Flexitale - instructions for use, dose, side effects, contraindications

Excipients: lactose, corn starch, cellulose microcrystalline, sodium lauryl sulfate, povidone K-30, talc purified, magnesium stearate, silicon dioxide colloidal anhydrous, acrylic acid copolymer type B, acrylic acid copolymer type C, dibutyl phthalate, titanium dioxide, macrogol 6000, dye diamond blue.

Description:Round tablets of blue color, covered with enteric film membrane.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

It blocks phosphodiesterase and promotes the accumulation of cyclic AMP in tissues. Increases the elasticity of erythrocyte membranes, inhibits the aggregation of platelets and erythrocytes, reduces the increased concentration of fibrinogen in the plasma and enhances fibrinolysis, which leads to a decrease in blood viscosity and improves its rheological properties. Has a weak myotropic vasodilator effect, somewhat reduces the overall peripheral vascular resistance (OPSS) and has a positive inotropic effect. As a result of the use of the drug, improvement in microcirculation and tissue supply with oxygen is noted, mostly in the limbs and central nervous system, and to a moderate degree in the kidneys. Slightly dilates the coronary vessels. The therapeutic effect usually occurs after 2-4 weeks of treatment.

Pharmacokinetics:

After oral administration, it is almost completely absorbed from the gastrointestinal tract.At the "first passage" through the liver is metabolized with the formation of various metabolites. When administered inside a dose of 100 mg, the time to reach a maximum concentration of -1 hour. The main metabolites: metabolite 1 (1-15-hydroxyhexyl) -3,7-dimethylxanthine) and metabolite V (1- [3-carboxypropyl] -3,7-dimethylxanthine). The concentration of these metabolites in the blood plasma, respectively, is 5 and 8 times higher than the concentration of the active substance. The half-life of pentoxifylline is 0.4 to 0.8 hours; the half-life of metabolites is -1-1.6 hours.

It is excreted mainly by kidneys in the form of metabolites. Less than 4% of the accepted dose is excreted with feces. When administered inside at a dose of 100 mg, the maximum concentration of the basic substance and metabolites is determined after 2-4 hours and remains stable for an extended period of time.

Indications:

- violations of peripheral circulation, caused by atherosclerosis, diabetes (diabetic angiopathy);

- chronic disorders of cerebral circulation of the ischemic type;

- atherosclerotic and dyscirculatory encephalopathies; angioneuropathy (paresthesia, Raynaud's disease);

- trophic tissue disorders due to violation of arterial or venous microcirculation (trophic ulcers, postthrombophlebitic syndrome, frostbite, gangrene);

- obliterating endarteritis;

- subacute and chronic circulatory insufficiency in the retina or in the choroid of the eye;

- hearing disorders of vascular genesis.

Contraindications:

Hypersensitivity to pentoxifylline and other methylxanthine derivatives; acute myocardial infarction; massive bleeding; nosebleeds, acute hemorrhagic stroke, cerebral hemorrhage; massive hemorrhage in the retina of the eye; pregnancy, the period of breastfeeding, age to 18 years (safety and efficacy of the drug in children is not established).

Carefully:lability of blood pressure or with a tendency to arterial hypotension, chronic heart failure, atherosclerosis of cerebral and / or coronary vessels, peptic ulcer and duodenal ulcer, conditions after recent surgery, hepatic and / or renal failure, severe arrhythmias, increased addiction to bleeding, for example,as a result of the use of anticoagulants or with violations in the blood coagulation system (the risk of developing more severe bleeding).

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside, with food, not liquid, squeezed a small amount of liquid. Established individually, taking into account the severity of circulatory disorders, the patient's body weight and tolerability of the drug. Assign a dose of 100 mg 2-3 times a day. The maximum daily dose is 1200 mg. The duration of treatment is not less than 8 weeks. In case of side effects, the dose should be reduced to 100 mg twice a day.

Patients with chronic renal failure (creatinine clearance less than 10 ml / min.) Are prescribed 50-70% of the usual dose.

Side effects:

From the digestive system: dry mouth, decreased appetite, nausea, vomiting, epigastric pain, diarrhea, intestinal atony; bleeding from the vessels of the stomach, intestines.

From the cardiovascular system: tachycardia, arrhythmia, cardialgia, the progression of symptoms of angina, lowering blood pressure.

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

Allergic reactions: skin rash, itching, urticaria, bleeding from the vessels of the skin and mucous membranes, skin hyperemia, angioedema, anaphylactic shock.

From the side of the liver: cholecystitis, hepatitis, jaundice.

From the skin and subcutaneous fat: hyperemia. skin of the face, "tides" of blood to the skin of the face and upper chest, swelling.

On the part of the organs of hematopoiesis and the system of hemostasis: Thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; changes in the pattern of peripheral blood. Laboratory indicators: an increase in the activity of "hepatic" enzymes (ALT, ACT, LDH) and alkaline phosphatase.

Rarely there are cases of development of aseptic meningitis.

Rarely: malaise, unpleasant taste in the mouth, hypersalivation, conjunctivitis, scotoma, blurred vision, earache, increased brittleness of the nails, changes in body weight, swelling of glands, nasal congestion;

Overdose:

Symptoms: nausea, weakness, dizziness, tachycardia, lowering blood pressure, hyperthermia, drowsiness or agitation,loss of consciousness, areflexia, clonic-tonic convulsions, as a sign of gastrointestinal bleeding, vomiting like "coffee grounds".

Treatment: there is no specific antidote.

If a little time passes after taking the drug, you should wash the stomach (to prevent further absorption of the drug) and appoint Activated carbon. In the case of vomiting with traces of blood, gastric lavage is unacceptable.

Conduction of symptomatic therapy.

Interaction:

Pentoxifylline potentiates the anticoagulant effect of heparin, fibrinolytic agents, enhances the effect of antihypertensive and hypoglycemic agents (insulin and oral hypoglycemic agents).

Pentoxifylline can enhance the action of antibiotics (including cephalosporins - cefamandol, cefotetana), 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 of patients.

Special instructions:

Caution should be exercised in appointing Flexitale to patients with severe cerebral and / or coronary atherosclerosisvessels, especially with concomitant arterial hypertension and heart rhythm disturbances. These patients may have angina attacks, arrhythmias and hypotension.

Carefully should be prescribed to patients with peptic ulcer of the stomach and duodenum (including in the history); patients who have recently undergone surgical intervention (in these cases there is an increased risk of bleeding, therefore systematic monitoring of hemoglobin and hematocrit concentration is necessary).

In the case of using the drug in patients with chronic heart failure, a phase of blood circulation compensation must first be achieved. Patients with labile arterial pressure or with a tendency to arterial hypotension, the dose of the drug is increased gradually. Patients with severe renal dysfunction are given a dose of the drug individually. In the case of simultaneous application of Flexitals and oral anticoagulants, regular monitoring of prothrombin time is necessary. With the simultaneous use of Flexital and antidiabetic or antihypertensive agents, the dose of the last drugs should be reduced.

In the event of a hemorrhage in the retina of the eye during treatment Flexitol, it is necessary to immediately cancel the drug.

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

In elderly people, a dose reduction may be required (increased bioavailability and reduced rate of excretion).

The safety and efficacy of pentoxcillin in children have not been adequately studied.

Smoking can reduce the therapeutic effectiveness of the drug.

Form release / dosage:

Tablets coated with enteric film coating, 100 mg.

10 tablets per strip, made of aluminum foil. For 6 strips, together with the instructions for use are placed in a cardboard box.

Packaging:(10) - packings without cell contour (6) - packs cardboard

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:4 years. Do not use after the expiration date indicated.

Terms of leave from pharmacies:On prescription

Registration number:П N012965 / 02

Date of registration:25.05.2009

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp24.08.2015

Illustrated instructions

Instructions

Flexital (Flexital)