ペンシクロビル

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

  H225：引火性の高い液体および蒸気

  H315：皮膚刺激

  H319：強い眼刺激

• 注意書き

  P210：熱/火花/裸火/高温のもののような着火源から遠ざ けること。－禁煙。

  P233：容器を密閉しておくこと。

  P240：容器を接地すること/アースをとること。

  P241：防爆型の電気機器/換気装置/照明機器/．．．機器を使 用すること。

  P242：火花を発生させない工具を使用すること。

  P243：静電気放電に対する予防措置を講ずること。

  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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ 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。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

  P370+P378：火災の場合：消火に．．．を使用すること。

  P403+P235：換気の良い場所で保管すること。涼しいところに 置くこと。

ペンシクロビル 価格

MSDS Information

• 2-Amino-9-[4-hydroxy-3-(hydroxymethyl)butyl]-3,9-dihydropurin-6-one

ペンシクロビル 化学特性,用途語,生産方法

• 外観

  白色〜わずかにうすい褐色, 結晶〜粉末

• 溶解性

  水に溶ける。

• 用途

  ウィルス DNA ポリメラーゼ / 逆転写酵素による基質の取り込みを競合的 に阻害し、DNA 鎖の伸長を停止することによ りウィルスの増殖阻害作用を示します。

• 用途

  ウイルス DNA ポリメラーゼ / 逆転写酵素による基質の取り込みを競合的 に阻害し、DNA 鎖の伸長を停止することによ りウイルス増殖阻害作用を示します。

• 効能

  抗ウイルス薬, DNAポリメラーゼ阻害薬

• 説明

  Vectavir was launched in the UK for herpes labialis. Penciclovir is synthetically available by two routes of four steps each from 2- (hydroxymethyl)butane-l,4-diol and is active against HSV-1, HSV-2 VZV but has limited activity against CMV. Vectavir is an acyclic guanosine analog that acts as a competitive inhibitor of DNA polymerase. It is a metabolic product of famcyclovir that is preferentially phosphorylated by viral infected cells (by thymidine kinases) over normal cells. The triphosphate has a low activity against cellular DNA polymerase which is one possible explanation for its low toxicity. While its spectrum of activity is similar to acyclovir, it is longer acting because its triphosphate is 20 times more stable and is not metabolized.

• 化学的特性

  White Cyrstalline Solid

• 使用

  A deuterated version of Penciclovir, an antiviral

• 定義

  ChEBI: A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclo ir, is used for oral administration.

• 適応症

  Penciclovir has activity against HSV-1, HSV-2, VZV, and HBV. After oral administration, famciclovir is converted to penciclovir by first-pass metabolism. Penciclovir has a mechanism of action similar to that of acyclovir. It is first monophosphorylated by viral thymidine kinase; then it is converted to a triphosphate by cellular kinases.

• 獲得抵抗性

  Penciclovir is inactive against thymidine kinase-deficient strains of HSV.

• 応用例（製薬）

  A synthetic acyclic purine nucleoside analog, usually administered orally as the diacetyl ester, famciclovir, which acts as a prodrug undergoing rapid first-pass metabolism to release the active compound in vivo. The parent compound has virtually no oral bioavailability, but is supplied as a topical formulation.

• 薬物動態学

  Oral absorption, penciclovir： 5%
  famciclovir： 77%
  C_max famciclovir 250 mg oral： 1.6 mg/L after 0.5–1.5 h
  famciclovir 500 mg oral： 3.3 mg/L after 0.5–1.5 h
  famciclovir 750 mg oral： 5.1 mg/L after 0.5–1.5 h
  Plasma half-life： 2.1–2.7 h
  Volume of distribution： c. 1.5 L/kg
  Plasma protein binding： <20%
  Following absorption famciclovir is converted rapidly by enzyme-mediated deacetylation and oxidation to penciclovir. Food does not lead to any significant change in the availability or elimination.
  The pharmacokinetics in elderly subjects are similar to those seen in younger subjects, although small increases in AUC and plasma half-lives were seen, consistent with slightly decreased renal clearance.
  Renal excretion is the major route of elimination, 50–60% of an oral dose being recovered in the urine. After intravenous infusion, about 70% is excreted unchanged in the urine. After oral administration of famciclovir, penciclovir accounts for 82% of urinary drug-related material. The remainder includes metabolites, of which the largest is the 6-deoxy precursor of penciclovir. Renal clearance exceeds glomerular filtration, indicating renal tubular secretion.

• 臨床応用

  Penciclovir is approved as a topical formulation for the treatment of herpes labialis. In immunocompetent individuals, penciclovir shortens the duration of lesion presence and pain by approximately half a day when it is initiated within an hour of lesion development and applied every 2 hours during waking hours for 4 days.

• 副作用

  In clinical trials the incidence of adverse events after famciclovir, aciclovir and placebo were similar, the most common adverse events being headache and nausea.

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