Trental pills 100mg, 60pcs

Composition

Active ingredients:

pentoxifylline 100 mg.

Auxiliary substances:

lactose,

starch,

talc,

colloidal silicon dioxide,

magnesium stearate.

Shell composition:

methacrylic acid copolymer,

sodium hydroxide,

macrogol (polyethylene glycol) 8000,

talc,

titanium dioxide (E171).

Pharmacological action

Pharmacodynamics

A drug that improves microcirculation, an angioprotector, a derivative of xanthine. Trental improves the rheological properties of blood (fluidity) by affecting the pathologically altered deformability of red blood cells, inhibiting platelet aggregation and reducing the increased blood viscosity. Improves microcirculation in areas of impaired blood circulation.

The mechanism of action of pentoxifylline is associated with inhibition of phosphodiesterase and accumulation of cAMP in vascular smooth muscle cells and blood cells.

Having a weak myotropic vasodilating effect, pentoxifylline slightly reduces OPSS and slightly dilates the coronary vessels.

Treatment with Trental leads to an improvement in the symptoms of cerebral circulatory disorders.

Treatment success in cases of occlusive peripheral artery disease (e. g. intermittent claudication) is shown by lengthening the walking distance, eliminating nocturnal cramps in the calf muscles, and eliminating pain at rest.

Pharmacokinetics

Suction

After oral use, pentoxifylline is almost completely absorbed from the gastrointestinal tract.

Bioavailability is on average 19%.

Metabolism

The main pharmacologically active metabolite of 1-(5-hydroxyhexyl) – 3,7-dimethylxanthine is determined in plasma at a concentration exceeding 2 times the concentration of the unchanged substance, and is in a state of reversible biochemical equilibrium with it. For this reason, pentoxifylline and its metabolite should be considered as an active whole, therefore, it can be considered that the bioavailability of the Active ingredient is significantly higher. Pentoxifylline is completely biotransformed in the body.

The elimination

of T1 / 2 pentoxifylline is 1.6 hours.

More than 90% is excreted by the kidneys as unconjugated water-soluble polar metabolites.

Pharmacokinetics in special clinical cases

In patients with severe renal impairment, the excretion of metabolites is slowed.

In patients with impaired liver function, an elongation of T1/2 of pentoxifylline and an increase in its bioavailability were noted.

Indications

• Violations of the peripheral circulation of atherosclerotic (for example intermittent claudication);
• diabetic angiopathy;
• trophic disorders (e. g. leg ulcers, gangrene);
• cerebrovascular disease (consequences of cerebral atherosclerosis, as, for example, impaired concentration, dizziness, memory loss);
• ischemic and post-stroke conditions
• of circulatory disorders in the retina and choroid;
• otosclerosis;
• degenerative changes in the background of the pathology of the vessels of the inner ear and hearing loss.

Contraindications

• Hypersensitivity to the components of the drug;
• massive bleeding;
• extensive retinal hemorrhages;
• brain hemorrhages;
• acute myocardial infarction;
• age up to 18 years;
• pregnancy and lactation (breastfeeding);
• hypersensitivity to other methylxanthines.

Use with caution in patients with: severe cardiac arrhythmias (risk of worsening arrhythmia), hypotension (risk of further lowering blood pressure), chronic heart failure, gastric and duodenal ulcers, impaired renal function – creatinine clearance less than 30 ml/min (risk of accumulation and increased risk of side effects), severe hepatic impairment (risk of accumulation and increased risk of side effects), increased tendency to bleeding, including as a result of the use of anticoagulants or in case of disorders of the blood coagulation system (risk of more severe bleeding), after recent surgical interventions.

Side effects

From the central nervous system: headache, dizziness, anxiety, sleep disorders, convulsions; very rarely-aseptic meningitis.

Dermatological reactions: hyperemia of the skin of the face, flushes of blood to the skin of the face and upper chest, edema, increased fragility of nails.

From the digestive system: xerostomia, anorexia, intestinal atony, feeling of pressure and overflow in the stomach, nausea, vomiting, diarrhea; in some cases-intrahepatic cholestasis and increased activity of hepatic transaminases (AST, ALT), alkaline phosphatase (alkaline phosphatase).

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

Hematopoietic disorders: leukopenia, thrombocytopenia, pancytopenia, bleeding from the vessels of the skin, mucous membranes, stomach, intestines, hypofibrinogenemia.

From the side of the organ of vision: visual impairment, scotoma.

Allergic reactions: pruritus, hyperemia of the skin, urticaria, angioedema, anaphylactic shock.

Side effects are possible with the use of Trental in high doses.

Interaction

Pentoxifylline can enhance the effect of drugs that reduce blood pressure (ACE inhibitors, nitrates).

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins).

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

Co-use with other xanthines can lead to excessive nervous excitement.

The hypoglycemic effect of insulin or oral hypoglycemic agents may be increased when taking pentoxifylline (increased risk of hypoglycemia). If combination therapy is necessary, strict monitoring of the patient’s condition is required.

In some patients, simultaneous use of pentoxifylline and theophylline may lead to an increase in the concentration of theophylline in the blood plasma. This may lead to an increase or increase in the side effects associated with theophylline.

How to take, course of use and dosage

The dose is set individually, in accordance with the characteristics of the patient.

The drug is prescribed orally at 100 mg (1 tab. ) 3 times / day, followed by a gradual increase in the dose to 200 mg 2-3 times/day. The maximum single dose is 400 mg. The maximum daily dose is 1200 mg. Tablets should be swallowed whole during or immediately after a meal, washed down with a sufficient amount of water.

In patients with impaired renal function (creatinine clearance less than 30 ml/min), the dose should be reduced to 1-2 tablets/day.

In patients with severe hepatic impairment, it is necessary to reduce the dose, taking into account individual tolerability of the drug.

In patients with low blood pressure, as well as in those who are at risk due to a possible decrease in blood pressure (patients with severe CHD or with hemodynamically significant cerebral vascular stenosis), treatment can be started in small doses, in these cases the dose should be increased gradually.

Overdose

Symptoms: nausea, dizziness, tachycardia, decreased blood pressure, arrhythmia, hyperemia of the skin, chills, loss of consciousness, areflexia, tonic-clonic convulsions.

Treatment: if necessary, conduct symptomatic therapy. The patient should be given a horizontal position with raised legs. The specific antidote is unknown. They monitor the vital functions of the body and general measures aimed at maintaining them, monitor the patency of the respiratory tract. For convulsions – diazepam.

Special instructions

Use in patients with liver function disorders

In patients with severe hepatic impairment, the T1/2 of pentoxifylline increases. Use the drug with caution in patients with severe hepatic impairment (risk of accumulation and increased risk of side effects).

Use in patients with impaired renal function

In severe renal impairment, the excretion of metabolites is slowed down. Use the drug with caution in patients with impaired renal function-creatinine clearance less than 30 ml / min (risk of accumulation and increased risk of side effects).

Special instructions

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

In patients with diabetes mellitus who take hypoglycemic agents, the use of the drug in high doses may cause severe hypoglycemia (dose adjustment is required).

When prescribed simultaneously with anticoagulants, it is necessary to carefully monitor the parameters of the blood coagulation system.

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit levels is necessary.

In the elderly, it may be necessary to reduce the dose (increase bioavailability and decrease the rate of elimination).

Smoking may reduce the therapeutic effectiveness of the drug.

Use in pediatrics

The safety and efficacy of pentoxifylline in children are poorly understood.

Form of production

Enteric film-coated tablets

Storage conditions

Store in a dry place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 4 years.

Active ingredient

Pentoxifylline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets