2010/06/14

Pentoxifylline

International name:
Pentoxifylline (Pentoxifylline)

Group Affiliation:
Vasodilating means

Description of the active substance (INN):
Pentoxifylline

Dosage form:
tablets, capsules, concentrate for solution for intravenous and intraarterial administration, concentrate for solution for infusion, the solution for intravascular injection, tablets, tablets coated with enteric shell

Mode of action:
Spasmolytic of the group of purines. It improves the microcirculation and blood rheology, inhibits PDE and increases the concentration of cAMP in platelets and ATP in erythrocytes with simultaneous saturation of energy potential, which in turn leads to vasodilation, reduced TPVR, ascending CRM and IOC, with no significant change in heart rate. Expanding the coronary arteries, increases delivery of oxygen to the myocardium (antianginal effect), pulmonary vessels - improves blood oxygenation. increases the tone of respiratory muscles (intercostal muscles and diaphragm). In / in the introduction, along with the steps above, leads to increased collateral circulation, increase the volume of blood flowing through the unit section. Increasing the concentration of ATP in the brain, a positive effect on the bioelectrical activity of the CNS. Reduces blood viscosity, causes disaggregation of platelets, increases the elasticity of red blood cells (due to the impact on pathologically altered deformability of red blood cells). It improves the microcirculation in areas of disturbed blood supply. In peripheral arterial occlusive lesion ("intermittent" claudication) leads to a lengthening of the distance away, the elimination of night cramps calf muscle pain at rest.

Indications:
Violations of the peripheral circulation ("intermittent" claudication on the background of diabetic angiopathy, obliterative endarteritis), Raynaud's disease, a violation trophic tissue (postthrombotic syndrome, varicose veins, leg sores, gangrene, frostbite), ischemic: ischemic and postapopleksicheskie state; cerebral atherosclerosis (dizziness, headache, memory impairment, sleep disturbance), discirculatory encephalopathy, viral neuro (prevention of possible violations of microcirculation) coronary heart disease, post myocardial infarction, acute disorders of blood circulation in the retina and choroid, otosclerosis, degenerative changes in the background vascular pathology of the inner ear with a gradual decrease in hearing, COPD, asthma, impotence of vascular origin.

Contraindications:
Hypersensitivity to pentoxifylline and other xanthine derivatives; acute myocardial infarction; porphyria, massive bleeding, hemorrhagic stroke, bleeding in the retina, pregnancy and lactation. For iv injection (optional) - arrhythmias, marked atherosclerosis of the coronary or cerebral arteries, uncontrolled Arterial gipotenziya.C caution. Lability of blood pressure (tendency to arterial hypotension), chronic heart failure, peptic ulcer and 12 duodenal ulcer (Oral), state after recently migrated surgical interventions, liver and / or renal failure, age 18 years (effectiveness and safety have not been studied) .

Adverse effects:
Of the nervous system: headache, dizziness, anxiety, sleep disorders; cramps. On the part of the skin and subcutaneous fat: flushing facial skin, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails. On the part of the digestive system: dry mouth, loss of appetite, intestinal aggravation cholecystitis, cholestatic hepatitis. On the part of the senses: blurred vision, scotoma. On the part of the SSA: tachycardia, arrhythmia, false angina, progression of angina, lower blood pressure. From the side of hematopoiesis and hemostasis system: thrombocytopenia, leukopenia, pancytopenia, fibrinopenia, bleeding from the vessels of the skin, mucous membranes, stomach, intestines. Allergic reactions: itching, skin flushing, urticaria, angioedema, anaphylactic shock. Laboratory indicators: increase in activity of "liver" transaminase (ALT, AST, LDH) and SchF.Peredozirovka. Symptoms: weakness, dizziness, lowering of blood pressure, fainting, tachycardia, drowsiness or agitation, loss of consciousness, hyperthermia, arefleksiya, tonic-clonic seizures, signs of gastrointestinal bleeding (vomiting type "coffee grounds"). Treatment: gastric lavage followed oral administration of activated charcoal, symptomatic therapy (including measures to maintain respiration and blood pressure), urgent measures for bleeding.

Dosage and administration:
V / a and / v (the patient must be in a position of "lying"), in / m, inside. Patients with chronic renal failure (CC <10 mL / min) designate 50-70% of the normal dose. V / in a slow, 50 mg per 10 ml of 0.9% solution of NaCl (for 10 min), followed by infusion at a dose of 100 mg in 250 - 500 ml 0.9% NaCl solution or 5% dextrose (the length of the introduction - 90-180 min.) V / A - first dose of 100 mg in 20-50 ml 0.9% solution of NaCl, but in the next few days - 200-300 mg in 30-50 ml of solvent (the rate of introduction - 10 mg / min). V / m deep - at 100-200 mg 2-3 times a day. In parallel with parenteral appointment can be given orally, in doses of up to 800-1200 mg / day for 2-3 reception after the meal. Tablets, enteric-coated shell, swallow whole, washed down with sips of water. The daily dose is divided into 3. Initial dose - 600 mg / day. With the improvement of the dose can be reduced to 300 mg / day. Prolonged dosage forms prescribed 2-3 times a day.

Cautions:
Treatment should be under the control of blood pressure. In patients with diabetes receiving hypoglycemic drugs, the appointment in large doses can cause pronounced hypoglycemia (required dosage adjustment). In the appointment along with anticoagulants should be monitored closely for indicators of the blood coagulation system. Patients who had undergone recent rapid intervention, a systematic control of Hb and hematocrit. Commissioned dose should be reduced in patients with low and unstable blood pressure. Older people may need to decrease dose (increased bioavailability and reduced clearance rate). The safety and efficacy of pentoxifylline in children are not well understood. Tobacco smoke can reduce the therapeutic efficacy of the drug. pentoxifylline solution compatible with the infusion solution should be checked in each case. In conducting in / infusion, the patient should be in position "lying".

Interaction:
Pentoxifylline may exacerbate the effects of drugs that affect blood clotting (indirect and direct anticoagulants, thrombolytics), anitibiotikov (including cephalosporins - tsefamandola, tsefaperazona, tsefotetana), valproic acid. It increases the effectiveness of antihypertensive drugs, insulin and oral hypoglycemic drugs. cimetidine increases the concentration of pentoxifylline in the plasma (the risk of side effects). Joint appointment with other xanthine may lead to excessive nervous excitement patients.