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解説
フェノバルビタール,白色の結晶．融点174～178 ℃．エタノール，エーテル，アセトンに易溶，クロロホルムに可溶，水に難溶．pK1 7.3，pK2 11.8．λmax 240 nm(ε 6600)．バルビツル酸系の長時間型催眠薬で，抗けいれん作用も強く，抗てんかん薬としても用いられる．LD50 660 mg/kg(ラット，経口)．
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用途
中枢神経系を抑制し、催眠作用や鎮静作用を有する。抗てんかん薬にも用いる。
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製法
ルミナールともいう．フェニルエチルマロン酸ジエチルと尿素とを縮合させると得られるフェノバルビタール．
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効能
抗不安薬, 抗けいれん薬, 催眠鎮静薬
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商品名
フェノバルビタール (シオエ製薬); フェノバルビタール (マイラン製薬); フェノバルビタール (丸石製薬); フェノバルビタール (丸石製薬); フェノバール (藤永製薬); フェノバール (藤永製薬)
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説明
Phenobarbital (Item No. 9001494) is an analytical reference material categorized as a barbiturate. Phenobarbital is regulated as a Schedule IV compound in the United States. This product is intended for research and forensic applications.
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化学的特性
Crystalline Solid
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使用
Phenobarbital exhibits relaxant, soporific, and anticonvulsant activities. It is widely used
in treating epilepsy, chorea, and spastic paralysis, and is used as a component of a large
number of combined drugs, valocordin and corvalol in particular.
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適応症
Phenobarbital can reduce cholestatic pruritus, possibly
by enhancing hepatic microsomal function. Phenobarbital is sedating and
may interfere with the metabolism of many drugs.
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定義
ChEBI: A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.
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世界保健機関（WHO）
Phenobarbital is a long-acting barbiturate which is controlled
under Schedule IV of the 1971 Convention on Psychotropic Substances.
Phenobarbital is of value in the treatment of epilepsy and preparations for such
use are included in the WHO Model List of Essential Drugs. See also WHO
comment for barbiturates.
(Reference: (UNCPS4) United Nations Convention on Psychotropic Substances (IV),
, , 1971)
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一般的な説明
Phenobarbital, 5-ethyl-5-phenylbarbituricacid (Luminal), is a long-acting sedative and hypnotic.It is also a valuable anticonvulsant, especially in generalizedtonic–clonic and partial seizures (see the discussionon anticonvulsants). Metabolism to the p-hydroxylphenylcompound followed by glucuronidation accounts for about90% of a dose.
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空気と水の反応
Sensitive to hydrolysis. Alkaline solutions react more rapidly than acidic solutions. At pH 7 and 176°F, has a half life of 74 hours. Insoluble in water.
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反応プロフィール
Phenobarbital is also sensitive to prolonged exposure to light. Incompatible with strong oxidizing agents. Forms a complex of reduced solubility with macrogol 4000. Able to form metal derivatives .
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火災危険
Phenobarbital is combustible.
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安全性プロファイル
Confirmed carcinogen
with experimental carcinogenic,
neoplastigenic, tumorigenic, and teratogenic
data. A human poison by ingestion. An
experimental poison by ingestion,
intraperitoneal, subcutaneous, intravenous,
and rectal routes. Human systemic effects by
ingestion: somnolence, motor activity
changes, pulmonary changes, allergc
dermatitis, and fever. Human reproductive
effects by ingestion: drug dependence and
other postnatal measures or effects. Human
teratogenic effects include developmental abnormalities of the central nervous system,
body wall, musculoskeletal, respiratory,
gastrointestinal, and urogenital systems.
Experimental reproductive effects. Human
mutation data reported. Used as a drug in
the treatment of epilepsy, and as a hypnotic
and sedative. When heated to
decomposition it emits toxic fumes of NOx.See also BARBITURATES.
