Pentoxifylline
Organica
901 Items
2019-09-19
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Clinical Pharmacology
Pentoxifylline is a derivative of xanthine. 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 the energy potential, which in turn leads to vasodilatation, decrease in total peripheral vascular resistance, an increase in systolic and minute blood volume without a significant change in heart rate. Expanding the coronary arteries, increases the delivery of oxygen to the myocardium (a slight antianginal effect), the vessels of the lungs - improves blood oxygenation.
When administered intravenously leads to increased collateral circulation, an increase in the volume of blood flowing through the unit section.
Reduces blood viscosity, causes disaggregation of platelets, increases the elasticity of red blood cells (due to the impact on the pathologically changed deformability of red blood cells). Improves microcirculation in the areas of impaired blood circulation.
When occlusive lesion of peripheral arteries ("intermittent" lameness), leads to a lengthening of the walking distance, the elimination of night cramps of the calf muscles and pain at rest.
Pharmacokinetics
The drug after administration is rapidly metabolized in the liver. In the process of metabolism, the formation of two major metabolites: 1- (5-hydroxyhexyl) -3,7-dimethylxanthine (metabolite I) and 1- (3-carboxypropyl) -3,7-dimethylxanthine (metabolite V), which have a similar activity to pentoxifylline . 1.5-2 hours after the infusion, the concentration of metabolites I and V in plasma is 5 and 8 times higher, respectively, than the concentration of the initial substance. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood is significantly reduced (up to 10% of the initial).
The half-life is from 30 minutes to 1.5 hours. Excreted predominantly by the kidneys (94%) in the form of metabolites (mainly metabolite V), the intestine (4%). up to 90% of the dose is eliminated in the first 4 hours. 2% of the drug is excreted unchanged. Pentoxifylline and its metabolites do not bind to plasma proteins.
It is excreted in breast milk.
In severe renal impairment, excretion of metabolites is delayed. With abnormal liver function, there is a prolongation of the half-life and an increase in bioavailability.
Indications
- impaired peripheral circulation due to atherosclerosis, diabetes mellitus (diabetic angiopathy);
- chronic disorders of cerebral circulation of ischemic genesis;
- atherosclerotic and dyscirculatory encephalopathy; angiopathies (paresthesias, Raynaud's disease);
- trophic disorders of tissues due to violations of arterial or venous microcirculation (trophic ulcers, postthrombotic syndrome, frostbite, gangrene);
- obliterating endarteritis;
- acute, subacute and chronic circulatory failure in the retina or in the choroid;
- hearing impairment of vascular genesis.
Composition
1 tablet contains:
Active substance: pentoxifylline (in terms of 100% substance) - 100 mg;
Excipients: stearic acid, potato starch, water-soluble methylcellulose, lactose (milk sugar), povidone (low molecular weight medical polyvinylpyrrolidone)
Shell composition: cellulose (acetylcellulose), titanium dioxide, castor oil, liquid paraffin (vaseline oil), azorubine (acid red 2 C), talc, beeswax
Pentoxifylline is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Pentoxifylline | Organica | Russia | pills |
| pills | |||
| Pentoxifylline-SOLOpharm | solution | ||
| Trental | Sanofi-aventis | France | ampoules |
| Trental | Sanofi-aventis | India | pills |
| Pentoxifylline | Zentiva KS | Czech | pills |
| Pentoxifylline | Pharmproject | Russia | pills |
| Pentoxifylline | Biochemist Saransk | Russia | ampoules |
| Vasonit | G.L.Farma GmbH | Austria | pills |
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Dosage and Administration
For oral use. after eating. pills are coated with a special coating that is soluble in the intestines, so they are swallowed whole, washed down with a small amount of water. Take 0.2 g (2 pills) 3 times a day. After reaching 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 the dosage regimen of Pentoxifylline is determined by the attending physician individually, depending on the clinical picture of the disease and the resulting therapeutic effect.
Adverse reactions
From the digestive system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.
From the senses: blurred vision, scotoma.
Since the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, lowering blood pressure.
From the side of blood-forming organs and hemostasis system:thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from the vessels of the skin, mucous membranes. stomach, intestines.
Allergic reactions: itching, skin flushing, urticaria, angioedema, anaphylactic shock.
Laboratory indicators: increased activity of liver transaminases (ALT, ACT, LDH) and alkaline phosphatase.
Contraindications
Carefully:the drug is prescribed to patients with atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and cardiac arrhythmias, heart failure, liver failure. Caution should also be exercised when prescribing pentoxifylline in patients with gastric ulcer and duodenal ulcer in patients who have recently undergone surgery (risk of bleeding).
Drug interactions
Pentoxifylline enhances the action of heparin, fibrinolytic drugs, theophylline, antihypertensives and hypoglycemic agents (both insulin and oral hypoglycemic agents).
Pentoxifylline can enhance the action of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefoperazone, cefotetan), valproic acid.
Cimetidine increases the concentration of pentoxifylline in the blood plasma (the risk of side effects).
Joint appointment with other xanthines can lead to excessive nervous excitement of patients.
Pregnancy and Lactation
Pentoxifylline is contraindicated during pregnancy and is not recommended for use during breastfeeding.
Overdosage
Symptoms: nausea, dizziness, cyanosis, tachycardia, marked reduction in blood pressure, redness of the skin, fever (chills), agitation, areflexia, tonic-clonic convulsions, vomiting “coffee grounds”, arrhythmia, loss of consciousness.
Treatment: symptomatic. Particular attention should be paid to maintaining blood pressure and respiratory function. Convulsions are relieved by the administration of diazepam. Urgent measures in case of severe anaphylactic reactions (shock):
- with the appearance of primary symptoms (sweating, nausea, cyanosis) immediately stop taking the drug;
- in addition to other necessary measures, they ensure a lower position of the head and upper torso and provide freedom for breathing;
- urgent medical measures: injected into / in epinephrine (adrenaline). If necessary, the introduction of epinephrine can be repeated.
- Brand name: Pentoxifylline
- Active ingredient: Pentoxifylline
- Dosage form: Pills
- Manufacturer: Organics
- Country of Origin: Russia
Studies and clinical trials of Pentoxifylline (Click to expand)
- Potentiation of cytotoxicity and radiosensitization of (E)-2-deoxy-2′-(fluoromethylene) cytidine by pentoxifylline In vitro
- Inhibitory effects of pentoxifylline on ultraviolet B light–induced cutaneous inflammation
- Efficacy of Ibuprofen and Pentoxifylline in the Treatment of Phosgene-induced Acute Lung Injury
- Clinical update: Pentoxifylline is no Antidote for Cachexia
- Pentoxifylline inhibits gene-specific repair of UV-induced DNA damage in hamster cells
- Pentoxifylline improves the oxygenation and radiation response of BA1112 rat rhabdomyosarcomas and EMT6 mouse mammary carcinomas
- Pentoxifylline: Clinical application in human immunodeficiency virus—associated optic neuropathy
- Synergistic immunomodulatory effects of interferon-β1b and the phosphodiesterase inhibitor pentoxifylline in patients with relapsing-remitting multiple sclerosis
- New NO-Donors with Antithrombotic and Vasodilating Activities, X: Antiplatelet and Antithrombotic Effects of 3-Methylsydnone-5-nitrosimine (RE 2047) in Combination with ASA, Pentoxifylline, and Ticlopidine
- Successful treatment of Raynaud's phenomenon with pentoxifylline
- Study of the solid phase extraction of pentoxifylline and its major metabolite as a basis of their rapid low concentration gas chromatographic determination in serum
- Bioanalysis of pentoxifylline and related metabolites in plasma samples through LC-MS/MS
- Use of liquid chromatography–tandem mass spectrometry for the analysis of pentoxifylline and lisofylline in plasma
- The relative efficacy of aminoguanidine and pentoxifylline in modulating endotoxin-induced cardiac stress
- Effects of pentoxifylline on the different steps during adhesion and transendothelial migration of flowing neutrophils
- Effects of erythropoietin and pentoxifylline on the oxidant and antioxidant systems in the experimental short bowel syndrome
- Stereoselective metabolism of pentoxifylline in vitro and in vivo in humans
- Interconversion and tissue distribution of pentoxifylline and lisofylline in mice
- Protective role of pentoxifylline and propentofylline against the increase in osmotic fragility of the human red cell induced by protoporphyrin photosensitization
- Phosphodiesterase inhibitor pentoxifylline, a selective suppressor of T helper type 1- but not type 2-associated lymphokine production, prevents induction of experimental autoimmune encephalomyelitis in Lewis rats
- Major healing of refractory mandible osteoradionecrosis after treatment combining pentoxifylline and tocopherol: A phase II trial
- Pentoxifylline prevents fibrosis in an animal model and inhibits platelet-derived growth factor–driven proliferation of fibroblasts
- Effects of pentoxifylline pretreatment on Kupffer cells in rat liver transplantation
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