A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Rifampicin has a Profound Effect on the Pharmacokinetics of Oral S-Ketamine and Less on Intravenous S-Ketamine
Tekijät: Peltoniemi MA, Saari TI, Hagelberg NM, Laine K, Kurkinen KJ, Neuvonen PJ, Olkkola KT
Kustantaja: WILEY-BLACKWELL
Julkaisuvuosi: 2012
Journal: Basic and Clinical Pharmacology and Toxicology. Supplement
Tietokannassa oleva lehden nimi: BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Lehden akronyymi: BASIC CLIN PHARMACOL
Numero sarjassa: 5
Vuosikerta: 111
Numero: 5
Aloitussivu: 325
Lopetussivu: 332
Sivujen määrä: 8
ISSN: 1742-7835
DOI: https://doi.org/10.1111/j.1742-7843.2012.00908.x
Tiivistelmä
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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