Arzneimittel Forsch
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The spinal nociceptive system is the target of various pain depressing agents. It is capable to function without control from the brain. It is activated by tissue damage which, by excitation of nociceptive afferents, evokes activity in axons ascending to the brain (sensory nociceptive response) and in spinal reflex pathways (motor and autonomic responses). ⋯ Ceruletide and cholecystokinin octapeptide depress nociceptive motor responses but do not affect the nociceptive sensory response. This indicates that motor and sensory responses of the spinal nociceptive system are not rigidly linked together. With the help of appropriate drugs, it is possible to manipulate them separately.
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Arzneimittel Forsch · Jan 1984
2-Acetylpyridine thiosemicarbazones. 10. 2-Propionyl-, 2-butyryl-, and 2-(2-methylpropionyl)pyridine thiosemicarbazones as potential antimalarial agents.
In view of the antimalarial properties observed for many 2-acetylpyridine thiosemicarbazones, a series of N4,N4-disubstituted thiosemicarbazones derived from 2-propionyl-, 2-butyryl-, and 2-(2-methylpropionyl)pyridine was prepared for evaluation against the malaria parasite, Plasmodium berghei, in the mouse. The thiosemicarbazones were made by the reaction of methyl hydrazinecarbodithioate with a 2-acylpyridine to give the intermediate methyl 3-[1-2-pyridinyl)alkylidene]hydrazinecarbodithioates. ⋯ The three thiosemicarbazones derived from 3-azabicyclo[3.2.2]nonane were most effective, the greatest potency being exhibited by 3-azabicyclo-[3.2.2]nonane-3-thiocarboxylic acid 2-[1-(2-pyridinyl)butylidene]hydrazide (4) which cured 4/5 mice at a dose of 160 mg/kg. In contrast to the related thiosemicarbazones derived from 2-acetylpyridine, virtually no toxic effects were observed in the series described here.
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Arzneimittel Forsch · Jan 1983
Randomized Controlled Trial Clinical Trial[Treatment of postoperative wound pain with suprofen].
The present randomized double-blind study was performed to investigate the analgesic effects of single doses of suprofen (alpha-methyl-4-(2-thienylcarbonyl)benzene acetic acid; Suprol) 200 mg, suprofen 400 mg paracetamol (APAP, acetaminophen) 650 mg, and combination suprofen 100 mg + APAP 650 mg versus placebo. The five treatment groups were homogeneous as to their demographic features and comprised 28--32 subjects each. Data for a total of 146 patients were evaluated. ⋯ Suprofen 200 mg ranked third. Statistical significance was only seen for the parameter pain intensity (SPID) on comparison of suprofen 100 mg + APAP 650 mg versus suprofen 200 mg. Side effects, homogeneously distributed over the treatment groups, were observed in four cases.
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Arzneimittel Forsch · Jan 1983
Randomized Controlled Trial Comparative Study Clinical Trial[A controlled clinical single-dose comparative study of suprofen and diflunisal].
In a single-dose, double-blind randomized study, the analgesic efficacy of suprofen 200, suprofen (alpha-methyl-4-(2-thienylcarbonyl)-benzene acetic acid; Suprol) 400 mg and diflunisal 750 mg capsules was determined in comparison to placebo capsules. A total of 130 patients participated in the study, all of them requiring analgesic treatment on the first post-operative day following meniscectomy. ⋯ Despite great differences in dosage and half-life, the active test substances must be regarded as equipment. Side effects were reported by 2 patients each in the diflunisal 750 mg and the placebo group, and by 1 patient treated with suprofen 200 mg.
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The antiarrhythmic, local anesthetic and acute local and systemic toxic effects of DL-N-(2-hydroxyethyl)-pipecolinyl-2,6-dimethylanilide (AL-S-1249, droxicainide) and lidocaine were compared in animals. When given intravenously both substances suppressed ouabain-induced arrhythmias in pentobarbital-anesthetized guinea pigs; they were equipotent in this regard and had the same duration of antiarrhythmic action. ⋯ When given intravenously to unanesthetized mice and unanesthetized and pentobarbital-anesthetized rats, the LD50's for droxicainide were consistently higher than those for lidocaine. Since droxicainide has antiarrhythmic and local anesthetic properties that are quantitatively similar to lidocaine but local and systemic toxicity that is relatively weaker, its antiarrhythmic and local anesthetic actions merit further study.