Ganciclovir

Ganciclovir sodium (Cytovene®) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. more...

Administration

Oral or intravenous. Acute infections are treated in two phases:

• induction phase, 5 mg per kilogram intravenously every 12 hours for 14-21 days, the intravenous dose given as a 1 hour infusion
• maintenance phase, 5 mg per kg intravenously every day

Stable disease is treated with 1000 mg orally three times daily. Similar dosing is used to prevent disease in high-risk patients, such as those infected with human immunodeficiency virus (HIV) or those with organ transplants.

Ganciclovir is also available in slow-release formulations for insertion into the vitreous of the eye, as treatment for CMV retinitis.

Mechanism of action

Ganciclovir is a synthetic analogue of 2'-deoxy-guanosine. It is first phosphorylated to a deoxyguanosine triphosphate (dGTP) analog. This competitively inhibits the incorporation of dGTP by viral DNA polymerase, resulting in the termination of elongation of viral DNA.

Pharmacokinetics

Absorption of the oral form is very limited - about 5% fasting, about 8% with food. It achieves a concentration in the central nervous system of about 50% of the plasma level. About 90% of plasma ganciclovir is eliminated unchanged in the urine, with a half-life of 2-6 hrs, dependending on renal function (elimination takes over 24 hours in end-stage renal disease).

Side effects

Possible side effects include:

• Headache
• Rash
• Neutropenia
• Anemia
• Low platelets
• Kidney failure
• Confusion
• Seizures

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