Pentoxifylline

Pentoxifylline has vasodilating activity relative to peripheral vessels.

The medication is a methylxanthine derivative. The principle of its effect is based on the suppression of the action of PDE and the accumulation of cAMP inside blood cells and smooth muscle vascular cells, and in addition, inside other organs and tissues. [1]

The drug increases the flexibility of erythrocytes with platelets and slows down their aggregation, reduces the increased plasma fibrinogen values and potentiates fibrinolysis, which weakens blood viscosity and improves rheological blood parameters. [2]

Indications Pentoxifylline

It is used in the case of such disorders:

• having atherosclerotic or discirculatory encephalopathy ;
• cerebral ischemic stroke;
• a disorder of peripheral blood flow caused by the development of atherosclerosis, inflammation or diabetes mellitus (this also includes diabetic angiopathy);
• angioneuropathy ( Raynaud's syndrome );
• trophic tissue lesions caused by venous disease or microcirculation disorder (trophic ulcers, frostbite, post-thrombophlebitic syndrome or gangrene);
• obliterating endarteritis;
• disorders of intraocular blood flow (having a subacute, acute or chronic insufficiency of blood flow inside the retina or choroid);
• problems with the work of the inner ear, which have a vascular etiology (in this case, hearing impairment develops).

Release form

The release of the drug element is realized in tablets - 10 pieces inside the cell pack; inside the box - 5 such packs.

Pharmacodynamics

Pentoxifylline can lead to the development of a slight vasodilating effect, which has a myotropic nature. At the same time, it slightly weakens the systemic resistance of peripheral vessels and causes a positive inotropic effect.

The use of the drug leads to an improvement in microcirculation and oxygen supply to tissues (mainly inside the central nervous system with the extremities; a weaker effect is exerted on the kidneys). The medication causes some expansion of the coronary vessels. [3]

Pharmacokinetics

The main metabolic component demonstrating pharmacological effects (1- (5-hydroxyhexyl) -3,7-dimethylxanthine) is found inside the blood plasma in values that are twice the level of the unchanged element, and is in a state of reverse biochemical balance relative to it. Because of this, the active substance of the drug with its metabolite is considered as an active whole.

The half-life of pentoxifylline is 1.6 hours. The medication is fully involved in metabolic processes; more than 90% of drugs are excreted through the kidneys (in the form of non-conjugated, water-soluble polar metabolic elements). Less than 4% of the applied dosage is excreted in faeces.

In people with severe renal dysfunction, there is a slowdown in the excretion of the metabolic components of the drug.

In individuals with hepatic dysfunction, the half-life of pentoxifylline is prolonged.

Dosing and administration

Pentoxifylline is used in the amount of 2-4 tablets, 2-3 times a day. The tablets are taken after meals, without chewing and washed down with plain water. A maximum of 1200 mg of the drug is allowed per day.

Individuals with unstable or low blood pressure levels or with a significant weakening of renal function (CC value below 30 ml per minute) and people from the group with a high risk of complications with a decrease in blood pressure (for example, in the case of severe lesions in the area of coronary vessels or intensive stenosis of the great cerebral vessels), it is required to start therapy with minimal dosages. The portions are selected personally, and their increase is made gradually, taking into account the tolerance of the therapy.

• Application for children

There is no experience of using the medication in pediatrics.

Use Pentoxifylline during pregnancy

There is only limited experience with the use of Pentoxifylline during pregnancy, which is why it is not prescribed during the noted period.

The drug in small volumes is excreted in breast milk, and therefore it is necessary to stop breastfeeding for the period of therapy.

Contraindications

Among the contraindications:

• severe intolerance to pentoxifylline, other methylxanthines or auxiliary elements of the drug;
• the presence of profuse bleeding (there is a possibility of potentiation of bleeding);
• severe hemorrhage in the retinal region or intracerebral hemorrhage (there is a risk of potentiation of bleeding). With the development of hemorrhage in the retinal area during the use of drugs, you must immediately cancel the reception;
• active phase of myocardial infarction;
• ulcerative lesions in the gastrointestinal tract;
• diathesis having a hemorrhagic form.

Side effects Pentoxifylline

The main side symptoms:

• disturbances in the work of the CVS: tachycardia, hot flashes, decrease or increase in blood pressure values, arrhythmia, peripheral edema and angina pectoris;
• problems with hematopoietic function: bleeding, aplastic anemia, neutro- or leukopenia, pancytopenia, which can lead to death, as well as thrombocytopenia along with purpura of the thrombocytopenic type;
• disorders of the activity of the National Assembly: headaches, paresthesias, hallucinations, dizziness and convulsions, as well as sleep disorder, agitation, tremor and meningitis of an aseptic nature;
• lesions affecting the gastrointestinal tract: feeling of pressure in the stomach, vomiting, hypersalivation, gastrointestinal disturbances, nausea, constipation, bloating and diarrhea;
• symptoms associated with the subcutaneous layer and epidermis: urticaria, redness, itching, rash, SS and TEN;
• immune disorders: bronchial spasm, anaphylactic or anaphylactoid symptoms, anaphylaxis and Quincke's edema;
• problems with the activity of the bile ducts and liver: intrahepatic cholestasis;
• visual disturbances: conjunctivitis, retinal detachment or hemorrhage in it, as well as visual dysfunction;
• change in test readings: an increase in transaminase values;
• others: the development of hyperhidrosis or hypoglycemia and an increase in temperature.

Overdose

Among the early manifestations of acute intoxication are dizziness, nausea, or a decrease in blood pressure. Along with this, the following signs may appear - excitement, tachycardia, arrhythmias, hot flashes, fever, areflexia and seizures that have a tonic-clonic form. There may also be a loss of consciousness and the appearance of vomiting, which has a dark brown tint (a symptom of bleeding inside the gastrointestinal tract).

Elimination of acute poisoning and prevention of the development of complications is carried out by carrying out symptomatic procedures and intensive specific medical monitoring of the patient's condition.

Interactions with other drugs

The antidiabetic effect that develops with the use of hypoglycemic drugs for oral administration, as well as insulin, can be potentiated in the case of administration with medication. Because of this, persons treating diabetes mellitus must be under constant medical supervision.

In post-marketing studies, an increase in the anticoagulant effect was found in individuals who used the drug together with K-vitamin antagonists. During the appointment or change in the dosage of Pentoxifylline, it is necessary to monitor the anticoagulant effect in such combinations.

The drug can potentiate the antihypertensive properties of antihypertensive substances and other drugs that can lead to a decrease in blood pressure values.

The use of the drug together with theophylline can cause an increase in the blood counts of the latter in some individuals. Because of this, the severity and frequency of the development of side symptoms of theophylline may increase.

In some patients, administration together with ciprofloxacin causes an increase in the serum level of pentoxifylline. Because of this, the intensity of side effects may increase and the frequency of their development may increase.

In theory, an additive effect can develop when substances that slow down platelet aggregation are used. Due to the increased likelihood of bleeding, combine these substances (among them tirofiban, clopidogrel with iloprost, anagrelide, ticlopidine and eptifibatide with abciximab, and in addition dipyridamole, epoprostenol, NSAIDs (excluding selective inhibitors of COX-2 activity) and acetyls it is necessary to be extremely careful.

Use in combination with cimetidine can cause an increase in the plasma level of pentoxifylline along with its metabolic element I.

Storage conditions

Store pentoxifylline out of the reach of small children. Temperature values - no more than 25 ° C.

Shelf life

Pentoxifylline can be used within a 36-month term from the date of marketing of the therapeutic product.

Analogs

The analogs of the drug are the substances Trental, Latren with Vasonite, Pentoxpharm and Agapurin with Xanthinol nicotinate, and in addition Flexital, Pentylin and Trentan.