ペンタゾシン 化学特性,用途語,生産方法
解説
ペンタゾシン，作用の強力な鎮痛薬の一種。白色の結晶性粉末。モルヒネなどの麻薬に拮抗(きっこう)作用があるが、これ自体にも軽度の習慣性がある。
用途
非麻薬性鎮痛薬鎮痛作用を示す
効能
鎮痛薬, オピオイド受容体作動薬/拮抗薬
商品名
ソセゴン (丸石製薬); ソセゴン (丸石製薬)
化学的特性
Crystalline Solid
使用
(?)-Pentazocine is a benzomorphan-type opiate with analgesic properties. It binds to opioid receptors (Ki values = 7.2, 31, and 5.7 nM for κ-, δ-, μ-opioid receptors, respectively) and to the type 1 σ-receptor (Kd = 12 nM). (?)-Pentazocine is abused with methylphenidate and other drugs. It is regulated as a Schedule IV compound in the United States. This product is intended for forensic and research applications.
世界保健機関（WHO）
Pentazocine, which has both agonist and weak opioid antagonist
activity, was introduced in 1967 for the treatment of moderate and severe pain. The
risk of drug dependence is lower with pentazocine than with morphine-like drugs
and pentazocine has been controlled under Section III of the 1971 Convention on
Psychotropic Substances since 1984. The risk of dependence is now widely
acknowledged to exist in vulnerable individuals and at least one country has
applied controls analogous to those of Schedule I of the 1961 Single Convention
on Narcotic Drugs.
(Reference: (UNCPS3) United Nations Convention on Psychotropic Substances (III),
, , 1971)
一般的な説明
The benzomorphans are prepared synthetically and thus resultin several stereoisomers. The active benzomorphans arethose that have the equivalent bridgehead carbons in thesame absolute configuration of morphine (carbons 9, 13,and 14 of morphine). The only benzomorphan in clinical useis pentazocine, which is prepared as the 2(R), 6(R), 11(R)enantiomer (Chemical Abstracts numbering). Pentazocineis a mixed agonist/antagonist displaying differing intrinsicactivity at the opioid receptor subtypes. At the κ-receptor,pentazocine is a partial agonist and a weak antagonist.
According to the manufacturer, a 50-mg dose of pentazocinehas about the same analgesic potency as 60 mg of codeineand about 1/50th the antagonistic activity of nalorphine.74Pentazocine is also an agonist at the κ-receptor, and thismay be responsible for the higher percentage of patients thatexperience dysphoria with pentazocine versus morphine.75Some evidence also exists that women respond better to κ-agonists than men. Pentazocine is available in a 50-mgtablet along with a low dose of the antagonist naloxone 0.5mg (Talwin NX). Naloxone 0.5 mg orally is expected tohave no pharmacological effect but is included to dissuadeIV drug abusers from dissolving and injecting Talwin NX.
安全性プロファイル
Poison by ingestion,
subcutaneous, intramuscular, intraperitoneal,
and intravenous routes. Experimental
reproductive effects. Human systemic
effects by intramuscular and intravenous
routes: wakefulness, euphoria, hallucinations
or distorted perceptions, tremors,
convulsions, excitement, motor activity
changes, muscle weakness, analgesia,
withdrawal, parasympathomimetic effects,
nausea or vomiting, and dernlititis. Can
cause drug dependency and other central
nervous system effects, An analgesic. When
heated to decomposition it emits toxic
fumes of NOx. See also ALLIT
COMPOUNDS.
ペンタゾシン 上流と下流の製品情報
原材料
準備製品