TRENTAL (Pills)
Active material: Pentoxifylline
When ATH: C04AD03
CCF: Preparation, improving microcirculation. Angioprotektor
ICD-10 codes (testimony): F07, G45, H31.1, H34, H35.0, H93.0, I63, I67.2, I69, I73.0, I73.1, I73.9, I79.2, I83.2
When CSF: 01.14.01
Manufacturer: AVENTIS PHARMA Ltd. (India)
Pharmaceutical form, composition and packaging
Pills, enteric-coated film-coated white, round, lenticular.
| 1 tab. | |
| pentoxifylline | 100 mg |
Excipients: lactose, starch, talc, colloidal silicon dioxide, magnesium stearate.
The composition of the shell: methacrylic acid copolymer, Sodium hydroxide, macrogol (polyethylene glycol) 8000, talc, Titanium dioxide (E171).
10 PC. – blisters (6) – packs cardboard.
Pharmacological action
Preparation, improving microcirculation, angioprotektor, xanthine derivative. Trental® improves blood rheology (flowability) due to the impact of the pathology of the deformability of red blood cells, inhibiting platelet aggregation and reducing an increased blood viscosity. It improves the microcirculation in the areas of impaired circulation.
The mechanism of action of pentoxifylline associated with inhibition of phosphodiesterase and cAMP accumulation in vascular smooth muscle cells and blood cells.
By providing a weak vasodilatory effect myotropic, pentoxifylline decreases somewhat round and slightly dilates coronary vessels.
Treatment Trentalom® leads to improvement of symptoms of cerebrovascular accidents.
The success of the treatment of peripheral arterial occlusive disease (eg, intermittent claudication) It manifested in the lengthening distance walk, elimination of night cramps in the calf muscles and the disappearance of pain at rest.
Pharmacokinetics
Absorption
After oral pentoxifylline is almost completely absorbed from the gastrointestinal tract. Absolute bioavailability averages 19±13%.
Metabolism
Pentoxifylline is completely metabolized in the body. The main pharmacologically active metabolite 1-(5-gidroksigeksil)-3,7-dimetilksantin (metabolite I) determined in plasma at a concentration, exceeding the 2 fold concentration of the unchanged substance (pentoxifylline).
Deduction
Once inside the T1/2 pentoxifylline is 1.6 no.
More 90% excreted by the kidneys in the form of water-soluble non-conjugated metabolites.
Pharmacokinetics in special clinical situations
Excretion of metabolites is slowed down in patients with severely impaired renal function.
In patients with impaired liver function observed elongation T1/2 pentoxifylline and increasing its absolute bioavailability.
Testimony
- Peripheral circulatory disorders of atherosclerotic (eg, intermittent claudication), diabetic angiopathy, trophic disorders (eg, leg ulcers, gangrene);
- Cerebrovascular accident (the effects of cerebral arteriosclerosis, as, eg, impaired concentration, dizziness, memory impairment), ischemic and post stroke status;
- Circulatory disorders in the retina and choroid;
- Otosclerosis, degenerative changes in the background of vascular pathology of the inner ear and hearing loss.
Dosage regimen
Dose set individually, according to the characteristics of the patient.
The drug is prescribed inside of 100 mg (1 tab.) 3 times / day, followed by a gradual increase in dose to 200 mg 2-3 times / day. The maximum single dose – 400 mg. The maximum daily dose – 1200 mg. Tablets should be swallowed whole during or immediately after a meal., drinking plenty of water.
In patients with impaired renal function (CC less than 30 ml / min) dose should be reduced to 1-2 tab. / day.
In Patients with severe hepatic impairment to reduce the dose based on the individual tolerability.
In patients with low blood pressure, and in individuals, at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenosis of cerebral vessels) Treatment can be initiated with small doses, in these cases, the dosage should be increased gradually.
Side effect
CNS: headache, dizziness, anxiety, sleep disorders, convulsions; rarely – aseptic meningitis.
Dermatological reactions: facial flushing, rush of blood to the face and upper chest, swelling, increased brittleness of nails.
From the digestive system: xerostomia, anorexia, bowel atony, a feeling of pressure and fullness in the stomach, nausea, vomiting, diarrhea; in some cases – intrahepatic cholestasis, increase in liver transaminases.
Cardio-vascular system: tachycardia, arrhythmia, kardialgija, progression of angina, decrease in blood pressure.
From the hematopoietic system: leukopenia, thrombocytopenia, pancytopenia, bleeding from vessels in the skin, mucosas, stomach, bowel, fibrinopenia.
On the part of the organ of vision: blurred vision, scotoma.
Allergic reactions: itch, dermahemia, hives, angioedema, anaphylactic shock.
Side effects are possible when using Trental® high dose.
Contraindications
- Massive bleeding;
- Extensive retinal hemorrhage;
- Bleeding in the brain;
- Acute myocardial infarction;
- Up to 18 years;
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug;
- Hypersensitivity to other methylxanthines.
FROM caution should be used in patients with severe cardiac arrhythmias (risk of worsening arrhythmias), hypotension (the risk of further reduction in blood pressure), chronic heart failure, with peptic ulcer of the stomach and duodenum, impaired renal function in QA < 30 ml / min (the risk of accumulation and an increased risk of side effects), with severely impaired hepatic function (the risk of accumulation and an increased risk of side effects), increased tendency to bleeding, incl. as a result of the use of anticoagulants or violations on the part of the blood coagulation system (the risk of more severe bleeding), after recently undergone surgeries.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breast-feeding).
Cautions
Treatment should be under the control of blood pressure.
In patients with diabetes, taking hypoglycemic agents, use of the drug at high doses can cause pronounced hypoglycemia (Dosage adjustment).
When assigning simultaneously with anticoagulants should be carefully monitored for indicators of blood coagulation system.
Patients, recently underwent surgery, requires systematic monitoring of the level of hemoglobin and hematocrit.
Older people may require a dose reduction (increased bioavailability and reduced clearance rate).
Smoking may reduce the therapeutic efficacy of the drug.
Use in Pediatrics
The safety and efficacy of pentoxifylline in children are not well understood.
Overdose
Symptoms: dizziness, urge to vomit, drop in blood pressure, tachycardia, arrhythmia, redness of the skin, loss of consciousness, chills, areflexia, tonic-clonic seizures.
Treatment: when the first symptoms of an overdose appear (Sweating, nausea, cyanosis) stop taking the drug immediately, it is necessary to ensure a lower position of the head and upper body, control airway patency. Symptomatic therapy, special attention should be paid to maintaining blood pressure and respiratory function. Diazepam is administered to relieve seizures..
In case of overdose symptoms, the patient should immediately consult a doctor.
Drug Interactions
Pentoxifylline is able to increase the effects of drugs, lowering blood pressure (ACE, nitrates).
Pentoxifylline may increase the effects of drugs, influencing blood clotting (indirect and direct anticoagulants, thrombolytics), antibiotics (incl. cephalosporins).
Cimetidine increases the concentration of pentoxifylline in plasma (the risk of side effects).
Co-administration with other xanthines may cause excessive nervous excitement.
Perhaps increased hypoglycemic action of insulin or oral hypoglycemic agents while taking pentoxifylline (an increased risk of hypoglycaemia). If necessary, combination therapy requires strict monitoring of the patients.
In some patients, the simultaneous reception of theophylline and pentoxifylline may lead to increased concentrations of theophylline in plasma. This may lead to increased side effects or enhance, associated with theophylline.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, dry place at temperatures no higher than 25 ° C. Shelf life - 4 year.
