CARBAMAZEPINE [TEGRETOL]

Chewable tablets of 100mgs-red speckled,pink

Tablets of 200mgs- pink tablets
Suspension of 100mgs/5mls

Warnings;
 serious and sometimes life threatening dermatological reactions including toxic epidermal
nectrolysis( TEN) and steven johnson syndrome.
 Aplastic anaemia and agranulocytosis
 Suicidal behaviour and ideation
 Can cause fetal harm(congenital malformations-craniofacial defects,cardiovascular
malformations and hypospadias) when used in pregnancy
Uses; Used as an anticonvulsant( grandmal seizures and psychomotor seizures) and treatment of
trigeminal neuralgia

Mechanisms of action; it appears to work by reducing polysynaptic responses and blocking the post
tetanic potentiation.
It also reduces pain induced by stimulation of infraorbital nerves

Pk-Absorption
Bioavailability: 85% (oral suspension)
Peak serum time: 4.5 hr (immediate-release tablets); 3-12 hr (extended-release
tablets); 1.5 hr (oral suspension)
Distributions
Protein bound: 75-90%
Vd: 1.5 L/kg (neonates); 1.9 L/kg (children); 0.59-2 L/kg (adults)
Metabolism
Via hepatic CYP3A4
Metabolites: Carbamazepine 10,11-epoxide
Enzymes induced: CYP1A2, CYP2C9, CYP3A4
Elimination
Half-life: 25-65 hr (initial dosing); decreases to 10-20 hr after autoinduction; 35-40 hr
(extended release)
Excretion: Urine (72%); feces (28%)

Indications and usage

Epilepsy( apat from petit mal seizures) and in treatment of trigeminal neuralgia

Contraindications: should not be used in patients with a history of previous bone marrow suppression,
hypersensitivity to the drug and any sensitivity to the tricyclic compounds such as
amitriptylin,desipramine,imipramine, protriptyline,norttriptyline. Usage with monoamine oxidase
inhibitors is also not recommended

Agents that may affect tegretol plamsa levels

CYP 3A4 inhibitors- cimetidine,danazol,macrolides,
erythromycin,fluoxetine,loratiidine,isoniazid,valproate,verapamil
CYP 3A4 Inducers-cisplastin,doxorubicin,rifampin, phenobarbital, phenytoin, theophyline