バルデナフィル塩酸塩

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

  H301：飲み込むと有毒

  H311：皮膚に接触すると有毒

  H331：吸入すると有毒

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける 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。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P310：ただちに医師に連絡すること。

  P330：口をすすぐこと。

  P361：汚染された衣類をすべて脱ぐこと。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  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。

バルデナフィル塩酸塩 化学特性,用途語,生産方法

• 効能

  血管拡張薬, 勃起不全治療薬, ホスホジエステラーゼV阻害薬

• 説明

  Vardenafil was the second agent to be marketed and had the advantage that its onset time was not reduced by taking the medication on a full stomach . It is 30 times more potent as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil, with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4 and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000 nM.

• 化学的特性

  White to Off-White Cyrstalline Solid

• 使用

  vardenafil hydrochloride is a selective phsphodiesterase type 5 (pde5) inhibitor that is used as a urological agent in the treatment of erectile dysfunction.

• 一般的な説明

  Vardenafil, 4-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one(Levitra), was the second PDE5 introduced in the U.S. market.The metabolism of vardenafil is primarily by CYP3A4.As such, concomitant use of CYP3A4 inhibitors such as ritonavir,indinavir, ketoconazole, as well as moderate CYP3Ainhibitors such as erythromycin typically results in significantincreases of plasma levels of vardenafil.

• in vitro

  Vardenafil hydrochloride specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM. Vardenafil hydrochloride increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow.

• 酵素阻害剤

  Vardenafil also is rapidly absorbed and peaks in concentration (9.05 μg/mL after a 10-mg dose) after 0.9 hours, displaying a half-life of 4 to 5 hours. The absorption rate of both sildenafil and vardenafil are reduced when taken with a high-fat diet. The drug also is metabolized by hepatic CYP3A4, and a potential for drug–drug interaction with inhibitors or enhancers of CYP3A4 exists. Biochemical studies demonstrate a significant increase in selectivity of vardenafil over sildenafil for PDE5 versus PDE6. Whether this translates into a significant improvement in side effects must await studies in a greater population of patients.

バルデナフィル塩酸塩 生産企業

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