Trade Names:Carbatrol- Capsules, extended-release 100 mg- Capsules, extended-release 200 mg- Capsules, extended-release 300 mg
Trade Names:Epitol- Tablets 200 mg
Trade Names:Equetro- Capsules, extended-release 100 mg- Capsules, extended-release 200 mg- Capsules, extended-release 300 mg
Trade Names:Tegretol- Tablets, chewable 100 mg- Tablets 200 mg- Suspension 100 mg per 5 mL
Trade Names:Tegretol XR- Tablets, extended-release 100 mg- Tablets, extended-release 200 mg- Tablets, extended-release 400 mgApo-Carbamazepine (Canada)Gen-Carbamazepine CR (Canada)PMS-Carbamazepine (Canada)Sandoz Carbamazepine (Canada)Taro-Carbamazepine (Canada)
Appears to provide anticonvulsant effects by reducing polysynaptic responses and blocking posttetanic potentiation. Mechanism of action for other effects is unknown.
Therapeutic levels are 4 to 12 mcg/mL.Suspension
T max is approximately 1.5 h.Tablets
T max is 4 to 5 h.Extended-release
T max is 3 to 12 h ( Tegretol XR ).
76% protein bound. Rapidly crosses the placenta.
Induces its own metabolism; metabolized in the liver by CYP3A4 to the active metabolite carbamazepine-10,11-epoxide (shown to be equipotent to carbamazepine).
Initial t ½ is 25 to 65 h, decreasing to 12 to 17 h on repeated doses. 72% is excreted in the urine (3% as unchanged drug) and 28% in the feces.
More rapidly metabolized to 10,11-epoxide.
Treatment of epilepsy (eg, partial seizures with complex symptoms, generalized tonic-clonic seizures, mixed seizure patterns, other partial or generalized seizures); treatment of pain associated with trigeminal neuralgia.Equetro only
Treatment of acute manic and mixed episodes associated with bipolar 1 disorder.
Treatment of restless leg syndrome; alternative/adjunctive treatment for certain symptoms associated with borderline personality disorder; alternative to benzodiazepines for managing alcohol withdrawal; adjunctive therapy for schizophrenia; treatment of postherpetic neuralgia.
Hypersensitivity to tricyclic antidepressants or carbamazepine; history of bone marrow depression; concomitant use of MAOIs. Discontinue MAOIs at least 14 days before administration of carbamazepine.
PO 200 mg twice daily (tablets) or 100 mg (1 tsp) 4 times daily (suspension). Increase weekly by up to 200 mg/day in 2 divided doses for extended-release or 3 to 4 divided doses for other formulations to reach minimum effective dose (max, 1,000 mg/day in children 12 to 15 yr of age; 1,200 mg/day in children older than 15 yr of age; 1,600 mg/day in adults).Maintenance
800 to 1,200 mg/day.Adults and Children older than 12 yr of age (extended-release) Initial dosage
PO 200 mg twice daily.Children 6 to 12 yr of age Initial dosage
PO 100 mg twice daily (tablets) or 50 mg 4 times daily (suspension). Increase weekly by 100 mg/day in 3 to 4 divided doses (extended-release formulations use a twice-daily regimen) to reach minimum effective dose (max, 1,000 mg/day).Maintenance
400 to 800 mg/day in 3 to 4 divided doses.Children younger than 6 yr of age Initial dosage
PO 10 to 20 mg/kg/day in 2 or 3 divided doses (tablet) or 10 to 20 mg/kg/day in 4 divided doses (suspension). Increase weekly to achieve optimal clinical response when administered in 3 or 4 divided daily doses (max, 35 mg/kg/day).Maintenance
Less than 35 mg/kg/day.Trigeminal NeuralgiaAdults Initial dosage
PO 100 mg twice daily (tablets) or 50 mg 4 times daily (suspension). May increase by up to 200 mg/day (tablets, 100 mg increments every 12 h; suspension, 50 mg 4 times daily) as needed (max, 1,200 mg/day).Maintenance
Usually 400 to 800 mg/day. Attempt to reduce the dosage or discontinue the drug once every 3 mo.Adults (extended-release) Initial dosage
PO 100 mg twice daily (tablets) or 200 mg once daily (capsules) (max, 1,200 mg/day).Bipolar Disorder ( Equetro only)Adults Initial dosage
PO 200 mg twice daily. Increase in 200 mg/day increments to optimal clinical response (max, 1,600 mg/day).
May be used alone or in combination with other antiepileptic drugs (AEDs) for treatment of seizures or with analgesics for treatment of trigeminal neuralgia.
Store all doseforms at controlled room temperature (59° to 86°F). Protect from light and moisture. Protect suspension from freezing.
Levels may be reduced by carbamazepine.Acetazolamide, azole antifungal agents, danazol, diltiazem, grapefruit juice, loratadine, macrolide antibiotics (except azithromycin), niacinamide, nicotinamide, propoxyphene, quinine, terfenadine, verapamil
May increase carbamazepine levels and result in toxicity.Alcohol
Increased risk of CNS adverse reactions.Anticoagulants
May decrease anticoagulant effects.Barbiturates
May result in decreased carbamazepine serum concentrations, possibly leading to decreased effectiveness.Charcoal, activated
May reduce absorption of carbamazepine.Cimetidine
May result in carbamazepine toxicity.Cisplatin, doxorubicin, methsuximide, rifamycins (eg, rifampin)
May increase carbamazepine metabolism, reducing plasma levels and the therapeutic effect.Clomipramine
Levels may be increased by carbamazepine.Contraceptives, hormonal
Causes breakthrough bleeding and reduces effectiveness of contraceptives.Delavirdine
Coadministration may lead to loss of virologic response and possible resistance. May decrease delavirdine levels and increase carbamazepine levels.Doxycycline hyclate
May decrease doxycycline hyclate levels.Felbamate
May decrease concentrations of felbamate or carbamazepine.Felodipine
May decrease effects of felodipine.Haloperidol
May decrease effects of haloperidol.Hydantoins (eg, phenytoin)
May decrease carbamazepine levels; may alter hydantoin levels.Isoniazid
May result in toxicity of isoniazid, carbamazepine, or both.Lamotrigine
Lamotrigine levels may be decreased, while levels of the active metabolite of carbamazepine may be increased.Liquid medicinals or diluents
May result in the formation of an insoluble precipitate in the GI tract.Lithium
May cause adverse CNS effects regardless of drug levels.MAOIs, voriconazole
Coadministration with carbamazepine is contraindicated.Nefazodone
Coadministration is contraindicated. Elevated carbamazepine levels and lower nefazodone levels may result.Nondepolarizing muscle relaxants
May make these agents less effective.Primidone
Decreased carbamazepine levels. Primidone's active metabolite (phenobarbital) may be increased.Protease inhibitors (eg, indinavir)
Carbamazepine levels may be elevated and protease inhibitor levels may be decreased, resulting in antiretroviral treatment failure.Quetiapine
Quetiapine levels may be reduced; concentrations of the active carbamazepine metabolite may be increased.SSRIs (eg, fluoxetine, fluvoxamine)
Increased carbamazepine levels with possible toxicity.Theophylline
May reduce effects of theophylline and carbamazepine. Theophylline levels may be increased or decreased.Tricyclic antidepressants
May increase carbamazepine levels; may decrease tricyclic antidepressant levels.Valproic acid
May decrease valproic acid levels; may alter carbamazepine levels.
Thyroid function tests showed decreased values. Interference with some pregnancy tests has been reported.
Aggravation of coronary artery disease, aggravation of hypertension, arrhythmias, AV block, CHF, fainting, hypotension, syncope, thrombophlebitis.
Dizziness (44%); somnolence (32%); headache (22%); ataxia (15%); amnesia, asthenia (8%); anxiety, depression, manic depressive reaction (7%); speech disorder (6%); ataxia (5%); depersonalization, extrapyramidal syndrome, insomnia, nervousness, suicide attempts (less than 5%); aseptic meningitis with myoclonus, cerebral artery insufficiency, confusion, depression with agitation, disturbances in coordination, drowsiness, fatigue, hyperacusis, involuntary movements, neuroleptic malignant syndrome, paralysis, paresthesias, peripheral neuritis, talkativeness, visual hallucinations.
Rash (13%); pruritus (8%); alopecia, photosensitivity (less than 5%); aggravation of disseminated systemic lupus erythematosus, altered skin pigmentation, diaphoresis, erythema multiforme and nodosum, erythematous rash, exfoliative dermatitis, hirsutism, pruritic rash, purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), urticaria.
Amblyopia (6%); diplopia, ear pain, pharyngitis, rhinitis (less than 5%); blurred vision, conjunctivitis, dry pharynx, nystagmus, oculomotor disturbances, scattered punctuate cortical lens opacities, tinnitus.
Nausea (29%); vomiting (18%); diarrhea, dyspepsia (10%); dry mouth (8%); constipation (5%); abdominal pain, anorexia, gastric distress, glossitis, pancreatitis, stomatitis.
UTI (less than 5%); acute urinary retention, albuminuria, azotemia, elevated BUN, glucosuria, impotence, microscopic urine deposits, oliguria with elevated blood pressure, renal failure, urinary frequency.
Leukopenia, lymphadenopathy (less than 5%); acute intermittent porphyria, adenopathy, agranulocytosis, aplastic anemia, bone marrow suppression, eosinophilia, leukocytosis, pancytopenia, thrombocytopenia.
Abnormal LFTs (less than 5%); cholestatic jaundice, hepatic failure, hepatitis, hepatocellular jaundice.
Decreased plasma calcium; elevated cholesterol, HDL cholesterol, and triglycerides; hyponatremia; SIADH; water intoxication.
Back pain (5%); aching joints and muscles, leg cramps.
Bronchitis, sinusitis (less than 5%); dyspnea, pneumonia, pneumonitis, pulmonary hypersensitivity.
Infection, pain (12%); accidental injury (7%); chest pain (5%); edema, peripheral edema (less than 5%); chills, fever, lupus erythematosus–like syndrome, multi-organ hypersensitivity.
WarningsAplastic anemia and agranulocytosis
Has been reported with use. The risk is 5 to 8 times greater than in the general population.
Obtain complete pretreatment hematological testing as a baseline. If, in the course of treatment, a patient exhibits low or decreased WBC or platelet count, monitor the patient closely.Serious dermatologic reactions and HLA-B∗1502 allele
Serious and sometimes fatal dermatologic reactions, including Stevens-Johnson syndrome and TEN, have been reported in 1 to 6 per 10,000 carbamazepine users. Studies in patients of Chinese ancestry found a strong association between the risk of developing Stevens-Johnson syndrome or TEN and the inherited genetic allelic variant HLA-B∗1502. Screen patients who are genetically at risk and, if positive for the allele, when possible, do not prescribe carbamazepine.
Monitor carbamazepine serum levels as indicated to evaluate therapeutic response, compliance, and possible toxicity. Assess CBC and renal and hepatic function prior to initiating therapy. Monitor renal and hepatic function periodically during treatment. Monitor CBC closely if, in the course of treatment, low or decreased WBC or platelet count is noted. Obtain baseline and periodic eye examinations, including slit-lamp, funduscopy, and tonometry. Obtain high-resolution HLA-B∗1502 typing for patients who are genetically at risk.
Category D .
Excreted in breast milk.
Management of epilepsy in children is derived from clinical investigations in adults. Safety and efficacy of Equetro are not established.
No data are available.
Use with caution in patients with prior adverse hematologic reactions to any drug; cardiac, renal, or hepatic disease; interrupted courses of therapy with carbamazepine; and mixed seizure disorders that include atypical absence seizures.
May cause dizziness or drowsiness.
Carbamazepine has mild anticholinergic activity; closely observe patients with increased IOP during therapy.
Rarely, severe dermatologic reactions, including TEN and Stevens-Johnson syndrome, have been reported.
Abrupt discontinuation in patients with seizure disorder may precipitate status epilepticus. If treatment is to be discontinued, gradually taper the dose and monitor patient for seizure activity.
Possibility of suicide attempts is inherent in bipolar disorder. Closely supervise high-risk patients.
Because of the relationship of carbamazepine to other tricyclic compounds, latent psychosis can possibly be activated.
Abnormal EEG, acetonuria, anuria, ataxia, coma, conduction disorders, convulsions, dizziness, drowsiness, dysmetria, glucosuria, hyperreflexia followed by hyporeflexia, hypertension, hypotension, impairment of consciousness, irregular breathing, leukocytosis, motor restlessness, muscle twitching, mydriasis, nausea, nystagmus, oliguria, psychomotor disturbances, respiratory depression, shock, tachycardia, tremor, urinary retention, vomiting.
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