Carbamazepine

Carbamazepine
TEGRETOL (carbamazepine) tablet, chewable , TEGRETOL (carbamazepine) suspension , TEGRETOL (carbamazepine) tablet , TEGRETOL XR (carbamazepine) tablet, extended release® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Carbamazepine
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [2]

For patient information about Carbamazepine, click here.

Synonyms / Brand Names: Tegretol^®, Biston^®, Calepsin^®, Carbatrol^®, Epitol^®, Equetro^®, Finlepsin^®, Sirtal^®, Stazepine^®, Telesmin^®, Timonil^®, Trimonil^®, Epimaz^®, Degranol^®.

Overview

Carbamazepine

File:Carbamazepine.png
File:Carbamazepine 3D.png
Clinical data
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	N03AF01 (WHO)
Legal status
Legal status	UK: POM (Prescription only)
Pharmacokinetic data
Bioavailability	80%
Protein binding	76%
Metabolism	Hepatic—by CYP3A4, to active epoxide form (carbamazepine-10,11 epoxide)
Elimination half-life	25–65 hours
Excretion	2–3% excreted unchanged in urine
Identifiers
IUPAC name 5H-dibenz[b,f]azepine-5-carboxamide
CAS Number	298-46-4 85756-57-6 (dihydrate)
PubChem CID	2554
DrugBank	APRD00337
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C15H12N2O
Molar mass	236.269 g/mol

Carbamazepine ("CBZ") is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy and bipolar disorder. It is also used to treat ADD, ADHD, schizophrenia and trigeminal neuralgia.

History

Carbamazepine was discovered by chemist Walter Schindler at J.R. Geigy AG (now part of Novartis) in Basel, Switzerland, in 1953. Schindler then synthesized the drug in 1960, before its anti-epileptic properties had been discovered.

Carbamazepine was first marketed as a drug to treat trigeminal neuralgia in 1962. It has been used as an anticonvulsant in the UK since 1965, but only approved in the U.S. since 1974.

Adverse effects

Carbamazepine renders certain methods of hormonal contraception ineffective because it is an enzyme inducer of the cytochrome P450 system which metabolises the oral contraceptive, leaving less active contraceptive in the plasma.

Common side effects include drowsiness, motor coordination impairment and/or upset stomach. Carbamazepine preparations can greatly decrease alcohol tolerance.

Less common side effects include cardiac arrhythmias, blurry or double vision and/or the temporary or mild loss of blood cells or platelets. In rare cases the latter can be life-threatening if unnoticed, so frequent blood tests are required during the first few months' use, followed by three or four tests per year. In the UK testing would be less frequent in long-term use, typically once every year or two. Underactivity of the thyroid gland may be provoked, so thyroid function tests are advisable every year or two.

Small reductions in white cell count and serum sodium are common.

There are also reports of an auditory side effect, whereby patients perceive musical notes about a semitone lower than their actual pitch (so middle C would be heard as the note B3 just below it, etc).

Oxcarbazepine, a derivative of carbamazepine, has fewer and less serious side effects.

Carbamazepine may cause SIADH (syndrome of inappropriate antidiuretic hormone), since it both increases the release and potentiates the action of ADH (vasopressin).

Carbamazepine may aggravate juvenile myoclonic epilepsy, so it is important to mention any history of jerking, especially in the morning, before starting to take this drug.

Pregnant women taking carbamazepine for seizures are putting their fetuses at increased risk for teratogenic effects and should be given folic acid supplementation and undergo prenatal ultrasonography for diagnosis.

In addition, carbamazepine has been linked to serious adverse cognitive effects, including EEG slowing and cell apoptosis.

TEGRETOL (carbamazepine) tablet,chewable, TEGRETOL (carbamazepine) suspension, TEGRETOL (carbamazepine) tablet, TEGRETOL XR (carbamazepine) tablet, extended release Normal 0 false false false EN-US X-NONE X-NONE

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of Action

    By inhibiting mEH, valproic acid and valnoctamide cause a buildup of the active metabolite, prolonging the effects of carbamazepine and delaying its excretion.

Carbamazepine,as CYP 450 inducer, may increase clearance of many drugs, decreasing their blood levels.

See also

• Oxcarbazepine

External links

• Carbatrol website
• Equetro website
• TA warning
• Carbamazepine overview from PsychEducation.org
• U.S. Patent 2,948,718, August 1960

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