メプロバメート 化学特性,用途語,生産方法
解説
2-methyl-2-propyl-1,3-propanediyl dicarbamateの一般名．C9H18N2O4(218.25)．プロピオンアルデヒドを原料に，2-メチル-2-プロピル-1,3-プロパンジオールを合成し，これにホスゲンを作用させて炭酸エステルとし，さらにNH3を作用させると得られる．白色の結晶性粉末．熱水から再結晶する．融点104～106 ℃．無臭で，苦味がある．20 ℃ の水に0.34％(重量/重量)溶ける．エタノールに易溶．酸およびアルカリに安定である．向精神薬に用いられる．視床の介在ニューロン系の機能を抑制し，脊髄の多シナプス反射弓の介在ニューロンを遮断し，不安，緊張状態を緩和·消失させる．自律神経系にはほとんど作用しない．森北出版「化学辞典（第2版）
医薬用
メプロバメートは，中枢性筋弛緩薬のメフェネシンから誘導された抗不安薬である。白色の結晶性の粉末で味は苦い。トランキライザーの一種(弱トランキライザー)で，不安，緊張を軽減する。バルビツレートに比べて精神活動に対する抑制がはるかに小さい。視床下部，視床，大脳辺縁系に対し抑制的に作用すると考えられる。脊髄反射をも抑制し，中枢性筋弛緩作用を示すが，抗コリン作用も抗アドレナリン作用もない。消化管から容易に吸収される。不安，不眠，各種の神経症に1回0.2～0.4g(内服)用いる。
効能
抗不安薬, 催眠鎮静薬
化学的特性
white crystalline powder
使用
An anxiolytic.
This is a controlled substance.
世界保健機関（WHO）
Meprobamate, a bis-carbamate ester, was introduced in 1955 for
the treatment of anxiety and was subsequently used as a sedative-hypnotic drug.
Psychological and physical dependence can occur and abuse has been reported.
Meprobamate is controlled under Schedule IV of the 1971 Convention on
Psychotropic Substances.
(Reference: (UNCPS4) United Nations Convention on Psychotropic Substances (IV),
, , 1971)
一般的な説明
Meprobamate,2-methyl-2-propyltrimethylene dicarbamate, 2-methyl-2-propyl-1,3-propanediol dicarbamate (Equanil, Miltown), is officiallyindicated as an antianxiety agent. It is also a sedative–hypnotic agent. It has several overall pharmacological properties resembling those of benzodiazepines and barbiturates.The mechanism of action underlying anxiolytic effectsis unknown but may involve effects on conductivity inspecific brain areas.It does not appear to act through effectson GABAergic systems.The drug is effective againstabsence seizures and may worsen generalized tonic–clonicseizures.
空気と水の反応
Insoluble in water.
反応プロフィール
Meprobamate is a carbamate ester. Carbamates are chemically similar to, but more reactive than amides. Like amides they form polymers such as polyurethane resins. Carbamates are incompatible with strong acids and bases, and especially incompatible with strong reducing agents such as hydrides. Flammable gaseous hydrogen is produced by the combination of active metals or nitrides with carbamates. Strongly oxidizing acids, peroxides, and hydroperoxides are incompatible with carbamates.
危険性
Central nervous system depressant, use
restricted by law.
火災危険
Flash point data for Meprobamate are not available; however, Meprobamate is probably combustible.
臨床応用
Meprobamate is also a centrally acting skeletal musclerelaxant. The agents in this group find use in several conditions,such as strains and sprains that may produce acutemuscle spasm. They have interneuronal blocking propertiesat the level of the spinal cord, which are said to bepartly responsible for skeletal muscle relaxation.Also,the general CNS depressant properties they possess maycontribute to, or be mainly responsible for, the skeletalmuscle relaxant activity.
安全性プロファイル
Human poison by
unspecified routes. Moderately toxic to
humans and experimentally by ingestion.
Experimental poison by intravenous,
intraperitoneal, and subcutaneous routes. An
experimental teratogen. Human systemic
effects by ingestion: coma, blood pressure
decrease, regional or general arteriolar
constriction, dyspnea, cyanosis, respiratory
depression, nausea or vomiting, and allergic
skin dermatitis. Experimental reproductive
effects. Mutation data reported. Implicated
in aplastic anemia. Used as a tranquilizer.
When heated to decomposition it emits
toxic fumes of NOx.
純化方法
Crystallise it from hot water, aqueous EtOH (m 104-105.5o) or xylene (m 104.1-105.3o). It can be an addictive drug. [Beilstein 3 IV 73.]
メプロバメート 上流と下流の製品情報
原材料
準備製品