| Systematic (IUPAC) name | |
|---|---|
| 2-amino-9-{[(1,3-dihydroxypropan-2-yl)oxy]methyl}-6,9-dihydro-3H-purin-6-one | |
| Clinical data | |
| Trade names | Cytovene |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a605011 |
| Pregnancy cat. | D (Au), C (U.S.) |
| Legal status | S4 (Au), POM (UK), ℞-only (U.S.) |
| Routes | IV, oral, intravitreal |
| Pharmacokinetic data | |
| Bioavailability | 5% (oral) |
| Metabolism | guanylate kinase (CMV UL97 gene product) |
| Half-life | 2.5–5 hours |
| Excretion | Renal |
| Identifiers | |
| CAS number | 82410-32-0 |
| ATC code | J05AB06 S01AD09 |
| PubChem | CID 3454 |
| DrugBank | APRD00263 |
| ChemSpider | 3336 |
| UNII | P9G3CKZ4P5 |
| KEGG | D00333 |
| ChEBI | CHEBI:465284 |
| ChEMBL | CHEMBL182 |
| Chemical data | |
| Formula | C9H13N5O4 |
| Mol. mass | 255.23 g/mol |
| SMILES | eMolecules & PubChem |
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Ganciclovir INN ( /ɡænˈsaɪkləvɪər/) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections.Ganciclovir sodium is marketed under the trade names Cytovene and Cymevene (Roche). Ganciclovir for ocular use is marketed under the trade name Vitrasert (Bausch & Lomb). A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.
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Ganciclovir is a synthetic analogue of 2'-deoxy-guanosine. It is first phosphorylated to a deoxyguanosine triphosphate (dGTP) analogue. This competitively inhibits the incorporation of dGTP by viral DNA polymerase, resulting in the termination of elongation of viral DNA.
Ganciclovir is indicated for:[1]
It is also used for acute CMV colitis in HIV/AIDS and CMV pneumonitis in immunosuppressed patients.
Ganciclovir is commonly associated with a range of serious haematological adverse effects. Common adverse drug reactions (≥1% of patients) include: granulocytopenia, neutropenia, anaemia, thrombocytopenia, fever, nausea, vomiting, dyspepsia, diarrhoea, abdominal pain, flatulence, anorexia, raised liver enzymes, headache, confusion, hallucination, seizures, pain and phlebitis at injection site (due to high pH), sweating, rash, itch, increased serum creatinine and blood urea concentrations.[1]
Ganciclovir is considered a potential human carcinogen, teratogen, and mutagen. It is also considered likely to cause inhibition of spermatogenesis. Thus, it is used judiciously and handled as a cytotoxic drug in the clinical setting.[1][2]
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, depending on renal function (elimination takes over 24 hours in end-stage renal disease).
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 the vitreous humour of the eye, as treatment for CMV retinitis (associated with HIV infection).
A topical ophthalmic gel preparation of ganciclovir was recently approved for the treatment acute herpes simplex keratitis.
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