TRENTAL 400

Active material: Pentoxifylline
When ATH: C04AD03
CCF: Preparation, improving microcirculation. Angioprotektor
ICD-10 codes (testimony): F07, G45, H31.1, H34, H35.0, H93.0, I63, I67.2, I69, I73.0, I73.1, I73.9, I79.2, I83.2
When CSF: 01.14.01
Manufacturer: AVENTIS PHARMA Ltd. (India)

Pharmaceutical form, composition and packaging

Sustained-release tablets, Film-coated white, oblong, lenticular, Engraved “ATA” one side.

Excipients: povidone (polyvinylpyrrolidone), gietelloza (hydroxyethyl), talc, magnesium stearate.

The composition of the shell: gipromelloza (hydroxypropyl), benzyl alcohol, Titanium dioxide, talc, macrogol (polyethylene glycol) 6000.

10 PC. – blisters (2) – packs cardboard.

Pharmacological action

Preparation, improving microcirculation. Trental^® 400 It improves the rheological properties of blood due to exposure to diseased deformability of red blood cells, inhibiting platelet aggregation and reducing an increased blood viscosity. Trental^® 400 improves microcirculation in areas of impaired circulation.

Active substance formulation – pentoxifylline – a xanthine derivative. The mechanism of action of pentoxifylline associated with the inhibition of phosphodiesterase and cAMP accumulation in vascular smooth muscle cells and blood corpuscles.

It has little myotropic vasodilator effect, slightly reduces round and slightly dilates coronary vessels.

Application Trental^® 400 It leads to improvement of symptoms in cerebral circulatory disorders.

When peripheral arterial occlusive disease (eg, for claudication) the action of the drug is in walking distance of elongation, elimination of night cramps in the calf muscles and the disappearance of pain at rest.

Pharmacokinetics

Absorption

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

Bioavailability is an average of 19 ± 13%.

Metabolism

The main pharmacologically active metabolite 1-(5-gidroksigeksil)-3,7-theobromine determined in plasma concentration, exceeding the 2 fold concentration of the unchanged substance (pentoxifylline), and it is with him in a state of reversible biochemical equilibrium. For this reason, pentoxifylline and its metabolite should be regarded as the active unit, Consequently, it could be considered, The bioavailability of the active substance is considerably higher.

Pentoxifylline completely biotransformed in the body.

Deduction

T_1/2 pentoxifylline is 1.6 no.

More 90% excreted by the kidneys in the form of water-soluble non-conjugated metabolites.

Pharmacokinetics in special clinical situations

In patients with severely impaired renal function excretion of metabolites delayed.

In patients with impaired liver function observed elongation T_1/2 pentoxifylline and increase its bioavailability.

Testimony

- Peripheral circulatory disorders of atherosclerotic (eg, intermittent claudication), diabetic angiopathy, trophic disorders (eg, leg ulcers, gangrene);

- Cerebrovascular accident (the effects of cerebral arteriosclerosis, as, eg, impaired concentration, dizziness, memory impairment), ischemic and post stroke status;

- Circulatory disorders in the retina and choroid;

- Otosclerosis, degenerative changes in the background of vascular pathology of the inner ear and hearing loss.

Dosage regimen

Establish individually.

The average dose for oral administration is 400 mg (1 tab.) 2-3 times / day. The maximum daily dose – 1200 mg (3 tab.).

The tablets are completely, without chewing, during or immediately after a meal, drinking plenty of water.

In patients with severe renal impairment (CC less than 30 ml / min) dose can be reduced to 400-800 mg / day.

In Patients with liver failure reduce the dose, taking into account individual tolerance.

In patients with arterial hypertension, and in individuals, at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenosis of cerebral vessels) Treatment can be initiated with small doses. In these cases, an increase in dose should be gradual.

Side effect

CNS: headache, dizziness, anxiety, sleep disorders, convulsions; rarely – aseptic meningitis.

Dermatological reactions: facial flushing, rush of blood to the face and upper chest, swelling, increased brittleness of nails.

From the digestive system: xerostomia, anorexia, bowel atony, a feeling of pressure and fullness in the stomach, nausea, vomiting, diarrhea; rarely – intrahepatic cholestasis, increase in liver transaminases, Alkaline phosphatase.

Cardio-vascular system: tachycardia, arrhythmia, kardialgija, progression of angina, decrease in blood pressure.

From the hematopoietic system: leukopenia, thrombocytopenia, pancytopenia.

From the blood coagulation system: bleeding from vessels in the skin, mucosas, stomach, bowel, fibrinopenia.

From the senses: blurred vision, scotoma.

Allergic reactions: itch, dermahemia, hives, angioedema, anaphylactic shock.

Side effects occur when using Trental^® 400 high dose.

Contraindications

- Acute myocardial infarction;

- Massive bleeding;

- Bleeding in the brain;

- Massive retinal hemorrhage;

- Pregnancy;

- Lactation (breast-feeding);

- Childhood and adolescence up 18 years;

- Hypersensitivity to the drug.

- Hypersensitivity to other methylxanthine derivatives.

FROM caution the drug should be used in patients with severe arrhythmias (the risk of worsening of arrhythmia); hypotension (the risk of further reduction in blood pressure); chronic heart failure; gastric ulcer and duodenal ulcer; impaired renal function (CC less than 30 ml / min) (the risk of accumulation and an increased risk of side effects); severe hepatic impairment (the risk of accumulation and an increased risk of side effects); after recently undergone surgeries; with a tendency to bleeding, eg, as a result of the use of anticoagulants or violations on the part of the blood coagulation system (the risk of more severe bleeding).

Pregnancy and lactation

The drug is contraindicated during pregnancy.

If necessary, use during lactation should stop breastfeeding.

Cautions

Treatment should be under the control of blood pressure.

In patients with diabetes, taking hypoglycemic agents, use of the drug at high doses can cause pronounced hypoglycemia (Dosage adjustment).

When assigning simultaneously with anticoagulants should be carefully monitored parameters of blood coagulation.

Patients, recently underwent surgery, requires systematic monitoring of the level of hemoglobin and hematocrit.

In patients with low and unstable blood pressure dose should be reduced.

Elderly patients may require a dose reduction (increased bioavailability and reduced clearance rate of pentoxifylline).

The safety and efficacy of pentoxifylline in children are not well understood.

Smoking may reduce the therapeutic efficacy of the drug.

Overdose

Symptoms: increased perspiration, nausea, cyanosis, dizziness, tachycardia, decrease in blood pressure, arrhythmia, flushing of the skin, chills, loss of consciousness, areflexia, tonic-clonic seizures.

Treatment: cancel product, give the patient a horizontal position with raised legs. Symptomatic therapy, ensuring the maintenance of blood pressure and respiratory function. Care should be free airway. When seizures are administered diazepam.

Drug Interactions

Pentoxifylline increases the effects of drugs, lowering blood pressure (ACE inhibitors, nitrates).

Pentoxifylline may increase the effects of drugs, influencing blood clotting (indirect and direct anticoagulants, thrombolytics), antibiotics (incl. cephalosporins).

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

Co-administration with other xanthines may cause excessive nervous excitement.

Hypoglycemic effect of insulin or hypoglycemic drugs can be enhanced while taking pentoxifylline (an increased risk of hypoglycaemia). Such patients require strict clinical monitoring.

With simultaneous use of pentoxifylline and theophylline may increase the concentration of theophylline in plasma and increased side effects of theophylline.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry place at temperatures no higher than 25 ° C. Shelf life – 4 year.