Translation of the instructions can be
ACICLOVIR-ASTRAPHARM tablets 200 mg
Instructions for use of the medicinal product
composition
Active ingredient: aciclovir;
1 tablet contains acyclovir 200 mg
Excipients: lactose, microcrystalline cellulose, sodium starch glycolate (type A); povidone, magnesium stearate.
Dosage form
Pills.
Pharmacotherapeutic group
Antivirals for systemic use. Direct-acting antivirals. Nucleosides and nucleotides, except reverse transcriptase inhibitors. Acyclovir.
PBX code J05A B01.
Clinical characteristics
Indication
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 recurrence) 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 virus (chickenpox and shingles).
Contraindication
Hypersensitivity to acyclovir, valacyclovir or other components of the drug.
Method of administration and doses
The tablet should be taken whole with water. When using high doses of acyclovir, adequate 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-Astrapharm tablets at a dose of 200 mg 5 times a day with an interval of approximately 4 hours, except at night.
Treatment should last 5 days, but in case of severe primary infection it may be extended.
For patients with severe immunodeficiency (for example, after bone marrow transplantation) or for patients with reduced intestinal absorption, the dose can be doubled to 400 mg or the dosage form of the drug for intravenous administration can be used.
Treatment should be started as early as possible after the onset of infection. In the case of recurrent herpes, it is best to start treatment in the prodromal period or after the first signs of skin lesions appear.
Prevention of recurrence (suppressive therapy) of infections caused by the herpes simplex virus
Patients with normal immunity are prescribed Acyclovir-Astrapharm tablets at a dose of 200 mg 4 times a day with a 6-hour interval to prevent recurrence of infections caused by the herpes simplex virus.
For convenience, most patients can take 400 mg 2 times a day, 12 hours apart.
Treatment will be effective even after reducing the dose of the tableted drug Acyclovir-Astrapharm to 200 mg, which is taken 3 times a day with an 8-hour interval or even 2 times a day with an 12-hour interval.
Some patients experience radical improvement after taking a daily dose of Acyclovir-Astrapharm 800 mg.
To monitor possible changes in the natural course of the disease, acyclovir therapy should be interrupted periodically 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 should take Acyclovir-Astrafarm tablets at a dose of 200 mg 4 times a day with a 6-hour interval. For patients with significant 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 for intravenous administration can be used.
The duration of prophylaxis depends on the duration of the risk period.
Treatment of chickenpox and herpes zoster
For the treatment of infections caused by the varicella and herpes zoster viruses, take Acyclovir-Astrapharm tablets at a dose of 800 mg 5 times a day at 4-hour intervals, except at night. Treatment should last 7 days.
Patients with severe immunodeficiency (for example, after bone marrow transplantation) or patients with reduced absorption in the intestine are better off using intravenous administration.
Treatment should be started as early as possible after the onset of the disease; the result will be better if treatment is started immediately after the rash appears.
children
For the treatment and prevention of infections caused by the herpes simplex virus, doses similar to those for adults can be used in immunocompromised children from 2 years of age.
For the treatment of chickenpox in children aged 6 years and older, 800 mg of acyclovir is prescribed 4 times a day, children aged 2 to 6 years can receive 400 mg of acyclovir 4 times a day. The duration of treatment is 5 days.
The dose can be calculated more accurately based on the child's body weight - 20 mg/kg of body weight per day (not to exceed 800 mg), which is divided into 4 doses.
There are no specific data on the use of acyclovir for the prophylaxis (prevention of recurrence) 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 is not used for children under 2 years of age.
Elderly patients
The possibility of impaired renal function in elderly patients should be considered and the dose should be adjusted accordingly (see Renal Failure). Adequate hydration should be maintained.
Acyclovir should be administered with caution to patients with renal insufficiency. Adequate hydration should be maintained.
In the prevention and treatment of infections caused by the herpes simplex virus, in patients with renal insufficiency, the recommended oral doses do not lead to accumulation of acyclovir, the level of which would exceed the safe limit established for intravenous administration. However, for patients with severe renal insufficiency (creatinine clearance
In the treatment of infections caused by the Varicella zoster virus (chickenpox and shingles), for patients with significantly reduced immunity, it is recommended in severe renal failure (creatinine clearance
Adverse reactions
Blood disorders: anemia, thrombocytopenia, leukopenia.
Immune system disorders: anaphylaxis.
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 in patients with renal insufficiency or other risk factors.
Respiratory system: shortness of breath.
On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain.
From the hepatobiliary system: reversible increase in bilirubin and liver enzymes, jaundice, hepatitis.
Skin: itching, rash (including photosensitivity), urticaria, accelerated diffuse hair loss (since hair loss can be associated with a large number of diseases and drugs, a clear connection with acyclovir has not been identified); angioedema.
Renal and urinary disorders: increased blood urea and creatinine, acute renal failure, kidney pain. Kidney pain may be associated with renal failure and crystalluria.
General disorders: increased fatigue, fever.
Overdose
Symptoms: Accidental repeated overdose of oral acyclovir produces gastroenterological (such as nausea and vomiting) and neurological symptoms (headache and confusion) over several days.
Neurological manifestations of overdose may include confusion, hallucinations, agitation, seizures, and coma.
Treatment: the patient should be carefully examined for symptoms of intoxication. Gastric lavage is recommended. Treatment is symptomatic. Since the level of acyclovir in the blood is well removed by hemodialysis, it should be used in case of overdose.
Application features
Use during pregnancy and breastfeeding.
There has been no increase in the number of birth defects in children whose mothers used acyclovir during pregnancy. However, acyclovir tablets should be used only when the potential benefit to the mother outweighs the potential risk to the fetus.
When taken orally at a dose of 200 mg 5 times a day, acyclovir passes into breast milk. Therefore, acyclovir should be prescribed to breastfeeding women with caution, taking into account the risk/benefit ratio.
Children.
The drug in this dosage form is not prescribed to children under 2 years of age.
Acyclovir is eliminated primarily by renal clearance, and therefore the dose should be reduced in patients with renal impairment (see Dosage and Administration). Elderly patients are also more likely to have impaired renal function, and a dose reduction may be necessary in this patient group. Both groups (renal impairment and the elderly) are at increased risk for neurological adverse events and should be monitored closely for these adverse events. These events have been reported to be reversible upon discontinuation of treatment.
Special attention should be paid to maintaining adequate hydration in patients receiving high doses of acyclovir.
The drug contains lactose, so it should not be used in patients with rare hereditary forms of galactose intolerance, congenital lactase deficiency or glucose-galactose malabsorption syndrome.
The ability to influence the reaction speed when driving or working with other mechanisms.
When deciding whether to drive or use machines, the patient's clinical status and the side-effect profile of the drug should be taken into account. Clinical studies of the effect of acyclovir on the speed of reaction when driving or operating machinery have not been conducted. In addition, the pharmacology of acyclovir does not give reason to expect any negative effects.
Interaction with other medicinal products and other types of interactions
Acyclovir is excreted mainly unchanged by the kidneys by tubular secretion, so any drugs that have a similar mechanism of excretion can 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. With simultaneous use 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, given the wide therapeutic index of acyclovir, dose adjustment is not required.
Pharmacological properties
Pharmacodynamics. Acyclovir is a synthetic purine nucleoside analogue with inhibitory activity in vivo and in vitro against human herpesviruses, 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, 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 by herpes simplex viruses, varicella zoster viruses, and Epstein-Barr viruses, converts acyclovir to acyclovir monophosphate, a nucleoside analogue, which is then converted sequentially to diphosphate and triphosphate by cellular enzymes. Following incorporation into viral DNA, acyclovir triphosphate interacts with viral DNA polymerase, resulting in termination of viral DNA chain synthesis.
With prolonged or repeated courses of treatment in severely immunocompromised patients, cases of reduced sensitivity of individual virus strains may occur, which do not always respond to treatment with acyclovir. Most clinical cases of insensitivity are associated with a deficiency of viral thymidine kinase, but there are reports of damage to viral thymidine kinase and DNA. In vitro interaction of individual herpes simplex viruses with acyclovir can also lead to the formation of less sensitive strains. The relationship between the sensitivity of individual herpes simplex viruses in vitro and the clinical results of treatment with acyclovir is not fully understood.
The use of acyclovir together with antiretroviral drugs reduces the mortality of patients with advanced HIV infection, and also, subject to prior use of acyclovir for 1 month for intravenous administration, reduces the mortality of patients after bone marrow transplantation.
Pharmacokinetics. Acyclovir is only partially absorbed from the intestine. The mean peak steady-state plasma concentration (C ssmax) after a 200 mg dose administered 4 hours apart is 3.1 μmol (0.7 μg/ml) and the plasma level (C ssmin) is 1.8 μmol (0.4 μg/ml). The corresponding C ss max levels after 400 mg and 800 mg doses administered 4 hours apart are 5.3 μmol (1.2 μg/ml) and 8 μmol (1.8 μg/ml), and the equivalent C ssmin levels are 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. Renal clearance of acyclovir is significantly higher than creatinine clearance, which indicates that renal excretion of the drug is carried out not only by glomerular filtration, but also by tubular secretion.
9-carboxymethoxymethylguanine is the only major metabolite of acyclovir that can be detected in the urine and accounts for approximately 10-15% of the administered dose. When 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 half-life of acyclovir during hemodialysis is 5.7 hours. The level of acyclovir in blood plasma during dialysis decreases by approximately 60%.
The concentration of the drug in the cerebrospinal fluid is approximately 50% of the corresponding concentration in blood plasma. The level of binding to plasma proteins is relatively low (9 - 33%), and it does not change when interacting with other drugs.
No changes in the pharmacokinetics of acyclovir and zidovudine were observed when acyclovir and zidovudine were co-administered for the treatment of HIV-infected patients.
Pharmaceutical characteristics
Main physicochemical properties: tablets are white or almost white, round, biconvex and scored on one side.
Expiration date
5 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister, 1 or 2 blisters in a box.
Vacation category
According to the recipe.
Producer
"Astrafarm" LLC.
Location
Ukraine, 08132, Kyiv region, Kyiv-Svyatoshyn district, Vyshneve, Kyivska st., 6
