Pentoxpharm

Pentoxipharm is a peripheral vasodilating drug. Contains the element pentoxifylline (3-substituted xanthine derivative).

The active substance improves the processes of microcirculation of blood flow, mainly through a positive effect on the rheological characteristics of the blood. Along with this, the drug inhibits platelet and erythrocyte aggregation, and also lowers fibrinogen and blood viscosity. In addition, it inhibits leukocyte activation and the participation of leukocytes in the development of inflammatory processes. [1]

Indications Pentoxpharm

It is used under the following conditions:

• disorders of peripheral blood flow ( angiopathy of a diabetic nature, intermittent claudication and trophic type 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 inside the retina;
• auditory or vestibular disorders of a vascular nature.

Release form

The release of the drug element is realized in the form of enteric tablets - 10 pieces inside a cell package. There are 6 such packages in a pack.

Pharmacodynamics

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

Pharmacokinetics

The drug is at high speed, fully absorbed inside the gastrointestinal tract. Combined use with food reduces the rate of absorption, but does not decrease its extent. 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]

Undergoes intensive metabolic processes after the 1st intrahepatic passage. In this case, a large volume of metabolites is formed - first inside the 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 faeces. Most of the medication taken is excreted over a 24-hour period.

In people with renal / hepatic dysfunctions, as well as in people 60-68 years of age, there is an increase in the AUC level, as well as a weakening of the degree of excretion.

Dosing and administration

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

Therapy should be started with a daily portion of 0.6 g, which is divided into 3 uses.

In the case of a strong decrease in blood pressure and the development of side signs, the daily portion can be lowered to 0.3 g.

A maximum of 1.2 g of medication is allowed per day (in the case of an active phase of the disease) for 3 uses (4 tablets 3 times a day). The maintenance dosage is 0.8 g per day (also divided into 3 applications).

The therapy cycle should last at least 2 months.

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

• Application for children

Due to the limited experience of using the medication in pediatrics, it is not prescribed for children.

Use Pentoxpharm during pregnancy

Although there is no information regarding the teratogenic and embryotoxic effects of pentoxifylline, it cannot be used during pregnancy, since there is a possibility of a decrease in blood pressure and the appearance of hemorrhages (due to the medicinal characteristics of the drug).

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

Contraindications

The main contraindications:

• severe intolerance to the active element and auxiliary components of drugs;
• severe stage of atherosclerosis, which is cerebral or coronary in nature;
• decreased blood pressure;
• recent myocardial infarction;
• intracerebral hemorrhage;
• very severe hemorrhages.

Side effects Pentoxpharm

The main side effects:

• lesions affecting the gastrointestinal tract: thirst and xerostomia, diarrhea, vomiting, a feeling of heaviness in the abdominal area, bloating and nausea;
• problems with the work of the CVS: tachycardia, redness with rushes of blood to the neck and face, a decrease in blood pressure values up to the development of orthostatic collapse, rhythm disturbances and angina pectoris;
• disorders associated with the function of the central nervous system: dizziness with headaches, sleep disorders, insomnia, tremors and anxiety, confusion, increased excitability, scotoma and visual disturbances (the appearance of a red background);
• immune disorders: urticaria, pruritus, epidermal eruptions, and erythema. Anaphylaxis develops singly;
• others: hepatitis, nosebleeds, swelling of the nasal mucosa, conjunctivitis, hemorrhages in the epidermis or gastrointestinal tract (while their development can occur when drugs are used in combination with antithrombotic substances (antiplatelet agents or anticoagulants)), leuko- or thrombocytopenia.

Overdose

In case of poisoning with Pentoxpharm, convulsions, facial flushing, drowsiness, reaching loss of consciousness, or agitation, a decrease in blood pressure, an increase in temperature and a disturbance in the rhythm of the heartbeat are noted.

Gastric lavage, the use of activated charcoal and symptomatic substances that eliminate convulsions and increase the blood pressure, as well as respiratory analeptics are performed. The drug has no antidote.

Interactions with other drugs

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

The introduction together with antihypertensive substances can provoke a strong decrease in blood pressure.

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

Combining pentoxifylline with insulin and hypoglycemic drugs can 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 in relation to smooth vascular muscles, since it has a vasoconstrictor effect.

Storage conditions

Pentoxipharm must be stored in a dark and dry place, closed from the penetration of children. Temperature values - no more than 25 ° С.

Shelf life

Pentoxipharm can be used within 36 months from the date of sale of the therapeutic product.

Analogs

Analogues of the medicine are the medicines Vasonit and Trental with Agapurin, Pentilin and Latren with Pentotren, as well as Pentoxifylline.