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Ganciclovir

Ganciclovir sodium (Cytovene®) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. more...

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Administration

Oral or intravenous. Acute infections are treated in two phases:

  • induction phase, 5 mg per kilogram intravenously every 12 hours for 14-21 days, the intravenous dose given as a 1 hour infusion
  • maintenance phase, 5 mg per kg intravenously every day

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 of the eye, as treatment for CMV retinitis.

Mechanism of action

Ganciclovir is a synthetic analogue of 2'-deoxy-guanosine. It is first phosphorylated to a deoxyguanosine triphosphate (dGTP) analog. This competitively inhibits the incorporation of dGTP by viral DNA polymerase, resulting in the termination of elongation of viral DNA.

Pharmacokinetics

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, dependending on renal function (elimination takes over 24 hours in end-stage renal disease).

Side effects

Possible side effects include:

  • Headache
  • Rash
  • Neutropenia
  • Anemia
  • Low platelets
  • Kidney failure
  • Confusion
  • Seizures

Read more at Wikipedia.org


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Use of oral ganciclovir for cytomegalovirus retinitis - adapted from the New England Journal of Medicine 1995;333:615-20 - Tips from Other Journals
From American Family Physician, 1/1/96

Retinitis, a complication in 40 percent of patients with acquired immunodeficiency syndrome, may lead to partial or complete vision loss if left untreated. Intravenous ganciclovir and foscarnet are approved treatments for cytomegalovirus retinitis. However, intravenous therapy is associated with substantial cost, inconvenience and risk of catheter-related complications. Drew and colleagues studied the efficacy and safety of oral ganciclovir for the treatment of cytomegalovirus retinitis in patients with AIDS.

The multicenter, open-label randomized study included 117 persons with AIDS and newly diagnosed, stabilized cytomegalovirus retinitis. The disease was stabilized by three weeks of treatment with intravenous ganciclovir. Sixty subjects were assigned to receive oral ganciclovir (500 mg six times daily during waking hours, taken with food), and 57, subjects were assigned to receive daily intravenous ganciclovir (5 mg per kg once daily). Photographs of the fundi, taken every other week over the 20-week study period, were evaluated by an experienced ophthalmologist who was unaware of treatment assignment.

The mean time to the progression of retinitis, based on the assessment of photographs, was 57 days in the oral ganciclovir group and 62 days in the intravenous ganciclovir group. Based on funduscopy performed by ophthalmologists who were aware of the treatment assignments, the mean time to progression was 68 days in the oral treatment group, compared with 96 days in the intravenous treatment group. Neutropenia, anemia and catheter-related adverse events (including sepsis) were more common in the patients treated with intravenous ganciclovir.

The authors conclude that oral ganciclovir is safe and effective as maintenance therapy, as well as more convenient than intravenous therapy, in patients with cytomegalovirus retinitis related to AIDS. (Drew WL, et al. Oral ganciclovir as maintenance treatment for atomegalovirus retinitis in patients with AIDS. N Engl J Med 1995;333:615-20.)

COPYRIGHT 1996 American Academy of Family Physicians
COPYRIGHT 2004 Gale Group

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