英文药名: Cytovene(Ganciclovir Capsules & Injection Vials)

中文药名: 更昔洛韦胶囊

生产厂家: Roche Pharmaceuticals

药品名称

产品名称 更昔洛韦胶囊
英文名称 Ganciclovir Capsulels
用途分类 血液疾病类/其它
主要成份 更昔洛韦
生产厂家

Roche Pharmaceuticals
药理作用

本品为鸟嘌呤类抗病毒药，与阿昔洛韦是同系物， 但作用更强，尤其对艾滋病患者的巨细胞病毒有强大的抑制作用。本品进入细胞内后迅速被磷酸化形成单磷酸化合物，然后经细胞激酶的作用转化为三磷酸化合物，本药在感染巨细胞病毒的细胞内， 其磷酸化的过程较正常细胞中更快。本药三磷酸盐可竞争性抑制DNA多聚酶，并掺入病毒及宿主细胞的DNA中，从而抑制DNA的合成，本药对病毒DNA多聚酶的抑制作用比对宿主细胞的DNA多聚酶强。
适应症

本品用于免疫功能损伤引起巨细胞病毒感染的患者：
1. 于免疫功能损伤（包括艾滋病患者）发生的巨细胞病毒性视网膜炎的维持治疗；
2. 预防可能发生于器官移植受者的巨细胞病毒感染；
3. 预防晚期HIV感染患者的巨细胞病毒感染 。
肾功能正常情况下： CMV视网膜炎的维持治疗：在诱导治疗后，推荐维持量为每次1000mg， 一天3次，与食物同服。也可在非睡眠时每次服500mg，每3小时1次，每日6次，与食物同服。维持治疗时，若CMV视网膜炎有发展，则应重新进行诱导治疗。
用法用量

晚期HIV感染患者CMV病的预防：预防剂量为每次1000mg，一天3次，与食物同服。
器官移植受者CMV病的预防：预防剂量为每次1000mg，一天3次，与食物同服。
用药疗程根据免疫抑制时间和程度确定，若患者肾功能减退，则应根据肌酐清除率酌情调整用量。
任何疑问，请遵医嘱！
不良反应

本品可引起粒细胞减少/中性白细胞减少及血小板减少。
罕见：头痛，头昏，呼吸困难，恶心， 呕吐，腹痛，腹泻，厌食，消化道出血，心律失常，血压升高或血压降低，寒战，血尿，血尿素氨增加，脱发，瘙庠，荨麻疹，血糖降低，浮肿，周身不适，肌酐增加，嗜伊红胞增多症等。
有巨细胞病感染性视网膜炎的艾滋病患者可出现视网膜剥离。
禁忌症

对更昔洛韦或阿昔洛韦过敏者禁用。
注意事项

给患者的信息：更昔洛韦的主要毒性为中性粒细胞减少症、贫血和血小板减少症，必要时需进行剂量调整包括停药。应强调在治疗中密切接受血细胞计数检查的重要性。更昔洛韦与肌酐升高有关。
药物相互作用

地丹诺辛：在口服本品前2小时或同时服用地丹诺辛，可合地丹诺辛稳态AUCo-12增加111±114%。
在口服本品前期小时服用地丹诺辛，更昔洛韦的稳态AUC下降21±17%。但两药同时用时更昔洛韦的AUC不受影响。
两种药物的肾清除率均匀没有显著改变。

包装规格：

·250mg *30 胶囊
·500mg *30 胶囊

General description
Cytovene is the name for the drug ganciclovir, or ganciclovir sodium, put out by Roche Laboratories. Ganciclovir is a synthetic guanine derivative and an active antiviral agent for cytomegalovirus (CMV) infections. It is available in two forms: Cytovene-IV is found as a sterile lyophilized powder for use with intravenous administration. Each vial contains 500 mg of ganciclovir, which can be reconstituted with 10 mL of sterile water for injection (see usage). Cytovene is the capsular form available in 250 mg and 500 mg dosages.

Mechanism

Ganciclovir acts to inhibit CMV replication. It is phosphorylated to ganciclovir triphosphate in the body by cellular kinases whereupon the drug enters the infected cells where it persists for days. Ganciclovir triphosphate then inhibits DNA synthesis by competitively inhibiting DNA polymerases and incorporating itself into the viral DNA, terminating viral DNA elongation.

Indications

Cytovene-IV is indicated for treating immunocompromised patients infected with CMV. This includes patients already infected with HIV. It is also indicated as a preventive agent for transplant recipients at risk for CMV infection.

Cytovene capsules are indicated for prevention of CMV infection in organ transplant recipients and for patients with advanced HIV infection at risk for CMV infection. Capsules are also indicated as alternative treatment to Cytovene-IV intravenous administration for maintaining treatment for CMV retinitis and for cases where the benefit of avoiding intravenous administration outweighs the risk of more rapid progression of disease course.

Usage/Dosage

preparation
Reconstitute Cytovene-IV by adding 10 mL of sterile water to the ganciclovir vial. Shake the vial to dissolve the drug and inspect the solution for particles or discoloration (vial should be discarded if particulate matter or discoloration is observed). Reconstituted solution should be stable at room temperature for 12 hours. For IV infusion, concentrations greater than 10 mg/mL are not recommended.

CMV retinitis
induction treatment: recommended initial dosage for normal renal function patients is 5mg/kg intravenously at a constant rate over 1 your every 12 hours for 14 to 21 days.
maintenance treatment: following induction treatment, Cytovene-IV can be given intravenously at 5 mg/kg in a constant rate IV infusion over 1 hour daily, 7 days per week or 6 mg/kg once daily, 5 days a week. Or Cytovene capsules can be used at 1000 mg tid with food. Alternatively, a dosage of 500 mg 6 times daily every 3 hours with food during waking hours can be used. if CMV retinitis progresses, reinduction treatment is recommended.

Preventing CMV disease in patients with advanced HIV disease and normal renal function
recommended prophylactic treatment is Cytovene capsules at 1000 mg tid with food.

Preventing CMV in Transplant recipients with normal renal function
Cytovene-IV can be used initially at at 5 mg/kg every 12 hours for 7 to 14 days followed by 5 mg/kg once daily7 days per week or 6 mg/kg once daily, 5 days per week. Cytovene capsules can be used at 1000 mg tid with food. Duration of treatment for either form is dependent on the degree and duration of immunosuppression

With Renal impairment
Dosing for patients receiving hemodialysis treatment should not exceed 1.25 mg/kg 3 times per week. Treatment should be administered shortly following hemodialysis. Dosage should be adjusted as according to the following tables:

Creatine Clearance* (mL/min>	Cytovene-IV induction Dose	Dosing Interval (hrs)	Cytovene-IV maintenance Dose (mg/kg)	Dosing Interval (hrs)
>70	5.0	12	5.0	24
50-69	2.5	12	2.5	24
25-49	2.5	24	1.25	24
10-24	1.25	24	0.625	24
<10	1.25	3 times per week, following hemodialysis	0.625	3 times per week, following hemodialysis