Active substance: acyclovir;
1 tablet contains 200 mg of acyclovir;
Excipients : microcrystalline cellulose, colloidal anhydrous silica, sodium starch (type A) kopovidon, magnesium stearate.
Basic physical and chemical properties: white, round, biconvex tablets with a print of «VS 1".
Antiviral medications for regular use.
ATC Code J05A B01.
Acyclovir is a synthetic purine nucleoside analogue with inhibitory activity in vivo and in vitro respect human herpes virus, including herpes simplex virus type I and II virus and varicella zoster virus, Epstein-Barr virus and cytomegalovirus. In cell culture aciclovir are most active against herpes simplex virus type I and further, for decreasing activity against herpes simplex virus type II virus and varicella zoster virus, Epstein-Barr virus and cytomegalovirus.
Inhibitory activity of acyclovir against the aforementioned viruses are highly selective. The enzyme thymidine kinase in normal uninfected cells does not use acyclovir as a substrate because toxic effects on the cells of the host organism is minimal. However thymidine kinase encoded by herpes simplex virus, varicella-zoster virus, herpes zoster and Epstein-Barr virus, converts acyclovir to acyclovir monophosphate - nucleoside analogue, which is then converted successively to diphosphate and triphosphate cells by enzymes. Following embedding of acyclovir triphosphate viral DNA interacts with the viral DNA polymerase, resulting in the termination of the synthesis of viral DNA chain.
Prolonged or repeated courses of treatment of severe patients with lowered immunity may decrease the sensitivity of some strains that do not always respond to treatment acyclovir. It was found that most cases of insensitivity associated with viral thymidine kinase deficiency, but there are reports of damage to viral thymidine kinase and DNA. In vitro interaction of certain viruses of herpes simplex acyclovir may also lead to the formation of less sensitive strains. The interdependence between the individual sensitivity of herpes simplex virus in vitro and clinical results of treatment acyclovir is not fully understood.
Acyclovir is only partially absorbed in the intestine. The average peak stable concentration (C ssmax ) in plasma after taking a dose of 200 mg of 4-hourly intervals of 3.1 mmol (0.7 mg / ml) and accordingly level in plasma (C ssmin ) is 1.8 mmol ( 0.4 mg / ml). Suitable C ssmax level after doses of 400 mg and 800 mg of 4-hourly intervals up 5.3 mmol (1.2 mg / ml) and 8 mmol (1.8 mg / mL) and the equivalent C ssmin levels were 2.7 mmol (0.6 mg / ml) and 4 mmol (0.9 mg / ml).
In adults terminal half-life at vnurishnovennomu administration of acyclovir is about 2.9 hours. Most of the drug is excreted unchanged by the kidneys. Renal clearance of acyclovir significantly higher than the creatinine clearance, indicating that the drug excretion by the kidneys is done by not only glomerular filtration and tubular secretion and.
9 karboksymetoksymetylhuanin is the only significant metabolite of acyclovir, which can be measured in urine, and approximately 10-15% of the applied dose. If acyclovir applied 1 hour after administration of 1 g probenecid, the final half-life and area under the curve "concentration / time" increased by 18% and 40% respectively.
In patients with chronic renal failure the average level of the final half-life of 19.5 hours. Average half-life of acyclovir during hemodialysis is 5.7 hours. The level of acyclovir in plasma during dialysis is reduced by about 60%.
The concentration of the drug in the cerebrospinal fluid is approximately 50% of corresponding plasma concentrations. The level of protein binding is relatively low (9 to 33%), and the interaction with other drugs it does not change.
Concomitant administration of acyclovir and zidovudine to treat HIV-infected patients, there were no changes in the pharmacokinetics of these drugs.
Treatment of viral infections of the skin and mucous membranes caused by the herpes simplex virus, including initial and recurrent genital herpes.
Suppression (prevention of recurrences) infections caused by the herpes simplex virus in patients with normal immune systems.
Prevention of infections caused by the herpes simplex virus in patients with immunodeficiency.
Treating infections caused by virus Varicella zoster (chickenpox and herpes zoster).
Hypersensitivity to acyclovir, valaciclovir or to any other drug.
Interaction with other medicinal products and other forms of interaction
Clinically important interaction acyclovir with other drugs was found.
Acyclovir is excreted largely unchanged through the kidney tubular secretion, so any drugs with a similar mechanism of withdrawal may increase the concentration of acyclovir in plasma. Probenecid and cimetidine acyclovir prolong the half-life and area under the curve "concentration / time." Concomitant administration of Immunosuppressants in patients after organ transplantation also increased plasma levels of acyclovir and the inactive metabolite, immunosuppressive drugs, but because of the wide therapeutic index of acyclovir correct dose is required.
The application features
Acyclovir is excreted mainly by renal clearance, therefore patients with renal insufficiency, the dose should be reduced (see. "Dosage and Administration"). In elderly patients and a high probability of renal dysfunction, so this group of patients may also be necessary to reduce the dose. Both groups (patients with renal impairment and elderly patients) are groups of risk of neurological side effects and should therefore be carefully monitored to detect them. Such reactions are generally reversible upon termination of drug treatment (see. Section "Adverse Reactions").
It is necessary to pay special attention to maintain adequate hydration of patients receiving high doses of acyclovir.
Pregnancy and lactation
There was no increase in the number of birth defects in children whose mothers used acyclovir during pregnancy, compared with the general population. However, acyclovir tablets should apply only if the potential benefits of the drug to the mother outweighs the possible risk to the fetus.
If oral acyclovir 200 mg 5 times daily acyclovir gets into breast milk in concentrations that are 0,6-4,1% acyclovir appropriate level in blood plasma. Potentially child that fed this milk can learn acyclovir at a dose of 0.3 mg / kg body weight per day. Because acyclovir administered to women who are breastfeeding, you should carefully considering risk / benefit ratio.
Effects on ability to drive a car or other mechanisms
In deciding on the possibility of driving or operating machinery should take into account the patient's clinical status and profile of side effects of the drug. The influence of acyclovir on the reaction rate when driving or operating other mechanisms not performed. In addition, pharmacology acyclovir no reason to expect any negative impact.
Dosage and Administration
The tablet should be taken whole with water. When using high doses of acyclovir should maintain an adequate level of hydration.
Treating infections caused by herpes simplex virus
For the treatment of infections caused by the herpes simplex virus, you need to take tablets acyclovir 200 mg 5 times per day with approximately 4-hourly intervals, except for the night period.
Treatment should last 5 days, but if severe primary infection it can be extended.
For patients with severe immunodeficiency (eg, bone marrow transplant) or in patients with decreased gut absorption the dose may be doubled to 400 mg or apply the appropriate dose for intravenous administration.
Treatment should begin as soon as possible after the onset of infection. In the case of recurrent herpes is best to start treatment at prodrome or when the first signs of skin lesions.
Prevention of relapse (suppressive therapy) infections caused by the herpes simplex virus
In patients with normal immune systems to prevent recurrence of infections caused by the herpes simplex virus, tablets 200 mg take 4 times daily with 6-hour intervals.
For convenience, most patients can take acyclovir 400 mg 2 times a day with 12-hour intervals.
The treatment will be effective even after dose reduction to 200 mg of acyclovir, which should be taken 3 times a day with 8-hour intervals or even 2 times a day with 12-hour intervals.
In some patients there is a radical improvement after taking daily doses of acyclovir 800 mg.
To monitor possible changes in the natural course of the disease acyclovir therapy must be periodically interrupted at intervals of 6-12 months.
Prevention of infections caused by the herpes simplex virus
For the prevention of infections caused by the herpes simplex virus, patients with immunodeficiency tablets 200 mg should be taken four times daily with 6-hour intervals. For patients with significant immunodeficiency (eg, bone marrow transplant) or in patients with decreased gut absorption the dose may be doubled to 400 mg or apply the appropriate dose for intravenous administration.
Duration of prophylaxis depends on the duration of the period of risk.
Treatment of varicella and herpes zoster
For the treatment of infections caused by viruses and varicella zoster virus, you need to take tablets 800 mg 5 times a day with 4-hour intervals, except for the night period. Treatment should last 7 days.
Patients with severe immunodeficiency (eg, bone marrow transplant) or patients with low absorption in the intestine is better to use intravenous.
Treatment should begin as soon as possible after the onset, the result will be better if treatment is started immediately after the onset of rash.
For the treatment and prevention of infections caused by the herpes simplex virus in immunocompromised children aged 2 years can apply the dose as adults.
For treatment of varicella in children aged 6 years prescribe acyclovir 800 mg 4 times a day, children 2 to 6 years of age may receive 400 mg of acyclovir 4 times daily. Treatment duration is 5 days.
More precisely dose can be calculated by weighing the child: 20 mg / kg body weight per day (not to exceed 800 mg) of acyclovir for 4 doses.
Children under 2 years of this dosage form of the drug should not be used.
Keep in mind the possibility of renal impairment in elderly patients, and dose for them to change accordingly (see. Renal insufficiency ). It is necessary to maintain adequate levels of hydration.
Acyclovir should be used with caution in patients with renal insufficiency. It is necessary to maintain adequate levels of hydration.
In the prevention and treatment of infections caused by the herpes simplex virus to patients with renal impairment is recommended oral dose not lead to accumulation of acyclovir, the level which would exceed the safe level established for vnurishnovennoho input. However, for patients with severe renal impairment (creatinine clearance less than 10 ml / min) should establish the dose of 200 mg 2 times a day at intervals of about 12 hours.
In the treatment of infections caused by the virus Varicella zoster (chickenpox and herpes zoster), for patients with significantly reduced immunity is recommended in severe renal insufficiency (creatinine clearance less than 10 mL / min) to establish the dose of 800 mg 2 times per day with approximately 12-hour intervals and for patients with moderate renal impairment (creatinine clearance within 10-25 mL / min) - 800 mg 3 times a day at intervals of about 8 hours.
Tablets use immunocompromised children aged 2 years.
Specific data on the use of acyclovir for prophylaxis (prevention of recurrences) infections caused by the herpes simplex virus or to treat infections caused by herpes zoster virus, children with normal immune systems do not.
Acyclovir is only partially absorbed from the gastrointestinal tract. Reported accidental ingestion by patients to 20 g acyclovir without occurrence of toxic effects. In case of accidental overdose of oral repeated oral acyclovir for several days occurring gastrointestinal (such as nausea and vomiting) and neurological symptoms (headache and confusion).
If overdose of intravenous acyclovir increased levels of serum creatinine, blood urea nitrogen, leading to kidney failure. Neurological symptoms of overdose can be confusion, hallucinations, agitation, seizures and coma.
The patient should carefully examine to identify the symptoms of intoxication. As well acyclovir from the blood eliminated by hemodialysis, the latter should be used in case of overdose.
Adverse reactions, details of which are listed below, classified by organs and systems.
From the blood and lymphatic system : anemia, thrombocytopenia, leukopenia.
Immune system: anaphylaxis.
Mental disorders and disorders of the nervous system : headache, dizziness, excitement, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, somnolence, encephalopathy, coma.
The aforementioned neurological reactions are generally reversible and usually occur in patients with renal impairment or other risk factors (see. Section "Peculiarities of Application").
From the respiratory system and chest, shortness of breath.
From the digestive system : nausea, vomiting, diarrhea, abdominal pain.
From the hepatobiliary system , reversible increase in bilirubin and liver enzymes, jaundice, hepatitis.
Skin and subcutaneous tissue : itching, rashes (including photosensitivity), urticaria, accelerated diffuse hair loss (because hair loss may be associated with many diseases and drugs, acyclovir clear connection was found) , angioedema.
From the kidneys and urinary system , increased levels of blood urea and creatinine, acute renal failure, pain in the kidneys.
Pain in the kidney may be associated with renal failure and crystalluria.
General disorders : increased fatigue, fever.
Do not use the drug after the expiry date.
It does not require special storage conditions.
Keep out of reach of children.
25 tablets in a blister; 4 blisters in a cardboard box;
5 tablets in a blister; 5 blisters in a cardboard box.
Herd Artsnaymittel AG.
Location manufacturer and address of the place where
Stadashtrasse 2-18, 61118 Bad Vilbel, Germany.
dosage Herd acyclovir 200 mg tablets of 200 №100 (25h4)
producer of Herd Artsnaymyttel AG, Germany
Pharm. group Imunostymulyatory.Protyvirusni medications for regular use.
Registration Number UA / 3840/01/01 from 12.04.2015. Ordinance number 821 from 04.12.2015
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