フェントラミン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H302：飲み込むと有害

  H314：重篤な皮膚の薬傷?眼の損傷

• 注意書き

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ 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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P330+P331：飲み込んだ場合：口をすすぐこと。無理に吐かせ ないこと。

  P303+P361+P353：皮膚（または髪）に付着した場合：直ちに汚染された衣 類をすべて脱ぐこと/取り除くこと。皮膚を流水/シャワー で洗うこと。

  P363：汚染された衣類を再使用す場合には洗濯をすること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

MSDS Information

• 3-[(4,5-Dihydro-1H-imidazol-2-yl)methyl-(4-methylphenyl)-amino]phenol

フェントラミン 化学特性,用途語,生産方法

• 効能

  血管拡張薬, αアドレナリン受容体拮抗薬

• 説明

  Phentolamine is also a derivative of imidazoline that exhibits a direct α-adrenoblocking, muscle-relaxant effect on smooth muscle as well as cholinomimetic, histamine, and sympathomimetic effects. The chemical variation of its structure permits a few of its properties to be more expressed. For example, the aforementioned tolazoline, 2-benzyl-2-imidazoline, a structural analog of phentolamine, has more of an expressed muscle-relaxant effect on smooth muscle than an α-adrenoblocking effect.

• 使用

  Anti-adrenergic.
  Phentolamine is used to prevent or control hypertensive episodes that occurin patients with pheochromocytoma. It also has been used incombination with papaverine to treat impotence.

• 定義

  ChEBI: A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used fo the treatment of hypertension.

• 適応症

  Human erectile tissue has a population of membrane receptors that are predominantly of the -adrenoceptor subtype. Phentolamine (Vasomax) is a nonselective - adrenoceptor blocking agent (see Chapter 11), and like other such agents, it has been used to treat ED. Nonselective adrenoceptor antagonists may provoke a reflex that increases both sympathetic outflow and the release of norepinephrine.

• 一般的な説明

  Phentolamine isthe more effectiveα -blocker.

• 作用機序

  Its mechanism of action is as an α-adrenergic antagonist of both α1- and α2-receptors, causing vasodilation and reduction in peripheral resistance. When administered by intracavernosal injection, it is thought to cause relaxation of the cavernous smooth muscles and vasodilation of the penile arteries. This results in increased arterial blood flow into the corpus cavernosa as well as swelling and elongation of the penis. Venous outflow also is reduced, possibly as a result of increased venous resistance. Phentolamine is slowly released into venous circulation with minimal, if any, systemic effects. Time to peak effect is within 10 minutes, and duration of action when used with papaverine is 1 to 6 hours.

• 臨床応用

  Phentolamine has been used orally and intracavernosally in the treatment of ED. Following oral administration, phentolamine has a plasma half-life of about 30 minutes and a duration of action of 2 to 4 hours. An intracavernosal injection of phentolamine results in the drug reaching maximum serum levels in about 20 to 30 minutes. It is rapidly metabolized. Phentolamine has been used in combination with papaverine, chlorpromazine, and vasoactive peptides in the treatment of ED.

• 副作用

  Side effects of phentolamine are dose related. It may cause orthostatic hypotension, reflex tachycardia, cardiac arrhythmias, and rarely, myocardial infarction. Phentolamine also may reduce sperm motility in vitro.

• 安全性プロファイル

  Poison by subcutaneous, intravenous, and intraperitoneal routes. Moderately toxic by ingestion. Experimental reproductive effects. When heated to decomposition it emits toxic fumes of NOx.

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