Pentoxifylline
Pentoxifylline: 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. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Pentoxifylline
ATX code: C04AD03
Active ingredient: pentoxifylline (pentoxifylline)
Manufacturer: Pharmproject, JSC (Russia); Organika, JSC (Russia); Shreya Life Science Pvt. Ltd. (Shreya Life Sciences Pvt. Ltd.) (India); Moskhimpharmpreparaty them. N. A. Semashko (Russia); Atoll, LLC (Russia); Pharmproject, CJSC (Russia); Borisov Plant of Medical Products, JSC (Republic of Belarus); Promomed Rus, OOO (Russia)
Description and photo update: 2019-19-08
Prices in pharmacies: from 37 rubles.
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Pentoxifylline is a drug with a vasodilator, antiaggregatory, angioprotective effect, which improves microcirculation.
Release form and composition
Dosage forms of the drug Pentoxifylline:
- Solution for intravenous and intra-arterial administration 20 mg / ml: transparent, colorless or slightly yellowish (in 5 ml ampoules, 5 or 10 ampoules in blisters or plastic containers (pallets), 1 or 2 packages (pallets) in a cardboard box);
- Solution for injection 20 mg / ml (in 5 ml ampoules, 3, 5 or 10 ampoules in blister strip or plastic packaging (pallets), 1-4 packages (pallets) in a cardboard box or 5 or 10 ampoules in a cardboard box pack);
- Solution for infusion 0.04%, 0.08%, 0.2%: transparent, colorless (in polymer containers of 100, 250 or 500 ml);
- Concentrate for the preparation of a solution for infusion 20 mg / ml (in ampoules of 5 ml, 5 ampoules in blisters or blisters, 1 or 2 blisters or packaging in a cardboard box, ampoule knife included);
- Concentrate for the preparation of a solution for intravenous and intra-arterial administration 20 mg / ml: slightly yellowish or colorless, transparent (in 5 ml ampoules, 5 or 10 ampoules in a set with an ampoule knife in a cardboard box or 5 or 10 ampoules in a contour cell or plastic packages (pallets), 1 or 2 packages (pallets) in a cardboard box complete with an ampoule knife);
- Film-coated retard tablets: pink, capsule-shaped, on one side there is a break line (in blisters of 10 or 20 pcs., 1-6 or 10 packs in a cardboard box);
- Enteric-coated tablets: biconvex, pink, two layers are visible in cross-section (in blisters of 10 or 20 pcs., 1-6 or 10 packs in a cardboard box; in dark polymer or glass jars of 10, 20, 30, 40, 50 or 60 pcs., 1 can in a cardboard box).
Composition of 1 ml solution for intravenous and intra-arterial administration:
- Active substance: pentoxifylline - 20 mg;
- Additional components: monobasic sodium phosphate, sodium chloride, water for injection.
Composition of 1 ml solution for injection:
- Active substance: Pentoxifylline - 20 mg;
- Additional components: sodium chloride, water for injection.
Composition of 1 ml solution for infusion:
- Active substance: pentoxifylline - 0.4, 0.8 or 2 mg;
- Additional components: sodium chloride, water for injection.
Composition of 1 ml of concentrate for preparation of solution for infusion:
- Active substance: pentoxifylline - 20 mg;
- Additional components: water for injection.
Composition of 1 ml of concentrate for preparation of solution for intravenous and intra-arterial administration:
- Active substance: pentoxifylline - 20 mg;
- Additional components: sodium dihydrogen phosphate, sodium chloride, sodium hydroxide solution 0.1 M, water for injection.
Composition of 1 retard film-coated tablet:
- Active substance: pentoxifylline - 400 mg;
- Additional components and shell: ethylcellulose, magnesium stearate, dibasic calcium phosphate, talc, hydroxypropyl methylcellulose, diethyl phthalate, titanium dioxide, carmoisin varnish.
Composition of 1 enteric-coated tablet:
- Active ingredient: pentoxifylline - 100 mg;
- Additional components: talc, lactose (milk sugar), carmoisine (azorubin), povidone (polyvinylpyrrolidone), potato starch, stearic acid, copolymer of methacrylic acid and ethyl acrylate 1: 1 (MAE-100 R collikut), polyethylene oxide-4000 (macrogol-4000), titanium dioxide (pigment titanium dioxide).
Pharmacological properties
Pharmacodynamics
Pentoxifylline is a xanthine derivative. Improves microcirculation and blood rheological properties. The mechanism of its action is based on the inhibition of phosphodiesterase and an increase in the content of adenosine triphosphate in erythrocytes, and cyclic 3,5-adenosine monophosphate in platelets. In this case, a simultaneous saturation of the energy potential occurs, which in turn leads to vasodilation, a decrease in the total peripheral vascular resistance, an increase in the minute and stroke volume of blood. The heart rate does not change significantly.
Pentoxifylline improves blood oxygenation (due to vasodilation of the lungs).
With intravenous administration, in addition to the indicated effects, there is an increase in collateral blood circulation, an increase in the volume of blood flowing through a unit of section.
In areas of impaired blood supply, the drug improves microcirculation. This is due to a decrease in blood viscosity, platelet disaggregation, and an increase in the elasticity of erythrocytes (due to the effect on the pathologically altered deformability of erythrocytes).
Against the background of occlusive lesions of the peripheral arteries (intermittent claudication), an increase in the walking distance is observed, night cramps of the calf muscles and pain at rest are eliminated.
Pharmacokinetics
Oral absorption is high.
Pentoxifylline undergoes a first pass effect through the liver. In this case, two main pharmacologically active metabolites are formed: 1-5-hydroxyhexyl-3,7-dimethylxanthine (I metabolite) and 1-3-carboxypropyl-3,7-dimethylxanthine (V metabolite). Their plasma concentration is 5 and 8 times higher than that of pentoxifylline, respectively.
C max (maximum concentration) is achieved in 1 hour, the substance is evenly distributed over tissues and organs.
T 1/2 (half-life) is in the range from 0.5 to 1.5 hours. In the first 4 hours, up to 90% of the dose is eliminated. Excretion route: kidneys - 94% in the form of metabolites (mainly V metabolite); intestines - 4%. Excreted in breast milk.
Excretion of metabolites in patients with severe renal impairment is slowed down. Against the background of liver dysfunction, bioavailability increases and T 1/2 is lengthened.
Indications for use
- Angioneuropathy (paresthesia, Raynaud's disease);
- Peripheral circulatory disorders caused by inflammatory processes, diabetes mellitus, atherosclerosis;
- Cerebral circulation disorders of the ischemic type (acute and chronic course);
- Obliterating endarteritis;
- Chronic, acute and subacute circulatory failure in the retina or choroid;
- Trophic tissue disorders associated with disorders of venous or arterial microcirculation (frostbite, trophic ulcers, gangrene, post-thrombophlebitic syndrome);
- Hearing impairment with a vascular etiology;
- Encephalopathy of atherosclerotic and discirculatory etiology.
Contraindications
Absolute:
- Myocardial infarction (acute course);
- Retinal hemorrhage;
- Severe atherosclerosis (coronary or cerebral);
- Massive bleeding;
- Hemorrhagic stroke (acute course);
- Severe heart rhythm disturbances;
- Age under 18;
- Pregnancy and lactation period;
- Hypersensitivity to the components of the drug, as well as other methylxanthines.
Relative (Pentoxifylline should be administered with caution in the presence of the following conditions / diseases):
- The tendency to arterial hypotension and labile blood pressure (the doctor sets the dosage regimen individually, the dose should be increased gradually);
- Peptic ulcer of the stomach and duodenum;
- Pronounced functional disorders of the kidneys (the doctor sets the dosage regimen individually, the dose should be increased gradually);
- Recently postponed surgical intervention (there is a high likelihood of bleeding).
Instructions for use Pentoxifylline: method and dosage
Solution for infusion, solution for intravenous and intra-arterial administration
Intra-arterial injection: speed - 10 mg per minute; the initial dose is 100 mg of the drug (in a 0.9% sodium chloride solution with a volume of 20-50 ml), then the dose is increased to 200-300 mg (in a 0.9% sodium chloride solution with a volume of 30-50 ml).
Intravenous Pentoxifylline is injected slowly drip over 90-180 minutes:
- Solution for infusion: dose - 50-100 mg, if necessary - 200 mg (maximum per day - 300 mg). During the introduction, the patient should be in the supine position;
- Solution for intravenous and intra-arterial administration: dose - 100 mg of the drug in 0.9% sodium chloride solution or 5% glucose (dextrose) solution with a volume of 250-500 ml. With severe atherosclerosis of the cerebral vessels, the introduction of the drug into the carotid artery is prohibited.
Patients with chronic renal failure (creatinine clearance less than 30 ml per minute) need a dose reduction of 30-50%.
For the treatment of diabetic or atherosclerotic lesions in a chronic form, a course of intravenous infusions is performed every other day or daily.
Pills
Pentoxifylline tablets are taken orally, without chewing or breaking (whole), washed down with water, preferably after meals.
As a rule, Pentoxifylline enteric-coated tablets are prescribed in 2 pieces. 3 times a day. The average daily dose is 600 mg, the maximum is 1200 mg. Most often, after 1-2 weeks, a single dose is reduced to 1 tablet, while the frequency of administration of Pentoxifylline remains unchanged.
The doctor determines the duration of the therapeutic course individually, as a rule, it is 1-3 months.
In chronic renal failure (creatine clearance less than 10 ml per minute), the dose should be reduced by 2 times.
Pentoxifylline in prolonged dosage forms is usually prescribed with a frequency of administration 2 times a day, the duration of the therapeutic course is from 2-3 weeks or more.
Side effects
- Central nervous system: anxiety, dizziness, convulsions, sleep disturbances, headache;
- Digestive system: loss of intestinal tone (atony), dry mouth, loss of appetite, hepatitis, occurring with intrahepatic cholestasis, exacerbation of cholecystitis;
- Cardiovascular system: arrhythmia, tachycardia, lowering blood pressure, cardialgia, progression of angina pectoris;
- Hemostatic system and hematopoietic organs: thrombocytopenia, pancytopenia, hypofibrinogenemia, leukopenia, bleeding from the vessels of the skin, mucous membranes of the intestine and / or stomach;
- Sense organs: visual impairment, visual field defect that does not reach its boundaries (scotoma);
- Skin and subcutaneous fat: swelling, increased brittleness of the nails, hyperemia of the skin of the face, rush of blood to the skin of the face and upper chest;
- Allergic reactions: skin hyperemia, angioedema, urticaria, itching, anaphylactic shock;
- Laboratory parameters: increased activity of hepatic transaminases (lactate dehydrogenase, alanine aminotransferase, aspartate aminotransferase) and alkaline phosphatase;
- Others: aseptic meningitis (rare).
In the case of the development of the first symptoms of a hypersensitivity reaction, it is necessary to urgently cancel the use of the drug.
During therapy, blood counts should be monitored regularly, which is associated with reports of bleeding (in the mucous membranes, skin, gastrointestinal tract), thrombocytopenia and aplastic anemia.
Overdose
The main symptoms: tonic-clonic seizures, tachycardia, dizziness, weakness, hyperthermia, lowering blood pressure, areflexia, fainting, signs of gastrointestinal bleeding (vomiting like coffee grounds), agitation / drowsiness, loss of consciousness.
Therapy: gastric lavage, intake of activated charcoal, then symptomatic treatment is prescribed, which is aimed at maintaining respiratory function and blood pressure; with bleeding, urgent measures are taken.
special instructions
When used together with anticoagulants, it is necessary to carefully monitor the indicators of the blood coagulation system.
The compatibility of Pentoxifylline with infusion solutions must be checked on an individual basis.
Patients with severe renal impairment need careful monitoring of the condition.
In cases of retinal hemorrhage, treatment is immediately canceled.
After undergoing surgical interventions in recent years, it is necessary to systematically monitor the level of hemoglobin and hematocrit.
Therapy, especially intra-arterial and intravenous administration of Pentoxifylline, should be carried out under the control of blood pressure. For patients with unstable or low blood pressure, the dose is reduced.
In chronic heart failure, before starting the course, compensation of blood circulation should be achieved.
The appointment of Pentoxifylline in large doses to patients with diabetes mellitus undergoing therapy with hypoglycemic drugs can lead to hypoglycemia (such patients need dose adjustment).
In smoking patients, the therapeutic efficacy of Pentoxifylline may be reduced.
In elderly patients, in some cases, the drug is prescribed in reduced doses (associated with a decrease in the rate of excretion of the active substance and an increase in its bioavailability).
Application during pregnancy and lactation
According to the instructions, Pentoxifylline is not prescribed during pregnancy / lactation.
Pediatric use
Pentoxifylline therapy is contraindicated in patients under 18 years of age.
With impaired renal function
In severe renal failure, treatment is carried out under medical supervision.
For violations of liver function
Pentoxifylline for liver failure is prescribed under medical supervision.
Drug interactions
The combined use of Pentoxifylline with certain drugs / substances can lead to the development of the following effects:
- Cimetidine: the concentration of pentoxifylline in the blood plasma increases and, as a result, the likelihood of adverse reactions;
- Valproic acid, heparin, theophylline, fibrinolytic drugs, antihypertensive and hypoglycemic agents (insulin, oral hypoglycemic agents), drugs that affect the blood coagulation system (anticoagulants, thrombolytics), antibiotic drugs (including cephalosporins): their effect is enhanced
- Other xanthines: Excessive nervous excitement develops.
Analogs
The analogues of Pentoxifylline are: Agapurin, Vazonit, Latren, Pentilin, Pentoxipharm, Pentoxifylline NAN, Pentoxifylline Zentiva, Pentoxifylline-Eskom, Pentoxifylline-Darnitsa, Trental, Trental 400, Trenpental, Flexital.
Terms and conditions of storage
Store in a dry, dark place, out of reach of children.
Shelf life:
- Retard tablets - 3 years at temperatures up to 25 ° C;
- Enteric-coated tablets - 2 years at temperatures up to 30 ° C;
- Concentrate for preparation of solution for intravenous and intra-arterial administration, solutions for injections, infusions, intravenous and intra-arterial administration - 2 years at temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pentoxifylline
According to reviews, Pentoxifylline is an effective vasodilator that improves microcirculation. It has a wide range of indications, improves blood properties, reduces its viscosity. They also indicate a low cost in comparison with analogs. The disadvantages include the need for a long course and the development of adverse reactions.
Price for Pentoxifylline in pharmacies
The approximate price for Pentoxifylline is: retard tablets (400 mg each, 20 pcs.) - from 273 rubles, enteric-coated tablets (100 mg each, 60 pcs.) - from 62 rubles, injection solution (20 mg / ml, 10 ampoules of 5 ml each) - from 35 rubles, concentrate for the preparation of a solution for intravenous and intra-arterial administration (20 mg / ml, 10 ampoules of 5 ml each) - from 36 rubles.
Pentoxifylline: prices in online pharmacies
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Drug name Price Pharmacy |
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Pentoxifylline 100 mg enteric-coated tablets 60 pcs. RUB 37 Buy |
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Pentoxifylline (for injection) 20 mg / ml concentrate for preparation of a solution for intravenous and intra-arterial administration 5 ml 10 pcs. RUB 40 Buy |
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Pentoxifylline (for injection) 20 mg / ml concentrate for preparation of a solution for intravenous and intra-arterial administration 5 ml 10 pcs. RUB 42 Buy |
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Pentoxifylline (for injection) 20 mg / ml concentrate for preparation of a solution for intravenous and intra-arterial administration 5 ml 10 pcs. 43 rbl. Buy |
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Pentoxifylline (for injection) 20 mg / ml concentrate for preparation of solution for infusion 5 ml 10 pcs. RUB 54 Buy |
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Pentoxifylline 100 mg enteric-coated tablets 60 pcs. RUB 69 Buy |
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Pentoxifylline sol. for in. 20 mg / ml amp. 5 ml 10 Pcs. RUB 78 Buy |
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Pentoxifylline 100 mg enteric-coated tablets 60 pcs. RUB 78 Buy |
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Pentoxifylline Sanofi 100 mg film-coated tablets 60 pcs. 231 RUB Buy |
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Pentoxifylline 400 mg film-coated tablets retard 20 pcs. 265 RUB Buy |
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Pentoxifylline SR Zentiva 400 mg film-coated prolonged-release tablets 20 pcs. 267 r Buy |
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Reviews Pentoxifylline SR Zentiva 267 r Buy |
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Pentoxifylline Sanofi tablets p.o. 100mg 60 pcs. 278 r Buy |
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Pentoxifylline tablets retard p.o. enteric solution. 400mg 20 pcs. 305 RUB Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
