トリヘキシフェニジル塩酸塩 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
解説
1-cyclohexyl-1-phenyl-3-piperidinopropanol hydrochloride．C20H31NO·HCl(337.93)．トリヘキシフェニジル塩酸塩は，アセトフェノン，ホルムアルデヒド，ピペリジンのマンニッヒ反応で得られる．β-ピペリジノプロピオフェノンに，シクロヘキシルマグネシウムブロミドを反応させると得られる．白色の結晶．分解点258 ℃．水に難溶，エタノール，クロロホルムに可溶．アトロピン類似の作用を示し，筋けいれん性硬直の軽減に有効で，抑うつ症状や精神無力症を軽減させるので，パーキンソン症候群治療剤として使用される．LD50 39 mg/kg(マウス，静注)．森北出版「化学辞典（第2版）
効能
パーキンソン病治療薬, ムスカリン受容体拮抗薬
商品名
アーテン (ファイザー); セドリーナ (第一三共); トリヘキシフェニジル塩酸塩 (キョーリンリメディオ); トリヘキシフェニジル塩酸塩 (共和薬品工業); トリヘキシフェニジル塩酸塩 (武田テバファーマ); トリヘキシフェニジル塩酸塩 (長生堂製薬); トリヘキシフェニジル塩酸塩 (高田製薬); トリヘキシン (キョーリンリメディオ); パキソナール (高田製薬); パーキネス (東和薬品); 塩酸トリヘキシフェニジル (ニプロ)
説明
Trihexyphenidyl is an antagonist of M
1 muscarinic acetylcholine receptors. It binds to rat M
1 receptors in cerebral cortex selectively over rat M
2 receptors in heart tissue (IC
50s = 3.7 and 31 nM, respectively). Trihexyphenidyl inhibits contractions induced by acetylcholine in guinea pig ileum (IC
50 = 22 nM). It also inhibits oxotremorine-induced tremors and physostigmine-induced mortality in mice (ED
50s = 2 and 3.6 mg/kg, respectively). Trihexyphenidyl (20 mg/kg) improves abnormal movement in a mouse model of L-3,4-dihydroxyphenylalanine (L-DOPA) responsive dystonia (DRD) that expresses mutant tyrosine hydroxylase (TH). Formulations containing trihexyphenidyl have been used in the symptomatic treatment of Parkinson''s disease.
化学的特性
Benzhexol hydrochloride is White Solid
使用
Benzhexol hydrochloride is an anticholinergic tertiary amine that can gain access to the CNS. It is used to treat parkinsonism and the extrapyramidal side effects of anti-psychotic drugs. The drug is a muscarinic anta gonist that qualitatively resembles the belladonna alkaloids in its pharmacological actions and side effects.
一般的な説明
Trihexyphenidylhydrochloride, α-cyclohexyl-α-phenyl-1-piperidinepropanolhydrochloride (Artane, Tremin, Pipanol), introduced in1949, is approximately half as active as atropine as an antispasmodicbut is claimed to have milder side effects, such asmydriasis, drying of secretions, and cardioacceleration. It hasa good margin of safety, although it is about as toxic as atropine.It has found a place in the treatment of parkinsonismand is claimed to provide some measure of relief from themental depression often associated with this condition. It does, however, exhibit some of the side effects typical of theparasympatholytic-type preparation, although adjusting thedose carefully may often eliminate these.
副作用
Common side effects of Benzhexol hydrochloride include drowsiness, dizziness, constipation, flushing, nausea, nervousness, blurred vision or dry mouth. Severe may include: decreased sexual performance, severe stomach/abdominal pain, difficulty/pain in swallowing, difficulty in urinating, chest pain, severe dizziness/fainting, high fever, fast/irregular/slow heartbeat, mental/mood changes (e.g., blurred consciousness, hallucinations, memory problems), pain/swelling/reddening of the eyes, changes in vision (e.g., seeing rainbows around lights at night). Symptoms of very severe allergic reactions in some patients include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, and difficulty breathing. In addition, studies have shown that Benzhexol hydrochloride has minimal side effects in the treatment of salivation in children with cerebral palsy.
安全性プロファイル
Poison by ingestion,intraperitoneal, intravenous, and subcutaneous routes. Ananticholinergic agent which causes human psychotropiceffects. Human systemic effects by ingestion: distortedperceptions, eye effects, hallucinations, toxic psychosis.When he
トリヘキシフェニジル塩酸塩 上流と下流の製品情報
原材料
準備製品