Comparative bioavailability of carbimazole and methimazole

• Published in: International journal of clinical pharmacology, therapy, and toxicology Vol. 21; no. 10; p. 505
• Main Authors: Jansson, R, Dahlberg, P A, Lindström, B
• Format: Journal Article
• Language: English
• Published: Germany 01.10.1983
• Subjects: Administration, Oral; Adult; Biological Availability; Carbimazole - administration & dosage; Carbimazole - metabolism; Chromatography, Gas; Female; Half-Life; Humans; Kinetics; Male; Mass Spectrometry; Methimazole - administration & dosage; Methimazole - metabolism
• ISSN: 0174-4879

In this study we investigated the oral bioavailability of therapeutic doses of two antithyroid drugs, methimazole and carbimazole, in seven euthyroid subjects. To increase the statistical power deuterium-labeled methimazole was given orally as an internal standard together with the tested drugs. Using a recently described highly sensitive gas chromatographic-mass spectrometric assay for methimazole we found that intake of 15 mg carbimazole resulted in plasma concentrations of methimazole and pharmacokinetic data comparable to intake of an equimolar amount of methimazole, i. e., 9.2 mg. Maximum concentrations of 163 and 149 ng/ml, respectively, were reached in both instances at 0.9 h after intake of 15 mg carbimazole and 10 mg methimazole. The plasma half-life was 5.7 and 5.4 h, respectively. In contrast to previous suggestions the interindividual differences in pharmacokinetics were small. In conclusion, carbimazole was rapidly and totally bioactivated to methimazole, and the drugs should be regarded as equipotent when compared on a molar basis.