Pentoxifarm

Pentoxifarm is a peripheral vasodilator drug. It contains the element pentoxifylline (3-substituted xanthine derivative).

The active substance improves blood microcirculation processes, mainly by positively affecting blood rheological characteristics. At the same time, the drug inhibits platelet and erythrocyte aggregation, and also reduces fibrinogen levels and blood viscosity. In addition, it inhibits leukocyte activation and the participation of leukocytes in the development of inflammatory processes. [ 1 ]

Indications Pentoxifarm

It is used in the following conditions:

• peripheral blood flow disorders ( angiopathy of diabetic origin, intermittent claudication and trophic ulcers affecting the legs);
• problems with intracerebral blood flow (temporary intracerebral lesions of the ischemic type, atherosclerosis affecting the vessels of the brain, and vascular dementia);
• disturbances of blood flow within the retina;
• auditory or vestibular disorders of vascular origin.

Release form

The release of the medicinal element is realized in the form of enteric-coated tablets - 10 pieces inside a cellular package. In a pack - 6 such packages.

Pharmacodynamics

The drug slows down the action of PDE and increases the cAMP levels inside myocytes with erythrocytes of the vascular membrane, and at the same time reduces the levels of intracellular Ca. It exhibits a vasodilating effect, which develops with a moderate weakening of peripheral vascular resistance and a moderate increase in cardiac output and stroke volume. [ 2 ]

Pharmacokinetics

The drug is fully absorbed in the gastrointestinal tract at high speed. Combined use with food reduces the rate of absorption, but does not reduce its degree. Plasma values of Cmax of the unchanged active element are noted after 1 hour, and metabolic components - after 1.5 hours.

Synthesis with the erythrocyte wall is noted. Pentoxifylline with its metabolic elements is excreted in breast milk. [ 3 ]

It undergoes intensive metabolic processes after the first intrahepatic passage. In this case, a large volume of metabolites is formed - first inside erythrocytes, and later - inside the liver. The main metabolic components of pentoxifylline are 1-5-hydroxyhexyl-3,7-dimethylxanthine, together with 1-3-carboxyhexyl-3,7-imethylxanthine.

Excretion is mainly carried out by the kidneys, in the form of metabolic elements; less than 4% of the administered portion is excreted in the feces. Most of the drug taken is excreted within 24 hours.

In people with renal/hepatic dysfunction, as well as in people aged 60-68 years, an increase in AUC levels and a decrease in the degree of elimination are observed.

Dosing and administration

The duration of the treatment cycle and the daily dosage are selected taking into account the type of disease and the severity of its symptoms.

Therapy should begin with a daily dose of 0.6 g, divided into 3 doses.

In case of a strong decrease in blood pressure and the development of side effects, the daily dose can be reduced to 0.3 g.

A maximum of 1.2 g of the drug is allowed per day (in case of the active phase of the disease) in 3 doses (4 tablets 3 times per day). The maintenance dose is 0.8 g per day (also divided into 3 doses).

The therapeutic cycle should last at least 2 months.

The tablets must be taken whole, without chewing, with food and washed down with plain water.

• Application for children

Due to limited experience with the use of the drug in pediatrics, it is not prescribed to children.

Use Pentoxifarm during pregnancy

Although there is no information regarding the teratogenic and embryotoxic effects of pentoxifylline, it should not be used during pregnancy, since there is a risk of decreased blood pressure and the occurrence of hemorrhages (due to the medicinal properties of the drug).

To prevent the development of negative symptoms in infants, breastfeeding should be discontinued during the period of using Pentoxipharm.

Contraindications

Main contraindications:

• severe intolerance to the active ingredient and auxiliary components of the drug;
• severe stage of atherosclerosis of cerebral or coronary nature;
• decreased blood pressure;
• recent myocardial infarction;
• intracerebral hemorrhage;
• very severe bleeding.

Side effects Pentoxifarm

Main side effects:

• lesions affecting the gastrointestinal tract: thirst and xerostomia, diarrhea, vomiting, feeling of heaviness in the abdominal area, bloating and nausea;
• problems with the functioning of the cardiovascular system: tachycardia, redness with flushes of blood to the neck and face, decreased blood pressure up to the development of orthostatic collapse, rhythm disorders and an attack of angina pectoris;
• disorders associated with the function of the central nervous system: dizziness with headaches, sleep disorders, insomnia, tremor and anxiety, confusion, increased excitability, scotoma and visual disturbances (appearance of a red background);
• immune disorders: urticaria, itching, epidermal rashes and erythema. Anaphylaxis develops occasionally;
• others: hepatitis, nosebleeds, swelling of the nasal mucosa, conjunctivitis, hemorrhages in the epidermis or gastrointestinal tract (their development may occur when using drugs in combination with antithrombotic agents (antiplatelet agents or anticoagulants)), leukopenia or thrombocytopenia.

Overdose

In case of poisoning with Pentoxifarm, convulsions, facial flushing, drowsiness leading to loss of consciousness, or agitation, decreased blood pressure, increased temperature and irregular heartbeat are observed.

Gastric lavage, activated carbon and symptomatic substances that eliminate convulsions and increase blood pressure, as well as respiratory analeptics are used. The drug has no antidote.

Interactions with other drugs

In case of combination with anticoagulants or antiplatelet agents, the risk of bleeding increases.

Administration together with antihypertensive substances may provoke a strong decrease in blood pressure readings.

Use in combination with theophylline may lead to an increase in its plasma values and the development of its toxic effects.

The combination of pentoxifylline with insulin and hypoglycemic drugs may potentiate their antidiabetic properties.

Taking the medication with food reduces the rate of its absorption, but does not lead to a decrease in the degree of absorption.

Nicotine weakens the activity of pentoxifylline on smooth vascular muscles because it has a vasoconstrictor effect.

Storage conditions

Pentoxipharm must be stored in a dark and dry place, out of the reach of children. Temperature values - no more than 25 ° C.

Shelf life

Pentoxipharm can be used for a period of 36 months from the date of sale of the therapeutic product.

Analogues

Analogues of the drug are the medications Vazonit and Trental with Agapurin, Pentilin and Latren with Pentotren, as well as Pentoxifylline.