Acyclovir Sandoz - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 35.0 mg, microcrystalline cellulose 30.0 mg, sodium carboxymethyl starch 10.0 mg, copovidone 7.5 mg, magnesium stearate 2.5 mg.

Description:White, round, biconvex tablets with a risk on one side.

Pharmacotherapeutic group:Antiviral agent

ATX: & nbsp

S.01.A.D Antiviral drugs

Pharmacodynamics:

The antiviral drug is a synthetic analogue of thymidine nucleoside. Highly active against the virus Herpes simplex 1 and 2 types; a virus that causes varicella and shingles (Varicella zoster); of the Epstein-Barr virus (virus types are listed in order of increasing minimum inhibitory concentration of acyclovir). Moderately active against cytomegalovirus.

In infected cells containing viral thymidine kinase, phosphorylation and conversion to acyclovir monophosphate occurs.

Under the influence of guanylyl cyclase acyclovir, monophosphate is converted to diphosphate and under the influence of several cellular enzymes - into triphosphate. High selectivity of action and low toxicity for humans are due to the lack of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.

Acyclovir triphosphate, "embedded" in the DNA synthesized by the virus, blocks the multiplication of the virus. Specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus.

When treating herpes, it prevents the formation of new elements of the rash, reduces the likelihood of cutaneous dissemination and visceral complications, accelerates the formation of crusts on the skin, reduces pain in the acute phase of herpes zoster. It has an immunostimulating effect.

Pharmacokinetics:

After oral administration in part absorbed from the gastrointestinal tract. Due to low lipophilicity, the absorption of acyclovir after oral administration is 20% (15-30%), but at the same time dose-dependent concentrations are created sufficient to effectively treat viral diseases. Food has no significant effect on the absorption of acyclovir. As the dose increases, bioavailability decreases. The maximum concentration after ingestion of 200 mg 5 times a day - 0.7 μg / ml. The time to reach the maximum concentration is 1.5-2.0 hours. The connection with plasma proteins is 9-33%.

Penetrates through blood-brain and placental barriers; excreted in breast milk. It penetrates well into various organs and tissues, the concentration in the cerebrospinal fluid is 50% of that in the blood. After ingestion of 1 g per day, the concentration of acyclovir in breast milk is 0.6-4.1% of its concentration in the plasma (at such concentrations in breast milk, infants who are breastfed can receive acyclovir with milk of mother in a dose to 0.3 mg / kg per day).

Metabolized in the liver with the formation of a metabolite - 9 carboxymethoxymethylguanine. 62-91% unchanged is displayed kidneys by glomerular filtration and tubular secretion. Less than 2% is excreted through the gastrointestinal tract; trace amounts are determined in the exhaled air. The half-life (T1/2) when ingested in adults - 3.3 hours, in children and adolescents from 3 to 18 years - 2.6 hours. The rate of excretion slows down with age, but T_1/2the active drug increases slightly.

In patients with severe chronic renal insufficiency T_1/2 - Up to 20 hours. T_1/2with renal failure (in adults, depending on the values of creatinine clearance): with creatinine clearance 80 ml / min - 2.5 hours, 50-80 ml / min - 3 hours, 15-50 ml / min - 3.5 hours, with anuria - 19.5 hours, during hemodialysis - 5.7 hours, with permanent ambulatory peritoneal dialysis - 14-18 hours.

With a single hemodialysis session for 6 hours, the concentration of acyclovir in the plasma decreases by approximately 60%.

Indications:

- Treatment of infections of the skin and mucous membranes caused by the herpes simplex virus, including primary and recurrent genital herpes;

- prevention of recurrence of infections caused by the herpes simplex virus, in patients with normal immune status;

- Prevention of infections caused by the herpes simplex virus, in patients with immunodeficiency;

- treatment of varicella and herpes zoster;

- treatment of patients with severe immunodeficiency, mainly with late stages of HIV infection (number of cells Cd4+ less than 200 / mm³ in patients with AIDS or severe manifestations of AIDS-associated complex) and patients who underwent bone marrow transplantation.

Contraindications:

- Hypersensitivity to acyclovir, valaciclovir and / or other components of the drug;

- Children under 3 years old (for this dosage form);

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:

With caution, the drug should be used in patients with chronic renal failure and in various conditions accompanied by dehydration (vomiting, diarrhea, etc.).

Pregnancy and lactation:

The use of the drug during pregnancy is possible in the event that the intended use for the mother exceeds the potential risk to the fetus.

Acyclovir penetrates into breast milk, so during lactation a woman should refuse breastfeeding.

Dosing and Administration:

Inside, squeezed a little water, if possible, after eating. For the greatest effectiveness of acyclovir, it is necessary to start taking the drug as early as possible after the appearance of skin symptoms of the disease.

Application in adults

Treatment of infections caused by herpes simplex viruses

For the treatment of infections caused by the herpes simplex virus, the recommended dose of the drug Acyclovir Sandoz® is 200 mg (1 tablet) 5 times a day every 4 hours, except during the night sleep. Usually the course of treatment is 5 days, but can be prolonged with severe primary infections.

In the case of severe immunodeficiency (for example, after bone marrow transplantation) or with a violation of absorption from the intestine, the dose of the drug Acyclovir Sandoz® for oral administration can be increased to 400 mg (2 tablets) 5 times a day.

Treatment should be started as soon as possible after the onset of infection; with relapses the drug is recommended to be prescribed already in the prodromal period or with the appearance of the first elements of the rash.

Prevention of recurrence of infections caused by the herpes simplex virus in patients with normal immune status.

To prevent the recurrence of infections caused by the herpes simplex virus in patients with normal immune status, the recommended dose of the drug Acyclovir Sandoz® is 200 mg (1 tablet) 4 times a day (every 6 hours). A more convenient scheme of 400 mg (2 tablets) therapy is suitable for many patients 2 times a day (every 12 hours).

In some cases, lower doses of the drug are effective Acyclovir Sandoz® - 200 mg (1 tablet) 3 times a day (every 8 hours) or 2 times a day (every 12 hours).

The treatment period should not exceed 6-12 months.

If against the background of a daily dose of 800 mg recurrence of infection occurs, 200 mg of the drug should be prescribed Acyclovir Sandoz® (1 tablet) 5 times a day (every 4 hours) for 5 days. Then you should return to the original dose.

Prevention of infections caused by the herpes simplex virus in patients with immunodeficiency

To prevent infections caused by the herpes simplex virus, in immunocompromised patients, the recommended dose of the drug Acyclovir Sandoz® is 200 mg 4 times a day (every 6 hours). In the case of severe immunodeficiency (for example, after bone marrow transplantation) or with a violation of absorption from the intestine, the dose of the drug Acyclovir Sandoz® for oral administration can be increased to 400 mg 4 times a day (every 6 hours). The duration of the preventive course of therapy is determined by the length of the period when there is a risk of infection. It is important to remember that in patients with impaired immunity, resistance to the drug may develop.

Treatment of varicella and herpes zoster

For the treatment of varicella and herpes zoster, the recommended dose of the drug Acyclovir Sandoz® is 800 mg 5 times a day; the drug is taken every 4 hours, except during the night sleep. The course of treatment is 7 days.

The drug should be prescribed as soon as possible after the onset of infection, since in this case the treatment is more effective.

Treatment of patients with severe immunodeficiency

For the treatment of patients with severe immunodeficiency, the recommended dose of the drug Acyclovir Sandoz® is 800 mg 4 times a day (every 6 hours). Patients who underwent bone marrow transplantation before prescribing the drug Acyclovir Sandoz® recommends the use of intravenous therapy with acyclovir for 1 month.

Use in children aged 3 years

Treatment of infections caused by the herpes simplex virus; prevention of infections caused by the virus, herpes simplex, in children with immunodeficiency

- from 3 years and older - the same dose as for adults.

Treatment of chicken pox

- over 6 years - 800 mg (4 tablets) 4 times a day;

- from 3 to 6 years - 400 mg (2 tablets) 4 times a day.

More precisely, the dose can be determined from the calculation of 20 mg / kg body weight (but not more than 800 mg) 4 times a day. The course of treatment is 5 days.

Data on the prevention of recurrence of infections caused by the herpes simplex virus and the treatment of herpes zoster, herpes in children with normal immunity parameters are absent.

Treatment of pediatric patients with severe immunodeficiency

According to available very limited information, for the treatment of children older than 3 years with severe immunodeficiency, the same doses of the drug can be used as for the treatment of adults with immunodeficiency (800 mg 4 times a day,every 6 hours).

Use in elderly patients

In the elderly, there is a decrease in clearance of acyclovir in the body in parallel with a decrease in the clearance of creatinine.

Elderly patients should receive a sufficient amount of fluid on the background of taking high doses of the drug Acyclovir Sandoz® inside, with renal failure they need to solve the problem of reducing the dose of the drug.

Use in patients with renal insufficiency

Care should be taken when prescribing the drug Acyclovir Sandoz® patients with renal insufficiency.

In patients with renal insufficiency, taking acyclovir orally at the recommended doses for the treatment and prevention of infections caused by the herpes simplex virus does not result in cumulation of the drug to concentrations exceeding the established safe levels. However, in patients with severe renal failure (creatinine clearance less than 10 ml / min), the dose of the drug is recommended to be reduced to 200 mg twice a day (every 12 hours).

In the treatment of varicella zoster, herpes zoster, and also in the treatment of patients with severe immunodeficiency, the recommended dose of the drug Acyclovir Sandoz® are:

- with moderate renal failure (creatinine clearance 10-25 ml / min) 800 mg 3 times a day every 8 hours;

- with severe renal failure (creatinine clearance less than 10 ml / min) 800 mg 2 times a day every 12 hours.

Side effects:

According to the World Health Organization (WHO) the undesirable effects are classified according to their frequency of development as follows: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1/10000, <1/1000), very rarely (<1/10000).

From the immune system: rarely: anaphylaxis.

From the digestive system: often: nausea, vomiting, diarrhea, abdominal pain; rarely: transient increase in activity of "hepatic" transaminases and bilirubin concentration; rarely: hepatitis, jaundice.

From the nervous system: often: headache, dizziness; rarely: psychotic disorders, tremor, ataxia, dysarthria, convulsions, encephalopathy, coma, hallucinations, drowsiness, agitation, confusion, paresthesia. Usually found in patients with impaired renal function or in the presence of other provoking factors, were, in general, reversible.

From the genitourinary system: rarely: transient increase in the concentration of urea, creatinine in the blood plasma; rarely: acute renal failure, renal colic. Renal colic can be associated with kidney failure.

From the respiratory system, chest and mediastinum: rarely: dyspnea.

From the skin and subcutaneous tissues: often: rash, including photosensitivity, itchy skin; infrequently: urticaria, rapid diffuse hair loss (since this type of hair loss is associated with various diseases and medications, the relationship between this event and acyclovir is uncertain); rarely: angioedema; rarely: multiforme exudative erythema, incl. Stevens-Johnson syndrome, Lyell syndrome.

From the side of the blood and lymphatic system: rarely: anemia, leukopenia, thrombocytopenia.

Other: often: fever, fatigue; rarely: malaise.

Overdose:

Acyclovir is only partially absorbed in the gastrointestinal tract. With occasional single-dose aciclovir oral doses of up to 5 g, no toxic effects have been reported.

Symptoms: vomiting, nausea, shortness of breath, impaired renal function, neurological symptoms, agitation, coma, convulsions, lethargy.It is possible to precipitate acyclovir in the renal tubules if its concentration exceeds the solubility in the renal tubules (2.5 mg / ml).

Treatment: monitoring of basic vital functions, hemodialysis.

Interaction:

There were no clinically significant interactions with acyclovir.

Drugs that block tubular secretion (for example, probenecid and cimetidine), immunosuppressive drugs, increase the concentration of acyclovir in plasma. However, dose adjustment is not required due to a wide range of therapeutic doses of acyclovir.

Special instructions:

It is important to remember that prolonged or repeated treatment with acyclovir in patients with reduced immunity can lead to the appearance of strains of viruses that are insensitive to its action. The majority of isolated strains of viruses, insensitive to acyclovir, show a relative lack of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. In vitro action of acyclovir on isolated strains of the virus Herpes simplex may cause the appearance of less sensitive strains.

During treatment with high oral doses of the drug should ensure sufficient fluid intake in the patient's body. Acyclovir does not prevent the transmission of sexual herpes, therefore during the treatment it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.

Special precautions when destroying an unused preparation

There is no need for special precautions when destroying an unused preparation.

Effect on the ability to drive transp. cf. and fur:Data on the negative effect Acyclovir Sandoz® in recommended doses for the ability to drive a car or work with mechanisms there. However, since the drug may develop drowsiness and dizziness, care should be taken when driving vehicles and engaging in other activities that require concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets 200 mg.

Packaging:

For 5 tablets in a blister of PVC /Al foil.

For 1, 2, 3 or 5 blisters together with instructions for medical use are placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use at the end of the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001538

Date of registration:27.02.2012

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

SALUTAS PHARMA, GmbH Germany

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp11.09.2014

Illustrated instructions

Instructions

Acyclovir Sandoz® (Aciclovir Sandoz®)