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| Pronunciation | /ɡænˈsaɪkləvɪər/ |
| Trade names | Cytovene; Cymevene; Vitrasert |
| Other names | gancyclovir; DHPG; 9-(1,3-dihydroxy-2-propoxymethyl)guanine |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605011 |
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| Routes of administration | Intravenous,by mouth, intravitreal |
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| Pharmacokinetic data | |
| Bioavailability | 5% (oral) |
| Metabolism | guanylate kinase (CMV UL97 gene product) |
| Eliminationhalf-life | 2.5–5 hours |
| Excretion | Kidney |
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| ECHA InfoCard | 100.155.403 |
| Chemical and physical data | |
| Formula | C9H13N5O4 |
| Molar mass | 255.234 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 250 °C (482 °F) (dec.) |
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Ganciclovir, sold under the brand nameCytovene among others, is anantiviral medication used to treatcytomegalovirus (CMV) infections.
Ganciclovir was patented in 1980 and approved for medical use in 1988.[4]
Ganciclovir is indicated for:[5]
It is also used for acute CMV colitis in HIV/AIDS and CMV pneumonitis in immunosuppressed patients.[medical citation needed]
Ganciclovir has also been used with some success in treatingHuman herpesvirus 6 infections.[6]
Ganciclovir has also been found to be an effective treatment forherpes simplex virus epithelial keratitis.[7]
Ganciclovir (in gel form) appears to be effective for treating the ophthalmicFelid herpesvirus 1 (FHV-1) virus infection in cats.[8]
Ganciclovir is commonly associated with a range of serioushaematological adverse effects. Commonadverse drug reactions (≥1% of patients) include:granulocytopenia,neutropenia,anaemia,thrombocytopenia, fever, nausea, vomiting,dyspepsia, diarrhea, abdominal pain, flatulence, anorexia, raised liver enzymes, headache, confusion, hallucination, seizures, pain andphlebitis at injection site (due to high pH), sweating, rash, itch, increased serumcreatinine and bloodurea concentrations.[5]
Ganciclovir is considered a potential humancarcinogen,teratogen, andmutagen. It is also considered likely to cause inhibition ofspermatogenesis. Thus, it is used judiciously and handled as acytotoxic drug in the clinical setting.[5][9]
Ganciclovir (9-[(1,3-dihydroxy-2-propoxy)methyl]guanine) is a potent inhibitor of viruses of theherpes family, including cytomegalovirus (CMV), that are pathogenic for humans and animals. The primary mechanism of ganciclovir action against CMV is inhibition of the replication of viral DNA by ganciclovir-5'-triphosphate (ganciclovir-TP). This inhibition includes a selective and potent inhibition of the viralDNA polymerase. Ganciclovir is metabolized to the triphosphate form by primarily three cellular enzymes: (1) a deoxyguanosine kinase induced by CMV-infected cells; (2) guanylate kinase; and (3) phosphoglycerate kinase. Other nucleotide-metabolizing enzymes may be involved as well. The selective antiviral response associated with ganciclovir treatment is achieved because of the much weaker inhibition of cellular DNA polymerases by ganciclovir-TP. Activity and selectivity are also amplified by the accumulation of ganciclovir-TP in CMV-infected cells.
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Acute infections are treated in two phases:
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 thevitreous humour of theeye, as treatment forCMV retinitis (associated with HIV infection).
A topical ophthalmic gel preparation of ganciclovir was recently[when?] approved for the treatment of acute herpes simplex keratitis.[citation needed]
Valganciclovir – theprodrug of ganciclovir
