Description
Latin name
TRENTAL
Release form
Concentrate for solution for infusion.
Packaging
5 ampoules per pack.
Pharmacological action
Trental – normalizes the rheological properties of blood, improves microcirculation, vasodilator.
Pharmacodynamics
Trental improves the rheological properties of blood (fluidity) by acting on the pathologically altered deformability of red blood cells, inhibiting platelet aggregation and reducing increased blood viscosity. Trental improves microcirculation in areas of impaired circulation.
As an active ingredient, Trental contains a xanthine derivative – pentoxifylline. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the smooth muscle cells of blood vessels and blood cells.
Having a weak myotropic vasodilator effect, pentoxifylline somewhat reduces OPSS and slightly dilates the coronary vessels.
Treatment with Trental improves symptoms in cases of cerebrovascular accident.
The success of treatment for occlusive lesions of the peripheral arteries (for example, intermittent claudication) is manifested in lengthening the walking distance, eliminating night cramps in the calf muscles and the disappearance of pain at rest.
Pharmacokinetics
Tablets 100, 400 mg
After oral administration, pentoxifylline is rapidly and almost completely absorbed.
After almost complete absorption, pentoxifylline is metabolized. The absolute bioavailability of the starting substance is (19 ± 13)%. The main active metabolite 1- (5-hydroxyhexyl) -3,7-dimethylxanthine (metabolite-1) has a plasma concentration of 2 times the initial concentration of pentoxifylline.
T1 / 2 of pentoxifylline after oral administration is 1.6 hours.
Pentoxifylline is completely metabolized, more than 90% is excreted through the kidneys in the form of unconjugated water-soluble metabolites. Excretion of metabolites is delayed in patients with impaired renal function.
In patients with impaired liver function, T1 / 2 of pentoxifylline lengthens and absolute bioavailability increases.
Solution for infusion
Pentoxifylline is extensively metabolized in red blood cells and the liver. Among the most famous metabolites, metabolite-1 (M-1 hydroxypentoxifylline) is formed due to cleavage, and metabolite-4 (M-IV) and metabolite-5 (MV carboxypentoxyphylline) due to the oxidation of the main substance. M-l has the same pharmacological activity as pentoxifylline. More than 90% of the dose of pentoxifylline taken is excreted through the kidneys and 3-4% with feces.
T1 / 2 of pentoxifylline after iv administration of 100 mg was approximately 1.1 hours. In patients with severely impaired hepatic function, T1 / 2 of pentoxifylline is increased. Pentoxifylline has a large volume of distribution (168 L after 30 min infusion of 200 mg) and a high clearance of approximately 4,500-5100 ml / min. Pentoxifylline and its metabolites do not bind to plasma proteins. In severe renal impairment, excretion of metabolites is slowed down.
Indications
Peripheral circulatory disorders of atherosclerotic origin (e.g. intermittent claudication)
diabetic angiopathy
trophic disorders (e.g. calf ulcers, gangrene)
cerebrovascular accidents, such as cerebrospinal disorders, such as consequences memory impairment)
ischemic and post-stroke conditions
circulatory disorders in the retina and choroid
otosclerosis
degenerative changes due to vascular pathology of the inner ear and hearing loss.
Contraindications
Hypersensitivity to the components of the
preparation massive bleeding
extensive retinal hemorrhage
cerebral hemorrhage
acute myocardial infarction srdlkrp arrhythmia arrhythmia arrhythmias arrhythmia arrhythmia arrhythmia arrhythmia arrhythmia arrhythmia arrhythmia of the brain lactation (breastfeeding)
hypersensitivity to other methylxanthines.
Caution should be used in patients with: arterial hypotension (risk of lowering blood pressure), chronic heart failure, impaired renal function – QC less than 30 ml / min (risk of cumulation and increased risk of side effects), with severe impaired liver function (risk of cumulation and an increased risk of side effects), an increased tendency to bleeding, including as a result of the use of anticoagulants or in disorders of the blood coagulation system (risk of more severe bleeding), after recent surgery.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and during lactation (breastfeeding).
Composition
Concentrate for the preparation of an infusion solution 1 ml
tocilizumab 20 mg
excipients: polysorbate 80 sucrose sodium hydrogen phosphate dodecahphosphate difhydrate phosphate 9 for hydrate phosphate 9 solution forhydrate phosphate 9 hydrofluoride for solution 9
Active ingredient: pentoxifylline 20 mg in 1 ml (100 mg in 1 ampoule).
Excipients: sodium chloride, water d / and.
Dosage and administration
Dose and regimen are determined by the severity of circulatory disorders, and also taking into account the individual tolerance of the drug and the characteristics of the patient.
The drug is administered iv in the form of infusion 2 times a day, in the morning and in the afternoon. A single dose (per 1 infusion) is 200 mg of pentoxifylline (2 ampoules of 5 ml each) or 300 mg of pentoxifylline (3 ampoules of 5 ml each) in 250 ml or 500 ml of 0.9% sodium chloride solution or Ringer’s solution.
Compatibility with other infusion solutions should be tested separately. Only clear solutions can be used. A dose of 100 mg should be administered, but at least within 60 minutes. Depending on concomitant diseases (heart failure), it may be necessary to reduce the volume administered. In such cases, it is recommended to use a special infuser for controlled infusion.
After a day’s infusion, an additional 2 tablets of Trental 400 can be prescribed. If 2 infusions are separated by a longer interval, then 1 tablet of Trental 400 of the additional two prescribed can be taken earlier (at about noon).
If, due to clinical conditions, an intravenous infusion is possible only 1 time per day, additionally 3 tablets of Trental 400 may be prescribed after it (2 tablets at noon and 1 tablet in the evening).
Prolonged IV infusion of Trental for 24 hours is indicated in more severe cases, especially in patients with severe pain at rest, with gangrene or trophic ulcers (Fontaine stage III-IV).
Trental dose for parenteral administration within 24 hours, as a rule, should not exceed 1200 mg, while the individual dose can be calculated by the formula: 600 mcg / kg body weight per hour. The daily dose of the drug, calculated in this way, will be for a patient with a body weight of 70 kg 1000 mg, and for a patient with a body weight of 80 kg – 1150 mg.
In patients with renal failure (CC less than 30 ml / min), it is necessary to reduce the dose by 30-50%, which depends on the individual tolerance of the drug.
In patients with severely impaired liver function, a dose reduction is necessary taking into account the individual tolerance of the drug.
In patients with low blood pressure, as well as in people at risk due to a possible decrease in blood pressure (patients with severe coronary artery disease or with hemodynamically significant stenosis of the cerebral vessels), treatment can be started in small doses, in these cases the dose should be increased gradually.
Side effects
From the nervous system: headache, dizziness, anxiety, sleep disturbances, cramps.
From the skin and subcutaneous fat: flushing of the skin, flushing of the face and upper chest, swelling, increased fragility of the nails.
From the digestive system: xerostomia, anorexia, intestinal atony.
From the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, decreased blood pressure.
On the part of the hemostatic system and hemopoietic organs: leukopenia, thrombocytopenia, pancytopenia, bleeding from blood vessels of the skin, mucous membranes, stomach, intestines, hypofibrinogenemia.
On the part of the sensory organs: impaired vision, scotoma.
Allergic reactions: itching, flushing of the skin, urticaria, angioedema, anaphylactic shock.
Drug Interaction
Pentoxifylline is able to potentiate the effects of drugs that reduce blood pressure (ACE inhibitors, nitrates).
Pentoxifylline can increase the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins).
Cimetidine increases the concentration of pentoxifylline in plasma (risk of side effects).
Co-administration with other xanthines can lead to excessive nervous excitation.
Increased hypoglycemic effects of insulin or oral hypoglycemic agents with pentoxifylline (increased risk of hypoglycemia). If combination therapy is required, strict monitoring of the patient’s condition is required.
In some patients, concomitant administration of pentoxifylline and theophylline may lead to increased plasma concentrations of theophylline. This can lead to an increase or increase in the side effect associated with theophylline.
Overdose
Symptoms: weakness, sweating, nausea, cyanosis, dizziness, decreased blood pressure, tachycardia, syncope, drowsiness or agitation, arrhythmia, hyperthermia, areflexia, loss of consciousness, tonic-clonic convulsions, signs of gastrointestinal bleeding (vomiting such as coffee grounds).
Treatment: symptomatic, special attention should be paid to the maintenance of blood pressure and respiratory function. Convulsive seizures are removed by the introduction of diazepam.
Storage conditions
Store at a temperature of +8 C to +25 C in a dark place.
Keep out of the reach of children.
Shelf suitability
4 Year
Active ingredient
Pentoxifylline
Conditions of supply of pharmacies
Prescription Pharmacy terms
Prescription
dosage form
dosage form
infusion solution
Sanofi India Ltd, France
