Pentylin
Pentilin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Pentilin
ATX code: C04AD03
Active ingredient: Pentoxifylline (Pentoxifylline)
Manufacturer: KRKA (Slovenia)
Description and photo update: 2018-25-10
Pentylin is a vasodilator.
Release form and composition
- solution for intravenous and intra-arterial administration: transparent, colorless or slightly yellowish (5 ml in ampoules, 5 ampoules in a blister or a plastic tray, in a cardboard box 1 blister or tray);
- tablets of prolonged action, film-coated: oval, biconvex, white (10 pcs. in a blister, 2 blisters in a cardboard box).
Composition of 1 ampoule of Pentylin solution (5 ml):
- active substance: pentoxifylline - 100 mg;
- additional components: sodium hydrogen phosphate dihydrate, sodium dihydrogen phosphate dihydrate, sodium chloride, disodium edetate, water for injection.
Composition of 1 tablet Pentilin:
- active substance: pentoxifylline - 400 mg;
- additional components: magnesium stearate, hypromellose, macrogol 6000, colloidal anhydrous silicon dioxide;
- shell: hypromellose, macrogol 6000, talc, titanium dioxide E171.
Pharmacological properties
Pharmacodynamics
Pentoxifylline - the active substance Pentylin is an antispasmodic agent from the group of purines that improves rheological properties (fluidity) and blood microcirculation. The mechanism of action of the drug is due to its ability to inhibit phosphodiesterase and increase the concentration of cyclic AMP in platelets and ATP in erythrocytes, while simultaneously saturating the energy potential, as a result of which vasodilation develops, the total peripheral vascular resistance decreases, the stroke and minute blood volume increases, while the heart rate does not significantly changes.
Pentoxifylline dilates the coronary arteries, thereby increasing the delivery of oxygen to the myocardium (antianginal effect), and the vessels of the lungs, thereby improving blood oxygenation.
The drug increases the tone of the respiratory muscles, in particular the diaphragm and intercostal muscles.
Improves blood microcirculation in areas of impaired blood circulation, increases the elasticity of the erythrocyte membrane, reduces blood viscosity.
In case of occlusive lesion of the peripheral arteries (intermittent claudication), Pentylin lengthens the walking distance, eliminates night cramps of the calf muscles and pain at rest.
Pharmacokinetics
Pentoxifylline is extensively metabolized in erythrocytes and liver. After oral administration, it is almost completely absorbed from the gastrointestinal tract. The prolonged form of tablets provides continuous release of the active component of the drug and its uniform absorption.
Pentoxifylline undergoes primary passage through the liver, resulting in the formation of two main pharmacologically active metabolites: 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V) and 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I), plasma the concentration of which is 8 and 5 times higher, respectively, than pentoxifylline.
Pentoxifylline and its metabolites do not bind to blood plasma proteins.
The drug in prolonged form reaches the maximum concentration within 2–4 hours. Distributed evenly. The half-life is 0.5-1.5 hours.
The half-life of pentoxifylline after an intravenous dose of 100 mg is approximately 1.1 hours. It has a large volume of distribution (after a 30-minute infusion of 200 mg - 168 l), as well as a high clearance (4500-5100 ml / min).
94% of the received dose is excreted by the kidneys in the form of metabolites (mainly V metabolite), about 4% - by the intestine. In this case, up to 90% of the dose is excreted within the first 4 hours. Excretion of metabolites is slowed down in patients with severe renal impairment. In case of impaired liver function, the half-life of pentoxifylline is lengthened and its bioavailability increases.
Pentoxifylline is excreted in breast milk.
Indications for use
- hearing impairment of vascular origin;
- chronic, subacute and acute circulatory failure in the retina and in the choroid;
- chronic disorders of cerebral circulation of ischemic genesis;
- obliterating endarteritis;
- peripheral circulatory disorders due to atherosclerosis, diabetes mellitus (diabetic angiopathy);
- angiopathy (paresthesia, Raynaud's disease);
- trophic tissue damage due to impaired venous or arterial microcirculation (frostbite, post-thrombophlebitic syndrome, trophic ulcers, gangrene);
- discirculatory and atherosclerotic encephalopathy.
Contraindications
- hemorrhage in the brain;
- hemorrhage in the retina;
- massive bleeding;
- acute hemorrhagic stroke;
- severe arrhythmias;
- uncontrolled arterial hypotension;
- acute myocardial infarction;
- severe atherosclerotic lesions of the coronary or cerebral arteries;
- porphyria;
- pregnancy, lactation period;
- age up to 18 years;
- hypersensitivity to the components of Pentylin or other methylxanthines.
Carefully:
- arterial hypotension;
- chronic heart failure;
- impaired renal function (creatinine clearance below 30 ml / min);
- severe liver dysfunction;
- increased tendency to bleeding, including with the use of anticoagulants, disorders of the blood coagulation system, after recently underwent surgery;
- peptic ulcer and 12 duodenal ulcer - for tablets.
Instructions for use of Pentylin: method and dosage
Injection
In the form of a solution, Pentylin is administered intravenously or intraarterially.
The doctor determines the route of administration and the optimal dose of the drug for each patient, depending on the severity of circulatory disorders and the individual tolerance of pentoxifylline. Intravenous infusions are performed with the patient lying down.
As a rule, for adult patients, the drug is prescribed intravenously 2 times a day (morning and afternoon), 200 mg (2 ampoules of 5 ml) or 300 mg (3 ampoules of 5 ml) in 250 or 500 ml of 0.9% sodium chloride solution or Ringer's solution. Compatibility with other infusion solutions must be tested separately, but only clear solutions should be used.
The duration of the infusion is at least 60 minutes for a dose of 100 mg pentoxifylline. The volumes administered may decrease in the presence of concomitant diseases, for example, heart failure. In such cases, it is worth using a special infuser to control the infusion.
After a daily infusion, if necessary, Pentylin tablets 400 mg are additionally prescribed - 2 pcs. If two infusions are made at longer intervals, then 1 tablet can be taken earlier (at about 12 noon).
In cases where intravenous infusion due to clinical conditions can be performed only once a day, it is possible to additionally prescribe Pentylin in tablets in the amount of 3 pcs. (2 tablets at noon, 1 in the evening).
In severe cases, for example, with gangrene, trophic ulcers of the III-IV stage according to the Fontaine-Leriche-Pokrovsky classification, severe pain at rest, prolonged intravenous administration of the drug is indicated - within 24 hours.
Recommended dosages for intra-arterial administration: at the beginning of treatment - 100 mg of pentoxifylline in 50-100 ml of 0.9% sodium chloride solution, on the following days - 100-400 mg in 50-100 ml of 0.9% sodium chloride solution. The rate of administration is 10 mg / minute, the duration of the administration is 10-30 minutes.
During the day, you can enter the drug in a dose of up to 1200 mg. In this case, the individual dose can be calculated using the following formula: 0.6 mg of pentoxifylline per kg of body weight per hour. Thus, the daily dose will be 1000 mg for a patient with a body weight of 70 kg, 1150 mg for a patient with a body weight of 80 kg.
Patients with renal insufficiency, depending on the individual tolerance of the drug, the dose is reduced by 30-50%.
A dose reduction is also required in patients with severely impaired liver function, while the individual tolerance of Pentylin should be taken into account.
It is recommended to start treatment with lower doses with a gradual increase in them in patients with low blood pressure, as well as in patients prone to lower blood pressure (for example, with severe coronary heart disease, hemodynamically significant cerebral vascular stenosis).
Pills
Pentylin 400 mg tablets should be taken orally, after meals: swallow whole and drink plenty of water.
The recommended dose is 1 tablet 2 or 3 times a day. Do not exceed a daily dose of 1200 mg.
For patients with chronic renal failure (creatinine clearance <10 ml / minute), the dose is halved.
The recommended starting dose for patients on hemodialysis is 400 mg (1 tablet) per day. Further, if the need arises, it is gradually increased.
The doctor sets the duration of treatment individually, depending on the clinical picture of the disease and the severity of the therapeutic effect. An improvement in the condition is usually noted after 2-4 weeks, but therapy is recommended for at least 8 weeks - this is how much is required to adequately assess the effectiveness of the treatment.
Side effects
- allergic reactions: pruritus, urticaria, skin flushing, anaphylactic shock, angioedema;
- on the part of the hemostatic system and hematopoietic organs: hypofibrinogenemia, pancytopenia, thrombocytopenia, leukopenia, bleeding from the vessels of the skin / intestines / mucous membranes of the stomach;
- from the digestive system: increased activity of liver enzymes, intestinal atony, anorexia, nausea, xerostomia, diarrhea, vomiting, cholestatic hepatitis, increased alkaline phosphatase, exacerbation of cholecystitis;
- from the central and peripheral nervous system: anxiety, dizziness, sleep disturbances, headache, convulsions;
- on the part of the cardiovascular system: progression of angina pectoris, cardialgia, lowering blood pressure, arrhythmia, tachycardia;
- from the senses: scotoma, visual impairment;
- on the part of the skin and subcutaneous fat: increased brittleness of the nails, edema, flushing of the skin of the face and upper chest, hyperemia of the skin of the face;
- others: hypoglycemia.
Overdose
Symptoms: dizziness, cyanosis, sweating, weakness, nausea, signs of gastrointestinal bleeding (vomiting like "coffee grounds"), drowsiness or agitation, hyperthermia, tachycardia, arrhythmia, decreased blood pressure, tonic-clonic seizures, loss of consciousness, areflexia, fainting.
Treatment of overdose is symptomatic, special attention should be paid to maintaining blood pressure and respiratory function, as well as urgent measures for bleeding, if required. You should immediately stop using the drug, provide the patient with a horizontal position with a lower position of the head and upper body. After an overdose of Pentylin in tablet form, gastric lavage and intake of activated charcoal are recommended. Convulsive seizures are stopped by the introduction of diazepam.
special instructions
Treatment with Pentylin should be carried out under the control of blood pressure.
Patients who have undergone surgery in the near past need to systematically monitor the level of hematocrit and hemoglobin.
In the case of the combined use of anticoagulants, it is necessary to monitor the indicators of the blood coagulation system.
In high doses, Pentilin can cause the development of severe hypoglycemia in patients with diabetes mellitus receiving hypoglycemic agents, therefore, a dose adjustment of pentoxifylline is required.
Dose reduction is required in patients with low or unstable blood pressure.
Smoking can reduce the therapeutic efficacy of pentoxifylline.
Whether the Pentylin solution is compatible with other infusion solutions or not should be checked in each case before starting therapy.
Influence on the ability to drive vehicles and complex mechanisms
There is no data on the effect of Pentylin on a person's ability to drive vehicles and perform work with potentially dangerous consequences (activities requiring speed of reactions and / or increased attention).
Application during pregnancy and lactation
According to the instructions, Pentylin is contraindicated during pregnancy.
If it is necessary to carry out therapy during lactation, the issue of stopping breastfeeding should be resolved.
Pediatric use
Pentylin is contraindicated before the age of 18.
With impaired renal function
The drug should be used with caution in case of impaired renal function (creatinine clearance below 30 ml / min).
For violations of liver function
Pentylin should be used with caution in severe liver dysfunction.
Use in the elderly
In old age, an increase in bioavailability and a decrease in the rate of excretion of pentoxifylline are possible. In this case, a decrease in the dose of Pentylin is required.
Drug interactions
- drugs that lower blood pressure (including nitrates, angiotensin-converting enzyme inhibitors): their effect is enhanced;
- meloxicam: the risk of bleeding increases;
- valproic acid, antibiotics (including cephalosporins - cefoperazone, cefamandol, cefotetan), drugs affecting the blood coagulation system (including thrombolytics, direct and indirect anticoagulants): their effect is enhanced;
- ciprofloxacin: the plasma concentration of pentoxifylline increases (it is recommended to reduce its dose by 2 times);
- oral hypoglycemic agents, insulin: it is possible to enhance their action and increase the risk of hypoglycemia (it is necessary to strictly monitor patients receiving such combinations);
- cimetidine: increases the plasma concentration of pentoxifylline and the risk of side effects;
- blockers of H 2 -receptors (nizatidine, ranitidine, famotidine): excessive nervous excitement is possible;
- ketorolac: increases prothrombin time and the risk of bleeding;
- theophylline: an increase in its concentration is possible and, as a result, an increase / increase in its side effects.
Analogs
Pentoxifylline analogs are: Trental, Agapurin, Trenpental, Vazonit, Pentoxifylline-Eskom, Flexital, Pentoxifylline, Pentoxifylline Zentiva, Pentoxifylline Sandoz, Pentoxifylline-FPO, Pentoxifylline-SZ, Trentaline 400, Pentoxifylline.
Terms and conditions of storage
Store at temperatures up to 25 ° C out of reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pentilin
According to reviews, Pentylin is an effective antispasmodic agent that improves blood circulation and the rheological properties of blood, eliminates calf muscle cramps and pain.
The disadvantages of the drug, many include a large list of side effects and contraindications to its use.
Price for Pentylin in pharmacies
The price of Pentylin is not known, since the drug is not registered in the Russian Federation today.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
