Trental 400,400 mg 20 pcs

Pharmacodynamics

The drug improving microcirculation, angioprotector, xanthine derivative. Trental improves rheological properties of the blood (fluidity) due to influence on pathologically changed deformability of erythrocytes, inhibiting platelet aggregation and reducing high blood viscosity. It improves microcirculation in the areas of disturbed blood circulation.

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

With a weak myotropic vasodilatory effect, pentoxifylline slightly decreases RPS and slightly dilates coronary vessels.

The treatment with Trental leads to improvement of the symptomatology of cerebral circulatory disorders.

The success of treatment in peripheral arterial occlusive disease (e.g., intermittent claudication) is seen in prolongation of walking distance, elimination of night cramps in the calf muscles and disappearance of pain at rest.

Pharmacokinetics

Intake

After oral administration pentoxifylline is almost completely absorbed from the GI tract.

Bioavailability averages 19%.

Metabolism

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

The T1/2 of pentoxifylline is 1.6 h.

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

Pharmacokinetics in special clinical cases

The excretion of metabolites is delayed in patients with severe renal impairment.

In patients with impaired hepatic function, prolongation of T1/2 of pentoxifylline and increased bioavailability have been noted.

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

pentoxifylline 400 mg.

How to take, the dosage

The average oral dose is 400 mg (1 tablet) 2 to 3 times a day. Maximum daily dose is 1200 mg (3 tablets).

The tablets are taken whole, without chewing, with or immediately after a meal, with plenty of water.

In patients with significant renal dysfunction (CKR less than 30 ml/min) the dose may be reduced to 400-800 mg/day.

In patients with hepatic impairment the dose of the drug is adjusted individually.

Interaction

When used together, Trental potentiates the effect of a number of antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

The simultaneous use of pentoxifylline and theophylline may lead to an increase in blood levels of theophylline and increase its side effects.

Special Instructions

Close monitoring is necessary in patients with significant cardiac rhythm disturbances (risk of worsening arrhythmia), with arterial hypotension (risk of further BP decrease), renal dysfunction with a CKR less than 30 ml/min (risk of cumulation and increased risk of side effects), Severe liver dysfunction (risk of cumulation and increased risk of side effects) and increased susceptibility to bleeding, such as with anticoagulants or clotting disorders (risk of more severe bleeding).

We should be careful when prescribing Trental for patients with a history of gastric and duodenal ulcer; patients who have recently undergone surgery (increased risk of bleeding, in connection with which systematic control of hemoglobin and hematocrit levels is necessary).

Patients with arterial hypotension and labile circulation require parenteral administration of Trental gradually, since BP may decrease (up to and including collapse), and in some cases – angina pectoris attacks.

Patients with heart failure require appropriate treatment to compensate blood circulation. At the same time, large volume of fluids should be avoided.

In patients with impaired renal function the dosing regimen should be adjusted individually.

Contraindications

With caution, use in patients with: severe cardiac rhythm disturbances (risk of worsening arrhythmia), arterial hypotension (risk of further BP decline), chronic heart failure, gastric and duodenal ulcer disease, renal impairment – CKR less than 30 ml/min (risk of cumulation and increased risk of side effects), severe liver function disturbances (risk of cumulation and increased risk of side effects), increased tendency to bleeding, incl.as a result of anticoagulant use or in case of disorders of the blood coagulation system (risk of more severe bleeding), after recent surgical interventions.

Side effects

When using Trental 400 in high doses there may be “flushes” (redness of the face or a feeling of heat), disorders of the digestive system, such as a feeling of pressure and overflow in the stomach, nausea, vomiting, diarrhea; very rarely – heart rhythm disorders (tachycardia).

CNS disorders: dizziness, headache, agitation, sleep disturbances are possible; very rare – cases of aseptic meningitis.

Allergic reactions: sometimes – itching, skin hyperemia, urticaria; rarely – severe anaphylactic/anaphylactoid reactions with the development of angioedema, bronchospasm, and even shock.

Digestive system disorders: very rarely – increase of liver transaminases activity, intrahepatic cholestasis.

With the coagulative system: very rarely – thrombocytopenia; in patients with increased tendency to bleeding – bleeding (eg, from vessels of the skin, mucous membranes, stomach, intestines).

Cardiovascular system disorders: very rarely – angina pectoris attacks, tachycardia, arterial hypotension.

Overdose

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

Treatment: if necessary symptomatic therapy is carried out.

The patient should be put in horizontal position with elevated legs.

The specific antidote is unknown.

Vital body functions are monitored and general measures are taken to maintain them, airway patency is monitored; diazepam is used for seizures.

Similarities