Autoinduction and steady-state pharmacokinetics of carbamazepine and its major metabolites. 1992

T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
Mental Health Research Centre Russian AMS, Moscow.

1. The effect of carbamazepine (CBZ) dose change on mean plasma concentrations of CBZ, its two metabolites and apparent steady-state clearance was studied in 77 affectively ill patients receiving CBZ at doses of 100-1200 mg day-1. 2. Autoinduction of CBZ metabolism appeared to be complete within 1 week of starting CBZ therapy or dose change, and its degree was linearly related to CBZ daily dose. 3. Curvilinear plots were obtained for steady-state concentrations of CBZ and its -10,11-epoxide metabolite, and for the ratio of CBZ-10,11-epoxide to CBZ level, versus daily dose of CBZ. 4. On the contrary, steady-state concentration of CBZ-10,11-diol increased proportionately with the dose. This indicates that there is no dose dependency in absorption of CBZ, and that dose-dependent autoinduction of CBZ metabolism is the main cause of the curvilinear relationship between dose and steady-state concentration of CBZ and its intermediary metabolite, CBZ-10,11-epoxide.

UI MeSH Term Description Entries
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D002220 Carbamazepine A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties. Amizepine,Carbamazepine Acetate,Carbamazepine Anhydrous,Carbamazepine Dihydrate,Carbamazepine Hydrochloride,Carbamazepine L-Tartrate (4:1),Carbamazepine Phosphate,Carbamazepine Sulfate (2:1),Carbazepin,Epitol,Finlepsin,Neurotol,Tegretol
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults

Related Publications

T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
September 1999, Journal of clinical pharmacology,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
November 1997, Journal of clinical pharmacology,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
June 1990, British journal of clinical pharmacology,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
January 1986, Journal of clinical pharmacology,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
January 1997, Chirality,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
March 1991, Clinical pharmacokinetics,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
January 1986, The Journal of international medical research,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
January 1991, International journal of clinical pharmacology research,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
June 2012, Journal of clinical pharmacy and therapeutics,
T B Kudriakova, and L A Sirota, and G I Rozova, and V A Gorkov
March 1996, Biopharmaceutics & drug disposition,
Copied contents to your clipboard!