Pentoxifylline | Pentoxifylline tablets 0.1 g, 60 pcs.

packaging 60 pcs

Pharmacological action

Pentoxifylline is a xanthine derivative. Improves microcirculation and rheological properties of blood. The mechanism of action is associated with inhibition of phosphodiesterase and an increase in the content of cyclic 3,5 adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (ATP) in red blood cells with simultaneous saturation of the energy potential, which in turn leads to vasodilation and a decrease in total peripheral vascular resistance, an increase in systolic and minute blood volume without a significant change in heart rate. Expanding the coronary arteries, increases oxygen delivery to the myocardium (a slight antianginal effect), lung vessels - improves blood oxygenation.

When administered intravenously, it leads to increased collateral circulation, an increase in the volume of flowing blood through a unit section.

Reduces blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (due to the impact on pathologically altered deformability of red blood cells). Improves microcirculation in areas of impaired circulation.

In case of occlusive lesion of peripheral arteries ("intermittent" lameness), it leads to an increase in walking distance, elimination of night cramps of calf muscles and pain at rest.

Pharmacokinetics

The drug is rapidly metabolized in the liver after administration. In the process of metabolism, two main metabolites are formed: 1- (5-hydroxyhexyl) -3,7-dimethylxanthine (metabolite I) and 1- (3-carboxypropyl) -3,7-dimethylxanthine (metabolite V), which have similar pentoxifylline activity . 1.5-2 hours after infusion, the concentration of metabolites I and V in the blood plasma is 5 and 8 times higher than the concentration of the starting substance, respectively. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood is significantly reduced (up to 10% of the initial).

Elimination half-life from 30 minutes to 1.5 hours. It is excreted mainly by the kidneys (94%) in the form of metabolites (mainly metabolite V), by the intestines (4%). in the first 4 hours, up to 90% of the dose is excreted. In unchanged form, 2% of the drug is excreted. Pentoxifylline and its metabolites do not bind to plasma proteins.

Excreted in breast milk.

In severe renal impairment, excretion of metabolites is slowed down. In case of impaired liver function, an elimination half-life and increased bioavailability are noted.

Indications

peripheral circulatory disorders caused by atherosclerosis, diabetes mellitus (diabetic angiopathy)

chronic cerebrovascular disorders ischemic

atherosclerotic and discirculatory encephalopathy disorders, angiopathy or pulmonary arteriofiriopathy disorders (venereal fibrosis or parasitic fibrosis) postthrombophlebitis syndrome, frostbite, gangrene)

acute endarteritis

acute, subacute Secondary and chronic circulatory failure in the retina or choroid of the eye

hearing impairment of vascular origin.

Contraindications

Hypersensitivity to pentoxifylline, other derivatives of methylxanthine or other ingredients of the finished dosage form, Porphyria

acute myocardial infarction

massive hemorrhage

retinal hemorrhage

cerebral hemorrhage, acute hemorrhagic stroke

severe coronary or cerebral atherosclerosis

severe cardiac arrhythmias

long-term pregnancy and gestational age 18 years of gestation .

Caution: the drug is prescribed for patients with cerebral and / or coronary arteriosclerosis, especially in cases of arterial hypotension and cardiac arrhythmias, heart failure, and liver failure. Caution should also be exercised when prescribing Pentoxifylline to patients with peptic ulcer of the stomach and duodenum, to patients who have recently undergone surgery (risk of bleeding).

Pregnancy and lactation

Pregnancy and lactation are contraindicated.

Composition

1 tablet contains:

Active substance: pentoxifylline (in terms of 100% substance) - 100 mg srdl kp Excipients: stearic acid, potato starch, water-soluble methyl cellulose, lactose (milk sugar), povidone (low molecular weight polyvinylpyrrolidone medical)

Shell composition: cellacephate (acetylphthalyl cellulose), titanium dioxide, castor oil, liquid paraffin (liquid petrolatum), azorubine (acid red 2C), talc, beeswax

Dosage and Administration

Inside after a meal. The tablets are coated with a special membrane, soluble in the intestine, so they are swallowed whole, washed down with a small amount of water. Take 0.2 g (2 tablets) 3 times a day. After achieving a therapeutic effect (usually 1-2 weeks), the dose is reduced to 0.1 g (1 tablet) 3 times a day.

The maximum daily dose is 1200 mg. The course of treatment is 1-3 months.

In patients with chronic renal failure (creatine clearance less than 10 ml / min.), the dose is halved.

The duration of treatment and the dosage regimen of pentoxifylline is determined individually by the attending physician, depending on the clinical picture of the disease and the resulting therapeutic effect.

Side effects

From the central nervous system: headache, dizziness, anxiety, sleep disturbances cramps.

From the skin and subcutaneous fat: hyperemia of the skin, flushing of the face and upper chest, swelling, increased fragility of the nails.

From the digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.

On the part of the sensory organs: impaired vision, scotoma.

From the cardiovascular system: tachycardia, arrhythmia, cardialgia, angina progression, lowering blood pressure.

From the hemopoietic organs and the hemostatic system: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia of bleeding from blood vessels of the skin, mucous membranes. stomach, intestines.

Allergic reactions: itching, flushing of the skin, urticaria, angioedema, anaphylactic shock.

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

Drug interaction

Pentoxifylline enhances heparin action, fibrinolytic drugs, theophylline, antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

Pentoxifylline can increase the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetane), valproic acid.

Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects).

Co-administration with other xanthines can lead to excessive nervous excitation of patients.

Overdose

Symptoms: nausea, dizziness, cyanosis, tachycardia, marked decrease in blood pressure, reddening of the skin, fever (agitation), agitation, areflexia, tonico-clonic, and tonic-clonitic sunoid

Treatment: symptomatic. Particular attention should be paid to maintaining blood pressure and respiratory function. Convulsions are removed with the introduction of diazepam. Urgent measures in the event of severe anaphylactic reactions (shock): when the primary signs (sweating, nausea, cyanosis) immediately discontinue

in addition to other necessary measures provide a lower position of the head and upper torso and provide the freedom to breathe

urgent medical measures: enter / into epinephrine (adrenaline). If necessary, the introduction of epinephrine can be repeated.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25 РC.

Expiration

2 Year

dosage form

dosage form

tablets

Organics, Russia