Sanofi Pentoxifylline SR Long-acting tablets 400mg, 20pcs

Composition

Each tablet contains:

Active ingredient:

pentoxifylline 400 mgg;

excipients:

core:

hypromellose 2200/15000-0.12000 g, povidone 40-0.01650 g, talc-0.01050 g, magnesium stearate-0.00300 g;

shell:

sepifilm 752 white (hypromellose-35.0%-45.0%, microcrystalline cellulose-27.0%-37.0%, macrogol stearate-6.0%-10.0%, titanium dioxide-18.0%-22.0%) – 0.01500 g, dimethicone emulsion-0.000075 g, macrogol 6000-0.000175 g

Pharmacological action

Pentoxifylline improves microcirculation and rheological properties of blood.

The mechanism of action is associated with inhibition of the enzyme phosphodiesterase and an increase in the content of cyclic adenosine monophosphate (cAMP) 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 (OPSS), an increase in stroke and minute blood volume without significant changes in heart rate (HR).

Pentoxifylline reduces blood viscosity, increases the elasticity of the red blood cell membrane (by affecting the pathologically altered deformability of red blood cells), reduces the aggregation of red blood cells, platelets and neutrophils, reduces the content of fibrinogen in the blood, reduces the adhesion of white blood cells to the vascular endothelium, reduces the stimulation of white blood cells and, as a result, the destruction of the endothelium.

Improves microcirculation in areas of impaired blood circulation. With occlusive diseases of the peripheral arteries (“intermittent” claudication), it leads to an extension of the walking distance, elimination of nocturnal cramps of the calf muscles and pain at rest.

Indications

– Occlusive disease of peripheral arteries of atherosclerotic or diabetic origin (for example, “intermittent” claudication, diabetic angiopathy).

– Cerebrovascular disease (consequences of cerebral atherosclerosis, such as impaired concentration, dizziness, memory loss), ischemic and post-stroke conditions.

– Trophic tissue disorders due to violations of arterial or venous microcirculation (trophic ulcers, post-thrombophlebitic syndrome, frostbite, gangrene).

– Circulatory disorders in the vessels of the eye (acute and chronic circulatory insufficiency in the retina or in the vascular membrane of the eye).

– Disorders of the middle ear function of vascular origin, accompanied by hearing loss.

Contraindications

-Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other components that make up the drug.

– Acute myocardial infarction.

– Massive bleeding (risk of increased bleeding).

– Retinal hemorrhage (risk of increased bleeding).

– Acute hemorrhagic stroke.

– Pregnancy.

– The period of breastfeeding.

– Age up to 18 years (efficacy and safety have not been established).

With caution:

Use with caution in patients with a marked decrease in blood pressure (BP) (risk of further lowering blood pressure) and hemodynamically significant cardiac arrhythmias; chronic heart failure (CHF); severe liver function disorders (risk of accumulation and increased risk of side effects); impaired renal function (creatinine clearance (CC) less than 30 ml/min) (risk of accumulation and increased risk of side effects); peptic ulcer of the stomach and duodenum; with an increased tendency to bleeding for example, as a result of the use of indirect anticoagulants [vitamin K antagonists] or for disorders in the blood coagulation system (risk of more severe bleeding); after a recent surgical intervention (risk of bleeding); with proliferative diabetic retinopathy.

Caution should be exercised when using pentoxifylline concomitantly with platelet aggregation inhibitors (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [except selective cyclooxygenase-2 inhibitors], acetylsalicylic acid, ticlopidine, dipyridamole), hypoglycemic agents (insulin and hypoglycemic agents). drugs for oral use), ciprofloxacin and theophylline

Side effects

The frequency of adverse reactions was determined according to the World Health Organization classification: very common (≥ 1/10); common (≥ 1/100 and < 1/10); infrequent (≥ 1/1000 and < 1/100); rare (≥ 1/10000 and < 1/1000); very rare (

Nervous system disorders:  frequency unknown-headache, dizziness, convulsions, aseptic meningitis.

Mental disorders:  frequency unknown – agitation, sleep disorders, anxiety.

Cardiac disorders:  the frequency is unknown-tachycardia, arrhythmia, angina pectoris, decreased blood pressure.

Vascular disorders:  the frequency is unknown – “hot flashes” of blood to the skin, bleeding (including bleeding from blood vessels of the skin, mucous membranes, gastrointestinal bleeding, nosebleeds).

Skin and subcutaneous tissue disorders:  the frequency is unknown – pruritus, rash, erythema (redness of the skin), urticaria, edema, increased fragility of the nails.

Disorders of the gastrointestinal tract:  the frequency is unknown – anorexia, intestinal atony, epigastric discomfort, bloating (feeling full of stomach), vomiting, diarrhea, dry mouth, constipation, hypersalivation (increased salivation).

Visual disturbances:  frequency unknown-visual impairment, scotoma.

Disorders of the blood and lymphatic system:  frequency unknown-thrombocytopenia, leukopenia / neutropenia, pancytopenia, hypofibrinogenemia.

Immune system disorders:  frequency unknown – anaphylactic / anaphylactoid reactions, angioedema, anaphylactic shock, bronchospasm.

Liver and biliary tract disorders:  frequency unknown-intrahepatic cholestasis, increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (ACT), increased activity of alkaline phosphatase.

Interaction

Antihypertensive agents

The drug pentoxifylline may increase the reduction of blood pressure when used simultaneously with antihypertensive agents (for example, ACE inhibitors) or other drugs that have a potential hypotensive effect (for example, nitrates).

Medications that affect the blood coagulation system

The drug pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (direct and indirect anticoagulants, thrombolytics, antibiotics, such as cephalosporins).

When pentoxifylline and indirect anticoagulants (vitamin K antagonists) were co-administered in post-marketing studies, cases of increased anticoagulant action (risk of bleeding) were noted. Therefore, at the beginning of taking pentoxifylline or changing its dose, it is recommended to monitor the severity of anticoagulant action in patients taking this combination of drugs (for example, regular monitoring of the international normalized ratio (INR)).

Cimetidine

Cimetidine may increase the concentration of pentoxifylline and active metabolite I in blood plasma (risk of adverse reactions).

Other Xanthines

Co-use with other xanthines can lead to excessive nervous excitement.

Hypoglycemic agents (insulin and hypoglycemic agents for oral use)

The hypoglycemic effect of insulin or hypoglycemic agents for oral use may be enhanced with simultaneous use of the drug pentoxifylline (increased risk of hypoglycemia). Strict monitoring of the condition of such patients is necessary, including regular glycemic control.

Theophylline

In some patients, when pentoxifylline and theophylline are co-administered, an increase in the concentration of theophylline in blood plasma is noted. In the future, this may lead to an increase in the frequency of adverse reactions associated with theophylline.

Ciprofloxacin

In some patients, with simultaneous use of the drug pentoxifylline and ciprofloxacin, an increase in the concentration of pentoxifylline in blood plasma is noted. In the future, this may lead to an increase or increase in adverse reactions associated with the use of this combination.

Valproic Acid

When used together, the drug pentoxifylline may enhance the effect of valproic acid.

Platelet aggregation inhibitors

When pentoxifylline is co-administered with platelet aggregation inhibitors (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [except selective cyclooxygenase-2 inhibitors], acetylsalicylic acid, ticlopidine, dipyridamole), a potential additive effect may develop, increasing the risk of bleeding. Therefore, due to the risk of bleeding, pentoxifylline should be used with caution simultaneously with the above-mentioned platelet aggregation inhibitors.

How to take it, course of use and dosage

Inside, without chewing, regularly, at the same time, during or after meals, with a sufficient amount of water.

Cerebrovascular disease: 400 mg 2-3 times a day or 600 mg 1-2 times a day.

Stage II occlusive peripheral artery disease (intermittent claudication): 400 mg 3 times a day or 600 mg 2 times a day. The daily dose is 1200 mg.

Trophic tissue disorders due to impaired arterial or venous microcirculation: 400 mg 2-3 times a day or 600 mg 1-2 times a day.

The maximum daily dose is 1200 mg.

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

Patients with impaired liver function

When using the drug pentoxifylline in patients with severe hepatic impairment, caution should be exercised, possible dose reduction should be carried out taking into account individual tolerability of the drug.

Patients with impaired renal function

– Creatinine clearance below 30 ml / min: caution should be exercised, the dose of the drug can be reduced by 50-70%.

Children and teenagers

The use of pentoxifylline in patients under 18 years of age is contraindicated. The safety and efficacy of pentoxifylline in this age group has not been established.

Overdose

Symptoms: dizziness, nausea, vomiting like “coffee grounds”, marked decrease in blood pressure, tachycardia, arrhythmia, redness of the skin, loss of consciousness, chills, areflexia, tonic-clonic convulsions.

In case of the above violations, you should immediately consult a doctor.

Treatment: treatment is symptomatic. At the first signs of overdose (sweating, nausea, cyanosis), immediately stop taking the drug. If the drug is taken recently, measures should be taken to prevent further absorption of the drug by removing it (gastric lavage) or slowing its absorption (for example, taking activated charcoal). Special attention should be paid to maintaining blood pressure and respiratory function. For convulsive seizures, diazepam is administered.

The specific antidote is unknown.

Special instructions

Treatment should be carried out under the control of blood pressure.

In patients with diabetes mellitus who are taking hypoglycemic agents, the use of high doses of pentoxifylline may cause severe hypoglycemia (dose adjustment is required). When prescribing pentoxifylline simultaneously with anticoagulants, it is necessary to carefully monitor the parameters of the blood coagulation system.

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit parameters is necessary.

Patients with low and unstable blood pressure should choose the dose of pentoxifylline individually. In elderly patients, it may be necessary to reduce the dose of pentoxifylline (increase bioavailability and decrease the rate of elimination). The safety and efficacy of pentoxifylline in children are poorly understood. Caution should be exercised when using pentoxifylline in patients with severe hepatic impairment. Taking into account the risk of accumulation of the drug and the increased risk of side effects, dose reduction should be carried out taking into account individual tolerability. Patients with severe renal impairment (creatinine clearance below 30 ml / min) should be closely monitored when taking pentoxifylline.

If patients develop retinal hemorrhages during the period of use of the drug, the drug is immediately discontinued.

Smoking may reduce the therapeutic effectiveness of the drug pentoxifylline. Influence on the ability to drive vehicles and mechanisms:There was no negative effect of the drug pentoxifylline on the ability to drive vehicles and mechanisms. However, caution should be exercised when driving vehicles and during activities that require increased concentration of attention and speed of psychomotor reactions, due to the possibility of dizziness and visual impairment when using the drug pentoxifylline.

Storage conditions

It does not require special storage conditions.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Pentoxifylline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

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