Last Updated on January 18, 2019 by Dr.Derek Fhisher

Zovirax Acyclovir 200, 400 mg
Most popular brand: Zovirax
Active ingredient: Acyclovir
Available dosage forms: 200, 400 mg
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Acyclovir (Aciclovir): instruction, and the use of a formula

The nosological classification (ICD – 10)

Code CAS

Feature substance Acyclovir

Acyclovir ; White crystalline powder with a maximum solubility in water (at 37 ° C) 2,5 mg / ml, molecular weight 225.21. Acyclovir sodium salt ; maximum solubility in water (at 25 ° C) higher than 100 mg / ml, molecular weight 247.19; prepared solution (50 mg / ml) has a pH of about 11.


Mode of action -. Antiviral, antiherpethetical

It is a synthetic purine nucleoside analogue. After entering into the infected cells containing the viral thymidine kinase, acyclovir is phosphorylated and converted into acyclovir monophosphate which is influenced by cell guanilatkinazy converted to the diphosphate and then under the action of several cellular enzymes ; a triphosphate. Acyclovir triphosphate interacts with the viral DNA – polymerase chain incorporated into viral DNA. is an open circuit or blocking further replication of viral DNA without damaging the cells of the host.

Acyclovir inhibits the in vitro and in vivo replication of herpesviruses person, including the following (listed in descending order of the antiviral activity of acyclovir in cell culture): virus Herpes simplex 1 and type 2, virus Varicella zoster, Epstein – Barr virus and CMV.

With long-term treatment or re-use of acyclovir in patients with severe immunodeficiency viruses develop resistance Herpes simplex and Varicella zoster to acyclovir. In most clinical isolates derived from acyclovir – resistant patients, found the relative scarcity of viral thymidine kinase, or violation of the structure of the virus thymidine kinase or DNA – polymerase.

When herpes prevents new elements disease, reduces the likelihood of cutaneous dissemination and visceral complications accelerates education crusts, reduces pain in the acute phase of herpes zoster. It has immunostimulatory effects.

If ingestion is partially absorbed from the gastrointestinal tract. bioavailability ; 20% (15 – 30%), regardless of the formulation decreases with increasing dose; Food has no significant effect on the absorption of acyclovir. After oral administration of 200 mg acyclovir every 4 h in adults average equilibrium values ​​of C max ; 0.7 mcg / mL and C min ; 0.4 g / ml; T max ; 1,5 – 2 hours.

After the on / in the drip of adult average C max 1 hour after infusion at a dose of 2.5; 5 and 10 mg / kg was 5.1; 9.8 and 20.7 ug / ml, respectively. C min 7 hours after infusion, respectively, equal to 0.5; 0.7 and 2.3 ug / ml. In children older than 1 year, the values ​​of C max and C min at a dose of 250 and 500 mg / m 2 were similar to those in adults at doses of 5 and 10 mg / kg, respectively . In newborns and infants up to 3 months, which acyclovir was administered at a dose of 10 mg / kg / drip for 1 hour every 8 hours C max was 13.8 pg / ml), C min ; 2.3 ug / ml.

Binding of low protein (9 – 33%). It passes through the BBB. placental barrier found in human milk (at a dose of 1 g / day orally with mother’s milk to the baby receives 0.3 mg / kg). Well into the organs, tissues and fluids of the body, including the brain, kidneys, liver, lungs, aqueous humor, lacrimal fluid, intestine, muscle, spleen, uterus, mucous membranes, and the secret of the vagina, semen, spinal – cerebral fluid contents of herpetic vesicles . The highest concentrations found in the kidney, liver and intestine. The concentration in the spinal cord – cerebrospinal fluid is 50% of that in plasma. It is metabolized in the liver under the influence of alcohol – and aldehyde and, to a lesser extent, aldehyde oxidase into inactive metabolites. Metabolism of acyclovir is not associated with the cytochrome enzymes P450.

The main route of elimination of ; through the kidneys by glomerular filtration and tubular secretion. When administered in unchanged output of about 14%, with a / in the introduction – 45-79%. The main metabolite found in the urine – 9 – karboksimetoksimetilguanin. The share of the main metabolite accounts for up to 14% (with normal renal function). Less than 2% is excreted in the faeces, trace amounts determined in the exhaled air.

T 1/2 at intake in adult ; 2,5 – 3,3 h T 1/2 at / in the introduction: adult ;. 2.9 h in children and adolescents from 1 year to 18 years ; 2.6 hours in children under the age of 3 months ; 3.8 hours (when administered / drip 10 mg / kg for 1 hour three times a day). In patients with chronic renal insufficiency T 1/2 ; 19.5 hours during hemodialysis ; 5.7 hours, with continuous ambulatory peritoneal dialysis ; 14 – 18 hours For a single dialysis session for 6 hours acyclovir concentration is reduced by 60% in the plasma, in peritoneal dialysis clearance acyclovir not change significantly.


When applied to the affected skin (eg with herpes zoster) moderate absorption; in patients with normal renal function, serum concentrations of up to 0.28 g / ml, with impaired renal function ; to 0.78 g / ml. Report the news (about 9% of the daily dose).

Eye ointment easily penetrates through the epithelium of the cornea and creates a therapeutic concentration in the aqueous humor.

carcinogenicity, mutagenicity, effects on fertility, teratogenicity

in rats and mice fed for acyclovir life at doses up to 450 mg / kg / day by gavage (the value C max were above observed in humans 3 – 6 times in mice and 1 – 2 times the rat), carcinogenicity is not revealed.

Acyclovir showed mutagenic effects in some tests: 16 in vivo and in vitro tests for genetic toxicity of acyclovir results of 5 tests were positive.

Acyclovir no effect on reproduction and fertility in mice when administered orally at doses of 450 mg / kg / day in rats and s / to a dose of 50 mg / kg / day. wherein the plasma levels were 9 – 18 times higher (mice) or 8 – 15 times higher (in rats) than in humans. At the highest dose (50 mg / kg / day p / c) in rats and rabbits (plasma levels were 11 – 22 or 16 – 31 such a person) is set to decline implantation efficiency.

Teratogenicity. Acyclovir had no teratogenic effects when administered during the period of organogenesis in mice (450 mg / kg / day. Inside), rabbits (50 mg / kg / day. P / and / in ) as well as in a standard test in rats (50 mg / kg / day. n / k).

carcinogenicity studies with topical acyclovir is not carried out.

In humans, disruption of spermatogenesis, sperm motility or morphology have been reported. However, high doses of acyclovir ; 80 or 320 mg / kg / day intraperitoneally in rats, as well as 100 or 200 mg / kg / day / in dogs ; It causes atrophy of the testes and aspermatogenez. Testicular disorders were observed at / in the introduction of acyclovir dogs at doses of 50 mg / kg / day for 1 month or 60 mg / kg / day orally for 1 year.

Application of the substance Acyclovir

for systemic use: primary and recurrent infections of the skin and mucous membranes caused by the herpes simplex virus (type 1 and 2), including genital herpes, herpes lesions in immunocompromised patients (treatment and prevention); herpes zoster, chickenpox.

For external use: herpes simplex skin and mucous membranes, genital herpes (primary and recurrent); localized zoster (adjuvant treatment).

For topical use in ophthalmology: herpetic keratitis.


Hypersensitivity to acyclovir or valacyclovir.

Restrictions on the use

The on / in the introduction: dehydration, renal failure (risk of nephrotoxicity), neurological disorders, or neurological reactions to receiving cytotoxic drugs. including history.

If ingestion: dehydration, kidney failure.

Application of pregnancy and breastfeeding

Pregnancy. Perhaps if the expected effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety in pregnant women has not carried out). Acyclovir passes through the placenta. Data on the outcome of pregnancy in women who received systemic effects of acyclovir in the I trimester of pregnancy, showed no increase in the number of birth defects in children compared with the general population. As the observation was included a small number of women, credible and specific about the safety of acyclovir conclusions can not be done during pregnancy.

Breastfeeding. Acyclovir passes into breast milk. After receiving acyclovir by mouth, it was determined in breast milk in concentrations, the ratio of which to the blood plasma concentration of 0,6 – 1,4. At such concentrations in the breast milk of children who are breastfed may receive acyclovir at a dose of 0.3 mg / kg / day. With this in mind, should be prescribed acyclovir lactating women with caution, only when necessary.

Side effects of substance Acyclovir

In the systemic application:

From the digestive tract: at / in the introduction ; anorexia, nausea and / or vomiting; when administered ; nausea and / or vomiting, diarrhea, abdominal pain.

From the nervous system: at / in the introduction ; dizziness, symptoms of encephalopathy (confusion, hallucinations, convulsions, tremors, coma), delirium, depression or psychosis (neurological disorders are commonly observed in patients with predisposing conditions); when administered ; malaise, headache, dizziness, agitation, drowsiness.

From the cardio – vascular system and blood: at / in the introduction ; anemia, neutropenia / neutrophilia, thrombocytopenia / thrombocytosis, leukocytosis, hematuria, DIC – syndrome, hemolysis, blood pressure reduction.

With the genitourinary system: at / in the introduction ; transient increase in blood urea nitrogen and creatinine levels in serum (associated with the value of C max in the plasma and the state of the water the patient’s balance), acute renal failure (often with fast I / injection).

Other: anaphylactic reactions, allergic skin reactions (itching, rash, Lyell’s syndrome, urticaria, erythema multiforme, and others.), Blurred vision, fever, leukopenia, lymphadenopathy, peripheral edema, transient increase in hepatic transaminase and bilirubin levels; at / in the introduction ; reaction at the site / in the introduction: phlebitis or local inflammation (pain, swelling or redness), necrosis (in contact with the drug under the skin); when administered ; myalgia, paresthesia, alopecia.

When the external application: soreness, burning, itching, skin rash, vulva.

In the application of eye ointment: a burning sensation at the site of application, blepharitis, conjunctivitis, superficial punctate keratopathy.


Other nephrotoxic drugs increase the risk of nephrotoxicity. In an application with probenecid (block tubular secretion) increased T 1/2 and AUC acyclovir reduced renal clearance and excretion slows down, may increase the toxic effect.


Symptoms: headache, neurological disorders, shortness of breath, nausea, vomiting, diarrhea, kidney failure, lethargy, convulsions, coma.

Treatment: symptomatic therapy, maintaining vital functions, adequate hydration, hemodialysis (especially in acute renal failure and anuria).

There is no data on overdose with topical application.

Dosing and Administration

B / drip in, inside, locally. Dosage is determined individually, depending on the evidence and the degree of severity of the process. The dosage for children is calculated according to the indication, the age, surface area / weight. Treatment should begin as soon as possible, at the first signs and symptoms of the disease.

B / drip (introduced at a constant speed of at least 1 hour): the herpes infection, severe herpetic lesions genitals and shingles adult ; 5 mg / kg three times a day (every 8 hours) 5 days; patients with immune system disorders, in herpetic encephalitis ; 10 mg / kg every 8 hours for 10 days. The maximum dose for adults with a / in the introduction of ; 30 mg / kg or 1.5 g / m 2 / day.

Inside: adult ; 0.2 g of 5 once a day (except night) for 5 – 10 days. When chicken pox and shingles ; 0.8 g of 5 times a day for 7 days.

If the system applying in the elderly may require an adjustment of dose or the interval between doses, in patients with impaired renal excretory function, reduce the dose based on creatinine clearance.

Outer: cream or ointment applied to the affected area 5 times a day for 5 – 10 days.

Eye ointment: for adults and children a strip of ointment 10 mm lay in the lower conjunctival sac five times a day (every 4 hours) for 7 – 10 days (treatment should be continued for at least 3 days full treatment).

Precautions substance Acyclovir

In the treatment with acyclovir is recommended that drinking large amounts of fluids (to prevent the formation of sludge acyclovir in renal tubules).

It is necessary to be careful when on / in patients with neurological disorders, impaired liver function, electrolyte imbalance, severe hypoxia, as well as with impaired renal function (and in the appointment of the inside). To reduce the risk of kidney damage with a / in the introduction of the drug should be administered slowly over 1 hour. If you have symptoms of nephropathy drug overturned.

The toxic effect of acyclovir on the central nervous system are more likely in patients with impaired immunity in older patients with high doses.

When acyclovir therapy in clinical practice were recorded thrombocytopenic purpura and / or hemolytic uremic syndrome, in rare cases with fatal outcome, in patients with symptomatic forms of HIV – infection.

It is not recommended for use in children for the treatment of varicella, if the disease is mild.

In the treatment of genital herpes should avoid sex or use condoms because application of acyclovir does not prevent transmission of the virus to the partner.

The cream and ointment for external use (5%) should not be applied on the mucous membranes of the mouth and eyes, as may develop pronounced local inflammation.

In the treatment of eye ointment should not wear contact lenses.

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