Britomar - instructions for use, doses, side effects, contraindications

Active substanceTorasemideTorasemide

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Dosage form: & nbsp

sustained-release tablets

Composition:

1 tablet of 5 mg prolonged action contains: active substance - torasemide 5 mg

Excipients: guar gum 3.40 mg, corn starch 30.77 mg, silicon colloidal dioxide 0.42 mg, magnesium stearate 0.25 mg, lactose monohydrate up to 85 mg;

1 tablet of the prolonged action of 10 mg contains:

active substance - torasemide 10 mg

Excipients: guar gum 6.80 mg, corn starch 61.54 mg, silicon dioxide colloid 0.85 mg, magnesium stearate 0.51 mg, lactose monohydrate up to 170 mg.

Description:Round biconvex tablets white or almost white with engraved "SN" on one side.

Pharmacotherapeutic group:Diuretics

ATX: & nbsp

C.03.C.A Sulfonamide diuretics

C.03.C.A.04 Torasemide

Pharmacodynamics:Torasemide is a "loop" diuretic. The main mechanism of action of the drug is due to the reversible binding of torasemide to the sodium / chlorine / potassium transporter located in the apical membrane, the thick segment of the ascending loop of Henle, resulting in reduced or completely inhibited reabsorption of sodium ions and decreases the osmotic pressure of the intracellular fluid and water reabsorption. Torasemide to a lesser extent than furosemide, causes hypokalemia, while it shows great activity and its effect is more prolonged. The diuretic effect develops approximately an hour after ingestion, reaching a maximum in 3-6 hours, and lasts from 8 to 10 hours.

Reduces systolic and diastolic blood pressure (BP) in the "lying" and "standing".

Pharmacokinetics:

The drug sustained-release tablets Britomar provides for gradual release torasemide, reducing fluctuations in the blood concentration, compared with preparations of torasemide in a dosage form of a tablet with a conventional release.

Suction

After taking several doses of the drug, the relative bioavailability of the prolonged form, compared with the usual dosage form, is about 102%. The active substance is absorbed in the gastrointestinal tract (GIT) with a limited effect of the "first passage" through the liver and the maximum concentration (C_m_Oh) in the blood plasma is achieved within 1.5 hours after ingestion. Eating does not have a significant effect on the absorption of the drug. Impaired renal and / or liver function does not affect the absorption of the drug.

Distribution

More than 99% of torasemide binds to blood plasma proteins.

Volume of distribution (V_d) in healthy volunteers and in patients with mild and moderate renal failure or chronic heart failure - from 12 to 15 liters. Have patients with cirrhosis of the liver V_d doubled.

Metabolism

Metabolized by isoenzyme CYP2C9 cytochrome P450 in the liver with the formation of three metabolites.

The main metabolite is a carboxylic acid derivative, is pharmacologically inactive. Two other metabolites, which in the body are formed in a small amount,have some diuretic activity, but their concentrations are too low to have any meaningful clinical effect.

Excretion

Half-life (T_1/2) of torasemide in healthy volunteers is 4 hours.

About 80% of the ingested dose is excreted by the kidneys in the form of metabolites and about 20% in unchanged form (in patients with normal renal function).

The total clearance of torasemide is 41 ml / min and the renal clearance is about 10 ml / min, which corresponds to approximately 25% of the total.

Pharmacokinetics in special clinical cases

In patients with chronic heart failure in the stage of decompensation, hepatic and renal clearance of the drug is decreased. In such patients, the total clearance of torasemide is 50% less than in healthy volunteers, and T_1/2 and overall bioavailability, respectively, is higher.

In patients with renal failure, the renal clearance of torasemide is markedly reduced, but this does not affect the overall clearance of the drug. Diuretic effect in renal failure can be achieved by using large doses of the drug. Total clearance of torasemide and T_1/2 remain at the same level in the case of decreased kidney function, due to metabolism in the liver.

In patients with cirrhosis of the liver V_d_, T_1/2 and renal clearance of the drug are increased, but the overall clearance remains unchanged.

The pharmacokinetic profile of torasemide in elderly patients is similar to that in young patients, except that there is a decrease in renal clearance of the drug due to a characteristic age-related impairment of decreased renal function in elderly patients. Total ground clearance and T_1/2 they do not change.

Indications:

- Ocular syndrome of various genesis, incl. with chronic heart failure, liver diseases, and kidneys;

- arterial hypertension.

Contraindications:

- hypersensitivity to torasemide or to any of the components of the drug; patients with allergies to sulfonamides (sulfonamide antimicrobial agents or sulfonylureas) may have a cross-allergy to torasemide;

- anuria;

- hepatic coma and precoma;

- refractory hypokalemia; refractory hyponatremia;

- dehydration;

- marked abnormalities of urine outflow from any etiology (including unilateral urinary tract damage);

- digitalis intoxication;

- acute glomerulonephritis;

- sinoatrial and AV blockade of II-III degree;

- age under 18 years (safety and efficacy in children not studied);

- pregnancy;

- intolerance to galactose, deficiency of lactase or glucose-galactose malabsorption.

Carefully:

- arterial hypotension;

- hypovolemia (with or without arterial hypotension)

- disorders of urinary outflow (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis);

- ventricular arrhythmia in the anamnesis;

- acute myocardial infarction (increased risk of developing cardiogenic shock);

- diarrhea;

- pancreatitis;

- diabetes mellitus (decreased glucose tolerance);

- liver diseases complicated by cirrhosis and ascites, renal failure, hepatorenal syndrome;

- gout, hyperuricemia;

- anemia,

- simultaneous use of cardiac glycosides, amnoglycosides or cephalosporins, corticosteroids or adrenocorticotropic hormone (ACTH);

- hypokalemia;

- hyponatremia,

- lactation period.

Pregnancy and lactation:

Torasemide does not have a teratogenic effect and fetotoxicity, it penetrates the placental barrier, causing disturbances in water-electrolyte metabolism and thrombocytopenia in the fetus.

The drug Britomar is not recommended for use during pregnancy.

It is not known whether the torasemide in breast milk. The drug Britomar in the lactation period (breastfeeding) should be administered with caution.

Dosing and Administration:

Take inside. Tablets are swallowed whole, not liquid, squeezed with liquid. Tablets can be taken at any convenient constant time, regardless of food intake.

Edema Syndrome in Chronic Heart Failure

The usual initial dose is 10-20 mg orally once a day. If necessary, the dose can be doubled until the desired effect is achieved.

Edema syndrome with kidney disease

The usual initial dose is 20 mg orally once a day. If necessary, the dose can be doubled until the desired effect is achieved.

Edema syndrome with liver disease

The usual initial dose is 5-10 mg orally once a day, together with preparations of aldosterone antagonists or potassium-sparing diuretics. If necessary, the dose of Britomar can be doubled until the desired effect is achieved.

Not recommended single dose of more than 40 mg, t.its action has not been studied. The drug is prescribed for a long period or until the disappearance of edema.

Arterial hypertension

The usual initial dose is 5 mg once a day.

In the absence of an adequate reduction in blood pressure for 4-6 weeks, the dose is increased to 10 mg once a day. If this dose does not give the desired effect, a hypotensive drug of another group should be added to the treatment regimen.

To patients of advanced age correction of the dose is not required.

Dose Transmission: In case of missing the next dose, you can not take a double dose of the drug. Immediately take the forgotten dose. The next dose is taken at the usual time the next day.

Side effects:

Classification of undesirable adverse reactions (NDP) according to the frequency of development:

very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1 000); very rarely (1/10 000, including individual reports); frequency is unknown (can not be estimated from available data).

Disorders from the metabolism and nutrition:

Infrequently: hypercholesterolemia (increase in blood cholesterol), hypertriglyceridemia (an increase in triglyceride levels in the blood), polydipsia (increased thirst).

Impaired nervous system:

Often: dizziness, headache, drowsiness.

Infrequently: cramps of the muscles of the lower extremities.

Frequency not known: confusion, fainting, paresthesia in the extremities (sensation of numbness, "crawling crawling" and tingling).

Disorders from the cardiovascular system:

Infrequently: extrasystole (heart rhythm disturbance), tachycardia (increased frequency cardiac contractions), increased heart rate, redness of the face.

Frequency not known: excessive arterial hypotension, deep vein thrombosis (formation of blood clots), thromboembolism, hypovolemia (decrease in volume, circulating blood).

Disturbances from the respiratory system, chest and mediastinal organs:

Infrequently: nasal bleeding.

Disorders from the digestive system:

Often: diarrhea.

Infrequently: abdominal pain, flatulence.

Frequency not known: nausea, vomiting, loss of appetite, pancreatitis, dyspeptic disorders.

Disorders from the kidneys and urinary tract:

Often: increased frequency of urination, polyuria (increased urine production), nocturia (frequent urination at night).

Infrequently: frequent urge to urinate.

Frequency not known: urinary retention (in patients with urinary tract obstruction), increased urea and creatinine concentrations in the blood.

General disorders and disorders at the site of administration:

Infrequently: asthenia (exhaustion), thirst, weakness, fatigue, hyperactivity, nervousness.

Laboratory and instrumental data:

Infrequently: increase in the number of platelets.

Frequency not known: Hyperglycemia (increased blood glucose concentration), hyperuricemia (increased serum uric acid concentration), hypokalemia (decrease in potassium content in the blood), a decrease in the concentration of cellular blood components (erythrocytes, leukocytes and platelets), a slight increase in the concentration, alkaline phosphatase in the blood, an increase in the activity of certain "hepatic" enzymes for example, gamma-GT), hyponatremia, hypochloraemia, metabolic alkalosis.

Disturbances on the part of the organ of sight

Frequency not known: impaired vision,

Hearing disorders and labyrinthine disorders

Frequency not known: ringing in the ears and hearing loss (usually, reversible).

Disturbances from the skin and subcutaneous tissues

Frequency not known: skin reactions (skin itch, rash, photosensitization).

If any of the side effects indicated in the manual are aggravated or any other side effects not indicated in the instructions are noted, you should inform your doctor.

Overdose:

Symptoms: excessively elevated diuresis, accompanied by a decrease in bcc and a violation of the electrolyte balance of blood, followed by a marked decrease in blood pressure, drowsiness and confusion, collapse. Gastrointestinal disorders may occur.

Treatment: there is no specific antidote. Provocation of vomiting, gastric lavage, Activated carbon. Treatment is symptomatic, dose reduction or drug withdrawal and at the same time replenishment of bcc and indicators of water-electrolyte balance and acid-base state under the control of serum concentrations of electrolytes, hematocrit, symptomatic treatment.

Hemodialysis is not effective, because the excretion of torasemide and its metabolites is not accelerated.

Interaction:

Torasemide increases the toxicity of cardiac glycosides.

With simultaneous administration with mineral- and glucocorticoids, laxatives, an increase in the excretion of potassium is possible.

Torasemide enhances the effect of antihypertensive drugs.

Torasemide, especially in high doses, can enhance the nephrotoxic and ototoxic effect of aminoglycosides, antibiotics, platinum (Pt) preparations, cephalosporins. Torasemide can strengthen the action of curare-like muscle relaxants and theophylline. When salicylates are used in high doses, their toxic effect can be enhanced.

Torasemide weakens the effect of hypoglycemic drugs.

Sequential or simultaneous administration of torasemide with angiotensin-converting enzyme (ACE) inhibitors can lead to a short-term drop in blood pressure. This can be avoided by decreasing the initial dose of an ACE inhibitor or by lowering the dose of torasemide (or temporarily abolishing it).

Nonsteroidal anti-inflammatory drugs (NSAIDs) and probenecid can reduce the diuretic and hypotensive effect of torasemide.

Bioavailability and as a consequence, the effectiveness of torasemide can be reduced by joint therapy with colestyramine.

Torasemide can increase the toxicity of drugs, lithium (Li +) and ethoxyric acid ototoxicity.

Special instructions:

Apply strictly according to the doctor's prescription.

Patients with hypersensitivity, to sulfonamides and sulfonylureas may have cross-sensitivity to the Britomar preparation. In patients, especially at the beginning of treatment with the drug Britomar and the elderly, it is recommended to monitor the electrolyte balance, volume and concentration of circulating blood.

With long-term treatment with the drug Britomar, it is recommended to carry out regular monitoring of the electrolyte balance (especially the level of potassium), glucose, uric acid, creatinine, lipids and cellular components of the blood.

Patients receiving high doses of the drug Britomar, in order to avoid the development of hyponatremia and metabolic alkalosis, it is inappropriate to limit the intake of table salt.

The risk of hypokalemia is greatest in patients with liver cirrhosis expressed by diuresis, with insufficient intake of electrolytes with food, and also with simultaneous treatment with corticosteroids or ACTH.

Increased risk of development of violations of water-electrolyte balance is observed in patients with renal insufficiency. During the course of treatment, it is necessary to periodically monitor the concentration of blood plasma electrolytes (including sodium, calcium, potassium, magnesium), acid-base, residual nitrogen, creatinine, uric acid and, if necessary, appropriate corrective therapy (with higher multiplicity in patients with frequent vomiting and against the background of parenterally injected fluids).

In patients with developed water-electrolyte disorders, hypovolemia or prerenal azotemia, laboratory analysis data may include: hyper- or hyponatremia, hyper- or hypochloraemia, hyper- or hypokalemia, acid-base balance disturbances, and increased urea levels. In the event of these disorders, it is necessary to stop taking the drug Britomar before restoring normal values, and then resume treatment with Brithomar in a smaller dose. With the appearance or strengthening of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended to suspend treatment.The choice of the dosage regimen for patients with ascites against the background of cirrhosis of the liver should be carried out under stationary conditions (violations of the water-electrolyte balance may lead to the development of hepatic coma). This category of patients shows regular monitoring of plasma electrolytes.

For the prevention of hypokalemia, the use of potassium and potassium-sparing diuretics (primarily spironolactone) is recommended, as well as a diet rich in potassium.

The use of the drug Britomar may cause an exacerbation of gout. In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of glucose concentrations in the blood and urine is required.

In patients with prostatic hyperplasia, narrowing of the ureters, diuretic control is necessary in connection with the possibility of acute urinary retention.

In patients with diseases of the cardiovascular system, especially those taking cardiac glycosides, diuretic-induced hypokalemia can cause arrhythmias.

Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to avoid practicing potentially dangerous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Long-acting tablets 5 mg and 10 mg.

Packaging:For 15 tablets in PVC / PVDC / Al blister; 1 and 2 blisters with instructions for use are placed in a cardboard box.

Storage conditions:In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000318

Date of registration:22.02.2011 / 24.02.2016

Expiration Date:Unlimited

The owner of the registration certificate:Ferrer International, S.A.Ferrer International, S.A. Spain

Manufacturer: & nbsp

FERRER INTERNACIONAL, S.A. Spain

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp24.02.2017

Illustrated instructions

Instructions

Britomar (Britomar)