Pharmacological properties
Pharmacodynamics.
acyclovir is an antiviral drug that exhibits high activity in vitro against herpes simplex virus types I and II. the toxic effect on the cells of the host body is minimal. When acyclovir enters cells infected with the herpes virus, it is phosphorylated to form the active compound, acyclovir triphosphate. the first step of this process depends on the presence of virus-encoded thymidine kinase. Acyclovir triphosphate acts as an inhibitor and substrate for viral DNA polymerase, preventing further synthesis of viral DNA without affecting normal cellular processes. Pharmacokinetics. The level of systemic absorption of acyclovir after repeated topical application of Gerpevir ointment is minimal.
Geviran tablets p/o 800 mg No. 10x3
Name
Geviran tablet p/o 800 mg in blister pack. №10x3
Description
Film-coated tablets, round, biconvex.
Main active ingredient
Acyclovir
Release form
Pills
Dosage
800mg
pharmachologic effect
Acyclovir is a synthetic analogue of purine nucleoside, which in vitro and in vivo suppresses the replication of Herpes group of viruses pathogenic to humans, such as Herpes simplex virus (HSV) types 1 and 2 and Varicella-Zoster virus (VZV). The inhibitory effect of acyclovir on the replication of these viruses is very selective. In uninfected cells, endogenous thymidine kinase (TK) does not use acyclovir as a substrate, therefore, the toxic effect on mammalian cells is small. However, viral-derived TK, encoded by the HSV and VZV viruses, phosphorylates acyclovir to a monophosphate derivative (nucleoside analogue), which is then phosphorylated by cellular enzymes, sequentially into acyclovir di- and triphosphate. Acyclovir triphosphate is a substrate for viral DNA polymerase and is incorporated into viral DNA, which, as a result, leads to the completion of the synthesis of the viral DNA chain and inhibits its replication. Long-term treatment with acyclovir or repeated courses of treatment in patients with severe immunodeficiency may lead to the selection of virus strains resistant to acyclovir. Most isolated strains with reduced sensitivity exhibit a relative deficiency of TK, but strains with altered viral TK or DNA polymerase have also been described. In vitro studies have also revealed the ability to produce HSV strains with reduced sensitivity. The relationship between the in vitro sensitivity of HSV to acyclovir and the clinical response to treatment is unknown.
Indications for use
for the treatment of infections of the skin and mucous membranes caused by the herpes simplex virus, including primary and recurrent genital herpes (excluding neonatal herpes and severe herpes infections and children with weakened immune systems) for suppressive therapy (prevention of relapses) of herpes simplex virus) in patients with unimpaired immunity for the prevention of herpes simplex virus in patients with immunodeficiency.
Directions for use and doses
The medicinal product Geviran should be taken in accordance with the doctor's recommendations. If in doubt, consult your doctor again. The dosage of the drug may be different for different patients. Treatment should begin immediately after diagnosis. During treatment, the patient should take plenty of fluids to avoid the risk of kidney damage and reduce the risk of side effects. The tablets should be swallowed whole with water. Dosage in adults Treatment of infections caused by the herpes simplex virus The drug should be taken at a dose of 200 mg five times a day, every 4 hours, with a break at night for 5 days. In severe cases, treatment is prolonged. In patients with reduced immunity (for example, after bone marrow transplantation) or with impaired absorption from the gastrointestinal tract, the dose can be increased to 400 mg (as an option, intravenous administration of the drug may be considered). Treatment should begin as soon as possible, immediately after diagnosis. For recurrent infections, it is especially important to begin treatment in the prodromal period or immediately after the first changes appear on the skin. Suppressive therapy of herpes simplex virus (Herpes simplex virus) in patients with unimpaired immunity The drug is prescribed 200 mg four times a day, every 6 hours. For most patients, taking the drug twice a day, every 12 hours, 400 mg can be effective and convenient. Gradually reducing the dose to 200 mg three times daily, every 8 hours, or even twice daily, every 12 hours may also be effective. In some patients, a reaction to taking the drug occurs after prescribing a total daily dose of the drug product of 800 mg. Drug therapy may be interrupted every 6 to 12 months in order to monitor possible changes in the course of the disease. Prevention of herpes simplex virus in patients with immunodeficiency The drug is prescribed 200 mg four times a day, every 6 hours. In patients with reduced immunity (for example, after bone marrow transplantation) or with impaired absorption from the gastrointestinal tract, the dose can be increased to 400 mg (as an option, intravenous administration of the drug may be considered). The duration of preventive treatment is determined by the length of the risk period. Treatment of infections caused by the chickenpox virus and herpes zoster (Varicella-Zoster virus) The drug is prescribed 800 mg five times a day (every 4 hours), with a night break. Treatment is continued for 7 days. Patients with reduced immunity (for example, after bone marrow transplantation) or with impaired absorption from the gastrointestinal tract should consider intravenous administration of the drug. Treatment should begin as soon as possible, immediately after symptoms of infection appear. In both chickenpox and herpes zoster, the best treatment results were observed after taking the drug within the first 24 hours of the onset of the rash. Dosing in Children Treatment of Herpes simplex virus infections in immunocompromised patients Children 2 years of age and older should be dosed as in adult patients. Children under two years of age are prescribed half the dose for adults. The dose can be set more precisely, at the rate of 20 mg/kg body weight (up to a maximum dose of 800 mg) four times a day. Treatment should be continued for 5 days. There are no data on the specifics of suppressive therapy for infections caused by herpes simplex virus or chickenpox in children with unimpaired immunity. Dosing in Elderly Patients: In elderly patients, the risk of renal impairment should be considered and the dosage adjusted accordingly (see Use in Patients with Impaired Renal Function). Fluid replacement should be monitored in these patients. Use in patients with impaired renal function Caution is recommended when using acyclovir in patients with impaired renal function. Fluid replacement should be monitored in these patients. During the treatment of infections caused by the herpes simplex virus or the prevention of viral infection in patients with moderate to severe renal failure, the use of recommended oral doses does not lead to the accumulation of acyclovir in the body at concentrations higher than those considered safe during intravenous administration of the drug. However, in patients with severe renal impairment (creatinine clearance less than 10 ml/min), it is recommended to reduce the dose to 200 mg twice daily, every 12 hours. During the treatment of infections caused by the varicella zoster virus and herpes zoster in patients with moderate renal impairment (creatinine clearance 10-25 ml/min), it is recommended to reduce the dose to 800 mg three times a day, every 8 hours, and in patients with severe renal impairment insufficiency (creatinine clearance less than 10 ml/min), it is recommended to reduce the dose to 800 mg twice a day, every 12 hours. If you take a larger dose of the drug than recommended. In case of overdose, you should immediately consult a doctor who will prescribe appropriate treatment. If you miss a dose of your drug If you forget to take a dose of your drug, take it as quickly as possible. However, if it is near time for your next dose of the drug, you should not take the missed dose. Do not take a double dose to make up for a missed dose. Discontinuation of the drug Treatment should not be interrupted, even if the patient does not feel well. Only a doctor can make such a decision. If you have any further doubts regarding the use of the medicinal product, you should consult your doctor or pharmacist.
Use during pregnancy and lactation
In post-marketing trials of medicinal products containing acyclovir, cases of use of acyclovir by pregnant women were noted. The results of these trials did not show an increase in the incidence of malformations in newborns whose mothers took acyclovir compared with the general population. There is no causal relationship between the use of acyclovir by pregnant women and the occurrence of birth defects. Prescribing acyclovir to pregnant women is possible only when the expected benefit to the mother outweighs the potential threat to the fetus. After oral administration of acyclovir at a dose of 200 mg five times a day, its concentration in breast milk ranged from 60% to 410% of the drug concentration determined in blood plasma. Such a concentration of acyclovir in breast milk could lead to the drug reaching the fetus in a daily dose of up to 0.3 mg/kg body weight. Therefore, special care should be taken when using the drug in nursing mothers.
The ability to influence the reaction rate when driving a vehicle or working with other mechanisms
No studies have been conducted on the effect of acyclovir on the ability to drive vehicles and operate machinery. Geviran may cause undesirable effects (for example, headaches or dizziness), which may affect driving and operating moving machinery.
Precautionary measures
Patients taking acyclovir by mouth should receive sufficient fluids. The risk of renal failure increases when used concomitantly with other nephrotoxic drugs. Acyclovir is excreted from the body by the kidneys, so the dose of the drug in people with renal failure should be reduced (see “Dosage and Administration”). In elderly patients, the risk of renal dysfunction should be taken into account, and a dose reduction of the drug should be evaluated in this group of patients. Elderly people and patients with renal failure are at increased risk of adverse effects from the nervous system, and therefore patients in these groups should be carefully monitored. Until now, known symptoms usually disappeared after stopping the drug (see "Side effects"). Long-term treatment with acyclovir or repeated courses of treatment in patients with severe immunodeficiency may lead to the selection of virus strains resistant to acyclovir.
Interaction with other drugs
With the simultaneous use of acyclovir with drugs eliminated by active tubular secretion, an increase in the concentration of active substances or their metabolites in plasma is possible (caution is required when prescribing such combinations). Probenecid and cimetidine increase the AUC of acyclovir and reduce its renal clearance. The combined use of acyclovir and mycophenolate mophenil, an immunosuppressant used in organ transplantation, leads to an increase in the AUC of acyclovir and the inactive metabolite mycophenolate mophenil. However, no adjustment of the acyclovir dosage regimen is required. When acyclovir was administered 1 hour after taking 1 g of probenecid, the half-life and AUC increased by 18 and 40%, respectively. In patients receiving antiretroviral drugs, additional administration of acyclovir did not cause a significant increase in toxic effects. A study conducted in five male patients showed that coadministration of acyclovir with theophylline increased the total AUC of theophylline by approximately 50%. It is recommended to assess the level of theophylline in blood plasma during combined use with acyclovir.
Contraindications
Hypersensitivity to acyclovir or valacyclovir or to other ingredients of the drug.
Compound
One tablet contains: active ingredient: 400 mg of acyclovir excipients: tablet core: microcrystalline cellulose, povidone, sodium starch glycolate, magnesium stearate; tablet shell: hypromellose, macrogol 6000, titanium dioxide (E171), triethyl citrate, talc.
Overdose
Symptoms: acyclovir is only partially absorbed from the gastrointestinal tract. A single dose of acyclovir up to 20 g by a patient usually does not cause toxic symptoms. Sporadic, repeated cases of overdose of oral acyclovir within 7 days have been associated with gastrointestinal symptoms (nausea, vomiting) and neurological symptoms (headache, confusion). In case of an overdose of the intravenous form of the drug, an increase in the level of urea nitrogen and creatinine in the blood and a disorder of renal function were observed. Neurological symptoms, including confusion, hallucinations, agitation, seizures and coma, have also been described with an overdose of the drug in injectable form. Treatment: The patient should be monitored for the development of toxic symptoms. Hemodialysis accelerates the removal of acyclovir from the blood and may be a treatment option in cases of overdose symptoms.
Side effect
Adverse effects are classified according to their frequency of occurrence as follows: very often (? 1/10); often (? 1/100 to
Storage conditions
Store in original packaging to protect from light and moisture, at a temperature not exceeding 25°C. Keep out of the reach of children.
Buy Geviran tablet p/o 800 mg in blister pack. No. 10x3 in the pharmacy
Price for Geviran tablet p/o 800 mg in a pack. №10x3
Instructions for use for Geviran tablet p/o 800 mg in blister pack. №10x3
Application
The drug is intended for external use only.
For children over 12 years of age and adults, Gerpevir ointment is applied 5 times a day at approximately 4-hour intervals, with the exception of night time. It is important to begin treatment as quickly as possible at the onset of infection, preferably during the prodrome or erythema stage. You can start treatment in the later stages - papules or bubbles.
Treatment should continue for at least 4 days. If healing does not occur, treatment can be continued for up to 10 days. If the symptoms of the disease do not disappear after 10 days of treatment, you should consult a doctor. You should wash your hands before and after applying the ointment and avoid excessive rubbing or touching the affected area with a towel to prevent aggravation or transmission of infection.
Gerpevir 2.5% 5 g ointment
Instructions for the use of the drug for specialists GERPEVIR Trade name Gerpevir International nonproprietary name Acyclovir Dosage form Ointment 2.5%, 5 g Composition 1 g of ointment contains the active substance - acyclovir in terms of dry matter 0.025 g, excipients: proxanol 268, propylene glycol, polyethylene oxide 400, emulsifier No. 1. Description Homogeneous ointment of white color, with a slight specific odor Pharmacotherapeutic group Other antimicrobial drugs for external use. Antiviral drugs. Acyclovir. ATC code D06BB03 Pharmacological properties Pharmacokinetics When used externally, it is practically not absorbed into the systemic circulation and does not have a systemic effect. When applying the ointment to the affected area of the skin, a therapeutic concentration of the drug is created in it, which is maintained at a constant level for at least 5 hours. Pharmacodynamics Gerpevir is an analogue of the purine nucleoside deoxyguanidine, a component of DNA (deoxyribonucleic acid). The drug is especially effective against herpes simplex and shingles viruses. The similarity of the structures of herpevir and deoxyguanidine allows it to interact with viral enzymes, which leads to an interruption of the virus reproduction cycle. After herpevir is introduced into a cell affected by herpes, under the influence of thymidine kinase secreted by the virus, it is converted into acyclovir monophosphate. Acyclovir monophosphate is converted by host cell enzymes into acyclovir diphosphate. After which, it is converted into the active form of acyclovir triphosphate, which selectively blocks the synthesis of viral DNA. Acyclovir triphosphate has virtually no effect on DNA replication of the host (human) cell. Herpevir for herpes prevents the formation of new rash elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster. Indications for use: herpetic lesions of the skin and external mucous membranes (herpes of the lips, external genitalia) caused by Herpes simplex viruses types 1 and 2, Varicella zoster - primary and recurrent herpetic infections in patients with immunodeficiency. Directions for use and dosage: For external use only! It is recommended to use rubber gloves or finger caps to prevent the spread of infection. Treatment should be prescribed when the first symptoms of a herpes infection occur. The ointment is applied to the affected skin and external mucous membranes. Before applying the ointment, the affected surface must be washed with soap and water and dried thoroughly. The ointment is applied in a thin layer at the following rate (for adults): a 1.25 cm strip of ointment should be applied to 25 cm2 of the affected area 4-5 times a day and rubbed in with light movements for 1 minute. Children from 3 months. up to 12 years of age, the ointment is applied in a thin layer at the rate of acyclovir 250 mg/m2 of body surface. The ointment should also be applied to areas bordering the affected surface. The ointment must be applied regularly; in cases where you miss the next application, you should not double the dose the next time you use the drug. It is recommended to complete the full course of treatment - 10 days, even if the symptoms of the disease disappear before the specified period. If there is no effect when applied externally, it is recommended to prescribe the drug in tablet form for oral administration. Side effects - burning sensation, mild pain at the site of the lesion, itching - if it comes into contact with the internal mucous membranes, inflammation may develop Contraindications - hypersensitivity to Gerpevir - infectious diseases with similar symptoms, but caused by other pathogens - pregnancy and lactation - children under 3 months Drug interactions Probenecid slows down the elimination of the drug - the half-life is extended. The interaction of Gerpevir with other drugs that are also used topically has not been studied. Special instructions Gerpevir is used as soon as possible after the first symptoms of herpes appear. Protect affected areas from irritation. Avoid sexual intercourse if one of your sexual partners has symptoms of herpes. Do not allow the ointment to come into contact with the mucous membranes of the mouth, nose, eyes, or vagina. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms. Not studied. Overdose Symptoms: erythema, peeling, burning sensation, burns are possible in areas where the ointment is applied for a long time. Treatment: drug withdrawal. Release form and packaging Ointment 2.5%, 5 g in a tube, 1 tube in a cardboard box. Storage conditions Store in a dry place at a temperature from +8 °C to +15 °C. Keep out of the reach of children! Shelf life 3 years Do not use after the expiration date indicated on the package Conditions for dispensing from pharmacies Without a prescription Manufacturer OJSC “Kievmedpreparat” Ukraine, 01032, Kiev, st. Saksaganskogo, 139 tel./fax; 216-14-74.
Side effects
Some patients may experience temporary, rapidly passing sharp or burning pain when using the ointment. In approximately 5% of patients, slight drying and peeling of the skin may occur. Erythema (redness) and itching are also possible in a small proportion of patients. Cases of contact dermatitis have been very rarely reported after topical use of acyclovir preparations, and most often this is associated with components of the ointment base rather than with acyclovir. There are isolated reports of immediate hypersensitivity reactions, including angioedema, due to topical use of acyclovir.
special instructions
The ointment should only be used to treat herpes on the lips and face. It is not recommended to apply the ointment to the mucous membranes of the mouth, eyes, or use it to treat genital herpes. Accidental contact of the ointment with the eyes should be avoided.
Individuals who suffer from particularly severe and recurring manifestations of Herpes labialis need to consult a doctor. Patients with herpes labialis should be warned against contact transmission of the virus to other people, especially if there are open lesions (for example, wash your hands before and after using the ointment). Not recommended for use in immunocompromised patients. Such persons need to consult a doctor regarding treatment of any infection.
During pregnancy and breastfeeding, the drug is recommended to be used only in cases where the benefit, in the opinion of the doctor, outweighs the risk.
Children. There is insufficient data regarding the safety of the drug in children under 12 years of age, therefore it is recommended to use the drug in children over 12 years of age.
The ability to influence reaction speed when driving vehicles and working with other mechanisms. No data.
Gerpevir – capsules, lyophilisate, suspension, tablets
Inside, intravenously.
To prevent relapses of Herpes simplex, patients with immunodeficiency are prescribed 200 mg 4 times a day every 6 hours. In case of severe immunodeficiency (after bone marrow transplantation or in case of impaired absorption from the intestine) - 400 mg 5 times a day.
Children over 6 years old - 800 mg 4 times a day; 2-6 years - 400 mg 4 times a day; under 2 years - 200 mg 4 times a day. More accurately, the dose can be determined at the rate of 20 mg/kg, but not more than 800 mg 4 times a day. The course of treatment is 5 days.
For children from 3 months to 12 years, the dose for intravenous administration is determined based on body area: infections caused by the Herpes simplex virus - 250 mg/sq.m of body surface every 8 hours; reduced immunity, herpetic encephalitis, chickenpox, herpes zoster - 500 mg/sq.m.
Inside. Genital herpes: initial therapy - 200 mg every 4 hours while awake, 5 times a day for 10 days;
recurrent genital herpes (less than 6 episodes per year), intermittent therapy - 200 mg every 4 hours while awake, 5 times a day for 5 days;
recurrent genital herpes (more than 6 episodes per year), long-term suppressive therapy - 400 mg 2 times a day or 200 mg 3-5 times a day.
Herpes simplex of the skin and mucous membranes (treatment): 200-400 mg 5 times a day for 10 days in patients with impaired immunity.
Herpes simplex of the skin and mucous membranes (prevention): 400 mg every 12 hours.
Herpes zoster: 800 mg every 4 hours while awake, 5 times a day for 7-10 days.
Chicken pox: 800 mg 4 times a day for 5 days. Treatment should begin at the earliest signs or symptoms of chickenpox.
For chronic renal failure, dose adjustment is necessary depending on the size of the CK and the required dosing regimen for normal renal function: normal renal function and chronic renal failure with CK more than 10 ml/min - 200 mg every 4 hours, 5 times a day CK less than 10 ml/min - 200 mg every 12 hours;
normal renal function, chronic renal failure with creatinine clearance more than 10 ml/min - 400 mg every 12 hours, with creatinine clearance less than 10 ml/min - 200 mg every 12 hours;
normal renal function, chronic renal failure with CK more than 25 ml/min - 800 mg every 4 hours while awake, 5 times a day, CK 10-25 ml/min - 800 mg every 8 hours, CK less than 10 ml/min - 800 mg every 12 hours
Children under 2 years of age - the dose has not been determined. However, when studying the drug, no unusual toxic effects or specific pediatric problems were identified in children receiving acyclovir in doses of up to 3 g/m2 and 80 mg/kg per day.
Children 2-12 years old, weighing up to 40 kg, with chickenpox: orally, 20 mg/kg, up to 800 mg per dose, 4 times a day for 5 days.
Children 2-12 years old, weighing 40 kg or more, with chickenpox: adult dose.
IV drip (administered at a constant rate for at least 1 hour).
Severe genital herpes, initial therapy: adults and children over 12 years of age - 5 mg/kg every 8 hours for 5 days; children under 12 years old - 250 mg/sq.m every 8 hours for 5 days.
Herpes simplex of the skin and mucous membranes in patients with impaired immunity: adults and children over 12 years old - 5-10 mg/kg every 8 hours for 7 days; children under 12 years old - 250 mg/sq.m every 8 hours for 7 days.
Encephalitis caused by the Herpes simplex virus: adults and children over 12 years of age - 10 mg/kg every 8 hours for 10 days; children from 3 months to 12 years - 20 mg/kg every 8 hours for 10 days.
Herpes zoster in patients with impaired immunity: adults and children over 12 years of age - 10 mg/kg every 8 hours for 7 days; children under 12 years of age - 20 mg/kg every 8 hours for 7 days.
Generalized infection in newborns caused by the Herpes simplex virus: newborns and children under 3 months - 10 mg/kg every 8 hours for 10 days. A dose of 15-20 mg/kg every 8 hours can be used, but the effectiveness and safety of such doses have not been established.
For chronic renal failure in adults and children, a dose reduction and/or change in the interval between administration is required: CC more than 50 ml/min, dose - 100%, interval - 8 hours; CC 25-50 ml/min, dose - 100%, interval - 12 hours; CC 10-25 ml/min, dose - 100%, interval - 24 hours; CC less than 10 ml/min, dose - 50%, interval - 24 hours.
The maximum dose for adults when administered intravenously is 30 mg/kg or 1.5 g/m2/day.
Note!
The description of the drug Gerpevir ointment 2.5% tube 5g on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.