Acyclovir Avexima - Instructions For Use Of Tablets 200 And 400 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Acyclovir Avexima

Acyclovir Avexima: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Aciclovir Avexima

ATX code: J05AB01

Active ingredient: acyclovir (Aciclovir)

Producer: JSC "Irbitskiy Khimfarmzavod" (Russia)

Description and photo update: 2020-11-06

Prices in pharmacies: from 57 rubles.

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Acyclovir Avexima is an antiviral agent.

Release form and composition

Dosage form - tablets: flat-cylindrical; dosage 200 mg - white, scored and chamfered; dosage of 400 mg - round, white or almost white, with a double-sided chamfer and a line on one side (in packs of cell contour of polyvinyl chloride film and aluminum foil, 10 pcs., in a cardboard box together with instructions for medical use of the drug 2 packs; in cans from low-pressure polyethylene, 20 pcs., in a cardboard box 1 can and instructions for the use of Acyclovir Avexim).

Composition of 1 tablet 200 mg:

• active ingredient: acyclovir (in terms of anhydrous substance) - 200 mg;
• additional substances: milk sugar (lactose monohydrate) - 119.4 mg; sugar (sucrose) - 13.2 mg; magnesium stearate - 3.4 mg; potato starch - 66.2 mg; Povidone K17 (low molecular weight medical polyvinylpyrrolidone) - 5.6 mg; sodium lauryl sulfate - 1.6 mg; stearic acid - 0.6 mg.

Composition of 1 tablet 400 mg:

• active ingredient: acyclovir (in terms of anhydrous substance) - 400 mg;
• additional substances: MCC (microcrystalline cellulose) - 43.12 mg; sodium carboxymethyl starch - 25 mg; povidone K25 - 7.88 mg; magnesium stearate - 4 mg.

Pharmacological properties

Pharmacodynamics

Acyclovir is a synthetic analogue of a purine nucleoside with the ability to inhibit in vivo and in vitro human herpes viruses, including chickenpox and herpes zoster (herpes zoster), cytomegalovirus, herpes simplex virus types I and II, and Epstein-Barr virus. In cell culture, acyclovir exhibits the most pronounced antiviral activity against herpes simplex virus type I, then, in decreasing order of activity, follow: herpes simplex virus type II, chickenpox and herpes zoster virus (herpes zoster), Epstein-Barr virus and cytomegalovirus.

The depressing effect of acyclovir on the herpes viruses listed above is quite selective. Since acyclovir is not a substrate for the thymidine kinase enzyme of uninfected cells, it is of low toxicity to mammalian cells. Thymidine kinase of cells infected with herpes simplex viruses, varicella zoster and herpes zoster (lichen) virus, Epstein-Barr virus and cytomegalovirus converts acyclovir into a nucleoside analogue, acyclovir monophosphate, which is subsequently sequentially converted into di- and triphosphate under the influence of cellular enzymes. The insertion of acyclovir triphosphate into the viral DNA chain (deoxyribonucleic acid) and the subsequent termination of the chain lead to blocking further viral DNA replication.

Repeated or prolonged courses of treatment with acyclovir in patients with severe immunodeficiency can contribute to the emergence of resistant strains, and therefore further therapy with the drug may be ineffective. Most of the isolated strains with reduced sensitivity to acyclovir were characterized by a relatively low content of viral thymidine kinase, as well as a violation of the structure of viral thymidine kinase or DNA polymerase. The in vitro effect of acyclovir on herpes simplex virus strains can cause the formation of strains that are less sensitive to it. No correlation has been established between the clinical efficacy of the drug and the sensitivity of herpes simplex virus strains to acyclovir in vitro.

Pharmacokinetics

Pharmacokinetic parameters of acyclovir:

• absorption: acyclovir is only partially absorbed from the intestine. After taking at a dose of 200 mg every 4 hours, C _ssmax (average maximum equilibrium concentration) in plasma was 0.7 μg / ml (3.1 μM), and C _ssmin (average equilibrium minimum concentration) in plasma was 0.4 μg / ml (1.8 μM). When taking Acyclovir Avexim 400 and 800 mg every 4 hours, C _ssmax was 1.2 μg / ml (5.3 μM) and 1.8 μg / ml (8 μM), and C _ssmin was 0.6 μg / ml (2, 7 μM) and 0.9 μg / ml (4 μM), respectively;
• distribution: in cerebrospinal fluid, acyclovir is found at a concentration of ~ 50% of this indicator in blood plasma. The connection with blood plasma proteins is insignificant (from 9 to 33%), therefore, the occurrence of drug interactions is unlikely due to the displacement of binding with blood plasma proteins from the sites;
• metabolism: the main metabolite of acyclovir is 9-carboxymethoxy-methylguanine, found in urine in an amount of ~ 10-15% of the dose taken;
• excretion: in adult patients, after taking acyclovir inside T _1/2 (half-life) from blood plasma is ~ 3 hours. To a greater extent, the drug is excreted unchanged in the urine. The renal clearance of acyclovir is significantly higher than the creatinine clearance, which indicates the excretion of the substance using both glomerular filtration and tubular secretion. Taking the drug 60 minutes after taking 1000 mg of probenecid leads to an increase in the AUC (area under the concentration-time pharmacokinetic curve) of acyclovir by 40%, and its T _1/2 - by 18%.

Pharmacokinetic parameters of acyclovir in special groups of patients:

• impaired renal function: in patients with chronic renal insufficiency, T _{1/2 of} acyclovir averaged 19.5 hours. The hemodialysis procedure reduced the mean T _1/2 to 5.7 hours. During dialysis, the concentration of acyclovir in blood plasma decreased by approximately 60 %;
• old age: with age, in parallel with a decrease in creatinine clearance in elderly patients, the clearance of acyclovir also decreases, while the T _{1/2 of} acyclovir does not change significantly;
• presence of HIV infection: when acyclovir was administered to HIV-infected patients simultaneously with zidovudine, the pharmacokinetic characteristics of both drugs remained practically unchanged.

Indications for use

• treatment of infections of the skin and mucous membranes caused by the herpes simplex virus, including primary and recurrent genital herpes;
• treatment of chickenpox and herpes zoster (acyclovir, used at an early stage of the disease, has an analgesic effect and helps to reduce the incidence of postherpetic neuralgia);
• prevention of herpes simplex virus infections in immunocompromised patients;
• prevention of recurrence of infections caused by the herpes simplex virus in patients with normal immune status.

Contraindications

Absolute:

• glucose-galactose malabsorption, fructose, lactose intolerance, lactase deficiency, isomaltase / sucrase;
• children under 3 years of age (for this dosage form);
• hypersensitivity to the active substance of the drug, acyclovir, or valacyclovir, or one or more additional components in the composition of the drug.

Relative (Acyclovir Avexima tablets must be used with precautions):

• renal failure;
• dehydration;
• combination therapy with other nephrotoxic drugs;
• pregnancy;
• lactation (breastfeeding period);
• elderly age.

Acyclovir Avexima, instructions for use: method and dosage

Acyclovir Avexim tablets can be taken with meals (food intake does not significantly affect the absorption of acyclovir) with a full glass of water.

Recommended dosing regimen for adult patients:

• treatment of infections caused by the herpes simplex virus: the dose of Acyclovir Avexim 200 mg 5 times / day (every 4 hours, with the exception of the period of night sleep), the course of therapy is 5 days, but in case of severe primary infections it can be extended. Severe immunodeficiency (for example, after bone marrow transplantation) or impaired absorption from the intestine is the reason for increasing the dose of the drug to 400 mg. An alternative method is the use of acyclovir in the form of a lyophilisate for the preparation of a solution for infusion. Therapy should be started as early as possible after signs of infection appear; in case of relapses, Acyclovir Avexima is recommended to be prescribed already in the prodromal period (the period of the disease located between the incubation period and the disease itself) or when the first elements of the rash appear;
• treatment of chickenpox and herpes zoster (lichen): 800 mg 5 times / day (every 4 hours, with the exception of the period of night sleep), the course of therapy is 7 days. Treatment of herpes zoster (herpes zoster) should be started as soon as possible from the onset of the first signs of the disease, since in this case the effectiveness of therapy increases. Treatment of chickenpox in patients with normal immune status is recommended to begin within the first 24 hours after the onset of the rash. For patients with severe immunodeficiency (for example, after bone marrow transplantation) or with impaired absorption from the intestine, it is possible to prescribe acyclovir in the form of a lyophilisate for preparing a solution for infusion;
• prevention of infections caused by the herpes simplex virus in patients with immunodeficiency: 200 mg 4 times / day (every 6 hours). Severe immunodeficiency (for example, after bone marrow transplantation) or impaired absorption from the intestine is the reason for increasing the dose of Acyclovir Avexim to 400 mg. An alternative method is the use of acyclovir in the form of a lyophilisate for the preparation of a solution for infusion. The duration of the preventive course of therapy depends on the length of the period during which the risk of infection is increased;
• prevention of recurrence of infections caused by the herpes simplex virus in patients with normal immune status: 200 mg 4 times / day (every 6 hours). A more convenient treatment regimen is suitable for most patients - 400 mg 2 times / day (every 12 hours). In some cases, lower doses of Acyclovir Avexim are effective - 200 mg 3 times / day (every 8 hours) or 200 mg 2 times / day (every 12 hours). In some patients, when taking a total daily dose of 800 mg, an exacerbation of the infection is possible. Therapy with Acyclovir Avexim must be interrupted periodically for a period from six months to a year in order to detect possible changes in the course of the disease.

The recommended dosage regimen of Acyclovir Avexim for children:

• treatment of infections caused by the herpes simplex virus: at the age of 3 years and older - doses similar to those for adult patients;
• treatment of chickenpox: at the age of 3 to 6 years - 400 mg 4 times / day; at the age of 6 years and older - 800 mg 4 times / day. More precisely, the dose is determined at the rate of 20 mg / kg of body weight (but not more than 800 mg) 4 times / day. The course of therapy is 5 days. Treatment for herpes zoster - no dosage data available;
• prevention of infections caused by the herpes simplex virus in immunocompromised patients: at the age of 3 years and older - doses similar to those for adult patients;
• prevention of recurrence of herpes simplex virus infections in patients with normal immune status: no data on dosing regimen.

Recommendations for the use of Acyclovir Avexim in special groups of patients:

• patients with impaired renal function: the appointment of acyclovir to patients in this category requires caution. They should ensure that the water balance is maintained at an adequate level. In patients with impaired renal function, who are using acyclovir orally in recommended doses for the treatment and prevention of herpes simplex virus infections, the accumulation of the drug to exceed the established safe levels of concentrations was not observed. Nevertheless, patients with creatinine clearance (CC) less than 10 ml / min should reduce the dose of Acyclovir Avexim to 200 mg 2 times / day (every 12 hours). In the treatment of chickenpox and herpes zoster (lichen), the following doses of acyclovir are recommended: with CC less than 10 ml / min - 800 mg 2 times / day (every 12 hours); with CC 10-25 ml / min - 800 mg 3 times / day (every 8 hours);
• elderly patients: the likelihood of renal failure in patients of this age category should be taken into account. When confirming the diagnosis, it is necessary to adjust the dose in accordance with the degree of renal failure. It is important to ensure that adequate hydration is maintained during therapy.

Side effects

The categories of frequency of adverse reactions below are estimates. For most adverse events, the information required to determine the frequency of occurrence is not available. In addition, this characteristic may vary depending on the indications for which the drug is used.

Adverse events that occur during therapy with Acyclovir Avexim [are given in accordance with the following frequency of occurrence: very often (> 1/10); often (> 1/100 and 1/1000 and 1/10 000 and <1/1000); extremely rare (<1/10 000); frequency is unknown (it is impossible to determine the incidence of adverse reactions based on the available data)]:

• nervous system and mental status: often - dizziness, headache; extremely rare - tremor, psychotic symptoms, agitation, dysarthria, drowsiness, confusion, hallucinations, ataxia, encephalopathy, convulsions, coma (as a rule, these adverse reactions were observed in patients with impaired renal function or the presence of other provoking factors and were reversible);
• blood and lymphatic system: extremely rare - thrombocytopenia, leukopenia, anemia;
• immune system: rarely - anaphylaxis;
• respiratory system, organs of the chest and mediastinum: rarely - shortness of breath;
• digestive system: often - abdominal pain, diarrhea, nausea, vomiting;
• skin and subcutaneous tissues: often - rash, including photosensitivity, itching; infrequently - rapid diffuse hair loss (it can be observed in various diseases, as well as during therapy with many drugs; it was not possible to establish a connection between this undesirable phenomenon and the use of acyclovir), urticaria; rarely - angioedema; extremely rarely - exudative erythema multiforme (MEE), toxic epidermal necrolysis (Lyell's syndrome);
• liver and biliary tract: rarely - a reversible increase in the concentration of liver enzymes and bilirubin in the blood; extremely rare - jaundice, hepatitis;
• kidneys and urinary tract: rarely - an increase in the concentration of creatinine and urea in the blood serum; extremely rarely - renal colic (may be associated with crystalluria and renal failure), acute renal failure;
• general disorders: often - fever, fatigue.

Overdose

Since acyclovir is only partially absorbed in the intestine, no toxic effects were observed with an accidental single dose of the drug in a dose of up to 20,000 mg. With repeated ingestions for several days at doses exceeding the recommended ones, disturbances in the digestive (nausea, vomiting) and nervous (confusion, headache) systems were noted. In rare cases, neurological effects have been observed (seizures, coma).

If an overdose is suspected, symptomatic treatment is prescribed. Patients require careful medical monitoring to identify possible symptoms of intoxication. Acyclovir is removed from the body by hemodialysis, so this method can be used in the treatment of overdose.

special instructions

As a result of clinical studies, sufficient data were not obtained to conclude that the use of acyclovir helps to reduce the risk of chickenpox disease in immunocompetent (without clinical and laboratory signs of AIDS of any etiology) patients.

With the combined use of Acyclovir Avexim with other nephrotoxic drugs, the risk of developing renal failure increases.

Repeated or prolonged courses of treatment with acyclovir in patients with severe immunodeficiency can contribute to the emergence of resistant (with reduced sensitivity to acyclovir) strains, and therefore further therapy with the drug may be ineffective.

Patients who are prescribed high doses of acyclovir by mouth should be provided with sufficient fluid intake.

Since acyclovir is excreted by the kidneys, it is necessary to adjust the dose of the drug in patients with impaired renal function.

Elderly patients, who may experience impaired renal function with age, need to adjust the dose of Acyclovir Avexim.

Both patients with impaired renal function and elderly patients are at an increased risk of developing side effects from the central nervous system (most of these reactions are reversible and disappear after discontinuation of the drug), and therefore they should be closely monitored …

All patients, especially those with signs of clinical manifestations, must be careful to avoid potential transmission of the virus. In addition, it is important to inform all patients about cases of asymptomatic virus carriage.

Influence on the ability to drive vehicles and complex mechanisms

There have been no adequate studies on the effect of Acyclovir Avexim on a person's ability to drive vehicles and complex mechanisms. Based on the pharmacological properties of the active substance, it is impossible to predict any negative effects of acyclovir on these activities, however, the profile of side effects arising from its use should be taken into account. So, for example, it must be borne in mind that dizziness may occur when taking acyclovir, and therefore persons employed in potentially hazardous industries or driving a car should be careful.

Application during pregnancy and lactation

The post-registration register of pregnancies with acyclovir therapy contains information on pregnancy outcomes in women who took acyclovir in different dosage forms. An analysis of the registry data showed no increase in the number of birth defects in newborns whose mothers took acyclovir during gestation, in comparison with the general population. The birth defects that were identified did not differ in regularity or uniformity, which does not allow us to assume the presence of a common cause of their occurrence. Nevertheless, it is necessary to observe precautions when prescribing acyclovir to pregnant women and preliminary assess the degree of predominance of the intended benefits to the mother over the possible risks to the fetus.

After taking acyclovir orally at a dose of 200 mg 5 times / day, its content in a woman's breast milk ranged from 60 to 410% of the concentration of the substance in plasma. With this amount of substances in milk, breastfed babies can receive acyclovir at a dose of 0.3 mg / kg / day. It is important to take this information into account and, when prescribing Acyclovir Avexim to nursing women, draw their attention to the observance of precautions during therapy with acyclovir.

There are no data on the effect of acyclovir on female fertility. During the study, which involved 20 male patients with normal sperm count, it was proved that acyclovir taken orally in a daily dose of up to 1000 mg for 6 months has no clinically significant effect on morphology, motility and sperm count.

Pediatric use

Acyclovir Avexim tablets are contraindicated in the treatment of pediatric patients under 3 years of age.

With impaired renal function

Renal failure is a relative contraindication for therapy with Acyclovir Avexim. Patients with this pathology should take the drug with caution.

It is important to ensure that adequate hydration is maintained during therapy.

Correction of doses to patients of this category is performed taking into account the level of CC.

For violations of liver function

For patients with impaired liver function, there are no special recommendations for the dosage regimen of Acyclovir Avexim.

Use in the elderly

Elderly patients should be careful when taking Acyclovir Avexim.

When prescribing the drug to patients of this age category, the likelihood of their having renal failure should be taken into account. When confirming the diagnosis, it is necessary to adjust the dose in accordance with the degree of renal failure. It is important to ensure that adequate hydration is maintained during therapy.

Drug interactions

There were no clinically significant interactions with acyclovir.

Acyclovir is excreted from the body unchanged in the urine through active tubular secretion. All drugs that have a similar route of elimination are able to increase its concentration in plasma.

Cimetidine and probenecid decrease the renal clearance of acyclovir and increase its AUC.

An increase in AUC in blood plasma was also noted with the combined use of acyclovir and an inactive metabolite of mycophenolate mofetil (used in transplantation of an immunosuppressant). However, due to the wide therapeutic index of acyclovir, dose adjustment is not required in this case.

Theophylline AUC increases on average by 50% when taken simultaneously with acyclovir. For this reason, it is necessary to measure plasma theophylline concentrations when the two drugs are taken together.

Analogs

The analogs of Acyclovir Avexim are Atsigerpine, Acyclovir, Acyclovir Forte, Acyclovir Belupo, Acyclostad, Acyclovir Velpharm, Acyclovir Ferein, Acyclovir-SZ, Vivorax, Virolex, Herperax, Acyclovir-AKOS, Acyclovir-AKOS, Gervirax, Acyclovir Acyclovir Reneval, Acyclovir Sandoz, Zovirax, etc.

Terms and conditions of storage

Keep out of the reach of children. Store in a dry place, away from sunlight, at temperatures up to 25 ° C.

Shelf life is 2 years.

It is prohibited to use the drug after the expiration date.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Acyclovir Avexim

On the Internet, you can find mostly positive reviews about Acyclovir Avexim. Among the advantages of the drug are its effectiveness, quick action and affordable cost. Also, patients note the good tolerance of the drug and the fact that taking the tablets enhances the effect of using a similar ointment. Most consider Acyclovir Avexima to be the best herpes treatment that has no competitors in this price category.

Some users do not like the frequency of use of the tablets, they consider frequent use the only drawback of the drug.

Price for Acyclovir Avexima in pharmacies

The price for Acyclovir Avexima 200 mg is 56–68 rubles, for Acyclovir Avexima 400 mg - 101–125 rubles. per pack of 20 tablets.

Acyclovir Avexima: prices in online pharmacies

Drug name Price Pharmacy

Acyclovir Avexima 200 mg tablets 20 pcs. RUB 57 Buy

Acyclovir Avexima tab. 400mg 20 pcs. 106 RUB Buy

Acyclovir Avexima 400 mg tablets 20 pcs. 106 RUB Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!