GA2
GA2 Brand names, GA2 Analogs
GA2 Brand Names Mixture
- No information avaliable
GA2 Chemical_Formula
C9H13N5O4
GA2 RX_link
http://www.rxlist.com/cgi/generic2/vitrasert.htm
GA2 fda sheet
GA2 msds (material safety sheet)
GA2 Synthesis Reference
Alhede, Boerge; et al.; J.Org.Chem.; 56; 6;2139-2143(1991)
GA2 Molecular Weight
255.231 g/mol
GA2 Melting Point
250 oC
GA2 H2O Solubility
4.3 mg/mL
GA2 State
Solid
GA2 LogP
-1.438
GA2 Dosage Forms
Occular insert; Oral capsule; Injection
GA2 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.
GA2 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 limited to assessment of efficacy in patients with CMV infection. Ganciclovir is a prodrug that is structurally similar to acyclovir. It inhibits virus replication 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.
GA2 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).
GA2 side effects and 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.
GA2 Patient Information
All patients should be informed that the major toxicities of ganciclovir are granulocytopenia
(neutropenia), anemia and thrombocytopenia and that dose modifications may be required, including
discontinuation. The importance of close monitoring of blood counts while on therapy should be emphasized.
Patients should be informed that ganciclovir has been associated with elevations in serum creatinine.
Patients should be instructed to take CYTOVENE capsules with food to maximize bioavailability.
Patients should be advised that ganciclovir has caused decreased sperm production in animals and may cause
infertility in humans. Women of childbearing potential should be advised that ganciclovir causes birth
defects in animals and should not be used during pregnancy. Women of childbearing potential should be
advised to use effective contraception during treatment with CYTOVENE-IV or CYTOVENE. Similarly, men
should be advised to practice barrier contraception during and for at least 90 days following treatment
with CYTOVENE-IV or CYTOVENE.
Patients should be advised that ganciclovir causes tumors in animals. Although there is no information
from human studies, ganciclovir should be considered a potential carcinogen.
All HIV+ Patients: These patients may be receiving zidovudine (Retrovir?*). Patients should be counseled
that treatment with both ganciclovir and zidovudine simultaneously may not be tolerated by some patients
and may result in severe granulocytopenia (neutropenia). Patients with AIDS may be receiving didanosine
(Videx?#). Patients should be counseled that concomitant treatment with both ganciclovir and didanosine
can cause didanosine serum concentrations to be significantly increased.
HIV+ Patients With CMV Retinitis: Ganciclovir is not a cure for CMV retinitis, and immunocompromised
patients may continue to experience progression of retinitis during or following treatment. Patients
should be advised to have ophthalmologic follow-up examinations at a minimum of every 4 to 6 weeks while
being treated with CYTOVENE-IV or CYTOVENE. Some patients will require more frequent follow-up.
Transplant Recipients: Transplant recipients should be counseled regarding the high frequency of impaired
renal function in transplant recipients who received CYTOVENE-IV solution in controlled clinical trials,
particularly in patients receiving concomitant administration of nephrotoxic agents such as cyclosporine
and amphotericin B. Although the specific mechanism of this toxicity, which in most cases was reversible,
has not been determined, the higher rate of renal impairment in patients receiving CYTOVENE-IV solution
compared with those who received placebo in the same trials may indicate that CYTOVENE-IV played a
significant role.
(neutropenia), anemia and thrombocytopenia and that dose modifications may be required, including
discontinuation. The importance of close monitoring of blood counts while on therapy should be emphasized.
Patients should be informed that ganciclovir has been associated with elevations in serum creatinine.
Patients should be instructed to take CYTOVENE capsules with food to maximize bioavailability.
Patients should be advised that ganciclovir has caused decreased sperm production in animals and may cause
infertility in humans. Women of childbearing potential should be advised that ganciclovir causes birth
defects in animals and should not be used during pregnancy. Women of childbearing potential should be
advised to use effective contraception during treatment with CYTOVENE-IV or CYTOVENE. Similarly, men
should be advised to practice barrier contraception during and for at least 90 days following treatment
with CYTOVENE-IV or CYTOVENE.
Patients should be advised that ganciclovir causes tumors in animals. Although there is no information
from human studies, ganciclovir should be considered a potential carcinogen.
All HIV+ Patients: These patients may be receiving zidovudine (Retrovir?*). Patients should be counseled
that treatment with both ganciclovir and zidovudine simultaneously may not be tolerated by some patients
and may result in severe granulocytopenia (neutropenia). Patients with AIDS may be receiving didanosine
(Videx?#). Patients should be counseled that concomitant treatment with both ganciclovir and didanosine
can cause didanosine serum concentrations to be significantly increased.
HIV+ Patients With CMV Retinitis: Ganciclovir is not a cure for CMV retinitis, and immunocompromised
patients may continue to experience progression of retinitis during or following treatment. Patients
should be advised to have ophthalmologic follow-up examinations at a minimum of every 4 to 6 weeks while
being treated with CYTOVENE-IV or CYTOVENE. Some patients will require more frequent follow-up.
Transplant Recipients: Transplant recipients should be counseled regarding the high frequency of impaired
renal function in transplant recipients who received CYTOVENE-IV solution in controlled clinical trials,
particularly in patients receiving concomitant administration of nephrotoxic agents such as cyclosporine
and amphotericin B. Although the specific mechanism of this toxicity, which in most cases was reversible,
has not been determined, the higher rate of renal impairment in patients receiving CYTOVENE-IV solution
compared with those who received placebo in the same trials may indicate that CYTOVENE-IV played a
significant role.
GA2 Organisms Affected
Human herpes virus
