Therapeutic Class |
Anticonvulsant |
Indications |
Partial seizures with complex symptomatology (psychomotor, temporal lobe), generalized tonic-clonic seizures (grand mal), mixed seizure patterns, trigeminal neuralgia, Acute manic and mixed episodes associated with bipolar 1 disorder, Treatment of restless leg syndrome and post-traumatic stress disorders |
Adult Doses |
Epilepsy |
Pediatric Doses |
Epilepsy: Oral: Children <6 years: Children 6-12 years: Children >12 years: Refer to adult dosing. |
Doses in Renal impairment |
Administer 75% of dose |
Doses in Hepatic impairment |
Use with caution in hepatic impairment; metabolized primarily in the liver |
Contraindications |
Hypersensitivity; bone marrow depression; porphyria, pregnancy. |
Boxed Warning |
Potentially fatal blood cell abnormalities have been reported following treatment. Patients of Asian descent should be screened for the variant HLA-B*1502 allele prior to initiating therapy. |
Warnings / Precautions |
Lactation; CV disease, hepatic or renal disorders, history of blood disorders or haematological reactions to other drugs; glaucoma; skin disorders; elderly, patients on MAO inhibitors; abrupt withdrawal of treatment. |
Adverse Reactions |
Dizziness, drowsiness, ataxia; dry mouth, abdominal pain, nausea, vomiting, anorexia; leucopenia, proteinuria, renal failure, heart failure and hyponatraemia. |
Drug Interactions |
Reduces tolerance to alcohol; shortens T1/2 of doxycycline. Decreased efficacy of oral contraceptives when used with carbamazepine. Increased plasma concentrations of carbamazepine by propoxyphene. Serum level decreases with phenytoin, phenobarbital, primidone. |
Lab Interactions |
False-positive result in urine sugar, elevated serum alkaline phosphatase and serum bilirubin values. |
Food Interactions |
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects. Food: Carbamazepine serum levels may be increased if taken with food. Carbamazepine serum concentration may be increased if taken with grapefruit juice; avoid concurrent use. Herb/Nutraceutical: Avoid evening primrose (seizure threshold decreased). Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression). |
Mechanism of Actions |
In addition to anticonvulsant effects, carbamazepine has anticholinergic, antineuralgic, antidiuretic, muscle relaxant, antimanic, antidepressive, and antiarrhythmic properties; may depress activity in the nucleus ventralis of the thalamus or decrease synaptic transmission or decrease summation of temporal stimulation leading to neural discharge by limiting influx of sodium ions across cell membrane or other unknown mechanisms; stimulates the release of ADH and potentiates its action in promoting reabsorption of water; chemically related to tricyclic antidepressants |
Metabolism |
Substrate of CYP2C8 (minor), 3A4 (major); Induces CYP1A2 (strong), 2B6 (strong), 2C8 (strong), 2C9 (strong), 2C19 (strong), 3A4 (strong), P-glycoprotein |
Pharmacodynamics |
Absorption: Slow Distribution: Vd: Neonates: 1.5 L/kg; Children: 1.9 L/kg; Adults: 0.59-2 L/kg Protein binding: Carbamazepine: 75% to 90%, may be decreased in newborns; Epoxide metabolite: 50% Metabolism: Hepatic via CYP3A4 to active epoxide metabolite; induces hepatic enzymes to increase metabolism Bioavailability: 85% Half-life elimination: Note: Half-life is variable because of autoinduction which is usually complete 3-5 weeks after initiation of a fixed carbamazepine regimen. Carbamazepine: Initial: 25-65 hours; Extended release: 35-40 hours; Multiple doses: Children: 8-14 hours; Adults: 12-17 hours Epoxide metabolite: Initial: 25-43 hours Time to peak, serum: Unpredictable: Immediate release: Suspension: 1.5 hour; tablet: 4-5 hours Extended release: Carbatrol®, Equetro®: 12-26 hours (single dose), 4-8 hours (multiple doses); Tegretol®-XR: 3-12 hours Excretion: Urine 72% (1% to 3% as unchanged drug); feces (28%) |
Monitoring |
CBC with platelet count, reticulocytes, serum iron, lipid panel, liver function tests, urinalysis, BUN, serum carbamazepine levels, thyroid function tests, serum sodium; pregnancy test; ophthalmic exams (pupillary reflexes); observe patient for excessive sedation, especially when instituting or increasing therapy; signs of rash; HLA-B*1502 genotype screening prior to therapy initiation in patients of Asian descent; suicidality (eg, suicidal thoughts, depression, behavioral changes) |
Administration |
Should be taken with food. (Avoid grapefruit juice.) |
Pregnancy Category |
D: There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. |
Lactation |
Enters breast milk/not recommended |
Storage Conditions |
Oral: Store below 30°C Rectal: Store below 30°C |
ATC Classification |
N03AF01 - carbamazepine ; Belongs to the class of carboxamide derivatives antiepileptic. |
GenericPedia Classification |
|
Storage |
Oral: Store below 30°C Rectal: Store below 30°C |
Available As |
|
Carbamazepine
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Carbamazepine Containing Brands
Carbamazepine is used in following diseases
Drug - Drug Interactions of Carbamazepine
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