|
Viminol (marketed under the brandname Dividol) is an opioid analgesic developed by a team at the drugs company Zambon in the 1960s. Viminol is based on the α-Pyrryl-2-Amino-Ethanol structure unlike any other class of opioids;〔Contri AM. Chromatographic separation of diastereoisomers of aminoalcohol salts and their densitometric determination. (Italian). ''Il Farmaco''. 1981 Apr;36(4):215-22.〕〔Neto JM, Murad JE, Monteiro SS. Psychopharmacological properties of the viminol-p-hydroxybenzoate. ''Revista Brasileira de Pesquisas Medicas e Biologicas''. 1977 Dec;10(6):361-8.〕 Viminol has both antitussive (cough suppressing) and analgesic (pain reducing) effects. It has six different stereoisomers which have varying properties. 4 are inactive, the 1S-(R,R)-disecbutyl isomer being a μ-opioid full agonist around 5.5 times more potent than morphine while the 1S-(S,S)-disecbutyl isomer is an antagonist.〔US Patent 3857857 - Davide Della Bella, Carlo Veneziani Bresso, Dario Chiarnio Monza & Uberio Maria Tiotino 'Stereoisomers of 1(1'(-O-Chlorobenzyl)-2'-Pyrryl)-2-Disec.Butylamino-Ethanol'〕〔Shook JE, Kallman MJ, Dewey WL. The discriminative stimulus properties of the R2 isomer of viminol. ''Pharmacology, Biochemistry and Behaviour''. 1984 Jan;20(1):59-62.〕 Since vimonol is supplied as a racemic mixture of isomers, the overall effect produces a mixed agonist–antagonist profile similar to that of opioids such as pentazocine, although with somewhat fewer side effects.〔Cinelli M, Costa V, Ventresca GP, Lodola E. Viminol R2 analgesic activity in patients with postoperative pain: comparison with pentazocine. ''International Journal of Clinical Pharmacology, Therapy and Toxicology''. 1986 May;24(5):232-5.〕 Later work〔US Patent 4148907〕 showed that replacing the -Cl moiety with an -F or a -CF3 produced a compound with twice the potency and half the acute toxicity. A later team at Zambon modified the pyrrolidine with a pyrrolidone〔US Patent 4960788〕 could produce an analogue some 318x morphine in its analgesic activity in animal studies (the latter overlays beta hydroxy fentanyl). A number of related compounds were found to be active allowing a QSAR to be constructed. Viminol has similar effects to other opioids, and produces analgesia, sedation and euphoria. ==Side Effects== Side effects are similar to other opioids, and can include: * Itching * Nausea * Sedation * Respiratory depression - can be potentially life-threatening However, since viminol is supplied as a racemic mixture of agonist and antagonist isomers, the abuse potential and respiratory depression tends to be less than that of μ-opioid full agonist drugs. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Viminol」の詳細全文を読む スポンサード リンク
|