ブトルファノール
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- CAS番号.
- 42408-82-2
- 化学名:
- ブトルファノール
- 别名:
- 17-(シクロブチルメチル)モルフィナン-3,14-ジオール;ブトルファノール;(1S,9R,10S)-17-(シクロブチルメチル)-17-アザテトラシクロ[7.5.3.01,10.02,7]ヘプタデカ-2,4,6-トリエン-4,10-ジオール
- 英語名:
- BUTORPHANOL
- 英語别名:
- 17-(cyclobutylmethyl)-morphinan-14-diol;C06863;l-BC 2627;BUTORPHANOL;Levo-BC 2627;BC 2627, (-)-;(-)-Butorphanol;17-(cyclobutylmethyl)morphinan-3,14-diol;l-3,14-Dihydroxy-N-(cyclobutylmethyl)morphinan;(-)-17-(Cyclobutylmethyl)-3,14b-dihydroxymorphinan
- CBNumber:
- CB6728719
- 化学式:
- C21H29NO2
- 分子量:
- 327.46
- MOL File:
- 42408-82-2.mol
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ブトルファノール 物理性質
- 融点 :
- 215-217°
- 比旋光度 :
- D -70.0° (c = 0.1 in methanol)
- 沸点 :
- 507.3±50.0 °C(Predicted)
- 比重(密度) :
- 1.24±0.1 g/cm3(Predicted)
- 酸解離定数(Pka):
- pKa 8.6 (Uncertain)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
絵表示(GHS) |
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注意喚起語 |
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危険有害性情報 |
コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
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P264, P270, P301+P312, P330, P501 |
H317 |
アレルギー性皮膚反応を起こすおそれ |
感作性、皮膚 |
1 |
警告 |
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P261, P272, P280, P302+P352,P333+P313, P321, P363, P501 |
H332 |
吸入すると有害 |
急性毒性、吸入 |
4 |
警告 |
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P261, P271, P304+P340, P312 |
H334 |
吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ |
感作性、呼吸器 |
1 |
危険 |
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P261, P285, P304+P341, P342+P311,P501 |
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注意書き |
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。 |
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。 |
P271 |
屋外または換気の良い場所でのみ使用すること。 |
P272 |
汚染された作業衣は作業場から出さないこと。 |
P285 |
換気が十分でない場合には、呼吸用保護具を着用する 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。 |
P304+P340 |
吸入した場合:空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。 |
P304+P341 |
吸入した場合:呼吸が困難な場合には、空気の新鮮な場 所に移し、呼吸しやすい姿勢で休息させること。 |
P312 |
気分が悪い時は医師に連絡すること。 |
P330 |
口をすすぐこと。 |
P342+P311 |
呼吸に関する症状が出た場合:医師に連絡すること。 |
P501 |
内容物/容器を...に廃棄すること。 |
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ブトルファノール 化学特性,用途語,生産方法
効能
鎮痛薬, 鎮咳薬, オピオイド受容体作動/拮抗薬
使用
Mixed opioid agonist-antagonist. Analgesic (narcotic); antitussive.
Controlled substance.
定義
ChEBI: Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is
sed as its (S,S)-tartaric acid salt for relief or moderate to severe pain.
生物学の機能
Butorphanol (Stadol) is chemically related to levorphanol
but pharmacologically similar in action to pentazocine.
As an opioid antagonist it is nearly 30 times as
potent as pentazocine and has one-fortieth the potency
of naloxone. It is a potent opioid analgesic indicated for
the relief of moderate to severe pain. Its potency is 7
times that of morphine and 20 times that of pentazocine
as an analgesic. Its onset of action is similar to that of
morphine.The side effects and signs of toxicity are similar
to those produced by pentazocine. It produces excitatory
effects and sedation and precipitates withdrawal
in opioid-dependent patients. Although generally administered
parenterally because of its low bioavailability
following oral administration, it is also unique in that
a nasal spray formulation is available.The nasal spray is
indicated for the relief of postoperative pain and migraine
headache. The low molecular weight of butorphanol,
its high lipophilicity, and its lack of vasoconstrictor
effects make it particularly suitable for nasal
administration.
Nasal administration of butorphanol decreases the
onset of action to 15 minutes and decreases the firstpass
effect of the drug, which increases bioavailability.
Generally the patient sprays a set dose of 1 mg per hour
for 2 hours. The duration of action is 4 to 5 hours.
The convenience of such administration is a major advantage to patients requiring repeat dosing. The
abuse potential following such administration has not
been extensively studied, although it is thought to be
small. Butorphanol is not a federally controlled
(“scheduled”) drug, so physicians are not required to
obtain the licenses and security safeguards required for
other opioid analgesics.
Adverse effects, contraindications, and drug interactions
are similar to those for pentazocine and morphine.
一般的な説明
Structurally, butorphanol is a morphinan and shares the samecyclobutyl methyl group on the nitrogen as nalbuphine. Likenalbuphine, butorphanol is an agonist at the κ-receptor but atthe μ-receptor butorphanol is both a partial agonist and anantagonist. The affinity for opioid receptors in vitro is1:4:25 for the μ-, δ-, and κ-receptors respectively. Thehigh affinity for the κ-receptors is proposed to give butorphanolits analgesic properties and is also responsible for theCNS adverse effects such as hallucinations, psychosis, andparanoid reactions. Butorphanol binds with μ-receptors as apartial agonist, and administration to humans maintained onhigh-potency μ-agonists such as morphine may precipitatewithdrawal. Butorphanol was found to produce convulsionsin morphine-deprived, morphine-dependent monkeys.
ブトルファノール 上流と下流の製品情報
原材料
準備製品
42408-82-2(ブトルファノール)キーワード:
- 42408-82-2
- (-)-17-(Cyclobutylmethyl)-3,14b-dihydroxymorphinan
- BC 2627, (-)-
- l-3,14-Dihydroxy-N-(cyclobutylmethyl)morphinan
- l-BC 2627
- Levo-BC 2627
- C06863
- (-)-17-(CyclobutylMethyl)-3,14β-
dihydroxyMorphinan
- 17-(cyclobutylmethyl)morphinan-3,14-diol
- BUTORPHANOL
- (4bS,8aS,9R)-11-(cyclobutylmethyl)-6,7,8,8a,9,10-hexahydro-5H-9,4b-(epiminoethano)phenanthrene-3,8a-diol
- (-)-Butorphanol
- 17-(cyclobutylmethyl)-morphinan-14-diol
- 17-(シクロブチルメチル)モルフィナン-3,14-ジオール
- ブトルファノール
- (1S,9R,10S)-17-(シクロブチルメチル)-17-アザテトラシクロ[7.5.3.01,10.02,7]ヘプタデカ-2,4,6-トリエン-4,10-ジオール
- 麻薬拮抗薬
- 麻薬性鎮痛薬
- 鎮咳薬