オキシモルホン

オキシモルホン 化学特性,用途語,生産方法

効能

麻薬性鎮痛薬, オピオイド受容体作動薬

化学的特性

Crystalline Solid

使用

Controlled substance (opiate). Analgesic (narcotic)

生物学の機能

Oxymorphone is 10 times as potent as morphine, with actions similar to those of hydromorphone. Oxymorphone, however, has little antitussive activity, and as such is a useful analgesic in patients with pulmonary disease who need to retain the ability to cough.

一般的な説明

Oxymorphone is the 14 beta-hydroxyl version of hydromorphone,analogous to the hydrocodone, oxycodone pair discussedabove. Although the addition of the 14 beta-hydroxylgroup to hydrocodone (30 mg) yielded oxycodone (20 mg),a more potent drug, the opposite is true for the conversion ofhydromorphone (7.5 mg) to oxymorphone (10 mg). The reasonfor this is that the oral bioavailability of oxymorphone(10%) is lower than that of hydromorphone (35%) becauseof decreased absorption and increased first-pass metabolism.Presumably, the addition of the OH group does increaseits binding affinity at the receptor as the injectableform of oxymorphone (1 mg) is more potent than injectablehydromorphone (1.5 mg).
Oxymorphone is available as a suppository (5 mg), an injection(1 mg/mL), an immediate-release tablet (5 mg, 10mg), and in 2003 the FDA approved a sustained release formulation(Opana ER 5 mg, 10 mg, 20 mg, and 40 mg). The12-hour coverage of the extended release tablet provides anotheroption for those patients suffering from chronic pain.The side effect profile of the extended release formulationsof morphine, oxycodone, and oxymorphone are similar, andthere appears to be no clear advantage of one over the other.

オキシモルホン 上流と下流の製品情報

原材料

準備製品

76-41-5(オキシモルホン)キーワード:

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• 76-41-5
• (5a)-4,5-Epoxy-3,14-dihydroxy-17-methyl-morphinan-6-one
• NIH 10323
• NSC 19045
• 4,5-Epoxy-3,14-dihydroxy-N-methyl-6-oxomorphinan
• OXYMORPHONE (MW 301.35)
• Oxymorphone (base and/or unspecified salts)
• (14S)-14-Hydroxydihydromorphinone
• 14-Hydroxydihydromorphinone
• 3,14-dihydroxy-4,5-alpha-epoxy-17-methyl-morphinan-6-on
• 3,14-Dihydroxy-4,5-alpha-epoxy-17-methylmorphinan-6-one
• 4,5alpha-Epoxy-3,14-dihydroxy-17-methylmorphinan-6-one
• 5-epoxy-3,14-dihydroxy-17-methyl-(5-alpha)-morphinan-6-on
• 7,8-Dihydro-14-hydroxymorphinone
• Dihydro-14-hydroxymorphinone
• Dihydro-14-hydroxymorphinonel 14-hydroxydihydromorphinone
• Dihydrohydroxymorphinone
• Dihydroxymorphinone
• Morphinan-6-one, 3,14-dihydroxy-4,5-alpha-epoxy-17-methyl-
• Morphinan-6-one, 4,5alpha-epoxy-3,14-dihydroxy-17-methyl-
• Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-methyl-, (5alpha)-
• Morphinone, dihydro-14-hydroxy-
• Numorphan
• Oxymorphine
• OXYMORPHONE
• Oxymorphone CII (500 mg)
• Oxymorphone solution
• 4,5α-Epoxy-3,14-dihydoroxy-17-methylmorphinan-6-one
• 4,5α-Epoxy-3,14-dihydroxy-17-methylmorphinan-6-one
• Oxymorphone (CRM)
• (4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
• 17-メチル-3,14-ジヒドロキシ-4,5α-エポキシモルフィナン-6-オン
• 4,5α-エポキシ-3,14-ジヒドロキシ-6-オキソ-17-メチルモルフィナン
• ジヒドロヒドロキシモルヒノン
• 4,5α-エポキシ-3,14-ジヒドロキシ-17-メチルモルフィナン-6-オン
• オキシモルフォン
• ジヒドロヒドロキシモルフィノン
• オキシモルホン
• (1S,5R,13R,17S)-10,17-ジヒドロキシ-4-メチル-12-オキサ-4-アザペンタシクロ[9.6.1.01,13.05,17.07,18]オクタデカ-7,9,11(18)-トリエン-14-オン
• 麻薬性鎮痛薬