Pentoxifylline, pills 0.1 g, 60 pcs.

Composition

Active ingredient:

pentoxifylline – 100 mg;

Auxiliary substances:

milk sugar (lactose),

potato starch,

stearic acid,

polyvinylpyrrolidone (povidone),

copolymer methacrylic acid-ethyl acrylate 1 : 1 (collicutin-100 R),

macrogol-4000 (polyethylene oxide-4000),

talc,

titanium dioxide pigment (titanium dioxide),

azorubin (carmoisine)

Pharmacological action

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

By dilating the coronary arteries, it increases oxygen delivery to the myocardium (a slight antianginal effect), and improves blood oxygenation in the lungs.

When administered intravenously, it leads to increased collateral blood circulation, an increase in the volume of blood flowing through the unit section.

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

With occlusive damage to the peripheral arteries (“intermittent” claudication), it leads to an extension of the walking distance, elimination of night cramps of the calf muscles and pain at rest.

Pharmacokinetics

The drug is rapidly metabolized in the liver after administration. In the process of 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.1.5-2 hours after the infusion, the concentration of metabolites I and V in the blood plasma is 5 and 8 times higher than the concentration of the initial substance, respectively. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood significantly decreases (up to 10% of the initial level).

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

It is excreted in breast milk.

In severe renal impairment, the excretion of metabolites is slowed down. With impaired liver function, there is an elongation of the elimination half-life and an increase in bioavailability.

Indications

• of violations of the peripheral circulation due to atherosclerosis, diabetes mellitus (diabetic angiopathy);
• chronic cerebrovascular ischemic;
• and atherosclerotic dyscirculatory encephalopathy; angiopathy (paresthesia, Raynaud’s disease);
• trophic disorders of the tissues due to violations of the arterial or venous circulation (venous stasis ulcers, post-thrombotic syndrome, frostbite, gangrene);
• occlusive disease;
• acute, subacute and chronic insufficiency of blood circulation in the retina or in the choroid of the eye;
• hearing impairment of vascular origin.

Contraindications

Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, Porphyria; acute myocardial infarction; massive bleeding; retinal hemorrhage; brain hemorrhage, acute hemorrhagic stroke; severe coronary or cerebral atherosclerosis; severe cardiac arrhythmias; pregnancy; breast-feeding period; age up to 18 years (efficacy and safety have not been established).

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

In patients with labile blood pressure and a tendency to hypotension and in patients with severe renal impairment, the dose is increased gradually and selected individually

Side effects

From the central nervous system: headache, dizziness; anxiety, sleep disorders; seizures.

From the side of the skin and subcutaneous fat: hyperemia of the skin of the face, “flushes” of blood to the skin of the face and upper chest, edema, increased fragility of nails.

From the digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.

From the side of the senses: visual impairment, scotoma.

From the cardiovascular system: tachycardia, arrhythmia, cardialgia, angina progression, low blood pressure.

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

Allergic reactions: pruritus, hyperemia of the skin, urticaria, angioedema, anaphylactic shock.

Laboratory parameters: increased activity of “hepatic” transaminases (ALT, ACT, LDH) and alkaline phosphatase.

Interaction

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

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins-cefamandol, cefoperazone, cefotetane), valproic acid.

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

Co-administration with other xanthines can lead to excessive nervous excitement in patients.

How to take, course of administration and dosage

Inside after eating. Tablets are coated with a special coating that is soluble in the intestines, so they are swallowed whole, washed down with a small amount of water. Take 0.2 g (2 tablets) 3 times a day. After achieving a therapeutic effect (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 failure (creatine clearance less than 10 ml / min) the dose is halved.

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

Overdose

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

Treatment: symptomatic. Special attention should be paid to maintaining blood pressure and respiratory function. Convulsions are removed by the introduction of diazepam. Urgent measures in case of severe anaphylactic reactions (shock):

• when primary signs (sweating, nausea, cyanosis) appear, immediately stop taking the drug;
• in addition to other necessary measures, they provide a lower position of the head and upper torso and provide freedom for breathing;
• urgent medical measures: enter intravenous epinephrine (adrenaline). If necessary, the administration of epinephrine can be repeated.

Composition

Tablet Form of production

Storage conditions

In a dry place, at a temperature not exceeding 30°C.

Shelf life

3 years

Active ingredient

Pentoxifylline

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Purpose

For adults as directed by your doctor

Indications

Diabetic retinopathy, Vascular diseases of the eyes, Vascular lesions in diabetes mellitus, Consequences of stroke, Frostbite, Raynaud’s disease, Trophic ulcers, Atherosclerosis, Cerebral circulation disorders

Weight

Weight: 50 gr.