Ganciclovir is an antiviral medication primarily used to treat cytomegalovirus (CMV) infections. It is particularly effective in immunocompromised individuals, such as those with AIDS or those who have undergone organ transplants . Ganciclovir is marketed under various brand names, including Cytovene, Cymevene, and Vitrasert .
Ganciclovir was patented in 1980 and approved for medical use in 1988 . It was developed as a potent inhibitor of herpesvirus DNA replication, making it a valuable tool in the treatment of CMV infections . The drug’s development was driven by the need for effective antiviral therapies for immunocompromised patients who are particularly vulnerable to CMV infections.
Ganciclovir is a synthetic analog of 2’-deoxy-guanosine, a component of DNA. Its chemical formula is C9H13N5O4, and it has a molar mass of 255.234 g/mol . The drug is metabolized to its active triphosphate form by cellular enzymes, which then inhibits viral DNA polymerase more effectively than cellular polymerase .
Ganciclovir’s antiviral activity is highly selective. It requires conversion to its active form by a virus-encoded enzyme, thymidine kinase (TK), which is present in CMV-infected cells . Once activated, ganciclovir triphosphate inhibits viral DNA polymerase, preventing the replication of viral DNA and thereby controlling the infection .
Ganciclovir is available in various forms, including intravenous (IV) infusion, oral capsules, and intravitreal implants . The IV form is typically used for severe infections and is prepared by reconstituting a dry powder equivalent to 500 mg of ganciclovir in a sterile environment . The reconstituted solution is then administered via a volumetric pump over one hour to minimize venous irritation .
Ganciclovir is indicated for the treatment of:
It has also been used with some success in treating Human herpesvirus 6 infections and herpes simplex virus epithelial keratitis .
Ganciclovir is associated with a range of serious hematological adverse effects, including granulocytopenia, neutropenia, anemia, and thrombocytopenia . Other common side effects include fever, nausea, vomiting, diarrhea, abdominal pain, and increased liver enzymes . Due to its potential carcinogenic, teratogenic, and mutagenic effects, ganciclovir is handled as a cytotoxic drug in clinical settings .