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

Composition:1 ml of the solution contains the active substance: pentoxifylline - 20 mg; Excipients: sodium chloride - 7.0 mg, sodium dihydrogen phosphate dihydrate - 0.10 mg, sodium phosphate dodecahydrate - 0.10 mg, water for injection - q.s.

Description:

A clear, colorless solution.

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 increases 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, the microcirculation and supply of tissues with oxygen are noted, especially in the extremities and the 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:

With the "first pass" through the liver, metabolite is metabolized to form various metabolites. The main metabolites: metabolite 1 (1-15-hydroxy-syhexyl] -3,7-dimethyl-xanthine) and metabolite V (1- [3-carboxypropyl] -3,7-dimethyl-xanthine). 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 through the intestine. 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:

- peripheral circulatory disorders due to atherosclerosis, diabetes mellitus (diabetic angiopathy);

- acute and 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;

- acute, 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; acute hemorrhagic stroke,cerebral hemorrhage; massive hemorrhage in the retina of the eye; porphyria, pregnancy, the period of breastfeeding, age under 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, cardiac arrhythmias, chronic heart failure, cerebral and / or coronary arteriosclerosis, conditions after recent surgery, hepatic and / or renal insufficiency.

Dosing and Administration:

Duration of treatment and dosing regimen are set individually by the attending physician, depending on the clinical picture of the disease and the therapeutic effect obtained. The drug is administered intravenously in the supine position, slowly, not less than for 5 minutes. The drug is usually used at the beginning of the course treatment or if it is necessary to obtain a faster therapeutic effect in the course of treatment with Fleck ital.

With the drip IV infusion Fleksital 100 mg (1 ampoule) is diluted in 250-500 ml of 0.9% solution of sodium chloride, 5% glucose solution.

The duration of the infusion is usually 120-180 minutes.

The initial infusion dose of 100 mg, if necessary, can be increased to 300 mg per day. At the maximum allowable infusion daily dose. A 300 mg infusion of 120-180 minutes is done twice in the morning and evening hours.

Patients with chronic renal failure (creatinine clearance less than 10 ml / min.) Are administered 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, progression of symptoms of angina pectoris, lowering of 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 of the skin of the face," tides "of blood to the skin of the face and upper chest, edema.

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: 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, after taking the drug, a little time has passed, gastric lavage should be performed (to prevent further absorption of the drugs) and to prescribe 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 atherosclerosis of the vessels, especially with concomitant arterial hypertension and cardiac rhythm disturbances. These patients may have angina attacks, arrhythmias and hypotension.

FROM caution 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 blood 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 hypoglycemic or antihypertensive agents, the dose of the latter 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 effectiveness of pentoxifylline in children is not well understood.

Smoking can reduce the therapeutic effectiveness of the drug.

The compatibility of a solution of pentoxifylline with the infusion solution should be checked in each case.

When carrying out intravenous infusions the patient should be in the "lying" position.

Form release / dosage:Concentrate for the preparation of a solution for infusions of 20 mg / ml. 5 ml in ampoules, made of colorless glass with a ring of green. 5 ampoules in a plastic pallet, 1 tray with ampoules, along with instructions for use in a cardboard box.

Packaging:(5) - ampoules (1) - cardboard packages

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date indicated.

Terms of leave from pharmacies:On prescription

Registration number:П N012965 / 01

Date of registration:16.01.2009

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)