Aciclovir (acyclovir) 200mg 20 tablets — Made in Ukraine — Free Delivery

Brand: Lekhim
Product Code: Aciclovir
Availability: In Stock

$19.11

Description

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 type I and II, chickenpox and herpes zoster virus, Epstein-Barr virus and cytomegalovirus. In cell culture, acyclovir has the greatest activity against herpes simplex virus type I and further, as activity decreases, against herpes simplex virus type II, chickenpox and herpes 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, therefore, the toxic effect on the cells of the host organism is minimal. However, thymidine kinase, encoded in herpes simplex viruses, chickenpox viruses, herpes zoster viruses and Epstein-Barr viruses, converts acyclovir into acyclovir monophosphate, a nucleoside analogue, which is then converted sequentially into 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, there may be cases of decreased 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, but there are reports of viral thymidine kinase and DNA damage. 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 intestine. The average peak stable concentration (Cssmax) in blood plasma after taking a dose of 200 mg with a 4-hour interval is 3.1 μmol (0.7 μg / ml), and, accordingly, the level in blood plasma (Cssmin) will be 1.8 μmol (0 , 4 μg / ml). Corresponding Cssmax levels after doses of 400 mg and 800 mg with

The 4-hour intervals are 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 preparation is excreted unchanged by the kidneys. The renal clearance of acyclovir is significantly higher than the creatinine clearance, which indicates that the excretion of the preparation by the kidneys is carried out by not only glomerular filtration, but also by 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 urine. If acyclovir is used 1 hour after taking 1 g of probenecid, the terminal half-life and the area under the concentration / time curve increase by 18% and 40%, respectively.

In patients with chronic renal failure, the mean final elimination half-life is 19.5 hours. The average elimination half-life of acyclovir during hemodialysis is 5.7 hours. Plasma acyclovir levels are reduced by about 60% during dialysis.

The concentration of the preparation in the cerebrospinal fluid is approximately 50% of the corresponding concentration in the blood plasma. The level of binding to blood plasma proteins is relatively low (from 9% to 33%), and it does not change when interacting with other preparations.

With the simultaneous use of acyclovir and zidovudine for the treatment of HIV-infected patients, no changes in the pharmacokinetics of these preparations 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 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 herpes zoster).

Composition:

Active substance: aciclovir;

1 tablet contains acyclovir 200 mg (0.2 g);

excipients: lactose monohydrate, corn starch, magnesium stearate, croscarmellose sodium.

Contraindications

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

Interaction with other medicinal products and other types of interactions.

No clinically important interactions of acyclovir with other preparations have been found.

Acyclovir is excreted mainly unchanged by the kidneys by tubular secretion, therefore, any preparations that have a similar release mechanism 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 preparation also increases in the blood plasma, but due to the wide therapeutic index of acyclovir, there is no need to adjust the dose.

Features of the application.

Acyclovir is excreted from the body mainly by renal clearance, therefore, the dose should be reduced in patients with renal insufficiency (see "method of administration and dosage"). in elderly patients, the likelihood of impaired renal function is also high, therefore, 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 therefore should be closely monitored to identify these side effects. according to the data obtained, such reactions are generally reversible when the preparation is discontinued.

Particular attention should be paid to maintaining an adequate level of hydration in patients receiving high doses of acyclovir.

The preparation contains lactose, so it should not be used in patients with hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

Application during pregnancy or lactation.

There was no increase in the number of congenital defects in children whose mothers used acyclovir during pregnancy, compared with the general population. however, acyclovir tablets should be used when the potential benefit of the preparation to the mother outweighs the potential risk to the fetus.

When taken orally 200 mg of acyclovir 5 times a day, acyclovir passes into breast milk at concentrations of 0.6–4.1% of the corresponding level of acyclovir in blood plasma. Potentially, an infant can assimilate acyclovir at a dose of up to 0.3 mg / kg of body weight per day. Therefore, caution should be exercised when prescribing acyclovir to women who are breastfeeding, taking into account the benefit / risk ratio.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

When deciding on the possibility of driving a car or other mechanisms, the clinical status of the patient and the profile of side effects of the preparation should be taken into account.

Clinical studies of the effect of acyclovir on the reaction rate when driving or working with other mechanisms have not been conducted. In addition, the pharmacology of acyclovir does not give reason to expect any negative effects.

Method of administration and dosage.

The tablet should 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.

For the treatment of herpes simplex virus infections, 200 mg acyclovir tablets should be taken 5 times a day at approximately 4-hour intervals, except during the night period.

Treatment should be continued for 5 days, but in the case of a severe primary infection, it can be extended.

For some immunocompromised patients (for example, after bone marrow transplantation) or for patients with reduced intestinal absorption, the dose can be doubled to 400 mg or an appropriate intravenous dose can be used.

Treatment should be started as early 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 relapse (suppressive therapy) of infections caused by the herpes simplex virus.

In patients with normal immunity, to prevent recurrence of infections caused by the herpes simplex virus, 200 mg of acyclovir tablets should be taken 4 times a day with a 6-hour interval.

For convenience, most patients can take 400 mg of acyclovir 2 times a day at 12-hour intervals.

Treatment will be effective even after reducing the dose of tableted acyclovir to 200 mg, which should be taken 3 times a day with an 8-hour interval or even 2 times a day with a 12-hour interval.

In some patients, a radical improvement is observed after taking a daily dose of 800 mg acyclovir.

To monitor possible changes in the natural course of the disease, therapy with acyclovir 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 in patients with immunodeficiency, acyclovir tablets at a dose of 200 mg should be taken 4 times a day with

6 hour intervals. In patients with significant immunodeficiency (for example, after bone marrow transplantation) or in patients with reduced absorption in the intestine, the dose can be doubled to 400 mg or an appropriate dose for intravenous administration can be used.

The duration of prophylactic use is determined by the duration of the risk period.

Treatment for chickenpox and herpes zoster.

For the treatment of infections caused by the viruses of chickenpox and herpes zoster, 800 mg acyclovir tablets should be taken 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 intestinal absorption, intravenous administration is better.

Treatment should be started as early as possible after the onset of the disease, the result will be better if the 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 from 2 years of age with immunodeficiency, the same doses can be used as for adults.

For the treatment of chickenpox, children from 6 years old should be prescribed 800 mg of acyclovir 4 times a day, children from 2 to 6 years old can use 400 mg of acyclovir 4 times a day. The duration of treatment is 5 days.

More precisely, the dose of the preparation can be calculated by the child's body weight - 20 mg / kg of body weight per day (not to exceed 800 mg) of acyclovir, divided into 4 doses.

There is no specific data on the use of acyclovir for the prevention (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.

Do not use this dosage form of the preparation for children under 2 years of age.

Elderly patients.

It should be borne in mind the possibility of impaired renal function in elderly patients and the dose of the preparation for them must be changed accordingly (see Renal failure). It is necessary to maintain an adequate level of hydration of the body.

Renal failure

Acyclovir should be used with caution in patients with renal insufficiency. It is necessary to maintain an adequate level of hydration of the body.

In the prevention and treatment of herpes simplex virus infections 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 level established for intravenous administration. However, in patients with severe renal insufficiency (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 about 12 hours.

In the treatment of infections caused by the Varicella zoster virus (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 establish a dose of 800 mg 2 times a day with an approximately 12-hour interval and for patients with moderate renal failure (creatinine clearance within 10-25 ml / min) - 800 mg 3 times a day with an interval of about 8 hours.

Children.

Acyclovir tablets should be used in children from 2 years of age.

Overdose.

Symptoms

Acyclovir is only partially absorbed from the gastrointestinal tract. There have been cases of accidental internal intake of up to 20 g of acyclovir by patients without the occurrence of a toxic effect. Accidental repeated overdose of oral acyclovir over several days causes gastroenterological (such as nausea and vomiting) and neurological symptoms (headache and confusion).

In case of an overdose of intravenous acyclovir, the level of serum creatinine, blood urea nitrogen increases and, accordingly, renal failure appears.

Overdose neurological manifestations can be confusion, hallucinations, agitation, convulsions, and coma.

Treatment: the patient should be carefully examined to identify symptoms of intoxication. Recommended gastric lavage, symptomatic treatment. 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.

On the part of the blood and lymphatic system.

Anemia, thrombocytopenia, leukopenia.

From the immune system.

Anaphylaxis.

Mental and nervous system disorders.

Headache, dizziness, agitation, confusion, tremors, 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.

On the part of the respiratory system and chest organs.

Dyspnea.

From the gastroenterological system.

Nausea, vomiting, diarrhea, abdominal pain.

From the hepatobiliary system.

Reversible increase in the level of bilirubin and liver enzymes, jaundice, hepatitis.

On the part of 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 preparations used by the patient, no clear association has been found with acyclovir. Angioedema.

On the part of the kidneys and urinary system.

Increased blood urea and creatinine levels, acute renal failure, kidney pain.

Kidney pain can be associated with renal failure and crystalluria.

General violations.

Increased fatigue, fever.

Shelf life.

3 years.

Storage conditions.

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

Keep out of the reach of children.

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