Clinical pharmacokinetics and oral bioavailability of ketobemidone.

Abstract

The basic pharmacokinetics and oral bioavailability of ketobenmidone have been studied in 6 patients after surgery. Plasma concentrations were first determined following intravenous administration of Ketogin 2 ml, containing ketobemidone chloride 10 mg and the spasmolytic N,N-dimethyl-3,3-diphenyl-1-methylallylamine chloride 50 mg, and then, on the second postoperative day, following oral administration of 2 tablets of Ketogin, each containing ketobemidone chloride 5 mg and the spasmolytic agent 25 mg. The average oral bioavailability of ketobemiodone was 34% +/- 16% (SD, n = 6). The mean plasma half-life of elimination (t1/2 beta) was about the same following oral (2.45 +/- 0.73 h; SD, n = 5) as after intravenous administration (2.25 +/- 0.35 h; SD, n = 6). The low oral bioavailability and rapid elimination of ketobemidone demonstrated in this study suggest that the usual dosage recommendation for oral Ketogin (ketobemidone 5--10 mg every 6--7 h) in patients with severe pain is too low.

• Authors: U Bondesson, S Arnér, P Anderson, L O Boréus, P Hartvig
• Journal: European journal of clinical pharmacology (Eur J Clin Pharmacol) Vol. 17 Issue 1 Pg. 45-50 (Jan 1980) ISSN: 0031-6970 [Print] Germany
• PMID: 6102913 (Publication Type: Journal Article)

Chemical References

• Analgesics, Opioid
• Drug Combinations
• Allylamine
• ketobemidone, N,N-dimethyl-3,3-diphenyl-1-methylallylamine drug combination
• Meperidine
• ketobemidone

Topics

• Administration, Oral
• Adult
• Allylamine (administration & dosage, analogs & derivatives, metabolism)
• Analgesics, Opioid (administration & dosage, metabolism)
• Biological Availability
• Drug Combinations (administration & dosage, metabolism)
• Female
• Gas Chromatography-Mass Spectrometry
• Humans
• Injections, Intravenous
• Kinetics
• Male
• Meperidine (administration & dosage, analogs & derivatives, metabolism)
• Middle Aged