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HEALTH CARE
Zovirax aciclovir (acyclovir) 200mg 25 tablets — Made in Poland — Free Delivery
Zovirax aciclovir (acyclovir) 200mg 25 tablets — Made in Poland — Free Delivery
Brand:
GlaxoSmithKline
Product Code:
Zovirax 200mg
Availability:
In Stock
$24.19
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Description
Pharmacological properties
Acyclovir is a synthetic analogue of a purine nucleoside with high inhibitory activity in vitro and in vivo against herpes viruses, including herpes simplex virus types 1 and 2, varicella zoster virus, Epstein-barr virus and cytomegalovirus. in cell culture, acyclovir is most active against herpes simplex virus type 1, less active against herpes simplex virus type 2, varicella zoster virus, epstein-barr virus and cytomegalovirus. the antiviral activity of acyclovir is highly selective. the inhibitory activity of acyclovir against these viruses is highly selective. the enzyme thymidine kinase in a normal uninfected cell does not use acyclovir as a substrate, therefore toxicity to the host cells is minimal. nevertheless, thymidine kinase, encoded in herpes simplex viruses, varicella zoster virus, herpes zoster virus and Epstein-barr virus, converts acyclovir to acyclovir monophosphate, a nucleoside analogue, which is then sequentially converted to diphosphate and triphosphate using cell enzymes. after incorporation into the viral DNA of acyclovir, triphosphate interacts with viral DNA polymerase and disrupts viral DNA replication.
With prolonged or repeated courses of treatment of seriously ill patients with reduced immunity, cases of resistance of certain viral strains to acyclovir are possible. Most clinical cases of resistance are associated with viral thymidine kinase deficiency, but there are reports of damage to thymidine kinase and DNA. 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 applying a dose of 200 mg with a 4-hour interval is 3.1 μmol (0.7 μg / ml), respectively, Cssmin - 1.8 μmol (0.4 μg / ml) ... Cssmax after applying doses of 400 and 800 mg with a 4-hour interval are 5.3 μmol (1.2 μg / ml) and 8 μmol (1.8 μg / ml), equivalent to Cssmin - 2.7 μmol (0.6 μg / ml) and 4 μmol (0.9 μg / ml).
In adults, T½ with the on / in the introduction of acyclovir is about 2.9 hours. Most of the preparation is excreted unchanged by the kidneys. 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 not only by glomerular filtration, but also by tubular secretion.
9-carboxymethoxymethylguanine, the only important metabolite of acyclovir that can be detected in urine, accounts for about 10-15% of the dose. If acyclovir is administered 1 hour after taking 1 g of probenecid, T½ and AUC increase by 18 and 40%, respectively.
In patients with chronic renal failure, the average T½ is 19.5 hours. The average T½ of acyclovir during hemodialysis is 5.7 hours. The concentration of acyclovir in blood plasma during dialysis decreases by about 60%.
The CSF concentration is about 50% of the corresponding plasma concentration. The degree of binding to blood plasma proteins is relatively low (from 9 to 33%) and 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 have been revealed.
Indications
Treatment for 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).
Application
The tablet should be taken whole with water. when using acyclovir in high doses, an adequate level of body hydration should be maintained.
Adults. Treatment for infections caused by the herpes simplex virus. For treatment of infections caused by the herpes simplex virus, it is necessary to take Zovirax tablets at a dose of 200 mg 5 times a day with an approximate 4-hour interval, with the exception of the night period. Treatment should be 5 days, but if the primary infection is severe, it can be extended.
For therapy in persons with severe immunodeficiency (for example, after bone marrow transplantation) or patients with reduced absorption in the intestine, the dose can be doubled to 400 mg or the appropriate dose can be administered intravenously. Treatment should be started as early as possible after the onset of the infection. In the case of recurrent herpes, it is better to start therapy 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. In patients with normal immunity, to prevent recurrence of infections caused by the herpes simplex virus, Zovirax tablets at a dose of 200 mg are taken 4 times a day with a 6-hour interval. For convenience, most patients can take 400 mg of Zovirax 2 times a day at 12-hour intervals. Treatment will be effective even after reducing the dose of Zovirax tablets to 200 mg, which is 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 Zovirax 800 mg. To monitor possible changes in the natural course of the disease, Zovirax 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 Zovirax 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 in persons with reduced absorption in the intestine, the dose can be doubled to 400 mg or the corresponding dose can be used for intravenous administration. The duration of prophylaxis depends on the length of the risk period.
Treatment for chickenpox and herpes zoster. For treatment of infections caused by the chickenpox virus and herpes zoster, you must take Zovirax tablets at a dose of 800 mg 5 times a day at 4-hour intervals, with the exception of the night period. The treatment should last 7 days.
In patients with severe immunodeficiency (for example, after bone marrow transplantation) or with reduced absorption in the intestine, it is better to use intravenous administration. Therapy 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 with immunodeficiency at the age of 2 years, the preparation can be used in doses as for adults. For the treatment of chickenpox in children aged 6 years and older, 800 mg of Zovirax is prescribed 4 times a day, children aged 2–6 years can receive 400 mg of Zovirax 4 times a day. The duration of treatment is 5 days.
More precisely, the dose of the preparation can be calculated based on the child's body weight - 20 mg / kg of body weight (not to exceed 800 mg) of Zovirax 4 times a day.
There is no special data on the use of Zovirax 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.
For the treatment of infections caused by herpes viruses in newborns and children under the age of 3 months, Zovirax is used, a lyophilisate for the preparation of a solution for infusion.
Elderly patients. It should be borne in mind the possibility of impaired renal function in the elderly, and the dose of the preparation for them must be changed accordingly (see Renal failure). It is required to maintain an adequate level of hydration of the body in elderly people using Zovirax in a high dose.
Renal failure Zovirax 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, for patients with severe renal failure (creatinine clearance 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), for patients with significantly reduced immunity, it is recommended in severe renal failure (creatinine clearance 10 ml / min) to establish a dose of 800 mg 2 times a day with approximately 12-hour intervals. and for persons with moderate renal failure (creatinine clearance within 10-25 ml / min) - 800 mg 3 times a day with an interval of about 8 hours.
Contraindications
Hypersensitivity to acyclovir, valacyclovir or other components of the preparation.
Side effects
Side effects, the data on which are given below, are classified by organs and systems and the frequency of their occurrence. by frequency are divided into the following categories: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥1 / 1000 and 1/100), rarely (≥1 / 10,000 and 1 / 1000), very rarely (1/10 000).
Blood and lymphatic system: very rarely - anemia, thrombocytopenia, lymphopenia.
Immune system: rarely - anaphylaxis.
Mental and nervous system disorders: often - headache, dizziness; very rarely - agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.
These neurological symptoms are mostly reversible and usually occur in patients with renal failure or other risk factors (see SPECIAL INSTRUCTIONS).
Respiratory system and chest organs: rarely - shortness of breath.
Gastroenterological system: often - nausea, vomiting, diarrhea, abdominal pain.
Hepatobiliary system: rarely - a reversible increase in the level of bilirubin and liver enzymes; very rarely - jaundice, hepatitis.
Skin and subcutaneous tissue: often - itching, rashes (including photosensitivity); infrequently - urticaria, accelerated diffuse hair loss. Since hair loss can be associated with a large number of diseases and preparations used, a clear connection with acyclovir has not been established; rarely - angioedema.
Kidneys and urinary system: rarely - increased levels of creatinine and urea in the blood; very rarely - acute renal failure, kidney pain. Kidney pain can be associated with renal failure and crystalluria.
General disorders: often - fatigue, fever.
Special instructions
Patients with renal insufficiency and the elderly. acyclovir is excreted from the body mainly by renal clearance, therefore, the dose should be reduced in patients with renal insufficiency (see application). in the elderly, there is a high likelihood of impaired renal function, therefore, this group of patients may also require dose reduction. both of these groups (patients with renal insufficiency and the elderly) are at risk for the occurrence of adverse reactions from the nervous system and therefore require careful monitoring to identify these adverse reactions. according to the data obtained, such reactions are reversible if treatment is discontinued (see side effects). long-term or repeated courses of treatment with acyclovir in persons with severely weakened immunity can lead to the release of viral strains with reduced sensitivity, which may not respond to long-term treatment with acyclovir.
Particular attention should be paid to maintaining an adequate level of hydration in patients using high doses of acyclovir.
The risk of kidney damage increases with simultaneous use with other preparations that have nephrotoxic effects.
The available data from clinical trials are not sufficient to conclude that treatment with acyclovir reduces the incidence of complications associated with chickenpox in immunocompetent patients.
Use during pregnancy and lactation. There is no information available on the effects of acyclovir on female fertility.
In a study involving 20 male patients with a normal sperm count when administered orally at a dose of up to 1 g / day for 6 months, no clinically significant effect on sperm count, locomotor activity or morphology was found.
In the post-registration register of observation of pregnant women, the results of the use of various dosage forms of Zovirax in pregnant women are documented. The increase in the number of congenital defects in children whose mothers took Zovirax during pregnancy has not been determined, compared with the general population. However, taking Zovirax tablets is necessary in cases where the potential benefit of the preparation to a pregnant woman outweighs the potential risk to the fetus.
When taken orally 200 mg of acyclovir 5 times a day, acyclovir is determined in breast milk at concentrations of 0.6–4.1 acyclovir plasma levels. Potentially, a child fed with this milk can take acyclovir at a dose of up to 0.3 mg / kg of body weight per day. Therefore, caution should be exercised when prescribing acyclovir for breastfeeding, taking into account the risk / benefit ratio.
Children. Zovirax tablets are used in children over the age of 2 years.
The ability to influence the reaction rate when driving or working with other mechanisms. When deciding on the possibility of driving vehicles and working with other mechanisms, the general condition of the patient and the profile of adverse reactions 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 pharmacological properties of acyclovir do not give reason to expect any negative effects.
Interactions
No clinically significant interactions of acyclovir with other preparations have been identified.
Acyclovir is mainly excreted by the kidneys by tubular secretion, so any preparations with a similar release mechanism can increase the concentration of acyclovir in the blood plasma.
Probenicid and cimetidine lengthen the T½ of acyclovir and increase the AUC, but due to the wide therapeutic index of acyclovir, there is no need to adjust the dose of the preparation.
With simultaneous use with an immunosuppressant in the treatment of patients after organ transplantation (mycophenolate mofetil) in the blood plasma, the level of acyclovir and the inactive metabolite of mycophenolate mofetil also increases, but taking into account the wide therapeutic index of acyclovir, dose adjustment is not required.
An experimental study of 5 men indicates that concomitant therapy with acyclovir increases the AUC of fully administered theophylline by about 50%. It is recommended to measure the concentration of theophylline in blood plasma when combined with acyclovir.
Overdose
Symptoms acyclovir is only partially absorbed in the gastrointestinal tract. there have been cases of patients unintentionally ingesting up to 20 g of acyclovir without a toxic effect. with an accidental repeated overdose of oral acyclovir for several days, gastroenterological (nausea, vomiting) and neurological symptoms (headache and confusion) occur.
Treatment. The patient must be examined to identify symptoms of intoxication. Since the level of acyclovir in the blood is well eliminated by hemodialysis, the latter is used in case of overdose.
Storage conditions
At temperatures up to 25 ° c in a dry place.
1 reviews
User
06/02/2021
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Fast shipment, high quality product! Thanks! ++++++++++