Agapurin

Агапурин Drug photo

The description is actual on 02.02.2016

  • Latin name: Agapurin
  • ATH code: C04AD03
  • Active ingredient: Pentoksifillin
  • Producer: Zentiva a.s (Slovak Republic)

Structure

1 tablet includes 100 mg of a pentoksifillin.

In addition (together with a cover): anhydrous colloid silicon, karmeloz of sodium, monohydrate of lactose, methylparaben, corn starch, talc, acacia gum, magnesium stearate, crystal and powdery sucrose, titanium dioxide.

1 tablet WEDNESDAY includes 400 mg or 600 mg of a pentoksifillin.

In addition (together with a cover): gipromelloza, talc, macrogoal 6000, magnesium stearate, povidone 40, sepifilm 752 white, emulsion of a dimetikon.

1 ml of injection solution includes 20 mg of a pentoksifillin.

In addition: water for infection, sodium chloride.

Release form

Drug Agapurin is made in the form of tablets, on 60 pieces in glass bottles; in the form of tablets retard (WEDNESDAY), on 20 pieces in secondary packaging; in the form of solution for injections, in ampoules on 5 ml No. 5 in a box.

Pharmacological action

Anti-aggregation, vasodilating, improving microcirculation.

Pharmacodynamics and pharmacokinetics

Agapurin is a spasmolytic remedy and treats group of purines. Action of a pentoksifillin is directed to improvement of rheological qualities of blood and strengthening of microcirculation. Efficiency of a pentoksifillin is shown thanks to its ability to suppression of phosphodiesterase and increase in concentration of ATP in erythrocytes and tsAMF in thrombocytes with parallel filling of an energy potential. This mechanism of action leads to a notable vazodilatation, reduction of the general resistance of peripheral vessels, increase in a minute and stroke output of blood and proceeds without significant changes of ChSS.

Pentoksifillin influences in an expanding way pulmonary vessels and coronary arteries, thereby increasing delivery of oxygen in a blood channel and to a cardiac muscle (anti-anginal action) and strengthens a tone of muscles of respiratory system (a diaphragm and intercostal muscles). In case of introduction of a pentoksifillin increase in collateral circulation and increase of volume of the blood passing through section unit is intravenously observed. In a brain increase in concentration of ATP and strengthening of bioelectric activity of TsNS is noted. Viscosity of blood decreases and elasticity of erythrocyte membranes increases (because of influence of drug on patholologically the deformed erythrocytes). In areas of the broken blood circulation microcirculation amplifies. At the alternating lameness the maximum distance of walking increases, and also expressiveness of a pain syndrome at rest and the frequency of night spasms of the lower extremities (generally gastrocnemius muscles) decreases.

Pentoksifillin is characterized by a fast hepatic metabolism with allocation of several active products of a metabolism. As significant metabolites it is considered to be 1-3-carboxypropyl-3,7-dimethylxantine which plasma concentration by 8 times exceeds the serumal maintenance of a pentoksifillin and 1-5-hydroxyhexyl-3,7-dimethylxantine which plasma level is 5 times higher than pentoksifillinovy.

Bioavailability of this drug is variable and varies within 6-32%. Parallel meal increases Cmax of a pentoksifillin by 28%, and its AUC for 13%, at this Cmax of 1-5-hydroxyhexyl-3,7-dimethylxantine increases by 20%.

At oral administration of simple tablets average TCmax of a pentoksifillin makes 60 minutes, at reception of tablets retard – 120-240 minutes. After carrying out half-hour infusion with pentoksifilliny is in a dose of 200 mg, its Vd at the level of 168 liters, and the clearance is equal to 4500-5100 ml/min.

Observed T1/2 after drop injection of 100 mg of a pentoksifillin makes 1.1 hours, after internal reception of tablets – 0.4-0.8 hours. T1/2 of two significant products of a metabolism fluctuates from 1 to 1.6 hour.

Removal for 94% is carried out by kidneys and for 4% intestines, in the form of metabolites. For the first 4 hours about 90% of a pentoksifillin are excreted.

At heavy pathologies of kidneys the slowed-down removal of metabolites is noted.

At pathologies of a liver increase of bioavailability and increase in T1/2 is observed.

Indications to use

Agapurin's use is shown for treatment:

  • the disturbances of peripheral blood supply happening against inflammatory, diabetic, atherosclerotic processes (including the alternating lameness associated with an obliterating endarteritis, a diabetic angiopatiya, atherosclerosis);
  • angioneyropatiya (including Crocq's disease, paresthesias, Raynaud's disease);
  • the trophic fabric disturbances which arose because of pathologies of venous or arterial microcirculation (including freezing injury, gangrene and varicose ulcers);
  • pathologies of blood circulation of a brain of an ischemic etiology of an acute and chronic current (inclusive with cerebral atherosclerosis);
  • disturbances of eye blood circulation (including insufficiency of blood supply of vascular and mesh covers of an eye);
  • the states observed after the had stroke both ischemic, and hemorrhagic;
  • vascular disorders of functionality of a middle ear with observed relative deafness.

Contraindications

Agapurin's appointment is absolutely contraindicated at:

  • the expressed atherosclerosis (cerebral or coronary);
  • pregnancies;
  • myocardial infarction (in its acute period);
  • porphyrias;
  • feeding by a breast;
  • significant disturbances of a cordial rhythm;
  • hemorrhagic stroke (in its acute period);
  • personal hypersensitivity to a pentoksifillin and/or other components of HP;
  • uncontrollable arterial hypotonia;
  • hemorrhages in an eye retina;
  • massive bleedings;
  • aged till 18 years.

Treat relative contraindications:

Side effects

Sense bodys:

  • scotoma;
  • visual disturbances.

Nervous system:

Integuments:

  • hyperemia of the person;
  • fragility of nails;
  • inflow (as a rule, in relation to upper part of a breast and a face);
  • puffiness.

Cardiovascular system:

Alimentary system:

Bodies of a hemopoiesis:

  • pancytopenia;
  • hypofibrinogenemia;
  • thrombocytopenia;
  • development of bleedings from skin vessels;
  • leukopenia.

Allergic manifestations:

Indicators of laboratory researches:

  • increase in levels of transaminases of a liver.

Agapurin, application instruction

The application instruction of Agapurin provides peroral regular (in at one time days) reception, both simple tablets, and tablets retard. It is preferable to take a pill right after food in the whole look.

At purpose of treatment with use of usual tablets the first week of therapy carry out in a dose 200 mg (2 tablets) with its triple reception in days. In case of manifestation of negative symptomatology from TsNS, ZhKT or sharp decrease in the ABP the dosage should be lowered twice with preservation of frequency of reception of tablets.

At course therapy, as a rule, appoint thrice reception of 100 mg (1 tablet) of Agapurin at 24 o'clock, with the most admissible daily dose making 1200 mg.

In case of observed insufficiency of renal function with the creatinine level exceeding 400 mmol/l practice decrease in dosages by 30-50%.

When using of the prolonged forms of drug, tablets Agapurin retard, the therapeutic course and a dosage are established in the individual mode according to a clinical picture of the diagnosed disease and the had therapeutic effect.

Agapurin 400 WEDNESDAY it is necessary to accept tablets 2-3 times a day, 600 WEDNESDAY – twice a day. The most admissible daily dosage equals 1200 mg.

At pathologies of kidneys with KK less than 30 ml/min. as much as possible at 24 o'clock it is possible to take 2 pill on 400 mg.

At heavy pathologies of a liver decrease in dosages of the prolonged tablets taking into account personal portability of a pentoksifillin is required.

In case of Agapurin's appointment retard patients with hypotonia or to persons the ABP, inclined to decrease (an ischemic heart disease, vascular stenoses of a brain and so forth) need to begin treatment with the minimum dosages of a pentoksifillin, with their gradual increase to optimum effective values.

Injection solution of Agapurin can be entered in/in, in / and or in oil, at horizontal position of a body of the patient.

Intravenous infusions carry out in the daily dose 100 mg (1 ampoule) dissolved in 250-500 ml of solutions of sodium chloride (0,9%) or Dextrosums (5%) for 1,5-3 hours. At an affirmative answer on the carried-out infusion increase in a dosage twice is possible. As much as possible per day it is possible in/in to enter 300 mg.

Intra arterial introduction carry initially out in a dose 100 mg dissolved in 20-50 ml of solution of sodium chloride (0,9%). Further appoint on 200-300 mg in 30-50 ml of solution of sodium chloride (0,9%). Rate of administering of 100 mg of Agapurin has to be not less than 10 minutes. In case of the observed expressed vascular atherosclerosis of a brain administration of solution in a carotid artery is not allowed.

At pathologies of kidneys with KK less than 10 ml/min. lower injection Agapurin's dosage by 30-50%.

Intramuscular administration of solution is carried out by 1-2 times at 24 o'clock in a dose of 100 mg (1 ampoule).

Overdose

At overdose by Agapurin observed: weakness manifestations, lowering of the ABP, feeling of dizziness, a hyperthermia, tachycardia, unconscious states, the increased drowsiness, an areflexia, a loss of consciousness, nervous irritability, toniko-clonic spasms, the phenomena of bleedings of a gastrointestinal tract (for example, vomiting "a coffee thick").

The carried-out treatment of such states has to correspond to observed symptoms, with parallel maintenance (in need of) the normal ABP and respiratory function.

Interaction

Parallel use of Agapurin with other xanthines can become the reason of the increased nervous excitement.

Effects of a pentoksifillin can strengthen effect of valproic acid, the drugs influencing coagulability of blood (trombolitik, anticoagulants) and also antibiotics (including cephalosporins).

Agapurin increases efficiency of insulin, antihypertensives and peroral hypoglycemic drugs.

The combined reception with Cimetidinum can increase the plasma maintenance of a pentoksifillin that increases possibility of side effects.

Terms of sale

All dosage forms of Agapurin are on sale according to the recipe.

Storage conditions

The greatest possible temperature of storage of drug Agapurin in any pharmaceutical form makes 25 °C.

Period of validity

Tablets on 100 mg and 400 mg are stored for 5 years; tablets on 600 mg for 4 years; injection solution for 3 years.

Special instructions

Therapy by Agapurin needs to be carried out under a constant control of the ABP. With HSN it is necessary to achieve blood circulation compensation from patients.

At parallel reception of anticoagulants it is necessary to watch closely coagulability of blood.

Use of high doses of Agapurin for treatment of patients with a diabetes mellitus which accept hypoglycemic HP can lead to forming of the expressed hypoglycemia that demands correction of the dosing mode.

At the patients who recently transferred operative measures it is necessary to control concentration of a hematocrit and hemoglobin systematically.

When diagnosing at the patient of the underestimated or unstable ABP it is necessary to use the minimum effective dosages of Agapurin.

Correction of the dosing mode, in connection with reduction of speed of excretion can be necessary for treatment of elderly patients.

At nicotinodependent patients reduction of a therapeutic effectiveness of Agapurin can be observed.

Injection Agapurin's compatibility with solutions for carrying out infusions needs to be checked separately.

Analogs

Coincidence on the ATH code of the 4th level:

Zdravzona

  • Agapurin of 100 mg No. 60 of a tabletkizentiv
  • Agapurin Wednesday of 600 mg No. 20 of a tablet pro-longum. p/ozentiva
  • Agapurin Wednesday of 400 mg No. 20 of a tablet pro-longum. p/ozentiva
to show still

Apteka24

  • Agapurinzentiva (Slovak Republic)
  • Agapurin WEDNESDAY of the 600th tablet of the prolonged action of 600 mg No. 20zentiva International a.o. (Slovakia)
  • Agapurin SR of a tablet 400 of mg No. 20zentiva International a.o. (Slovakia)

Paniapteka

  • Agapurin of other 100 mg No. 60zentiva International a.o.
  • Agapurin of other 100 mg No. 60zentiva International a.o.
  • Agapurin of other 100 mg No. 60zentiva International a.o.
Section: Cardiological Cardiovascular
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.

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