バラシクロビル塩酸塩水和物 化学特性,用途語,生産方法
外観
白色～うすい黄色, 結晶性粉末～粉末
溶解性
水に可溶
用途
逆転写酵素阻害剤です。逆転
写酵素を阻害し、DNA 鎖の伸長を停止するこ
とによりウイルスの増殖を抑制します。
効能
抗ウイルス薬, DNAポリメラーゼ阻害薬
商品名
バルトレックス (グラクソ・スミスクライン); バルトレックス (グラクソ・スミスクライン)
説明
Valacyclovir hydrochloride, an orally active L-valyl ester of the potent antiviral agent aciclovir, was launched in 1995 in the United Kingdom for the treatment of herpes simplex virus (HSV) infections of the skin and mucous membranes, including initial and recurrent genital herpes. As a prodrug, valaciclovir has an improved pharmacokinetic profile to aciclovir. It is rapidly absorbed after oral administration and extensively converted to aciclovir via first-pass metabolism to achieve plasma levels of aciclovir comparable to those seen with aciclovir via i.v. route. Valacyclovir is then activated selectively in virus-infected cells by viral thymidine kinase to form aciclovir triphosphate in a stepwise fashion. This active species inhibits viral DNA polymerase via irreversible binding to the active site of the enzyme. Once aciclovir is incorporated into the elongating viral DNA, it terminates replication of the viral DNA strand, an antiviral mechanism unique to aciclovir. Valacyclovir is reportedly in clinical trials for the suppression of cytomegalovirus infection and disease in renal transplant patients.
化学的特性
White Crystalline Powder
来歴
Valacyclovir hydrochloride is an antiviral drug developed by GlaxoSmithKline and marketed under the brand name Valtrex. It was first approved by the FDA in June 2001 for the treatment of infections caused by the herpes simplex virus (HSV), including genital herpes, cold sores, and shingles in adults, as well as cold sores in children.
使用
Acyclovir (A192400) impurity. The L-Valine ester prodrug of Acyclovir.
一般的な説明
Valacyclovir (Valtrex) is the hydrochloride salt of the Lvalylester of acyclovir. The compound is a water-solublecrystalline solid, and it is a prodrug intended to increase thebioavailability of acyclovir by increasing lipophilicity.Valacyclovir is hydrolyzed rapidly and almost completely toacyclovir following oral administration.
Valacyclovir has been approved for the treatment of herpeszoster (shingles) in immunocompromised patients. Theside effect profile observed in valacyclovir is comparablewith bioequivalent doses of acyclovir.
薬物動態学
The binding of valacyclovir to human plasma proteins ranges between 13.5 to 17.9%. The plasma elimination half-life of acyclovir is 2.5 to 3.3 hours. The bioavailability of valacyclovir hydrochloride is 54%, compared to approximately 20% for oral acyclovir, and it is as effective as acyclovir in decreasing the duration of pain associated with posttherapeutic neuralgia and episodes of genital lesion healing.
副作用
The adverse effects are similar to acyclovir, which include nausea, headache, vomiting, constipation, and anorexia.
バラシクロビル塩酸塩水和物 上流と下流の製品情報
原材料
準備製品