Pentoxifylline-N

PENTOXIFYLLINE-N

Solution for injection 20 mg/ml 5 ml in ampoules No.5

The product belongs to the group of peripheral vasodilators. It  blocks aggregation of thrombocytes and erythrocytes, increases their flexibility, reduces the high fibrinogen concentration in blood plasma and increases fibrinolysis which in its turn reduces blood viscosity and improves its rheological properties.

As the result, microcirculation and oxygen supply improvement is observed.

Marketing Authorization No. UA/14521/01/01

Composition

Activeingredient: pentoxifylline;

1 ml of the solution contains 20 mg of pentoxifylline;

Excipients: sodium chloride, sodium hydroxide, water for injections.

Pharmaceutical form

Solution for injection.

Physicalandchemicalproperties

Colorless clear solution.

Pharmacotherapeuticgroup

Peripheral vasodilators. ATC code С04А D03.

Pharmacological properties

Pharmacodynamics.

Pentoxifylline  is a methylxanthine derivative. The mechanism of action of pentoxifylline is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the cells of the smooth muscles of blood vessels, blood cells, as well as in other tissues and organs. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their flexibility, reduces the increased concentration of fibrinogen in the blood plasma and enhances fibrinolysis, which reduces the viscosity of blood and improves its rheological properties. In addition, pentoxifylline has a weak myotropic vasodilator effect, somewhat reduces the overall peripheral vascular resistance and has a positive ionotropic effect. Due to the use of pentoxifylline, microcirculation and tissue supply with oxygen improves, most of all in the limbs, the central nervous system, and moderately in the kidneys. The drug slightly dilates the coronary vessels.

Pharmacokynetics.

The main pharmacologically active metabolite, 1- (5-hydroxyhexyl) -3,7-dimethylxanthine (metabolite I), is determined in blood plasma with a concentration exceeding the concentration of unchanged substance in 2 times  and is in condition of reverse biochemical balance with it. In this regard, pentoxifylline and its metabolite should be considered as an active unity. The half-life of the excretion of pentoxifylline is 1.6 hours.

Pentoxifylline is fully metabolized, more than 90% is excreted by  kidneys as unconjugated water-soluble polar metabolites. Less than 4% of the administered dose are excreted with feces. Patients with severe impairment of renal function have slowed the excretion of the metabolites. Patients with impaired liver function have prolonged  half-life period of the excretion of pentoxifylline.

Clinical performance

Indications.

Atherosclerotic encephalopathy; ischemic cerebral stroke; discirculatory encephalopathy; violation of peripheral circulation due to atherosclerosis, diabetes mellitus (including diabetic angiopathy), inflammation; trophic disorders in tissues associated with vein or microcirculatory disorders (postthrombophlebitic syndrome, trophic ulcers, gangrene, frostbites); obliterating endarteritis; angioneuropathy (Raynaud's disease); disorders of the blood circulation of the eye (acute, subacute, chronic circulatory failure in the retina and choroid of the eye), disturbances in the function of the inner ear of the vascular genesis, accompanied by a decrease in hearing.

Contraindications

Pentoxifylline is contraindicated for the patients:

- with increased sensitivity to pentoxifylline, to other methylxanthines or to any excipient substance of Pentoxifylline-N;

- with massive bleeding (risk of increased bleeding);

- with a vast hemorrhage in the eye retina with hemorrhages in the brain (risk of increased bleeding);

If during the pentoxifylline treatment the bleeding occurs in the retina of the eye, the drug should be discontinued immediately:

- in the acute period of myocardial infarction;

- with a stomach ulcer and / or intestinal ulcers;

- with hemorrhagic diathesis.

Interaction with other medicinal products and other forms of interaction

The effect of lowering blood sugar level intrinsic to insulin or oral antidiabetics, can be enhanced. Therefore, patients receiving medication for diabetes should be closely monitored.

There are cases of increased anticoagulant activity among the patients who were simultaneously treated with pentoxifylline and antivitamins K. When pentoxifylline dosage is prescribed or modified, it is recommended that anticoagulant activity should  be controlled at this group of patients.

Pentoxifylline may enhance the antihypertensive action of antihypertensive agents and other drugs that can cause a drop of  blood pressure.

The concomitant use of pentoxifylline and theophylline at some patients may lead to the increase of the level of theophylline in the blood. Therefore, increase of the frequency and increase of the manifestations of adverse reactions of theophylline are possible.

Among some some patients, simultaneous use with ciprofloxacin may lead to increase of pentoxifylline concentrations in blood serum. As a consequence, the frequency and severity of adverse reactions associated with the simultaneous use of drugs may increase.

Potential additive effect with platelet aggregation inhibitors: due to increased risk of bleeding, simultaneous use of platelet aggregation inhibitors (eg clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs, in addition to selective inhibitors of COX-2, acetylsalicylates [ASA / LAS ], ticlopidine, dipyridamole) with pentoxifylline should be administered with caution.

Simultaneous use with cimetidine may increase the concentration of pentoxifylline and metabolite I in the blood plasma.

Precaustions for use.

At the first signs of the development of an anaphylactic reaction, it is  necessary to stop immediately the infusion of pentoxifylline and obtain medical treatment.

In the case of application of pentoxifylline  in patients with chronic heart failure,  it is necessary to reach a blood circulation compensation phase firstly.

Among patients with diabetes and treated with insulin or oral hypoglycemic agents, when using high doses of pentoxifylline, the effects of these medicines on the level of sugar in the blood may be increased (see section "Interaction with other medicines and other types of interactions"). In these cases, it is advisable to reduce the dose of insulin or oral antidiabetic medicines and take special care of the patient.

In patients with systemic lupus erythematosus (SLE) or other connective tissue disease, pentoxifylline may be prescribed only after a thorough analysis of possible risks and benefits.

Since there is a risk of aplastic anemia during pentoxifylline treatment, a regular common blood test is required.

Among patients with renal failure (creatinine clearance is less than 30 ml / min) or severe liver dysfunction, pentoxifylline withdrawal may be delayed. Appropriate monitoring is required.

Particular careful observation is required for the following patients:

- with severe cardiac arrhythmias;

- with arterial hypotension;

- with marked atherosclerosis of cerebral and coronary vessels, especially with concomitant arterial hypertension and heart rhythm disorders. Among these patients, when taking the medicine, there are possible attacks of angina, arrhythmias and arterial hypertension;

- with renal failure (clearance of creatinine is below 30 ml / min);

- with severe hepatic failure;

- with a high predisposition to bleeding, caused, for example, by treatment with anticoagulants or blood coagulation disorders. Regarding the bleeding, see section "Contraindications";

- who have recently undergone surgical treatment (increased risk of bleeding, which necessitates systematic monitoring of hemoglobin and hematocrit levels);

- for whom the reduction of blood pressure is a high risk (for example, patients with severe coronary heart disease or stenosis of vessels that supply blood to the brain);

- who simultaneously receive treatment with pentoxifylline and antivitamin K or platelet aggregation inhibitors (see section "Interaction with other medicines and other types of interactions");

- who simultaneously receive treatment with pentoxifylline and antidiabetics (see section "Interaction with other medicines and other types of interactions");

- who simultaneously receive treatment with pentoxifylline and ciprofloxacin (see section "Interaction with other medicines and other types of interactions");

- who simultaneously receive treatment with pentoxifylline and theophylline (see section "Interaction with other medicines and other types of interactions");

Use during pregnancy or lactation.

Pregnancy. Due to the lack of adequate experience, pentoxifylline should not be prescribed during pregnancy.

Lactation. Small amounts of pentoxifylline penetrates into breast milk. If pentoxifylline is prescribed, breastfeeding should be stopped.

Effects on ability to drive and use machines. Does not affect.

Posology and method of administration

Intravenous infusions are the most effective forms of parenteral administration of the medicine, which are better tolerated. The dosage regimen is determined by the physician and depends on the degree of severity of circulatory disturbances, body weight and tolerability of treatment. Infusion can only be performed if the solution is clear.

The following adult treatment schemes are recommended:

1.Intravenous infusion of 100-600 mg of pentoxifylline in 100-500 ml of Ringer's lactate solution, 0.9% solution of sodium chloride or 5% glucose solution 1-2 times a day. The duration of intravenous drip infusion is 60-360 minutes, ie, administration of 100 mg pentoxifylline should last at least 60 minutes. Infusion may be supplemented by pentoxifylline oral administration (400 mg), based on the assumption that the maximum daily dose (infusion and oral) is 1200 mg.

2.In case of severe condition of the patient (especially with constant pain, gangrene or trophic ulcers), pentoxifylline infusion may be performed within 24 hours. In this scheme, the dose is determined at a rate of 0.6 mg / kg / h. The calculated daily dose for a patient with a body weight of 70 kg is 1000 mg, for a patient with a body weight of 80 kg - 1150 mg. Regardless of the patient's body weight, the maximum daily dose is 1200 mg. The volume of the infusion solution is calculated individually, taking into account the concomitant diseases, the condition of the patient and it is on average 1-1,5 liters per day.

3.In some cases, the medicine is administered by intravenous injection of 5 ml (100 mg). The injection is performed slowly, for 5 minutes, the patient's position is lying down.

Duration of the parenteral treatment course  is determined by the physician who carries out the treatment. After improvement of the patient's condition, it is recommended to continue treatment using the oral form of pentoxifylline.

Instruction for use of  ampule.

  1. Separate one ampoule from the block and shake the contents gently, holding the ampoule by its neck.
  2. Squeeze the ampoule in your hand (the product leakage shall not occur) and remove the cap by rotating it.
  3. Immediately put a syringe in the ampoule through the obtained hole.
  4. Turn the ampoule over and slowly suck the liquid in the syringe.
  5. Put a needle on the syringe.

Children.

Do not apply.

Overdose

Symptoms. The initial symptoms of acute overdose with pentoxifylline are nausea, dizziness, or low blood pressure. In addition, symptoms such as fever, anxiety, feeling of heat (tides), tachycardia, loss of consciousness, arreflexia, arrhythmia, tonic-clonic seizures and vomiting of the color of the coffee grounds as a sign of gastrointestinal bleeding may develop.

Treatment. In order to treat acute overdose and prevent the onset of complications, general and specific intensive medical observation and the introduction of therapeutic measures are required.

Adverse reactions

Cardiac disorders: arrhythmia, tachycardia, stenocardia.

Vascular Disorders: decreasing or increasing of blood pressure; feeling of heat (tides), bleeding, peripheral edema.

From the blood and lymphatic system: thrombocytopenia with thrombocytopenic purpura and aplastic anemia (partial or complete cessation of the formation of all blood cells, pancytopenia), with possibly lethal outcome, leukopenia / neutropenia.

Neurological disorders: dizziness, headache, aseptic meningitis, tremor, paresthesia, seizures.

Gastrointestinal disorders: sensation of pressure in the stomach, flatulence, nausea, vomiting or diarrhea, constipation, hyperalsalivation.

On the skin and subcutaneous tissue: itching, reddening of the skin and urticaria, toxic epidermal necrolysis, Stevens & Johnson’s syndrome, rash.

From the immune system: anaphylactic reactions, bronchospasm, anaphylactic shock, angioedema, anaphylactoid reactions.

Hepatobiliary disorders: intrahepatic cholestasis; increased levels of transaminases.

From the organs of vision: visual impairment, conjunctivitis, retinal hemorrhage, retinal detachment.

Mental disorders: arousal and disturbance of sleep, hallucinations.

General disorders: hypoglycemia, increased sweating, increased body temperature.

Shelflife.

2.5 years.

Storage conditions.

Store in original package at the temperature not above 25 °С. Do not freeze. Keep away from children.

 

Incompatibility.

The product should not be mixed in one container with other  unless specified in section “Posology and method of administration.

Packaging.

5 ml in the ampoules №5.

Prescription category.

Following the doctor’s prescription.

Feedback

Materials on the medicine

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Calculation of dose

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