Furosemid-Darnitsa, table on 0:04 g No. 50

General characteristics. Structure:

Active ingredient: furosemide;

1 tablet contains furosemide (in terms of 100% dry matter) 40 mg;

excipients: potato starch; lactose, monohydrate; sodium of a kroskarmelloz; sodium lauryl sulfate; magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Furosemid-Darnitsa – high-speed natriuretic diuretic. Works throughout a thick segment of the ascending department of a Henle's loop and blocks a reabsorption of 15-20% of the filtered sodium ions. Increases removal from an organism of sodium, chlorine, bicarbonate, phosphates, calcium, magnesium and potassium, raises рН urine. Possesses secondary action due to release of intra renal mediators and redistribution of an intra renal blood-groove. The diuretic effect is characterized by short duration, considerable expressiveness and dependence on a drug dose.

Action on excretion of ions of sodium has wavy character. At the beginning, in process of increase of concentration of drug in blood, excretion of sodium accrues, and then, in process of reduction concentration of furosemide in blood, excretion of sodium decreases below initial (a phenomenon of "return"). It is caused by compensatory activation of an anti-natriuretic neurohumoral link of regulation in response to the increased diuresis. Diuretic effect of drug develops within the first hour (15-30 minutes) after reception and continues till 46 o'clock.

Pharmacokinetics. At intake bioavailability of furosemide makes 60-70%. Linkng with proteins of a blood plasma – 91-97%. It Biotransformirutsya in a liver with formation of glucuronides. 13% – with bile are excreted for 87% by kidneys. An elimination half-life (T1/2) – from 0,5 to 1 hours. Time of achievement of the maximum concentration in a blood plasma (Tmax) – 1-2 hours.

 

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of a round form of color, white or white with a creamy shade.

Indications to use:

Hypostases of different genesis: at chronic congestive heart failure (if treatment using diuretics is necessary), at a chronic renal failure, at a nephrotic syndrome (if treatment using diuretics is necessary), at liver diseases (in case of need – for addition of treatment using antagonists of Aldosteronum). An acute renal failure, including at pregnant women or at the time of delivery. Arterial hypertension.

Route of administration and doses:

The mode of dosing is set by the doctor individually depending on expressiveness of disorders of water and electrolytic balance, size of glomerular filtering, weight of a condition of the patient. Drug is accepted, as a rule, on an empty stomach.

For adults the maximum total daily dose of Furosemida-Darnitsa (at oral and parenteral administration) should not exceed 1500 mg.

Drug in this dosage form is appointed to children aged from 3 years. For children the recommended furosemide dose for oral administration makes 2 mg/kg of body weight, but the maximum daily dose should not exceed 40 mg.

Special recommendations concerning dosing for adults.

At hypostases at chronic congestive heart failure the recommended initial drug dose for oral administration makes 20-50 mg a day. In case of need it is possible to regulate a dose depending on the therapeutic answer of the patient. It is recommended to accept the day dose divided into two or three receptions.

At hypostases at a chronic renal failure it is necessary to titrate carefully a dose for ensuring gradual initial loss of liquid. It means introduction of such dose which leads to a day degrowth of a body approximately on 2 kg (about 280 mmol of Na+) for adult patients. The recommended initial daily dose for oral administration makes 40-80 mg. In case of need it is possible to adjust a dose depending on the therapeutic answer of the patient. The general daily dose can be appointed once or be divided into two receptions. For patients who are on a hemodialysis the general daily peroral dose makes 250-1500 mg.

At an acute renal failure before beginning furosemide use, it is necessary to compensate a hypovolemia, hypotension and an essential electrolytic and acid-base imbalance. It is recommended to carry out as soon as possible transition from intravenous administration to oral administration.

At hypostases at a nephrotic syndrome the recommended initial dose for oral administration makes 40-80 mg a day. In case of need it is possible to regulate a dose depending on the therapeutic answer of the patient. The general daily dose can be appointed once or be divided into several receptions.

At hypostases at diseases of a liver of Furosemid-Darnitsa appoint as addition to therapy to antagonists of Aldosteronum in those cases, a code use only of antagonists of Aldosteronum is insufficient. For prevention of complications, such as orthostatic hypotension or disturbances of electrolytic and acid-base balance, the dose should be titrated carefully to provide gradual initial loss of liquid. It means purpose of such dose which leads to a day degrowth of a body approximately on 0,5 kg for adult patients. The recommended initial daily peroral dose makes 20-40-80 mg. In case of need it is possible to regulate a dose depending on the therapeutic answer of the patient. The general daily dose can be accepted once or to divide into several receptions.

In need of use of doses of 20 mg, 50 mg appoint other drugs of furosemide in the corresponding dosage form and a dosage.

Features of use:

Use during pregnancy or feeding by a breast.

Furosemid-Darnitsa usually do not apply during pregnancy. Use to pregnant women is also at the time of delivery admissible only according to vital indications at an acute renal failure when need of use for the woman exceeds risk for a fruit. Performing treatment during pregnancy demands observation of growth and fetation.

As furosemide gets into breast milk, during treatment it is necessary to stop feeding by a breast.

Children. Drug in this dosage form is used to children aged from 3 years.

In the presence of an edema without peripheral hypostases drug is recommended to be used in doses, providing an additional diuresis of no more than 700-900 ml/days that does not cause essential changes of indicators of ions of plasma, residual nitrogen, promotes prevention of an oliguria.

At treatment of arterial hypertension the daily dose is divided on 2-3 one-time that gives the chance to avoid development of a phenomenon of "return".

At preservation of an oliguria within 24 hours treatment by drug should be stopped.

At prolonged use of drug it is necessary to measure periodically the arterial pressure (AP), level of electrolytes (especially potassium) plasmas, an urea nitrogen, creatinine, uric acid. It is reasonable to recommend to the patient meal with the high content of potassium (baked potato, bananas, tomatoes, spinach, dried fruits). It is necessary to take into account that during use of drug there can be a need for medicamentous compensation of losses of potassium.

At a diabetes mellitus drug is used under control of level of glucose in blood and urine. With care apply at gout, a hypoproteinemia.

During treatment continuous outflow of urine has to be provided with furosemide. Patients with partial obstruction of outflow of urine require careful attention, especially at the initial stages of treatment.

Treatment using furosemide demands regular medical observation. Especially careful monitoring of patients with arterial hypotension is necessary; patients who get into group of special risk owing to essential lowering of blood pressure, for example, of patients with the expressed stenosis of the coronary arteries or blood vessels delivering blood to a brain; patients with a gepatorenalny syndrome, that is with a functional renal failure which is associated with a serious illness of a liver; patients with a hypoproteinemia, for example, which is associated with a nephrotic syndrome (the effect of furosemide can be weakened along with ototoxicity strengthening). Careful titration of a dose is necessary.

Development of disturbances of electrolytic balance is influenced by such factors as the existing diseases (for example, cirrhosis, heart failure), the accompanying use of medicines and food. For example, as a result of vomiting or diarrhea there can be a lack of potassium.

Drug contains lactose therefore to patients with rare hereditary intolerance of a galactose, lactose deficit of Lapp or glyukozo-galaktozny malabsorption it is not necessary to accept drug. Patients with intolerance of some sugars need to consult with the doctor.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

At administration of drug of Furosemid-Darnitsa it is impossible to exclude probability of decline in the ability to concentrate attention that is important for the persons managing vehicles and working with mechanisms.

Side effects:

From the central and peripheral nervous system: a headache, dizziness, a depression, the strengthened feeling of thirst, paresthesia, decrease in concentration of attention, dryness in a mouth, confusion of consciousness, drowsiness, weakness, nonsense, feeling of pressure in the head.

From sense bodys: passing hearing disorder, sonitus, vision disorder.

From digestive tract: nausea, vomiting, diarrhea, pancreatitis.

From a liver and biliary tract: intra hepatic cholestatic jaundice, increase in level of hepatic transaminases, hepatic encephalopathy at patients with hepatocellular insufficiency.

Metabolic disturbances and disturbances from a metabolism: a hyperglycemia, a hyperuricemia, a hypercalcemia, a hypopotassemia, a hypochloraemia, a hypomagnesiemia, a hyponatremia, a metabolic alkalosis, an exacerbation of gout, electrolytic deficit, a giperkreatininemiya, a hypovolemia, organism dehydration, increase in level of cholesterol and triglycerides in a syrovatka of blood.

From cardiovascular system: disturbances of a cordial rhythm, acute and/or orthostatic hypotension, necrotic vasculitis, thrombophlebitis.

From system of blood: eosinophilia, purpura, aplastic anemia, thrombocytopenia, agranulocytosis, hemolitic anemia. Essential reduction of an amount of water in an organism can lead to strengthening of processes of a blood coagulation with a tendency to development of thromboses.

From a musculoskeletal system: muscular weakness, spasms, tetany.

From an urinary system: a vasculitis, intersticial nephrite, an acute ischuria at patients with disturbance of bladder emptying, a prostate hyperplasia, narrowing of an urethra.

Dermatological reactions: skin itch, exfoliative dermatitis, multiformny erythema, small tortoiseshell, violent rashes, vasculitis of vessels of skin, photosensitivity.

Allergic reactions: heavy anaphylactic and anaphylactoid reactions, acute anaphylaxis.

From an organism in general: fervescence.

Interaction with other medicines:

At simultaneous use of the drug Furosemid-Darnitsa with the following groups of medicines the following effects can be observed.

Glucocorticoids – it is necessary to apply with care glucocorticoids with Furosemidom-Darnitsa because of possible development of an imbalance of electrolytes.

Theophylline, warfarin, diazoxide, kurarepodobny drugs (tubocurarine) – amplifies effect of these drugs.

Heart glucosides (digoxin) – simultaneous use with Furosemidom-Darnitsa can cause development of arrhythmia against the background of a hypopotassemia and lead to emergence of a syndrome of lengthening of an interval of QT. Development of a hypopotassemia under the influence of Furosemida-Darnitsa increases toxicity of heart glucosides.

Amphotericinum, Cefaloridinum, cefalexin – increases nephrotoxicity  of Furosemida-Darnitsa.

Anti-hypertensive means (inhibitors of aniotenzinprevrashchayushchy enzyme, adrenoblockers, ganglioblokator) – the anti-hypertensive effect amplifies.

Phenobarbital, Phenytoinum – decreases diuretic effect of Furosemida-Darnitsa.

Thiazide diuretics – the diuretic effect of Furosemida-Darnitsa amplifies.

Ototoksichny medicines (antibiotics aminoglycosides, cephalosporins, Acidum etacrynicum) – ototoxicity of Furosemida-Darnitsa increases.

Chlorali hydras – in some cases reception of furosemide for 24 hours after Chlorali hydras can cause rushes of blood, the strengthened sweating, the excited state, nausea, increase in arterial pressure and tachycardia. Therefore, the accompanying purpose of furosemide and Chlorali hydras is not recommended.

Cisplatinum – in case of simultaneous use of Cisplatinum and furosemide exists risk of emergence of ototoksichesky effects. Besides, nephrotoxicity of Cisplatinum can amplify if furosemide is not appointed in low doses (for example 40 mg to patients with normal function of kidneys) and with positive balance of liquid when it is applied to achievement of effect of an artificial diuresis during therapy by Cisplatinum.

Sukralfat, холестирамин, холестипол –         less than 2 hours as сукральфат reduces absorption of furosemide from intestines should not be applied with an interval, that is reduces its action.

Lithium drugs – furosemide reduces removal of salts of lithium and can lead to increase in levels of lithium in blood serum what the increased risk of toxicity of lithium, including bigger risk of emergence of cardiotoxic and neurotoxic effects of lithium is result of. Thus, it is recommended to carry out careful monitoring of levels of lithium at patients who receive this combination therapy.

Inhibitors of an angiotensin-converting enzyme (APF inhibitors) or antagonists of receptors of angiotensin ΙΙ – patients who receive diuretics can suffer from heavy hypotension and deterioration in function of kidneys, including cases of a renal failure, especially at the first use of inhibitor of an angiotensin-converting enzyme or the antagonist of receptors of angiotensin ΙΙ or at the first use of these medicines in the increased dose. It is necessary to solve: or it is necessary to stop temporarily furosemide use, or at least to umenshit a furosemide dose three days before an initiation of treatment, or to increase a dose of APF inhibitor or the antagonist of receptors of angiotensin ΙΙ.

Corticosteroids, карбеноксолон, a glycyrrhiza root in high doses and prolonged use of purgatives – increases risk of development of a hypopotassemia.

Antidiabetic medicines, sympathomimetics (Epinephrinum, Norepinephrinum) – the effect of these drugs decreases.

High doses of cephalosporins – the renal failure can develop.

Cyclosporine A – the accompanying use of cyclosporine A and furosemide is associated with the increased risk of developing of gouty arthritis, secondary in relation to the hyperuricemia caused by furosemide, and disturbance of the renal excretion of urates caused by cyclosporine.

Probenetsid, the methotrexate and other medicines which, like furosemide, are exposed to considerable canalicular secretion in kidneys can reduce efficiency of furosemide. To the contrary, furosemide can reduce removal of these medicines kidneys. Performing treatment using high doses (in particular, both furosemide, and other medicines) can lead to increase in their levels in blood serum and to increase in risk of the side effects caused by furosemide or use of the accompanying therapy.

Simultaneous use of nonsteroid antiinflammatory medicines, including acetylsalicylic acid, can reduce effect of furosemide. At patients with dehydration of an orgnanizm or with a hypovolemia nonsteroid antiinflammatory medicines can lead to an acute heart failure. Under the influence of furosemide toxicity of salicylates can increase.

Nefrotoksichny medicines – strengthening of an adverse effect on kidneys is possible.

Radiocontrast substances – at the patients belonging to group of high risk of development of a nephropathy owing to therapy by radiocontrast substances at therapy furosemide observed the big frequency of deterioration in function of kidneys after purpose of radiocontrast substances in comparison with that at patients of group of high risk by which carried out only intravenous hydration to purpose of radiocontrast substances.

Contraindications:

Hypersensitivity to furosemide or to other components which are a part of drug and also to sulfonamides, sulfourea.

Patients with prekomatozny and comas which are associated with hepatic encephalopathy, an end-stage of a renal failure, an anury at nonsensitivity to furosemide.

Expressed giponatry-and a hypopotassemia, a hypovolemia, dehydration.

Pregnancy, except use at an acute renal failure for pregnant women and at the time of delivery (performing treatment during pregnancy demands observation of growth and fetation). Feeding period breast.

Overdose:

Arterial hypotension, decrease in volume of the circulating blood, increase in a hematocrit, hypopotassemia and gipokhloremicheskiya анкалоз, dehydration, a collapse, arrhythmias, an acute renal failure.

Treatment. Correction of acid-base equilibrium, correction of ions of plasma, normalization of the central venous pressure.

Storage conditions:

Period of validity. 3 years. To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on 5 blister strip packagings in a pack.