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

Pentoxifylline is a derivative of xanthine. Improves microcirculation and rheological properties of blood.The mechanism of action is associated with inhibition of phosphodiesterase, and an increase 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 the systolic and minute volume of the heart without a significant change in the heart rate.

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

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm). With intravenous administration leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section. It leads to an increase in the content of ATP in the brain, favorably affects the bioelectric activity of the central nervous system.

Reduces the viscosity of blood, causes disaggregation of platelets, increases elasticity membranes of erythrocytes (due to the impact on pathologically altered erythrocyte deformity).Improves microcirculation in areas of impaired blood circulation.

In the occlusal lesion of peripheral arteries ("intermittent" lameness) leads to the elimination of night cramps calf muscles and pain at rest.

Pharmacokinetics:

Metabolised by the liver. In the process of metabolism, several active metabolites are formed, the main ones being metabolite 1 and metabolite 5. Their concentration in blood plasma is 5 and 8 times (respectively) higher than the concentration of the initial substance. It is excreted mainly in the form of metabolites (94%) by the kidneys and through the intestine (4%). Excreted in breast milk. In the first 4 hours, up to 90% of the dose is excreted. Unchanged, 2 % preparation. Pentoxifylline and its metabolites do not bind to blood plasma proteins.

With severe renal dysfunction, excretion of metabolites is slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

- violations of peripheral blood circulation against atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis);

- trophic tissue disorders due to violation of arterial and venous microcirculation (varicose ulcers, gangrene, frostbite);

- angioneuropathy (paresthesia, acrocyanosis, Raynaud's disease);

- acute and chronic disorders of cerebral circulation of the ischemic type (including cerebral atherosclerosis);

- condition after hemorrhagic and ischemic stroke;

- disorders of blood circulation in the vessels of the eye (acute and chronic insufficiency of the blood supply to the retina and choroid of the eye);

- disturbances in the functions of the middle ear of vascular genesis, accompanied by deafness.

Contraindications:

- hypersensitivity to pentoxifylline, other xanthine derivatives or other components included in the formulation;

- severe coronary or cerebral atherosclerosis;

- acute myocardial infarction;

- severe cardiac rhythm disturbances;

- uncontrolled arterial hypotension;

- massive bleeding;

- hemorrhage in the retina of the eye;

- hemorrhagic stroke;

- pregnancy, lactation;

- age to 18 years (efficacy and safety not established).

Carefully:patients with a labile arteryalumnithe, inclinedarterial hypotension, chronic heart failure, a penchant for hemorrhages, a condition following recent surgery, hepatic and / or renal insufficiency.

Pregnancy and lactation:contraindicated

Dosing and Administration:

The drug is administered intravenously. When carrying out infusions the patient should be in the "lying" position.

Intravenously drip slowly in a dose of 100 mg in 250-500 ml of 0.9% solution of sodium chloride or in a 5% solution of dextrose (glucose) (duration of administration - 90-180 minutes).

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

Side effects:

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

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

From the skin: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails.

From the digestive system: nausea, vomiting, dryness of the oral mucosa, a feeling of heaviness in the stomach, a decrease in appetite, an exacerbation of cholecystitis, cholestatic hepatitis, intestinal atony, bleeding from the mucous membranes of the stomach, intestines.

From the sense organs: impaired vision, scotoma.

From the hemostasis and hematopoiesis system: Thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; nasal bleeding.

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

Laboratory indicators: increased activity of "hepatic" transaminases - alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH) and alkaline phosphatase.

Other: Aseptic meningitis (rare).

Overdose:

Symptoms: weakness, dizziness, marked decrease in blood pressure, tachycardia, drowsiness, loss of consciousness, tonic-clonic convulsions, increased nervous excitability, hyperthermia, areflexia, signs of gastrointestinal bleeding (vomiting like "coffee grounds").

Treatment: symptomatic, aimed at maintaining vital body functions.

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 hypoglycemic agents for receptiona internalь.

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.

Special instructions:

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

Patients with chronic heart failure should be compensated for blood circulation.

In patients with diabetes mellitus taking hypoglycemic agents, the administration of large doses of Pentoxifylline may 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 had recently undergone surgery,a systematic control of hemoglobin and hematocrit.

The administered dose should be reduced in patients with low and unstable blood pressure. Older patients may need a dose reduction (increased bioavailability and reduced elimination rate).

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.

Effect on the ability to drive transp. cf. and fur:The effect of the drug on the ability to drive vehicles with an intravenous route of administration has not been studied.

Form release / dosage:

Solution for intravenous administration of 20 mg / ml in ampoules of 5 ml. 5 ampoules per contour cell packaging made of polyvinyl chloride film. 1 or 2 contoured cell packs with scarifier ampoule ceramic or knife for opening ampoules and instructions for use in a pack of cardboard. When using ampoules with a fracture ring or break point, the knife or scarifier is not inserted.

Packaging:(5) - ampoule (2) / 2 contoured cell packs with scarifier ampoule ceramic or knife for opening ampoules and instructions for applying to a pack ofcardboard. When using ampoules with a break ring or a break point, the knife or scarifier is not put in. / - Cardboard bundle
(5) - ampoule (5) / 1 contour mesh package with scarifier ampoule ceramic or knife for opening ampoules and instructions for application in a pack of cardboard. When using ampoules with a break ring or a break point, the knife or scarifier is not put in. / - Cardboard bundle

Storage conditions:

List B. Store in a 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008014/10

Date of registration:12.08.2010

The owner of the registration certificate:BINNOFARM, CJSC BINNOFARM, CJSC Russia

Manufacturer: & nbsp

BINNOFARM, CJSC Russia

Information update date: & nbsp23.12.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)