TEVA #Urogenital_tract #Urolithiasis #HEALTH_CARE
Pharmacological properties
Pharmacodynamics. Torasemide is a loop diuretic that inhibits renal reabsorption of sodium and chlorine ions in the ascending part of the henle loop. However, in low doses, the pharmacodynamic profile of torasemide in the degree and duration of diuresis brings it closer to the thiazide class. in high doses, torasemide provides diuresis with dose-dependent intensity and a high limit of effect. The maximum diuretic activity of torasemide is achieved 2-3 hours after oral administration. In healthy volunteers, doses of 5–100 mg caused a logarithmic increase in diuretic activity. The antihypertensive effect of torasemide is associated with a decrease in the ovarian pressure due to a decrease in patients with arterial hypertension of the increased activity of free ca2 + in the cells of the muscle layer of the arteries. as a result of this, contractility and the reaction of the vessels to the body's own pressor substances, for example, catecholamines, are probably reduced.
Pharmacokinetics. After oral administration, torasemide is rapidly and almost completely absorbed in the gastrointestinal tract. Cmax in blood plasma is achieved within 1–2 hours. Systemic bioavailability after oral administration is 80–90%. More than 99% of torasemide binds to blood plasma proteins, and the binding to proteins of metabolites M1, M3 and M5 is 86, respectively; 95 and 97%. The volume of distribution reaches 16 liters. During the metabolism of torasemide due to stepwise oxidation, hydroxylation or ring hydroxylation, three metabolites are formed - M1, M3 and M5. Hydroxyl metabolites are diuretic. The share of metabolites M1 and M3 accounts for about 10% of the pharmacodynamic action, and the metabolite M5 is inactive.
In healthy volunteers, the final T½ of torasemide and its metabolites is 3-4 hours. The total clearance of torasemide reaches 40 ml / min, and the renal clearance is about 10 ml / min. Approximately 80% of the dose is excreted by the renal tubules in the form of torasemide and its metabolites: torasemide - 24%, M1 - 12%, M3 - 3%, M5 - 41%. In case of impaired renal function, the T½ of torasemide does not change, but the T½ of the metabolites M3 and M5 increases. Hemodialysis and hemofiltration do not significantly remove torasemide and its metabolites. If in patients with impaired renal function there is an increase in the concentration of torasemide in the blood plasma, then this is most likely a consequence of a weakening of hepatic metabolism. In patients with heart failure or impaired liver function, the T½ of torasemide and the M5 metabolite increases slightly, but accumulation is unlikely.
Indications
Essential ag. swelling and / or effusion caused by congestive heart failure.
Application
Essential ag: the recommended dose of torasemide is 2.5 mg (½ torasemide-teva tablet 5 mg) once a day. if necessary, the dose can be increased to 5 mg / day. the use of doses of 5 mg / day does not cause an additional decrease in blood pressure. the maximum hypotensive effect is achieved after about 12 weeks of continuous treatment.
Edema: the usual recommended dose is 5 mg once a day. This is usually a maintenance dose. If necessary, the dose can be gradually increased to 20 mg once a day.
Elderly patients. Use with caution, since there is insufficient information about the need for dose adjustment for elderly patients.
Patients with impaired liver and kidney function. Information on dose adjustment in patients with impaired liver and kidney function is limited. In patients with impaired liver function, it should be used with caution, since an increase in the concentration of torasemide in the blood plasma is possible.
Reception method. Used internally. Torasemid-Teva tablets should be used in the morning, without chewing, with a small amount of liquid. Bioavailability of Torasemid-Teva does not depend on food intake. The duration of treatment depends on the course of the disease.
Children. Safety and efficacy in children have not been established, therefore, torasemide should not be prescribed to this age group of patients.
Contraindications
Hypersensitivity to torasemide, sulfonylurea or any component of the drug. impaired renal function, accompanied by anuria, impaired urination. disorders of urination (for example, benign prostatic hyperplasia). hepatic coma and precoma. arterial hypotension. arrhythmia (for example, sinoatrial blockade, av-block II – III degree). hypokalemia, hyponatremia, hypovolemia.
Side effects
From the side of metabolism: violations of water and electrolyte balance (especially with a noticeable restriction of salt in the diet), hypokalemia (especially in the case of insufficient potassium in the diet, as well as vomiting, diarrhea, frequent use of laxatives and liver dysfunction); an increase in the level of uric acid, glucose and lipids in the blood plasma; exacerbation of metabolic alkalosis, hyperuricemia, hypovolemia, hyponatremia.
With a sufficiently strong diuresis, especially at the initial stage of treatment and in elderly patients, symptoms and signs of a decrease in the amount of electrolytes and their volume may occur, for example, headache, dizziness, arterial hypotension, weakness, drowsiness, confusion, loss of appetite and convulsions. Dose adjustment is required.
From the side of the cardiovascular system: thromboembolic complications; cardiac and cerebral ischemia, which can lead, in particular, to cardiac arrhythmias, angina pectoris, acute myocardial infarction or fainting; extrasystole, palpitations, tachycardia.
From the digestive system: loss of appetite, stomach pain, nausea, vomiting, diarrhea, constipation, pancreatitis, flatulence.
From the side of the kidneys and urinary tract: urinary retention in patients with urinary tract obstruction, urgent urge to urinate, increased levels of creatinine and urea in the blood plasma.
From the hepatobiliary system: an increase in the level of certain liver enzymes, for example, gamma-glutamyl transpeptidase.
On the part of the blood and lymphatic system: a decrease in the number of erythrocytes, leukocytes and platelets.
On the part of the skin and subcutaneous tissues: allergic reactions, including rash, itching, photosensitivity, severe skin reactions.
From the nervous system: headache, dizziness, fatigue, weakness, paresthesia of the extremities, drowsiness, increased activity, nervousness.
From the respiratory system: nosebleeds.
Others: asthenia, dry mouth, thirst, blurred vision, tinnitus, deafness.
Special instructions
Treatment with torasemid-teva should be started after correction of hypokalemia, hyponatremia and hypovolemia.
Dysfunction of the kidneys and liver. So far, limited information has been collected on dose adjustment in patients with impaired renal and hepatic function. Care should be taken to treat patients with impaired liver function, since it is possible to increase the concentration of the drug in the blood plasma. Torasemide should be used with extreme caution in patients with liver disease, accompanied by cirrhosis and ascites, since sudden changes in water and electrolyte balance can lead to hepatic coma. Therapy with torasemide (as well as other diuretics) for patients of this group should be carried out in a hospital setting. To prevent hypokalemia and metabolic alkalosis, the drug should be prescribed with drugs - aldosterone antagonists or potassium-sparing drugs.
With long-term diuretic treatment, it is recommended to regularly assess the balance of electrolytes (in particular in patients with concomitant therapy with digitalis glycosides, GCS, mineralocorticoids or laxatives), glucose, uric acid, creatinine and blood lipids, as well as blood cells (erythrocytes, leukocytes and platelets) ...
Careful monitoring of patients with a tendency to hyperuricemia and gout is recommended. Blood glucose control is necessary for latent or severe diabetes. Due to the lack of sufficient experience in clinical use, it is not recommended to prescribe torasemide for:
- pathological changes in acid-base balance;
- concomitant use of lithium, aminoglycosides or cephalosporins;
- impaired renal function caused by nephrotoxic agents;
- pathological changes in the blood (for example, thrombocytopenia or anemia in patients without impaired renal function).
Torasemid-Teva tablets contain lactose. The drug should not be used in patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Use during pregnancy and lactation. There is no data on the effect of torasemide on the embryo and fetus. Animal studies have shown no fetal or maternal toxicity after high doses. Torasemide penetrates the fetal membrane and causes electrolyte disturbances. There is also a risk of neonatal thrombocytopenia.
During pregnancy, the drug is used only when the expected benefit to the mother significantly outweighs the risk to the fetus. In this case, the lowest possible dose should be used. There are currently no data on the penetration of torasemide into breast milk. Torasemide is contraindicated for use during lactation.
The ability to influence the reaction rate when driving or working with other mechanisms. As in the case of other drugs that affect blood pressure, patients using torasemide should not drive vehicles and work with mechanisms that require concentration of attention, since dizziness and other associated symptoms may occur. This is especially true when starting treatment, increasing dosage and switching to other drugs.
Interactions
When combined with cardiac glycosides, a deficiency of potassium or magnesium can increase the sensitivity of the heart muscle to these drugs. with the simultaneous use of torasemide with mineral and glucocorticoids, laxatives, the excretion of potassium may increase.
With the simultaneous use of torasemide enhances the effect of antihypertensive drugs, in particular ACE inhibitors.
Sequential or combination therapy, as well as the beginning of a new concomitant therapy with an ACE inhibitor, can cause severe arterial hypotension. It can be reduced by lowering the initial dose of the ACE inhibitor or by reducing the dose / temporarily discontinuing the drug 2 or 3 days before starting the ACE inhibitor.
Torasemide can reduce the sensitivity of the arteries to vasoconstrictors, such as epinephrine, norepinephrine.
Torasemide is able to weaken the effect of antidiabetic drugs.
Torasemide, especially in high doses, can enhance the nephrotoxic and ototoxic effects of aminoglycoside antibiotics and ethacrynic acid, especially in patients with renal insufficiency; the toxicity of cisplatin drugs and the nephrotoxic effect of cephalosporins.
It is also possible to enhance the action of theophylline and muscle relaxants based on curare.
NSAIDs (eg indomethacin) can reduce the hypotensive and diuretic effect of torasemide, probably due to inhibition of prostaglandin synthesis.
Probenecid reduces the effectiveness of torasemide due to inhibition of tubular secretion.
An increase in plasma concentrations of lithium is possible, as well as an increase in the severity of its cardio- and neurotoxic effects.
Torasemide inhibits the excretion of salicylates by the kidneys, which increases the risk of their toxicity in patients using high doses of salicylates.
With the simultaneous use of torasemide and cholestyramine, the absorption of torasemide may decrease, thereby weakening the effect of the latter.
Overdose
Symptoms in case of an overdose, an increase in side reactions (strong diuresis, causing dehydration, hypovolemia, arterial hypotension, hyponatremia, hypochloremic alkalosis, hemoconcentration, drowsiness, confusion, cardiovascular failure, loss of consciousness) is possible. possible gastrointestinal disturbances.
Treatment. The specific antidote is unknown. Symptoms and signs of an overdose may necessitate a dose reduction or discontinuation of Torasemid-Teva with a parallel restoration of fluid and electrolyte balance and symptomatic treatment.
Storage conditions
At a temperature not exceeding 30°c.
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