Torasemide

Pharmacological properties

the main mechanism of action of the drug is due to inhibition of renal reabsorption of sodium and chlorine ions in the ascending part of the loop of Henle. does not significantly affect the level of glomerular filtration, renal plasma flow.

Pharmacokinetics Britomar, tablets of prolonged action, provide a gradual release of the active active substance, which reduces the fluctuation of its concentration in the blood serum in contrast to immediate-acting drugs.

Suction. After repeated use, the relative bioavailability of torasemide in the form of sustained-release tablets compared with immediate-acting drugs is 100%. After oral administration C_max in blood plasma is reached after 1.5 hours. Absorption rates do not change in the presence of hepatic or renal failure.

Distribution. The binding of torasemide to plasma proteins is 99%. The volume of distribution of torasemide is 12-15 liters. In patients with cirrhosis, the volume of distribution is almost doubled.

T_½ torasemide is approximately 4 hours. The excretion process is provided by metabolism in the liver (about 80% of the total clearance) and excretion by the kidneys (approximately 20% in patients with normal renal function) due to excretion of the compound through the proximal tubules in the urine.

In patients with decompensated heart failure, hepatic and renal clearance decreases, T_½ and AUC lengthen.

In patients with renal failure, the renal clearance of torasemide is significantly reduced, the total clearance indicator does not significantly change. The necessary diuretic effect in this group of patients is provided by increasing the dosage.

Indications

Edema caused by congestive heart failure, kidney or liver disease; essential hypertension - in the form of monotherapy or in combination therapy with other antihypertensive drugs.

Application

Take the tablets without chewing or crushing, regardless of food intake and time of day, with a small amount of liquid.

Congestive Heart Failure

The total initial dose is 10–20 mg once a day.

In the absence of the necessary diuretic effect, the dose must be increased by 2 times (20–40 mg / day) until the desired effect is achieved.

Chronic renal failure

The total initial dose is 20 mg once a day.

In the absence of the necessary diuretic effect, the dose must be increased 2 times (40 mg / day) until the desired effect is achieved.

Cirrhosis of the liver

The total initial dose is 5–10 mg once a day with combined use with drugs - aldosterone antagonists or potassium-sparing diuretics. In the absence of the necessary diuretic effect, the dose must be increased by 2–3 times (10–20 mg / day) until the desired effect is achieved.

Data on a single dose of doses in excess of 40 mg / day are not available.

Essential hypertension

The total initial dose is 5 mg 1 time per day.

If such a dosage regimen does not provide the necessary reduction in blood pressure within 4-6 weeks, the dose must be increased to 10 mg once a day.

If necessary, complex therapy with other hypotonic agents should be used.

Elderly patients do not need a special selection of doses.

Patients with renal failure may need to increase the dose to achieve the necessary diuretic effect due to reduced clearance of torasemide. Patients with severe hepatic impairment should be aware that increased renal clearance of torasemide may be accompanied by a decrease in the excretion of sodium ions.

Contraindications

Hypersensitivity to the components of the drug or sulfonylurea derivatives.

Renal failure accompanied by anuria.

Rare hereditary galactose intolerance, lactase deficiency or malabsorption of glucose-galactose.

Side effects

Side effects by frequency of occurrence are classified into the following categories: very often (1/10), often (1/100, 1/10), infrequently (1/1000, 1/100), rarely (1/10 000, 1/1000 ), very rarely (1/10 000), including individual messages.

Metabolic disorders: infrequently - hypercholesterolemia, hyperlipidemia, polydipsia.

From the nervous system: often - dizziness, headache, drowsiness; infrequently - cramps of the lower extremities.

On the part of the cardiovascular system: infrequently - extrasystole, palpitations, tachycardia, facial redness.

From the respiratory system: infrequently - nosebleeds.

From the digestive tract: often - diarrhea; infrequently - abdominal pain, flatulence.

From the kidneys and urinary system: often - an increase in the frequency of urination, polyuria, nocturnal polyuria; infrequently - peremptory urination.

General disorders: infrequently - thirst, weakness, fatigue, increased activity, nervousness.

Changes in laboratory parameters: infrequently - a decrease in platelet count.

Other adverse reactions may occur in the form of nausea, vomiting, hyperglycemia, hyperuricemia, hypovolemia, arterial hypotension, impotence, thrombosis, skin reactions, syncope.

special instructions

Britomar should be used with extreme caution in patients with liver diseases that are accompanied by liver cirrhosis and ascites, since sudden changes in water-electrolyte balance can lead to hepatic coma. therapy with Britomar (as well as other diuretics), patients in this group should be carried out in a hospital. to prevent hypokalemia and metabolic acidosis, this drug should be prescribed with drugs - aldosterone antagonists or drugs that help potassium to be retained in the body. after taking torasemide, ototoxicity phenomena (tinnitus and hearing loss) were observed, which were reversible, but there was no direct connection with the use of the drug.

When prescribing diuretics, it is necessary to carefully monitor the clinical symptoms of electrolyte imbalance, hypovolemia, extrarenal azotemia, and other disorders manifested in the form of dry mouth, thirst, weakness, lethargy, drowsiness, agitation, muscle pain or seizures, myasthenia gravis, hypotension, oliguria, tachycardia , nausea, vomiting. Excessive diuresis can cause dehydration, lead to a decrease in bcc, thrombosis and embolism of blood vessels, especially in elderly patients. Patients with a violation of the water-electrolyte balance must stop using the drug and, after eliminating the side effects, restore Britomar therapy, starting with lower doses.

In patients with cardiovascular disease, especially when taking digitalis preparations, hypokalemia that occurs when taking diuretics may increase the risk of arrhythmia.

When prescribing the drug, regular laboratory monitoring of serum potassium and other electrolytes is necessary.

During pregnancy and breastfeeding. There are no clinical data on the use of Britomar during pregnancy and its excretion into breast milk. Therefore, during pregnancy and lactation, the drug is used if the expected benefit to the mother outweighs the potential risk to the fetus.

Children. Clinical data on the effectiveness and safety of the drug in children are not available, therefore, it is not recommended to assign it to patients of this age category.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms.The drug can change the reaction rate of a person, reducing it, while driving vehicles and working with other mechanisms, especially when used simultaneously with alcohol. Therefore, you should avoid driving and working with potentially dangerous mechanisms during treatment with the drug.

Interactions

With the simultaneous use of Britomar with β-adrenoreceptor blockers, calcium channel blockers, apf inhibitors, digitalis preparations, organic nitrates, no new or unforeseen side effects have been identified.

Taking Britomar does not affect the ability to bind glibenclamide or warfarin to proteins, does not change the anticoagulant properties of fenprocoumone, and does not affect the pharmacokinetic characteristics of digoxin or carvedilol. In the case of combined use of torasemide with spironolactone, the renal clearance of the latter decreases, but there is no need for dose adjustment of drugs.

With simultaneous use with salicylates in high doses, the toxic effect of salicylates is enhanced. NSAIDs (including acetylsalicylic acid) when combined with Britomar and other diuretics acting on the Henle loop can impair renal function.

With simultaneous use with indomethacin, the diuretic effect of torasemide is partially suppressed (only with a limited intake of sodium in the body - 50 mEq / day), under the conditions of normal sodium intake (150 mEq / day), such phenomena were not observed.

Cimetidine, spironolactone do not alter the effectiveness of torasemide.

Digoxin can increase AUC of torasemide by 50%, however dose adjustment is not necessary.

Combined therapy with cholestyramine is recommended at different intervals. With simultaneous administration with probenecid, the diuretic effect of torasemide is reduced. Diuretics reduce the renal clearance of lithium, increasing its toxic effect, and can increase the ototoxic effect of aminoglycosides and ethacrine acid, especially in patients with renal failure. No studies of interaction with Britomar have been performed.

Overdose

To date, overdose phenomena resulting from the use of Britomar have not been noted. in case of overdose, there may be an increase in adverse reactions (hypovolemia, arterial hypotension, hyponatremia, hypochloremic alkalosis, hemoconcentration). in case of an overdose, it is necessary to carry out therapy aimed at maintaining water-electrolyte balance.

Storage conditions

At a temperature not exceeding 25 ° C.