Gantsiklovir

Gantsiklovir – the drug with antiviral action used at treatment of a Cytomegaloviral infection.

Form of release and structure

Gantsiklovir release in the form of powder of the solution lyophilized for preparation for infusions: porous weight white with a yellowish shade or white color, hydroscopic, condensed in a tablet (in bottles on 500 mg, 1 or 40 bottles in a cardboard pack).

Is a part of 1 bottle:

• Active agent: ганцикловир (in the form of a gantsiklovir of sodium) – 500 mg;
• Auxiliary components: sodium hydroxide – to рН 10,8-11,4.

Indications to use

• Treatment life-threatening or to sight of a manifest Cytomegaloviral (TsMV) infection at patients with immunodeficiencies, including acquired immunodeficiency syndrome (AIDS), an iatrogenic immunodeficiency which is connected with chemotherapy of new growths or organ transplantation;
• Prevention of manifest TsMV of an infection at the patients receiving immunosuppressive therapy after organ transplantation.

Contraindications

• Pregnancy and period of a lactation (feeding by a breast);
• Hypersensitivity to drug components, and also to a valgantsiklovir, an acyclovir and a valatsiklovir.

Route of administration and dosage

Treatment of TsMV of an infection at adults:

• Initial therapy: infusion in a dose of 5 mg/kg within an hour at a constant speed, every 12 hours (a daily dose – 10 mg/kg). Course duration – 2-3 weeks;
• Maintenance therapy: the patient with immunodeficiencies at risk of a recurrence of TsMV of a retinitis intravenous infusion is entered daily in a dose of 6 mg/kg within 5 days or on 5 mg/kg within 7 days;
• Therapy of a progression of a disease: by the patient with AIDS termless treatment can be appointed, however, even at long use of drug there is a probability of a progression of a retinitis. To patients at whom during a maintenance therapy or because of drug withdrawal the retinitis progresses purpose of initial therapy gantsikloviry is admissible.

For prevention of TsMV of an infection:

• Initial therapy: infusion on 5 mg/kg every 12 hours (10 mg/kg a day) within 1-2 weeks;
• Maintenance therapy: intravenous infusion is entered daily in a dose of 6 mg/kg within 5 days or on 5 mg/kg within 7 days.

Patients with a renal failure during Gantsiklovir's use need to control serum creatinine level carefully.

Patients of advanced age need to appoint drug, considering a functional condition of kidneys.

Experience of use of Gantsiklovir for children up to 12 years is limited. The side effects developing in therapy time are similar with observed at adults. Because of probability of emergence of toxic action on reproductive system and the remote carcinogenicity, during treatment it is necessary to observe extreme care, correlating advantages of treatment to possible risk. Gantsiklovir is contraindicated at neonatal and inborn TsMV of an infection.

For decrease in weight of a neutropenia or other cytopenia it is necessary to reduce a daily dose of a gantsiklovir. As a rule, the quantity of cells is normalized in 3-7 days after a dose decline or cancellation of therapy. At indisputable signs of recovery of marrow under careful control of number of white blood cells perhaps gradual increase in a dose of drug.

At considerable reduction of number of blood cells during treatment it is necessary to suspend the main therapy and/or to appoint treatment hemopoietic growth factors.

For preparation of solution of Gantsiklovir the lyophilized powder needs to be dissolved in 10 ml of sterile water for injections. Bacteriostatic water for injections with the content of parabens (parahydroxybenzoates) cannot be used.

The solution prepared in a bottle within 12 hours keeps stability at the room temperature. It is forbidden to store solution in the refrigerator.

Before introduction the single dose of Gantsiklovir should be added to basic infusion solution (5% aqueous solution of a dextrose, 0,9% sodium chloride solution, Ringer-laktata solution or Ringer).

More than 10 mg/ml are not recommended to use drug in concentration.

Gantsiklovir it is not necessary to mix with other drugs administered intravenously.

Side effects

The most frequent hematologic side effects arising during treatment are the neutropenia, thrombocytopenia and anemia.

At patients is after transplantation of solid bodies and HIV-positive patients at Gantsiklovir's use there can be disturbances from some systems of an organism:

• Circulatory and lymphatic system: very often – anemia, a neutropenia; often – a pancytopenia, a leukopenia, thrombocytopenia; infrequently – suppression of activity of marrow;
• Invasions and infections: often – sepsis (a viremiya, bacteremia), a hypodermitis, candidiasis, infections of urinary tract;
• Food and metabolism: often – anorexia, a loss of appetite;
• Immune system: infrequently – anaphylactic reactions;
• Mental disorders: often – pathological thinking, concern, a depression, confusion of consciousness; infrequently – psychotic frustration, excitement;
• Nervous system: often – sleeplessness, a headache, a hypesthesia, a dysgeusia, peripheral neuropathy, paresthesia, spasms, dizziness (except вертиго); infrequently – a tremor;
• Cardiovascular system: infrequently – hypotension, arrhythmia;
• Respiratory organs: very often – an asthma; often – cough;
• Sense bodys: often – ear pains, a floating opacity of a vitreous, peeling of a retina, macular hypostasis, pains in an eyeglobe; infrequently – conjunctivitis, a vision disorder, decrease in hearing;
• Urinogenital system: often – a renal failure, reduction of clearance of creatinine of kidneys; infrequently – a renal failure, a hamaturia, male infertility;
• Musculoskeletal system: often – an arthralgia, a mialgiya, a back pain, muscular spasms;
• Alimentary system: very often – diarrhea; often – pains in an upper part of a stomach, vomiting, nausea, abdominal pains, a lock, a dysphagy, a meteorism, dyspepsia; infrequently – a stomacace, abdominal distention, pancreatitis;
• Biliary tract and liver: often – increase in an alkaline phosphatase of blood, an abnormal liver function, increase in aspartate aminotransferase (nuclear heating plant); infrequently – increase in alaninaminotranspherase (ALT);
• Hypodermic fatty tissue and skin: often – an itch, night perspiration, dermatitis; infrequently – a small tortoiseshell, an alopecia, a xeroderma;
• Laboratory indicators: often – weight reduction, increase in creatinine in blood;
• Reactions in an injection site and the general frustration: often – an indisposition, fatigue, a fever, a pyrexia, pain, pain behind a breast, weakness, reaction in an injection site.

Special instructions

Gantsiklovir it is possible to apply only to intravenous administration, it is preferable through a plastic cannula, in a vein with an adequate blood-groove.

Drug cannot be entered intravenously quickly or struyno. Hypodermic or intramuscular introduction of Gantsiklovir can lead to strong irritation of fabrics because of high pH of solution.

To exceed the recommended dosage, the speed or frequency of infusion does not follow.

Before an initiation of treatment it is necessary to inform pregnant women on probable risk for a fruit as drug possesses potential cancerogenic and teratogenic action and can cause malignant new growths and inborn malformations.

Gantsiklovir can with firmness or is temporary oppress a spermatogenesis. During therapy women of childbearing age are recommended to use reliable methods of contraception, to men – to use a barrier method of contraception for the period of use of drug and at least 90 days later after the end of treatment.

Because of the probable remote carcinogenicity and toxic action on reproductive system children and teenagers should show extreme care at Gantsiklovir's appointment. Before purpose of drug it is necessary to correlate advantages of treatment to possible risk.

At the patients receiving Gantsiklovir cases of the expressed leukopenia, neutropenias, pancytopenias, anemias, thrombocytopenia, a miyelosupressiya and aplastic anemia were observed. It is not necessary to begin treatment at absolute number:

• Neutrophils – it is less than 500 cells in 0,00001 dl.;
• Thrombocytes – it is less than 25000 cells in 0,00001 dl.;
• Hemoglobin – is less than 8 g/dl.

Gantsiklovir patients at whom the cytopenia or the cytopenia connected with reception of medicines in the anamnesis, and also to the patients receiving radiotheraphy was observed earlier need to apply with care.

During treatment it is recommended to carry out an integrated analysis of blood, including number of thrombocytes. More often hematologic monitoring should be done to patients with a renal failure.

At patients with a heavy neutropenia, a leukopenia, thrombocytopenia and/or anemia performing treatment by hemopoietic growth factors or temporary interruption of therapy is recommended.

Gantsiklovir's influence on ability to manage potentially dangerous mechanisms or vehicles was not studied, however it is necessary to be careful in case of development during treatment of convulsive attacks, drowsiness, dizziness, an ataxy and confusion of consciousness.

Medicinal interaction

At simultaneous use of Gantsiklovir with other drugs perhaps:

• Imipenem-tsilastatin – developing of spasms;
• Probenetsid – decrease in renal clearance of a gantsiklovir;
• The zidovudine – increases AUC of a zidovudine and reduces concentration of a gantsiklovir;
• Didanozin – increase in its concentration in a blood plasma;
• Mikofenolata mofetit (MMF) – increase in concentration of a phenolic glucuronide of mikofenolovy acid (GMFK) and Gantsiklovir;
• Trimethoprimum – increase in risk of development of toxicity;
• Zaltsitabin – developing of peripheral neuropathy.

Strengthening of toxicity is possible at simultaneous use of Gantsiklovir with the drugs suppressing replication of quickly sharing cell populations: Amphotericinum In, pentamidine, dapsone, Vincristinum, флуцитозин, adriamycin, vinblastine, Trimethoprimum / сульфа combinations, a hydroxycarbamide and nukleozidny analogs.

The concomitant use of Gantsiklovir with the drugs having nefrotoksichny or myelosuppressive effects can lead to development of the additive toxicity.

Terms and storage conditions

To store in protected from light, the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 2 years.