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

Excipients, (core): lactose monohydrate (milk sugar) - 41.5866 mg, potato starch - 9.0000 mg, methyl cellulose (water-soluble SM-100) - 1.0076 mg, povidone (low molecular weight polyvinylpyrrolidone or Plasdon K-17) - 6.8000 mg, stearic acid - 1.6058 mg;

Auxiliary substances (shell): cellulose acetate 5,9560 mg, titanium dioxide 1,8190 mg, castor oil ordinary castor oil 1.0300 mg, liquid paraffin (vaseline oil) 1.11220 mg, azorubin dye (acidic red 2C) - 0.0205 mg, beeswax - 0.0225 mg, talc - 0.0300 mg.

Description:

tablets covered with an enteric-insoluble coat of pink color, biconvex round in shape, two layers are visible on the transverse section: the first layer is pink, the second is white or almost white.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline is a derivative of xanthine. Improves microcirculation and rheological properties of blood. The mechanism of action is related to inhibition of phosphodiesterase, and an increase in the concentration of cyclic adenosine monophosphate 3.5 (3.5 AMP) in platelets and adenosine triphosphate (ATP) in erythrocytes with simultaneous saturation of the energy potential, which in turn leads to vasodilation, reducing the total peripheral vascular resistance, an increase in systolic and minute blood volume without a significant change in heart rate.

Expanding the coronary arteries, increases the delivery of oxygen to the myocardium (antianginal effect), the vessels of the lungs - improves oxygenation of the blood.

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm).

Reduces the viscosity of the blood, causes disaggregation of platelets,increases the elasticity of erythrocytes (due to the effect on the pathologically changed deformability of erythrocytes). Improves microcirculation in areas of impaired blood circulation. In the occlusal lesion of peripheral arteries ("intermittent" lameness), leads to lengthening the distance of walking, eliminating night cramps calf muscles and pain at rest.

Pharmacokinetics:

Absorption when ingested - high.

It is subjected to the "first pass" through the liver with the formation of 2 basic pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V). The concentration of metabolites I and V in the plasma, respectively, is 5 and 8 times higher than that of pentoxifylline.

The time to reach the maximum concentration (TCmax) - 1 hour. It is distributed evenly.

The half-life period (T1 / 2) -0.5-1.5 hours, is excreted by the kidneys - 94% in the form of metabolites (mainly metabolite V), intestine - 4%, in the first 4 hours up to 90% of the dose is excreted. Excreted in breast milk.

With severe renal dysfunction, excretion of metabolites is slowed down. If liver function is impaired, lengthening T1 / 2 and increasing bioavailability are noted.

Indications:

Disorders of peripheral blood circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy), chronic cerebral circulatory disorders of ischemic genesis, atherosclerotic and discirculatory encephalopathy, angiopathy (paresthesia, Raynaud's disease), trophic tissue disorders (postthrombotic syndrome, varicose veins, trophic ulcers of the lower leg, gangrene, frostbite); obliterating endarteritis; acute circulatory disorders in the retina and choroid of the eye; otosclerosis, degenerative changes on the background of the pathology of the vessels of the inner ear with a gradual decrease in hearing.

Contraindications:Hypersensitivity to pentoxifylline, other xanthine derivatives or other components that make up the drug (lactose monohydrate); acute myocardial infarction; porphyria, massive hemorrhage, hemorrhagic stroke, bleeding in the retina of the eye, pregnancy, lactation, children under 18 years of age (efficacy and safety not studied).

Carefully:

Lability of blood pressure (propensity to arterial hypotension), chronic heart failure,peptic ulcer of the stomach and duodenum, conditions after recent surgery, hepatic and / or renal failure.

Patients with labile arterial pressure and with a tendency to arterial hypotension and patients with severe impairment of kidney function increase the dose gradually and select individually.

Dosing and Administration:

Pentoxifylline is taken orally after a meal. The tablets are covered with a special shell, soluble in the intestines, so they are swallowed whole, washed down with a small amount of water.

Take 200 mg (2 tablets) 3 times a day. If necessary, the dose is gradually increased to 1200 mg per day, divided into 2-3 doses. The maximum daily dose is 1200 mg. The course of treatment 1-3 months.

In patients with chronic renal failure (creatinine clearance less than 10 ml / min), the dose is halved.

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.

Side effects:

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

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, cells, swelling, increased brittleness of the nails.

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

From the sense organs: impaired vision, scotoma.

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

On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from the vessels of the skin, mucous membranes, stomach, intestines.

Allergic reactions: itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

Laboratory indicators: an increase in the activity of "hepatic" transaminases: alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH) and alkaline phosphatase.

Overdose:

Symptoms: weakness, dizziness, low blood pressure, fainting, tachycardia, drowsiness or agitation, loss of consciousness, hyperthermia, areflexia, tonic-clonic convulsions, signs of gastrointestinal bleeding (vomiting like "coffee grounds").

Treatment: rinse the stomach, take Activated carbon, further - treatment symptomatic, aimed at maintaining the function of respiration and blood pressure; emergency measures for bleeding.

Interaction:

Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetana), valproic acid.

Increases the effectiveness of antihypertensive drugs, insulin and oral hypoglycemic drugs.

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:

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

In patients with diabetes mellitus taking hypoglycemic agents, the administration of large doses of pentoxifylline can cause severe hypoglycemia (dose adjustment is required).

At appointment simultaneously with anticoagulants it is necessary to watch carefully indicators of a coagulating system of a blood.

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

The administered dose should be reduced in patients with low and unstable arterial pressure.

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

Tobacco smoke can reduce the therapeutic effectiveness of the drug.

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

Form release / dosage:

Intestinal-coated tablets, 100 mg

For 10 tablets in a contour mesh box made of PVC film and aluminum foil, b contour mesh packages together with instructions for use are placed in a pack of cardboard.

Packaging:(10) - contour mesh package (6) / with instruction for use / - package

Storage conditions:

List B.Store in a dry, dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000361

Date of registration:05.04.2010

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)