A1 Refereed original research article in a scientific journal
Rifampicin has a Profound Effect on the Pharmacokinetics of Oral S-Ketamine and Less on Intravenous S-Ketamine
Authors: Peltoniemi MA, Saari TI, Hagelberg NM, Laine K, Kurkinen KJ, Neuvonen PJ, Olkkola KT
Publisher: WILEY-BLACKWELL
Publication year: 2012
Journal: Basic and Clinical Pharmacology and Toxicology. Supplement
Journal name in source: BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Journal acronym: BASIC CLIN PHARMACOL
Number in series: 5
Volume: 111
Issue: 5
First page : 325
Last page: 332
Number of pages: 8
ISSN: 1742-7835
DOI: https://doi.org/10.1111/j.1742-7843.2012.00908.x
Abstract
Low-dose ketamine is currently used in several acute and chronic pain conditions as an analgesic. Ketamine undergoes extensive metabolism and is thus susceptible to drugdrug interactions. We examined the effect rifampicin, a well-known inducer of many cytochrome P450 (CYP) enzymes and transporters, on the pharmacokinetics of intravenous and oral S-ketamine in healthy volunteers. Eleven healthy volunteers were administered in randomized order 600 similar to mg rifampicin or placebo orally for 6 similar to days in a four-session paired cross-over study. On day 6, S-ketamine was administered intravenously (0.1 similar to mg/kg) in the first part of the study and orally (0.3 similar to mg/kg) in the second part. Plasma concentrations of ketamine and norketamine were measured up to 24 similar to hr and behavioural and analgesic effects up to 12 similar to hr. Rifampicin treatment decreased the mean area under the plasma ketamine concentrationtime curve extrapolated to infinity (AUC 08) of intravenous and oral S-ketamine by 14% (p similar to=similar to 0.005) and 86% (p similar to
Low-dose ketamine is currently used in several acute and chronic pain conditions as an analgesic. Ketamine undergoes extensive metabolism and is thus susceptible to drugdrug interactions. We examined the effect rifampicin, a well-known inducer of many cytochrome P450 (CYP) enzymes and transporters, on the pharmacokinetics of intravenous and oral S-ketamine in healthy volunteers. Eleven healthy volunteers were administered in randomized order 600 similar to mg rifampicin or placebo orally for 6 similar to days in a four-session paired cross-over study. On day 6, S-ketamine was administered intravenously (0.1 similar to mg/kg) in the first part of the study and orally (0.3 similar to mg/kg) in the second part. Plasma concentrations of ketamine and norketamine were measured up to 24 similar to hr and behavioural and analgesic effects up to 12 similar to hr. Rifampicin treatment decreased the mean area under the plasma ketamine concentrationtime curve extrapolated to infinity (AUC 08) of intravenous and oral S-ketamine by 14% (p similar to=similar to 0.005) and 86% (p similar to
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