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Eur. J. Clin. Pharmacol. · Jan 1980
Clinical pharmacokinetics and oral bioavailability of ketobemidone.
- U Bondesson, S Arnér, P Anderson, L O Boréus, and P Hartvig.
- Eur. J. Clin. Pharmacol. 1980 Jan 1;17(1):45-50.
AbstractThe 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.
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