デクストロプロポキシフェン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H225：引火性の高い液体および蒸気

  H319：強い眼刺激

• 注意書き

  P210：熱/火花/裸火/高温のもののような着火源から遠ざ けること。－禁煙。

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

  P403+P235：換気の良い場所で保管すること。涼しいところに 置くこと。

デクストロプロポキシフェン 化学特性,用途語,生産方法

• 効能

  鎮痛薬, オピオイド受容体作動薬

• 使用

  Analgesic.

• 定義

  ChEBI: The (1S,2R)-(+)-diastereoisomer of propoxyphene.

• 生物学の機能

  Propoxyphene (dextropropoxyphene; Darvon) is structurally related to methadone but is much less potent as an analgesic. Compared with codeine, propoxyphene is approximately half as potent and is indicated for the treatment of mild pain. It is not antipyretic or antiinflammatory like aspirin and is less useful than aspirin in most cases of mild pain. Toxicity from propoxyphene, especially in combination with other sedatives, such as alcohol, has led to a decrease in its use. Death following ingestion of alcohol in combination with propoxyphene can occur rapidly (within 20 minutes to 1 hour). The drug is not indicated for those with histories of suicide or depressive illnesses.
  Like meperidine, propoxyphene has an active metabolite, norpropoxyphene, that is not analgesic but has excitatory and local anesthetic effects on the heart similar to those of quinidine. Use of the drug during pregnancy is not safe.Teratogenic effects have been observed in newborns, as have withdrawal signs at birth. As with morphine, propoxyphene requires adequate hepatic and renal clearance to prevent toxicity and drug accumulation. It is thus contraindicated in the elderly patient and those with renal or liver disease.
  Propoxyphene interacts with several drugs. The use of sedatives in combination with propoxyphene can be fatal. In addition, the metabolism of the drug is increased in smokers due to induction of liver enzymes. Thus, smokers may require a higher dose of the drug for pain relief. Propoxyphene enhances the effects of both warfarin and carbamazepine and may increase the toxicity associated with both drugs, such as bleeding and sedation, respectively.
  The abuse liability of propoxyphene is low because of the extreme irritation it causes at the site of injection. Oral use is the preferred route of administration for this reason.

• 一般的な説明

  Most of the structural changes to the methadone skeletonresulted in compounds with decreased opioid potencies, thusmost of these compounds, with the exception of LAAM werenot developed. Propoxyphene is a derivative of methadonemarketed in 1957 as the enantiomerically pure (2S, 3R)-4-(Dimethylamino)-3-methyl-1,2,-diphenyl-2-butanol propionate(ester). It is only about 1/10th as potent as morphine asan analgesic yet retains all the same opioid adverse effects.One propoxyphene 65-mg capsule has the same analgesic effectof 650 mg of aspirin or 1,000 mg of acetaminophen, thusoverdoses of propoxyphene can occur if patients do not followthe prescribed dose. Between 1981 and 1999, 2,110 accidentaldeaths were reported because of propoxyphene.Propoxyphene and all propoxyphene combination productsare listed using the Beers criteria as medications to avoid inpatients older than 65 years of age. The metabolism ofpropoxyphene also contributes to the potential dangers of thedrug. Propoxyphene is metabolized via N-demethylation toform norpropoxyphene. Norpropoxyphene has been shownto build up in cardiac tissues and result in naloxone-insensitivecardiotoxicity. The weak analgesic action and potentialrisk to the patient have some health practitioners advocatingto remove all drugs containing propoxyphene from the market.The hydrochloride salt is marketed as Darvon, the napsylatesalt as Darvon-N, both salts are also available combinedwith acetaminophen (Darvocet, Darvocet-N) and apropoxyphene, aspirin, caffeine product is also available.

• 安全性プロファイル

  Poison by ingestion, intraperitoneal, subcutaneous, and intravenous routes. Human systemic effects by ingestion: change in cardiac rate, respiratory depression, and coma. When heated to decomposition it emits toxic fumes of NOx.

469-62-5, デクストロプロポキシフェン キーワード