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

Pharmacodynamics:Reduction in the concentration of fibrinogen in the blood plasma and inhibition of aggregation of erythrocytes and platelets, followed by a decrease in blood viscosity, an improvement in the elasticity of red blood cells (probably by inhibiting phosphodiesterase and subsequent accumulation of cAMP in erythrocytes), microcirculation and tissue oxygenation.

Pharmacokinetics:Absorption from the gastrointestinal tract is fast and complete (more than 95%).A pronounced (60-70%) effect of the first passage through the liver is characteristic. Admission with food slows down absorption (but does not affect its degree) and reduces the concentration of the drug in the blood plasma. It is distributed in the body evenly. It binds to the erythrocyte membrane. Penetrates into breast milk. Elimination by the kidneys (94% - in the form of metabolites, mainly metabolite V) and with feces (less than 4%). During the first 4 hours, up to 90% of the dose is withdrawn. With severe renal dysfunction, the elimination of metabolites is slowed down, if the liver function is impaired, the half-life is prolonged and bioavailability is increased.

Indications:Violation of peripheral blood circulation (including obliterating endarteritis, diabetic angiopathy, Raynaud's disease).

Atherosclerotic and discirculatory angiopathy, angioneuropathy.

Trophic tissue disorders (including varicose veins, trophic ulcers of the lower leg, gangrene, frostbite, post-thrombotic syndrome).

Violation of cerebral circulation (the consequences of cerebral atherosclerosis, for example, reduced concentration, dizziness, memory impairment), ischemic and post-insult conditions.

Disturbance of blood circulation in the retina and choroid of the eye.

Otosclerosis, degenerative changes on the background of the pathology of the vessels of the inner ear and hearing loss.

ICD-10

V.F80-F89.F81 Specific developmental disorders of teaching skills

V.F90-F98.F90.0 Violation of activity and attention

VII.H30-H36.H31.9 Vascular disease, unspecified

VII.H30-H36.H35.9 Retinal disease, unspecified

VIII.H80-H83.H80 Otosclerosis

VIII.H80-H83.H83.9 Disease of inner ear, unspecified

VIII.H90-H95.H91.9 Hearing loss, unspecified

IX.I60-I69.I63 Cerebral infarction

IX.I60-I69.I67.9 Cerebrovascular disease, unspecified

IX.I60-I69.I69.4 The consequences of a stroke, not specified as a hemorrhage or a cerebral infarction

IX.I60-I69.I69.8 Consequences of other and unspecified cerebrovascular diseases

IX.I70-I79.I73.0 Raynaud's syndrome

IX.I70-I79.I73.8 Other specified diseases of peripheral vessels

IX.I70-I79.I79.2 * Peripheral angiopathy in diseases classified elsewhere

IX.I80-I89.I83 Varicose veins

IX.I80-I89.I86 Varicose veins of other sites

IX.I80-I89.I87.0 Postphlebitic syndrome

IX.I95-I99.I99 Other and unspecified disorders of the circulatory system

XII.L80-L99.L89 Decubital ulcer

XVIII.R00-R09.R02 Gangrene, not elsewhere classified

XVIII.R40-R46.R42 Dizziness and dizziness

Contraindications:Hypersensitivity, including other methylxanthine derivatives (caffeine, theophylline, theobromine).

Hemorrhagic stroke.

Massive hemorrhage.

Extensive hemorrhage in the retina of the eye.

Acute myocardial infarction.

Pregnancy, breast-feeding.

For intravenous administration (additionally): arrhythmia, marked atherosclerosis of the coronary or cerebral arteries, uncontrolled arterial hypotension.

Carefully:Lability of blood pressure (propensity to arterial hypotension).

Chronic heart failure.

Stomach ulcer and duodenal ulcer.

Violation of kidney function (clearance less than 30 ml / min).

Severe liver dysfunction.

Recently suffered surgery, increased tendency to bleeding.

Age under 18 years (safety and efficacy not determined).

Pregnancy and lactation:The action category for the fetus is FDA - C. The drug is contraindicated in pregnancy and breastfeeding.

Dosing and Administration:Inside, the initial dose: 600 mg per day in 2-3 divided doses; As the condition improves, they switch to maintenance doses: 100 mg 3 times a day; course of treatment 2-3 weeks or more.

Intravenously, intraarterially, intramuscularly.Doses and treatment regimens are set individually.

Side effects:Nervous system and sensory organs: headache, dizziness, anxiety, sleep disturbances, convulsions, vision disorders, scotoma; very rarely - aseptic meningitis.

The cardiovascular system: tachycardia, cardialgia, arrhythmia, angina progression, lowering of arterial pressure

Blood: leukopenia, pancytopenia, thrombocytopenia, hypofibrinogenemia.

Digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, increased activity of hepatic enzymes.

Leather: hyperemia of the skin of the face, flushing of the blood to the face and upper chest, swelling, increased brittleness of the nails.

Allergic reactions: itching, hyperemia of the facial skin, hives, angioedema, anaphylactic shock.

For tablets additionally: feeling of pressure and overflow in the area of the stomach, nausea, vomiting, diarrhea.

Overdose:When an overdose is observed, weakness, dizziness, lower blood pressure, a sensation of hot flashes, drowsiness or agitation, impaired consciousness, convulsions.

Treatment: gastric lavage, the appointment of activated charcoal, anticonvulsants, maintenance of vital functions.

Interaction:Anticoagulants, derivatives of coumarin or indanedione, heparin sodium, agents that affect platelet function and / or cause hypoprothrombinemia (cefamandol, cefoperazone, cefotetan, plikamycin, valproic acid), other inhibitors of platelet aggregation (abciximab, alprostadil, acetylsalicylic acid), valproate, valproic acid, water-soluble radiocontrast agents (for intravascular administration), dextrans, dipyridamole, clopidogrel, mezlocillin, non-steroidal anti-inflammatory drugs, piperacillin, sulfinpyrazone, ticarcillin, ticlopidine, tirofiban, thrombolytic agents, cephalosporins, eptifibatide - pentoxifylline inhibits platelet aggregation and prolongs prothrombin time and bleeding time; may increase the risk of bleeding with concomitant use; should be combined with caution; it is necessary to monitor more carefully any signs of bleeding and more often to determine prothrombin time.

Increased antihypertensive effect when used simultaneously with antihypertensive drugs; a dose adjustment of an antihypertensive agent may be required.

Pentoxifylline enhances the effectiveness of insulin and sugar reducing agents taken internally.

Cimetidine significantly increases Css of pentoxifylline in the blood plasma, which can increase the incidence of side effects with parallel application.

Because the pentoxifylline is not a peripheral vasodilator, nicotine, being a vasoconstrictor, can influence its therapeutic effect and worsen the patient's condition; recommend refraining from smoking during treatment.

With the simultaneous use of sympathomimetics and other xanthines, hyperstimulation of the central nervous system is possible.

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

Special instructions:In case of violations of kidney function or severe violations of liver function, correction of the pentoxifylline dosage regimen is required.

During the treatment period, the level of blood pressure should be monitored.

When used simultaneously with antihypertensive agents, insulin, oral hypoglycemic drugs, a reduction in the dose of pentoxifylline may be required.

When used simultaneously with anticoagulants, blood coagulation should be closely monitored.

Instructions

Pentoxifylline (Pentoxyphyllinum)