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Ganciclovir

Ganciclovir is an antiviral medication used to treat cytomegalovirus infections. A prodrug form with improved oral bioavailability has also been developed. More

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Description

Ganciclovir is an antiviral medication used to treat cytomegalovirus infections. A prodrug form with improved oral bioavailability has also been developed.

Generic Name

Ganciclovir

Chemical names

Ganciclovir; Gancyclovir; Cytovene; Vitrasert

Brand names

Cymevene, Cytogan, Ganguard, Gatlevir, Gavir, Natclovir

IUPAC name

2-amino-9-{[(1,3-dihydroxypropan-2-yl)oxy]methyl}-6,9-dihydro-1H-purin-6-one

Pharmacokinetics

Oral absorption is poor.

Actions

It is a prodrug structurally similar to acyclovir, is a 2'-deoxyguanosine synthetic nucleoside analogue of 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 limited to assessment of efficacy in patients with CMV infection. It is inhibited the replication of virus by its encorporation into viral DNA. This encorporation inhibits dATP and leads to defective DNA, ceasing or retarding the viral machinery required to spread the virus to other cells.

Dosage/Dosage form

The recommended dose is 5mg/kg as IV.

Therapeutic uses

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 CMV gastrointestinal disease, CMV pneumonia, and disseminated CMV infections in immunocompromised patients.

Adverse effects/Side effects

Haematolgical disturbances; marrow depression; GI disturbances; fever, rash and abnormal LFTs; irritation and phlebitis at inj site. CNS, CV, metabolic, musculoskeletal, urogenital, respiratory, cutaneous symptoms, ocular effects, and increased serum-creatinine and BUN concentration are less frequent. Potential risk of testicular effects and female fertility.

Interaction

Renal clearance reduced by probenecid; imipenem cilastatin (generalised seizures); zidovudine; didanosine; additive toxic effects with myelosuppressants; oral mycophenolate mofetil.

Contraindications

Hypersensitivity; absolute neutrophil count <500 cells/mm3; platelet count <25,000/mm3; pregnancy, lactation. Not to be used as a bolus inj.

Storage

Store at 15-25 ?

Information

Molecular weight

255.2306

Molecular formula

C9H13N5O4

CAS number

82410-32-0

Precautions

  • Renal impairment; preexisting cytopenias or history of cytopenic reactions to drugs; child; contraceptive precautions to be followed during and at least 90 days thereafter; care in administering only into veins with good blood flow.
  • Avoid contact with the skin and eyes.
  • Maintain adequate hydration during infusion.
  • Monitor WBC and platelet counts regularly during treatment.
  • Eye examinations should be conducted at least once every 4-6 wk during treatment for CMV retinitis.