Trental - instructions for use, dose, side effects, contraindications

Sheath: methacrylic acid copolymer-1 1.45 mg, sodium hydroxide - 0.168 mg, macrogol (polyethylene glycol) 8000 - 1.40 mg, talc - 0.388 mg, titanium dioxide (E 171) - 1.272 mg.

Description:

round biconvex tablets, coated with a white coating.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Preparation Trental® decreases blood viscosity and improves the flow properties of the blood (flowability) due to:

- Improvements impaired deformability of erythrocytes;

- reduce aggregation of platelets and erythrocytes;

- Reducing the concentration of fibrinogen;

- a decrease in the activity of leukocytes and a decrease in the adhesion of leukocytes to the vascular endothelium.

As an active substance, the preparation Trental® contains a xanthine derivative - pentoxifylline. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in the cells of the smooth muscles of blood vessels and blood cells.

Having a weak myotropic vasodilator effect, pentoxifylline somewhat reduces the overall peripheral vascular resistance and slightly dilates the coronary vessels.

Pentoxifylline has a weak positive inotropic effect on the heart.

Improves microcirculation in areas of impaired blood circulation. Treatment with Trental^® leads to an improvement in the symptoms of disorders cerebral blood circulation.

With occlusive diseases of peripheral arteries, the use of Trental® leads to lengtheningthe distance of walking, the elimination of nocturnal cramps in the gastrocnemius muscles and the disappearance of pain at rest.

Pharmacokinetics:

After oral administration pentoxifylline quickly and almost completely absorbed.

Pentoxifylline effect of the "primary" passage through liver. Absolute the bioavailability of the starting substance is 19 ± 13%. The concentration of the main active metabolite 1- (5- hydroxyhexyl) -3,7-dimethyl xanthine (metabolite I) in blood plasma in two times the concentration of the original pentoxifylline.

Metabolite I is found with peptoxifylline in reversible biochemical redox equilibrium. therefore pentoxifylline and metabolite 1 are considered together as the active unit. As a consequence, the availability of the active substance is much greater. Half-life pentoxifylline after intravenous administration is 1.6 h.

Pentoxifylline has a large volume distribution (168 liters after the 30-minute infusion of 200 mg) and high clearance of approximately 4500-5100 ml / min.

Pentoxifylline and its metabolites are not bind to blood plasma proteins.

Pentoxifylline completely is metabolized and more than 90% is excreted through the kidneys in the form of unconjugated water-soluble metabolites. Patients with impaired renal function In patients with impaired renal function excretion of metabolites slows down.

Patients with hepatic impairment

In patients with impaired liver function, the half-life of pentoxifylline is prolonged and absolute bioavailability is increased.

Indications:

- Occlusive disease peripheral arteries atherosclerotic or diabetic genesis (for example, "intermittent" lameness, diabetic angiopathy).

- Trophic disorders (for example, trophic ulcers of the shins, gangrene).

- Violations of the brain blood circulation (the consequences of cerebral atherosclerosis, such as a decrease in concentration attention, dizziness, memory impairment), ischemic and post-insult conditions.

- Disturbances of blood circulation in the mesh and choroid of the eye.

- Otosclerosis, degenerative changes on the background of the pathology of the vessels of the inner ear and hearing loss.

Contraindications:Hypersensitivity to pentoxifylline, other methylxanthines or to any auxiliary substance of the preparation.

- Massive bleeding (risk of increased bleeding).

- Extensive hemorrhages in the retina of the eye (the risk of amplification is bleedingand I).

- Hemorrhages in the brain.

- Acute myocardial infarction.

- Age to 18 lay down.

- Pregnancy (insufficient data).

- The period of the breast feeding (not enough data).

- Galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the formulation).

Carefully:

- Severe arrhythmias (risk of worsening of arrhythmia).

- Arterial hypotension (risk further reduce arterial pressure, see section "Method of administration and dose");

- High risk of decline blood pressure (including, with severe ischemic disease hearts or hemodynamically significant stenoses of cerebral vessels).

- Chronic cardiac failure

- Abnormal kidney function (creatinine clearance less than 30 ml / min) (risk of cumulation and an increased risk of side effects, see section "Method of administration and dose").

- Severe violations of liver function (risk of cumulation and an increased risk of side effects, see section "Method of administration and dose").

- Recently transferred surgical interventions.

- Increased tendency to bleeding, for example, as a result of the use of anticoagulants (including indirect anti-coagulant [vitamin K antagonists] or in disorders in the blood coagulation system (risk of developing more severe bleeding), see "Interaction with other drugs" ".

Simultaneous use with hypoglycemic agents (insulin and hypoglycemic agents for oral administration) section "Interaction with other medicines".
- Simultaneous use with ciprofloxacin (see section "Interaction with other drugs").

Pregnancy and lactation:

Pregnancy

The drug Trental® is not recommended for use in pregnancy (as there is not enough data).

Breastfeeding period Pengoksifillin penetrates into breast milk in small amounts.

If necessary, use of the drug should stop breastfeeding (given the lack of experience in the application).

Dosing and Administration:

Dosage is established by the doctor in accordance with the individual characteristics of the patient.

The usual dose is: one tablet of Trental three times a day, followed by a slow increase in the dose to 200 mg 2-3 times a day. The maximum single dose is 400 mg. The maximum daily dose is 1200 mg. The drug should be swallowed whole during or immediately after eating, squeezed with enough water.

In patients with impaired renal function (creatinine clearance below 30 ml / min), the dosage can be reduced to 1-2 tablets per day.

Dose reduction, taking into account individual tolerability, is necessary in patients with severe impairment of liver function.

Treatment can be started in small doses in patients with low blood pressure, as well as in people at risk because of possible lowering of arterial pressure (patients with severe CAD or with hemodynamically significant stenoses of cerebral vessels). In these cases, the dose can be increased only gradually.

Side effects:

The following are secondary reactions that were noted in clinical research and postmarketing application drug (frequency is unknown).

Violation of the nervous system: headache, dizziness, aseptic meningitis, convulsions.

Disorders of the psyche: agitation, sleep disturbance, anxiety.

Heart Disease: tachycardia, arrhythmia, decrease arterial pressure, stenocardia.

Vascular disorders: "tides" of blood to the skin, bleeding (including, bleeding from the vessels of the skin, mucous membranes, stomach, intestines).

Infringements from digestive system: xerostomia (dryness of the oral cavity), anorexia, intestinal atony, feeling pressure and overflow in the area stomach, nausea, vomiting, diarrhea.

Disorders from the liver and bile ducts: intrahepatic cholestasis, increased activity of "hepatic" transaminase, increased activity alkaline phosphatase.

Violation of blood and lymphatic system: leukopenia, thrombocytopenia, pancytopenia, hypofibrinogenemia.

Violation by the body vision: impaired vision, scotoma.

Breaking from the skin and subcutaneous tissues: itching, erythema (redness of the skin), urticaria, increased brittleness of the nails, edema.

Breaking from the immune system: anaphylactic / anaphylactoid reactions, angioedema, anaphylactic shock, bronchospasm.

Overdose:

Symptoms overdosage: dizziness, nausea, vomiting like "coffee grounds", decrease arterial pressure, tachycardia,

arrhythmia, redness of skin covers, loss of consciousness, chills,

areflexia, tonic-clonic convulsions.

In case of occurrence of the described higher violations are urgently needed consult a doctor.

Treatment is symptomatic. When appearance of the first signs

overdose (sweating, nausea, cyanosis) immediately stop taking the drug. If the drug adopted recently, the measures aimed at prevention of further absorption of the drug by excretion (gastric lavage) or suction slowdown (for example, reception of activated carbon).

Particular attention should be paid to is aimed at maintaining blood pressure and respiratory function. When seizures are injected diazepam.

The specific antidote is unknown.

Interaction:

With antihypertensive drugs

Pentoxifylline increases the risk development of arterial hypotension when used simultaneously with antihypertensive agents and (for example, angiotensin-converting enzyme (ACE) inhibitors) or other drugs having a potential antihypertensile effect (for example, nitrates);

FROM drugs affecting the blood coagulation system Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (direct and indirect anti-coagulants, thrombolysis, antibiotics, such as cephalosporins).

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

FROM Cimetidine

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

With other xanthines

Co-administration with other xanthines can lead to excessive nervous excitement. With hypoglycemic and agents and (insulin and hypoglycemic agents for oral administration) Hypoglycemic the action of insulin or hypoglycemic agents for oral ingestion may be enhanced with simultaneous application pentoxifylline (increased risk of hypoglycemia). Strict monitoring of the condition of such patients is required, including regular glycemic control.

With theophylline

In some patients with simultaneous application of pentoxifylline and theophylline there was an increase in the concentration of theophylline in the blood. In the future, this may lead to an increase or increase in side effects, associated with theophylline.

With ciprofloxacil

In some patients, while the use of pentoxifylline and ciprofloxacin marked increase in the concentration of pentoxifylline in plasma. In the future, this may lead to an increase or increase in side effects associated with the use of this combination.

Special instructions:

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

In patients with diabetes mellitus taking hypoglycemic agents, the administration of large doses can cause a pronounced hypoglycemia (may be required correction of doses of hypoglycemic agents and the conduct of glycemic control).

With the appointment of Trental® It is necessary simultaneously with anticoagulants to monitor the parameters of the blood coagulation system.

In patients who have recently undergone operative intervention, regular monitoring of hemoglobin and hematocrit is necessary. Patients with low and unstable blood pressure should reduce the dose of pentoxifylline.

The elderly patients can require dose reduction pentoxifylline (increase bioavailability and reduced rate of excretion).

Security and efficiency pentoxifylline in children are not studied enough.

Smoking can reduce therapeutic effectiveness of the drug.

Effect on the ability to drive transp. cf. and fur:Considering possible side effects (for example, dizziness), care should be taken when driving vehicles and engaging in potentially hazardous activities.

Form release / dosage:

Tablets coated with enteric film coating 100 mg.

For 10 tablets in a blister of PVC / aluminum foil. For 6 blisters together with instructions for use in a cardboard box.

Packaging:(10) - blisters (6) - packs cardboard

Storage conditions:

Store in a dry place at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Shelf life:

4 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014229 / 01

Date of registration:21.05.2008

The owner of the registration certificate:Sanofi India LimitedSanofi India Limited India

Manufacturer: & nbsp

SANOFI INDIA, Limited India

Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Trental® (Trental®)