Ganciclovir for injection

This product is an analog of 2'-deoxyguanine nucleotides that can inhibit the replication of herpes viruses. Its mechanism of action is: ganciclovir is first phosphorylated into monophosphate by a protein kinase homolog encoded by cytomegalovirus (CMV) (UL97 gene), and then further phosphorylated into diphosphate and triphosphate by cellular kinases. In CMV-infected cells, the amount of triphosphate is 100 times higher than that in non-infected cells, indicating that this product can be preferentially phosphorylated in infected cells. Once ganciclovir forms triphosphate, it can persist for several days in CMV-infected cells. The triphosphate of ganciclovir can inhibit viral DNA synthesis in the following ways: 1) competitively inhibiting viral DNA polymerase; 2) incorporating into the DNA of viruses and host cells, resulting in the termination of viral DNA extension. Ganciclovir has a stronger effect on viral DNA polymerase than on host polymerase.

The main ingredient of this product is ganciclovir, whose chemical name is 9-(1,3-dihydroxy-2-propyloxymethyl)-guanine.

This product is white loose mass or powder. It is hygroscopic.

This product is only used for: 1. Prevention of cytomegalovirus disease that may occur in organ transplant recipients at risk of cytomegalovirus infection. 2. Treatment of cytomegalovirus retinitis in immunocompromised patients (including AIDS patients).

1. Standard dose for the treatment of CMV retinitis: 1) Initial dose: 5 mg/kg, once every 12 hours, intravenous drip at a constant rate, each drip time is more than 1 hour, for 14-21 days. 2) Maintenance dose: 5 mg/kg, once a day, 7 days/week, intravenous drip at a constant rate, each drip time is more than 1 hour; or 6 mg/kg, once a day, 5 days/week, intravenous drip at a constant rate, each drip time is more than 1 hour. 2. Prevention of cytomegalovirus disease in organ transplant recipients: 1) Initial dose: 5 mg/kg, once every 12 hours, intravenous drip at a constant rate, each drip time is more than 1 hour, for 7-14 days. 2) Maintenance dose: 5 mg/kg, once a day, 7 days/week, intravenous drip at a constant rate, each drip time is more than 1 hour; or 6 mg/kg, once a day, 5 days/week, intravenous drip at a constant rate, each drip time is more than 1 hour.

1. Common adverse reactions include bone marrow suppression. After taking the drug, about 40% of patients have a neutrophil count reduced to less than 1000/mm3, and about 20% of patients have a platelet count reduced to less than 50,000/mm3. In addition, anemia may occur. 2. Central nervous system symptoms such as mental abnormalities, tension, tremors, etc., with an incidence of about 5%, and occasionally coma, convulsions, etc. 3. Rash, itching, drug fever, headache, dizziness, dyspnea, nausea, vomiting, abdominal pain, loss of appetite, abnormal liver function, gastrointestinal bleeding, arrhythmia, increased or decreased blood pressure, hematuria, increased blood urea nitrogen, hair loss, decreased blood sugar, edema, general discomfort, increased creatinine, eosinophilia, local pain after injection, phlebitis, etc. may occur; AIDS patients with cytomegalovirus retinitis may experience retinal detachment.

It is contraindicated for patients who are allergic to this product or acyclovir.

Didanosine: When didanosine is taken 2 hours before or concurrently with oral ganciclovir, the steady-state didanosine AUC0-12 increases by 111±114% (range: 10% to 493%) (n=12). When didanosine is taken 2 hours before oral ganciclovir, the steady-state AUC of ganciclovir decreases by 21±17% (range: -44% to 5%), but the AUC of ganciclovir is not affected when the two drugs are taken together (n=12). Renal clearance of either drug was not significantly altered. When the standard IV ganciclovir initial dose (5 mg/kg IV infusion for 1 hour every 12 hours) is coadministered with didanosine 200 mg orally every 12 hours, the steady-state didanosine AUC0-12 increases by 70±40% (range: 3% to 121%, n=11) and the Cmax increases by 49±48% (range: -28% to 125%). In another study, when standard intravenous maintenance doses of ganciclovir (5 mg/kg intravenous infusion for 1 hour, once every 24 hours) were co-administered with didanosine 200 mg orally, once every 12 hours, during the first dose interval of didanosine, didanosine AUC0-12 increased by 50±26% (range: 22% to 100%, n=11) and Cmax increased by 36±36% (range: -27% to 94%). Plasma concentrations of didanosine (AUC12-24) were unchanged during the dose interval when not co-administered with ganciclovir. The pharmacokinetic parameters of ganciclovir were not affected by didanosine. Renal clearance of both drugs was not significantly altered in any of the studies. Zidovudine: When ganciclovir oral formulations at a dose of 1000 mg every 8 hours were combined with zidovudine 100 mg every 4 hours, the mean steady-state ganciclovir AUC0-8 decreased by 17±25% (range: -52% to 23%) (n=12). In the presence of ganciclovir, the steady-state zidovudine AUC0-4 increased by 19±27% (range: -11% to 74%). Because both zidovudine and ganciclovir may cause neutropenia and anemia, some patients may not tolerate the combination of the two drugs at full doses. Probenecid: When ganciclovir oral formulations at a dose of 1000 mg every 8 hours were combined with probenecid 500 mg every 6 hours, the mean steady-state ganciclovir AUC0-8 increased by 53±91% (range: -14% to 299%) (n=10). The renal clearance of ganciclovir was reduced by 22 ± 20% (range: -54% to -4%), and this interaction is related to competition for renal tubular secretion. Imipenem-cilastatin: There have been reports of seizures without significant features in patients receiving ganciclovir and imipenem-cilastatin simultaneously, so these drugs should not be used together unless the potential benefit outweighs the risk. Other drugs: Drugs that inhibit the replication of rapidly dividing cell populations, such as bone marrow, spermatogonia, and cells of the germinal layer of the skin and gastrointestinal mucosa, can increase toxicity when used together with ganciclovir. Therefore, such drugs, such as dapsone, pentamidine, 5-flucytosine, vincristine, vinblastine, doxorubicin, amphotericin B, trimethoprim/sulfamethoxazole complex, or other nucleoside antagonists, should be used together with ganciclovir only when the potential benefit outweighs the risk. There are no formal studies of interactions between ganciclovir and drugs commonly used in organ transplant recipients. Concomitant use of ganciclovir with known potential nephrotoxic drugs such as cyclosporine or amphotericin B may increase serum creatinine levels. In a retrospective analysis of 91 patients with heterotopic liver transplantation who received ganciclovir (5 mg/kg intravenous infusion for 1 hour, once every 12 hours) and oral cyclosporine (therapeutic doses), no effect on cyclosporine whole blood concentrations was observed.

Keep away from light and store in sealed container.

0.25g

Wuxi Kaifu Pharmaceutical Co., Ltd.

• Founded in:

  2001-02-15

• Address:

  No. 12, Xiaguang Road, Mashan, Binhu District, Wuxi City (Inside Mashan Town Industrial Park)

• Tax NO.:

  913202117265560329

• Registered Funds:

  70 million yuan

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