Pentoxifylline, 100 mg 60 pcs

Pentoxifylline is a derivative of xanthine. It improves microcirculation and rheological properties of blood. The mechanism of action is associated with inhibition of phosphodiesterase and increase of cyclic 3,5 adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (ATP) in red blood cells with simultaneous saturation of energy potential, which in turn leads to vasodilation, reduction of total peripheral vascular resistance, increase of systolic and minute blood volume without significant change in heart rate.

Dilating coronary arteries increases oxygen delivery to the myocardium (minor antianginal effect), pulmonary vessels – improves blood oxygenation.

In intravenous administration leads to increased collateral circulation, increasing the volume of blood flowing through the unit section.

Limits blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (by influencing the pathologically altered deformability of red blood cells). Improves microcirculation in areas of impaired circulation.

In case of occlusive lesions of the peripheral arteries (“intermittent” claudication), leads to the prolongation of walking distance, eliminates night cramps of the calf muscles and pain at rest.

Pharmacokinetics

The drug is rapidly metabolized in the liver after administration. During metabolism two main metabolites are formed: 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) and 1-(3-carboxypropyl)-3,7-dimethylxanthine (metabolite V), which have similar activity to pentoxifylline. In 1.5-2 hours after infusion, plasma concentrations of metabolites I and V are, respectively, 5 and 8 times higher than those of the parent substance. By 8 hours the concentration of pentoxifylline and its metabolites in blood is significantly reduced (up to 10% of the initial).

The elimination half-life is from 30 minutes to 1.5 hours. It is excreted mainly by the kidneys (94%) in the form of metabolites (mainly metabolite V), by the intestine (4%). 90% of the dose is excreted during the first 4 hours. 2% of the drug is excreted unchanged. Pentoxifylline and its metabolites do not bind to plasma proteins.

It is excreted with the breast milk.

In severe renal dysfunction, excretion of the metabolites is delayed. In impaired liver function, prolongation of the elimination half-life and increased bioavailability are noted.

Indications

Deterioration of hearing, Impaired cerebral circulation, Trophic ulcers, Impaired attention and memory, Cramps of the calf muscles, Raynaud’s disease, Dizziness, Vascular lesions in diabetes, Diabetic retinopathy, Atherosclerosis, Frostbite, Vascular eye disease, Stroke sequelae

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Active ingredient

Pentoxifylline

Composition

Active substance:

Pentoxifylline – 100 mg;

Ancillary substances:

Milk sugar (lactose),

Potato starch,

Stearic acid,

polyvinylpyrrolidone (povidone),

Methacrylic acid-ethylacrylate copolymer 1 : 1 (collicut MAE-100 R),

macrogoal-4000 (polyethylene oxide-4000),

talc,

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titanium dioxide pigment (titanium dioxide),

azorubin (carmoisine)

How to take, the dosage

In the mouth after a meal. Tablets are covered with a special coating, soluble in the intestine, so they are swallowed whole with a small amount of water. Take 0.2 g (2 tablets) 3 times a day. After a therapeutic effect is achieved (usually 1-2 weeks), the dose is reduced to 0.1 g (1 tablet) 3 times a day.

The maximum daily dose is 1200 mg. The course of treatment is 1-3 months.

In patients with chronic renal insufficiency (creatine clearance less than 10 ml/min) the dose is reduced by half.

The duration of treatment and dosing regimen of Pentoxifylline is determined by the attending physician individually, depending on the clinical picture of the disease and the therapeutic effect obtained.

Interaction

Pentoxifylline increases the effect of heparin, fibrinolytic drugs, theophylline, antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

Pentoxifylline may increase the effect of anticoagulant drugs (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins – cefamandol, cefoperazone, cefotetan), valproic acid.

Cimetidine increases the plasma concentration of pentoxifylline (risk of side effects).

The co-administration with other xanthines may lead to excessive patient jitters.

Contraindications

Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, Porphyria; acute myocardial infarction; massive bleeding; retinal hemorrhages; cerebral hemorrhage, acute hemorrhagic stroke; marked coronary or cerebral atherosclerosis; marked cardiac rhythm disturbances; pregnancy; breastfeeding period; age under 18 years (effectiveness and safety not established).

With caution: the drug is prescribed to patients with atherosclerosis of cerebral and/or coronary vessels, especially in cases of arterial hypotension and heart rhythm disorders, heart failure, liver failure. Caution should also be exercised when prescribing Pentoxifylline to patients with gastric and duodenal ulcer disease, patients who have recently undergone surgery (risk of bleeding).

Patients with labile blood pressure and with the tendency to arterial hypotension and patients with significant renal dysfunction the dose is increased gradually and adjusted individually.

Side effects

Central nervous system disorders: headache, dizziness; anxiety, sleep disturbances; convulsions.

Skin and subcutaneous fat: facial hyperemia, blood rush to the face and upper chest, edema, increased nail fragility.

Digestive system disorders: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.

Sensory system disorders: visual impairment, scotoma.

Cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, decreased blood pressure.

Hematopoietic and hemostatic system disorders: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from blood vessels of the skin, mucous membranes, stomach, intestines.

Allergic reactions: itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

Laboratory measures: increase of “liver” transaminases activity (ALT, ACT, LDH) and alkaline phosphatase.

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Overdose

Symptoms: nausea, dizziness, cyanosis, tachycardia, marked decrease in blood pressure, redness of the skin, increased body temperature (chills), agitation, areflexia, tonic-clonic convulsions, “coffee grounds” vomiting, arrhythmia loss of consciousness.

Treatment: symptomatic. Particular attention should be aimed at maintaining blood pressure and respiratory function. Seizures are relieved by administration of diazepam. Urgent measures in case of severe anaphylactic reactions (shock):

• in case of primary signs (sweating, nausea, cyanosis), immediately discontinue the drug;
• in addition to other necessary measures, ensure lower head and upper torso position and provide freedom for breathing;
• urgent medical measures: Administer intravenous epinephrine (adrenaline). If necessary, epinephrine can be repeated.

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Similarities

Vasonit, Trental, Trental 400, Pentoxifylline, Trental 100, Pentoxifylline-SZ