U.S. BRAND NAMES — VoSol® [DSC]
PHARMACOLOGIC CATEGORY Otic Agent, Anti-infectiveTopical Skin Product
DOSING: ADULTS Irrigation (Note: Dosage of an irrigating solution depends on the capacity or surface area of the structure being irrigated): For continuous irrigation of the urinary bladder with 0.25% acetic acid irrigation, the rate of administration will approximate the rate of urine flow; usually 500-1500 mL/24 hours For periodic irrigation of an indwelling urinary catheter to maintain patency, about 50 mL of 0.25% acetic acid irrigation is required
Otitis externa: Otic: Insert saturated wick; keep moist 24 hours; remove wick and instill 5 drops 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic (VoSol® [DSC]): 2% (15 mL)
DOSAGE FORMS: CONCISE Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic: 2% (15 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Not for internal intake or I.V. infusion; topical use or irrigation use only.
USE — Irrigation of the bladder; treatment of superficial bacterial infections of the external auditory canal
ADVERSE REACTIONS SIGNIFICANT — <1% (Limited to important or life-threatening): Hematuria, systemic acidosis, urologic pain
CONTRAINDICATIONS — Hypersensitivity to acetic acid or any component of the formulation; during transurethral procedures
WARNINGS / PRECAUTIONS — Not for internal intake or I.V. infusion; topical use or irrigation use only. Use of irrigation in patients with mucosal lesions of urinary bladder may cause irritation. Systemic acidosis may result from absorption.
PREGNANCY RISK FACTOR — C (show table)
Sunday, January 20, 2008
Acetic acid
U.S. BRAND NAMES — VoSol® [DSC]
PHARMACOLOGIC CATEGORY Otic Agent, Anti-infectiveTopical Skin Product
DOSING: ADULTS Irrigation (Note: Dosage of an irrigating solution depends on the capacity or surface area of the structure being irrigated): For continuous irrigation of the urinary bladder with 0.25% acetic acid irrigation, the rate of administration will approximate the rate of urine flow; usually 500-1500 mL/24 hours For periodic irrigation of an indwelling urinary catheter to maintain patency, about 50 mL of 0.25% acetic acid irrigation is required
Otitis externa: Otic: Insert saturated wick; keep moist 24 hours; remove wick and instill 5 drops 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic (VoSol® [DSC]): 2% (15 mL)
DOSAGE FORMS: CONCISE Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic: 2% (15 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Not for internal intake or I.V. infusion; topical use or irrigation use only.
USE — Irrigation of the bladder; treatment of superficial bacterial infections of the external auditory canal
ADVERSE REACTIONS SIGNIFICANT — <1% (Limited to important or life-threatening): Hematuria, systemic acidosis, urologic pain
CONTRAINDICATIONS — Hypersensitivity to acetic acid or any component of the formulation; during transurethral procedures
WARNINGS / PRECAUTIONS — Not for internal intake or I.V. infusion; topical use or irrigation use only. Use of irrigation in patients with mucosal lesions of urinary bladder may cause irritation. Systemic acidosis may result from absorption.
PREGNANCY RISK FACTOR — C (show table)
PHARMACOLOGIC CATEGORY Otic Agent, Anti-infectiveTopical Skin Product
DOSING: ADULTS Irrigation (Note: Dosage of an irrigating solution depends on the capacity or surface area of the structure being irrigated): For continuous irrigation of the urinary bladder with 0.25% acetic acid irrigation, the rate of administration will approximate the rate of urine flow; usually 500-1500 mL/24 hours For periodic irrigation of an indwelling urinary catheter to maintain patency, about 50 mL of 0.25% acetic acid irrigation is required
Otitis externa: Otic: Insert saturated wick; keep moist 24 hours; remove wick and instill 5 drops 3-4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic (VoSol® [DSC]): 2% (15 mL)
DOSAGE FORMS: CONCISE Solution for irrigation: 0.25% (250 mL, 500 mL, 1000 mL)
Solution, otic: 2% (15 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Not for internal intake or I.V. infusion; topical use or irrigation use only.
USE — Irrigation of the bladder; treatment of superficial bacterial infections of the external auditory canal
ADVERSE REACTIONS SIGNIFICANT — <1% (Limited to important or life-threatening): Hematuria, systemic acidosis, urologic pain
CONTRAINDICATIONS — Hypersensitivity to acetic acid or any component of the formulation; during transurethral procedures
WARNINGS / PRECAUTIONS — Not for internal intake or I.V. infusion; topical use or irrigation use only. Use of irrigation in patients with mucosal lesions of urinary bladder may cause irritation. Systemic acidosis may result from absorption.
PREGNANCY RISK FACTOR — C (show table)
Acetazolamide
U.S. BRAND NAMES — Diamox® Sequels®
PHARMACOLOGIC CATEGORY Anticonvulsant, MiscellaneousCarbonic Anhydrase InhibitorDiuretic, Carbonic Anhydrase InhibitorOphthalmic Agent, Antiglaucoma
DOSING: ADULTS — Note: I.M. administration is not recommended.
Glaucoma: Chronic simple (open-angle): Oral: 250 mg 1-4 times/day or 500 mg extended release capsule twice daily Secondary, acute (closed-angle): I.V.: 250-500 mg, may repeat in 2-4 hours to a maximum of 1 g/day
Edema: Oral, I.V.: 250-375 mg once daily
Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses, not to exceed 1 g/day. Note: Extended release capsule is not recommended for treatment of epilepsy.
Metabolic alkalosis (unlabeled use): I.V. 250 mg every 6 hours for 4 doses or 500 mg single dose; reassess need based upon acid-base status
Mountain sickness: Oral: 250 mg every 8-12 hours (or 500 mg extended release capsules every 12-24 hours). Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude. Note: In situations of rapid ascent (such as rescue or military operations), 1000 mg/day is recommended.
Urine alkalinization (unlabeled use): Oral: 5 mg/kg/dose repeated 2-3 times over 24 hours
Respiratory stimulant in COPD (unlabeled use): Oral, I.V.: 250 mg twice daily
DOSING: PEDIATRIC — Note: I.M. administration is not recommended.
(For additional information see "Acetazolamide: Pediatric drug information")
Glaucoma: Oral: 8-30 mg/kg/day or 300-900 mg/m2/day divided every 8 hours I.V.: 20-40 mg/kg/24 hours divided every 6 hours, not to exceed 1 g/day
Edema: Oral, I.V.: 5 mg/kg or 150 mg/m2 once every day
Epilepsy: Oral: Refer to adult dosing.
DOSING: ELDERLY — Oral: Initial: 250 mg once or twice daily; use lowest effective dose possible.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 12 hours.
Clcr <10 mL/minute: Avoid use (ineffective).
Moderately dialyzable (20% to 50%)
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
DOSAGE FORMS: CONCISE Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Injection, tablet
ADMINISTRATION Oral: May cause an alteration in taste, especially carbonated beverages. Short-acting tablets may be crushed and suspended in cherry or chocolate syrup to disguise the bitter taste of the drug; do not use fruit juices. Alternatively, submerge tablet in 10 mL of hot water and add 10 mL honey or syrup.
I.M.: I.M. administration is painful because of the alkaline pH of the drug; use by this route is not recommended.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS.
Y-site administration: Variable (consult detailed reference): Diltiazem, TPN.
Compatibility when admixed: Compatible: Cimetidine, ranitidine. Incompatible: Multivitamins.
USE — Treatment of glaucoma (chronic simple open-angle, secondary glaucoma, preoperatively in acute angle-closure); drug-induced edema or edema due to congestive heart failure (adjunctive therapy); centrencephalic epilepsies (immediate release dosage form); prevention or amelioration of symptoms associated with acute mountain sickness
USE - UNLABELED / INVESTIGATIONAL — Urine alkalinization; respiratory stimulant in COPD; metabolic alkalosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Flushing
Central nervous system: Ataxia, confusion, convulsions, depression, dizziness, drowsiness, excitement, fatigue, fever, headache, malaise
Dermatologic: Allergic skin reactions, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Endocrine & metabolic: Electrolyte imbalance, growth retardation (children), hyperglycemia, hypoglycemia, hypokalemia, hyponatremia, metabolic acidosis
Gastrointestinal: Appetite decreased, diarrhea, melena, nausea, taste alteration, vomiting
Genitourinary: Crystalluria, glycosuria, hematuria, polyuria, renal failure
Hematologic: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura
Hepatic: Cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency, liver function tests abnormal
Local: Pain at injection site
Neuromuscular & skeletal: Flaccid paralysis, paresthesia
Ocular: Myopia
Otic: Hearing disturbance, tinnitus
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency, cirrhosis; hyperchloremic acidosis, severe renal disease or dysfunction; severe pulmonary obstruction; long-term use in noncongestive angle-closure glaucoma
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS effects: Impairment of mental alertness and/or physical coordination may occur. Sulfa allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonylurea allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Discontinue if signs of hypersensitivity are noted.
Disease-related concerns: Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control. Hepatic impairment: Use with caution in patients with hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy. Respiratory acidosis: Use with caution in patients with respiratory acidosis.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to side effects.
Other warnings/precautions: I.M. administration: Painful because of the alkaline pH of the drug; use by this route is not recommended.
DRUG INTERACTIONS — Inhibits CYP3A4 (weak)
Amphetamines: Urinary excretion of amphetamine may be decreased; magnitude and duration of effects may be enhanced.
Carbamazepine: May increase serum concentrations of carbamazepine.
Cyclosporine trough concentrations may be increased resulting in possible nephrotoxicity and neurotoxicity.
Flecainide: May decrease excretion of flecainide.
Lithium: Serum concentrations may be decreased by acetazolamide; monitor.
Memantine: May decrease excretion of memantine.
Methenamine: Urinary antiseptic effect may be prevented by acetazolamide.
Phenytoin: Serum concentrations of phenytoin may be increased; incidence of osteomalacia may be enhanced or increased in patients on chronic phenytoin therapy.
Primidone serum concentrations may be decreased; carbonic anhydrase inhibitors may enhance the adverse/toxic effects of primidone.
Quinidine: Urinary excretion of quinidine may be decreased and effects may be enhanced.
Salicylate use (high dose) may result in carbonic anhydrase inhibitor accumulation and toxicity including CNS depression and metabolic acidosis. Salicylate toxicity might also be enhanced.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies, however, there are no adequate and well-controlled studies in pregnant women.
LACTATION — Enters breast milk/not recommended (AAP rates "compatible")
DIETARY CONSIDERATIONS — May be taken with food to decrease GI upset. May have additive effects with other folic acid antagonists. Sodium content of 500 mg injection: 47.2 mg (2.05 mEq).
PRICING — (data from drugstore.com)Capsule, 12-hour (Diamox Sequels) 500 mg (60): $169.03
Tablets (AcetaZOLAMIDE) 125 mg (60): $8.98 250 mg (60): $18.99
MONITORING PARAMETERS — Intraocular pressure, potassium, serum bicarbonate; serum electrolytes, periodic CBC with differential; monitor growth in pediatric patients
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include low blood sugar, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma. Hypoglycemia should be managed with 50 mL I.V. dextrose 50% followed immediately with a continuous infusion of 10% dextrose in water (administer at a rate sufficient enough to approach a serum glucose level of 100 mg/dL). The use of corticosteroids to treat the hypoglycemia is controversial, however, the addition of 100 mg of hydrocortisone to the dextrose infusion may prove helpful. In certain instances, hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acetazolamide®; Diamox®
INTERNATIONAL BRAND NAMES — Acetadiazol (MX); Albox (JP); Apo-Acetazolamide (CA, MY); Azol (TW); Carbinib (PT); Cetamid (PH); Defiltran (DE); Dehydratin (BG); Diamox (AE, AR, AT, AU, BE, BH, BR, CA, CH, CN, CO, CY, DK, EC, EG, ES, FI, FR, GB, HR, ID, IE, IN, IQ, IR, IT, JO, JP, KW, LB, LY, MX, MY, NL, NO, NZ, OM, PH, PY, QA, RU, SA, SE, SG, SY, TH, VE, YE, ZA); Diamox Sustets (CO); Diluran (CZ); Diural (UY); Diuramid (DE, PL); Edemox (ES); Evamox (PK); Genephamide (PE); Glaucomed (CO); Glaupax (CH, DK, HR, IE, JP, NO, TH); Huma-Zolamide (HU); Ledamox (JP); Lediamox (PT); Renamid (HR); Stazol (PY); Uramox (IL)
MECHANISM OF ACTION — Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons
PHARMACODYNAMICS / KINETICS Onset of action: Capsule, extended release: 2 hours; I.V.: 2 minutes Peak effect: Capsule, extended release: 8-12 hours; I.V.: 15 minutes; Tablet: 2-4 hours
Duration: Inhibition of aqueous humor secretion: Capsule, extended release: 18-24 hours; I.V.: 4-5 hours; Tablet: 8-12 hours
Distribution: Erythrocytes, kidneys; blood-brain barrier and placenta; distributes into milk (~30% of plasma concentrations)
Excretion: Urine (70% to 100% as unchanged drug)
PATIENT INFORMATION — Report numbness or tingling of extremities. Do not crush, chew, or swallow contents of long-acting capsule; may be opened and sprinkled on soft food. Ability to perform tasks requiring mental alertness and/or physical coordination may be impaired. Take with food; drug may cause substantial increase in blood glucose in some diabetic patients.
(For additional information see "Acetazolamide: Patient drug information")
PHARMACOLOGIC CATEGORY Anticonvulsant, MiscellaneousCarbonic Anhydrase InhibitorDiuretic, Carbonic Anhydrase InhibitorOphthalmic Agent, Antiglaucoma
DOSING: ADULTS — Note: I.M. administration is not recommended.
Glaucoma: Chronic simple (open-angle): Oral: 250 mg 1-4 times/day or 500 mg extended release capsule twice daily Secondary, acute (closed-angle): I.V.: 250-500 mg, may repeat in 2-4 hours to a maximum of 1 g/day
Edema: Oral, I.V.: 250-375 mg once daily
Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses, not to exceed 1 g/day. Note: Extended release capsule is not recommended for treatment of epilepsy.
Metabolic alkalosis (unlabeled use): I.V. 250 mg every 6 hours for 4 doses or 500 mg single dose; reassess need based upon acid-base status
Mountain sickness: Oral: 250 mg every 8-12 hours (or 500 mg extended release capsules every 12-24 hours). Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude. Note: In situations of rapid ascent (such as rescue or military operations), 1000 mg/day is recommended.
Urine alkalinization (unlabeled use): Oral: 5 mg/kg/dose repeated 2-3 times over 24 hours
Respiratory stimulant in COPD (unlabeled use): Oral, I.V.: 250 mg twice daily
DOSING: PEDIATRIC — Note: I.M. administration is not recommended.
(For additional information see "Acetazolamide: Pediatric drug information")
Glaucoma: Oral: 8-30 mg/kg/day or 300-900 mg/m2/day divided every 8 hours I.V.: 20-40 mg/kg/24 hours divided every 6 hours, not to exceed 1 g/day
Edema: Oral, I.V.: 5 mg/kg or 150 mg/m2 once every day
Epilepsy: Oral: Refer to adult dosing.
DOSING: ELDERLY — Oral: Initial: 250 mg once or twice daily; use lowest effective dose possible.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 12 hours.
Clcr <10 mL/minute: Avoid use (ineffective).
Moderately dialyzable (20% to 50%)
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
DOSAGE FORMS: CONCISE Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Injection, tablet
ADMINISTRATION Oral: May cause an alteration in taste, especially carbonated beverages. Short-acting tablets may be crushed and suspended in cherry or chocolate syrup to disguise the bitter taste of the drug; do not use fruit juices. Alternatively, submerge tablet in 10 mL of hot water and add 10 mL honey or syrup.
I.M.: I.M. administration is painful because of the alkaline pH of the drug; use by this route is not recommended.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS.
Y-site administration: Variable (consult detailed reference): Diltiazem, TPN.
Compatibility when admixed: Compatible: Cimetidine, ranitidine. Incompatible: Multivitamins.
USE — Treatment of glaucoma (chronic simple open-angle, secondary glaucoma, preoperatively in acute angle-closure); drug-induced edema or edema due to congestive heart failure (adjunctive therapy); centrencephalic epilepsies (immediate release dosage form); prevention or amelioration of symptoms associated with acute mountain sickness
USE - UNLABELED / INVESTIGATIONAL — Urine alkalinization; respiratory stimulant in COPD; metabolic alkalosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Flushing
Central nervous system: Ataxia, confusion, convulsions, depression, dizziness, drowsiness, excitement, fatigue, fever, headache, malaise
Dermatologic: Allergic skin reactions, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Endocrine & metabolic: Electrolyte imbalance, growth retardation (children), hyperglycemia, hypoglycemia, hypokalemia, hyponatremia, metabolic acidosis
Gastrointestinal: Appetite decreased, diarrhea, melena, nausea, taste alteration, vomiting
Genitourinary: Crystalluria, glycosuria, hematuria, polyuria, renal failure
Hematologic: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura
Hepatic: Cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency, liver function tests abnormal
Local: Pain at injection site
Neuromuscular & skeletal: Flaccid paralysis, paresthesia
Ocular: Myopia
Otic: Hearing disturbance, tinnitus
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency, cirrhosis; hyperchloremic acidosis, severe renal disease or dysfunction; severe pulmonary obstruction; long-term use in noncongestive angle-closure glaucoma
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS effects: Impairment of mental alertness and/or physical coordination may occur. Sulfa allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonylurea allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Discontinue if signs of hypersensitivity are noted.
Disease-related concerns: Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control. Hepatic impairment: Use with caution in patients with hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy. Respiratory acidosis: Use with caution in patients with respiratory acidosis.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to side effects.
Other warnings/precautions: I.M. administration: Painful because of the alkaline pH of the drug; use by this route is not recommended.
DRUG INTERACTIONS — Inhibits CYP3A4 (weak)
Amphetamines: Urinary excretion of amphetamine may be decreased; magnitude and duration of effects may be enhanced.
Carbamazepine: May increase serum concentrations of carbamazepine.
Cyclosporine trough concentrations may be increased resulting in possible nephrotoxicity and neurotoxicity.
Flecainide: May decrease excretion of flecainide.
Lithium: Serum concentrations may be decreased by acetazolamide; monitor.
Memantine: May decrease excretion of memantine.
Methenamine: Urinary antiseptic effect may be prevented by acetazolamide.
Phenytoin: Serum concentrations of phenytoin may be increased; incidence of osteomalacia may be enhanced or increased in patients on chronic phenytoin therapy.
Primidone serum concentrations may be decreased; carbonic anhydrase inhibitors may enhance the adverse/toxic effects of primidone.
Quinidine: Urinary excretion of quinidine may be decreased and effects may be enhanced.
Salicylate use (high dose) may result in carbonic anhydrase inhibitor accumulation and toxicity including CNS depression and metabolic acidosis. Salicylate toxicity might also be enhanced.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies, however, there are no adequate and well-controlled studies in pregnant women.
LACTATION — Enters breast milk/not recommended (AAP rates "compatible")
DIETARY CONSIDERATIONS — May be taken with food to decrease GI upset. May have additive effects with other folic acid antagonists. Sodium content of 500 mg injection: 47.2 mg (2.05 mEq).
PRICING — (data from drugstore.com)Capsule, 12-hour (Diamox Sequels) 500 mg (60): $169.03
Tablets (AcetaZOLAMIDE) 125 mg (60): $8.98 250 mg (60): $18.99
MONITORING PARAMETERS — Intraocular pressure, potassium, serum bicarbonate; serum electrolytes, periodic CBC with differential; monitor growth in pediatric patients
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include low blood sugar, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma. Hypoglycemia should be managed with 50 mL I.V. dextrose 50% followed immediately with a continuous infusion of 10% dextrose in water (administer at a rate sufficient enough to approach a serum glucose level of 100 mg/dL). The use of corticosteroids to treat the hypoglycemia is controversial, however, the addition of 100 mg of hydrocortisone to the dextrose infusion may prove helpful. In certain instances, hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acetazolamide®; Diamox®
INTERNATIONAL BRAND NAMES — Acetadiazol (MX); Albox (JP); Apo-Acetazolamide (CA, MY); Azol (TW); Carbinib (PT); Cetamid (PH); Defiltran (DE); Dehydratin (BG); Diamox (AE, AR, AT, AU, BE, BH, BR, CA, CH, CN, CO, CY, DK, EC, EG, ES, FI, FR, GB, HR, ID, IE, IN, IQ, IR, IT, JO, JP, KW, LB, LY, MX, MY, NL, NO, NZ, OM, PH, PY, QA, RU, SA, SE, SG, SY, TH, VE, YE, ZA); Diamox Sustets (CO); Diluran (CZ); Diural (UY); Diuramid (DE, PL); Edemox (ES); Evamox (PK); Genephamide (PE); Glaucomed (CO); Glaupax (CH, DK, HR, IE, JP, NO, TH); Huma-Zolamide (HU); Ledamox (JP); Lediamox (PT); Renamid (HR); Stazol (PY); Uramox (IL)
MECHANISM OF ACTION — Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons
PHARMACODYNAMICS / KINETICS Onset of action: Capsule, extended release: 2 hours; I.V.: 2 minutes Peak effect: Capsule, extended release: 8-12 hours; I.V.: 15 minutes; Tablet: 2-4 hours
Duration: Inhibition of aqueous humor secretion: Capsule, extended release: 18-24 hours; I.V.: 4-5 hours; Tablet: 8-12 hours
Distribution: Erythrocytes, kidneys; blood-brain barrier and placenta; distributes into milk (~30% of plasma concentrations)
Excretion: Urine (70% to 100% as unchanged drug)
PATIENT INFORMATION — Report numbness or tingling of extremities. Do not crush, chew, or swallow contents of long-acting capsule; may be opened and sprinkled on soft food. Ability to perform tasks requiring mental alertness and/or physical coordination may be impaired. Take with food; drug may cause substantial increase in blood glucose in some diabetic patients.
(For additional information see "Acetazolamide: Patient drug information")
Acetaminophen, isometheptene, and dichloralphenazone
U.S. BRAND NAMES — Amidrine [DSC]; Duradrin®; Midrin®; Migquin; Migratine; Migrazone®; Migrin-A
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Migraine headache: Oral: 2 capsules to start, followed by 1 capsule every hour until relief is obtained (maximum: 5 capsules/12 hours)
Tension headache: Oral: 1-2 capsules every 4 hours (maximum: 8 capsules/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: Acetaminophen 325 mg, isometheptene mucate 65 mg, dichloralphenazone 100 mg Amidrine [DSC], Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene mucate 65 mg, and dichloralphenazone 100 mg
DOSAGE FORMS: CONCISE Capsule: Acetaminophen 325 mg, isometheptene 65 mg, dichloralphenazone 100 mg Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene 65 mg, and dichloralphenazone 100 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of migraine and tension headache
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Central nervous system: Transient dizziness
Dermatological: Rash
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, isometheptene, dichloralphenazone, or any component of the formulation; glaucoma; severe renal disease; hypertension; organic heart disease; hepatic disease; MAO inhibitor therapy
RESTRICTIONS — C-IV
DRUG INTERACTIONS Based on acetaminophen component: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak) Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen; cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour) Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen; chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Acetaminophen and dichloralphenazone are excreted in breast milk; excretion of isometheptene is not known.
PRICING — (data from drugstore.com)Capsules (Amidrine) 325-65-100 mg (30): $13.99
Capsules (Migratine) 325-65-100 mg (100): $37.57
Capsules (Migrazone) 325-65-100 mg (100): $38.99
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Migraine headache: Oral: 2 capsules to start, followed by 1 capsule every hour until relief is obtained (maximum: 5 capsules/12 hours)
Tension headache: Oral: 1-2 capsules every 4 hours (maximum: 8 capsules/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: Acetaminophen 325 mg, isometheptene mucate 65 mg, dichloralphenazone 100 mg Amidrine [DSC], Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene mucate 65 mg, and dichloralphenazone 100 mg
DOSAGE FORMS: CONCISE Capsule: Acetaminophen 325 mg, isometheptene 65 mg, dichloralphenazone 100 mg Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene 65 mg, and dichloralphenazone 100 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of migraine and tension headache
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Central nervous system: Transient dizziness
Dermatological: Rash
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, isometheptene, dichloralphenazone, or any component of the formulation; glaucoma; severe renal disease; hypertension; organic heart disease; hepatic disease; MAO inhibitor therapy
RESTRICTIONS — C-IV
DRUG INTERACTIONS Based on acetaminophen component: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak) Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen; cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour) Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen; chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Acetaminophen and dichloralphenazone are excreted in breast milk; excretion of isometheptene is not known.
PRICING — (data from drugstore.com)Capsules (Amidrine) 325-65-100 mg (30): $13.99
Capsules (Migratine) 325-65-100 mg (100): $37.57
Capsules (Migrazone) 325-65-100 mg (100): $38.99
Acetazolamide
U.S. BRAND NAMES — Diamox® Sequels®
PHARMACOLOGIC CATEGORY Anticonvulsant, MiscellaneousCarbonic Anhydrase InhibitorDiuretic, Carbonic Anhydrase InhibitorOphthalmic Agent, Antiglaucoma
DOSING: ADULTS — Note: I.M. administration is not recommended.
Glaucoma: Chronic simple (open-angle): Oral: 250 mg 1-4 times/day or 500 mg extended release capsule twice daily Secondary, acute (closed-angle): I.V.: 250-500 mg, may repeat in 2-4 hours to a maximum of 1 g/day
Edema: Oral, I.V.: 250-375 mg once daily
Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses, not to exceed 1 g/day. Note: Extended release capsule is not recommended for treatment of epilepsy.
Metabolic alkalosis (unlabeled use): I.V. 250 mg every 6 hours for 4 doses or 500 mg single dose; reassess need based upon acid-base status
Mountain sickness: Oral: 250 mg every 8-12 hours (or 500 mg extended release capsules every 12-24 hours). Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude. Note: In situations of rapid ascent (such as rescue or military operations), 1000 mg/day is recommended.
Urine alkalinization (unlabeled use): Oral: 5 mg/kg/dose repeated 2-3 times over 24 hours
Respiratory stimulant in COPD (unlabeled use): Oral, I.V.: 250 mg twice daily
DOSING: PEDIATRIC — Note: I.M. administration is not recommended.
(For additional information see "Acetazolamide: Pediatric drug information")
Glaucoma: Oral: 8-30 mg/kg/day or 300-900 mg/m2/day divided every 8 hours I.V.: 20-40 mg/kg/24 hours divided every 6 hours, not to exceed 1 g/day
Edema: Oral, I.V.: 5 mg/kg or 150 mg/m2 once every day
Epilepsy: Oral: Refer to adult dosing.
DOSING: ELDERLY — Oral: Initial: 250 mg once or twice daily; use lowest effective dose possible.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 12 hours.
Clcr <10 mL/minute: Avoid use (ineffective).
Moderately dialyzable (20% to 50%)
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
DOSAGE FORMS: CONCISE Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Injection, tablet
ADMINISTRATION Oral: May cause an alteration in taste, especially carbonated beverages. Short-acting tablets may be crushed and suspended in cherry or chocolate syrup to disguise the bitter taste of the drug; do not use fruit juices. Alternatively, submerge tablet in 10 mL of hot water and add 10 mL honey or syrup.
I.M.: I.M. administration is painful because of the alkaline pH of the drug; use by this route is not recommended.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS.
Y-site administration: Variable (consult detailed reference): Diltiazem, TPN.
Compatibility when admixed: Compatible: Cimetidine, ranitidine. Incompatible: Multivitamins.
USE — Treatment of glaucoma (chronic simple open-angle, secondary glaucoma, preoperatively in acute angle-closure); drug-induced edema or edema due to congestive heart failure (adjunctive therapy); centrencephalic epilepsies (immediate release dosage form); prevention or amelioration of symptoms associated with acute mountain sickness
USE - UNLABELED / INVESTIGATIONAL — Urine alkalinization; respiratory stimulant in COPD; metabolic alkalosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Flushing
Central nervous system: Ataxia, confusion, convulsions, depression, dizziness, drowsiness, excitement, fatigue, fever, headache, malaise
Dermatologic: Allergic skin reactions, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Endocrine & metabolic: Electrolyte imbalance, growth retardation (children), hyperglycemia, hypoglycemia, hypokalemia, hyponatremia, metabolic acidosis
Gastrointestinal: Appetite decreased, diarrhea, melena, nausea, taste alteration, vomiting
Genitourinary: Crystalluria, glycosuria, hematuria, polyuria, renal failure
Hematologic: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura
Hepatic: Cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency, liver function tests abnormal
Local: Pain at injection site
Neuromuscular & skeletal: Flaccid paralysis, paresthesia
Ocular: Myopia
Otic: Hearing disturbance, tinnitus
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency, cirrhosis; hyperchloremic acidosis, severe renal disease or dysfunction; severe pulmonary obstruction; long-term use in noncongestive angle-closure glaucoma
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS effects: Impairment of mental alertness and/or physical coordination may occur. Sulfa allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonylurea allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Discontinue if signs of hypersensitivity are noted.
Disease-related concerns: Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control. Hepatic impairment: Use with caution in patients with hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy. Respiratory acidosis: Use with caution in patients with respiratory acidosis.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to side effects.
Other warnings/precautions: I.M. administration: Painful because of the alkaline pH of the drug; use by this route is not recommended.
DRUG INTERACTIONS — Inhibits CYP3A4 (weak)
Amphetamines: Urinary excretion of amphetamine may be decreased; magnitude and duration of effects may be enhanced.
Carbamazepine: May increase serum concentrations of carbamazepine.
Cyclosporine trough concentrations may be increased resulting in possible nephrotoxicity and neurotoxicity.
Flecainide: May decrease excretion of flecainide.
Lithium: Serum concentrations may be decreased by acetazolamide; monitor.
Memantine: May decrease excretion of memantine.
Methenamine: Urinary antiseptic effect may be prevented by acetazolamide.
Phenytoin: Serum concentrations of phenytoin may be increased; incidence of osteomalacia may be enhanced or increased in patients on chronic phenytoin therapy.
Primidone serum concentrations may be decreased; carbonic anhydrase inhibitors may enhance the adverse/toxic effects of primidone.
Quinidine: Urinary excretion of quinidine may be decreased and effects may be enhanced.
Salicylate use (high dose) may result in carbonic anhydrase inhibitor accumulation and toxicity including CNS depression and metabolic acidosis. Salicylate toxicity might also be enhanced.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies, however, there are no adequate and well-controlled studies in pregnant women.
LACTATION — Enters breast milk/not recommended (AAP rates "compatible")
DIETARY CONSIDERATIONS — May be taken with food to decrease GI upset. May have additive effects with other folic acid antagonists. Sodium content of 500 mg injection: 47.2 mg (2.05 mEq).
PRICING — (data from drugstore.com)Capsule, 12-hour (Diamox Sequels) 500 mg (60): $169.03
Tablets (AcetaZOLAMIDE) 125 mg (60): $8.98 250 mg (60): $18.99
MONITORING PARAMETERS — Intraocular pressure, potassium, serum bicarbonate; serum electrolytes, periodic CBC with differential; monitor growth in pediatric patients
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include low blood sugar, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma. Hypoglycemia should be managed with 50 mL I.V. dextrose 50% followed immediately with a continuous infusion of 10% dextrose in water (administer at a rate sufficient enough to approach a serum glucose level of 100 mg/dL). The use of corticosteroids to treat the hypoglycemia is controversial, however, the addition of 100 mg of hydrocortisone to the dextrose infusion may prove helpful. In certain instances, hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acetazolamide®; Diamox®
INTERNATIONAL BRAND NAMES — Acetadiazol (MX); Albox (JP); Apo-Acetazolamide (CA, MY); Azol (TW); Carbinib (PT); Cetamid (PH); Defiltran (DE); Dehydratin (BG); Diamox (AE, AR, AT, AU, BE, BH, BR, CA, CH, CN, CO, CY, DK, EC, EG, ES, FI, FR, GB, HR, ID, IE, IN, IQ, IR, IT, JO, JP, KW, LB, LY, MX, MY, NL, NO, NZ, OM, PH, PY, QA, RU, SA, SE, SG, SY, TH, VE, YE, ZA); Diamox Sustets (CO); Diluran (CZ); Diural (UY); Diuramid (DE, PL); Edemox (ES); Evamox (PK); Genephamide (PE); Glaucomed (CO); Glaupax (CH, DK, HR, IE, JP, NO, TH); Huma-Zolamide (HU); Ledamox (JP); Lediamox (PT); Renamid (HR); Stazol (PY); Uramox (IL)
MECHANISM OF ACTION — Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons
PHARMACODYNAMICS / KINETICS Onset of action: Capsule, extended release: 2 hours; I.V.: 2 minutes Peak effect: Capsule, extended release: 8-12 hours; I.V.: 15 minutes; Tablet: 2-4 hours
Duration: Inhibition of aqueous humor secretion: Capsule, extended release: 18-24 hours; I.V.: 4-5 hours; Tablet: 8-12 hours
Distribution: Erythrocytes, kidneys; blood-brain barrier and placenta; distributes into milk (~30% of plasma concentrations)
Excretion: Urine (70% to 100% as unchanged drug)
PATIENT INFORMATION — Report numbness or tingling of extremities. Do not crush, chew, or swallow contents of long-acting capsule; may be opened and sprinkled on soft food. Ability to perform tasks requiring mental alertness and/or physical coordination may be impaired. Take with food; drug may cause substantial increase in blood glucose in some diabetic patients.
(For additional information see "Acetazolamide: Patient drug information")
PHARMACOLOGIC CATEGORY Anticonvulsant, MiscellaneousCarbonic Anhydrase InhibitorDiuretic, Carbonic Anhydrase InhibitorOphthalmic Agent, Antiglaucoma
DOSING: ADULTS — Note: I.M. administration is not recommended.
Glaucoma: Chronic simple (open-angle): Oral: 250 mg 1-4 times/day or 500 mg extended release capsule twice daily Secondary, acute (closed-angle): I.V.: 250-500 mg, may repeat in 2-4 hours to a maximum of 1 g/day
Edema: Oral, I.V.: 250-375 mg once daily
Epilepsy: Oral: 8-30 mg/kg/day in 1-4 divided doses, not to exceed 1 g/day. Note: Extended release capsule is not recommended for treatment of epilepsy.
Metabolic alkalosis (unlabeled use): I.V. 250 mg every 6 hours for 4 doses or 500 mg single dose; reassess need based upon acid-base status
Mountain sickness: Oral: 250 mg every 8-12 hours (or 500 mg extended release capsules every 12-24 hours). Therapy should begin 24-48 hours before and continue during ascent and for at least 48 hours after arrival at the high altitude. Note: In situations of rapid ascent (such as rescue or military operations), 1000 mg/day is recommended.
Urine alkalinization (unlabeled use): Oral: 5 mg/kg/dose repeated 2-3 times over 24 hours
Respiratory stimulant in COPD (unlabeled use): Oral, I.V.: 250 mg twice daily
DOSING: PEDIATRIC — Note: I.M. administration is not recommended.
(For additional information see "Acetazolamide: Pediatric drug information")
Glaucoma: Oral: 8-30 mg/kg/day or 300-900 mg/m2/day divided every 8 hours I.V.: 20-40 mg/kg/24 hours divided every 6 hours, not to exceed 1 g/day
Edema: Oral, I.V.: 5 mg/kg or 150 mg/m2 once every day
Epilepsy: Oral: Refer to adult dosing.
DOSING: ELDERLY — Oral: Initial: 250 mg once or twice daily; use lowest effective dose possible.
DOSING: RENAL IMPAIRMENT Clcr 10-50 mL/minute: Administer every 12 hours.
Clcr <10 mL/minute: Avoid use (ineffective).
Moderately dialyzable (20% to 50%)
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
DOSAGE FORMS: CONCISE Capsule, extended release: Diamox® Sequels®: 500 mg
Injection, powder for reconstitution: 500 mg
Tablet: 125 mg, 250 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Injection, tablet
ADMINISTRATION Oral: May cause an alteration in taste, especially carbonated beverages. Short-acting tablets may be crushed and suspended in cherry or chocolate syrup to disguise the bitter taste of the drug; do not use fruit juices. Alternatively, submerge tablet in 10 mL of hot water and add 10 mL honey or syrup.
I.M.: I.M. administration is painful because of the alkaline pH of the drug; use by this route is not recommended.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS.
Y-site administration: Variable (consult detailed reference): Diltiazem, TPN.
Compatibility when admixed: Compatible: Cimetidine, ranitidine. Incompatible: Multivitamins.
USE — Treatment of glaucoma (chronic simple open-angle, secondary glaucoma, preoperatively in acute angle-closure); drug-induced edema or edema due to congestive heart failure (adjunctive therapy); centrencephalic epilepsies (immediate release dosage form); prevention or amelioration of symptoms associated with acute mountain sickness
USE - UNLABELED / INVESTIGATIONAL — Urine alkalinization; respiratory stimulant in COPD; metabolic alkalosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Flushing
Central nervous system: Ataxia, confusion, convulsions, depression, dizziness, drowsiness, excitement, fatigue, fever, headache, malaise
Dermatologic: Allergic skin reactions, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Endocrine & metabolic: Electrolyte imbalance, growth retardation (children), hyperglycemia, hypoglycemia, hypokalemia, hyponatremia, metabolic acidosis
Gastrointestinal: Appetite decreased, diarrhea, melena, nausea, taste alteration, vomiting
Genitourinary: Crystalluria, glycosuria, hematuria, polyuria, renal failure
Hematologic: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura
Hepatic: Cholestatic jaundice, fulminant hepatic necrosis, hepatic insufficiency, liver function tests abnormal
Local: Pain at injection site
Neuromuscular & skeletal: Flaccid paralysis, paresthesia
Ocular: Myopia
Otic: Hearing disturbance, tinnitus
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency, cirrhosis; hyperchloremic acidosis, severe renal disease or dysfunction; severe pulmonary obstruction; long-term use in noncongestive angle-closure glaucoma
WARNINGS / PRECAUTIONS Concerns related to adverse effects: CNS effects: Impairment of mental alertness and/or physical coordination may occur. Sulfa allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonylurea allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Discontinue if signs of hypersensitivity are noted.
Disease-related concerns: Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control. Hepatic impairment: Use with caution in patients with hepatic dysfunction; in cirrhosis, avoid electrolyte and acid/base imbalances that might lead to hepatic encephalopathy. Respiratory acidosis: Use with caution in patients with respiratory acidosis.
Special populations: Elderly: Use with caution in the elderly; may be more sensitive to side effects.
Other warnings/precautions: I.M. administration: Painful because of the alkaline pH of the drug; use by this route is not recommended.
DRUG INTERACTIONS — Inhibits CYP3A4 (weak)
Amphetamines: Urinary excretion of amphetamine may be decreased; magnitude and duration of effects may be enhanced.
Carbamazepine: May increase serum concentrations of carbamazepine.
Cyclosporine trough concentrations may be increased resulting in possible nephrotoxicity and neurotoxicity.
Flecainide: May decrease excretion of flecainide.
Lithium: Serum concentrations may be decreased by acetazolamide; monitor.
Memantine: May decrease excretion of memantine.
Methenamine: Urinary antiseptic effect may be prevented by acetazolamide.
Phenytoin: Serum concentrations of phenytoin may be increased; incidence of osteomalacia may be enhanced or increased in patients on chronic phenytoin therapy.
Primidone serum concentrations may be decreased; carbonic anhydrase inhibitors may enhance the adverse/toxic effects of primidone.
Quinidine: Urinary excretion of quinidine may be decreased and effects may be enhanced.
Salicylate use (high dose) may result in carbonic anhydrase inhibitor accumulation and toxicity including CNS depression and metabolic acidosis. Salicylate toxicity might also be enhanced.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies, however, there are no adequate and well-controlled studies in pregnant women.
LACTATION — Enters breast milk/not recommended (AAP rates "compatible")
DIETARY CONSIDERATIONS — May be taken with food to decrease GI upset. May have additive effects with other folic acid antagonists. Sodium content of 500 mg injection: 47.2 mg (2.05 mEq).
PRICING — (data from drugstore.com)Capsule, 12-hour (Diamox Sequels) 500 mg (60): $169.03
Tablets (AcetaZOLAMIDE) 125 mg (60): $8.98 250 mg (60): $18.99
MONITORING PARAMETERS — Intraocular pressure, potassium, serum bicarbonate; serum electrolytes, periodic CBC with differential; monitor growth in pediatric patients
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include low blood sugar, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma. Hypoglycemia should be managed with 50 mL I.V. dextrose 50% followed immediately with a continuous infusion of 10% dextrose in water (administer at a rate sufficient enough to approach a serum glucose level of 100 mg/dL). The use of corticosteroids to treat the hypoglycemia is controversial, however, the addition of 100 mg of hydrocortisone to the dextrose infusion may prove helpful. In certain instances, hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acetazolamide®; Diamox®
INTERNATIONAL BRAND NAMES — Acetadiazol (MX); Albox (JP); Apo-Acetazolamide (CA, MY); Azol (TW); Carbinib (PT); Cetamid (PH); Defiltran (DE); Dehydratin (BG); Diamox (AE, AR, AT, AU, BE, BH, BR, CA, CH, CN, CO, CY, DK, EC, EG, ES, FI, FR, GB, HR, ID, IE, IN, IQ, IR, IT, JO, JP, KW, LB, LY, MX, MY, NL, NO, NZ, OM, PH, PY, QA, RU, SA, SE, SG, SY, TH, VE, YE, ZA); Diamox Sustets (CO); Diluran (CZ); Diural (UY); Diuramid (DE, PL); Edemox (ES); Evamox (PK); Genephamide (PE); Glaucomed (CO); Glaupax (CH, DK, HR, IE, JP, NO, TH); Huma-Zolamide (HU); Ledamox (JP); Lediamox (PT); Renamid (HR); Stazol (PY); Uramox (IL)
MECHANISM OF ACTION — Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons
PHARMACODYNAMICS / KINETICS Onset of action: Capsule, extended release: 2 hours; I.V.: 2 minutes Peak effect: Capsule, extended release: 8-12 hours; I.V.: 15 minutes; Tablet: 2-4 hours
Duration: Inhibition of aqueous humor secretion: Capsule, extended release: 18-24 hours; I.V.: 4-5 hours; Tablet: 8-12 hours
Distribution: Erythrocytes, kidneys; blood-brain barrier and placenta; distributes into milk (~30% of plasma concentrations)
Excretion: Urine (70% to 100% as unchanged drug)
PATIENT INFORMATION — Report numbness or tingling of extremities. Do not crush, chew, or swallow contents of long-acting capsule; may be opened and sprinkled on soft food. Ability to perform tasks requiring mental alertness and/or physical coordination may be impaired. Take with food; drug may cause substantial increase in blood glucose in some diabetic patients.
(For additional information see "Acetazolamide: Patient drug information")
Acetaminophen, isometheptene, and dichloralphenazone
U.S. BRAND NAMES — Amidrine [DSC]; Duradrin®; Midrin®; Migquin; Migratine; Migrazone®; Migrin-A
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Migraine headache: Oral: 2 capsules to start, followed by 1 capsule every hour until relief is obtained (maximum: 5 capsules/12 hours)
Tension headache: Oral: 1-2 capsules every 4 hours (maximum: 8 capsules/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: Acetaminophen 325 mg, isometheptene mucate 65 mg, dichloralphenazone 100 mg Amidrine [DSC], Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene mucate 65 mg, and dichloralphenazone 100 mg
DOSAGE FORMS: CONCISE Capsule: Acetaminophen 325 mg, isometheptene 65 mg, dichloralphenazone 100 mg Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene 65 mg, and dichloralphenazone 100 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of migraine and tension headache
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Central nervous system: Transient dizziness
Dermatological: Rash
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, isometheptene, dichloralphenazone, or any component of the formulation; glaucoma; severe renal disease; hypertension; organic heart disease; hepatic disease; MAO inhibitor therapy
RESTRICTIONS — C-IV
DRUG INTERACTIONS Based on acetaminophen component: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak) Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen; cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour) Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen; chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Acetaminophen and dichloralphenazone are excreted in breast milk; excretion of isometheptene is not known.
PRICING — (data from drugstore.com)Capsules (Amidrine) 325-65-100 mg (30): $13.99
Capsules (Migratine) 325-65-100 mg (100): $37.57
Capsules (Migrazone) 325-65-100 mg (100): $38.99
PHARMACOLOGIC CATEGORY Analgesic, Miscellaneous
DOSING: ADULTS Migraine headache: Oral: 2 capsules to start, followed by 1 capsule every hour until relief is obtained (maximum: 5 capsules/12 hours)
Tension headache: Oral: 1-2 capsules every 4 hours (maximum: 8 capsules/24 hours)
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: Acetaminophen 325 mg, isometheptene mucate 65 mg, dichloralphenazone 100 mg Amidrine [DSC], Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene mucate 65 mg, and dichloralphenazone 100 mg
DOSAGE FORMS: CONCISE Capsule: Acetaminophen 325 mg, isometheptene 65 mg, dichloralphenazone 100 mg Duradrin®, Midrin®, Migquin, Migrazone®, Migratine, Migrin-A: Acetaminophen 325 mg, isometheptene 65 mg, and dichloralphenazone 100 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Relief of migraine and tension headache
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Central nervous system: Transient dizziness
Dermatological: Rash
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, isometheptene, dichloralphenazone, or any component of the formulation; glaucoma; severe renal disease; hypertension; organic heart disease; hepatic disease; MAO inhibitor therapy
RESTRICTIONS — C-IV
DRUG INTERACTIONS Based on acetaminophen component: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak) Decreased effect: Barbiturates, carbamazepine, hydantoins, rifampin, sulfinpyrazone may decrease the analgesic effect of acetaminophen; cholestyramine may decrease acetaminophen absorption (separate dosing by at least 1 hour) Increased toxicity: Barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone may increase the hepatotoxic potential of acetaminophen; chronic ethanol abuse increases risk for acetaminophen toxicity; effect of warfarin may be enhanced
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Acetaminophen and dichloralphenazone are excreted in breast milk; excretion of isometheptene is not known.
PRICING — (data from drugstore.com)Capsules (Amidrine) 325-65-100 mg (30): $13.99
Capsules (Migratine) 325-65-100 mg (100): $37.57
Capsules (Migrazone) 325-65-100 mg (100): $38.99
Acetaminophen, dextromethorphan, and pseudoephedrine
SPECIAL ALERTS Infant Deaths Associated with Cough and Cold Medications - January 2007
The Centers for Disease Control and Prevention (CDC) has released a report concerning the use of cough and cold medications in children <2 years of age. Products containing nasal decongestants (eg, pseudoephedrine), antihistamines (eg, carbinoxamine), cough suppressants (eg, dextromethorphan), and expectorants are often used in this age group. The CDC notes that during 2004 and 2005, ~ 1519 children <2 years of age were seen in emergency departments for adverse effects, including overdose, associated with these medications.
During this time period, 3 infants <6 months of age died. All 3 had postmortem blood levels of pseudoephedrine, ranging from 4743-7100 ng/mL (therapeutic levels for children 2-12 years: 180-500 ng/mL). In addition, 2 of the 3 infants also had detectable levels of dextromethorphan. Although dextromethorphan has been shown to be effective to reduce cough in adults, the same efficacy has not been documented in young children. The American Academy of Pediatrics and the American College of Chest Physicians do not recommend the use of dextromethorphan for over-the-counter (OTC) use in young children.
Safety and efficacy for the use of cough and cold products in children <2 years of age is limited. The Food and Drug Administration (FDA) notes that there are no approved OTC uses for these products in children <2 years of age. Clinicians are reminded to ask caregivers about the use of OTC products in order to avoid exposure to multiple medications containing the same ingredient. Caregivers are reminded that OTC cough and cold products should not be used in children <2 years of age except under specific direction by their healthcare provider.
For additional information, refer to the following CDC website: http://www.cdc.gov/mmwr/preview/mmwrhtml/mm5601a1.htm, Centers for Disease Control, "Infant Deaths Associated with Cough and Cold Medications - Two States, 2005,"MMWR Morb Mortal Wkly Rep, 2007, 56(01):1-4.
U.S. BRAND NAMES — Comtrex® Non-Drowsy Cold and Cough Relief [OTC] [DSC]; Infants' Tylenol® Cold Plus Cough Concentrated Drops [OTC] [DSC]; Sudafed® Severe Cold [OTC]; Triaminic® Cough and Sore Throat Formula [OTC] [DSC]; Tylenol® Cold Day Non-Drowsy [OTC]; Tylenol® Flu Non-Drowsy Maximum Strength [OTC]; Vicks® DayQuil® Multi-Symptom Cold and Flu [OTC] [DSC]
PHARMACOLOGIC CATEGORY AntihistamineAntitussive
DOSING: ADULTS Pain (Analgesic): Oral: Based on acetaminophen component: 325-650 mg every 4-7 hours as needed; do not exceed 4 g/day
Cough suppressant (Antitussive): Oral: Based on dextromethorphan component: 10-20 mg every 4-8 hours or 30 mg every 8 hours; do not exceed 120 mg/24 hours
Nasal congestion (Decongestant): Oral: Based on pseudoephedrine component: 60 mg every 4 hours (maximum: 360 mg/24 hours)
Product labeling:
Sudafed® Severe Cold, Tylenol® Flu Non-Drowsy Maximum Strength: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours)
Tylenol® Cold Non-Drowsy: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours)
DOSING: PEDIATRIC Analgesic: Oral: Based on acetaminophen component: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses/24 hours.
Cough suppressant: Oral: Based on dextromethorphan component: Children 6-12 years: 15 mg every 6-8 hours; do not exceed 60 mg/24 hours Children >12 years: Refer to adult dosing.
Decongestant: Oral: Based on pseudoephedrine component: Children: 2-6 years: 15 mg every 4 hours (maximum: 90 mg/24 hours) 6-12 years: 30 mg every 4 hours (maximum: 180 mg/24 hours) Children >12 years: Refer to adult dosing.
Product labeling:
Infants' Tylenol® Cold Plus Cough Concentrated Drops: Oral: Children 2-3 years (24-55 lb): 2 dropperfuls every 4-6 hours (maximum: 4 doses/24 hours)
Sudafed® Severe Cold, Thera-Flu® Non-Drowsy Maximum Strength (gelcap), Tylenol® Flu Non-Drowsy Maximum Strength: Oral: Children >12 years: Refer to adult dosing.
Tylenol® Cold Non-Drowsy: Oral: Children 6-11 years: 1 dose every 6 hours (maximum: 4 doses/24 hours) Children 12 years: Refer to adult dosing.
Thera-Flu® Non-Drowsy Maximum Strength: Oral: Children >12 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: Comtrex® Non-Drowsy Cold and Cough Relief: Acetaminophen 500 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg [contains benzoic acid] [DSC] Tylenol® Cold Day Non-Drowsy: Acetaminophen 325 mg dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Vicks® DayQuil® Multi-Symptom Cold and Flu: Acetaminophen 250 mg, dextromethorphan hydrobromide 10 mg, and pseudoephedrine hydrochloride 30 mg [DSC]
Gelcap: Tylenol® Cold Day Non-Drowsy: Acetaminophen 325 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg [contains benzyl alcohol] [DSC] Tylenol® Flu Non-Drowsy Maximum Strength: Acetaminophen 500 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg
Liquid: Triaminic® Cough and Sore Throat Formula: Acetaminophen 160 mg, dextromethorphan hydrobromide 7.5 mg, and pseudoephedrine hydrochloride 15 mg per 5 mL (120 mL, 240 mL) [contains benzoic acid; grape flavor] [DSC] Vicks® DayQuil® Multi-Symptom Cold and Flu: Acetaminophen 325 mg, dextromethorphan hydrobromide 10 mg, and pseudoephedrine hydrochloride 30 mg per 15 mL (175 mL) [DSC]
Suspension, oral [drops]: Infants' Tylenol® Cold Plus Cough Concentrated Drops: Acetaminophen 160 mg, dextromethorphan hydrobromide 5 mg, and pseudoephedrine hydrochloride 15 mg per 1.6 mL (15 mL) [1.6 mL = 2 dropperfuls] [cherry flavor] [DSC]
DOSAGE FORMS: CONCISE Caplet: Sudafed® Severe Cold [OTC], Tylenol® Cold Day Non-Drowsy [OTC]: Acetaminophen 325 mg, dextromethorphan 15 mg, and pseudoephedrine 30 mg
Gelcap: Tylenol® Flu Non-Drowsy Maximum Strength [OTC]: Acetaminophen 500 mg, dextromethorphan 15 mg, and pseudoephedrine 30 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of mild-to-moderate pain and fever; symptomatic relief of cough and congestion
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, dextromethorphan, pseudoephedrine, or any component of the formulation
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Dextromethorphan: Substrate of CYP2B6 (minor), 2C9 (minor), 2C19 (minor), 2D6 (major), 2E1 (minor), 3A4 (minor); Inhibits CYP2D6 (weak)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
CANADIAN BRAND NAMES — Contac® Complete; Contac® Cough, Cold and Flu Day & Night™; Sudafed® Cold & Cough Extra Strength; Tylenol® Cold Daytime
INTERNATIONAL BRAND NAMES — Contac Complete (CA); Contac Cough, Cold and Flu Day & Night® (CA); Sudafed Cold & Cough Extra Strength (CA); Tylenol Cold Daytime (CA)
PHARMACODYNAMICS / KINETICS — See individual agents.
The Centers for Disease Control and Prevention (CDC) has released a report concerning the use of cough and cold medications in children <2 years of age. Products containing nasal decongestants (eg, pseudoephedrine), antihistamines (eg, carbinoxamine), cough suppressants (eg, dextromethorphan), and expectorants are often used in this age group. The CDC notes that during 2004 and 2005, ~ 1519 children <2 years of age were seen in emergency departments for adverse effects, including overdose, associated with these medications.
During this time period, 3 infants <6 months of age died. All 3 had postmortem blood levels of pseudoephedrine, ranging from 4743-7100 ng/mL (therapeutic levels for children 2-12 years: 180-500 ng/mL). In addition, 2 of the 3 infants also had detectable levels of dextromethorphan. Although dextromethorphan has been shown to be effective to reduce cough in adults, the same efficacy has not been documented in young children. The American Academy of Pediatrics and the American College of Chest Physicians do not recommend the use of dextromethorphan for over-the-counter (OTC) use in young children.
Safety and efficacy for the use of cough and cold products in children <2 years of age is limited. The Food and Drug Administration (FDA) notes that there are no approved OTC uses for these products in children <2 years of age. Clinicians are reminded to ask caregivers about the use of OTC products in order to avoid exposure to multiple medications containing the same ingredient. Caregivers are reminded that OTC cough and cold products should not be used in children <2 years of age except under specific direction by their healthcare provider.
For additional information, refer to the following CDC website: http://www.cdc.gov/mmwr/preview/mmwrhtml/mm5601a1.htm, Centers for Disease Control, "Infant Deaths Associated with Cough and Cold Medications - Two States, 2005,"MMWR Morb Mortal Wkly Rep, 2007, 56(01):1-4.
U.S. BRAND NAMES — Comtrex® Non-Drowsy Cold and Cough Relief [OTC] [DSC]; Infants' Tylenol® Cold Plus Cough Concentrated Drops [OTC] [DSC]; Sudafed® Severe Cold [OTC]; Triaminic® Cough and Sore Throat Formula [OTC] [DSC]; Tylenol® Cold Day Non-Drowsy [OTC]; Tylenol® Flu Non-Drowsy Maximum Strength [OTC]; Vicks® DayQuil® Multi-Symptom Cold and Flu [OTC] [DSC]
PHARMACOLOGIC CATEGORY AntihistamineAntitussive
DOSING: ADULTS Pain (Analgesic): Oral: Based on acetaminophen component: 325-650 mg every 4-7 hours as needed; do not exceed 4 g/day
Cough suppressant (Antitussive): Oral: Based on dextromethorphan component: 10-20 mg every 4-8 hours or 30 mg every 8 hours; do not exceed 120 mg/24 hours
Nasal congestion (Decongestant): Oral: Based on pseudoephedrine component: 60 mg every 4 hours (maximum: 360 mg/24 hours)
Product labeling:
Sudafed® Severe Cold, Tylenol® Flu Non-Drowsy Maximum Strength: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours)
Tylenol® Cold Non-Drowsy: Oral: 2 doses every 6 hours (maximum: 8 doses/24 hours)
DOSING: PEDIATRIC Analgesic: Oral: Based on acetaminophen component: 10-15 mg/kg/dose every 4-6 hours as needed; do not exceed 5 doses/24 hours.
Cough suppressant: Oral: Based on dextromethorphan component: Children 6-12 years: 15 mg every 6-8 hours; do not exceed 60 mg/24 hours Children >12 years: Refer to adult dosing.
Decongestant: Oral: Based on pseudoephedrine component: Children: 2-6 years: 15 mg every 4 hours (maximum: 90 mg/24 hours) 6-12 years: 30 mg every 4 hours (maximum: 180 mg/24 hours) Children >12 years: Refer to adult dosing.
Product labeling:
Infants' Tylenol® Cold Plus Cough Concentrated Drops: Oral: Children 2-3 years (24-55 lb): 2 dropperfuls every 4-6 hours (maximum: 4 doses/24 hours)
Sudafed® Severe Cold, Thera-Flu® Non-Drowsy Maximum Strength (gelcap), Tylenol® Flu Non-Drowsy Maximum Strength: Oral: Children >12 years: Refer to adult dosing.
Tylenol® Cold Non-Drowsy: Oral: Children 6-11 years: 1 dose every 6 hours (maximum: 4 doses/24 hours) Children 12 years: Refer to adult dosing.
Thera-Flu® Non-Drowsy Maximum Strength: Oral: Children >12 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: HEPATIC IMPAIRMENT — Use with caution. Limited, low-dose therapy usually well tolerated in hepatic disease/cirrhosis; however, cases of hepatotoxicity at daily acetaminophen dosages <4 g/day have been reported. Avoid chronic use in hepatic impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Caplet: Comtrex® Non-Drowsy Cold and Cough Relief: Acetaminophen 500 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg [contains benzoic acid] [DSC] Tylenol® Cold Day Non-Drowsy: Acetaminophen 325 mg dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg
Capsule, liquid: Vicks® DayQuil® Multi-Symptom Cold and Flu: Acetaminophen 250 mg, dextromethorphan hydrobromide 10 mg, and pseudoephedrine hydrochloride 30 mg [DSC]
Gelcap: Tylenol® Cold Day Non-Drowsy: Acetaminophen 325 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg [contains benzyl alcohol] [DSC] Tylenol® Flu Non-Drowsy Maximum Strength: Acetaminophen 500 mg, dextromethorphan hydrobromide 15 mg, and pseudoephedrine hydrochloride 30 mg
Liquid: Triaminic® Cough and Sore Throat Formula: Acetaminophen 160 mg, dextromethorphan hydrobromide 7.5 mg, and pseudoephedrine hydrochloride 15 mg per 5 mL (120 mL, 240 mL) [contains benzoic acid; grape flavor] [DSC] Vicks® DayQuil® Multi-Symptom Cold and Flu: Acetaminophen 325 mg, dextromethorphan hydrobromide 10 mg, and pseudoephedrine hydrochloride 30 mg per 15 mL (175 mL) [DSC]
Suspension, oral [drops]: Infants' Tylenol® Cold Plus Cough Concentrated Drops: Acetaminophen 160 mg, dextromethorphan hydrobromide 5 mg, and pseudoephedrine hydrochloride 15 mg per 1.6 mL (15 mL) [1.6 mL = 2 dropperfuls] [cherry flavor] [DSC]
DOSAGE FORMS: CONCISE Caplet: Sudafed® Severe Cold [OTC], Tylenol® Cold Day Non-Drowsy [OTC]: Acetaminophen 325 mg, dextromethorphan 15 mg, and pseudoephedrine 30 mg
Gelcap: Tylenol® Flu Non-Drowsy Maximum Strength [OTC]: Acetaminophen 500 mg, dextromethorphan 15 mg, and pseudoephedrine 30 mg
GENERIC EQUIVALENT AVAILABLE — No
USE — Treatment of mild-to-moderate pain and fever; symptomatic relief of cough and congestion
ADVERSE REACTIONS SIGNIFICANT — See individual agents.
CONTRAINDICATIONS — Hypersensitivity to acetaminophen, dextromethorphan, pseudoephedrine, or any component of the formulation
DRUG INTERACTIONS Acetaminophen: Substrate (minor) of CYP1A2, 2A6, 2C9, 2D6, 2E1, 3A4; Inhibits CYP3A4 (weak)
Dextromethorphan: Substrate of CYP2B6 (minor), 2C9 (minor), 2C19 (minor), 2D6 (major), 2E1 (minor), 3A4 (minor); Inhibits CYP2D6 (weak)
Also see individual agents.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Excessive intake of ethanol may increase the risk of acetaminophen-induced hepatotoxicity. Avoid ethanol or limit to <3 drinks/day.
CANADIAN BRAND NAMES — Contac® Complete; Contac® Cough, Cold and Flu Day & Night™; Sudafed® Cold & Cough Extra Strength; Tylenol® Cold Daytime
INTERNATIONAL BRAND NAMES — Contac Complete (CA); Contac Cough, Cold and Flu Day & Night® (CA); Sudafed Cold & Cough Extra Strength (CA); Tylenol Cold Daytime (CA)
PHARMACODYNAMICS / KINETICS — See individual agents.
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