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 oppression of phosphodiesterase and an increase in the content of cyclic 3,5adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (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 the heart rate.

With intravenous administration leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section.

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.

Pharmacokinetics:

After intravenous administration pentoxifylline quickly distributed to tissues. Can penetrate the blood-brain barrier. Pentoxifylline is metabolized by the liver. In the process of metabolism, several active metabolites are formed, the main of which are: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V).Their concentration in blood plasma is 5 and 8 times (respectively) higher than the concentration of the starting substance. It 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. Unchanged, 2% of the drug is excreted. Pentoxifylline and its metabolites do not bind to blood plasma proteins. Excreted in breast milk. 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 circulation against the background of 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:

- acute myocardial infarction;

- massive bleeding;

- acute hemorrhagic stroke;

- retinal detachment and hemorrhage into the retina of the eye;

- severe atherosclerosis of the coronary or cerebral arteries;

- severe arrhythmias;

- increased sensitivity to pentoxifylline and other xanthine derivatives;

- uncontrolled arterial hypotension;

- pregnancy, the period of breastfeeding;

- age to 18 years.

Carefully:It should be applied carefully in patients with liver and kidney disease.

Pregnancy and lactation:

The drug is contraindicated for use during pregnancy.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

The drug is administered intravenously drip 3 times a day for 100-200 mg (50-100 ml of 2.0 mg / ml solution) for 20-30 minutes in a prone position.In severe patients, the daily dose can be increased to 300 mg per day.

Of necessity pentoxifylline can be administered intraarterially - first in a dose of 0.1 g in 20-50 ml of isotonic sodium chloride solution and in the following days - 0.2-0.3 g in 30-50 ml of solvent (rate of administration: 0.1 g ( 5 ml of a 2% solution of pentoxifylline) for 10 minutes).

With severe atherosclerosis of the cerebral vessels, the drug should not be administered into the carotid artery.

In the treatment of chronic atherosclerotic or diabetic lesions, a course of intravenous infusions of the drug is prescribed daily or every other day.

Side effects:

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

From the side of 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, 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 minotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH) and alkaline phosphatase.

Other: aseptic meningitis (rarely).

Overdose:

Symptoms: weakness, dizziness, marked decrease in blood pressure, syncope, tachycardia, drowsiness, loss of consciousness, hyperthermia, 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.

Interaction:

Pentoxifylline is able to enhance the action of drugs that reduce blood pressure (ACE inhibitors, nitrates). Pentoxifylline can enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins).

Cimetidine increases the concentration of pentoxifylline in the plasma (risk of side effects). Co-administration with other xanthines can lead to excessive nervous excitement. Sugar-reducing action of insulin or oral
antidiabetic drugs can be enhanced by taking pentoxifylline (an increased risk of developing hypoglycemia). Strict monitoring of such patients is necessary.

In some patients, simultaneous administration of pentoxifylline and theophylline may lead to an increase in the level of theophylline. This may lead to an increase or increase in side effects associated with theophylline.

Special instructions:

When pentoxifylline is prescribed concomitantly with anticoagulants, it is necessary to carefully monitor the parameters of the blood coagulation system.When prescribing the drug should also monitor blood pressure. Patients with chronic heart failure before the appointment of pentoxifylline should be treated with cardiac glycosides to ensure the optimal effect of pentoxifylline.

With special caution should be appointed pentoxifylline patients who have increased sensitivity to methylxanthines (caffeine, theophylline, theobromine).

It should be applied carefully in patients with liver and kidney disease.

In patients with diabetes mellitus, who take hypoglycemic drugs, the appointment in large doses can cause severe hypoglycemia (dose adjustment is required); in patients who have recently undergone surgery, systematic monitoring of the level of hemoglobin and hematocrit is necessary; older people may need a dose reduction (increased bioavailability and reduced elimination rate); Smoking can reduce the therapeutic effectiveness of the drug; compatibility of a solution of pentoxifylline with an 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:

100 ml in polymer containers for infusion solutions. Each polymer container, along with instructions for medical use, is placed in a transparent plastic bag.

For hospitals: each polymeric container is placed in a transparent polyethylene bag and laid together with instructions for medical use in an amount corresponding to the number of polymer containers into boxes of corrugated paperboard.

Packaging:(100) - polymer container (1) / 100 ml each in polymer containers placed in a polyethylene package. Polymeric containers, together with instructions for medical use in an amount corresponding to the number of containers, are placed in boxes of cardboard corrugated / - a packet of polyethylene

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Shelf life:

Shelf life. 2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001226

Date of registration:16.11.2011

The owner of the registration certificate:The Belarusian-Dutch joint venture FARMLEND, LLCThe Belarusian-Dutch joint venture FARMLEND, LLC Republic of Belarus

Manufacturer: & nbsp

"Belarusian-Dutch joint venture LLC" FARMLEND "" Republic of Belarus

Representation: & nbspPOLIFARM, LLCPOLIFARM, LLC

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)