Trental concentrate for solution for inf. 20mg / 5ml ampoules 5 ml Pieces

Description

Composition
Active substance:
1 ml of solution contains: pentoxifylline – 20.00 mg.
Excipients:
Sodium chloride – 7.00 mg Water for injection – up to 1.00 ml.
Description:
Almost clear, colorless solution.
Product form:
Concentrate for solution for infusion of 20 mg / ml. 5 ml of a clear, colorless glass vials (type I) with a fracture point. 5 in plastic vials contour cell uncoated packaging (pallet). 1 pallet together with instructions for use in a cardboard box.
Contraindications
Hypersensitivity to pentoxifylline, other methylxanthines or any excipient the formulation. Massive bleeding (risk of increased bleeding). Extensive bleeding in the retina of the eye (risk of increased bleeding). Bleeding in the brain. Acute myocardial infarction. Age up to 18 years. Pregnancy (insufficient data). breast-feeding period (insufficient data).
Carefully
Severe disorders of heart rhythm (arrhythmia risk of deterioration). Hypotension (risk of further blood pressure lowering. See section “Dosage and Administration”). High risk of lowering blood pressure (including with severe coronary heart disease or hemodynamically significant stenosis of cerebral vessels). Chronic heart failure. renal dysfunction (creatinine clearance less than 30 mL / min) (risk of accumulation and an increased risk of side effects. See section “Dosage and Administration”). Severe liver disorders (increased risk of accumulation and the risk of side effects. See section “Dosage and Administration”). Recently transferred surgery. The increased risk of bleeding (e.g., disorders in blood coagulation system (risk of a severe bleeding). See section “Interaction with other drugs”). The simultaneous use of anticoagulants (including indirect anticoagulants [antagonist of vitamin K]) (see. See “The interaction with other drugs”). The simultaneous use of the platelet aggregation inhibitor (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [cyclooxygenase-2 addition of selective inhibitors], acetylsalicylic acid, ticlopidine, dipyridamole) (see. See “The interaction with other drugs”) . The simultaneous use of hypoglycemic agents (insulin and hypoglycemic agents for oral administration). See section “interaction with other drugs.” The simultaneous use of ciprofloxacin (see. See “The interaction with other drugs”). Concomitant use with theophylline (see. See “The interaction with other drugs”).
Dosage
20 mg / ml
Indications
Peripheral arterial occlusive disease or diabetic atherosclerotic origin (e.g., “intermittent” claudication, diabetic angiopathy). Trophic disorders (e.g., leg sores, gangrene). Cerebrovascular accidents (the effects of cerebral arteriosclerosis, such as poor concentration, dizziness, memory impairment), ischemic and post stroke condition. Circulatory disturbances in the network and the choroid. Otosclerosis, degenerative changes in the background pathology of vessels of the inner ear and hearing loss.
Interaction with other drugs
With antihypertensives: pentoxifylline increases the risk of hypotension while the use of antihypertensive agents (e.g., angiotensin-converting enzyme (ACE)), or other drugs having potential antihypertensive effect (e.g., nitrates).
With drugs affecting the clotting of blood: pentoxifylline may exacerbate the effects of drugs influencing blood coagulation (direct and indirect anticoagulants, thrombolytics, antibiotics, such as cephalosporins). In a joint application of pentoxifylline and indirect anticoagulants (vitamin K antagonists) in the post-marketing studies have been cases enhance the anticoagulant action (risk of bleeding). Therefore, in the beginning of the reception of pentoxifylline or changing its dose recommended to control the degree of anticoagulant effect in patients treated with this combination of drugs, e.g., regular monitoring of INR (international normalized ratio).
With cimetidine: cimetidine increases the concentration of the active metabolite of pentoxifylline and I in the blood plasma (the risk of side effects).
With other xanthines: co-administration with other xanthines can lead to excessive nervous excitement.
With hypoglycaemic drugs (insulin and hypoglycemic agents for oral administration): the hypoglycemic effect of insulin or hypoglycemic agents for oral administration may be enhanced while the use of pentoxifylline (increased risk of hypoglycaemia). There must be strict control of the state of these patients, including regular blood glucose control.
With theophylline: in some patients, while the use of theophylline and pentoxifylline marked increase in the concentration of theophylline in blood. This further can increase or enhance the adverse effects associated with theophylline.
With ciprofloxacin: in some patients, while the use of pentoxifylline and ciprofloxacin pentoxifylline marked increase in plasma concentrations. This further can increase or enhance the adverse effects associated with the use of this combination.
C. Platelet aggregation inhibitors: the simultaneous use of pentoxifylline with platelet aggregation inhibitor (clopidogrel, eptifibatide, tirofiban, epoprostenol, iloprost, abciximab, anagrelide, NSAIDs [cyclooxygenase-2 addition of selective inhibitors], acetylsalicylic acid, ticlopidine, dipyridamole) may develop a potential additive effect which increases the risk of bleeding. Therefore, because of the risk of bleeding should be used with caution pentoxifylline together with the above-mentioned inhibitors of platelet aggregation (see. Section ”
Carefully “).
Overdose
Overdose symptoms: weakness, sweating, nausea, cyanosis, dizziness, decreased blood pressure, tachycardia, fainting, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic seizures, signs of gastrointestinal bleeding (vomiting-type coffee grounds ).
Treatment is symptomatic: special attention should be directed to maintain blood pressure and respiratory function. Seizures cropped diazepam. At the first signs of overdose immediately cease the drug administration. Provide a lower position of the head and upper torso.
pharmachologic effect
Pharmacological group:
Vasodilating agent.
Pharmacodynamics:
Preparation Trental® decreases blood viscosity and improves the flow properties of the blood (flowability) due to: improve impaired erythrocyte deformability; reducing platelet aggregation and erythrocytes; reducing the concentration of fibrinogen; reducing the activity of leukocytes, and reducing the adhesion of leukocytes to the vascular endothelium. As the active substance preparation contains Trental® xanthine derivative – pentoxifylline. Its mechanism of action is related to inhibition of phosphodiesterase and the accumulation of cyclic adenosine monophosphate (cAMP) in vascular smooth muscle cells of blood corpuscles and cells. Exerting slight myotropic vasodilator action, pentoxifylline somewhat reduces the total peripheral vascular resistance and slightly increasing coronary vessels. Pentoxifylline has a weak positive inotropic effect on the heart. Improves microcirculation in areas of impaired circulation. Treatment with Trental® leads to improvement of symptoms of cerebral blood flow. When occlusive diseases of the peripheral arteries Trental® use of the drug leads to a lengthening of the distance away, elimination of night cramps in the calves and disappearance of pain at rest.
Pharmacokinetics:
Pentoxifylline is extensively metabolized in the liver and erythrocytes. The concentration of the main active metabolite of 1- (5-hydroxyhexyl) -3,7-theobromine (metabolite I) in plasma twice the original concentration of pentoxifylline. Metabolite I is pentoxifylline in reversible biochemical redox equilibrium. Therefore, pentoxifylline and metabolite I are considered together as the active unit. Consequently, the availability of the active substance considerably more. The half-life after intravenous administration of pentoxifylline was 1.6 hours. Pentoxifylline has a large volume of distribution (168 l after 30 minute infusion of 200 mg) and high clearance of approximately 4500-5100 ml / min. Pentoxifylline and its metabolites do not bind to plasma proteins. Pentoxifylline is completely metabolized and more than 90% is excreted through kidneys in the form of water-soluble unconjugated metabolites.
Patients with impaired renal function: in patients with impaired renal excretion of metabolites is slowed down.
Patients with impaired hepatic function: in patients with impaired liver function the half-life of pentoxifylline is prolonged and the absolute bioavailability is increased.
Pregnancy and breast-feeding
Pregnancy: Trental® drug is not recommended during pregnancy (since insufficient data).
Breastfeeding: pentoxifylline passes into breast milk in small quantities. If necessary, the drug should stop breastfeeding (given the lack of experience of the application).
Conditions of supply of pharmacies
Prescription.
side effects
Below are adverse reactions that have been studied in clinical trials and post-marketing application of the drug (the frequency is unknown).
Disorders of the nervous system: headache, dizziness, aseptic meningitis, seizures.
Mental disorders: agitation, sleep disturbances, anxiety.
Violations of the heart: tachycardia, arrhythmia, lower blood pressure, angina pectoris.
Violations by the vessels, “tides” of blood to the skin, bleeding (including bleeding from vessels in the skin, mucous membranes, stomach, intestines).
Disorders of the digestive system: xerostomia (dry mouth), anorexia, intestinal atony, feeling of pressure and fullness in the stomach, nausea, vomiting, diarrhea, constipation, hypersalivation (excessive salivation).
Violations of the liver and biliary tract: intrahepatic cholestasis, increased activity of “liver” transaminases, increased alkaline phosphatase activity.
Blood disorders and lymphatic system: leukopenia / neutropenia, thrombocytopenia, pancytopenia, gipofibrinogenemia.
Violations by the organ of vision: blurred vision, scotoma.
Violations of the skin and subcutaneous tissue disorders: pruritus, rash, erythema (skin redness), rash, increased nail fragility, swelling.
Disorders of immune system: anaphylactic / anaphylactoid reactions, angioneurotic edema, anaphylactic shock, bronchoconstriction.
special instructions
Treatment should be under the control of blood pressure. In patients with diabetes, taking hypoglycemic agents, the appointment of large doses can cause pronounced hypoglycemia (may require dose adjustment of hypoglycemic agents and conduct of glycemic control). In appointing the drug Trental® simultaneously with anticoagulants should be monitored indicators of blood clotting. In patients who have recently had surgery, requires regular monitoring of hemoglobin and hematocrit. Patients with low and unstable blood pressure Trental® necessary to reduce the dose of the drug. Elderly patients may require a dose reduction of pentoxifylline (increased bioavailability and reduced clearance rate). The safety and efficacy of pentoxifylline in children are not well understood. Smoking may reduce the therapeutic efficacy of the drug. Compatibility with pentoxifylline solution infusion solution should be checked in each case. During the intravenous infusion the patient should be in a prone position.
Effects on ability to drive and engage in potentially hazardous activities
Given the potential side effects (eg, dizziness) should be careful when driving and occupation of potentially hazardous activities.
Storage conditions
Store in a dark place at a temperature of 8 C to 25 C.
Keep out of the reach of children!.
Dosing and Administration
The dose and method of administration are determined by the weight of circulatory disorders, as well as based on individual tolerance Trental® preparation. The dosage is set by the doctor according to the individual patient. The usual dose is 100 mg to 600 mg of drug Trental®, diluted in 250 ml or 500 ml 0.9% sodium chloride solution or Ringer’s solution, 1 or 2 times per day. Compatibility with other infusion solutions should be tested separately; use only transparent solutions Trental® 100 mg of the drug to be administered, at least for 60 minutes.
In addition to the infusion therapy can be administered Trental® preparation for oral administration. The total daily dose of the drug Trental® (intravenous infusion + ingestion) should not exceed 1200 mg. Depending on concomitant diseases (e.g., chronic heart failure) may be necessary to reduce the injection volume. In such cases it is recommended to use a special infuzator for controlled infusion. In more severe cases, particularly in patients with severe pain at rest, gangrene or trophic ulcers (III-IV stage of Fontaine classification) shows a continuous intravenous infusion of the drug Trental® at a dose of 1200 mg in 24 hours. This dose can be divided into two intravenous administration of 600 mg, each of which must continue for at least 6 hours. Thus individual dose may be calculated according to the formula: pentoxifylline 0.6 mg per kg body weight per hour. The daily dose, calculated in this way will be 1000 mg of pentoxifylline for a patient of 70 kg body weight and 1150 mg of pentoxifylline for a patient weighing 80 kg. When maintenance therapy Trental® go to the reception of the drug inside. In patients with renal failure is necessary to reduce the dosage of 30-50% (less than 30 ml / min creatinine clearance), depending on individual tolerability Trental® patient. Reducing the dose, taking into account the individual tolerance, it is necessary in patients with severely impaired hepatic function. Treatment can be initiated with small doses in patients with low blood pressure, as well as in patients at risk due to a possible decrease in blood pressure (patients with severe ischemic heart disease or hemodynamically significant stenosis of the cerebral vessels). In these cases, the dose can be increased only gradually.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist