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Active ingredients
- Acyclovir
Disease class
- Immunodeficiency, unspecified
- Anogenital herpetic viral infection
- Other and unspecified infectious diseases
- Cytomegalovirus disease
- Disease caused by HIV with manifestations of other viral infections
- Herpes simplex virus infections
- Herpetic gingivostomatitis and pharyngotonsillitis
- Herpetic eye disease
- Chicken pox [varicella]
- Shingles
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Antiviral
Pharmacological group
- Antiviral (except HIV) drugs
Oral tablets Acyclovir-AKOS (Aciclovir-AKOS)
Instructions for medical use of the drug
Description of pharmacological action
Penetrates into virus-infected cells, competitively interacts with viral thymidine kinase and is sequentially phosphorylated to form mono-, di- and triphosphate. Acyclovir triphosphate is integrated into the viral DNA chain, competitively inhibits the viral DNA polymerase and suppresses its replication.
Indications for use
For systemic use: - treatment of infections of the skin and mucous membranes caused by Herpes simplex viruses type I and II (primary and secondary, including genital herpes); - prevention of exacerbations of recurrent infections caused by Herpes simplex viruses type I and II in patients with normal immune status; - prevention of primary and recurrent infections caused by Herpes simplex viruses type I and II in patients with immunodeficiency; — as part of complex therapy for patients with severe immunodeficiency: with HIV infection (stage of AIDS, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation; - treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, herpes zoster). For external use: skin herpes simplex, genital herpes (simple and recurrent), labial herpes; herpes zoster and chicken pox.
Release form
tablets 200 mg; dark glass jar (jar) 20, cardboard pack 1; tablets 200 mg; contour packaging 10, cardboard pack 3; tablets 200 mg; contour packaging 10, cardboard pack 1; tablets 200 mg; contour packaging 10, cardboard pack 2;
Pharmacodynamics
It has high specificity for herpes simplex virus types I and II, the virus that causes chickenpox and herpes zoster (Varicella zoster), Epstein-Barr virus and cytomegalovirus.
Pharmacokinetics
When taken orally, bioavailability is 15–30%, Cmax is achieved after 1.5–2 hours. The concentration after oral administration of 200 mg 5 times a day is 0.7 mcg/ml. Plasma protein binding is 9–33% and is independent of the concentration of acyclovir in plasma. Penetrates well into all organs and tissues, including the brain and skin. The concentration in the cerebrospinal fluid is 50% of the concentration in plasma. Passes through the placental barrier and accumulates in breast milk. Metabolized in the liver to form a pharmacologically inactive derivative - 9-carboxymethoxymethylguanine. T1/2 in adults with normal renal function is 2-3 hours, in severe renal failure - 20 hours, in patients with hemodialysis - 5.7 hours (at the same time, the concentration of acyclovir in plasma decreases to 60% of the initial value). It is excreted by the kidneys (84% unchanged, 14% as a metabolite), less than 2% through the intestines. Renal clearance accounts for 75–80% of the total clearance.
Use during pregnancy
Possibly if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be stopped during treatment.
Contraindications for use
Hypersensitivity, incl. to acyclovir or components of the drug, breastfeeding; with caution - dehydration, renal failure, neurological disorders, incl. in the anamnesis.
Side effects
From the nervous system and sensory organs: rarely - headache, weakness; in some cases - tremor, dizziness, increased fatigue, drowsiness, hallucinations. From the gastrointestinal tract: in isolated cases - abdominal pain, nausea, vomiting, diarrhea. Allergic reactions: skin rash. Other: transient increase in liver enzyme activity; rarely - increased levels of urea and creatinine, hyperbilirubinemia, leukopenia, erythropenia, alopecia, fever.
Directions for use and doses
Orally, during or immediately after a meal, with plenty of water. In the treatment of infections of the skin and mucous membranes caused by Herpes simplex I or II, adults and children over 2 years of age - 200 mg 5 times a day for 5 days at 4 hour intervals during the day and at 8 hour intervals at night (if necessary the course can be extended). As part of complex therapy for severe immunodeficiency (including with a full-blown clinical picture of HIV infection, including early clinical manifestations of HIV infection and AIDS), after bone marrow transplantation - 400 mg 5 times a day. To prevent relapses of infections caused by Herpes simplex I or II, in patients with normal immune status and in case of relapse of the disease - 200 mg 4 times a day every 6 hours (maximum dose - up to 400 mg 5 times a day, depending on the severity of the infection). When treating infections caused by Varicella zoster, adults and children weighing more than 40 kg - 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. Duration of treatment is 7–10 days. Children over 2 years old - 20 mg/kg 4 times a day for 5 days. When treating infections caused by Herpes zoster, adults - 800 mg 4 times a day every 6 hours during the day for 5 days. If renal function is impaired during the treatment and prevention of infections caused by Herpes simplex, in patients with creatinine Cl less than 10 ml/min, the dose of the drug is reduced to 200 mg 2 times a day with a 12-hour interval. In the treatment and prevention of infections caused by Varicella zoster, in patients with creatinine Cl less than 10 ml/min, the dose of the drug is reduced to 800 mg 2 times a day with 12 hour intervals, with creatinine Cl up to 25 ml/min - 800 mg 3 times a day. day with 8 hour intervals.
Interactions with other drugs
When taken orally: probenecid increases the average T1/2 and reduces the clearance of acyclovir; nephrotoxic drugs increase the risk of renal dysfunction.
Precautions for use
Prescribe with caution to patients with impaired renal function and elderly patients (due to an increase in T1/2). When using the drug, it is recommended to take a sufficient amount of fluid. During treatment, it is necessary to monitor kidney function (urea and creatinine levels in the blood). The ointment is not recommended to be applied to the mucous membranes of the mouth, eyes, and genitals (local inflammation may develop).
Special instructions for use
Use internally strictly as prescribed by a doctor in adults and children over 2 years of age (to avoid complications). It is recommended to start treatment when the first signs of the disease appear (the effectiveness will be higher). In patients with immunodeficiency, with multiple repeated courses, viral resistance to acyclovir may develop.
Storage conditions
In a dry place, protected from light, at a temperature of 8–15 °C.
Best before date
36 months
ATX classification:
J Antimicrobials for systemic use
J05 Antiviral drugs for systemic use
J05A Direct acting antivirals
J05AB Nucleosides and nucleotides
J05AB01 Aciclovir
INSTRUCTIONS
on medical use of the drug
acyclovir
(aciclovir)
Compound:
active substance:
aciclovir;
1 tablet contains acyclovir 200 mg (0.2 g);
Excipients:
lactose monohydrate, corn starch, magnesium stearate, croscarmellose sodium
.
Dosage form.
Pills.
Basic physical and chemical properties:
tablets are white or almost white.
Pharmacotherapeutic group.
Antiviral agents for systemic use. Direct acting antiviral agents. Acyclovir. ATX code J05A B01.
Pharmacological properties.
Pharmacodynamics.
Acyclovir is a synthetic purine nucleoside analogue with inhibitory activity in vivo
and
in vitro
against human herpes virus, including herpes simplex virus types I and II, varicella zoster virus, Epstein-Barr virus and cytomegalovirus. In cell culture, acyclovir has the greatest activity against herpes simplex virus type I and then, as activity decreases, against herpes simplex virus type II, varicella zoster virus and herpes zoster, Epstein-Barr virus and cytomegalovirus.
The inhibitory activity of acyclovir against the above viruses is highly selective. The enzyme thymidine kinase in a normal uninfected cell does not use acyclovir as a substrate, so the toxic effect on host cells is minimal. However, thymidine kinase, encoded in herpes simplex virus, varicella zoster virus, herpes zoster virus, and Epstein-Barr virus, converts acyclovir to acyclovir monophosphate, a nucleoside analogue, which is then converted sequentially to diphosphate and triphosphate by cellular enzymes. Following the incorporation of acyclovir into the viral DNA, the triphosphate interacts with the viral DNA polymerase, resulting in the cessation of the synthesis of the viral DNA chain.
With long-term or repeated courses of treatment of severely ill patients with reduced immunity, there may be cases of reduced sensitivity of certain strains of the virus, which do not always respond to treatment with acyclovir. Most clinical cases of insensibility are due to viral thymidine kinase deficiency, but there are reports of viral thymidine kinase and DNA damage. In vitro
the interaction of individual herpes simplex viruses with acyclovir may also lead to the formation of less sensitive strains.
in vitro
susceptibility of individual herpes simplex viruses and the clinical results of treatment with acyclovir is not fully understood.
Pharmacokinetics.
Acyclovir is only partially absorbed in the intestine. The average peak steady-state concentration (Cssmax) in blood plasma after taking a dose of 200 mg at a 4-hour interval is 3.1 µmol (0.7 µg/ml), and accordingly the level in plasma (Cssmin) will be 1.8 µmol (0 .4 µg/ml). The corresponding Cssmax levels after doses of 400 mg and 800 mg at 4-hour intervals were 5.3 µmol (1.2 µg/ml) and 8 µmol (1.8 µg/ml) and the equivalent Cssmin levels were 2.7 µmol (0 .6 µg/ml) and 4 µmol (0.9 µg/ml).
In adults, the terminal half-life of intravenous acyclovir is approximately 2.9 hours. Most of the drug is excreted unchanged by the kidneys. The renal clearance of acyclovir is significantly higher than the clearance of creatinine, which indicates that the drug is eliminated by the kidneys by not only glomerular filtration, but also tubular secretion.
9-carboxymethoxymethylguanine is the only important metabolite of acyclovir and accounts for approximately 10-15% of the administered dose, which can be determined in the urine. If acyclovir is administered 1 hour after 1 g of probenecid, the terminal half-life and area under the concentration/time curve increase by 18% and 40%, respectively.
In patients with chronic renal failure, the mean terminal half-life is 19.5 hours. The average half-life of acyclovir during hemodialysis is 5.7 hours. Plasma acyclovir levels decrease by approximately 60% during dialysis.
The concentration of the drug in the cerebrospinal fluid is approximately 50% of the corresponding concentration in the blood plasma. The level of binding to plasma proteins is relatively low (from 9% to 33%), and it does not change when interacting with other drugs.
With the simultaneous use of acyclovir and zidovudine for the treatment of HIV-infected patients, no changes in the pharmacokinetics of these drugs were detected.
Clinical characteristics.
Indications.
- Treatment of viral infections of the skin and mucous membranes caused by the herpes simplex virus, including primary and recurrent genital herpes;
- suppression (prevention of relapses) of infections caused by the herpes simplex virus in patients with normal immunity;
- prevention of infections caused by the herpes simplex virus in patients with immunodeficiency;
- treatment of infections caused by the Varicella zoster
(chicken pox and herpes zoster).
Contraindications.
Hypersensitivity to acyclovir, valacyclovir or other components of the drug.
Interaction with other drugs and other types of interactions.
No clinically important interactions of acyclovir with other drugs were found.
Acyclovir is excreted predominantly unchanged by the kidneys by tubular secretion, therefore any drugs that have a similar mechanism of excretion may increase the concentration of acyclovir in the blood plasma. Probenecid and cimetidine prolong the half-life of acyclovir and the area under the concentration/time curve. When used simultaneously with immunosuppressants in the treatment of patients after organ transplantation, the level of acyclovir and the inactive metabolite of the immunosuppressive drug in the blood plasma also increases, but due to the wide therapeutic index of acyclovir, there is no need to adjust the dose.
Features of application.
Acyclovir is eliminated from the body mainly by renal clearance, so the dose should be reduced in patients with renal failure (see "Dosage and Administration"). Elderly patients are also more likely to have impaired renal function, so a dose reduction may also be required for this group of patients. Both of these groups (patients with renal failure and elderly patients) are at risk for neurological side effects and should therefore be closely monitored for these side effects. According to the data obtained, such reactions are generally reversible when treatment with the drug is stopped.
Particular attention should be paid to maintaining an adequate level of hydration in patients receiving high doses of acyclovir.
The drug contains lactose, so it should not be used in patients with hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Use during pregnancy or breastfeeding.
There was no increase in the number of birth defects in children whose mothers used acyclovir during pregnancy compared to the general population. However, acyclovir tablets should be used when the potential benefit of the drug for the mother outweighs the possible risk to the fetus.
When taken orally 200 mg of acyclovir 5 times a day, acyclovir passes into breast milk in concentrations of 0.6-4.1% of the corresponding level of acyclovir in blood plasma. Potentially, an infant can absorb acyclovir at a dose of up to 0.3 mg/kg body weight per day. Therefore, acyclovir should be prescribed to breastfeeding women with caution, taking into account the benefit/risk ratio.
The ability to influence the reaction rate when driving vehicles or other mechanisms.
When deciding whether to drive a car or operate machinery, the clinical status of the patient and the side effect profile of the drug should be taken into account.
There have been no clinical studies of the effect of acyclovir on the reaction rate when driving vehicles or operating other mechanisms. In addition, the pharmacology of acyclovir does not give reason to expect any negative effects.
Method of administration and dose.
The tablet should be taken whole with water. When using high doses of acyclovir, an adequate level of hydration should be maintained.
Adults
Treatment of infections caused by the herpes simplex virus.
To treat infections caused by the herpes simplex virus, it is necessary to take acyclovir tablets at a dose of 200 mg 5 times a day at approximately 4-hour intervals, with the exception of the night period.
Treatment should last 5 days, but may be extended in case of severe primary infection.
For some patients with immunodeficiency (for example, after bone marrow transplantation) or for patients with reduced intestinal absorption, the dose can be doubled to 400 mg or the appropriate dose can be used intravenously.
Treatment should begin as soon as possible after the onset of infection. In the case of recurrent herpes, it is better to start treatment in the prodromal period or after the first signs of skin lesions appear.
Prevention of relapses (suppressive therapy) of infections caused by the herpes simplex virus.
In patients with normal immunity, to prevent relapses of infections caused by the herpes simplex virus, take acyclovir tablets at a dose of 200 mg 4 times a day with a 6-hour interval.
For convenience, most patients can take 400 mg of acyclovir twice daily at 12-hour intervals.
Treatment will be effective even after reducing the dose of tableted acyclovir to 200 mg, which is taken 3 times a day with an 8-hour interval or even 2 times a day with a 12-hour interval.
In some patients, radical improvement is observed after taking a daily dose of acyclovir 800 mg.
To monitor for possible changes in the natural history of the disease, acyclovir therapy should be interrupted periodically at intervals of 6-12 months.
Prevention of infections caused by the herpes simplex virus.
To prevent infections caused by the herpes simplex virus, in patients with immunodeficiency, acyclovir tablets at a dose of 200 mg should be taken 4 times a day with a 6-hour interval. In patients with significant immunodeficiency (for example, after bone marrow transplantation) or in patients with reduced intestinal absorption, the dose can be doubled to 400 mg or the appropriate dose can be used intravenously.
The duration of prophylactic use is determined by the length of the risk period.
Treatment of chickenpox and herpes zoster.
To treat infections caused by chickenpox and herpes zoster viruses, you should take acyclovir tablets at a dose of 800 mg 5 times a day at 4-hour intervals, with the exception of the night period. Treatment should continue for 7 days.
In patients with severe immunodeficiency (for example, after bone marrow transplantation) or in patients with reduced absorption in the intestine, it is better to use intravenous administration.
Treatment should begin as soon as possible after the onset of the disease; the result will be better if treatment is started immediately after the appearance of the rash.
Children.
For the treatment and prevention of infections caused by the herpes simplex virus, in children over 2 years of age with immunodeficiency, the same doses can be used as for adults.
For the treatment of chickenpox, children from 6 years of age should be prescribed 800 mg of acyclovir 4 times a day; children from 2 to 6 years of age can be given 400 mg of acyclovir 4 times a day. The duration of treatment is 5 days.
More accurately, the dose of the drug can be calculated based on the child’s body weight - 20 mg/kg body weight per day (not to exceed 800 mg) of acyclovir, divided into 4 doses.
There are no specific data on the use of acyclovir for the prevention (prevention of relapses) of infections caused by the herpes simplex virus, or for the treatment of infections caused by the herpes zoster virus in children with normal immunity.
This dosage form of the drug should not be used in children under 2 years of age.
Elderly patients.
The possibility of renal dysfunction in elderly patients should be borne in mind and the dose of the drug for them should be adjusted accordingly (see Renal failure
). It is necessary to maintain an adequate level of body hydration.
Kidney failure.
Acyclovir should be administered with caution to patients with renal failure. It is necessary to maintain an adequate level of body hydration.
In the prevention and treatment of infections caused by the herpes simplex virus in patients with renal failure, recommended oral doses do not lead to the accumulation of acyclovir, the level of which would exceed the safe level established for intravenous administration. However, in patients with severe renal failure (creatinine clearance less than 10 ml/min), it is recommended to set a dose of 200 mg 2 times a day with an interval of approximately 12 hours.
For the treatment of infections caused by the Varicella zoster
(chickenpox and herpes zoster), in patients with significantly reduced immunity, it is recommended for severe renal failure (creatinine clearance less than 10 ml/min) to set a dose of 800 mg 2 times a day at approximately 12-hour intervals, and for patients with moderate renal failure ( creatinine clearance within 10-25 ml/min) – 800 mg 3 times a day with an interval of approximately 8 hours.
Children.
Acyclovir tablets are used for children from 2 years of age.
Overdose.
Symptoms.
Acyclovir is only partially absorbed from the gastrointestinal tract. There have been cases of patients accidentally taking up to 20 g of acyclovir internally without causing toxic effects. In case of accidental repeated overdose of oral acyclovir, gastroenterological (such as nausea and vomiting) and neurological symptoms (headache and confusion) occur over several days.
In case of an overdose of intravenous acyclovir, the level of serum creatinine and blood urea nitrogen increases and, accordingly, renal failure appears.
Neurological manifestations of overdose may include confusion, hallucinations, agitation, seizures and coma.
Treatment:
the patient should be carefully examined to identify symptoms of intoxication. Gastric lavage and symptomatic treatment are recommended. Due to the fact that the level of acyclovir in the blood is well eliminated by hemodialysis, it should be used in case of overdose.
Adverse reactions.
The side effects listed below are classified as follows.
From the blood and lymphatic system.
Anemia, thrombocytopenia, leukopenia.
From the immune system.
Anaphylaxis.
Mental disorders and disorders of the nervous system.
Headache, dizziness, agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.
The above neurological reactions are generally reversible and usually occur when used to treat patients with renal failure or other risk factors.
From the respiratory system and chest organs.
Dyspnea.
From the gastroenterological system.
Nausea, vomiting, diarrhea, abdominal pain.
From the hepatobiliary system.
Reversible increase in bilirubin and liver enzymes, jaundice, hepatitis.
From the skin and subcutaneous tissues.
Itching, rash (including photosensitivity), urticaria, increased diffuse hair loss. Since hair loss can be associated with a large number of diseases and medications used by the patient, no clear association with acyclovir was found. Angioedema.
From the kidneys and urinary system.
Increased blood urea and creatinine levels, acute renal failure, kidney pain.
Kidney pain may be associated with renal failure and crystalluria.
General violations.
Increased fatigue, fever.
Best before date.
3 years.
Storage conditions.
Store in original packaging at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Package.
10 tablets in a blister; 1 or 2 blisters per pack.
Vacation category.
On prescription.
Manufacturer.
Private joint-stock company "Lekhim-Kharkov".
The location of the manufacturer and its address of place of business.
Ukraine, 61115, Kharkov region, Kharkov city, Severin Pototsky street, building 36.
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Acyclovir-AKOS, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.
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