Heviran aciclovir (acyclovir) 400mg 30 tablets— Made in Poland by Polpharma — Free Delivery

Pharmacological properties

Pharmacodynamics. acyclovir is a synthetic analogue of a purine nucleoside, which in vitro and in vivo inhibits the replication of viruses of the herpes group pathogenic for humans: herpes simplex (hsv) types i and ii and varicella zoster virus (vzv).

The action of acyclovir in relation to inhibition of the replication of these viruses is very selective. In uninfected cells, acyclovir is not used as a substrate for endogenous thymidine kinase (TC), so the toxic effect on mammalian cells is insignificant. However, MC of viral origin, encoded by HSV and VZV viruses, phosphorylates acyclovir into a monophosphate derivative (nucleoside analog), which is then phosphorylated with the participation of cellular enzymes into di- and triphosphatacyclovir. Triphosphatacyclovir is a substrate for viral DNA polymerase, which integrates it into viral DNA, thus completing the synthesis of the viral DNA chain and suppressing its replication.

Long-term use of acyclovir or repeated courses of treatment in patients with severe immunodeficiency can cause the appearance of viral strains resistant to acyclovir. In most of the isolated strains with reduced sensitivity, a deficiency of MC is detected, but strains with altered viral MC or DNA polymerase are also described. In vitro studies also revealed the ability to form HSV strains with reduced sensitivity. The relationship between the in vitro sensitivity of the herpes virus to acyclovir and the clinical response to treatment is unknown.

Pharmacokinetics. Acyclovir is partially absorbed in the gastrointestinal tract. In the equilibrium state, the average maximum concentration (CSSmax) after taking the preparation at a dose of 200 mg every 4 hours is 3.1 μmol / L (0.7 μg / ml), and the corresponding minimum concentration (CSSmin) is 1.8 μmol / L ( 0.4 μg / ml). After taking the preparation at doses of 400 and 800 mg every 4 hours, CSSmax is 5.3 μmol / L (1.2 μg / ml) and 8 μmol / L (1.8 μg / ml), respectively, and CSSmin is 2.7 μmol / L (0.6 μg / ml) and 4 μmol / L (0.9 μg / ml).

After administration of acyclovir to adults, T½ from blood plasma is approximately 2.9 hours. Most of it is excreted in the urine unchanged. The renal clearance of acyclovir is significantly higher than that of creatinine, which indicates the participation of tubular secretion in the presence of glomerular filtration in the excretion of the preparation in the urine. The most significant metabolite of acyclovir is 9-carboxymethoxymethylguanine, which is excreted in the urine in an amount of about 10-15% of the administered dose.

Taking 1 g of probenicid 60 minutes before the administration of acyclovir lengthens the T½ of acyclovir by 18%, and the AUC in blood plasma increases by 40%.

In adults, CSSmax after 1-hour infusion of 2.5 doses of acyclovir; 5 and 10 mg / kg of body weight was 22.7 μmol (5.1 μg / ml), 43.6 μmol (9.8 μg / ml) and 92 μmol (20.7 μg / ml). The CSSmin after 7 h was 2.2 μmol (0.5 μg / ml), 3.1 μmol (0.7 μg / ml), and 10.2 μmol (2.3 μg / ml). When children aged 1 year and older were given 250 mg / m2 instead of 5 mg / kg body weight and 500 mg / m2 instead of 10 mg / kg body weight, the CSSmax and CSSmin values ​​were similar to those noted in adults. In newborns and children under the age of 3 months, who were administered acyclovir at doses of 10 mg / kg of body weight every 8 hours by 1-hour infusion, CSSmax was 61.2 μmol (13.8 μg / ml), and CSSmin - 10, 1 μmol (2.3 μg / ml).

T½ of the preparation from blood plasma is 3.8 hours.

In elderly patients, the total clearance of acyclovir decreases with creatinine clearance, although the change in T½ from blood plasma is insignificant.

In patients with chronic renal failure, the T½ of acyclovir is 19.5 hours. The T½ of acyclovir during hemodialysis is 5.7 hours. The concentration of the preparation in the blood plasma during dialysis is reduced by 60%.

The concentration of acyclovir in the CSF is about 50% of the plasma level. The binding of acyclovir to blood plasma proteins is insignificant (9–33%); therefore, no competitive displacement of acyclovir from the binding sites by other preparations was observed.

Indications

Treatment of viral infections of the skin and mucous membranes caused by the herpes simplex virus, including primary and recurrent genital herpes; 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 vzv virus (chickenpox and herpes zoster);

Application

The tablet must be taken whole with water. when using high doses of acyclovir, an adequate level of body hydration should be maintained.

Adults. Treatment of infections caused by the herpes simplex virus (HSV). To treat an infection caused by the herpes simplex virus, you should take Geviran 200 mg tablets 5 times a day (approximately every 4 hours) with a break overnight. The preparation  is taken for 5 days; in severe primary infections, the course of treatment can be extended to 10 days.

In patients with reduced immunity (for example, after bone marrow transplantation) or impaired absorption in the gastrointestinal tract, the dose can be doubled to 400 mg or the appropriate dose of the preparation can be used for intravenous administration.

Taking acyclovir should be started immediately, immediately after the diagnosis is made. In case of recurrent infections, it is very important to start taking the preparation in the prodromal period or immediately after the first signs of the disease appear.

Prevention of recurrence of herpes simplex (HSV) in immunocompromised patients

For patients with normal immunity, for the prevention of reidives of infection caused by the herpes simplex virus, take the preparation 200 mg 4 times a day approximately every 6 hours.

For many patients, the use of the preparation at a dose of 400 mg 2 times a day every 12 hours is effective.

Treatment will be effective even after reducing the dose of tabletted Geviran to 200 mg, which is taken 3 times a day at intervals of 8 hours or even 2 times a day at intervals of 12 hours. In some patients, a response to prophylactic use of the preparation appears after a daily dose of 800 mg ...

The preparation should be used intermittently every 6–12 months, observing possible changes in the course of the disease.

Prevention of infections caused by the herpes simplex virus. To prevent herpes simplex virus infections in immunocompromised patients, 200 mg tablets should be taken 4 times a day every 6 hours.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 use the appropriate dose for intravenous administration.

The duration of prophylactic use is determined by the doctor depending on the course of the disease and the individual sensitivity of the patient.

Treatment of infections caused by the chickenpox virus and herpes zoster. The preparation should be taken at 800 mg 5 times a day (approximately every 4 hours) with a break at night. The duration of treatment is 7 days.

In patients with reduced immunity (for example, after bone marrow transplantation) or impaired absorption in the gastrointestinal tract, intravenous administration of the preparation is possible.

Treatment should be started immediately after diagnosis. Treatment for chickenpox and herpes zoster is effective if you start taking the preparation immediately after the first rash appears.

Children

Treatment of infections caused by the herpes simplex virus (HSV). For children 2 years of age and older, administer doses as adults.

Treatment of infections caused by the varicella-zoster virus. Children aged 2 to 6 years: 400 mg 4 times a day.

Children over the age of 6: 800 mg 4 times a day.

The dose can be determined more precisely at the rate of 20 mg / kg of body weight (up to a maximum dose of 800 mg) 4 times a day. The duration of treatment is 5 days.

There is no data on the prevention of recurrence of infections caused by the herpes simplex virus and herpes zoster in children with normal immunity.

Elderly patients. In elderly patients, renal dysfunction should be taken into account and, accordingly, the dose should be changed. The level of hydration of the body should be monitored.

Patients with impaired renal function. Acyclovir should be used with caution in patients with impaired renal function and to monitor an adequate level of hydration of the body.

When treating infections caused by the herpes simplex virus, or preventing a viral infection in patients with moderate or severe renal impairment, the use of the recommended oral doses does not cause the accumulation of acyclovir in the body in concentrations higher than those considered safe for administration of the preparation. However, patients with severe renal failure (creatinine clearance 10 ml / min) are recommended to set the dose to 200 mg 2 times a day every 12 hours.

In the treatment of infections caused by the chickenpox virus and herpes zoster in patients with moderate renal failure (creatinine clearance 10-25 ml / min), it is recommended to set a dose of up to 800 mg 3 times a day every 8 hours, and in patients with severe renal failure ( creatinine clearance 10 ml / min) it is recommended to reduce the dose to 800 mg 2 times a day every 12 hours.

Contraindications

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

Side effects

On the part of the blood and lymphatic system: anemia, a decrease in the number of leukocytes, thrombocytopenia.

From the immune system: anaphylactic reactions.

On the part of the psyche and nervous system: headache, dizziness; very rarely - agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.

These symptoms are usually transient and occur mainly in patients with impaired renal function or other predisposing factors.

From the respiratory system, chest and mediastinal organs: suffocation.

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain.

From the liver and biliary tract: a temporary increase in the level of bilirubin and an increase in the activity of hepatic transaminases in the blood, hepatitis, jaundice.

On the part of the skin: itching, rash (also increased sensitivity to light), urticaria, generalized alopecia. Since the cause of the appearance of generalized alopecia can be many diseases and the use of various preparations, its occurrence when taking acyclovir has not been determined, vasomotor edema.

From the side of the kidneys: an increase in the level of creatinine and urea in the blood plasma, acute renal failure, pain in the kidney area.

Pain in the kidney area may be associated with kidney failure.

The patient's hydration status should be monitored. Renal dysfunction usually disappears quickly after replenishing the patient's fluid level and / or reducing the dose or discontinuing the preparation. In exceptional cases, arresters may occur.

General disorders and conditions at the injection site: fatigue, fever.

Special instructions

Acyclovir is excreted in the urine, therefore, in patients with renal insufficiency, the dose of the preparation should be reduced. in elderly people, possible impairment of renal function should be taken into account; in such patients, the possibility of reducing the dose of the preparation should be taken into account. the elderly and patients with renal insufficiency are at increased risk of developing side effects from the nervous system, therefore, the condition of patients in this category should be carefully monitored. currently known symptoms usually disappeared after discontinuation.

Use during pregnancy and lactation. In post-marketing studies of medicines containing acyclovir, cases of the use of acyclovir in pregnant women and the occurrence of disorders in them have been reported. According to the results of these studies, there was no increase in the incidence of developmental anomalies in newborns whose mothers took acyclovir compared to the general population. Pregnant women should be prescribed acyclovir only when the expected benefit to the mother outweighs the potential risk to the fetus.

When taken orally 200 mg 5 times a day, acyclovir passes into breast milk in concentrations that are 0.6–4.1% of acyclovir in blood plasma. Potentially, a child who is fed such breast milk can assimilate acyclovir at a dose of 0.3 mg / kg of body weight per day.

Prescribe the preparation to women during breastfeeding with extreme caution, taking into account the risk to the child.

Children. In children under the age of 2 years, the preparation in this dosage form is not used.

The ability to influence the reaction rate when driving or working with other mechanisms. When deciding on the possibility of driving vehicles and other mechanisms, the clinical status of the patient and the profile of adverse reactions should be taken into account. Studies on the effect of the preparation Geviran on the ability to drive vehicles and work with mechanisms have not been carried out. Given the possible occurrence of side effects, care should be taken when driving and operating other mechanisms.

Interactions

No clinically significant preparation  interactions have been identified.

Acyclovir is excreted mainly unchanged by active excretion in the renal tubules. Simultaneously taken preparations, which are transformed in the body in the same way, can cause an increase in the concentration of acyclovir in the blood plasma. Probenecid and cimetidine increase the AUC of acyclovir and decrease its renal clearance. A similar increase in blood plasma levels of acyclovir and an inactive metabolite, mycophenolate mofetil, an immunosuppressant used in patients after transplantation, was noted while taking these preparations. However, given the wide therapeutic range of acyclovir, there is no need to change the dose.

Overdose

Symptoms: acyclovir is partially absorbed into the gastrointestinal tract. a single dose of up to 20 g of acyclovir usually does not cause symptoms of poisoning. in some cases of an overdose of acyclovir for oral administration within 7 days, symptoms from the gastrointestinal tract (nausea, vomiting) and the nervous system (headache, confusion) appeared.

Neurological symptoms such as confusion, hallucinations, agitation, convulsions, and coma have also been described in overdose with the injectable form of the preparation.

Treatment: the patient should be monitored for the onset of symptoms of poisoning. Treatment is symptomatic. Hemodialysis accelerates the elimination of acyclovir from the blood and can be used in case of symptoms of an overdose.

Storage conditions

In a dry, dark place at a temperature not exceeding 25 ° C.