14 Mar 2017
Synonyms: Agapurin retard, Agapurin SR, Agapurin, Agapurun Retard, Agapurun, An Ruo Ning, Angiopent, Ao Le Ni, Ao Nuo Hong, Aotong, Apo-Pentox SR, Apo-Pentox, Apo-Pentoxifylline, Apo-Pentoxifylline SR, Aspen Pentoxifylline, Behrifil, Bo Shu Te, Cental, Cerator, Ceretal, Chang Long Lei, Chinotal, Circulaid LP, Claudicat, Damaton, DanKe, Dartelin, De Bao Xing, De Luo Wei, Dian Ke Shu, Dospan Pento, Duplat, Durapental, Dyna-Pentoxifylline, Elastab, Elorgan, Endopentoksas, Eshieton, Fei Ke Wei Kang, Fixoten, Flexital, Forflow, Fu Shu, Fucon, Fylin, Gan Feng, Hemalin, Hemopene, Hemovas, Hexopal, Ipentol, Ka Kai, Kinetal, Lentrin, Maoping, Nelorpin, Ni Fu Ping, Oxiflux, Oxifyl, Oxopurin, Pan Duo Xi Lai, Pan Ke Fu Lin, Papiror, Penphylline, Pental, Pentilin Retard, Pentilin, Pentiline, Pentoflux, Pentofyllin, PentoHexal, PentoHexal retard, Pentohexal retard, Pentoksifilin, Pentol, Pentolab, Pentomer, Pentomer retard, Pentop, Pento-Puren, Pentosin, Pentox, Pentoxal, Pentox-CT, Pentoxi Genericon retard, Pentoxi Retard, Pentoxicux, Pentoxifilin, Pentoxifilina Alter, Pentoxifilina Andromaco, Pentoxifilina Belmac, Pentoxifilina Davur, Pentoxifilina Generis, Pentoxifilina Genfar, Pentoxifilina L.CH., Pentoxifilina Mintlab, Pentoxifilina MK, Pentoxifilina Pharma Genexx, Pentoxifilina SR Zentiva, Pentoxifilina, Pentoxifyllin AbZ, Pentoxifyllin acis, Pentoxifyllin Actavis, Pentoxifyllin AL, Pentoxifyllin Basics, Pentoxifyllin Sandoz, Pentoxifyllin Stada, Pentoxifyllin-B, Pentoxifylline Biogaran, Pentoxifylline EG, Pentoxifylline Mylan, Pentoxifylline Qualimed, Pentoxifylline Ratiopharm, Pentoxifylline Sandoz, Pentoxifylline Valeant, Pentoxifylline, Pentoxifylline–1A, Pentoxifylline-Rivo, Pentoxifylline-Teva, Pentoxifyllin-ratiopharm, Pentoxifyllin-Tchaikapharma, Pentoxifyllinum Biotika, Pentoxifyllinum Rup Borisov, Pentoxil, Pentoxilline, Pentoxi-Mepha, Pentoxin, Pentoxipharm, Pentoxiphat LP, Pentox-SR, Pentoxy Heumann, Pentoxyl-EP, Perental, Perilax, Pexal, Platof, Polfilin prolongatum, Polfilin Retard, Polfilin, Previscan, Qi Ming, Qiquan, ratio-Pentoxifylline, Razyflin, Recital, Rentylin, Reotal, Retimax, Run Xin Shu, Sephylline, Shery, Shu An Ling, Shu Fu Luo, Shuang Ke, Sidmak Pentoxifylline, Sin Tong, Sipental, Sufisal, Suintol, Tai Tong, Tarontal, Throne, Tian Cun, Tian Mai, Tioxad, Tofilline, Torental, Torral, Toxipen, Trenace, Trenat, Trenfylline, Trenlin, Trental Bb Farma, Trental CR, Trental Programmi Sanitari, Trental Retard, Trental, Trentilin Retard, Trentilin, Trentolin, Trentox, Trenxy, Trepal, Tri-Plen (Pentoxifylline and Felodipine), Vantoxyl, Vasonit, Vasonit retard, Vasoplan, Vaspentox, Wei You, Xiang Di, Xin Ke Duo Na, Xinfu, YiShu.
Active substance: Pentoxifylline.
ATC - C04AD03 (Pentoxifylline).
Pharmacological group – Antiplatelet; Adenosynergic tools; Angioprotectors and cerebrovascular correctors.
Nosological classification (ICD–10)
H34 Retinal vascular occlusion;
H80 Otosclerosis;
H81.4 Vertigo of central origin;
H83 Other disorders of the inner ear;
H91 Other hearing loss;
I63 Cerebral infarction;
I67.2 Cerebral atherosclerosis;
I69 Effects of cerebrovascular diseases;
I70 Atherosclerosis;
I73.9 peripheral vascular disease, unspecified;
I79.2 Peripheral angiopathy in diseases classified elsewhere;
I87.0 Postflebitic syndrome;
L98.4.2 * skin trophic ulcer;
R02 Gangrene, not elsewhere classified;
R41.8.0 * Disorders Intellectual mnestic;
T35 Frostbite involving multiple body regions and unspecified frostbite.
Trental (Pentoxifylline) Composition, structure and packing
Tablets, film-coated, enterosoluble;
Concentrate for solution for infusion;
Sustained-release tablets, film-coated.
Trental (Pentoxifylline) Pharmacological action
Pharmacological action - normalizing blood rheology, improves microcirculation, vasodilator.
Pharmacodynamics
Trental improves blood rheology (flow) due to exposure to diseased erythrocyte deformability, inhibiting platelet aggregation and reducing elevated blood viscosity. Trental improves microcirculation in areas of poor circulation.
As the active principle Trental contains a xanthine derivative - pentoxifylline. Its mechanism of action is related to the inhibition of phosphodiesterase and cAMP accumulation in cells of the vascular smooth muscle and blood elements.
Providing weak miotropic vasodilator action, pentoxifylline decreases somewhat round and slightly dilates coronary vessels.
Trental treatment leads to an improvement of symptoms in violation of cerebral circulation.
The success of treatment for peripheral arterial occlusive disease (eg intermittent claudication) is manifested by the lengthening distance away, eliminating night cramps in the calf muscles and the disappearance of pain at rest.
Pharmacokinetics
The tablets 100, 400 mg
Following oral administration of pentoxifylline is rapidly and almost completely absorbed.
After almost complete absorption of pentoxifylline is metabolized. The absolute bioavailability of the original substance is (19 ± 13)%. The primary active metabolite of 1 - (5-hydroxyhexyl) –3,7-dimethylxanthine (metabolite–1) has a plasma concentration of 2 times greater than the initial concentration of pentoxifylline.
T 1/2 after oral administration of pentoxifylline was 1.6 hrs
Pentoxifylline completely metabolized, more than 90% is excreted through the kidneys in the form of water-soluble non-conjugated metabolites. Delayed excretion of metabolites in patients with impaired renal function.
In patients with impaired liver function of T 1/2 pentoxifylline elongates and absolute bioavailability increases.
Solution for infusion
Pentoxifylline is extensively metabolized in the liver and red blood cells. Among the most prominent metabolites - metabolite 1 (M–1; gidroxypentoxifylline) is formed by splitting a metabolite 4 (M-IV) and metabolite 5 (MV; carboxypentoxifylline) - by oxidation of the base material. M-l has the same pharmacological activity as pentoxifylline. More than 90% of the dose is excreted via the kidneys pentoxifylline and 4.3% - in the feces.
T 1/2 of pentoxifylline after/in the 100 mg was approximately 1.1 hours in patients with severely impaired hepatic function of T 1/2 pentoxifylline increases. Pentoxifylline has a large distribution volume (168 liters after 30 min of infusion of 200 mg) and a high clearance of approximately 4500–5100 ml/min. Pentoxifylline and its metabolites do not bind to plasma proteins. In severe kidney function is slowed metabolites.
Trental (Pentoxifylline) Dosage
Dosage set by the doctor according to the individual characteristics of the patient.
Tablets:
Inside, swallowing whole, during or immediately after meals, drinking plenty of water.
Usual dose - 1 table. Trental 100 mg 3 times a day followed by slow dose escalation to 200 mg 2–3 times a day. The maximum single dose - 400 mg.
Usual dose - 1 table. Trental 400 mg 2–3 times a day.
The maximum daily dose - 1200 mg. In patients with impaired renal function (Cl creatinine <30 ml/min), the dosage may be reduced to 1–2 tablets. night.
Solution for infusion:
Dosage set by the doctor according to the individual characteristics of the patient.
IV, drip, dosage and method of appointment determines the severity of circulatory disorders, as well as based on individual tolerability.
The usual dose is two IV infusion a day (morning and afternoon), each of which contains 200 mg of pentoxifylline (2 Amp. 5 mL) or 300 mg of pentoxifylline (3 Amp. 5 ml) in 250 ml or 500 ml 0 9% sodium chloride solution or Ringer’s solution. Compatibility with other infusion solutions should be tested separately, you can use only clear solutions.
Pentoxifylline (100 mg) must be administered at least 60 minutes. Depending concomitant diseases (cardiac insufficiency) it may be necessary to reduce the injection volume. In such cases it is recommended to use a special infuzator for controlled infusion.
After a day of infusion may be assigned additional 2 tablets. Trental 400 mg. If 2 infusions separated by a longer interval, the Table 1. Trental 400 mg of two additional appointments may be taken earlier (around noon).
If, due to medical conditions, performance of IV infusion maybe only 1 time a day later after it can be assigned to Table 3. Trental 400 mg (noon - 2 table. And evening - Table 1). Long IV infusion of Trental - for 24 hours is shown in more severe cases, especially in patients with severe pain at rest, with gangrene or trophic ulcers (III-IV stage at Fontaine).
Dose Trental, parenterally administered within 24 hours, typically should not exceed 1200 mg of pentoxifylline, wherein the individual dose may be calculated according to the formula: pentoxifylline 0.6 mg per kg per hour. Daily dose, thus calculated, will be 1000 mg pentoxifylline - a patient with a mass of 70 kg and 1150 mg pentoxifylline - for a patient weighing 80 kg. In patients with renal insufficiency (Cl creatinine <30 ml/min) is necessary to reduce the dose by 30–50%, depending on individual patient tolerability.
For all dosage forms dosage set by the doctor according to the individual characteristics of the patient. Reducing the dose, taking into account the individual tolerability necessary in patients with severe liver dysfunction. Treatment can be initiated in small doses in patients with low blood pressure, as well as in individuals at risk due to a possible reduction in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenosis of cerebral vessels). In these cases, the dose can be increased only gradually.
Trental (Pentoxifylline) Overdose
The tablets:
Symptoms: dizziness, retching, drop in blood pressure, tachycardia, arrhythmia, reddening of the skin, loss of consciousness, vomiting, areflexia, tonic-clonic seizures.
Solution for infusion
Symptoms: weakness, sweating, nausea, cyanosis, dizziness, decreased blood pressure, tachycardia, syncope, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic seizures, signs of gastrointestinal bleeding (vomiting type of coffee grounds).
Treatment: symptomatic, particular attention should be directed at maintaining blood pressure and respiratory function. Seizures remove diazepam.
At the first signs of overdose (excessive sweating, nausea, cyanosis), immediately stop taking the drug. Provide lower position of the head and upper torso. Watching free airway.
Trental (Pentoxifylline) Drug Interactions
For all dosage forms
Pentoxifylline is able to enhance the action means that reduce blood pressure (ACE inhibitors, nitrates).
Pentoxifylline may increase the effects of drugs affecting blood clotting (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins).
Cimetidine increases the concentration of pentoxifylline in plasma (the risk of side effects).
Co-administration with other xanthines may lead to excessive nervous excitement.
Glucose-lowering effect of insulin or oral antidiabetic agents may be enhanced when taking pentoxifylline (increased risk of hypoglycaemia). Strict control of these patients.
In some patients, concomitant use of pentoxifylline and theophylline may lead to increased levels of theophylline. This may lead to an increase or enhancement of side effects associated with theophylline. Trental (Pentoxifylline) at Pregnancy and lactation
Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.
Trental (Pentoxifylline) Side effects
For all dosage forms:
When Trental used in large doses or infusions at high speeds can sometimes cause the following side effects:
The nervous system: headache, dizziness, anxiety, sleep disorders, convulsions.
For the skin and subcutaneous fat: facial flushing, flushing and upper chest, swelling, nail fragility.
From the digestive system: dry mouth, anorexia, intestinal.
Cardio-vascular system: tachycardia, arrhythmia, false angina, worsening angina, blood pressure reduction.
On the part of the hemostatic system and of hematopoiesis: leukopenia, thrombocytopenia pancytopenia, bleeding from vessels in the skin, mucous membranes, stomach, intestines, gipofibrinogenemia.
From the senses: blurred vision, scotoma.
Allergic reactions: itching, redness of the skin, urticaria, angioedema, anaphylactic shock.
Very rare cases of aseptic meningitis, intrahepatic cholestasis and increased activity of “liver” transaminases, alkaline phosphatase.
Additional for tablets:
From the digestive system: the feeling of pressure and fullness in the stomach, nausea, vomiting, diarrhea.
Trental (Pentoxifylline) Indications
Peripheral circulatory disorders genesis of atherosclerosis (such as “intermittent” claudication, diabetic angiopathy), trophic disorders (eg shin trophic ulcer, gangrene), frostbite, post-thrombotic syndrome, etc. (in the application solution for infusion);
cerebrovascular accidents (cerebral atherosclerosis effects, such as impaired concentration, dizziness, memory impairment), ischemic and post stroke state;
circulatory disorders of the retina and choroid;
otosclerosis, degenerative changes in the background of vascular pathology of the inner ear and hearing loss.
Trental (Pentoxifylline) Contraindications
Tablets of 100 mg and 400 mg
Hypersensitivity to pentoxifylline, other methylxanthines or to any component of the formulation;
massive bleeding, extensive retinal hemorrhage, bleeding in the brain;
acute myocardial infarction;
pregnancy;
during breastfeeding;
children up to age 18 years.
Precautions:
serious cardiac arrhythmias (arrhythmia risk of deterioration);
hypotension (risk of further reduction of blood pressure, see “Dosage and Administration”);
chronic heart failure;
gastric ulcer and duodenal ulcer;
impaired kidney function (Cl creatinine below 30 ml/min) (risk of accumulation and increased risk of side effects, see “Dosage and Administration”);
severe liver problems (risk of accumulation and increased risk of side effects, see “Dosage and Administration”);
recently transferred after surgical interventions;
increased tendency to bleeding, such as the use of anticoagulants or irregularities in the blood coagulation system (risk of more severe bleeding).
Solution for infusion
Hypersensitivity to pentoxifylline, other methylxanthines or to any component of the formulation;
massive bleeding, extensive retinal hemorrhage, bleeding in the brain;
acute myocardial infarction;
severe arrhythmias;
severe atherosclerotic lesions of the coronary or cerebral arteries;
uncontrolled hypotension;
pregnancy;
during breastfeeding;
children up to age 18 years.
Precautions:
hypotension (blood pressure lowering risk);
chronic heart failure;
impaired kidney function (Cl creatinine below 30 ml/min) (the risk of cumulative and increased risk of side effects);
severe liver problems (risk of cumulative and increased risk of side effects);
increased tendency to bleeding, including the use of anticoagulants or violations in the blood coagulation system (risk of more severe bleeding);
recently transferred after surgical interventions.
Trental (Pentoxifylline) Cautions
Treatment should be under the control of blood pressure.
Diabetic patients taking hypoglycemic agents, the purpose of large doses may cause pronounced hypoglycemia (requires dose adjustment).
In appointing simultaneously with anticoagulants should be carefully monitored for blood coagulation system.
Patients who have recently had surgery, requires systematic monitoring of hemoglobin and hematocrit.
The administered dose should be reduced in patients with low and unstable blood pressure.
Older people may require a dose reduction (increase bioavailability and decrease the rate of excretion).
Safety and efficacy of pentoxifylline in children have been insufficiently studied.
Smoking may reduce the therapeutic efficacy of the drug.
Compatibility of the solution with pentoxifylline infusion solution should be checked in each case.
In conducting in/infusion, the patient should be in the supine position.
Trental (Pentoxifylline) Reviews
Jennifer 28 years,"Trental" to improve cerebral circulation - good drug tested
Good Trental pills helped me get rid of a headache, which arose because of poor microcirculation.
I never thought that such a bad microcirculation is suffering from a headache. The pressure was rising high, his head just popped.
Neurologist immediately diagnosed VVD (vegetative dystonia) and ordered a bunch of pills.
My mother advised me to take Trental - she, too, problems with cerebral circulation, so she knew she says!
And on the fifth day I felt much better! Headache subsided, the pressure is no longer rising.
The symptoms gradually went away, I have not even had time to buy that bunch of pills, which I appointed a neurologist.
So, I am quite successfully treated with Trental.
This drug, of course, does not reduce the pressure immediately and relieves headaches, for this is Andipal, but Trental has a therapeutic effect, so there should be some time.
If someone tonnes problems with circulation of the brain, Trental advice, but be sure to read the contraindications!
Daisy, 38 years, "Trental" to improve cerebral circulation - really improves peripheral arterial supply
Advantages:
a relatively small price, small tablet very successful form for ingestion
Trental I wrote a surgeon with Raynaud's disease. It is necessary to drink twice a year in spring and autumn. After taking pills abdomen is inflated, like a tight, not soft. The usual dose three times a day with a gradual increase does not suit me. Day discomfort, night can not sleep. I drink a few years as follows: Table 1. Morning Table 1. evening no later than 18 hours., nothing hurts, calm sleep. I have a high weight and low blood pressure. Tried counterparts - do not help, they are more easily tolerated. At reception Trental blood comes to peripheral arteries.
My illness sleeps 38 years, if you do not feel the fingers, shake hands and begin to drink Trental. If Raynaud's disease exacerbation, helped me a lot Solcoseryl injections.