Pentoxifylline tablets 100 mg, 60 pcs.
Manufacturer
Ozon, Russia
Compound
Each enteric-coated tablet contains as
an active substance:
pentoxifylline - 100 mg
Excipients: milk sugar (lactose), potato starch, stearic acid, polyvinylpyrrolidone (povidone), methacrylic acid copolymer - ethyl acrylate 1: 1 (collicut MAE-100 R), macrogol-4000 (polyethylene oxide-4000), talc, titanium dioxide pigment (titanium dioxide), azorubine (carmoisine).
pharmachologic effect
Pharmacotherapeutic group: Vasodilating agent.
ATX: C04AD03 Pharmacological properties Pharmacodynamics
Pentoxifylline improves microcirculation and rheological properties of blood, has a vasodilating effect, blocks phosphodiesterase and promotes the accumulation of cAMP in cells. Pentoxifylline inhibits the aggregation of platelets and erythrocytes, increases their elasticity, reduces the level of fibrinogen in plasma and enhances fibrinolysis, which reduces blood viscosity and improves its rheological properties. It has a weak myotropic, vasodilating effect. Pentoxifylline slightly reduces total peripheral resistance and slightly dilates the coronary vessels.
In general, Pentoxifylline causes an improvement in microcirculation and oxygen supply to tissues in the brain and limbs, and to a lesser extent in the kidneys.
Pharmacokinetics
After oral administration, Pentoxifylline is almost completely absorbed from the gastrointestinal tract. The drug undergoes a “first pass” through the liver to form 2 main pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite 1) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V). The concentration of metabolite I and V in plasma is, respectively, 5 and 8 times higher than pentoxifylline. The time to reach maximum concentration is 1 hour. The half-life is 0.5 - 1.5 hours.
Pentoxifylline is excreted primarily by the kidneys - 94% in the form of metabolites (mainly metabolite V), by the intestines - 4%, in the first 4 hours. up to 90% of the dose is excreted. Excreted in breast milk. In severe renal impairment, the elimination of metabolites is slowed down. If liver function is impaired, there is an increase in half-life and increased bioavailability.
Indications
- peripheral circulatory disorders caused by atherosclerosis, diabetes mellitus (diabetic angiopathy); — chronic cerebrovascular accidents of ischemic origin; - atherosclerotic and discirculatory encephalopathies; angiopathy (paresthesia, Raynaud's disease); - trophic tissue disorders due to impaired arterial or venous microcirculation (trophic ulcers, postthrombophlebitic syndrome, frostbite, gangrene); - obliterating endarteritis; - acute, subacute and chronic circulatory failure in the retina or choroid; - hearing impairment of vascular origin.
Contraindications
Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, Porphyria;
acute myocardial infarction; massive bleeding; hemorrhages in the retina of the eye; cerebral hemorrhage, acute hemorrhagic stroke; severe coronary or cerebral atherosclerosis; severe heart rhythm disturbances; pregnancy; breastfeeding period; age under 18 years (efficacy and safety have not been established). With caution: the drug is prescribed to patients with atherosclerosis of the cerebral and/or coronary vessels, especially in cases of arterial hypotension and cardiac arrhythmias, heart failure, and liver failure. You should also be careful when prescribing Pentoxifylline to patients with peptic ulcers of the stomach and duodenum, and to patients who have recently undergone surgery (risk of bleeding).
For patients with labile blood pressure and a tendency to arterial hypotension and patients with severe renal impairment, the dose is increased gradually and selected individually
Side effects
From the central nervous system: headache, dizziness;
anxiety, sleep disorders; convulsions. From the skin and subcutaneous tissue: hyperemia of the facial skin, “flushes” of blood to the skin of the face and upper chest, swelling, increased fragility of nails.
From the digestive system: dry mouth, loss of appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.
From the senses: blurred vision, scotoma.
From the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, decreased blood pressure.
From the hematopoietic organs and hemostasis system: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from blood vessels of the skin, mucous membranes. stomach, intestines.
Allergic reactions: itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.
Laboratory indicators: increased activity of “liver” transaminases (ALT, AST, LDH) and alkaline phosphatase.
Interaction
Pentoxifylline enhances the effect of heparin, fibrinolytic drugs, theophylline, antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).
Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetan), valproic acid.
Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects).
Co-administration with other xanthines may lead to excessive nervous agitation in patients.
How to take, course of administration and dosage
Pentoxifylline is taken orally after meals.
The tablets are coated with a special coating that is soluble in the intestines, so they are swallowed whole with a small amount of water. Take 0.2 g (2 tablets) 3 times a day. After achieving a therapeutic effect (usually 1-2 weeks), the dose is reduced to 0.1 g (1 tablet) 3 times a day. The maximum daily dose is 1200 mg. The course of treatment is 1-3 months.
In patients with chronic renal failure (creatine clearance less than 10 ml/min.), the dose is halved.
The duration of treatment and dosage regimen with Pentoxifylline is determined by the attending physician individually, depending on the clinical picture of the disease and the resulting therapeutic effect.
Overdose
Symptoms: nausea, dizziness, cyanosis, tachycardia, marked decrease in blood pressure, redness of the skin, increased body temperature (chills), agitation, areflexia, tonic-clonic convulsions, vomiting “coffee grounds,” arrhythmias, loss of consciousness.
Treatment: symptomatic. Particular attention should be paid to maintaining blood pressure and respiratory function. Convulsions are relieved by administering diazepam. Urgent measures in case of severe anaphylactic reactions (shock):
- when primary symptoms appear (sweating, nausea, cyanosis), immediately stop taking the drug;
- in addition to other necessary measures, ensure a lower position of the head and upper body and provide freedom for breathing;
— urgent medical measures: administer intravenous epinephrine (adrenaline). If necessary, the administration of epinephrine can be repeated.
Special instructions
Patients with severe renal impairment when taking Pentoxifylline require especially careful medical supervision. If during the period of use of the drug patients experience hemorrhages in the retina of the eye, the drug is immediately discontinued. Treatment should be carried out under blood pressure control. In patients with diabetes mellitus taking hypoglycemic agents, administration in large doses may cause hypoglycemia (dose adjustment required). When prescribed simultaneously with anticoagulants, it is necessary to carefully monitor the blood coagulation system. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit levels is necessary. In older adults, dose reduction may be necessary (increased bioavailability and decreased rate of elimination). Smoking may reduce the therapeutic effectiveness of the drug.
Storage conditions
List B. In a dry place, at a temperature not exceeding 30°C. Keep out of the reach of children.
Best before date
2 years. Do not use after expiration date.
Active substance
Pentoxifylline
Conditions for dispensing from pharmacies
On prescription
Dosage form
pills
Barcode and weight
Barcode: 4607027769727 Weight: 0.026 kg
Pentoxifylline-SZ tab ppo prolong release 400 mg No. 20
Interaction
- With antihypertensive drugs
Pentoxifylline increases the risk of developing arterial hypotension when used simultaneously with antihypertensive agents (for example, ACE inhibitors) or other drugs with a potential antihypertensive effect (for example, nitrates).
- With drugs that affect the blood coagulation system
Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (direct and indirect anticoagulants, thrombolytics, antibiotics such as cephalosporins).
With the combined use of pentoxifylline and indirect anticoagulants (vitamin K antagonists), post-marketing studies have reported cases of increased anticoagulant action (risk of bleeding). Therefore, when starting to take pentoxifylline or changing its dose, it is recommended to monitor the severity of the anticoagulant effect in patients taking this combination of drugs, for example, regularly monitor the INR.
- With cimetidine
Cimetidine increases the concentration of pentoxifylline and active metabolite I in the blood plasma (risk of side effects).
- With other xanthines
Co-administration with other xanthines may lead to excessive nervous stimulation.
- With hypoglycemic agents (insulin and hypoglycemic agents for oral administration)
The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced by simultaneous use of pentoxifylline (increased risk of hypoglycemia). Strict monitoring of the condition of such patients is necessary, including regular glycemic control.
- With theophylline
In some patients, with simultaneous use of pentoxifylline and theophylline, an increase in theophylline concentration is observed. This may subsequently lead to an increase or worsening of theophylline-related side effects.
- With ciprofloxacin
In some patients, with simultaneous use of pentoxifylline and ciprofloxacin, an increase in the concentration of pentoxifylline in the blood plasma is observed. In the future, this may lead to an increase or intensification of side effects associated with the use of this combination.
- With platelet aggregation inhibitors
With simultaneous use of pentoxifylline with platelet aggregation inhibitors (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [except selective COX-2 inhibitors], acetylsalicylic acid, ticlopidine, dipyridamole), a potential additive effect may develop, increasing the risk of bleeding . Therefore, due to the risk of bleeding, pentoxifylline should be used with caution simultaneously with the above platelet aggregation inhibitors.
Pentoxifylline, concentrate d/pig solution for infusion 20 mg/ml, ampoules 5 ml, 10 pcs.
Pentoxifylline is a xanthine derivative. Improves microcirculation and rheological properties of blood. The mechanism of action is associated with inhibition of phosphodiesterase and an increase in the content of cyclic 3,5 adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (ATP) in erythrocytes with simultaneous saturation of energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in systolic and minute blood volume without a significant change in heart rate. By dilating the coronary arteries, it increases the delivery of oxygen to the myocardium (minor antianginal effect), and the blood vessels of the lungs improve blood oxygenation. When administered intravenously, it leads to increased collateral circulation and an increase in the volume of blood flowing through a sectional unit. Reduces blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (due to the effect on the pathologically altered deformability of red blood cells). Improves microcirculation in areas of poor circulation. With occlusive lesions of the peripheral arteries (“intermittent” claudication), it leads to an increase in walking distance, elimination of night cramps of the calf muscles and pain at rest. Pharmacokinetics The drug after administration is rapidly metabolized in the liver. During the metabolism, two main metabolites are formed: 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) and 1-(3-carboxypropyl)-3,7-dimethylxanthine (metabolite V), which have activity similar to pentoxifylline . 1.5-2 hours after infusion, the concentration of metabolites I and V in the blood plasma is, respectively, 5 and 8 times higher than the concentration of the original substance. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood decreases significantly (up to 10% of the initial value). The half-life is from 30 minutes to 1.5 hours. It is excreted mainly by the kidneys (94%) in the form of metabolites (mainly metabolite V), and by the intestines (4%). in the first 4 hours, up to 90% of the dose is eliminated. 2% of the drug is excreted unchanged. Pentoxifylline and its metabolites do not bind to plasma proteins. Excreted in breast milk. In severe renal impairment, the elimination of metabolites is slowed down. If liver function is impaired, there is an increase in half-life and increased bioavailability.
Pentoxifylline SR Zentiva extended-release tablets 400 mg No. 20
A country
Slovakia
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Pentoxifylline
Compound
Active substance: pentoxifylline 400 mg. excipients: core: hypromellose 2200/15000 - 0.12000/0.12000 g, povidone 40 - 0.01650/0.02500 g, +C142 talc - 0.01050/0.02000 g, magnesium stearate - 0.00300 /0.00500 g; shell: sepifilm 752 white (hypromellose - 35.0% - 45.0%. microcrystalline cellulose - 27.0% - 37.0%, macrogol stearate - 6.0% - 10.0%. titanium dioxide - 18.0% - 22.0%) - 0.01500/0.01970 g, dimethicone emulsion - 0.000075/0.00010 g, macrogol 6000 - 0.000175/0.00020 g.
pharmachologic effect
An agent that improves microcirculation, angioprotector, and a dimethylxanthine derivative. Pentoxifylline reduces blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (due to the effect on the pathologically altered deformability of red blood cells), improves microcirculation and increases the concentration of oxygen in tissues. It increases the concentration of cAMP in platelets and ATP in erythrocytes with simultaneous saturation of energy potential, which in turn leads to vasodilation, a decrease in peripheral resistance, an increase in stroke volume and minute blood volume without a significant change in heart rate. By dilating the coronary arteries, it increases the delivery of oxygen to the myocardium, dilating the vessels of the lungs, and improves blood oxygenation. Increases the tone of the respiratory muscles (intercostal muscles and diaphragm). IV administration, along with the above action, leads to increased collateral circulation and an increase in the volume of blood flowing through a sectional unit. Increases the concentration of ATP in the brain, has a beneficial effect on the bioelectrical activity of the central nervous system. Improves microcirculation in areas of impaired blood supply. With occlusive lesions of the peripheral arteries (intermittent claudication), it leads to an increase in walking distance, elimination of night cramps of the calf muscles and pain at rest.
Indications for use
Peripheral circulatory disorders (including intermittent claudication) associated with chronic occlusive circulatory disorders in the arterial vessels of the lower extremities. Ischemic cerebrovascular accident, ischemic stroke and post-stroke conditions; cerebral atherosclerosis (dizziness, headache, memory impairment, sleep disturbances), dyscirculatory encephalopathy, viral neuroinfection (prevention of possible microcirculation disorders). IHD, a condition after myocardial infarction. Diabetic angiopathy. Acute circulatory disorders in the retina and choroid, acute ischemic optic neuropathy. Otosclerosis, degenerative changes against the background of pathology of the vessels of the inner ear with a gradual decrease in hearing. COPD, bronchial asthma. Impotence of vascular origin.
Mode of application
Use intravenously (stream or drip), intravenously (stream or drip), intramuscularly, orally. The dose and treatment regimen are determined individually.
Interaction
Pentoxifylline may potentiate the effect of antihypertensive drugs. Parenteral use of pentoxifylline in high doses may enhance the hypoglycemic effect of insulin in patients with diabetes mellitus. When used simultaneously with ketorolac, there may be an increased risk of bleeding and/or an increase in prothrombin time; with meloxicam - increased risk of bleeding; with sympatholytics, ganglion blockers and vasodilators - a decrease in blood pressure is possible; with heparin, fibrinolytic drugs - increased anticoagulant effect. Cimetidine significantly increases the concentration of pentoxifylline in the blood plasma, and therefore, with simultaneous use, the likelihood of developing side effects may increase.
Side effect
From the central nervous system: headache, dizziness; anxiety, sleep disturbances, seizures. Dermatological reactions: hyperemia of the facial skin, “flushes” of blood to the skin of the face and upper chest, swelling, increased brittleness of nails. From the digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, increased activity of liver transaminases and alkaline phosphatase. From the organ of vision: visual impairment, scotoma. From the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, decreased blood pressure. From the hematopoietic system: thrombocytopenia, leukopenia, pancytopenia. From the blood coagulation system: hypofibrinogenemia, bleeding from the vessels of the skin, mucous membranes, stomach, intestines. Allergic reactions: itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.
Contraindications
Acute myocardial infarction, porphyria, massive bleeding, hemorrhagic stroke, retinal hemorrhage, pregnancy, lactation. For intravenous administration (additionally) - arrhythmias, severe atherosclerosis of the coronary or cerebral arteries, uncontrolled arterial hypotension. Hypersensitivity to pentoxifylline and other xanthine derivatives.
special instructions
Use with caution in case of lability of blood pressure (tendency to arterial hypotension), chronic heart failure, peptic ulcer of the stomach and duodenum (for oral administration), after recent surgical interventions, with liver and/or kidney failure, in children and adolescents under the age of 18 years (efficacy and safety have not been studied). In cases of renal dysfunction or severe liver dysfunction, adjustment of the pentoxifylline dosage regimen is required. During treatment, blood pressure levels should be monitored. When used simultaneously with antihypertensive drugs, insulin, or oral hypoglycemic drugs, a reduction in the dose of pentoxifylline may be required. When used simultaneously with anticoagulants, blood clotting parameters should be carefully monitored.
Dispensing conditions in pharmacies
On prescription
