Effect of alosetron on the pharmacokinetics of alprazolam.
Article Details
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D'Souza DL, Levasseur LM, Nezamis J, Robbins DK, Simms L, Koch KM
Effect of alosetron on the pharmacokinetics of alprazolam.
J Clin Pharmacol. 2001 Apr;41(4):452-4.
- PubMed ID
- 11304902 [ View in PubMed]
- Abstract
Lotronex (alosetron hydrochloride) is a 5-HT3 receptor antagonist indicated for the treatment of irritable bowel syndrome (IBS) in females whose predominant bowel habit is diarrhea. Alosetron is extensively metabolized by multiple cytochrome P450 (CYP) enzymes, including CYP 2C9 and 3A4. Alprazolam is a short-acting benzodiazepine commonly prescribed for the treatment of anxiety disorders and a potential comedication in patients with IBS. Alprazolam is extensively metabolized by CYP3A4. This clinical study was conducted to assess the potential for a metabolic drug interaction between these two CYP3A4 substrates. This was an open-label, randomized, two-period, crossover study in 12 healthy female and male volunteers to determine the effect of concomitant administration of alosetron at the recommended dose of 1 mg p.o. bid on the pharmacokinetics of alprazolam following a single oral 1 mg dose. The results showed no effect of alosetron on the pharmacokinetics of alprazolam. Mean alprazolam AUC was 210 and 202 ng.h/mL in the absence and the presence of alosetron, respectively. Therefore, alprazolam may be safely coadministered with alosetron without the need for dosage adjustment.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Alosetron Cytochrome P450 2C9 Protein Humans NoSubstrateDetails Alosetron Cytochrome P450 3A4 Protein Humans UnknownSubstrateDetails