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Pharmacokinetics and analgesic effects of intravenous buprenorphine
Author(s) -
Escher M.,
Daali Y.,
Chabert J.,
Hopfgartner G.,
Dayer P.,
Desmeules J.
Publication year - 2005
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2004.12.087
Subject(s) - pharmacokinetics , analgesic , buprenorphine , pharmacodynamics , pharmacology , anesthesia , opioid , clinical pharmacology , placebo , medicine , chemistry , receptor , alternative medicine , pathology
Background buprenorphine (BUP), a semi‐synthetic opioid, is used as an analgesic for post‐operative and chronic pain. Because of very low plasma concentrations its pharmacokinetics and related pharmacodynamics are not well characterized. BUP pharmacokinetics and pharmacodynamics were investigated as part of a study on the efficacy of naltrexone (NTX) in reversing its analgesic effects. Methods randomized double‐blind placebo‐controlled cross‐over study in 12 healthy male volunteers who received 0.15 mg/70 kg BUP iv. Data were collected up to 8 hours after drug administration. Quantitative sensory testing, using thermal and electrical stimulations (Viking IV, Madison USA), and testing for pain tolerance (cold pressor) were performed. Plasma concentrations of BUP were quantified by liquid chromatography‐tandem mass spectrometry. The limit of quantification was 50 pg/mL. Results BUP significantly increased the nociceptive threshold and pain tolerance for the first 2 hours (p<0.05). A two compartment model adequately described BUP pharmacokinetics. The mean elimination half‐life was 3.9h (CV=75%). Plasma clearance was 7.6 L/h (CV=83%), and AUC was 39h ng/mL (CV=87%). Conclusions a two compartment pharmacokinetic model adequately characterizes buprenorphine pharmacokinetics. Significant analgesic effects are observed during the distribution phase. Clinical Pharmacology & Therapeutics (2005) 77 , P51–P51; doi: 10.1016/j.clpt.2004.12.087