Pentylline

Pentilin is a drug that dilates peripheral blood vessels. It contains the element pentoxifylline (methylxanthine derivative).

The principle of the active element's influence is associated with the suppression of PDE activity and the accumulation of cAMP inside smooth muscle vascular and blood cells, and also inside other tissues with organs. Pentoxifylline slows down platelet and erythrocyte aggregation and increases the flexibility of these elements. At the same time, it reduces elevated plasma fibrinogen levels and potentiates fibrinolysis, thereby improving blood rheological parameters and reducing blood viscosity. [ 1 ]

Indications Pentylline

It is used in case of such violations:

• encephalopathy of atherosclerotic or circulatory origin, cerebral ischemic stroke and peripheral blood flow disorders associated with inflammation, atherosclerosis or diabetes mellitus (this also includes angiopathy of diabetic origin);
• angioneuropathy ( Raynaud's syndrome );
• trophic tissue lesions caused by microcirculation disorders or problems with veins (trophic ulcers, frostbite, post-thrombophlebitic syndrome or gangrene);
• obliterating endarteritis;
• disorder of intraocular blood flow (insufficient blood flow inside the vascular membrane of the eye and retina, which can be subacute, acute or chronic);
• problems with the functioning of the inner ear, which are of a vascular nature (this results in hearing loss).

Release form

The release of the medicinal element is realized in the form of injection liquid - inside ampoules with a capacity of 5 ml (0.1 g). Inside the cellular pack there are 5 such ampoules; inside the box - 1 such pack.

Pharmacodynamics

Pentoxifylline can lead to the development of a weak myotropic vasodilating effect, which slightly weakens the systemic resistance of peripheral vessels and has a positive inotropic effect. The introduction of pentoxifylline improves microcirculation along with the oxygen supply of tissues (the greatest activity is noted within the central nervous system and extremities; moderately acts within the kidneys).

The drug has a weak vasodilating effect on the coronary vessels. [ 2 ]

Pharmacokinetics

The main metabolic element that exerts therapeutic action (1-(5-hydroxyhexyl)-3,7-dimethylxanthine) is found in blood plasma in amounts that exceed the unchanged component by two times, and also exist in the form of a reverse biochemical balance with it. For this reason, pentoxifylline with its metabolic element is considered as a single active substance.

The half-life of pentoxifylline is 1.6 hours.

The substance fully participates in metabolic processes, and more than 90% of it is excreted through the kidneys in the form of water-soluble polar metabolic components that are not subject to conjugation. Less than 4% of the applied portion is excreted with feces.

In people with severe renal dysfunction, the process of removing metabolic components slows down.

In individuals with liver dysfunction, a prolongation of the half-life of pentoxifylline is observed.

Dosing and administration

Intravenous infusions are considered the most effective parenteral methods of administration and have the best tolerability. The dosage scheme is selected by the doctor, taking into account the weight, severity of circulatory disorders and tolerability of therapy. Only completely transparent medicinal solution is used for infusion.

The following treatment regimens are generally prescribed:

• administration via infusion of 0.1-0.6 g of pentoxifylline (dissolved in 0.9% NaCl (0.1-0.5 l)), 1-2 times per day. The duration of intravenous administration of the substance is 1-6 hours (0.1 g of pentoxifylline should be administered within at least 1 hour). In addition to infusion, Pentilin is taken orally (a dose of 0.4 g, assuming that the highest daily dosage, including oral administration and infusion, is 1.2 g);
• in case of very severe course of the disease (especially with regular pain, trophic ulcers or gangrene), the infusion of the drug can be administered over a 24-hour period. In the case of the specified scheme of application, the portion size is selected in the ratio of 0.6 mg / kg / hour. With such a calculation, the daily dosage for a person weighing 70 kg will be equal to 1 g, and for a person weighing 80 kg - 1150 mg. At the same time, regardless of the patient's weight, it is prohibited to administer more than 1.2 g of the drug per day. The volume of infusion fluid is determined individually, taking into account concomitant pathologies and the patient's condition (on average, 1-1.5 l per day);
• Sometimes the medication can be administered via intravenous injection (at a dosage of 5 ml (0.1 g)). The procedure is performed at low speed, for 5 minutes. The patient must be in a lying position.

The duration of the parenteral therapeutic cycle is selected by the attending physician. When the patient's condition improves, it is necessary to transfer him to taking the medication tablets.

Dosage amounts in case of renal dysfunction.

If the CC level is below 30 ml per minute (0.5 ml/second), the portion is determined individually, reducing it by approximately 30-50% compared to the standard dosage.

Dosage sizes in case of liver dysfunction.

If a significant disorder of liver function is observed, the dose of Pentilin is reduced, taking into account personal tolerance to the drug.

• Application for children

There is no experience of using drugs in pediatrics.

Use Pentylline during pregnancy

There is only limited information regarding the use of Pentilin during pregnancy, which is why it is not prescribed during this period.

Small amounts of pentoxifylline are excreted in breast milk. If you need to use the drug, you should temporarily stop breastfeeding.

Contraindications

Among the contraindications:

• severe intolerance associated with pentoxifylline, other components of the drug or other substances from the methylxanthine subgroup (including choline theophylline, theobromine and caffeine with theophylline, as well as aminophylline);
• very heavy bleeding (there is a possibility of increased bleeding);
• hemorrhages in the area of the retina or brain (possibility of potentiation of hemorrhage). If hemorrhage in the area of the retina develops during the use of pentoxifylline, the drug should be discontinued immediately;
• active phase of myocardial infarction;
• ulcerative lesions in the gastrointestinal tract;
• diathesis having a hemorrhagic form.

Side effects Pentylline

Main side effects:

• changes in test results: increase in transaminase levels;
• disturbances in the functioning of the cardiovascular system: tachycardia, increase or decrease in blood pressure, arrhythmia and angina pectoris;
• problems with the function of the blood and lymph system: anemia, which has a plastic form, thrombocytopenic purpura or thrombocytopenia, as well as pancytopenia, which can lead to death;
• disorders of the nervous system: headaches, convulsions, dizziness, tremors, aseptic meningitis and paresthesia;
• lesions affecting the gastrointestinal tract: pressure in the stomach area, nausea, gastrointestinal dysfunction, diarrhea, bloating and vomiting;
• disorders in the subcutaneous layer and epidermis: epidermal redness, itching, TEN, urticaria and SJS;
• vascular dysfunction: bleeding, hot flashes, peripheral edema;
• immune damage: anaphylactoid or anaphylactic symptoms, anaphylaxis, Quincke's edema and bronchial spasm;
• problems associated with the functioning of the gallbladder and liver: intrahepatic cholestasis;
• mental disorders: sleep disorders, agitation and hallucinations;
• damage to the visual organs: conjunctivitis, retinal detachment or hemorrhage in its area, as well as visual impairment;
• Others: hypoglycemia, increased temperature or hyperhidrosis.

Overdose

Early signs of acute pentoxifylline poisoning include dizziness, nausea, decreased blood pressure, and tachycardia. In addition, agitation, areflexia, hot flashes, fever, and tonic-clonic seizures may occur, as well as loss of consciousness and dark brown vomit (a sign of bleeding in the gastrointestinal tract).

To eliminate acute intoxication and prevent the development of complications, intensive medical monitoring (specific and systemic) and therapeutic procedures are required.

Interactions with other drugs

The intensity of the decrease in blood sugar values observed when using hypoglycemic agents or insulin may be potentiated by the introduction of Pentilin. For this reason, the condition of people using medications for the treatment of diabetes mellitus should be closely monitored.

Post-marketing testing has shown an increase in anticoagulant properties in individuals using the drug in combination with K-antivitamins. When prescribing pentoxifylline or changing its dosage, anticoagulant effects in such patients should be monitored.

The medication is capable of potentiating the antihypertensive activity of antihypertensive drugs and other substances that can lower blood pressure.

Combined use of drugs with theophylline causes an increase in blood levels of the latter in some individuals. This may lead to an increase in the incidence and potentiation of the negative effects of theophylline.

Administration together with ketorolac may prolong the PT indices and increase the likelihood of bleeding. An increased likelihood of bleeding is also observed when using the drug together with meloxicam. For this reason, these medications should not be combined.

Storage conditions

Pentilin should be stored in a place inaccessible to small children. Temperature level – no more than 25°C.

Shelf life

Pentilin can be used within a 5-year period from the date of production of the medicinal substance.

Analogues

Analogues of the drug are Trental, Pentoxifarm and Flexital with Xanthinol nicotinate, as well as Agapurin, Trentan, Latren and Vazonit with Pentoxifylline.

Reviews

Pentilin receives different reviews, but for the most part they are positive. The drug is often used in the treatment of diseases in which blood flow disorders are observed. The drug has high therapeutic activity and has a fairly low price.

Doctors warn about the high probability of negative symptoms, which is why the drug can only be used with the prescription of the attending physician.