In vitro embryotoxicity of carbamazepine and carbamazepine-10,11-epoxide
β Scribed by Hansen, Deborah K.; Dial, Stacey L.; Terry, Ketti K.; Grafton, Thomas F.
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- English
- Weight
- 695 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0040-3709
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β¦ Synopsis
Carbamazepine
(Tegretol", CBZ) is an anticonvulsant drug that is very effective in the treatment of tonic-clonic seizures and is gaining acceptance as a treatment for various psychiatric disorders. The drug is embryotoxic in rodents and has been reported to produce neural tube defects in approximately 1 % of prenatally exposed human offspring. It is metabolized by the cytochrome P-450 system to a stable, pharmaco-'93). A recent case-control study found a n excess of in-
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Carbamazepine-lO,l l-epoxide is a metabolite of carbamazepine that has been identified in the urine OT the rat and in the urine and plasma of marV and which, in the rat, has been shown to have antiepileptic properties comparable to those of the parent drug. It has therefore been suggested3 that, in
A highly-sensitive microcolumn HPLC method for the simultaneous determination of carbamazepine and carbamazepine-l0,ll-epoxide in human serum and saliva is described. The method was successfully employed for the study of pharmacokinetics of carbamazepine in humans. After oral administration of 100 a
The in vivo serum protein binding characteristics of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZ-E) were assessed in sera from 23 paediatric patients on CBZ monotherapy. We assumed that CBZ and CBZ-E binding to serum proteins comprised specific binding sites on alpha 1-acid glycoprotein