$19.00
Manufacturer: Slovakia
Agapurin SR (pentoxifyllin) coated tablets with prolonged release are indicated for extension of painless walking distance in patients with chronic occlusive peripheral artery disease at Fonten IIb (intermittent claudication) when other measures such as gait training, angioplasty and / or recovery procedures cannot be performed or are not indicated.
Internal ear dysfunction caused by circulatory disorders (including hearing loss and sudden hearing loss).
Description
Composition
active substance: pentoxifylline;
1 tablet contains:
- 400 mg pentoxifylline;
excipients:
core: hypromellose 2208/15000, povidone 30, talc, magnesium stearate;
shell: Sepifilm 752 white dye (hypromellose, microcrystalline cellulose, polyethylene glycol (macrogol) 40 stearate, titanium dioxide (E 171)), simethicone emulsion SE4, macrogol 6000.
Pharmacotherapeutic group
Peripheral vasodilators. ATX code C04A D03.
Pharmacodynamics.
Pentoxifylline improves the rheological properties of blood (fluidity), reducing increased blood viscosity. Its pharmacological properties are explained by the fact that it:
- improves the impaired ability of erythrocytes to deform by inhibiting phosphodiesterase with a subsequent increase in intracellular cAMP and ATP concentrations, as well as inhibits erythrocyte aggregation;
- inhibits platelet aggregation;
- reduces pathologically high levels of fibrinogen in blood plasma;
- inhibits the activation of leukocytes and the adhesion of leukocytes to the endothelium of vessels.
Studies of the effect of pentoxifylline on cardiac and cerebrovascular mortality and/or morbidity have not been conducted.
Pharmacokinetics.
Prolonged release of pentoxifylline from the drug Agapurin SR 400 occurs for 10–12 hours, and its constant level is maintained in the blood all this time. Released pentoxifylline is quickly and almost completely absorbed. After that, pronounced presystemic metabolism of the substance takes place, so its systemic availability is only 20–30%.
It is almost completely metabolized in the liver. The main active metabolite
1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) is found in the blood plasma at a concentration two times higher than the concentration of the original substance with which it is in reversible biochemical equilibrium. Because of this, pentoxifylline and metabolite I are considered as an active unit. Elimination of pentoxifylline is biphasic; the initial half-life for the parent substance is 0.4-0.8 hours, and for metabolites – 1.0-1.6 hours. The final half-life of pentoxifylline from blood plasma is approximately 1.6 hours.
Entered mainly by the kidneys in the form of unconjugated water-soluble polar metabolites; only 4% is excreted in feces. Pentoxifylline is excreted unchanged in trace amounts.
In patients with severe renal or hepatic dysfunction, the half-life is longer and absolute bioavailability increases.
Indication
Prolongation of pain-free walking distance in patients with Fontan stage IIb chronic occlusive peripheral arterial disease (intermittent claudication) when other interventions such as gait training, angioplasty and/or restorative procedures cannot be performed or are not indicated.
Inner ear dysfunction caused by circulatory disorders (including tinnitus and sudden hearing loss).
Contraindications of Agapurin SR
- Hypersensitivity to pentoxifylline, other derivatives of methylxanthine or to any of the components of the drug.
- Acute myocardial infarction.
- Cerebral hemorrhage or other clinically significant bleeding.
- Stomach ulcers and/or intestinal ulcers.
- Hemorrhagic diathesis.
- Hemorrhage in the retina of the eye.
If a retinal hemorrhage occurs during treatment with pentoxifylline, the use of the drug should be stopped immediately.
Recent Reviews