Pentoxifylline retard tablets p / o 400mg, No. 20

- disorders of peripheral circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy);
- chronic disorders of cerebral circulation of ischemic genesis;
- atherosclerotic and discirculatory encephalopathy; angiopathy (paresthesia, Raynaud's disease);
- trophic tissue disorders due to impaired arterial or venous microcirculation (trophic ulcers, post-thrombophlebitic syndrome, frostbite, gangrene);
- obliterating endarteritis;
- acute, subacute and chronic circulatory failure in the retina or in the choroid of the eye;
- hearing impairment of vascular origin.

Pentoxifylline is taken orally after meals. The tablets are coated with a special coating that is soluble in the intestine, so they are swallowed whole with a little 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 the dosage regimen of Pentoxifylline is established by the attending physician individually, depending on the clinical picture of the disease and the therapeutic effect obtained.

Active substance
pentoxifylline - 100 mg

Excipients:
milk sugar (lactose), potato starch, stearic acid, polyvinylpyrrolidone (povidone), methacrylic acid - ethyl acrylate copolymer 1: 1 (MAE-100 R collikut), macrogol-4000 (polyethylene oxide-4000), talc, titanium dioxide (titanium dioxide), azorubin (carmoisine).

Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, Porphyria; acute myocardial infarction; massive bleeding; retinal hemorrhage; cerebral hemorrhage, acute hemorrhagic stroke; severe coronary or cerebral atherosclerosis; severe heart rhythm disturbances; pregnancy; lactation 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. Care should also be taken when prescribing Pentoxifylline to patients with gastric ulcer and duodenal ulcer, patients who have recently undergone surgery (risk of bleeding).

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

Tradename:

Pentoxifylline

International non-proprietary name:

Pentoxifylline

Dosage form:

Enteric-coated tablets.

Composition:

Each enteric-coated tablet contains as

Active substance
pentoxifylline - 100 mg

Excipients:
milk sugar (lactose), potato starch, stearic acid, polyvinylpyrrolidone (povidone), methacrylic acid - ethyl acrylate copolymer 1: 1 (MAE-100 R collikut), macrogol-4000 (polyethylene oxide-4000), talc, titanium dioxide (titanium dioxide), azorubin (carmoisine).

Description

Enteric-coated tablets, pink, biconvex. The cross section shows two layers.

Pharmacotherapeutic group:

Vasodilating agent.

ATX

C04AD03

Pharmacological properties

Pharmacodynamics
Pentoxifylline improves microcirculation and rheological properties of blood, has a vasodilating effect, blocks phosphodiesterase and promotes the accumulation of cAMP in cells. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the level of fibrinogen in plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. It has a weak myotropic, vasodilating effect. Pentoxifylline slightly reduces the total peripheral resistance and slightly dilates the coronary vessels.

In general, Pentoxifylline causes an improvement in microcirculation and oxygen supply to tissues in the brain and limbs, to a lesser extent in the kidneys.

Pharmacokinetics
After oral administration, Pentoxifylline is almost completely absorbed from the gastrointestinal tract. The drug undergoes 'first pass' through the liver with the formation of 2 main pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite 1) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V). The concentration of metabolite I and V in plasma, respectively, is 5 and 8 times higher than that of pentoxifylline. The time to reach maximum concentration is 1 hour. The half-life is 0.5 - 1.5 hours. Pentoxifylline is excreted mainly by the kidneys - 94% in the form of metabolites (mainly V metabolite), by the intestines - 4%, in the first 4 hours. up to 90% of the dose is eliminated. Excreted in breast milk. In severe renal impairment, excretion of metabolites is slowed down.In case of liver dysfunction, an elongation of the half-life and an increase in bioavailability are noted.

Indications for use:

- disorders of peripheral circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy);
- chronic disorders of cerebral circulation of ischemic genesis;
- atherosclerotic and discirculatory encephalopathy; angiopathy (paresthesia, Raynaud's disease);
- trophic tissue disorders due to impaired arterial or venous microcirculation (trophic ulcers, post-thrombophlebitic syndrome, frostbite, gangrene);
- obliterating endarteritis;
- acute, subacute and chronic circulatory failure 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; cerebral hemorrhage, acute hemorrhagic stroke; severe coronary or cerebral atherosclerosis; severe heart rhythm disturbances; pregnancy; lactation 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. Care should also be taken when prescribing Pentoxifylline to patients with gastric ulcer and duodenal ulcer, patients who have recently undergone surgery (risk of bleeding).

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

Method of administration and dosage:

Pentoxifylline is taken orally after meals. The tablets are coated with a special coating that is soluble in the intestine, so they are swallowed whole with a little 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 the dosage regimen of Pentoxifylline is established by the attending physician individually, depending on the clinical picture of the disease and the therapeutic effect obtained.

Side effects

From the side of the central nervous system: headache, dizziness; anxiety, sleep disturbances; convulsions.

On the part of the skin and subcutaneous fat: hyperemia of the skin of the face, 'hot flushes' of blood to the skin of the face and upper part of the chest, edema, increased fragility of the nails.

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

From the senses: visual impairment, scotoma.

From the side of the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, decreased blood pressure.

From the side of the hematopoietic system and the hemostatic system: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from the vessels of the skin, mucous membranes. stomach, intestines.

Allergic reactions: itching, flushing of the skin, urticaria, angioedema, anaphylactic shock.

Laboratory indicators: increased activity of 'hepatic' transaminases (ALT, ACT, LDH) and alkaline phosphatase.

Overdose

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

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

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

Interaction with other medicinal products

Pentoxifylline enhances the effect 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 - cefamandole, cefoperazone, cefotetan), valproic acid.

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

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

special instructions

Patients with severe renal impairment while taking Pentoxifylline require particularly careful medical supervision. If during the period of use of the drug in patients there are hemorrhages in the retina of the eye, then the drug is immediately canceled. Treatment should be carried out under the control of blood pressure. In patients with diabetes mellitus taking hypoglycemic agents, administration in large doses can cause hypoglycemia (dose adjustment is required). When administered simultaneously with anticoagulants, it is necessary to carefully monitor the indicators of the blood coagulation system. In patients who have undergone recent surgery, systematic monitoring of the level of hemoglobin and hematocrit is necessary. In the elderly, dose reduction (increased bioavailability and decreased elimination rate) may be required.Smoking can reduce the therapeutic efficacy of the drug.

Release form:

Enteric-coated tablets, 100 mg
10 tablets in a blister strip made of polyvinyl chloride film and lacquered aluminum foil.
10, 20, 30, 40, 50, 60, 100 tablets in polymer jars.
Each can or 1,2,3, 4, 5, 6 blisters with instructions for use are placed in a cardboard box for consumer packaging.

Storage conditions:

List B. In a dry place, at a temperature not exceeding 30 ? C.
Keep out of the reach of children.

Shelf life:

2 years.
Do not use after the expiration date.

Terms of dispensing from pharmacies:

On prescription.