ブプレノルフィン·塩酸塩

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H361：生殖能または胎児への悪影響のおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P281：指定された個人用保護具を使用すること。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P330：口をすすぐこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ブプレノルフィン·塩酸塩 価格

ブプレノルフィン·塩酸塩 化学特性,用途語,生産方法

• 用途

  習慣性医薬品

• 効能

  鎮痛薬, オピオイド受容体作動薬/拮抗薬

• 商品名

  レペタン (大塚製薬); レペタン (大塚製薬)

• 説明

  Buprenorphine (hydrochloride) (CRM) (Item No. ISO60178) is a certified reference material that is structurally categorized as an opioid. It is a partial agonist of the μ-opioid receptor (K_i = 4.18 nM) that less potently acts at δ- and κ-opioid receptors (K_is = 25.8 and 12.9 nM, respectively). Buprenorphine is used, alone or with naloxone (Item Nos. ISO60194 | 15594), to counter opiate addiction. This product is intended for research and forensic applications.

• 化学的特性

  White Solid

• 使用

  Controllled substance (narcotic). Analgesic that demonstrates narcotic agonist-antagonist properties.

• 定義

  ChEBI: The hydrochloride salt of buprenorphine.

• 獲得抵抗性

  Buprenorphine is 20 to 50 times more potent than morphine in producing an ED50 analgesic effect in animal studies; however, it cannot produce an ED100 (compared to morphine) in these tests. Thus, buprenorphine is a potent partial agonist at μ opioid receptors. It also is a partial agonist at κreceptors but more of an antagonist at δ receptors. Buprenorphine, at 0.4 mg intramuscular dose, will produce the same degree of analgesia as 10 mg of morphine. Because of its partial agonist properties, it has a lower ceiling on its analgesic action but also produces less severe respiratory depression. It is incapable of producing tolerance and addiction comparable to full μ agonists. In fact, buprenorphine's partial agonist action, very high affinity for opioid receptors, and high lipophilicity combine to give buprenorphine a tolerance, addiction, and withdrawal profile that is unique among the opioids. When given by itself to opioid-naive patients, little tolerance or addictive potential (Schedule 5) is observed. A mild withdrawal can occur some 2 weeks after the last dose of buprenorphine. Buprenorphine will precipitate withdrawal symptoms in highly addicted individuals, but it will suppress symptoms in individuals who are undergoing withdrawal from opioids. It effectively blocks the effect of high doses of heroin. Because of these properties, buprenorphine has been approved for office-based use in treating opioid dependence. It also has been reported to suppress cocaine use and addiction.

• 生物活性

  ORL 1 receptor agonist that also displays mixed antagonist/partial agonist activity at κ , δ and μ -opioid receptors.

• 臨床応用

  Buprenorphine undergoes extensive first-pass 3-O-glucuronidation, which negates its usefulness after oral dose. It is available in parenteral and sublingual dosage forms. The typical dose is 0.3 to 0.6 mg three times per day by intramuscular injection for analgesia or 8 mg/day as a sublingual tablet for opioid-dependence maintenance. The duration of analgesic effect is 4 to 6 hours. After parenteral dose, approximately 70% of the drug is excreted in the feces, and the remainder appears as N-dealkylated and conjugated metabolites in the urine. Naloxone is not an effective antagonist to buprenorphine because of the latter's high binding affinity to opioid receptors.

53152-21-9, ブプレノルフィン·塩酸塩 キーワード