Articles: opioid-analgesics.
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Drug Metab. Dispos. · Jul 1981
Comparative StudyQuantitative determination of the urinary excretion of ketobemidone and four of its metabolites after intravenous and oral administration in man.
The urinary excretion of ketobemidone and its metabolites has been quantified in man after intravenous and oral administration. The metabolism of ketobemidone was found to proceed via 4 metabolic pathways: N-demethylation, ring-hydroxylation, O-methylation, and conjugation. The metabolites were isolated and identified after hydrolysis of the corresponding conjugates. ⋯ Norketobemidone constituted 10-37% of the dose irrespective of route of administration. 4'-Hydroxyketobemidone amounted to 3-12% of the dose. Neither ketobemidone N-oxide nor metabolites formed after reduction of ketobemidone could be detected in the urine. Less than 2% of the dose was found in feces after iv administration.
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Randomized Controlled Trial Comparative Study Clinical Trial
Adverse effects of commonly ordered oral narcotics.
Approximately equianalgesic oral doses of codeine, an oxycodone compound resembling Percodan, and pentazocine were compared for adverse effects in a double-blind, randomized study of four doses of each drug given over two days to 247 postsurgical patients with pain. Placebo and parenteral morphine were also treated as negative and positive controls, respectively. Approximately 50 patients each received one of the five drugs. ⋯ One capsule of oxycodone compound was the analgesic equivalent of 12.5 mg morphine with an adverse effect incidence of 4 per cent (placebo 8 per cent). Smoking made no difference in analgesic effect or adverse effects. Analgesics given in the evening intervening between the two days may have affected the analgesic performance of placebo.
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Comparative Study
Respiratory effects of a new opiate analgesic, R 39209, in the rabbit: comparison with fentanyl.
The respiratory effects of R 39209, a new short-acting analgesic, were studied and compared with those of fentanyl, in the rabbit. Minute volume, respiratory frequency and pH, PCO2 and standard bicarbonate of arterialized venous blood were measured. ⋯ Fentanyl was between 2 and 3.5 times more potent than R 39209. Repeated doses of R 39209 produced reproducible peak effects even when only 10 min was allowed between administrations.