Acyclovir pills 400mg №21

Release form, composition and packaging

Tablets, film coated pale pink, elliptical, with a risk on one side.
1 tab. acyclovir 400 mg

Excipients: povidone, sodium carboxymethyl starch, microcrystalline cellulose, colloidal silicon dioxide, Magnesium stearate.

Shell composition: Opadry Pink OY-24926 (hypromellose, titanium dioxide, macrogol, iron dye red oxide, iron dye yellow oxide).

Mechanism of action

Acyclovir is an antiviral drug, a synthetic analogue of the acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside viral infected cells, viral thymidine kinase undergoes a series of consecutive transformations of acyclovir into mono-, di-, and acyclovir triphosphate. Acyclovir triphosphate is incorporated into the chain of viral DNA and blocks its synthesis through competitive inhibition of viral DNA polymerase.
In vitro, acyclovir is effective against herpes simplex virus - Herpes simplex type I and II, against Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.
In vivo acyclovir is therapeutically and prophylactically effective primarily in viral infections caused by Herpes simplex.

Pharmacokinetics

When ingestion bioavailability is 15-30%.Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Binding to plasma proteins is 9-33% and does not depend on its concentration in plasma. The concentration in the cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir penetrates the placental barrier and accumulates in breast milk. Cmax after administration orally 200 mg 5 times a day - 0.7 mcg / ml, Tmax - 1.5-2 hours.
Metabolized in the liver to form a pharmacologically inactive compound 9-carboxymethoxymethylguanine. T1 / 2 in adults with normal kidney function is 2-3 hours.
In patients with severe renal insufficiency T1 / 2 - 20 hours, with hemodialysis - 5.7 hours (while the concentration of acyclovir in plasma decreases to 60% of the initial value).
About 84% is excreted by the kidneys in unchanged form and 14% in the form of a metabolite. Renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted through the intestines.

Dosage

Inside
Treatment should begin as soon as possible, immediately after the appearance of the first symptoms of the disease.
The dosage regimen is set individually, depending on the severity of the disease.
In the treatment of infections of the skin and mucous membranes caused by Herpes simplex type I and II, for adults and children over 3 years old, the drug is prescribed 200 mg 5 times / day for 5 days with 4-hour intervals during the day and with 8-hour interval for the night. In more severe cases of the disease, the course of treatment may be extended by a doctor’s prescription.
As part of complex therapy for severe immunodeficiency, including with a developed clinical picture of HIV infection (including early clinical manifestations of HIV infection and the AIDS stage), after bone marrow implantation, 400 mg is prescribed 5 times / day.
For the prevention of recurrence of infections caused by Herpes simplex type I and II viruses, patients with a normal immune status and with a relapse of the disease are prescribed 200 mg 4 times / day every 6 hours.
For the prevention of infections caused by Herpes simplex type I and II viruses, adults and children over 3 years old with immunodeficiency, the drug is recommended to be prescribed 200 mg 4 times / day every 6 hours, maximum dose - up to 400 mg of acyclovir 5 times / day depending on the severity of the infection.
When treating infections caused by Varicella zoster, adults are prescribed 800 mg 5 times / day every 4 hours during the day and with an 8 hour interval for the night. Duration of treatment is 7-10 days. Children over 3 years old are prescribed 20 mg / kg 4 times / day for 5 days, children weighing more than 40 kg are prescribed the drug in the same dosage as adults.
When treating infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days.
In patients with impaired renal function:
In the treatment and prevention of infections caused by Herpes simplex, in patients with CC less than 10 ml / min, the dose should be reduced to 200 mg 2 times / day at 12-hour intervals.
In the treatment of infections caused by Varicella zoster, in patients with CC less than 10 ml / min, it is recommended to reduce the dose of the drug to 800 mg 2 times / day at 12-hour intervals; at QC up to 25 ml / min, 800 mg is prescribed 3 times / day with 8-hour intervals.
The drug is taken during or immediately after a meal and washed down with a sufficient amount of water.

Overdosage

Oral administration of 20 g of acyclovir did not lead to the development of specific symptoms.
There may be side effects from the central nervous system - convulsions, tremor, lethargy.
In case of overdose after ingestion, it is necessary to induce vomiting (preferably within 30 minutes after taking the drug) and take the adsorbents.
In the case of acute renal failure and anuria: maintenance of vital functions, hemodialysis.

Drug interaction

Simultaneous use with probenecid leads to an increase in the average half-life and a decrease in clearance of acyclovir.
When taken simultaneously with nephrotoxic drugs increases the risk of impaired renal function.
Amplification of the effect is observed with simultaneous administration of immunostimulants.

Pregnancy and lactation

Use during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus. Acyclovir penetrates the placental barrier and accumulates in breast milk.
If you need to take acyclovir during lactation requires interruption of breastfeeding.

Side effects

The drug is usually well tolerated.
On the part of the digestive system: in isolated cases - abdominal pain, nausea, vomiting, diarrhea.
On the part of laboratory parameters: passing a slight increase in the activity of liver enzymes, rarely a slight increase in urea and creatinine levels, hyperbilirubinemia, leukopenia, erythropenia.
From the side of the central nervous system and peripheral nervous system: rarely - headache, weakness; in some cases - tremor, dizziness, fatigue, drowsiness, confusion, hallucinations, paresthesia, agitation.
Allergic reactions: Anaphylactic reactions, skin allergic reactions (itching, Lyell's syndrome, urticaria, erythema multiforme exudative, including Stevens-Johnson syndrome), peripheral edema.
Other: rarely - alopecia, fever, myalgia, blurred vision, lymphadenopathy.

Indications

- treatment of infections of the skin and mucous membranes caused by Herpes simplex type I and II viruses, both primary and secondary, including genital herpes;
- prevention of exacerbations of recurrent infections caused by the viruses Herpes simplex type I and II, y patients with normal immune status;
- prevention of primary and recurrent infections caused by Herpes simplex type I and II viruses in patients with immunodeficiency;
- as part of the complex therapy of patients with severe immunodeficiency: in HIV infection (AIDS stage, early clinical manifestations and detailed clinical picture) and in patients undergoing bone marrow transplantation;
- treatment of primary and recurrent infections caused by the virus Varicella zoster (chickenpox, as well as herpes zoster - Herpes zoster).

Contraindications

- Hypersensitivity to acyclovir, ganciclovir, famciclovir, valacyclovir, or any excipient of the drug;
- lactation period;
- children's age up to 3 years (for this dosage form).
With care: dehydration, renal failure, neurological disorders, incl. in the anamnesis.

Special notes

Prolonged or repeated treatment with acyclovir in patients with reduced immunity can lead to the appearance of virus strains that are not sensitive to its action. Apply strictly on doctor's prescription in order to avoid complications in adults and children over 3 years old.
With caution prescribed to patients with impaired renal function, elderly patients due to an increase in the half-life of acyclovir.
When using the drug it is necessary to ensure the supply of a sufficient amount of liquid.
When taking the drug should monitor kidney function (blood urea and plasma creatinine).
Acyclovir does not prevent the transmission of herpes through sexual contact, therefore during the treatment period it is necessary to refrain from sexual intercourse, even in the absence of clinical manifestations.

In case of impaired renal function

In the treatment and prevention of infections caused by Herpes simplex, in patients with CC less than 10 ml / min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals.
When treating infections caused by Varicella zoster, in patients with QA less than 10 ml / min, it is recommended to reduce the dosage of the drug to 800 mg 2 times / day with 12-hour intervals; at QC up to 25 ml / min, 800 mg is prescribed 3 times / day with 8-hour intervals.

Use in old age

Be wary appoint elderly patients in connection with the increase in the half-life of acyclovir.

Use in childhood

The drug is contraindicated in children under 3 years (for this dosage form).

Terms and conditions of storage

Keep out of reach of children at a temperature not exceeding 25 ° C.
Shelf life - 2 years. Do not use after the expiration date printed on the package.