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Description
Ganciclovir is an oxopurine that is guanine substituted by a [(1,3-dihydroxypropan-2-yl)oxy]methyl group at position 9. Ganciclovir is an antiviral drug used to treat or prevent AIDS-related cytomegalovirus infections. It has a role as an antiviral drug and an antiinfective agent. It is an oxopurine and a member of 2-aminopurines. It is functionally related to a guanine.
Ganciclovir is an antiviral prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of cytomegalovirus retinitis (CMV retinitis) in adults who are immunocompromised, including individuals with AIDS. Ganciclovir is also FDA-approved for the prevention of CMV disease in recipients of organ transplants who are at risk for CMV diseases. CMV diseases, including CMV retinitis, can be opportunistic infections (OIs) of HIV.
Properties and characteristics of Ganciclovir
| Drug class | Antiviral drug |
| Brand Names | Cytovene, Zirgan |
| Synonyms | Ganciclovir, Ganciclovirum, Gancyclovir |
| Molecular Formula | C9H13N5O4 |
| Molecular Weight | 255.23 g/mol |
| IUPAC Name | 2-amino-9-(1,3-dihydroxypropan-2-yloxymethyl)-1H-purin-6-one |
| Structural formula of main components |  |
| Pure active ingredient | Ganciclovir |
| Appearance | White to off-white solid |
| Melting point | 250 °C |
| Solubility | In water (25 °C): 4.3 mg/mL at pH 7 |
| Excretion | Renal excretion of unchanged drug by glomerular filtration and active tubular secretion is the major route of elimination of ganciclovir. |
| Storage | Recommended storage temperature: 2 – 8 °C. Keep in a dry place. |
| Available Forms | Solution, Capsule, Injection, Powder for solution |
| Prescription | Do not consume without the doctors’ advice |
Ganciclovir uses
Ganciclovir is used for:
- Sight-threatening CMV retinitis in severely immunocompromised people
- CMV pneumonitis in bone marrow transplant recipients
- Prevention of CMV disease in bone marrow and solid organ transplant recipients
- Confirmed CMV retinitis in people with AIDS (intravitreal implant)
It is also used for acute CMV colitis in HIV/AIDS and CMV pneumonitis in immunosuppressed patients.
Ganciclovir has also been used with some success in treating Human herpesvirus 6 infections.
Ganciclovir has also been found to be an effective treatment for herpes simplex virus epithelial keratitis.
Ganciclovir Side Effects
Ganciclovir side effects for children and teens may include:
- Headaches
- Dizziness
- Nervousness
- Confusion
You may notice your child has less interest in eating than usual. Sometimes, people taking ganciclovir have stomach upset that ranges from mild upset to nausea and vomiting. Other side effects include tremor, weakness, and swollen ankles or feet. These side effects are all relatively common with this medication, and not cause for alarm.
In rare cases, some people have these side effects when taking ganciclovir:
- Skin rash
- Sore throat
- Fever
- Chills
- Cough
- Unusual bleeding or bruising
- Confusion or severe abdominal pain
If any of these side effects continues or becomes bothersome, inform your transplant doctor or transplant coordinator.
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 guanylate kinase and into the triphosphate by a number of cellular enzymes. In vitro, ganciclovir triphosphate stops replication of herpes viral DNA. When used as a substrate for viral DNA polymerase, ganciclovir triphosphate competitively inhibits dATP leading to the formation of ‘faulty’ DNA. This is where ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed.
Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Bupropion
- Emtricitabine
- Imipenem
- Levoketoconazole
- Maribavir
- Methotrexate
- Tenofovir Alafenamide
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Didanosine
Other Interactions
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Kidney disease—Ganciclovir may build up in the blood in patients with kidney disease, increasing the chance of side effects
- Low platelet counts or
- Low white blood cell count—Ganciclovir may make these blood diseases worse
Dosing
The dose of this medicine will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage form (capsules):
- For treatment of CMV retinitis after you have received ganciclovir injection for at least fourteen to twenty-one days:
- Adults and teenagers—1000 milligrams (mg) three times a day with food; or 500 mg six times a day, every three hours with food, during waking hours.
- Children—Use and dose must be determined by your doctor.
- For prevention of CMV disease in transplant patients and patients with advanced HIV infection:
- Adults and teenagers—1000 mg three times a day with food.
- Children—Use and dose must be determined by your doctor.
- For treatment of CMV retinitis after you have received ganciclovir injection for at least fourteen to twenty-one days:
- For injection dosage form:
- For treatment of CMV retinitis:
- Adults and teenagers—Dose is based on body weight and must be determined by your doctor. At first, 5 mg per kilogram (2.3 mg per pound) of body weight is injected into a vein every twelve hours for fourteen to twenty-one days. Then, 5 mg per kilogram (2.3 mg per pound) of body weight is injected into a vein once a day for seven days of the week; or 6 mg per kilogram (2.7 mg per pound) of body weight is injected into a vein once a day for five days of the week.
- Children—Use and dose must be determined by your doctor.
- For prevention of CMV in transplant patients:
- Adults and teenagers—Dose is based on body weight and must be determined by your doctor. At first, 5 mg per kilogram (2.3 mg per pound) of body weight is injected into a vein every twelve hours for seven to fourteen days. Then the dose is reduced to 5 mg per kilogram (2.3 mg per pound) of body weight once a day for seven days of the week; or 6 mg per kilogram (2.7 mg per pound) of body weight is injected into a vein once a day for five days of the week.
- Children—Use and dose must be determined by your doctor.
- For treatment of CMV retinitis:
What happens if I overdose on Ganciclovir?
Overdose symptoms may include
- Vomiting
- Diarrhea
- Decreased urination
- Yellowing of the skin or eyes
- Seizure
- Infections (fever, chills, frequent illness)
If you think you or someone else may have overdosed on: Ganciclovir (Cytovene), call your doctor or the Poison Control center.
Warnings
Ganciclovir can weaken (suppress) your immune system, and you may get an infection or bleed more easily. Call your doctor if you have unusual bruising or bleeding, pale skin, cold hands and feet, feeling light-headed or short of breath, or signs of infection (fever, chills, tiredness, mouth sores, skin sores, frequent or recurring illness).
Ganciclovir can cause birth defects. Both men and women using ganciclovir should use effective birth control to prevent pregnancy. Keep using birth control for at least 30 days (for women) or 90 days (for men) after your last dose. ganciclovir may also affect fertility in a man or a woman.
Before taking this medicine
You should not use this medicine if you are allergic to ganciclovir or valacyclovir.
Tell your doctor if you have ever had:
- Kidney disease (or if you are on dialysis);
- Low blood cell counts; or
- Radiation treatment.
Using ganciclovir may increase your risk of developing certain types of cancers. Ask your doctor about this risk.
Ganciclovir can harm an unborn baby or cause birth defects if the mother or the father is using this medicine.
- If you are a woman, do not use ganciclovir if you are pregnant. You may need to have a negative pregnancy test before starting this treatment. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 30 days after your last dose.
- If you are a man, use effective birth control if your sex partner is able to get pregnant. Keep using birth control for at least 90 days after your last dose.
- Tell your doctor right away if a pregnancy occurs while either the mother or the father is using ganciclovir.
This medicine may affect fertility (ability to have children) in both men and women. However, it is important to use birth control to prevent pregnancy because ganciclovir can harm an unborn baby.
Women with HIV or AIDS should not breastfeed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.
Do not give this medicine to a child without medical advice.
