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 the inhibition of phosphodiesterase and an increase in the content of cyclic 3,5 AMP in platelets and ATP in erythrocytes with a simultaneous saturation of the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in systolic and minute heart volume without a significant change in frequency heartbeats.

Expanding coronary artery, increasing oxygen delivery to the myocardium (antianginal effect), lung vessels - improves blood oxygenation.

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 the blood, causes disaggregation of platelets, increases the elasticity of the erythrocyte membrane (due to the effect on the pathologically altered erythrocyte deformity).Improves microcirculation in areas of impaired blood circulation.

In the occlusive lesion of peripheral arteries (intermittent claudication), leads to an elongation of the walking distance, elimination of night cramps of calf muscles and pain at rest.

Pharmacokinetics:

The drug is rapidly metabolized in the liver. In the process of metabolism, several active metabolites are formed, the main ones being metabolite 1 and metabolite 5. Their concentrations in the blood plasma are 5 and 8 times (respectively) higher than the concentration of the starting substance.

Isolated in the form of metabolites (94%) and through the intestine (4%), in the first 4 hours up to 90% of the dose is excreted. Unchanged, 2% of the drug is excreted. 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 or 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 function of the middle ear of vascular genesis, accompanied by deafness.

Contraindications:

- hypersensitivity to pentoxifylline and substances from the group of xanthion derivatives;

- severe coronary or cerebral atherosclerosis;

- acute myocardial infarction;

- severe cardiac rhythm disturbances;

- uncontrolled arterial hypotension;

- porphyria;

- massive bleeding;

- hemorrhage in the retina of the eye;

- cerebral hemorrhage;

- acute hemorrhagic stroke;

- pregnancy, lactation;

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

Carefully:

sick from labile arterial pressure, a tendency to arterial hypotension, heart failure, a penchant for hemorrhages, a condition after recent surgery, liver and / or kidney failure.

Pregnancy and lactation:contraindicated

Dosing and Administration:

The drug is administered intravenously. When carrying out intravenous infusions the patient should be in a prone position.

Intravenous injection: 100-300 mg (1-3 ampoules) is diluted in 100-500 ml of 0.9% sodium chloride solution and administered 1-2 times a day. The infusion rate is 100 mg / 60 min.

If necessary, you can increase the dose to 400 mg during the day. It can also be administered in the form of a slow 5-minute intravenous infusion of 100 mg (1 ampoule) 1-2 times per day.

Side effects:

From the side of 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 gastrointestinal tract: nausea, vomiting, a feeling of heaviness in the stomach, a decrease in appetite, exacerbation of cholecystitis, cholestatic hepatitis, 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; bleeding from the vessels of the skin.

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

Laboratory indicators: increased activity of "liver" transaminases (ALT, ACT, LDH) and alkaline phosphatase.

Overdose:

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

Treatment: symptomatic, aimed at maintaining the function of breathing and blood pressure, urgent 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, cefotetan, 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.

Special instructions:

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

In patients with diabetes mellitus taking hypoglycemic drugs, the administration of large doses 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 is necessary.

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

In elderly people, a dose reduction (reduction in the rate of excretion) may be required. 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:During the treatment period, be careful when driving vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration 20 mg / ml.

Ampoules of 5 ml of neutral glass.

For 10 ampoules with instructions for application and knife for opening

ampoules or scarifier The ampoule is placed in a box of

cardboard.

By 5 or 10 ampoules per circuit cell pack of film

polyvinyl chloride or ribbon polyethylene terephthalate and foil

aluminum or paper with polyethylene coating or without

foil, or without paper.

For 1 or 2 contour squares with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Packaging:ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - cardboard boxes
ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cell outlines without cover-packs cardboard
ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cellular contour-packs cardboard
ampoules (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cell outlines without cover-packs cardboard
ampoules (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cellular contour-packs cardboard

Storage conditions:

Store in the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children place.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002856 / 01

Date of registration:17.07.2008

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)