Geviran

General characteristics. Structure:

Active agent: acyclovir of 200 mg

Other ingredients: K30 povidone, sodium krakhmalglikolit, cellulose microcrystallic, magnesium stearate, a gipromelloz, triethyl citrate, talc, titanium dioxide, a macrogoal 6000.

Active agent: acyclovir of 400 mg

Other ingredients: K30 povidone, sodium krakhmalglikolit, cellulose microcrystallic, magnesium stearate, a gipromelloz, triethyl citrate, talc, titanium dioxide, a macrogoal 6000.

Active agent: acyclovir of 800 mg

Other ingredients: K30 povidone, sodium krakhmalglikolit, cellulose microcrystallic, magnesium stearate, a gipromelloz, triethyl citrate, talc, titanium dioxide, a macrogoal 6000.

Pharmacological properties:

Pharmacodynamics. The acyclovir is a synthetic analog of a purine nucleoside which in vitro and in vivo suppresses replication of Herpes group viruses, pathogenic for the person: Herpes simplex (HSV) I and II of type and Varicella Zoster (VZV) virus.
Action of an acyclovir concerning braking of replication of the specified viruses is very selective. In not infected cells the acyclovir is not used as substrate of an endogenous thymidinekinase (shopping mall) therefore toxic action on cells of mammals is insignificant. However the shopping mall of a virus origin, coded by the HSV and VZV viruses, phosphorylates an acyclovir in derivative monophosphate (a nucleoside analog) which then is phosphorylated with participation of cellular enzymes in di - and трифосфатацикловир. Trifosfatatsiklovir is substrate for a virus DNA polymerase which builds in it virus DNA, completing thus synthesis of a chain of virus DNA and suppresses its replication.
Prolonged use of an acyclovir or repeated courses of treatment of patients with the expressed immunodeficiency can cause emergence of virus strains, resistant to an acyclovir. In the majority of the allocated strains with reduced sensitivity reveal deficit of shopping mall, but also strains with shopping mall or the DNA polymerase changed virus are described. In the researches in vitro ability of formation of strains of HSV with reduced sensitivity is also revealed. Dependence between sensitivity of a virus of herpes to an acyclovir, certain in vitro, and the clinical response to treatment is unknown.

Pharmacokinetics. The acyclovir is partially soaked up in a GIT. In an equilibrium state average maximum concentration (CSSmax) after administration of drug in a dose of 200 mg each 4 h makes 3,1 µmol/l (0,7 mkg/ml), and the corresponding minimum concentration (CSSmin) makes 1,8 µmol/l (0,4 mkg/ml). After administration of drug in doses of 400 and 800 mg each 4 h CSSmax 5,3 µmol/l (1,2 mkg/ml) and 8 µmol/l (1,8 mkg/ml), and CSSmin — 2,7 µmol/l (0,6 mkg/ml) and 4 µmol/l (0,9 mkg/ml) respectively make.
After introduction of an acyclovir adult T½ makes about 2,9 h of a blood plasma. The most part is removed with urine in not changed look. The renal clearance of an acyclovir is much higher in comparison with clearance of creatinine that indicates participation of canalicular secretion in the presence of glomerular filtering in removal of drug with urine. The most significant metabolite of an acyclovir is 9-karboksimetoksimetilguanin which is removed with urine in number of about 10-15% of the entered dose.
Reception of 1 g of a probenitsid in 60 min. prior to introduction of an acyclovir extends acyclovir T½ for 18%, and AUC in a blood plasma increases by 40%.
At adult CSSmax after 1-hour infusion of an acyclovir in doses 2,5; 5 and 10 mg/kg of body weight made 22,7 µmol (5,1 mkg/ml), 43,6 µmol (9,8 mkg/ml) and 92 µmol (20,7 mkg/ml). CSSmin in 7 h made 2,2 µmol (0,5 mkg/ml), 3,1 µmol (0,7 mkg/ml) and 10,2 µmol (2,3 mkg/ml). When to children aged from 1 year instead of a dose at the rate of 5 mg/kg of body weight entered a dose of 250 mg/sq.m, and instead of a dose of 10 mg/kg of body weight appointed a dose of 500 mg/sq.m, CSSmax and CSSmin values were similar to those which are noted at adults. At newborns and children aged up to 3 months to which each 8 h by 1-hour infusion of CSSmax entered an acyclovir in doses of 10 mg/kg of body weight made 61,2 µmol (13,8 mkg/ml), and CSSmin — 10,1 µmol (2,3 mkg/ml).
Medicine T½ makes 3,8 h of a blood plasma.
At patients of advanced age the general clearance of an acyclovir decreases with clearance of creatinine though change of T½ from a blood plasma are insignificant.
At patients with HPN T½ of an acyclovir makes 19,5 h T½ of an acyclovir during a hemodialysis makes 5,7 h. Concentration of drug in a blood plasma during dialysis decreases by 60%.
Concentration of an acyclovir in SMZh makes about 50% of level in a blood plasma. Linkng of an acyclovir with proteins of a blood plasma insignificant (9–33%) therefore competitive replacement of an acyclovir from places of binding is noted by other drugs.

Indications to use:

• treatment of viral infections of skin and the mucous membranes caused by a herpes simplex virus including primary and recurrent genital herpes;
• prevention of a recurrence of the infections caused by a herpes simplex virus in patients with normal immunity;
• prevention of the infections caused by a herpes simplex virus in patients with an immunodeficiency;
• treatment of the infections caused by the VZV virus (chicken pox and the surrounding herpes);
• prevention and treatment of the infections caused by a herpes virus in patients with a heavy immunodeficiency namely: with the developed HIV infection stage (quantity of CD4+ <200/mm3, including the patients sick with AIDS or with the AIDS-associated complexes) and after transplantation of marrow.

Route of administration and doses:

Treatment of the infections caused by a virus of a herpes simplex (HSV)
It is necessary to accept drug on 200 mg of 5 times a day (approximately each 4 h) with a break for the night. Drug is accepted by 5 days, at heavy primary infections the course of treatment can be prolonged up to 10 days.
At patients with reduced immunity (for example after transplantation of marrow) or disturbances of absorption in a GIT the dose can be doubled to 400 mg.
Reception of an acyclovir should be begun immediately, right after establishment of the diagnosis. At recurrent infections it is very important to begin administration of drug in a prodromal stage or right after emergence of the first symptoms of a disease.
Prevention of a recurrence of a herpes simplex (HSV) at patients with normal immunity
To patients with normal immunity to accept drug on 200 mg 3–4 times a day approximately each 6–8 h.
For many patients use of drug in a dose of 400 mg 2 times a day each 12 h is effective.
With the preventive purpose effectively gradual dose decline to 200 mg 3 times a day (each 8 h) or even 2 times a day (each 12 h).
At some patients the response to preventive use of drug appears after use of a daily dose of 800 mg.
Drug should be used with breaks every 6-12 month, watching possible changes during a disease.
Duration of preventive use is determined by the doctor depending on the course of a disease and individual sensitivity of the patient.
Prevention of the infections caused by a herpes simplex virus
For prevention of the infections caused by a herpes simplex virus at patients with an immunodeficiency of a tablet of 200 mg it is necessary to accept 4 times a day each 6 h. At patients with a considerable immunodeficiency (for example after transplantation of marrow) or at patients with reduced absorption in intestines it is possible to double a dose to 400 mg or to apply the corresponding dose for in/in introductions.
Duration of preventive use is determined by the doctor depending on the course of a disease and individual sensitivity of the patient.
Treatment of the infections caused by a virus of chicken pox and the surrounding herpes
It is necessary to accept drug on 800 mg of 5 times a day (approximately each 4 h) with a break for the night. Duration of treatment makes 7 days.
At patients with reduced immunity (for example after transplantation of marrow) or disturbances of absorption in a GIT it is possible in/in administration of drug.
Treatment should be begun immediately, right after establishment of the diagnosis. Treatment at chicken pox and the surrounding herpes is effective if to begin administration of drug right after emergence of the first rashes.
Prevention and treatment of the infections caused by a herpes virus in patients with a considerable immunodeficiency
For treatment of patients with a considerable immunodeficiency it is necessary to accept 800 mg 4 times a day with approximately 6-hour interval. Geviran within a month has to precede treatment of patients after transplantation of marrow in/in therapy by drug.
Duration of treatment of patients after transplantation of marrow makes 6 months (from 1 to 7 month after transplantation). At patients with the developed HIV infection stage the course of treatment makes 12 months, for preservation of positive effect it is desirable to continue a course of treatment.

Children
Treatment of the infections caused by a virus of a herpes simplex (HSV)
To children at the age of 2 years is also more senior to appoint doses, as for adults.
Treatment of the infections caused by a virus of chicken pox
To children aged from 2 up to 6 years: 400 mg 4 times a day.
To children 6 years are aged more senior: 800 mg 4 times a day.
The dose can be defined more precisely at the rate of 20 mg/kg of body weight (to the maximum dose of 800 mg) 4 times a day. Duration of treatment makes 5 days.
Recrudesced about prevention of the infections caused by a virus of a herpes simplex and the surrounding herpes at children with normal immunity is not present.
Patients of advanced age
At patients of advanced age it is necessary to consider renal failures and, respectively, to change a dose. It is necessary to control the level of hydration of an organism.
Patients with a renal failure
It is necessary to apply with care an acyclovir at patients with a renal failure and to watch the adequate level of hydration of an organism.
At treatment of the infections caused by a herpes simplex virus, or prevention of a viral infection with a moderate or heavy renal failure use of the recommended peroral doses does not cause accumulation of an acyclovir in an organism in concentration in patients above those which are considered safe for administration of drug. However the patient with a heavy renal failure (clearance of creatinine <10 ml/min.) 2 times a day each 12 h recommend to establish a dose to 200 mg.
At treatment of the infections caused by a virus of chicken pox and the surrounding herpes at patients with a moderate renal failure (clearance of creatinine of 10-25 ml/min.) recommend to establish a dose to 800 mg 3 times a day each 8 h, and at patients with a heavy renal failure (clearance of creatinine <10 ml/min.) 2 times a day each 12 h recommend to lower a dose to 800 mg.

Features of use:

The acyclovir is brought out of an organism with urine therefore at patients with a renal failure the dose of drug should be lowered. At elderly people it is necessary to consider a possible renal failure, at such patients it is necessary to consider a possibility of a dose decline of drug. Elderly people and patients with a renal failure treat group of the increased risk of development of side effects from a nervous system therefore it is necessary to watch a condition of patients of this category carefully. Symptoms known now usually disappeared after the reception termination.
Use during pregnancy and feeding by a breast. In post-market researches of the medicines containing an acyclovir it was reported about cases of use of an acyclovir for pregnant women and emergence of disturbances in them. By results of these researches, increase in frequency of emergence of anomalies of development of newborns which mothers accepted an acyclovir in comparison with the general population it is not revealed. Relationship of cause and effect between reception of an acyclovir by pregnant women and developing of inborn malformations at newborns is not revealed.
It is necessary to appoint an acyclovir pregnant only when the expected advantage for mother exceeds potential risk for a fruit.
It is necessary to appoint drug to women during feeding a breast with extra care, taking into account risk for the child.
Children. At children under 2 years drug in this dosage form is not applied.
Ability to influence speed of response at control of vehicles or work with other mechanisms. Researches concerning drug influence Geviran on ability to control of vehicles and work with mechanisms were not conducted. Considering possible emergence of side effects, it is necessary to be careful at control of vehicles and work with other mechanisms.

Side effects:

Side effects are classified by the frequency of manifestations as follows: very often (≥1/10); often (≥1/100, <1/10); infrequently (≥1/1000, <1/100); seldom (≥1/10 000, <1/1000); very seldom (<1/10 000).
From system of blood and lymphatic system: very seldom — anemia, reduction of quantity of leukocytes, thrombocytopenia.
From immune system: seldom — anaphylactic reactions.
From mentality and nervous system: often — a headache, dizziness; very seldom — excitement, confusion of consciousness, a tremor, an ataxy, a dysarthtia, hallucinations, psychotic symptoms, spasms, drowsiness, encephalopathy, a coma.
These symptoms usually passing also arise preferential at patients with a renal failure or other contributing factors.
From respiratory system, bodies of a thorax and a mediastinum: seldom — suffocation.
From a GIT: often — nausea, vomiting, diarrhea, an abdominal pain.
From a liver and biliary tract: seldom — temporary increase in level of bilirubin and increase in activity of hepatic transaminases in blood; very seldom — hepatitis, jaundice.
From skin: often — an itch, rash (also hypersensitivity to light); infrequently — a small tortoiseshell, a generalized alopecia. As many diseases and use of various medicines can be the cause of emergence of a generalized alopecia, its emergence at reception of an acyclovir is not defined. Seldom — vasculomotor hypostasis.
From kidneys: seldom — increase in level of creatinine and urea in a blood plasma; very seldom — OPN, pain in kidneys.
Pain in kidneys can be connected with a renal failure.
It is necessary to control a condition of hydration of the patient. Renal failures usually quickly disappear after completion of level of liquid in an organism of the patient and/or a dose decline or drug withdrawal. In exceptional cases there can be OPN.
The general disturbances and states in an injection site: often — fatigue, fervescence.

Interaction with other medicines:

Clinically significant medicinal interaction is not revealed.
The acyclovir is removed preferential in not changed look by active removal in renal tubules. At the same time accepted drugs which are transformed in an organism in the same way can become the reason of increase in concentration of an acyclovir in a blood plasma. Probenetsid and Cimetidinum increase AUC of an acyclovir and reduce its renal clearance. Similar growth in a blood plasma of level of an acyclovir and an inactive metabolite — a mikofenolata of a mofetil, an immunosuppressant which is applied at patients after transplantation, was noted at a concomitant use of these medicines. However, considering the broad therapeutic range of an acyclovir, there is no need for change of a dose.

Contraindications:

Hypersensitivity to an acyclovir, a valatsiklovir or other components of drug.

Overdose:

Symptoms: the acyclovir is partially soaked up in a GIT. The single dose to 20 g of an acyclovir usually does not cause emergence of symptoms of poisoning. In some cases overdoses of an acyclovir for oral administration within 7 days appeared symptoms from a GIT (nausea, vomiting) and a nervous system (a headache, confusion of consciousness).
Neurologic symptoms, such as confusion of consciousness, hallucinations, excitement, spasms and coma, are also described at overdose at use of an injection form of drug.
Treatment: it is necessary to watch the patient concerning emergence of symptoms of poisoning. Symptomatic treatment. The hemodialysis accelerates removal of an acyclovir from blood, and it can be applied in case of symptoms of overdose.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. п / captivity. cover of 200 mg blister, No. 30
Tab. п / captivity. cover of 400 mg blister, No. 30
Tab. п / captivity. cover of 800 mg blister, No. 30.