Acyclovir-AKOS
Acyclovir-AKOS: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Aciclovir-AKOS
ATX code: J05AB01
Active ingredient: aciclovir (aciclovir)
Manufacturer: Sintez JSC (Russia)
Description and photo update: 2018-25-10
Prices in pharmacies: from 33 rubles.
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Acyclovir-AKOS is an antiviral (antiherpetic) drug.
Release form and composition
The drug is produced in the following forms:
- tablets: flat-cylindrical, with a line and a chamfer, white (10 pcs. in a contoured cell package, in a cardboard box 1, 2 or 3 packages; 20 pcs. in glass jars, in a cardboard box 1 can);
- ointment for external use: white or white with a yellow tinge (5 g each in aluminum tubes, in a cardboard box 1 tube).
1 tablet of Acyclovir-AKOS contains:
- active substance: acyclovir - 200 mg;
- additional components: potato starch, talc, magnesium stearate.
1 g of Acyclovir-AKOS ointment contains:
- active substance: acyclovir - 50 mg;
- additional components: 1,2-propylene glycol, lipocomp (lipid component of bird fat) or chicken oil, polyethylene oxide-400, emulsifier No. 1, nipazol, nipagin, purified water.
Pharmacological properties
Pharmacodynamics
Acyclovir is an antiviral (antiherpetic) agent that is a synthetic analogue of a purine nucleoside, which has the ability to suppress in vitro and in vivo replication of Herpes simplex viruses type 1 and 2, Epstein-Barr virus, Varicella zoster virus and cytomegalovirus.
Acyclovir-AKOS demonstrates high activity against Herpes simplex viruses type 1 and 2; the virus that excites herpes zoster and chickenpox - varicella zoster (Varicella Zoster); Epstein-Barr virus [types of viruses are arranged in ascending order of the value of the minimum inhibitory concentration (MIC) of the active substance]. It also has a moderate effect on cytomegalovirus.
In infected cells, including the enzyme thymidine kinase synthesized by viruses, phosphorylation and transformation of acyclovir to acyclovir monophosphate occurs. Subsequently, under the action of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and under the influence of several cellular enzymes into triphosphate. The drug is characterized by a high selectivity of action on viruses and low toxicity in relation to humans, due to the fact that acyclovir does not belong to the substrates for thymidine kinase of uninfected cells, and as a result is low toxic to mammalian cells.
Acyclovir triphosphate blocks viral DNA replication (synthesis) through the following mechanisms:
- Competitively replaces deoxyguanosine triphosphate in the process of DNA synthesis.
- Embedding in the synthesized DNA chain, it terminates it.
- Suppresses the activity of viral DNA polymerase.
As a result of the effect of acyclovir, the virus stops multiplying in the body. The specificity and high selectivity of the drug's action are also due to its predominant accumulation in the cells affected by viruses. Against the background of herpes infection, the drug prevents the appearance of new elements of the rash, reduces the risk of visceral complications and cutaneous dissemination, accelerates the formation of crusts, and reduces pain in the acute stage of herpes zoster. The drug has an immunostimulating effect.
Pharmacokinetics
After oral administration, acyclovir is partially absorbed in the intestine. Due to the low lipophilicity, after ingestion of 200 mg of the drug, absorption averages 20% (from 15 to 30%), but at the same time dose-dependent concentrations are formed, required for effective therapy of viral lesions. Food intake has no significant effect on the absorption of acyclovir. With an increase in the dose, the bioavailability of the drug decreases.
When used orally 5 times a day, 200 mg, the maximum concentration (Cmax) of the agent is 0.0007 mg / ml, the minimum (Cmin) is 0.0004 mg / ml, the time to reach Cmax is 1.5-2 hours. Plasma protein binding is low - 9–33%.
The active substance passes through the blood-brain barrier, also penetrates well into tissues and organs, such as the liver, lungs, kidneys, brain, lacrimal fluid, aqueous humor, intestines, spleen, muscles, mucous membrane and vaginal secretions, uterus, breast milk, semen, the contents of herpetic vesicles. The level of concentration of acyclovir in the cerebrospinal fluid is equal to 50% of that in the blood. Acyclovir-AKOS crosses the placenta, and is excreted in breast milk in small amounts. After prescribing a daily dose of 1000 mg, divided into 5 doses, acyclovir is detected in breast milk at concentrations equivalent to 0.6-4.1% of its plasma concentrations (with mother's milk, the substance can enter the child's body at a dose below 0.3 mg / kg / day).
Metabolic transformation occurs in the liver with the formation of a metabolite of 9-carboxymethoxymethylguanine. The drug is excreted by the kidneys through tubular secretion and glomerular filtration. When taken orally, about 62–91% of the dose is excreted unchanged and about 14% in the form of a metabolite. Less than 2% is excreted through the digestive tract; trace amounts are detected in the exhaled air.
When a single hemodialysis session is carried out for 6 hours, the plasma concentration of acyclovir decreases by approximately 60%; with peritoneal dialysis, there is no significant change in acyclovir clearance. The half-life (T ½) when the drug is taken orally is 3.3 hours in adults and 2.6 hours in children and adolescents from 1 year to 18 years. With age, the rate of excretion decreases, but at the same time T 1/2 of the active substance increases slightly.
In the presence of severe chronic renal failure, T 1/2 does not exceed 20 hours. In adult patients with renal insufficiency, T 1/2 depends on creatinine clearance (CC): with a CC value of 15-50 ml / min, it is 3.5 hours, with 50-80 ml / min - 3 hours, with 80 ml / min - 2.5 hours. In patients with anuria T 1/2 of the drug - 19.5 hours, during a hemodialysis session - 5.7 hours, against the background of constant outpatient peritoneal dialysis - 14-18 hours.
In the case of the combined use of acyclovir and zidovudine in HIV-infected patients, the pharmacokinetic parameters of both drugs remain practically unchanged.
When the ointment is applied to intact skin, there is minimal absorption, on the affected skin - moderate. When applied externally, the active substance is not detected in blood and urine.
Indications for use
Pills
Acyclovir-AKOS is recommended for the treatment and prevention of infections caused by Herpes simplex viruses types 1 and 2, as well as Varicella zoster:
- genital herpes (primary and recurrent);
- herpes simplex of the skin and mucous membranes (primary and recurrent);
- chickenpox (on the first day after the onset of a typical rash);
- herpes zoster (shingles).
Also, the drug is indicated for use in patients with severe immunodeficiency (including in HIV-infected patients in combination with immunosuppressive drugs, during the period after transplantation, against the background of chemotherapy).
Ointment
It is recommended to use Acyclovir-AKOS ointment for the following diseases:
- herpes simplex skin;
- labial herpes;
- genital herpes (simple and recurrent);
- shingles;
- chicken pox.
Contraindications
Absolute:
- age up to 3 years (for tablets);
- hypersensitivity to any of the constituents of the drug.
Relative (use Acyclovir-AKOS with extreme caution):
- renal failure;
- dehydration;
- pregnancy and the period of breastfeeding.
Instructions for use of Acyclovir-AKOS: method and dosage
Pills
Acyclovir-AKOS tablets are taken orally, regardless of food intake, with a glass of water.
Children over 3 years old take an antiviral agent at the same dose as adults.
The recommended dosage regimen of Acyclovir-AKOS, depending on the indications:
- herpes simplex of the skin and mucous membranes, genital herpes (for therapy purposes): adults are prescribed 1 tablet (200 mg) at 4-hour intervals throughout the day and at 8-hour intervals at night 5 times a day, for 5 days - with herpes simplex of the skin and mucous membranes, and 10 days - with genital herpes; if necessary, the course of treatment can be increased; for patients with immunodeficiency, the drug is prescribed in a single dose of 2 tablets (400 mg), the course is 10 days or more; therapy is required to begin when the first symptoms of the disease appear;
- infections caused by Herpes simplex I or II, including in patients with immunodeficiency (in order to prevent relapses): drug treatment should be started when the first elements of the rash appear or already in the prodromal period; appoint 1 tablet 4 times a day at intervals of 6 hours; with a normal immune status, to prevent herpes simplex of the skin and mucous membranes, it is allowed to take 2 tablets twice a day at intervals of 12 hours; with severe immunodeficiency (in case of impaired absorption from the intestine or after bone marrow transplantation), take 2 tablets 5 times a day;
- recurrent genital herpes: with a recurrence rate of less than 6 times a year, an intermittent course of therapy is prescribed - 1 tablet 5 times a day for 5 days; with a recurrence rate of more than 6 times a year, long-term suppressive therapy is performed - 1 tablet 3-5 times a day or 2 tablets 2 times a day, the course - up to 1 year; the duration of preventive treatment is set taking into account the duration of the period in which there is a threat of infection;
- herpes zoster (shingles), for therapy purposes: 4 tablets at 4-hour intervals throughout the day and at 8-hour intervals at night, 5 times a day for 7-10 days: the maximum allowable single dose should not be more 4 tablets (800 mg);
- chickenpox (for therapy purposes): children over 6 years old and adults take 4 tablets 4 times a day; children 3–6 years old - 2 tablets at the same frequency of administration; more precisely, the dose is set at the rate of 20 mg / kg of body weight, but not more than 4 tablets (800 mg) 4 times a day; the course of therapy is 5 days.
Patients taking high oral doses of Acyclovir-AKOS should receive adequate fluid intake.
In case of functional disorders of the kidneys, correction of the dosage regimen and doses is required depending on the type of infection and the value of CC. For the treatment of a disease excited by Herpes simplex, with a CC below 10 ml / min, the recommended daily dose is 2 tablets - 1 tablet 2 times a day at intervals of at least 12 hours. For the treatment of infections caused by Varicella zoster, as well as during maintenance therapy in patients with severe immunodeficiency with CC 10-25 ml / min, the drug is taken in a daily dose of 12 tablets (2400 mg), divided into 3 doses of 4 tablets (800 mg) at intervals of 8 hours. With CC below 10 ml / min, the dose is reduced to 8 tablets (1600 mg) per day - 2 times 4 tablets with an interval of 12 hours.
Ointment
Ointment Acyclovir-AKOS is applied externally, applied to the affected surface with a cotton swab or thoroughly washed hands 5 times a day (after 4 hours). Treatment is carried out until a crust forms on the herpetic vesicles, or their complete healing occurs. The course is 5-10 days.
Side effects
Systemic side effects when using Acyclovir-AKOS:
- nervous system: headache; rarely - confusion, dizziness, drowsiness, hallucinations, convulsions, paresthesia, coma. These neurological disorders are reversible and are usually observed in patients with renal insufficiency, taking the drug in doses higher than recommended;
- hematopoietic system: extremely rarely - leukopenia, anemia, thrombocytopenia;
- digestive system: abdominal pain, nausea, diarrhea, vomiting; rarely - a reversible increase in the activity of liver enzymes and the level of bilirubin;
- urinary system: rarely - an increase in the level of creatinine and urea in the blood; extremely rare - acute renal failure;
- allergic reactions: itching, rash, urticaria, photosensitivity; rarely - angioedema, shortness of breath, anaphylaxis;
- others: lymphadenopathy, fever, peripheral edema, agitation, visual impairment, fatigue, myalgia; rarely - alopecia.
In patients receiving antiretroviral drugs, the addition of Acyclovir-AKOS does not lead to a significant increase in toxic effects.
When the drug is used externally, redness, itching, peeling, burning or tingling at the site of application may occur. In rare cases, due to the use of the ointment, allergic dermatitis may develop.
Overdose
Against the background of oral administration of acyclovir at a dose of 20 g, there was no development of specific symptoms of overdose.
special instructions
In the course of treatment, kidney function should be monitored (to determine the content of creatinine and urea in the blood).
Since Acyclovir-AKOS does not protect against sexual transmission of herpes, during therapy one should refrain from sexual intercourse, even in the absence of clinical manifestations of the disease.
In patients with immunodeficiency against the background of multiple repeated courses or long-term treatment, it is possible to form virus strains resistant to the action of acyclovir.
In view of the possible development of local inflammation, Acyclovir-AKOS ointment should not be applied to the mucous membranes of the eyes, oral cavity, and genitals.
Application during pregnancy and lactation
There have been no strictly controlled and adequate clinical studies of the safety of acyclovir during pregnancy. As a result, during this period, the use of the drug is allowed only if the expected effect of the treatment exceeds the possible risk to the health of the fetus.
Due to the insignificant penetration of the drug into breast milk, women who are breastfeeding, Acyclovir-AKOS is prescribed only for a short course if absolutely necessary. Breastfeeding while using the drug should be continued with extreme caution under the strict supervision of a physician.
Pediatric use
For children under 3 years of age, taking pills is contraindicated. When treating children over 3 years old, it is recommended to follow the dosage regimen for adults.
With impaired renal function
According to the instructions, Acyclovir-AKOS should be used with caution in the presence of renal failure.
Drug interactions
With the combined use of Acyclovir-AKOS with immunostimulants, an increase in the effect is observed.
The combination of the drug with other nephrotoxic drugs may increase the threat of nephrotoxic effects.
When acyclovir is used externally with other medicinal substances / drugs, no interactions have been identified.
Analogs
Analogs of Acyclovir-AKOS are: Acyclovir Sandoz, Virolex, Atsigerpin, Zovirax, Acyclovir Belupo, Vivoraks, Acyclovir-Ferein, Acyclovir, Gervirax, Acyclovir-Akrikhin, Herperaks, Acyclovir forte, Acyclostad, Provirsan.
Terms and conditions of storage
Store in a place protected from moisture and light, out of the reach of children, tablets at temperatures below 25 ° C, ointment - from 8 to 15 ° C.
Shelf life of tablets - 3 years, ointments - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Acyclovir-AKOS
According to most reviews, Acyclovir-AKOS is an effective and affordable drug used for the treatment and prevention of herpes. The drug demonstrates a good result both when taking tablets and when using the ointment, but a particularly pronounced and quick effect, according to many patients, is achieved when they are used in combination.
However, in some reviews, patients also point to a short-term effect of the drug and the need for a long course (mainly for ointments), which can be addictive. The disadvantages of Acyclovir-AKOS include the possible development of side reactions and the need for its use at strictly set hours.
Price for Acyclovir-AKOS in pharmacies
The price for Acyclovir-AKOS can be approximately:
- 200 mg tablets (20 per pack): 25–30 rubles;
- ointment for external use 5% (5 g in a tube): 20–100 rubles.
Acyclovir-AKOS: prices in online pharmacies
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Drug name Price Pharmacy |
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Acyclovir-AKOS 200 mg tablets 20 pcs. RUB 33 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
