Famciclovir

Famciclovir 속성

Famciclovir MSDS

Famciclovir

Famciclovir C화학적 특성, 용도, 생산

개요

Famciclovir, an effective oral prodrug of the antiviral penciclovir, was launched in the UK and shortly after in the U.S.A. for the treatment of shingles (herpes zoster). As the diacetyl ester of the 6-deoxy- penciclovir, famciclovir has significantly improved oral absorption. It is converted to penciclovir in vivo with a bioavailability of 41 % in rats. Penciclovir is phosphorylated, and hence activated onty in herpesvirus infected cells. This stable metabolite, penciclovir-triphosphate, is a strong inhibitor of herpesvirus DNA polymerases and of viral DNA synthesis with long lasting effects. The high selectivity of famciclovir/penciclovir to herpes family of viruses and their rather low toxicity may make this agent superior to other existing drugs.

화학적 성질

Off-White Powder

용도

sterol absorption inhibitor.

Famciclovir (Famvir) a synthetic acyclic purine analog derived from guanine. It is the diacetyl ester (prodrug) of penciclovir, which exhibits no antiviral activity until hydrolyzed to penciclovir and its active metabolites. It is indicated for the management of acute herpes zoster infections. It has been shown to relieve acute symptoms as well as to shorten the duration of postherpetic neuralgia. It is also used for the treatment or suppression of recurrent episodes of genital herpes in immunocompetent patients and in the treatment of recurrent herpes simplex types 1 and 2 infections in patients with human immunodeficiency virus.

Indications

Famciclovir (Famvir) is the diacetyl ester prodrug of the acyclic guanosine analogue 6-deoxypenciclovir (Denavir).

정의

ChEBI: 2-Amino-9H-purine in which the hydrogen at position 9 is substituted by a 4-acetoxy-3-(acetoxymethyl)but-1-yl group. A prodrug of the antiviral penciclovir, it is used for the treatment of acute herpes zoster (shingles), for the treatmen or suppression of recurrent genital herpes in immunocompetent patients and for the treatment of recurrent mucocutaneous herpes simplex infections in HIV infected patients.

일반 설명

Famciclovir is a diacetyl prodrug of penciclovir.As a prodrug,it lacks antiviral activity. Penciclovir, 9-[4-hydroxy-3-hydroxymethylbut-1-yl] guanine, is an acyclic guanine nucleoside analog. The structure is similar to that of acyclovir,except in penciclovir, a side chain oxygen has beenreplaced by a carbon atom and an extra hydroxymethylgroup is present.
VSV-infected cells, penciclovir is first phosphorylated byviral thymidine kinase41 and then further elaborated to thetriphosphate by host cell kinases. Penciclovir triphosphate isa competitive inhibitor of viral DNA polymerase. The pharmacokineticparameters of penciclovir are quite different fromthose of acyclovir. Although penciclovir triphosphate is about100-fold less potent in inhibiting viral DNA polymerase thanacyclovir triphosphate, it is present in the tissues for longerperiods and in much higher concentrations than acyclovir.

Mechanism of action

Famciclovir is a synthetic purine nucleoside analogue related to guanine. It is the diacetyl 6-deoxy ester of penciclovir, which is structurally related to ganciclovir. Its pharmacological and microbiological activities are similar to those of acyclovir. Famciclovir is a prodrug of penciclovir, which is formed in vivo by hydrolysis of the acetyl groups and oxidation at the 6-position by mixed function oxidases. Penciclovir and its metabolite penciclovir triphosphate possess antiviral activity resulting from inhibition of viral DNA polymerase.

Pharmacokinetics

Famciclovir can be given with or without food. The most common adverse effects are headache and GI disturbances. Concomitant use of famciclovir with probenecid results in increased plasma concentrations of penciclovir. The recommended dose of famciclovir is 500 mg every 8 hours for 7 days. The absolute bioavailability of famciclovir is 77%, and the area under plasma concentration–time curve (AUC) is 86 μg/mL. Famciclovir with digoxin increased plasma concentration of digoxin to 19% as compared to digoxin given alone.

Pharmacology

Famciclovir (Famvir) undergoes extensive first-pass metabolism to penciclovir after oral administration. Penciclovir is another nucleoside analog that has a mechanism of action similar to that of acyclovir. Compared with oral acyclovir, famciclovir has improved bioavailability as well as a significantly prolonged intracellular half-life, allowing for less frequent dosing. Valacyclovir and famciclovir are similar in their high absorption, bioavailability, renal elimination, minimal drug interaction profiles, safety profiles, and efficacy.

Clinical Use

Famciclovir is indicated for the treatment of acute herpes zoster (shingles); it is at least as effective in reducing pain and healing time. Famciclovir is generally as effective as acyclovir in the treatment of HSV. In immunocompetent patients, famciclovir is approved for the treatment and prophylaxis of recurrent genital herpes. For HIV-infected individuals, famciclovir is approved for the treatment of all recurrent mucocutaneous HSV infections.

부작용

Famciclovir may interact with probenecid or other drugs eliminated by renal tubular secretion. This interaction may result in increased blood levels of penciclovir or other agents.

Famciclovir 준비 용품 및 원자재

원자재

준비 용품

Famciclovir 공급 업체

공급자	전화	이메일	국가	제품 수	이점
XI'AN TIANGUANGYUAN BIOTECH CO., LTD.	+86-029-86333380 18829239519	sales06@tgybio.com	China	959	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	994	58
airuikechemical co., ltd.	+undefined86-15315557071	sales02@airuikechemical.com	China	994	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	893	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Nanjing ChemLin Chemical Industry Co., Ltd.	025-83697070	product@chemlin.com.cn	CHINA	3012	60
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Hebei Guanlang Biotechnology Co., Ltd.	+86-19930503282	alice@crovellbio.com	China	8823	58

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