Acyclovir

Ацикловир Drug photo

The description is actual on 23.06.2016

  • Latin name: Aciclovir
  • ATH code: D06BB03
  • Active ingredient: Acyclovir (Aciclovir)
  • Producer: JSC Sintez, JSC Akrikhin, LLC Ozon, LLC Alvils, JSC of Tatkhimfarmpreparata, Altayvitamina's closed joint stock company, JSC Nizhpharm, CJSC Verteks, Belmedpreparata's (Russia) RUP; LLC Astrafarm, CIAO Darnitsa, PAO Farmak, LLC Farmeks of groups (Ukraine)

Structure of the Acyclovir

According to medical Wikipedia the composition of ointment, cream, tablets and injection solution as active ingredient included an anti-virus remedy – an acyclovir (MNN – Aciclovir) in mass part according to a dosage form of drug: 1 gram of ointment – 50 mg; 1 gram of an oculentum – 30 mg; 1 gram of cream – 50 mg; 1 tablet – 200 mg or 400 mg; 1 bottle with lyophilisate – 250 mg, 500 mg or 1000 mg.

Additional ingredients of medicines can differ depending on manufacturing plant.

Release form

The medicine Acyclovir is made in shape:

  • tablets No. 10-100;
  • lyophilisate in bottles No. 1;
  • ointment and cream in tubas on 2-30 grams;
  • oculentum in tubas on 2-5 grams.

Pharmacological action

Anti-virus (antiviral).

Pharmacodynamics and pharmacokinetics

The official summary to the drug Acyclovir carries its active ingredient to group of the anti-virus (anti-herpetic) remedies which are synthetic analogs of the purine nucleoside possessing ability to oppression of replication of virus strains of Varicella zoster (chicken pox, shingles), a cytomegalovirus, Epstein-Burra's virus and the 1st and 2nd type of the Herpes simplex virus (herpes simplex).

In the infected cells including virus enzyme a thymidinekinase owing to process of phosphorylation there is a transformation of an acyclovir to a monophosphate form. Then consistently under the influence of guanylate cyclase monophosphate passes into a form of diphosphate and further, under the influence of some cellular enzymes, into a triphosphate form. As for thymidinekinase enzyme in the healthy, not infected with a virus cells the acyclovir is not substrate, his sharp selectivity of influence directly in relation to viruses and insignificant toxicity for other cells of a human body is shown.

For this time three mechanisms of the inhibiting influence of drug in the form of triphosphate on replication of virus DNA which consist are known: in competitive substitution of a deoxyguanosine of triphosphate in the course of synthesis of DNA; in implementation in a synthesizable DNA chain and the termination of its lengthening; in suppression of virus enzyme of a DNA polymerase. These processes in a human body are resulted by blocking of further replication of a virus. High specificity and selectivity of effect of active ingredient of medicine are caused also by its preferential cumulation in the cells infected with a virus.

Use of drug at a herpes infection prevents emergence of fresh elements of rash, reduces probability of development of visceral complications and skin dissimination, accelerates formation of external crusts, reduces pain in an acute phase of treatment of shingles. Also some immunopromoting effect is observed.

The tablets Acyclovir after oral administration are soaked up in intestines only partially. Drug absorption, because of its low lipophilicity, happens on average for 20% from what the tablets Acyclovir possess bioavailability within 15-30%. Nevertheless, it is quite enough such concentration of a remedy for effective fight against viral infections. In parallel the eaten food practically does not influence absorption processes. At increase in a dosage decrease in bioavailability is noted.

At oral daily administration of 1000 mg (5 times on 200 mg) Cmax indicator observed after 1,5-2 hours is equal to 0,7 mkg/ml, the indicator of Cmin is at the level of 0,4 mkg/ml. Linkng with serum proteins varies within 9-33%. The entered acyclovir in/in (intravenously) or orally (inside) passes through a blood-brain barrier and a placenta. In medical concentration gets into fabrics/bodies of a human body, including: brain, intestines, muscles, liver, spleen, lungs, uterus, kidneys, the lacrimal liquid, breast milk, watery moisture, sperm, secret and mucous vaginas, amniotic liquid, herpetic bubbles. It is found in cerebrospinal fluid twice of smaller concentration, than in plasma. At reception of 1000 mg a day the content of drug in breast milk is in limits of 0,6-4,1% of serumal level that assumes receiving medicine about 0,3 mg/kg by the baby of a daily dose.

Metabolic transformations of active ingredient happen in a liver to forming of the main product of a metabolism – a 9-karboksimetoksimetilguanina. By means of canalicular secretion, and also glomerular filtering it is excreted by kidneys for 62-91% in not changed form and approximately for 14% in the form of a 9-karboksimetoksimetilguanin. Intestines remove less than 2% of drug, by lungs only its trace quantities.

When carrying out one-time 6 hour sessions of a hemodialysis about 60% of active ingredient of drug are filtered, at a peritoneal dialysis of considerable change of its clearance it is not observed.

At oral administration of T1/2 takes about 3,3 hours adult patients, at in introduction about 2,5 hours. At children till 18 years of T1/2 it is equal about 2,6 hours. With age the speed of excretion is slowed down, but at this T1/2 increases slightly.

At chronic insufficiency of renal function of difficult character of T1/2 can reach 20 hours. Depending on CC (clearance of creatinine) at adult patients with a renal failure of T1/2 it is on average equal: KK of 50-80 ml/min. – 3 hours; KK of 15-50 ml/min. – 3,5 hours; a condition of an anury – 19,5 hours; carrying out a hemodialysis – 5,7 hours; an out-patient constant peritoneal dialysis – 14-18 hours.

Ointment the Acyclovir and cream the Acyclovir when drawing on the intact (unimpaired) integuments actually are not soaked up. Active ingredient of local dosage forms of this drug, as well as products of its metabolism, are not defined in serum and urine. At application of outside forms of drug on structurally changed/affected skin moderate absorption of ingredients of cream and ointment the Acyclovir is observed from what their quantity after all gets into a blood plasma and in the subsequent into urine.

At patients with normal renal function the indicator of serumal Cmax of drug is equal to about 0,28 mkg/ml, at patients with HPN the plasma content of active ingredient reaches values to 0,78 mkg/ml.

About 9,4% of a daily dosage are excreted by kidneys.

The oculentum the Acyclovir easily overcomes a corneal epithelium and creates the therapeutic level of drug in intraocular liquid. At the moment methods of definition of active ingredient of this medicine in the form of an oculentum in blood serum do not exist. Small concentration of drug is defined only in urine and therapeutic is not significant.

Indications to use

The tablets Acyclovir Acre (Akos, Nizhpharm) and other producers, as well as lyophilisate (for example, Belmedpreparata's productions), are shown to appointment for the purpose of prevention and/or therapy of primary, secondary and recurrent infectious painful states provoked by virus strains of I and II Herpes simplex types (herpes simplex) including its genital form, and Varicella zoster strain (shingles and chicken pox). System use of these dosage forms of drug can practice as concerning patients with normal immunity, and patients with an immunodeficiency, including HIV infection and post-transplant states.

Gel and ointment (Acre, Synthesis, Ozone, Vertexum and so forth) use the Acyclovir outwardly at treatment (most often complex) the skin herpetic rashes provoked by strains of I and II types of a herpes simplex (including its genital form), and also at therapy of external displays of shingles and chicken pox.

The oculentum is applied to treatment of the herpetic keratitis provoked by strains of I and II types of a herpes simplex (it is previously possible to use cleaning drops for eyes).

Contraindications

Contraindications to purpose of tablets, lyophilisate and all outside forms of drug include: personal hypersensitivity of the patient to active ingredient or additional components of a dosage form; personal hypersensitivity to Valatsiklovir; age till 2 years (for tablets); feeding by a breast (for lyophilisate and tablets).

Pregnant women and the feeding women need careful use of outside forms of a remedy; peroral and injection forms – pregnant women, patients with neurologic disturbances, insufficiency of renal function (a possibility of nephrotoxic influence), dehydration, the neurologic response to reception of cytotoxic drugs (including references in the anamnesis).

Side effects

The tableted dosage forms of drug in certain cases can cause the following side effects:

Injection dosage forms of drug sometimes led to development of such by-effects:

  • nausea/vomiting;
  • renal failure (acute);
  • the encephalopathy (which is shown drowsiness, confusion of consciousness, psychosis, hallucinations, a tremor, excitement, spasms and even a coma);
  • crystalluria;
  • medicinal allergy (hypersensitivity reaction);
  • inflammation, phlebitis around introduction.

Outside dosage forms of drug (cream, ointment) occasionally became an origin:

  • erythema;
  • burning sensations;
  • peelings;
  • skin rash / itch;
  • xeroderma;
  • inflammations (at accidental drawing on mucous).

Local dosage forms of drug (oculentum) in some cases could cause:

Application instruction of the Acyclovir (Way and dosage)

Tablets Acyclovir, application instruction

The instruction on the tablets Atsiklovir-Akos, as well as the instruction on the tablets Acyclovir Acre, and also other producers, recommends reception peroral (inside) of the tableted drug forms together with water (200-250 ml) right after food or during meal. Purpose of daily dosages similar to doses for adult patients is shown to children after 2 years weighing more than 40 kilograms.

Therapy of a herpes simplex of mucous membranes and integuments usually assumes 5 one-time daily reception of 200 mg of drug (for example, the tablets Atsiklovir-Akos) patients with the normal immune status or 400 mg (for example, the tablets Acyclovir Acre) patients with an immunodeficiency for 5-10 days.

Prevention of a herpes simplex of mucous membranes and integuments, as a rule, takes place 400 mg (for example, the Acyclovir of Herd of 400 mg) accepted each 12 hours in tablets.

Treatment of uncomplicated genital herpes on average takes 10 days with peroral 5 multiple (each 4 hours) daily reception of tablets in a dose of 200 mg (for example, Atsiklovir-Akos).

Discontinuous therapy of recurrent genital herpes (it is less than 6 recurrence in a year) assumes to 5 multiple (each 4 hours) daily reception of 200 mg of drug for 5 days.

Prolonged overwhelming treatment of recurrent genital herpes (it is more than 6 recurrence in a year) means reception of 400 mg of drug, 2-times a day (for example, the tablets Acyclovir Forte) or 3-5 one-time reception in days of 200 mg of medicine.

Therapy of the surrounding herpes takes from 7 to 10 days with 5 multiple daily internal reception of 800 mg of drug in the form of tablets.

Treatment of chicken pox (chicken pox) is carried out for 5 days with 4-times daily reception of 800 mg of medicine. It is necessary to start such treatment at detection of the earliest symptoms or symptoms of a disease. 4-fold daily administration of drug in a dose of 20 mg on kilogram of weight is shown to children since 2 years weighing up to 40 kilograms.

Therapy of patients with HPN has to take place in the reduced dosages depending from CC (clearance of creatinine) in this connection before accepting drug it is necessary to establish the size of this indicator in accuracy. At treatment of herpetic defeats at patients with KK less than 10 ml/min. reduce a daily dose to 400 mg, with reception on 200 mg in 12 hours. At therapy of the diseases provoked by Varicella zoster less than 10 ml/min. recommend to patients with KK 2-times daily reception of 800 mg of drug; with KK of 10-25 ml/min. – 3-fold reception of a similar dose.

Lyophilisate the Acyclovir in/in, the application instruction

Remedy lyophilisate (for example, Belmedpreparata) is intended for cultivation and further use in the form of infusions.

Depending on the diagnosed viral infection and its weight to patients is more senior than 12 years it is shown in/in drop introduction of 5-10 mg on kilogram of weight with an interval at 8 o'clock. It is necessary to carry out to injection for at least 60 minutes. As much as possible in days patients of this age category can appoint 30 mg of drug to kilogram of weight.

To children of 3 months, as a rule, appoint each 8 hours infusional introduction of 250 mg (herpetic defeats by Herpes simplex strain) or 500 mg (reduced immunity, chicken pox, herpetic encephalitis, shingles) of a remedy at the rate on square meter of a body surface. The dosage for newborns is calculated according to their weight and makes 10 mg on kilogram of weight, with the same frequency of infusional injections (in 8 hours).

For therapy of a herpes simplex of mucous membranes and integuments at patients with reduced immunity for 7 days enter kapelno each 8 hours 5-10 mg on kilogram of weight the patient after 12 years or on 250 mg on square meter of a body to children till 12 years.

At treatment of heavy genital herpes as initial therapy appoint for 5 days of infusion each 8 hours 5 mg to kilogram of weight the patient after 12 years or on 250 mg on square meter of a body to children till 12 years.

Therapy of the encephalitis provoked by a virus strain of Herpes simplex takes place within 10 days with infusional introduction each 8 hours 10 mg on kilogram of weight by the patient after 12 years or on 20 mg on kilogram of weight to children till 12 years.

Treatment of the surrounding herpes with the suppressed immunity on average takes 7 days patients with in/in drop injection each 8 hours on 10 mg on kilogram of weight by the patient after 12 years or on 20 mg on kilogram of weight to children till 12 years.

When diagnosing HPN at patients of adult and children's age according to CC (clearance of creatinine) adjustment (towards decrease) the dosing mode and/or change (towards increase) an interval between carrying out infusions is necessary. So at KK of 25-50 ml/min. appoint the full-fledged dose of drug entered in 12 hours; at KK of 10-25 ml/min. – the full-fledged dose of drug entered in 24 hours; at KK it is less than 10 ml/min. – the vague dose entered in 24 hours.

Cream and ointment Acyclovir, application instruction

The application instruction the Acyclovir (Acre, Nizhpharm, Sandoz and so forth) in the form of cream or ointment assumes use of these drugs exclusively outwardly for what ointment the Acyclovir or cream of this remedy is shown to be applied on the infected skin sites with frequency of 5 times a day (every 4 hour).

Cream and ointment the Acyclovir (Geksal, Acre and so forth) should apply on the skin sites infected and adjoining on them with a thin layer, using for this purpose the fingers of hands (which are previously cleared and washed up) or a pure cotton plug. Cream and ointment the Acyclovir (Farmak, Synthesis, Ozone and so forth) need to be applied throughout time sufficient for formation of an external crust on herpetic bubbles or up to their full healing. Duration of such treatment, as a rule, borrows from 5 to 10 (at most) days. The fastest disposal of external displays of a disease depends on time of the beginning of therapy. The best results were shown by the treatment which is carried out from the first signs of the beginning of an infection or from a prodromal phase of its development.

Oculentum, application instruction

For therapy of a herpetic keratitis at adults and children use an oculentum in the form of small (length about 1 centimeter) the strip put by the finger (which is previously cleared and washed up) in the lower conjunctival sac with frequency of 5 times at 24 o'clock (usually every 4 hour) up to full healing and on an extent of 3 days after it.

Overdose

Episodes of overdose can arise at use of peroral or injection dosage forms, and also in case of a proglatyvaniye of outside forms of drug.

The negative symptomatology of overdose at excessive oral administration of a remedy is characterized: spasms, agitation, lethargy, coma. Precipitation of active ingredient of tablets in renal tubules, in case of exceeding of content of drug (2,5 mg/ml) in comparison with its solubility in renal tubules is possible.

At in introduction of the overestimated doses the following manifestations of overdose can be observed: giperkreatininemiya, increase in an urea nitrogen, disturbance of renal function, spasm, lethargy, coma.

In case of a proglatyvaniye of outside forms of drug noted: neurologic disturbances, headaches, short wind, spasms, nausea/vomiting, lethargy, diarrhea, disturbance of renal function, to whom.

Therapy of all above-stated painful states consists in control/support of the vital systems / bodies of an organism and purpose of a symptomatic treatment, including carrying out a hemodialysis.

Interaction

At parallel use of immunostimulators strengthening of efficiency of drug is observed.

The combined appointment with probenetsidy promotes reduction of canalicular secretion of an acyclovir that leads to increase of its serumal maintenance and lengthening of T1/2.

The combination therapy with use of a mikofenolat of a mofetil can become the reason of increase of AUC of an acyclovir, and also an inactive product of a metabolism of a mikofenolat of a mofetil.

Combined use with nephrotoxic remedies strengthens nephrotoxic effects, in particular at patients with the broken renal function.

At cultivation of lyophilisate it is necessary to take in attention alkali reaction (rn 11) this dosage form of drug.

Simultaneous use with a zidovudine at treatment of HIV-positive patients did not reveal any significant changes of pharmacokinetic characteristics of both medical drugs.

Terms of sale

Acquisition of tablets and lyophilisate demands presentation the recipe in Latin. Cream and ointment of drug are in free sale.

Storage conditions

All dosage forms of drug keep the medicinal properties at a surrounding temperature to 25 °C.

Period of validity

3-4 years depending on the producer and a dosage form.

Special instructions

Do not recommend to appoint the Acyclovir to patients with heavy pathologies of kidneys.

During therapy it is necessary to take into account possibility of acute insufficiency of kidneys owing to forming of a deposit from crystals of active ingredient of drug. The probability of development of this complication amplifies in case of a remedy, fast in/in introductions of an injection form, parallel reception of nephrotoxic drugs, and also at patients with the broken renal function or dehydration.

At all stage of use of the Acyclovir it is necessary to control renal functionality, defining serumal concentration of creatinine and urea.

Therapy of elderly patients, because of increase in drug T1/2 at them, should be carried out under supervision of the specialist doctor and at adequate increase of water loading.

Outside dosage forms of drug (cream and ointment) should not be applied on mucous membranes of an oral cavity, a vagina, organs of sight.

Before accepting the Acyclovir from herpes it is necessary to establish what better a route of administration of this medicine for treatment of this or that herpetic defeat. To find out in each separate case that ointment is better or tablets will be suitable for therapy of the diagnosed infection.

More effective and fast treatment of herpes on lips the Acyclovir takes place if in parallel to use cream or herpes ointment and herpes pills on lips, at the same time it is necessary to take place consultation at the doctor and to precisely learn how to drink HP at herpes on a lip and how to apply cream or ointment.

At genital herpes patients should abstain from sexual contacts or to use condoms as carrying out treatment does not prevent possible infection of the sexual partner.

The acyclovir at chicken pox is most often applied for the purpose of therapy of this disease and its prevention at adults and children with an immunodeficiency. Responses of doctors say that treatment of chicken pox at adults and children is effective at purpose of drug in the first 24 hours after detection of external rashes.

The acyclovir at chicken pox at adults and children with normal immunity, at its appointment at later stages of development of a disease, did not lead to any simplification of negative symptomatology. Cream or ointment the Acyclovir at chicken pox can be used as supportive outside application for decrease in external displays of chicken pox (rash).

Analogs of the Acyclovir

Analogs of peroral and parenteral forms of drug with similar ativirusny action, but excellent active ingredient (including capsules, tablets, injection solution), are provided by remedies:

The price of analogs considerably differs depending on the producer of this or that drug, its dosage form, quantity of medical units (a tablet, a capsule, an ampoule) and mass contents in them active ingredient. For example, 30 tablets of Ribavirin on 200 mg can be bought on average for 300 rubles, and 10 tablets of Famvir on 250 mg for 1500 rubles.

What is Valtreks or the Acyclovir better?

Considering these two drugs of analog it is necessary to pay attention that Valtreks with active ingredient – valatsiklovir was created much later the predecessor and for the purpose of overcoming of the forming resistance of herpes infections to the Acyclovir. The mechanism of effect of both drugs is almost identical, contraindications to their use identical, possible side effects are similar, and here cost differs very significantly. Today the price of 10 tablets of Valtreks in tens of times exceeds the price of the next analog and averages 1200 rubles. Proceeding from the aforesaid and considering a financial position of most of the population in the territory of the former Soviet Union, Valtreks's appointment can be justified only in case of total absence of the response of an organism of the patient to the carried-out treatment with use of the Acyclovir.

Analogs of outside dosage forms of drug (cream, ointment):

Analogs of a local dosage form (oculentum):

Zdravzona

  • Belupo's acyclovir of 5% cream 10gbelupo
  • Belupo's acyclovir of 5% cream 5gbelupo
  • Belupo's acyclovir of 400 mg No. 35 tabletkibelupo
  • Belupo's acyclovir of 5% cream 2gbelupo
  • Acyclovir of 5% ointment 5 of/Vertexum/Vertexum of closed joint stock company

Drugstore of IFC

  • Acyclovir Sandoz tbl 200 mg No. 25, Salutas Pharmagermaniya
  • Atsiklovir-Akrikhin ointment of 5% 5 g *, HFK (г.Москва) Russia Quinacrine
  • Acyclovir Sandoz cream of 5% 5 g, Salutas Pharmagermaniya
  • Acyclovir Sandoz cream of 5% 2 g, Salutas Pharmagermaniya
  • Atsiklovir-Akrikhin tbl 400 mg No. 20, HFK (г.Москва) Russia Quinacrine
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Apteka24

  • Atsiklovir20
  • Acyclovir cream of 5% 5 g tubafarmak (Ukraine, Kiev)
  • No. 20darnitsa tablet 0.2g acyclovir (Ukraine, Kiev)
  • No. 20farmak tablet 0.2g acyclovir (Ukraine, Kiev)
  • No. 20lekhim-Kharkiv mg tablet 200 acyclovir (Ukraine, Kharkiv)

Paniapteka

  • Ointment atsiklovir-ZhFF 2.5% 10 g of a tube

BIOSPHERE

  • Acyclovir of 5% 10 g ointment in a tuba
  • Atsiklovir-AKOS 200 mg No. 20 of table. Synthesis of joint stock company (Russia)
  • Atsiklovir-AKOS 5% 5 g ointment in a tuba
  • Acyclovir of 3% 5 g ointment glazn.
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Section: Dermatological Antiviral
in more detail

Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use the Acyclovir surely consult with the attending physician.