|
Oxymorphone (Opana, Numorphan, Numorphone) or 14-Hydroxydihydromorphinone is a powerful semi-synthetic opioid analgesic (painkiller) first developed in Germany in 1914, patented in the USA by Endo Pharmaceuticals in 1955 and introduced to the United States market in January 1959 and other countries around the same time.〔 The brand name Numorphan is derived by analogy to the Nucodan name for an oxycodone product (or vice versa) as well as Paramorphan/Paramorfan for dihydromorphine and Paracodin (dihydrocodeine). The only commercially available salt of oxymorphone in most of the world at this time is the hydrochloride, which has a free base conversion ratio of 0.891, and oxymorphone hydrochloride monohydrate has a factor of 0.85.〔 It is a Schedule II controlled substance in the United States with an ACSCN of 9652. The 2013 DEA annual manufacturing quotas were 18 375 kilos for conversion (a number of drugs can be made from oxymorphone, both painkillers and opioid antagonists like naloxone) and 6875 kilos for direct manufacture of end-products.〔http://www.deadiversion.usdoj.gov/fed_regs/quotas/2013/fr0620.htm〕 The onset of analgesia after parenteral administration is about 5–10 minutes and after rectal administration, 15–30 minutes.〔 The duration of analgesia is 3–4 hours for immediate-release tablets and 12 hours for extended-release tablets.〔 It is also a minor metabolite of oxycodone, which is formed by CYP2D6-mediated O-demethylation.〔 == Uses == Oxymorphone is indicated for the relief of moderate to severe pain and also as a preoperative medication to alleviate apprehension, maintain anaesthesia and as an obstetric analgesic. Additionally, it can be used for the alleviation of pain in patients with dyspnoea associated with acute left ventricular failure and pulmonary oedema. It is practically devoid of antitussive activity.〔 Opana extended-release tablets are indicated for the management of chronic pain and are indicated only for patients already on a regular schedule of strong opioids for a prolonged period. The immediate-release Opana tablets are recommended for management of breakthrough pain for patients on the extended-release version. Some protocols for chronic pain conditions characterised by severe breakthrough pain incidents add Numorphan ampoules as a third form of the drug for use when a breakthrough pain incident is in progress. An oxymorphone nasal spray is being developed for this purpose but the release date is unknown; some practitioners prefer fentanyl immediate-release formulations such as Actiq or Fentora for this purpose although some patients have severe side effects from fentanyl. Oxymorphone is mentioned, along with buprenorphine, oxycodone, dihydrocodeine, morphine and other opioids as a possible means of mitigating refractory depression. 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「Oxymorphone」の詳細全文を読む スポンサード リンク
|