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carisoprodol : ウィキペディア英語版 | carisoprodol
Carisoprodol is a centrally acting skeletal muscle relaxant of the carbamate class and produces all the effects associated with barbiturate receptor ligands. It is slightly soluble in water and freely soluble in ethanol, chloroform and acetone. The drug's solubility is practically independent of pH. Carisoprodol is manufactured and marketed in the United States by Meda Pharmaceuticals〔Meda Pharmaceuticals Inc. of Somerset, New Jersey is the U.S. subsidiary of Meda AB of Solna, Sweden 〕 under the brand name Soma, and in the United Kingdom and other countries under the brand names Sanoma and Carisoma. The drug is available by itself or mixed with aspirin, and in one preparation with codeine and caffeine, as well. Although carisoprodol has significant pharmacological activity, its benefit in therapy is likely due mostly to the meprobamate metabolite as meprobamate remains in the system significantly longer and reaches a higher peak plasma concentration than the parent drug a few hours following administration. This is further evidenced by carisoprodol's ability to maintain relevant benefits when administered 3-4 times a day despite its short half-life of only two hours. ==History== On June 1, 1959 several American pharmacologists convened at Wayne State University in Detroit, Michigan to discuss a new drug. The drug, originally thought to have antiseptic properties, was found to have central muscle-relaxing properties.〔Miller JG, ed. The pharmacology and clinical usefulness of carisoprodol. Detroit:Wayne State University; 1959.〕 It had been developed by Frank M. Berger at Wallace Laboratories and was named carisoprodol. Carisoprodol was a modification of meprobamate, intended to have better muscle relaxing properties, less potential for abuse, and less risk of overdose. The substitution of one hydrogen atom with an isopropyl group on one of the carbamyl nitrogens was intended to yield a molecule with new pharmacological properties.
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