Pentylin

Pentylin is a drug that dilates peripheral vessels. Contains the element pentoxifylline (methylxanthine derivative).

The principle of the influence of the active element is associated with the suppression of PDE activity and the accumulation of cAMP inside smooth muscle vascular and blood cells, and in addition, 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 the increased plasma levels of fibrinogen and potentiates fibrinolysis, thereby improving the rheological parameters of the blood and reducing the blood viscosity. [1]

Indications Pentylin

It is applied in case of such violations:

• encephalopathy of an atherosclerotic or dyscirculatory nature, having a cerebral form of ischemic stroke and disorders of peripheral blood flow associated with inflammation, atherosclerosis or diabetes mellitus (this includes angiopathy of diabetic origin);
• angioneuropathy ( Raynaud's syndrome );
• trophic tissue damage caused by microcirculation disorders or problems with veins (trophic type ulcers, frostbite, post-thrombophlebitic syndrome or gangrene);
• obliterating endarteritis ;
• disorder of intraocular blood flow (insufficiency of blood flow inside the choroid and retina, which has a subacute, acute or chronic form);
• problems with the work of the inner ear, which are of a vascular nature (with a weakening of hearing).

Release form

The release of the drug element is realized in the form of an injection liquid - inside ampoules with a capacity of 5 ml (0.1 g). Inside the cell pack contains 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 oxygen supply to tissues (the greatest activity is noted inside the central nervous system and extremities; it acts moderately inside the kidneys).

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

Pharmacokinetics

The main metabolic element that has a therapeutic effect (1- (5-hydroxyhexyl) -3,7-dimethylxanthine) is found inside the blood plasma in volumes that are twice the value of the unchanged component, and also remain in the form of an inverse biochemical balance with it. Because of this, pentoxifylline with its metabolic element is considered as a single active substance.

The half-life of pentoxifylline is 1.6 hours.

The substance is fully involved in metabolic processes, and more than 90% of it is excreted through the kidneys in the form of polar metabolic components soluble in water that cannot be conjugated. Less than 4% of the applied portion is excreted with feces.

In people with severe renal dysfunction, the processes of excretion of metabolic components slow down.

In individuals with hepatic dysfunction, there is a prolongation of the half-life of pentoxifylline.

Dosing and administration

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

Basically, the following therapy regimens are prescribed:

• introduction through infusion of 0.1-0.6 g of pentoxifylline (dissolved in 0.9% NaCl (0.1-0.5 l)), 1-2 times a day. The duration of the intravenous administration of the substance is 1-6 hours (0.1 g of pentoxifylline should be administered within a period of at least 1 hour). In addition to infusion, Pentylin is taken orally (0.4 g portion, with the expectation that the highest daily dosage, including oral administration and infusion, is 1.2 g);
• in the case of a very severe course of the disease (especially with regular pain, trophic type ulcers or gangrene), the drug infusion can be administered over a period of 24 hours. In the case of the specified scheme of use, the portion size is selected in the ratio of 0.6 mg / kg / h. With a similar 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 forbidden to inject more than 1.2 g of drugs per day. The volumes of the infusion fluid are determined personally, taking into account the concomitant pathologies and the patient's condition (on average, 1-1.5 liters per day);
• sometimes the medication can be injected through an intravenous injection (at a dosage of 5 ml (0.1 g)). The procedure is carried out at low speed, in 5 minutes. In this case, the patient should be in a supine position.

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

Dosage sizes in case of renal dysfunction.

When the CC level is below 30 ml per minute (0.5 ml / second), the portion is determined personally, reducing it by approximately 30-50% in comparison with the standard dosage.

Portion sizes for hepatic dysfunction.

If there is a marked disorder of hepatic activity, the portion of Pentylin is reduced, taking into account the personal tolerance in relation to drugs.

• Application for children

There is no experience with the use of drugs in pediatrics.

Use Pentylin during pregnancy

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

Small volumes of pentoxifylline are excreted in mother's milk. If you need to use the medicine, you should stop breastfeeding for a while.

Contraindications

Among the contraindications:

• severe intolerance associated with pentoxifylline, other elements of the drug or other substances from the subgroup of methylxanthines (including choline theophyllate, theobromine and caffeine with theophylline, and in addition aminophylline);
• very severe bleeding (there is a possibility of potentiation of bleeding);
• hemorrhage in the region of the eye retina or brain (the possibility of potentiation of bleeding). With the development of hemorrhage in the retinal region during the use of pentoxifylline, the drug should be discontinued immediately;
• active phase of myocardial infarction;
• ulcerative lesions in the gastrointestinal tract;
• having a hemorrhagic form of diathesis.

Side effects Pentylin

The main side symptoms:

• change in test readings: an increase in transaminase indicators;
• violations in the work of the CVS: tachycardia, an increase or decrease in blood pressure values, arrhythmia and angina pectoris;
• problems with the function of the blood system and lymph: aplastic anemia, thrombocytopenic purpura or thrombocytopenia, as well as pancytopenia, which can lead to death;
• disorders of the NA activity: headaches, convulsions, dizziness, tremors, meningitis of aseptic nature and paresthesia;
• lesions affecting the gastrointestinal tract: pressure in the stomach, nausea, gastrointestinal dysfunction, diarrhea, bloating and vomiting;
• violations in the subcutaneous layer and epidermis: epidermal redness, itching, TEN, urticaria and SS;
• disorder of vascular activity: bleeding, hot flashes, peripheral edema;
• immune lesions: anaphylactoid or anaphylactic signs, anaphylaxis, Quincke's edema and bronchial spasm;
• problems associated with the work 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, fever, or hyperhidrosis.

Overdose

Early signs of acute pentoxifylline poisoning include dizziness, nausea, decreased blood pressure and tachycardia. In addition, the appearance of excitement, areflexia, hot flashes, fever and seizures of the tonic-clonic type, as well as loss of consciousness and vomit that have a dark brown tint (a sign of bleeding in the gastrointestinal tract) is possible.

To eliminate acute intoxication and prevent complications, intensive medical supervision (specific and systemic) is required, as well as therapeutic procedures.

Interactions with other drugs

The intensity of the decrease in blood sugar values, observed with the use of hypoglycemic substances or insulin, can be potentiated with the introduction of Pentylin. Because of this, the condition of those using medications for the treatment of diabetes mellitus must be closely monitored.

In post-marketing tests, an increase in anticoagulant properties was found in individuals who used the drug in combination with K-antivitamins. When prescribing pentoxifylline or changing its dosage, the indicators of anticoagulant effect in such patients should be monitored.

The drug is able to potentiate the antihypertensive activity of antihypertensive drugs and other substances that can lower blood pressure.

The combined use of drugs with theophylline causes an increase in the blood values of the latter in some individuals. This can lead to an increase in the frequency of development and potentiation of the negative manifestations of theophylline.

Administration together with ketorolac can prolong PTT parameters and increase the likelihood of bleeding. An increase in the likelihood of bleeding is also noted when using drugs together with meloxicam. Because of this, these medications should not be combined.

Storage conditions

Pentylin must be kept out of the reach of small children. Temperature level - no more than 25 ° C.

Shelf life

Pentylin can be used within 5 years from the date of manufacture of the drug substance.

Analogs

Analogues of drugs are Trental, Pentoxipharm and Flexital with Xanthinol nicotinate, and in addition Agapurin, Trentan, Latren and Vazonit with Pentoxifylline.

Reviews

Pentylin has received varying reviews, but for the most part they are positive. The medication is often used in the treatment of diseases during which there is a disorder of the blood flow. The medicine has a high therapeutic activity and has a rather low price.

Doctors, on the other hand, warn of a high likelihood of negative signs, which is why drugs can be used only with the appointment of the attending doctor.