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盐酸更昔洛韦片|溶液VALCYTE（VALGANCICLOVIR HYDROCHLORIDE）

2013-04-19 18:06:34 作者：新特药房来源：互联网浏览次数：155 文字大小：【大】【中】【小】

简介： 部分中文更昔洛韦处方资料（仅供参考）药品英文名 Valganciclovir 药品别名克毒愈、Valcyte 药物剂型片剂：450mg。溶液 50毫克/毫升 100毫升/瓶药理作用本品为合成的2-脱氧鸟苷类似物， ...

部分中文更昔洛韦处方资料（仅供参考）
药品英文名
Valganciclovir
药品别名
克毒愈、Valcyte
药物剂型
片剂：450mg。

溶液 50毫克/毫升 100毫升/瓶

药理作用
本品为合成的2-脱氧鸟苷类似物，是抗病毒药更昔洛韦(ganciclovir)的前体药物，可大大减少更昔洛韦的毒性。它的药效学特点与更昔洛韦相同。口服缬更昔洛韦后在肠黏膜细胞酯酶和肝酯酶的作用下迅速水解成更昔洛韦，更昔洛韦在病毒内和细胞内酶磷酸化作用下生成三磷酸更昔洛韦，后者与三磷酸脱氧鸟苷(dGTP)竞争作为病毒DNA多聚酶的底物，因此抑制病毒DNA的合成，从而产生抗巨细胞病毒(CMV)活性。在体外，更昔洛韦对CMV的作用比阿昔洛韦强26倍。体内外研究都显示更昔洛韦能够抑制由CMV和移植排斥所引起的免疫反应，并在CMV严重感染的动物模型中也有效。从少数CMV感染的患者中分离出抗更昔洛韦的种系，它们在编码磷酸化更昔洛韦的蛋白激酶和病毒DNA聚合酶的基因中发生点突变。
药动学
研究表明，本品口服吸收的生物利用度为60%，是更昔洛韦的l0倍，并且很快吸收和水解成更昔洛韦。对CMV和HIV晚期感染以及接受肝脏移植患者来说，全身缬更昔洛韦的浓度很小，因为缬更昔洛韦24h的药时曲线下面积(AUC)值仅为更昔洛韦的1%～2%。在CMV和HIV晚期及肝脏移植的患者中，每日1次口服缬更昔洛韦900mg的效果相当于静注5mg/kg更昔洛韦。与空腹相比，与食物同服缬更昔洛韦可以提高更昔洛韦的浓度。缬更昔洛韦通过肾小球滤过和肾小管分泌而消除。口服单剂量缬更昔洛韦360mg和单剂量静注更昔洛韦5mg/kg，其终点时的消除半衰期(t1/2β)相似。在肝脏移植接受者中，更昔洛韦的肾清除率在口服单剂量缬更昔洛韦450mg或900mg以及在18h内口服单剂量的更昔洛韦1000mg和lh中静注更昔洛韦5mg/kg时所得到的结果相似。
适应证
用于获得性免疫缺陷综合征(AIDS)患者巨细胞病毒(CMV)性视网膜炎。
禁忌证
1．本品禁用于对更昔洛韦或缬更昔洛韦过敏者。
2．中性粒细胞＜0.5×109/L、血小板＜25×109/L、血红蛋白浓度＜80g/L者禁用。
3．血液透析患者禁用本品。
4．本品用于儿童的安全性和疗效尚未确定，故儿童不推荐使用。
注意事项
1．肾功能不全患者应慎用本品，并适当调整剂量。孕妇慎用。原先存在骨髓抑制者、接受骨髓抑制药物或放疗，及有血细胞减少症史或血细胞减少反应者慎用。
2．由于本品和更昔洛韦的生物利用度不同，因此不能一对一地替换用药。
3．由于更昔洛韦的诱变作用可严重影响精子生成和生育能力，因此用药者在治疗期间及治疗后至少90天应采取避孕措施。
4．过量服用可能导致肾毒性增加，血液透析和增加电解质可能有助于降低血浆药物浓度。
5．15～30℃保存。
不良反应
1．胃肠道反应：腹泻、恶心、呕吐和腹痛。
2．血液系统反应：中性粒细胞减少和贫血、血小板减少、骨髓抑制。
3．中枢神经系统反应：发热、头痛、失眠、外周神经障碍、感觉异常、癫痫、精神病、幻觉。
4．眼部反应：视网膜脱离。
5．其他不良反应：肾功能减退、其他局部或全身反应。在动物试验中更昔洛韦有致癌性、致畸性，并导致无精子生成。
用法用量
口服，每次900mg，每日2次，一般于3周后改为每日1次维持。
药物相应作用
1．齐多夫定、麦角酚酸酯或硫唑嘌呤与本品合用，使中性粒细胞减少和贫血等不良反应增加。
2．肾毒性药物损害肾功能，使更昔洛韦的体内消除减慢，药物蓄积，毒性增加。
3．丙磺舒和其他肾排泄药物能降低更昔洛韦的清除率，也导致其毒性增加。
4．与其他细胞毒药物合用会增大骨髓抑制、消化道和皮肤不良反应的危险，因此不能合用。
5．缬更昔洛韦的代谢产物更昔洛韦可显著增加去羟肌苷的生物利用度，应密切观察后者引起的毒性反应。
6．与亚胺培南/西司他丁合用会增加癫痫的可能。

Valcyte (valganciclovir HCl)
Company: Roche
Approval Status: Approved March 2001
Treatment for: Cytomegalovirus retinitis in patients with AIDS
Areas: Immunology/Infectious Diseases; Ophthalmology
General Information
Valcyte tablets have been approved by the FDA for the treatment of cytomegalovirus (CMV) retinitis in patients with acquired immunodeficiency syndrome (AIDS). Valcyte is an oral prodrug of Cytovene, a currently approved and widely prescribed anti-CMV medication.
The active ingredient in Valcyte is valganciclovir, which exists as a mixture of two diastereomers (compounds with the same atoms, but in different arrangements). In the body, the diastereomers are converted to ganciclovir, which inhibits the replication of human cytomegalovirus.
CMV belongs to the family of herpes viruses. The virus remains inactive in individuals with normal immune function; however, it can cause illness in those with compromised immune systems, such as individuals with AIDS or patients taking post-transplant immunosuppressants.
In patients with HIV/AIDS, the most common form of CMV is CMV retinitis, an infection of the eye that can lead to blindness.
Clinical Results
A randomized, open-label, controlled trial evaluated 160 subjects with AIDS and newly diagnosed CMV retinitis. Subjects were randomized to receive treatment with either Valcyte tablets or intravenous ganciclovir solution (Cytovene-IV). The median age of
the participants was 39 years, the median baseline HIV-1 RNA was 4.9 log10 and the median CD4 cell count was 23 cells/mm3. A determination of CMV retinitis progression by the masked review of retinal photographs taken at baseline and week four was the primary outcome measurement of the three week induction therapy. At four weeks, Valcyte tablets were found to have comparable efficacy for induction therapy when evaluated against Cytovene-IV.
Side Effects
Adverse events reported from two trials of Valcyte include (but are not limited to) the following:
Diarrhea
Nausea
Pyrexia (fever)
Neutropenia (decreased number of white blood cells)
Anemia
Headache
Vomiting
Abdominal pain
Insomnia
Retinal detachment
Mechanism of Action
Valganciclovir is an L-valyl ester (prodrug) of ganciclovir that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to ganciclovir by intestinal and hepatic esterases. Ganciclovir is a synthetic analogue of 2'-deoxyguanosine, which inhibits replication of human cytomegalovirus in vitro and in vivo.
In CMV-infected cells, ganciclovir is initially phosphorylated to ganciclovir monophosphate by the viral protein kinase, pUL97.
Further phosphorylation occurs by cellular kinases to produce ganciclovir triphosphate, which is then slowly metabolized intracellularly. As the phosphorylation is largely dependent on the viral kinase, phosphorylation of ganciclovir occurs preferentially in virus-infected cells.
The virustatic activity of ganciclovir is due to inhibition of viral DNA synthesis by ganciclovir triphosphate. (from Valcyte Prescribing/Label Information).
Additional Information
For additional information on Valcyte, please visit Hoffmann-La Roche.
If you are interested in further information on AIDS and CMV, please visit the National Institute of Allergy and Infectious Diseases or the Centers for Disease Control and Prevention.
附件:

201132118363740.pdf

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注：以下产品不同规格和不同价格，购买以咨询为准！
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产地国家: 美国
原产地英文商品名:
VALCYTE TABLET 450mg/tab 60tabs/bottle
原产地英文药品名:
VALGANCICLOVIR HYDROCHLORIDE
中文参考商品译名:
克毒愈片剂 450毫克/片 60片/瓶
中文参考药品译名:
盐酸更昔洛韦
生产厂家中文参考译名:
罗氏
生产厂家英文名:
ROCHE PALO

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原产地英文商品名:
VALCYTE SOLUTION 50mg/ml 100mls/bottle
原产地英文药品名:
VALGANCICLOVIR HYDROCHLORIDE
中文参考商品译名:
克毒愈溶液 50毫克/毫升 100毫升/瓶
中文参考药品译名:
盐酸更昔洛韦
生产厂家中文参考译名:
罗氏
生产厂家英文名:
ROCHE PALO