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  • Aciclovir-Darnitsa (Acyclovir) 200mg 20 tablets — Made in Ukraine — Free Delivery


    Brand: Darnitsa
    Product Code: Aciclovir-Darnitsa 200mg
    Availability: In Stock
    $21.88
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    Pharmacological properties

    Pharmacodynamics. acyclovir is a synthetic analogue of a purine nucleoside with in vivo and in vitro inhibitory activity against human herpesvirus, including herpes simplex virus types I and II, chickenpox and herpes zoster virus, Epstein-barr virus and cytomegalovirus. in cell culture, acyclovir is most active against herpes simplex virus type i and further, in decreasing activity, against herpes simplex virus type ii, varicella-zoster virus and herpes zoster, epstein-barr virus and cytomegalovirus.
    The inhibitory activity of acyclovir against the aforementioned viruses is highly selective. The enzyme thymidine kinase in a normal uninfected cell does not use acyclovir as a substrate, therefore, the toxic effect on the cells of the host organism is minimal. However, thymidine kinase, encoded in herpes simplex virus, varicella zoster virus, and Epstein-Barr virus, converts acyclovir into acyclovir monophosphate, a nucleoside analogue, which is then converted sequentially to diphosphate and triphosphate using cell enzymes. Following the insertion of acyclovir into the viral DNA, triphosphate interacts with the viral DNA polymerase, resulting in the termination of the synthesis of the viral DNA chain.
    With prolonged or repeated courses of treatment of critically ill patients with reduced immunity, it is possible to reduce the sensitivity of certain strains of the virus, which do not always respond to treatment with acyclovir. Most clinical cases of insensitivity are associated with viral thymidine kinase deficiency, however, viral thymidine kinase and DNA damage have been reported. In vitro interactions of certain 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.
    Pharmacokinetics. Acyclovir is only partially absorbed in the digestive tract (about 20% of the dose taken). Simultaneous food intake does not lead to a decrease in absorption. Cmax is reached after 1.5-2 hours.
    The level of its binding to blood plasma proteins is relatively low (from 9 to 33%) and does not change when interacting with other preparations.
    Acyclovir crosses the placental barrier, into the CSF (50% of the corresponding concentration in blood plasma), breast milk.
    Most of the preparation (85–90%) is excreted unchanged by the kidneys, and only a small part (10–15%) is excreted as a metabolite (9-carboxymethoxymethylguanine). The renal clearance of acyclovir is significantly higher than the clearance of creatinine, which indicates that the excretion of the preparation by the kidneys is carried out by not only glomerular filtration, but also by tubular secretion.
    The final T1 / 2 with intravenous administration of acyclovir is approximately 2.9 hours, in patients with chronic renal failure - 19.5 hours, during hemodialysis - 5.7 hours. The level of acyclovir in blood plasma during dialysis decreases by about 60%.

    Indications

    Treatment of infections of the skin and mucous membranes caused by the herpes simple virus, including primary and recurrent genital herpes.
    Prevention of recurrence of infections caused by the Herpes simple virus in patients with normal immunity.
    Prevention of infections caused by the Herpes simple virus in immunocompromised patients.
    Treatment of infections caused by the Varicella zoster virus (chickenpox, herpes zoster).

    Application

    The tablet should be taken whole with water. when using high doses of the preparation, an adequate level of hydration of the body should be maintained.
    Adults. Treatment of infections caused by the Herpes simple virus. The preparation should be used in a dose of 200 mg 5 times a day at approximately 4-hour intervals, with the exception of the night period. The duration of treatment is 5 days, but in the case of a severe primary infection, it can be continued.
    If necessary, in patients with severe immunodeficiency or with reduced absorption in the intestine, a single dose can be doubled to 400 mg or an appropriate dose can be used for intravenous administration.
    Treatment should be started as early as possible after the onset of the infection. In the case of recurrent herpes, it is best to start treatment during the prodromal period or after the first signs of skin lesions appear.
    Prevention of recurrence of infections caused by the Herpes simple virus in patients with normal immunity. The preparation  should be used at a dose of 200 mg 4 times a day with a 6-hour interval (or, for convenience, at a dose of 400 mg 2 times a day with a 12-hour interval).
    Treatment will be effective even after reducing the dose of the preparation to 200 mg 3 times a day with an 8-hour interval or even 2 times a day with a 12-hour interval.
    In some cases, a radical improvement is noted after taking a daily dose of 800 mg.
    To monitor possible changes in the natural course of the disease, preparation therapy should be interrupted periodically at intervals of 6–12 months.
    Prevention of infections caused by the Herpes simple virus in immunocompromised patients. The preparation should be used in a dose of 200 mg 4 times a day with a 6-hour interval.
    If necessary, in patients with severe immunodeficiency or with reduced absorption in the intestine, a single dose can be doubled to 400 mg or an appropriate dose can be used for intravenous administration.
    The duration of prophylaxis depends on the length of the risk period.
    Treatment of infections caused by the Varicella zoster virus. The preparation should be used in a dose of 800 mg 5 times a day at approximately 4-hour intervals, with the exception of the night period. Duration of treatment is 7 days.
    Treatment should be started as early as possible after the onset of the disease, the result will be better if therapy is started immediately after the appearance of the rash.
    For patients with severe immunodeficiency or with reduced absorption in the intestine, it is better to use intravenous administration of the preparation.
    Children from 2 years of age. Treatment and prevention of infections caused by the Herpes simple virus in immunocompromised children. The preparation should be used in doses as for adults.
    Chickenpox treatment. The preparation should be used in a dose: children aged 2 to 6 years - 400 mg 4 times a day, children over 6 years old - 800 mg 4 times a day.
    More precisely, the dose of the preparation can be calculated by the child's body weight - 20 mg / kg of body weight per day, divided into 4 doses. The maximum daily dose is 800 mg. Duration of treatment is 5 days.
    There is no specific data on the use of acyclovir for the prevention 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.
    Patients with impaired renal function. The preparation should be used with caution. It is necessary to maintain an adequate level of hydration of the body.
    In the prevention and treatment of infections caused by the Herpes simple virus in patients with renal insufficiency, the recommended oral doses do not lead to the accumulation of acyclovir, the level of which would exceed the safe values ​​established for intravenous administration. However, patients with severe renal insufficiency (creatinine clearance 10 ml / min) are recommended to use the preparation at a dose of 200 mg 2 times a day with approximately 12-hour intervals.
    In the treatment of infections caused by the Varicella zoster virus, patients with significantly reduced immunity are recommended to use the preparation in a dose: with severe renal failure (creatinine clearance 10 ml / min) - 800 mg 2 times a day with approximately 12-hour intervals, with moderate renal failure (creatinine clearance within 10-25 ml / min) - 800 mg 3 times a day with approximately 8-hour intervals.
    Elderly patients. The preparation should be used with caution. It is necessary to maintain an adequate level of hydration of the body.
    It should be borne in mind the possibility of impaired renal function in elderly patients, and the dose of the preparation for them should be changed accordingly.

    Contraindications

    Hypersensitivity to acyclovir, valacyclovir or other components of the preparation.

    Side effects

    From the side of the cardiovascular system: palpitations, chest pain.
    From the blood and lymphatic system: anemia, leukopenia, thrombocytopenia.
    From the nervous system and psyche: headache, dizziness, psychomotor agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.
    The above symptoms are in most cases reversible and occur mainly in patients with renal insufficiency or other risk factors (see SPECIAL INSTRUCTIONS).
    From the respiratory system, chest and mediastinal organs: shortness of breath.
    From the digestive tract: nausea, vomiting, diarrhea, abdominal pain, loss of appetite, gastritis, dysphagia.
    From the hepatobiliary system: a transient increase in the activity of liver enzymes and the level of bilirubin, jaundice, hepatitis.
    From the urinary system: an increase in the concentration of urea and creatinine in the blood, acute renal failure, pain in the kidney area. Pain in the kidney area may be associated with renal failure and crystalluria.
    From the immune system, skin and subcutaneous tissue: hypersensitivity reactions, including rash, itching, hyperemia, urticaria, angioedema, anaphylactic reactions; photosensitivity, alopecia.
    Since hair loss can be associated with a large number of diseases and taking medications, a clear connection with the use of acyclovir has not been established.
    General disorders: fatigue, fever.

    special instructions

    When using high doses of the preparation, an adequate level of hydration of the body should be maintained.
    The preparation should be used with caution in patients with impaired renal function, since acyclovir is excreted from the body mainly by renal clearance. Dose adjustments should be made (see APPLICATION).
    The preparation should be used with caution in elderly patients, since this group of patients is more likely to have renal impairment. If necessary, a dose adjustment should be made (see APPLICATION).
    Both of these groups (patients with impaired renal function and elderly patients) are at risk for neurological disorders, and therefore they should be closely monitored to identify these adverse reactions. According to the data obtained, such reactions are generally reversible if treatment is discontinued (see SIDE EFFECTS).
    Use during pregnancy and lactation. In the post-registration period of observation of pregnant women, the results of the use of various pharmaceutical forms of acyclovir in pregnant women have been documented. There was no increase in the number of congenital defects in children whose mothers used acyclovir during pregnancy, compared with the general population.
    When taken orally, acyclovir in a dose of 200 mg 5 times a day, it penetrates into breast milk at concentrations of 0.6–4.1% of the corresponding level of acyclovir in blood plasma. Potentially, a child can receive acyclovir at a dose of up to 0.3 mg / kg of body weight per day.
    During pregnancy and lactation, the preparation should be used when its potential benefit to the mother outweighs the possible risk to the fetus.
    Children. The preparation should be used in children aged 2 years and older.
    The ability to influence the reaction rate when driving or working with other mechanisms. Clinical studies of the effect of acyclovir on the reaction rate when driving or working with other mechanisms have not been conducted. The pharmacology of acyclovir does not give reason to expect any negative effect. When deciding on the possibility of driving a car and other mechanisms, the clinical status of the patient and the profile of adverse reactions of the preparation should be taken into account.

    Interactions

    Acyclovir is excreted mainly unchanged by the kidneys by tubular secretion, so any preparations that have a similar release mechanism can increase the concentration of acyclovir in the blood plasma.
    With simultaneous use with other preparations , it is possible:
    with probenecid, cimetidine - lengthening T½ of acyclovir and AUC;
    with immunosuppressants in patients after organ transplantation - an increase in the level of acyclovir and an inactive metabolite of the immunosuppressive preparation in the blood plasma, taking into account the wide therapeutic index of acyclovir, there is no need for dose adjustment.
    No clinically important interactions of acyclovir with other preparations have been identified.

    Overdose

    Symptoms acyclovir is only partially absorbed in the digestive tract. there have been reports of cases of patients unintentionally taking up to 20 g of acyclovir without causing a toxic effect.
    In case of an accidental overdose of ingested acyclovir, the following symptoms occur for several days: gastroenterological (nausea, vomiting) and neurological (headache, confusion).
    In case of an overdose of intravenous acyclovir, the level of creatinine in the blood plasma, urea nitrogen in the blood increases and, accordingly, renal failure appears. Overdose neurological manifestations can be confusion, hallucinations, agitation, convulsions, and coma.
    Treatment: the patient should be examined to identify symptoms of intoxication, symptomatic therapy should be carried out, in severe cases - hemodialysis.

    Storage conditions

    In its original packaging at a temperature not exceeding 25 ° C.

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