TRENTAL (Concentrate for solution for infusion)
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, T33
When CSF: 01.14.01
Manufacturer: AVENTIS PHARMA Ltd. (India)
Pharmaceutical form, composition and packaging
Concentrate for solution for infusion almost transparent, colorless.
| 1 ml | 1 amp. | |
| pentoxifylline | 20 mg | 100 mg |
Excipients: sodium chloride, water d / and.
5 ml – colorless glass vials (5) – 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® It leads to improvement of symptoms of cerebral circulation.
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
Distribution and metabolism
Pentoxifylline has a large Vd – 168 l after 30-minute infusion at a dose 200 mg.
Pentoxifylline is extensively metabolized in the liver and red blood cells. Among the most prominent metabolite metabolite-1 (M-I; gidroksipentoksifillin) formed by splitting, a metabolite-4 (M-IV) and metabolite-5 (M-V; karʙoksipentoksifillin) – by oxidation of the base material. MI has the same pharmacological activity, like pentoxifylline.
Pentoxifylline and its metabolites do not bind to plasma proteins.
Deduction
After the on / in a dose of 100 mg T1/2 pentoxifylline was about 1.1 no. High ground clearance – about 4500-5100 ml / min. More than 90% of the dose is excreted by the kidneys pentoxifylline, 3-4% with feces.
Pharmacokinetics in special clinical situations
In patients with severely impaired hepatic function T1/2 pentoxifylline increases.
In severe impaired renal function excretion of metabolites is slowed.
Elderly patients may increase bioavailability and decrease the rate of excretion of the drug (may require dose reduction).
Testimony
- Peripheral circulatory disorders of atherosclerotic (incl. intermittent claudication, diabetic angiopathy);
- Trophic disorders (incl. leg sores, gangrene);
- Frostbite;
- Post-thrombotic syndrome;
- Cerebrovascular accident (the effects of cerebral arteriosclerosis: 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
The dosage and pattern of use are determined by the severity of circulatory disorders, as well as the individual tolerability and patient characteristics.
The drug is introduced into / in the form of infusions 2 times / day, morning and afternoon. Single dose (on 1 infusion) is 200 mg pentoxifylline (2 ampoules 5 ml) or 300 mg pentoxifylline (3 ampoules 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; Use only clear solutions. Dose 100 mg should be administered, but at least, during 60 m. Depending on comorbidities (heart failure) it may be necessary to reduce the injected volume. In such cases it is advisable to use a special infuzator for controlled infusion.
After a day of infusion may be assigned additional 2 tab. Trentala® 400. If 2 infusions separated by longer intervals, then 1 tab. Trentala® 400 of the appointment of two additional, It could be adopted before (around noon).
If, by virtue of clinical conditions, perform I / infusion is only possible 1 time / day, further after it can be assigned 3 tab. Trentala® 400 (2 tab. – noon and 1 tab. – in the evening).
Prolonged / in infusion Trental® during 24 h shows in more severe cases,, especially in patients with severe pain at rest, with gangrene or trophic ulcers (III-IV stages according to Fontaine).
Dose Trentala® in parenteral administration for 24 no, usually, should not exceed 1200 mg, wherein the individual dose may be calculated according to the formula: 600 ug / kg of body weight per hour. The daily dose of the drug, thus calculated, will be for a patient weighing 70 kg 1000 mg, and patient body weight 80 kg – 1150 mg.
In patients with renal insufficiency (CC less than 30 ml / min) necessary to reduce the dose of 30-50%, depending on the individual tolerability.
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; in some cases – intrahepatic cholestasis and elevated liver transaminases, Alkaline phosphatase.
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® in high doses or at high speed infusion.
Contraindications
- 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;
- Up to 18 years;
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug;
- Hypersensitivity to other methylxanthines.
FROM caution It should be used in patients with arterial hypertension (reduce the risk of blood pressure), chronic heart failure, 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 in 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). The dose should be reduced in patients with low and unstable blood pressure.
Smoking may reduce the therapeutic efficacy of the drug.
Compatible solution with pentoxifylline infusion solution should be checked in each case.
During the I / infusion the patient should be supine.
Use in Pediatrics
The safety and efficacy of pentoxifylline in children are not well understood.
Overdose
Symptoms: weakness, Sweating, nausea, cyanosis, dizziness, decrease in blood pressure, tachycardia, insensibility, drowsiness or agitation, arrhythmia, hyperthermia, areflexia. loss of consciousness, tonic-clonic seizures, symptoms of gastrointestinal bleeding (vomiting type “coffee grounds”).
Treatment: when the first signs of overdose immediately stop administering the drug. Provides a lower position of the head and upper torso. Symptomatic therapy. Particular attention should be paid to the maintenance of blood pressure and respiratory function. Seizures cropped diazepam.
Drug Interactions
Pentoxifylline is able to increase the effects of drugs, lowering blood pressure (ACE inhibitors, 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
List B. The drug should be stored out of reach of children, dark place at a temperature of 8 ° to 25 ° C. Shelf life – 4 year.
