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Pharmacokinetics and bioequivalence of the main metabolites of selegiline: desmethylselegiline, methamphetamine and amphetamine after oral administration of selegiline.
- Source :
-
International journal of clinical pharmacology and therapeutics [Int J Clin Pharmacol Ther] 1997 Jan; Vol. 35 (1), pp. 9-13. - Publication Year :
- 1997
-
Abstract
- A bioavailability study of 2 different selegiline preparations were conducted in 20 healthy volunteers to test the bioequivalence. Almost no bioavailability study of selegiline has been published. As plasma levels of selegiline are very low and the elimination half-life is very short being about 9 minutes, therefore, a very sensitive and selective method for determining the 3 main metabolites desmethylselegiline (DMS), methamphetamine (MA) and amphetamine (A) was developed. After application of a single oral dose of 5 mg selegiline the Cmax values of DMS reached 5-6 ng/ml, of MA 6-7 ng/ml and of A about 2 ng/ml. The AUC infinity values were with DMS about 11 ng/ml x h +/- 4.5, with MA about 130 g/ml x h +/- 50 and with A about 50 ng/ml x h +/- 15. The 90% confidence interval was with logarithmic transformed AUC infinity values 92-107% with DMS, 89-107% with MA, and 84-104% with A. The logarithmic transformed Cmax values showed a 90% confidence interval of 92-127% with DMS, 91-101% with MA, and 90-103% with A. All relevant pharmacokinetic parameters showed bioequivalence with all 3 metabolites (DMS, MA, and A).
- Subjects :
- Administration, Oral
Adult
Biological Availability
Half-Life
Humans
Male
Monoamine Oxidase Inhibitors administration & dosage
Monoamine Oxidase Inhibitors pharmacokinetics
Selegiline administration & dosage
Selegiline pharmacokinetics
Therapeutic Equivalency
Amphetamine pharmacokinetics
Amphetamines pharmacokinetics
Central Nervous System Stimulants pharmacokinetics
Methamphetamine pharmacokinetics
Monoamine Oxidase Inhibitors metabolism
Selegiline metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0946-1965
- Volume :
- 35
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- International journal of clinical pharmacology and therapeutics
- Publication Type :
- Academic Journal
- Accession number :
- 9021435