WBC increased/decreased (10% to 25%), haptoglobin increased (10% to 25%), neutrophils increased (10% to 25%)
Hepatic: Liver function tests increased (25% to 50%), alkaline phosphatase increased (10% to 25%), direct bilirubin increased (10% to 25%), GGTP increased (10% to 25%)
Neuromuscular & skeletal: Paresthesia (10% to 25%), arthralgia (10% to 25%), rigors (10% to 25%), CPK increased (25% to 50%), spinal hyperostosis progression (10% to 25%)
Ocular: Xerophthalmia (10% to 25%),
Renal: Uric acid increased (10% to 25%), acetonuria (10% to 25%), hematuria (10% to 25%), RBC in urine (10% to 25%)
Respiratory: Rhinitis (25% to 50%), epistaxis (10% to 25%)
1% to 10%:
Cardiovascular: Flushing, edema
Central nervous system: Headache, pain, depression, insomnia, somnolence, fatigue
Dermatologic: Skin odor, hair texture change, bullous eruption, dermatitis, diaphoresis increased, psoriasiform rash, purpura, pyogenic granuloma, rash, seborrhea, ulcers, fissures, sunburn
Endocrine & metabolic: Hot flashes, potassium decreased, phosphorus decreased, sodium decreased, calcium increased or decreased, chloride increased or decreased
Gastrointestinal: Gingival bleeding, gingivitis, saliva increased, stomatitis, thirst, ulcerative stomatitis, abdominal pain, diarrhea, nausea, taste disturbance, anorexia, appetite increased, tongue disorder
Hepatic: Total bilirubin increased
Neuromuscular & skeletal: Arthritis, back pain, hypertonia, myalgia, osteodynia, peripheral joint hyperostosis, Bell's palsy
Ocular: Blurred vision, blepharitis, conjunctivitis, night blindness, photophobia, corneal epithelial abnormality, eye pain, eyebrow or eyelash loss, diplopia, cataract
Otic: Earache, tinnitus
Renal: BUN increased, creatinine increased, glycosuria, proteinuria
Respiratory: Sinusitis
<1% (Limited to important or life-threatening): Anxiety, bleeding time increased, chest pain, cirrhosis, conjunctival hemorrhage, constipation, corneal ulceration, cyanosis, deafness, diplopia, dizziness, dyspepsia, dysphonia, dysuria, eczema, esophagitis, fever, furunculosis, gastritis, glossitis, gum hyperplasia, hair discoloration, healing impaired, hemorrhage, hepatic dysfunction, hepatitis, hyperkeratosis, hypertrichosis, hypoesthesia, intermittent claudication, itchy eyes, jaundice, leukorrhea, malaise, melena, MI, moniliasis, myopathy, nervousness, neuritis, pancreatitis, papilledema, peripheral ischemia, photosensitivity, pseudotumor cerebri, scleroderma, skin fragility or thinning, spinal hyperostosis (new lesion), stroke, taste loss, tendonitis, thromboembolism
CONTRAINDICATIONS — Hypersensitivity to acitretin, other retinoids, or any component of the formulation; patients who are pregnant or intend on becoming pregnant; ethanol ingestion; severe hepatic or renal dysfunction; chronically-elevated blood lipid levels; concomitant use with methotrexate or tetracyclines
Acitretin is contraindicated in females of childbearing potential unless all of the following conditions apply.
1) Patient has severe psoriasis unresponsive to other therapy or if clinical condition contraindicates other treatments.
2) Patient must have two negative urine or serum pregnancy tests prior to therapy.
3) Patient must have pregnancy test repeated monthly during therapy. After discontinuation of therapy, a pregnancy test must be repeated every 3 months for at least 3 years.
4) Patient must commit to using two effective forms of birth control starting 1 month prior to acitretin treatment and for 3 years after discontinuation. Prescriber must counsel patient about contraception every month during therapy and every 3 months following discontinuation for at least 3 years.
5) Patient is reliable in understanding and carrying out instructions.
6) Patient has received, and acknowledged, understanding of a careful oral and printed explanation of the hazards of fetal exposure to acitretin and the risk of possible contraception failure; this explanation may include showing a line drawing to the patient of an infant with the characteristic external deformities resulting from retinoid exposure during pregnancy. Patient must sign an agreement/informed consent document stating that she understands these risks and that she should not consume ethanol during therapy or for 2 months after discontinuation.
7) All patients (male and female) should not donate blood during and for 3 years following treatment with acitretin.
WARNINGS / PRECAUTIONS
Boxed warnings: Blood donation: See "Other warnings/precautions" below. Ethanol use: See "Concurrent drug therapy issues" below. Hepatotoxicity: See "Concerns related to adverse effects" below. Medication guide: See "Other warnings/precautions" below. Pregnancy/Do Your P.A.R.T. program: See "Special populations" below.
Concerns related to adverse effects: Depression: Depression, including thoughts of self-harm have been reported; use with caution in patients with a history of mental illness. Hepatotoxicity: [U.S. Boxed Warning]: Changes in transaminases occur in up to1/3of patients. Monitor for hepatotoxicity; discontinue if significant elevations of liver enzymes occur. Use with caution in patients at risk of hypertriglyceridemias. Hyperostosis: Patients receiving long-term treatment should be periodically examined for bony abnormalities; if occur risk vs. benefit of therapy should be considered. Lipid effects: Lipid changes including, increased triglycerides, increased cholesterol, and decreased HDL are common (up to 66%); increased triglycerides may lead to pancreatitis. Photosensitivity: May be photosensitizing; minimize sun or other UV exposure to treated areas. Pseudotumor cerebri: Rarely associated with pseudotumor cerebri. Visual disturbances: May cause a decrease in night vision or decreased tolerance to contact lenses; discontinue if visual changes occur.
Concurrent drug therapy issues: Ethanol use: [U.S. Boxed Warning]: All patients (male and female) should abstain from ethanol or ethanol-containing products during therapy and for 2 months after discontinuation. Tetracyclines: Pseudotumor cerebri (benign intracranial hypertension) has been reported with use of tetracyclines and acitretin independently; concomitant use is contraindicated.
Special populations: Pediatrics: Safety and efficacy have not been established in children; growth potential may be affected. Pregnancy/Do Your P.A.R.T. program: [U.S. Boxed Warning]: Not for use by women who are pregnant or want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. The Do Your P.A.R.T. (Pregnancy Prevention Actively Required During and After Treatment) program explains teratogenic risks and requirements expected of females of childbearing potential to prevent pregnancies from occurring during use and 3 years following discontinuation; this should be used to educate patients and healthcare providers.
Other warnings/precautions: Blood donation: [U.S. Boxed Warning]: All patients should be advised not to donate blood during therapy or for 3 years following completion of therapy. Medication guide: [U.S. Boxed Warning]: All patients must be provided with a medication guide each time acitretin is dispensed. Female patients must also sign an informed consent prior to therapy.
DRUG INTERACTIONS
Alcohol (Ethyl): May enhance the teratogenic effect of Acitretin. Risk X: Avoid combination
Contraceptive (Progestins): Acitretin may diminish the therapeutic effect of Contraceptive (Progestins). Contraceptive failure is possible. Risk X: Avoid combination
Methotrexate: Acitretin may enhance the hepatotoxic effect of Methotrexate. Risk X: Avoid combination
Oral Contraceptive (Estrogens): Retinoic Acid Derivatives may diminish the therapeutic effect of Oral Contraceptive (Estrogens). Two forms of contraception are recommended in females of child-bearing potential during retinoic acid derivative therapy. Risk C: Monitor therapy
Oral Contraceptive (Progestins): Retinoic Acid Derivatives may diminish the therapeutic effect of Oral Contraceptive (Progestins). Two forms of contraception are recommended in females of child-bearing potential during retinoic acid derivative therapy. Risk C: Monitor therapy
Tetracycline Derivatives: May enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Risk X: Avoid combination
Vitamin A: Retinoic Acid Derivatives may enhance the adverse/toxic effect of Vitamin A. Risk X: Avoid combination
Vitamin A: May enhance the adverse/toxic effect of Retinoid-like Compounds. Risk D: Consider therapy modification
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Use leads to formation of etretinate, a teratogenic metabolite with a prolonged half-life; concomitant use of ethanol or ethanol-containing products is contraindicated.
PREGNANCY RISK FACTOR — X (show table)
PREGNANCY IMPLICATIONS — Acitretin is teratogenic in humans. Severe birth defects have been reported when conception occurred during treatment or after therapy was complete. [U.S. Boxed Warning]: Not for use by women who want to become pregnant; patient should not get pregnant for at least 3 years after discontinuation. In addition, because ethanol forms a teratogenic metabolite and would increase the duration of teratogenic potential, ethanol should not be consumed during treatment or for 2 months after discontinuation. Limited amounts of acitretin are found in seminal fluid; although it appears this poses little risk to a fetus, the actual risk of teratogenicity is not known. Any pregnancy which occurs during treatment, or within 3 years after treatment is discontinued, should be reported to the manufacturer at 1-888-500-3376 or to the FDA at 1-800-FDA-1088.
LACTATION — Enters breast milk/not recommended
BREAST-FEEDING CONSIDERATIONS — Acitretin should not be given prior to or during nursing due to the potential for adverse effects in the nursing infant.
DIETARY CONSIDERATIONS — Administer with food. Avoid ingestion of additional sources of exogenous vitamin A (in excess of RDA); use of ethanol and ethanol-containing products is contraindicated.
MONITORING PARAMETERS — Lipid profile (baseline and at 1- to 2-week intervals for 4-8 weeks); liver function tests (baseline, and at 1- to 2-week intervals until stable, then as clinically indicated); blood glucose in patients with diabetes; bone abnormalities (with long-term use)
CANADIAN BRAND NAMES — Soriatane®
INTERNATIONAL BRAND NAMES — Acetec (IN); Neo-Tigason (TH); Neotigason (AR, AT, AU, BB, BE, BF, BG, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CZ, DE, DK, EC, EE, EG, ET, FI, GB, GH, GM, GN, GR, GY, HN, IE, IL, IT, JM, KE, KP, LR, MA, ML, MR, MU, MW, MX, NE, NG, NL, NO, PE, PH, PL, PT, PY, SC, SD, SE, SL, SN, SR, TN, TT, TW, TZ, UG, UY, VE, ZA, ZM, ZW); Soriatane (FR)
PHARMACODYNAMICS / KINETICS — Etretinate has been detected in serum for up to 3 years following therapy, possibly due to storage in adipose tissue.
Onset of action: May take 2-3 months for full effect; improvement may be seen within 8 weeks.
Absorption: Oral: ~72% absorbed when given with food
Protein binding: >99% bound, primarily to albumin
Metabolism: Metabolized to cis-acitretin; both compounds are further metabolized. Concomitant ethanol use leads to the formation of etretinate (active).
Half-life elimination: Acitretin: 49 hours (range: 33-96); cis-acitretin: 63 hours (range: 28-157); etretinate: 120 days (range: 84-168 days)
Excretion: Feces (34% to 54%); urine (16% to 53%)
PATIENT INFORMATION — Take with food. Do not drink alcohol during therapy and for 2 months after discontinuation. Use contraception for 1 month before, during, and for 3 years after discontinuation. You may not be able to tolerate contact lenses during treatment. Do not donate blood during treatment and for 3 years after discontinuation (male and female patients). Avoid exposure to sunlight. Wear protective clothing and sunscreens. Avoid use of other vitamin A products. Females: Use two effective forms of birth control. If you have had your tubes tied, then use an additional form of birth control. If you become pregnant, contact your prescriber immediately.
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