Acyclovir
Acyclovir: 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. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Aciclovir
ATX code: J05AB01
Active ingredient: aciclovir (aciclovir)
Manufacturer: AZT PHARMA KB (Russia); Ozon, LLC (Russia); Belmedpreparaty RUE (Belarus); Tatkhimpharmpreparaty, JSC (Russia); Sintez, JSC (Russia); Vertex, JSC (Russia); Anhui Jianzhong Gobo Pharmaceutical Co. (China) and others.
Description and photo update: 2019-19-08
Prices in pharmacies: from 13 rubles.
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Acyclovir is an antiviral drug used to treat herpes.
Release form and composition
Dosage forms:
- cream for external use 5% (in aluminum tubes of 2 g, 5 g, 10 g);
- ointment for external use 5% (in aluminum tubes of 2 g, 3 g, 5 g, 10 g; in glass jars of 5 g, 10 g, 20 g);
- eye ointment 3% (in aluminum tubes of 5 g);
- lyophilisate for preparation of solution for infusion (in vials of 250 mg and 500 mg);
- tablets of 200 mg and 400 mg (in blisters of 10 pcs.).
The active substance is acyclovir:
- 1 g cream - 50 mg;
- 1 g of ointment - 50 mg;
- 1 g of eye ointment - 30 mg;
- 1 bottle of lyophilisate - 250 mg, 500 mg or 1000 mg;
- 1 tablet - 200 mg.
Pharmacological properties
Pharmacodynamics
Acyclovir is an antiviral agent for oral, parenteral, local and external use, a synthetic analogue of an acyclic purine nucleoside.
Acyclovir has a high specificity for Herpes simplex viruses (HSV), including type 1 and type 2, cytomegalovirus (CMV), Epstein-Barr virus (EBV), and Varicella zoster virus (VZV). The manifestation of the greatest activity of the substance is observed in relation to HSV-1, then in decreasing order - HSV-2, VZV, EBV and CMV.
The mechanism of action is based on the penetration of the drug directly into the virus-infected cells that produce viral thymidine kinase, as a result of which acyclovir is phosphorylated to acyclovir monophosphate.
The activity of viral thymidine kinase in relation to acyclovir is much higher than the effect of cellular enzymes on it (the concentration of acyclovir monophosphate in infected cells is 40-100 times higher). Further, acyclovir triphosphate is formed, which is a selective and extremely active inhibitor of viral DNA polymerase.
Most likely, the mechanism of inhibition of DNA synthesis (deoxyribonucleic acid) by acyclovir triphosphate is that it is a substrate for this enzyme, which allows the 3'– 5 'bond required to extend the DNA chain. As a result, premature termination of the DNA strand occurs.
Pharmacokinetics
Pills
After oral administration, acyclovir is only partially absorbed in the intestine. After application 5 times a day, 200 mg C max (maximum concentration) and C min (minimum concentration) of the substance in blood plasma is 0.7 and 0.4 μg / ml, respectively.
In cerebrospinal fluid, the concentration of acyclovir is 50% of the plasma concentration. The substance has a relatively low binding to plasma proteins (9–33%). It is excreted from the body, mainly through the kidneys, unchanged. Renal clearance significantly exceeds creatinine clearance, which indicates that the substance is excreted not only by glomerular filtration, but also by tubular secretion.
The only metabolite found in the urine is 9-carboxymethoxymethylguanine (10-15% of the dose).
Ointment (cream) for external use
When used externally on intact skin, acyclovir has minimal absorption. Not detected in blood / urine.
In case of application on the affected skin, the substance is absorbed moderately. In the absence of impaired renal function, the serum concentration is up to 0.28 μg / ml, in patients with chronic renal failure, this figure rises to 0.78 μg / ml. Excretion is carried out by the kidneys (up to 9.4% of the daily dose).
Eye ointment
Through the epithelium of the cornea, acyclovir easily penetrates, creating a therapeutic concentration in the intraocular fluid. There are no methods for determining a substance in the blood when using the drug in the form of an eye ointment.
Infusion solution
C ssmax (maximum equilibrium concentration) of acyclovir after infusion for 60 minutes at a dose of 2.5; five; 10 and 15 mg / kg are 5.1; 9.8; 20.7 and 23.6 μg / ml, respectively. C ssmin (minimum equilibrium concentration) of acyclovir in plasma 7 hours after infusion at the indicated doses is 0.5; 0.7; 2.3 and 2.0 μg / ml, respectively.
For children from one comparable C ssmah and C ssmin observed at a dose of 250 mg / m 2 equivalent to 5 mg / kg (adult dose) and 500 mg / m 2 equivalent to 10 mg / kg (adult dose).
In children from 0 to 3 months, who received acyclovir as infusions at a dose of 10 mg / kg for more than 60 minutes every 8 hours, C ssmax and C ssmin were 13.8 and 2.3 μg / ml, respectively.
In cerebrospinal fluid, the concentration of acyclovir is approximately 50% of its plasma concentration.
The connection with blood plasma proteins is insignificant - from 9 to 33%, as a result of this, the development of drug interactions as a result of displacement from the binding sites with plasma proteins is unlikely.
After intravenous administration of acyclovir in adults, T 1/2 (half-life) from plasma is approximately 2.9 hours. Most of the substance is excreted unchanged by the kidneys. The renal clearance of acyclovir is significantly higher than that of creatinine. This indicates the elimination of the substance not only by glomerular filtration, but also by tubular secretion.
The main metabolite of acyclovir is 9-carboxymethoxymethylguanine, in urine it accounts for approximately 10-15% of the administered dose. When acyclovir is prescribed 1 hour after taking probenecid at a dose of 1000 mg, T 1/2 of acyclovir and AUC (area under the concentration-time curve) increase by 18 and 40%, respectively.
The clearance of acyclovir in elderly patients decreases in parallel with a decrease in creatinine clearance, while T 1/2 changes insignificantly.
In chronic renal failure, T 1/2 of acyclovir averages 19.5 hours, during hemodialysis this figure is 5.7 hours, and the plasma concentration of acyclovir decreases by about 60%.
Indications for use
According to the instructions, parenteral and oral acyclovir is prescribed for the treatment of the following diseases:
- primary and recurrent genital herpes, which is severe;
- herpes zoster caused by the Varicella zoster virus;
- recurrent and primary herpes simplex with damage to the mucous membranes and skin, caused by the Herpes simplex virus types 1 and 2, in patients with impaired immunity;
- herpes zoster, accompanied by eye damage.
Inside, the use of Acyclovir is indicated for the prevention of often recurrent genital herpes, as well as herpes simplex and herpes zoster caused by the Varicella zoster virus, with impaired immunity.
Parenterally, the drug is prescribed for the treatment of encephalitis caused by the Herpes simplex virus of types 1 and 2, as well as generalized infection in newborns caused by the Herpes simplex virus.
In the treatment of chickenpox within 24 hours after the onset of a typical rash with intact immunity, Acyclovir is taken orally, in case of immunity disorders - parenterally.
Contraindications
The use of all dosage forms of Acyclovir is contraindicated in the presence of hypersensitivity to its constituent components.
Absolute contraindications for tablets:
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption (for a dosage form that includes lactose monohydrate as an auxiliary component);
- age up to 3 years;
- lactation period.
Relative contraindications for tablets (Acyclovir is prescribed under medical supervision):
- neurological disorders / reactions to taking cytotoxic drugs (including a burdened history);
- impaired renal function;
- the use of large doses of acyclovir, especially against the background of dehydration;
- elderly age;
- pregnancy.
Relative contraindications for an ointment (cream) for external use (Acyclovir is prescribed under medical supervision):
- pregnancy;
- lactation period.
An absolute contraindication for the use of eye ointment is breastfeeding. Under medical supervision, Acyclovir eye ointment is prescribed during pregnancy.
An absolute contraindication for the use of an infusion solution is breastfeeding.
Relative contraindications for infusion solution (Acyclovir is prescribed under medical supervision):
- dehydration;
- renal failure;
- neurological disorders;
- electrolyte disturbances;
- severe hypoxia;
- reactions to taking cytotoxic drugs (including a burdened history);
- combined therapy with drugs that impair renal function, in particular with cyclosporine, tacrolimus (control of renal function is required);
- combination therapy with mycophenolate mofetil (an immunosuppressive drug used in organ transplantation);
- pregnancy.
Instructions for the use of Acyclovir: method and dosage
In the treatment of primary infections and relapses of Herpes simplex of the skin and mucous membranes, adult patients are usually prescribed 1 tablet (200 mg) 5 times a day. The duration of the drug intake is 5 days. Longer treatment may be required in severe cases. With a significant weakening of immunity, it is possible to increase the dosage by 2 times or intravenous administration of the drug.
To suppress the development of relapses, Herpes simplex with a normal immune system is usually prescribed 1 tablet (200 mg) 4 times a day, or 2 tablets 2 times a day. With reduced immunity, an increase in dosage may be required.
Topically and externally, Acyclovir cream or ointment is applied with a cotton swab or with clean hands to the affected areas and adjacent skin areas with a thin layer. Frequency rate of application - 5 times a day at regular intervals. Treatment is continued until crusts form on the vesicles or until complete healing. The average duration of therapy is 5-10 days.
Eye ointment Acyclovir for adults and children should be placed in the lower conjunctival sac in the form of a strip 1 cm long. The procedure is carried out 5 times a day (every 4 hours) until complete healing. After healing, therapy is continued for another 3 days.
Intravenous drip for children over 12 years old and for adults is usually prescribed at 5-10 mg / kg with an interval between injections of 8 hours. For children aged 3 months to 12 years, the dosage is calculated based on body surface area - 250-500 mg / m 2, for newborns - 10 mg / kg.
Side effects
- skin allergic reactions;
- anaphylactic reactions;
- increased activity of hepatic transaminases;
- confusion of consciousness;
- hallucinations;
- fever;
- lymphadenopathy;
- headache;
- leukopenia;
- visual impairment;
- peripheral edema.
With parenteral administration of Acyclovir, there may be: acute renal failure, phlebitis or inflammation at the injection site, signs of encephalopathy, hematological disorders, hematuria, hemolysis, disseminated intravascular coagulation syndrome, decreased blood pressure, mental disorders, depression or psychosis, impaired gastrointestinal function.
Taking pills can lead to the development of malaise, paresthesia, dysfunction of the gastrointestinal tract (in the form of nausea, vomiting, diarrhea, abdominal pain), alopecia, agitation, myalgia, dizziness, drowsiness.
Overdose
Pills
There is information about the ingestion of 20 mg of acyclovir.
The main symptoms of an overdose: agitation, convulsions, coma, lethargy. If the concentration of acyclovir exceeds the solubility in the renal tubules (2.5 mg / ml), it may precipitate in the renal tubules.
Therapy: symptomatic.
Infusion solution
In case of an overdose, an increase in the concentration of serum creatinine, blood urea nitrogen and the development of renal failure occurs. Neurological symptoms include agitation, hallucinations, confusion, seizures, and coma.
Therapy: hemodialysis.
Ointment (cream) for external use, eye ointment
Acyclovir overdose is possible if accidentally swallowed.
The main symptoms: impaired renal function, neurological disorders, headache, shortness of breath, diarrhea, vomiting, nausea, convulsions, lethargy, coma.
Therapy: activities aimed at maintaining vital functions, hemodialysis.
special instructions
Prolonged use of Acyclovir or repeated courses in patients with reduced immunity can lead to the emergence of viral strains that are not sensitive to the action of the drug.
When taking the drug orally in high doses, you need to monitor the intake of a sufficient amount of fluid into the body.
The use of the drug does not prevent the transmission of herpes through sexual contact, therefore, during therapy, even in the absence of clinical manifestations, one should refrain from sexual intercourse.
Influence on the ability to drive vehicles and complex mechanisms
During the period of oral administration of Acyclovir in the form of tablets, patients should be careful when driving vehicles.
The infusion solution is intended exclusively for use in a hospital setting, therefore, there is no data on the effect of therapy on the ability to drive vehicles.
Application during pregnancy and lactation
- pregnancy: therapy can be carried out under medical supervision after assessing the ratio of the expected benefit with the possible risk;
- lactation period: tablets, eye ointment, infusion solution - the drug is contraindicated; external ointment / cream - therapy can be carried out under medical supervision after assessing the ratio of the expected benefit with the possible risk.
Pediatric use
Acyclovir in the form of tablets is not prescribed for patients under 3 years of age.
With impaired renal function
The drug in dosage forms for systemic use (tablets and infusion solution) is prescribed with caution in case of impaired renal function (renal failure).
Use in the elderly
Acyclovir tablets are prescribed for elderly patients with caution.
Drug interactions
With the simultaneous administration of probenecid, the average T 1/2 increases and the clearance of acyclovir decreases.
Co-administration with nephrotoxic drugs increases the risk of developing renal dysfunction, with immunostimulants - enhances the effect of acyclovir.
When mixing solutions, one should take into account the alkaline reaction of acyclovir for intravenous administration (pH 11).
Analogs
Acyclovir analogs are:
- by active substance: Herperax, Vivorax, Zovirax, Medovir, Provirsan, Acyclostad, Virolex;
- by the mechanism of action: Valcyte, Ribavirin, Trivorin, Arviron, Virazol, Rebetol, Valtrex, Valacyclovir, Tsimeven, Vacirex, Valogard, Valvir, Vairova, Famvir, Ribavin, Ribapeg, Minaker.
Terms and conditions of storage
- cream for external use - 2 years at temperatures up to 25 ° C;
- ointment for external use - 2 years at temperatures up to 8-15 ° C;
- eye ointment - 3 years at a temperature of 15–25 ° C;
- tablets, lyophilisate for preparation of solution for injection - 3 years at temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Acyclovir
Most of the reviews about Acyclovir are positive. The drug is considered effective, inexpensive and readily available.
The rapidity of development of the therapeutic effect of the ointment (cream) for external use is assessed in different ways. Some say that improvement comes quickly, while others point out that symptom relief is not immediate. It is also noted that the use of the drug can lead to the development of side effects (edema, dermatoses). In addition, there are negative reviews regarding the consistency and bitter taste of the ointment.
Acyclovir tablets are usually used in cases where it was not possible to stop the manifestations of herpes by external means. Users note that the best results are achieved when using the drug with the appearance of the first symptoms of the disease.
The main advantages of an eye ointment are considered to be its effectiveness, acceptable cost and convenient packaging. The disadvantages include the small volume of the tube.
The price of Acyclovir in pharmacies
The approximate price for Acyclovir is: tablets (20 pieces of 200 or 400 mg each) - 19-21 or 164-226 rubles; 5% ointment for external use (1 tube of 5 or 10 g) - 15 or 22 rubles; 3% eye ointment (1 tube 5 g each) - 86-123 rubles; lyophilisate for the preparation of a solution for infusion (1 bottle of 250 mg) - 193 rubles.
Acyclovir: prices in online pharmacies
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Drug name Price Pharmacy |
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Acyclovir 5% ointment for external use 5 g 1 pc. RUB 13 Buy |
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Acyclovir 5% ointment for external use 10 g 1 pc. RUB 18 Buy |
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Acyclovir 5% ointment for external use 5 g 1 pc. RUB 18 Buy |
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Acyclovir 5% ointment for external use 10 g 1 pc. RUB 19 Buy |
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Acyclovir 5% ointment for local and external use 5 g 1 pc. RUB 19 Buy |
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Acyclovir ointment 5% 10g n1 RUB 25 Buy |
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Acyclovir 5% cream for local and external use 5 g 1 pc. RUB 27 Buy |
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Acyclovir cream 5% 5g 28 RUB Buy |
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Acyclovir 5% ointment for external use 10 g 1 pc. 28 RUB Buy |
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Acyclovir 5% cream for external use 5 g 1 pc. RUB 33 Buy |
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Acyclovir 200 mg tablets 20 pcs. 34 rbl. Buy |
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Acyclovir 5% ointment for local and external use 10 g 1 pc. 34 rbl. Buy |
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Acyclovir 200 mg tablets 20 pcs. 35 RUB Buy |
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Acyclovir ointment for external use. approx. 5% tube 10g RUB 36 Buy |
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Acyclovir 5% cream for local and external use 10 g 1 pc. RUB 42 Buy |
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Acyclovir cream for places. and plank beds. approx. 5% tube 10g 43 rbl. Buy |
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Acyclovir Belupo 5% cream for external use 5 g 1 pc. RUB 46 Buy |
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Acyclovir 5% ointment for external use 10 g 1 pc. RUB 47 Buy |
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Acyclovir 5% cream for external use 2 g 1 pc. RUB 47 Buy |
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Acyclovir Belupo cream 5% 5g RUB 48 Buy |
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Acyclovir Avexima 200 mg tablets 20 pcs. RUB 57 Buy |
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Acyclovir Belupo 5% cream for external use 10 g 1 pc. RUB 60 Buy |
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Acyclovir Belupo cream 5% 10g RUB 65 Buy |
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Acyclovir tablets 200mg 20 pcs. Irbitsky KhFZ RUB 69 Buy |
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Acyclovir cream for outside. approx. 5% tube 2g RUB 70 Buy |
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Acyclovir Sandoz (cream) 5% cream for external use 2 g 1 pc. RUB 70 Buy |
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Acyclovir Sandoz cream 5% 2g RUB 75 Buy |
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Acyclovir (eye ointment) 3% eye ointment 5 g 1 pc. RUB 98 Buy |
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Acyclovir Avexima tab. 400mg 20 pcs. 106 RUB Buy |
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Acyclovir Avexima 400 mg tablets 20 pcs. 106 RUB Buy |
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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!
