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QuickView for ganciclovir (compound)
PubChem
| Name: | Ganciclovir |
|---|---|
| PubChem Compound ID: | 105070 |
| Description: | An ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections. |
| Molecular formula: | C9H13N5NaO4+ |
| Molecular weight: | 278.221 g/mol |
| Synonyms: |
6H-Purin-6-one, 2-amino-1,9-dihydro-9-((2-hydroxy-1-(hydroxymethyl)ethoxy)methyl)-, sodium salt; 84245-13-6; Ganciclovir sodium (unspecified MF); Cytovene IV; Sodium 2-amino-1,9-dihydro-9-((2-hydroxy-1-(hydroxymethyl)ethoxy)methyl)-6H-purin-6-one
|
DrugBank
Identification
| Name: | Ganciclovir |
|---|---|
| Name (isomeric): | DB01004 |
| Drug Type: | small molecule |
| Description: | An ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections. |
| Synonyms: |
GA2; Ganciclovir Sodium
|
| Brand: | Vitrasert, Cytovene, Cytovene IV, Cytovene-IV |
| Category: | Antiviral Agents |
| CAS number: | 82410-32-0 |
Pharmacology
| Indication: | For induction and maintenance in the treatment of cytomegalovirus (CMV) retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS). Also used in the treatment of severe cytomegalovirus (CMV) disease, including CMV pneumonia, CMV gastrointestinal disease, and disseminated CMV infections, in immunocompromised patients. |
|---|---|
| Pharmacology: |
Ganciclovir is a synthetic nucleoside analogue of 2'-deoxyguanosine that inhibits replication of herpes viruses both in vitro and in vivo. Sensitive human viruses include cytomegalovirus (CMV), herpes simplex virus -1 and -2 (HSV-1, HSV-2), Epstein-Barr virus (EBV) and varicella zoster virus (VZV), however clinical studies have been l...
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| Mechanism of Action: |
Ganciclovir's antiviral activity inhibits virus replication. This inhibitory action is highly selective as the drug must be converted to the active form by a virus-encoded cellular enzyme, thymidine kinase (TK). TK catalyzes phosphorylation of ganciclovir to the monophosphate, which is then subsequently converted into the diphosphate by cellular gu...
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| Absorption: | Poorly absorbed systemically following oral administration. Bioavailability under fasting conditions is approximately 5%, and when administered with food, 6 to 9% (about 30% with a fatty meal). |
| Protein binding: | 1 to 2% |
| Biotransformation: | Little to no metabolism, about 90% of plasma ganciclovir is eliminated unchanged in the urine. |
| Route of elimination: | Renal excretion of unchanged drug by glomerular filtration and active tubular secretion is the major route of elimination of ganciclovir. |
| Half Life: | 2.5 to 3.6 hours (mean 2.9 hours) when administered intravenously in adults. 3.1 to 5.5 hours when administered orally in adults. Renal function impairment causes a marked increase in half life (9 to 30 hours intravenously, 15.7 to 18.2 hours orally). |
| Clearance: | 128 +/- 63 mL/min [Patients with Renal Impairment (Clcr=50-79 mL/min)] 57+/- 8 mL/min [Patients with Renal Impairment (Clcr=25-49 mL/min)] 30 +/- 13 mL/min [Patients with Renal Impairment (Clcr<25 mL/min)] 4.7+/- 2.2 mL/min/kg [pediatric patients, aged 9 months to 12 years] |
| Toxicity: | Oral, mouse LD50: > 2g/kg. Intravenous, dog LD50: > 150mg/kg. Symptoms of overdose include irreversible pancytopenia, worsening GI symptoms, and acute renal failure. Suspected cancer agent. |
| Affected organisms: | Human Herpes Virus |
Interactions
| Food interaction: |
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Targets
Transporters
