Articles: analgesics.
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Zomepirac sodium (Zomax) is a new orally effective nonopioid analgesic that can relieve mild to severe pain. It is more effective than aspirin or codeine alone and is as effective as analgesic combinations containing codeine or other narcotics. ⋯ Like aspirin, zomepirac has anti-inflammatory and antipyretic actions and inhibits the synthesis of prostaglandins. Zomepirac is generally well tolerated with both short-term and long-term use; gastrointestinal reactions are the most frequently occurring side effects.
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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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Arch Int Pharmacodyn Ther · Jun 1981
The anti-inflammatory, analgesic and antipyretic activities of non-narcotic analgesic drug mixtures in rats.
The effects of non-narcotic analgesics have been examined, separately and in admixture, on carrageenan-induced hind paw oedema and on yeast-induced hyperalgesia and hyperthermia in adult rats. The efficacy of the drugs was evaluated using the kinetics of drug-receptor interaction. In addition, the hypothesis was tested that the anti-inflammatory, analgesic and antipyretic activities of the drug mixtures used equal the addition of the activities of the individual drugs and could be predicted from their intrinsic activities and affinities. ⋯ Incidentally, at some of the higher dose levels potentiation of the activity of the drugs was found. Low doses of the triple combinations: aspirin + paracetamol + caffeine and aspirin + phenacetin + caffeine showed anti-inflammatory and antipyretic activities which were not different from those expected on the basis of addition, but the activities observed with higher doses of these combinations indicated potentiation. It is concluded that, in the rat, the anti-inflammatory, analgesic and antipyretic activities of dual and triple combinations of aspirin, paracetamol, phenacetin and caffeine at least equal the activities expected on the basis of addition.
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Ten years ago, analgesics were studied using crossover designs. In recent years, analgesics have been studied only in parallel designs primarily because biostatisticians do not like crossover studies. The advantages of crossover studies are numerous: (1) patients serve as their own control; (2) there is less variability of responses among patients; and (3) a smaller number of patients is needed to provide statistically significant data. ⋯ One is a crossover study of Percodan with and without naloxone to placebo. The other is a parallel study comparing the effects of propoxyphene with naloxone to those of propoxyphene alone. The results of these studies reaffirm the value of the crossover method of evaluating analgesics.
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Int J Clin Pharmacol Ther Toxicol · Apr 1981
Randomized Controlled Trial Clinical TrialPropiram and codeine in episiotomy pain.
To evaluate relative efficacy, safety, and time course of analgesia, propiram fumarate (50 and 100 mg), a new narcotic agonist-antagonist, was compared with codeine sulfate (60 mg) and placebo in a clinical trial with a single peroral dose, parallel, stratified, randomized, and double-blind design involving 80 hospitalized postpartum women with medium or severe episiotomy pain. Using verbal subjective reports as index of response, patients rated pain intensity and side effects at periodic interviews for 6 h. Relative efficacy findings based on peak effects and summed pain-intensity differences suggested dose-dependent analgesia with propiram and also that 60 mg codeine lay between 50 mg propiram and placebo. ⋯ All three active drugs continued to act until the 5th or 6th h. Drowsiness was the only statistically significant side effect reported after propiram. These results suggest that single 50 or 100 mg doses of propiram were effective in episiotomy pain, induced stronger analgesia than 60 mg codeine, and took effect more rapidly.