Lasik - instructions for use, dose, side effects, contraindications

Excipients: lactose - 53.00 mg, starch - 56.88 mg, pregelatinized starch - 7.00 mg, talc - 2.40 mg, silicon dioxide colloid - 0.40 mg, magnesium stearate - 0.32 mg.

Description:White or almost white round tablets engraved with "DLI" above and below the risks on one side.

Pharmacotherapeutic group:diuretic

ATX: & nbsp

C.03.C.A.01 Furosemide

Pharmacodynamics:

A drug Lasix® is a strong and quick-acting diuretic, which is a sulfonamide derivative. A drug Lasix® blocks the ion transport system sodium (Na⁺), potassium (TO⁺⁾ chlorine (Cl) In the thick segment of the ascending knee of the Henle loop, in connection with this, its diuretic effect depends on the receipt of the drug in the lumen of the renal tubules (due to the mechanism of anion transport). Diuretic action of the drug Lasix® is associated with oppression reabsorption of sodium chloride in this loop section Henle. Secondary effects towards increase excretion of sodium are: an increase in the number of allocated urine (due to osmotically bound water) and enlargement secretion of potassium in distal part of the renal tubule. Simultaneously increases elimination of calcium and magnesium ions. With a decrease tubular secretion furosemide or in binding furosemide with the lumen of tubules by albumin (eg, with nephrotic syndrome) effect of furosemide decreases.

At the course of taking the drug Lasix® its diuretic activity does not decrease, as furosemide interrupts tubular-glomerular feedback in Macula densa (tubular structure, closely related to juxtaglomerular complex). A drug Lasix® causes dose-dependent stimulation renin-angiotensin-aldosterone system.

With heart failure A drug Lasix® rapidly reduces preload (by expanding the veins), reduces pulmonary artery pressure and the filling pressure of the left ventricle. This rapidly developing effect appears to be mediated through the effects of prostaglandins and therefore the condition for its development is the absence of disturbances in the synthesis of prostaglandins, in addition to which this effect also requires sufficient preservation of kidney function.

A drug Lasix® has an antihypertensive effect that is caused by increased sodium excretion, a decrease in the volume of circulating blood, and a decrease in the response of the smooth muscles of the vessels to vasoconstrictive stimuli (due to the natriuretic effect furosemide reduces the response of blood vessels on catecholamines, whose concentration in patients with arterial hypertension is increased).

After ingestion of 40 mg of the drug Lasix ® diuretic effect develops for 60 minutes and lasts about 3-6 hours.

In healthy volunteers who received 10 to 100 mg of Lazix®, dose-dependent diuresis and sodium nares were observed.

Pharmacokinetics:

Furosemide is rapidly absorbed in the gastrointestinal tract. Him t_max. (time to reach the maximum concentration in the blood) is from 1 to 1.5 hours. The bioavailability of furosemide in healthy volunteers is approximately 50-70%. Have patients The bioavailability of Lasix® can be reduced to 30%, since it can be influenced by various factors, including the underlying disease. The volume distribution of furosemide is 0.1-0.2 l / kg body weight. Furosemide binds to blood plasma proteins (more than 98%), in mainly with albumins.

Furosemide is displayed mainly in an unchanged form and, mainly, by secretion in the proximal tubules. G, fucosemide metabolites are fructose 10-20% of the kidney-excreted drug. The remaining dose is secreted through the intestine, apparently by biliary secretion.

The final half-life of furosemide is nApproximately 1-1.5 hours.

Furosemide penetrates through placental barrier and excreted in breast milk. Him Concentration in the fetus and newborn is the same as that of the mother.

Peculiarities of pharmacokinetics in individual groups patients

With renal insufficiency the elimination of furosemide slows down, and the half-life increases; with expressed renal deficiency, the terminal half-life may increase to 24 hours.

With nephrotic syndrome a decrease in plasma protein concentrations leads to an increase in the concentrations of unbound furosemide (its free fraction), in connection with which the risk of development of ototoxic effect increases. On the other hand, the diuretic effect of furosemide in these patients can be reduced by binding furosemide to albumin in the tubules and reducing the tubular secretion of furosemide.

With hemodialysis and peritoneal dialysis and permanent ambulatory peritoneal dialysis furosemide is slightly excreted.

With hepatic insufficiency the half-life of furosemide is increased by 30-90%, mainly due to an increase in the volume of distribution.

Pharmacokinetic parameters in this category of patients can vary greatly.

With heart failure, severe arterial hypertension and patients old age excretion of furosemide slows down due to decreased kidney function.

Indications:

edematous syndrome with chronic heart failure
edematous syndrome with chronic renal failure
acute renal failure, including those with pregnancy and burns (to maintain fluid excretion);
edematous syndrome with nephrotic syndrome (with nephrotic syndrome in the foreground is the treatment of the underlying disease);
edematous syndrome with liver diseases (if necessary in addition to treatment with aldosterone antagonists);
arterial hypertension.

Contraindications:

Hypersensitivity to active substance or to any from the components of the preparation; the patients with allergy to sulfonamides (sulfonamide antimicrobial agents or sulfonylureas), as it can develop "cross" allergy to furosemide.
Renal failure with anuria (in the absence of reaction to receive furosemide);
Hepatic coma and precoma, associated with hepatic encephalopathy.
Pronounced hypokalemia.
Pronounced hyponatremia.
Hypovolemia (with a decrease blood pressure or not lowering blood pressure) or dehydration.
Severe violations especially a dangerous outflow of urine of any etiology, including unilateral urinary tract damage.

Intoxication cardiac glycosides.

Acute glomerulonephritis.
Decompensated aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy.

An increase in the venous pressure (more than 10 mm Hg).

Children up to 3 years of age (solid dosage form).
Pregnancy (see "Pregnancy and the period thoracic feeding ").

Breastfeeding period (see "Pregnancy and the period of breastfeeding").

Carefully:

With arterial hypotension;
In situations where excessive lowering blood pressure is particularly dangerous (stenosing lesions of the coronary and / or cerebral arteries);
With acute myocardial infarction (increased risk of developing cardiogenic shock);
With latent-flowing or manifested diabetes mellitus;
With gout;
With hepatorenal syndrome (that is, with functional renal failure associated with liver disease);
With hypoproteinemia (for example, with nephrotic syndrome, when it is possible to reduce the diuretic effect and increase the risk of development of ototoxic effect of furosemide); the choice of dose in such patients should be carried out with extreme caution;
With partial obstruction of the urinary tract (prostatic hyperplasia, narrowing urethra);
With an increased risk of development of water-electrolyte balance disorders and acid-base state of or in case of significant fluid loss (vomiting, diarrhea, excessive sweating - it is required to monitor the state of the water-electrolyte balance and acid-ground state and, if necessary, correction of their disorders prior to the use of furosemide);
With pancreatitis;
With ventricular arrhythmias in the anamnesis;
With systemic lupus erythematosus;
With simultaneous prescription of risperidone in elderly patients with dementia (risk of increased mortality).

Pregnancy and lactation:

Furosemide penetrates through placental barrier, so it is not should be administered during pregnancy without strict medical evidence. If for life indications a drug Lasix® is prescribed to pregnant women, careful monitoring of the fetus's condition and development is necessary.

During lactation, admission preparation Lasix® contraindicated, since he suppresses lactation.

Women should not breast-feed if they take preparation Lasix®.

Dosing and Administration:

General recommendations:

Tablets should be taken on an empty stomach without chewing and drinking with a sufficient amount of liquid.

When using the drug Lasix® it is recommended to take it at the lowest doses, sufficient to achieve the necessary therapeutic effect. Recommended maximum daily intake for adults is 1500 mg, and in children - 40 mg.

Duration of treatment determined by a doctor individually depending on the indication.

Special recommendations for dosing regimen

Children

Children recommended daily dose for oral intake is 2 mg / kg body weight (but not more than 40 mg per day).

Adults

Edema syndrome with liver diseases

The drug Lasix is used in addition to treatment antagonists of aldosterone in their insufficient effectiveness. For prevention complications such as orthostatic regulation blood circulation, violations water-electrolyte balance or acid-base state, a careful dose selection is required so that the loss of fluid occurred gradually (at the beginning fluid loss is possible up to about 0.5 kg of mass body per day). Recommended the initial dose is 20-80 mg per day. She can be adjusted depending on the response of the patient. Daily dose can be applied once a day or divide into 2 admission.

Ocular syndrome in chronic renal failure

The natriuretic reaction to furosemide depends on several factors, including severity renal failure and the content of sodium in the blood, so the effect of the dose can not be accurately predictable. Have patients with chronic renal disease insufficiency is required careful selection of the dose, by gradual increase in order, so that fluid loss occurred gradually (at the beginning of the treatment, a loss of fluid up to about 2 liters per day, about 280 mmol Na + per day). The recommended initial dose is a dose of 40-80 mg per day. The necessary dose is selected depending on the diuretic response. The entire daily dose should be taken once or divided into two doses. In patients on hemodialysis, the maintenance dose is usually 250 to 1500 mg / day.

Acute renal failure (to maintain the excretion of fluid)

Before starting treatment with Lasix, hypovolemia, arterial hypotension and significant disturbances of the water-electrolyte balance and / or acid-base state should be eliminated. Treatment begins with intravenous administration of the drug Lasix®.The recommended initial dose is 40 mg intravenously. If this does not achieve the necessary diuretic effect, the drug Lasix can be administered in the form of continuous intravenous infusion, starting at a rate of 50-100 mg per hour. It is recommended to transfer the patient as soon as possible intravenous introduction of the preparation Lasix® on the taking of tablets of the drug Lasix® (the dose of tablets depends on the selected intravenous dose).

Edema with nephrotic syndrome

The recommended initial dose is 40-80 mg per day. The necessary dose is selected depending on the diuretic response. The daily dose can be taken at one time or divided into several receptions (see sections "Pharmacokinetics" and "Special instructions").

Ocular syndrome in chronic heart failure The recommended initial dose is 20-80 mg per day. The necessary dose is selected depending on the diuretic response. It is recommended that the daily dose be divided into two or three doses.

Arterial hypertension The drug Lasix can be used in monotherapy or in combination with other antihypertensive drugs.

The usual maintenance dose is a dose of 20-40 mg per day. With arterial hypertension in combination with chronic renal insufficiency can The use of higher doses of Laxix® is required.

Side effects:

Frequency of occurrence undesirable reactions / adverse events (HP / AE) is derived from the data literature and clinical research. If the frequency of occurrence for some and the same HP / AH in the literature and data from clinical trials differed, the highest incidence of HP / AH was indicated. The following gradations of the frequency of occurrence of HP / AH by classification CIOMS (Council of International Medical Scientific Organizations): Often >10%; often> 1% and <10%; infrequently> 0.1% and <1%; rarely> 0.01% and <0.1%; very rarely < 0,01 %, frequency unknown (it is not possible to determine the frequency of occurrence of HP / AH from the available data).

Disorders from the metabolism and nutrition

Often

- Violations of the water-electrolyte balance, including those that occur with clinical symptoms. Symptoms that indicate the development of violations of water electrolyte balance can be headache, seizures, tetany, muscle weakness, heart rhythm disturbances and dyspeptic disorders. These disorders can develop either gradually (for a long time) or quickly (for a very short time, for example, in the case of high doses of furosemide in patients with normal renal function). Factors contributing to the development of violations of water electrolyte balance are the main diseases (for example, cirrhosis of the liver or heart failure); concomitant therapy with means that change the water-electrolyte balance; malnutrition and drinking regimen; vomiting, diarrhea, profuse sweating.

-Dehydration and hypovolemia (decrease in the volume of circulating blood), especially in elderly patients, which can lead to hemoconcentration with a tendency to develop thrombosis (see below).

- Increased concentration creatinine in the blood.

- Increased concentration triglycerides in the blood.

Often

- Hyponatremia, hypochloraemia, hypokalemia, increase concentration of cholesterol in the blood.

- Increased urinary concentration acids in the blood and seizures gout.

Infrequently

- Decreased tolerance to glucose.A manifestation is possible latent sugar diabetes (see section "Special instructions ").

Frequency unknown

- Hypocalcemia, hypomagnesemia, increase in concentration urea in the blood, metabolic alkalosis, Barter's pseudosyndrome if incorrect and / or long-term use furosemide.

Vascular disorders

Very often (for intravenous infusion)

- Reduction of arterial pressure, including orthostatic hypotension (this AE mainly relates to parenteral use furosemide).

Rarely

- Vasculitis.

Frequency unknown

- Thrombosis.

Infringements from kidneys and urinary tract

Often

- Increase the volume of urine.

Rarely

- Tubulointerstitial nephritis.

Frequency unknown

- Increased sodium content and chloride in the urine.

- Urine retention (in patients with partial obstruction urinary tract, see section "Special instructions").

- Nephrocalcidinosis / nephrolithiasis of premature infants (see "Special instructions." This is NU applies only to injecting dosage form of furosemide, since children up to 3 years of taking tablets of the drug Lasix is contraindicated).

- Renal failure (see section "Interaction with other drugs").

Disorders from the digestive system

Infrequently

- Nausea.

Rarely

- Vomiting, diarrhea.

Rarely

- Acute pancreatitis.

Disturbances from the liver and bile ducts

Rarely

- Cholestasis, an increase in the activity of "liver" transaminases.

Disturbances from the nervous system

Often

- Hepatic encephalopathy in patients with hepatocellular insufficiency (see section "Contraindications").

Rarely

- Parrest.

Hearing disorders and labyrinthine disorders

Infrequently

- Hearing disorders, usually transient, especially in patients with renal failure, hypoproteinemia (eg, with nephrotic syndrome). There have been reported cases of deafness, sometimes irreversible, after taking furosemide by mouth or intravenously.

Rarely

- Noise in ears.

Disturbances from the skin and subcutaneous tissues

Infrequently

- Skin itching, urticaria, rash, bullous dermatitis, erythema multiforme, pemphigoid, exfoliative dermatitis, purpura, photosensitivity reactions.

Frequency unknown

- Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, DRESS- syndrome: drug rash with eosinophilia and systemic symptoms.

Disorders from the immune system systems

Rarely

- Severe anaphylactic or anaphylactoid reactions up to before the development of anaphylactic shock.

Frequency unknown

- Weighting the flow or exacerbation of systemic red lupus.

Violations from the blood and lymphatic system

Often

- Haemoconcentration.

Infrequently

- Thrombocytopenia.

Rarely

- Leukopenia, eosinophilia.

Rarely

- Agranulocytosis, aplastic anemia or hemolytic anemia.

Congenital, hereditary and genetic disorders

Frequency unknown

- Increased risk of non-infection arterial duct, when furosemide is administered preterm infants during first weeks of life only parenteral dosage form).

General disorders and disorders at the site of administration

Rarely

- Fever

Since some reactions (such as change blood paintings, heavy anaphylactic or anaphylactoid reactions, severe allergic skin reaction) under certain conditions can threaten life patients, then when any side effects must be reported immediately about them to the doctor.

Overdose:

If you suspect an overdose it is necessary to turn to The doctor, since in case of an overdose may require certain curative activities.

The clinical picture is acute or chronic overdose The drug depends mainly on the extent and consequences of fluid loss and electrolytes.

Overdose may manifest as hypovolemia, dehydration, hemoconcentration, heart rhythm disturbances and conduction (including atrioventricular blockade and ventricular fibrillation).

Symptoms of these disorders are expressed lowering blood pressure, progressing until the development of shock, acute renal failure, thrombosis, delirious condition, flaccid paralysis, apathy and confusion.

There is no specific antidote. If after the intake of a little time has passed, then to reduce the absorption of furosemide from the gastrointestinal The tract should be tried to induce vomiting or gastric lavage, and then take inside the activated angle.

Treatment is aimed at correction clinically significant violations of water-electrolyte balance and acid-base state of under control content electrolytes in the blood serum, acid-base state, hematocrit, as well as, on prevention or therapy of possible serious complications developing against the background of these disorders.

Interaction:

Not recommended combinations

- Chloral hydrate - an intravenous infusion of furosemide in a 24-hour period after the application of chloral hydrate can lead to hyperemia of the skin, excessive sweating, anxiety, nausea, increased blood pressure and tachycardia. Therefore, the use of furosemide with chloral hydrate is not recommended.

- Aminoglycosides - delayed excretion of aminoglycosides by the kidneys when they are used simultaneously with furosemide and an increased risk of development of ototoxic and nephrotoxic action of aminoglycosides. For this reason, use of this combination of drugs should be avoided,when it is necessary for the vital indications, and in this case correction (decrease) is required. supporting doses aminoglycosides.

Combinations where caution should be exercised

- Ototoxic drugs - furosemide potentiates their ototoxicity. Such drugs can be used concomitantly with Lasix only on strict medical indications, since joint application can lead to irreversible damage to the hearing organ

- Cisplatinum - at simultaneous application with the drug Lasix has a risk of development of ototoxic effect. In addition, it is possible enlargement nefrotoksicheskogo action of cisplatin in the application of furosemide for the conduct of forced diuresis in time of cisplatin treatment, if furosemide not applicable in low doses (for example, 40 mg in patients with normal renal function) and in combination with appropriate hydration of the patient.

- Inhibitors angiotensin converting enzyme (ACE) and angiotensin II receptor antagonists - administration of an ACE inhibitor or an angiotensin II receptor antagonist in patients previously treated with furosemide may result to excessive reduce arterial pressures from worsening kidney function, and in some cases - the development of acute renal failure, so three days before the start of treatment or increase the dose of ACE inhibitors or antagonists receptors angiotensin II is recommended to abolish furosemide, or reduction of its dose.

- Lithium salts - under the influence of furosemide, lithium removal decreases, which increases the lithium content in serum, which increases the risk of its toxic effect, including its damaging effects on the heart and nervous system. Therefore, when this combination is used, monitoring of lithium content in serum is required.

- Risperidia - caution should be exercised, carefully weighing the risk-benefit ratio, before using risperidone with furosemide or other potent diuretics because there was an increased mortality in elderly patients with dementia who were simultaneously treated with risperidone and furosemide.

Interactions that should be taken into account

- Cardiac glycosides, drugs that cause lengthening of the interval QT - in the case of development of furosemide disorders of water electrolyte balance (hypokalemia or hypomagnesemia), the toxic effect of cardiac glycosides and agents,causing an elongation interval QT (the risk of heart rhythm disturbances increases).

- Glucocorticosteroids, carbenoxolone, licorice preparations in large quantities and prolonged use of laxatives when combined with furosemide increase the risk of hypokalemia.

- Medicines with nephrotoxic action - when combined with furosemide, the risk of developing them nephrotoxic action.

- High doses of some cephalosporins (excreted mainly by the kidneys) - in combination with furosemide increase the risk of nephrotoxic effect of cephalosporins.

- Non-steroidal anti-inflammatory drugs (NSAIDs) - NSAIDs, including acetylsalicylic acid, can reduce the diuretic effect of furosemide. In patients with hypovolemia and dehydration (including those taking furosemide), NSAIDs can cause the development of acute renal failure. Furosemide can increase the toxicity of salicylates.

- Phenytoin - reduction of diuretic action of furosemide.

- Hypotensive drugs, diuretics or other drugs that can reduce arterial pressure - when combined with furosemide, a more pronounced decrease in blood pressure is possible.

- Probenecid, methotrexate or other drugs that, like furosemide, excreted in the renal tubules, can reduce the effects of furosemide (the same pathway of renal excretion); on the other hand furosemide can lead to a decrease in the excretion of these drugs by the kidneys. All this increases the risk of side effects as a drug Lasix, and taken simultaneously with the above medicines.

- Hypoglycemic agents, both for oral administration, and insulin preparations), pressor amines (epinephrine, norepinephrine) - weakening effects when combined with furosemide.

- Theophylline, diazoxide, curare-like muscle relaxants, enhancing effects when combined with furosemide.

- Sucralfate - decrease in absorption of furosemide with joint ingestion and weakening of its effect (furosemide ingestion and sucralfate should be taken at intervals of not less than two hours).

- Cyclosporin A - when combined with furosemide, the risk of gouty arthritis increases due to hyperuricemia caused by furosemide, and impaired excretion of urate by the kidneys under the influence of cyclosporine.

- Radiopaque substances - in patients with a high risk of developing nephropathy for the introduction of radiopaque substances, who received furosemide, a higher incidence of abnormalities was observed kidney function compared to patients at high risk development of nephropathy in introduction of radiopaque drugs, which before introduction of radiocontrast only intravenous administration fluid (hydration).

Special instructions:

Before starting treatment with the drug Lasix® should exclude the presence of pronounced violations outflow of urine, including one-sided. Patients with a partial disturbance of the outflow of urine need careful observation, especially at the beginning treatment with Lasix®. During treatment with the drug Lasix is required regular content control sodium, potassium and concentration serum creatinine; especially close monitoring should be performed in patients with high risk of development violations of water-electrolyte balance in cases of additional losses of liquid and electrolytes (for example, due to vomiting, diarrhea or intense sweating).

Before and during treatment with Lasix, monitor and, in case of occurrence, eliminate hypovolemia or dehydration, as well as clinically relevant disorders water-electrolyte balance and / or acid-base state, for what can a short-term cessation of treatment with Lasix is required.

When treating with Lasix® it is always advisable to eat foods rich in potassium (lean meat, potatoes, bananas, tomatoes, cauliflower, spinach, dried fruits, etc.). In some cases, the use of drugs may be indicated potassium or admission potassium-saving preparations.

In patients with hypoproteinemia, for example, related to nephrotic syndrome (possibly weakening effectiveness of furosemide and increase its ototoxicity).

A cautious dose increase is required.

There was a large frequency deaths in elderly patients with dementia, concomitantly treated with risperidone and furosemide, compared with patients, received or only furosemide, or only risperidone. The pharmacophysiological mechanism of this effect is not established. Simultaneous application risperidone with other diuretics (mainly low doses of thiazide diuretics) was not associated with an increase in mortality in elderly patients with dementia. In elderly patients with dementia, follow with caution, carefully weighing the ratio of use and risk, apply furosemide and risperidone simultaneously. As dehydration is a common increased risk factor mortality, when making a decision on the application of this combination of elderly patients with dementia should avoid dehydration of the patient.

There is a possibility of weighting the course or exacerbation of the systemic of lupus erythematosus.

Selection of the dosing regimen patients with ascites against cirrhosis liver should be carried out in hospital (violations of water-electrolyte balance can entail the development of hepatic coma).

Effect on the ability to drive transp. cf. and fur:

Some side effects (for example, a significant decrease blood pressure) can disrupt concentration and reduce psychomotor reactions that can be dangerous in running by truck or at lessons other potentially hazardous activities. Especially this refers to the period of treatment initiation or increasing the dose of the drug, and also to cases of simultaneous taking antihypertensive drugs or alcohol. In such cases it is not recommended drive vehicles or engage in potentially dangerous activities.

Form release / dosage:

Tablets of 40 mg.

Packaging:

10 tablets per strip of aluminum foil. On 5 strips in a cardboard pack together with the instruction on medical application.

15 tablets per strip of aluminum foil. For 3 strips in a cardboard box, along with instructions for medical use.

Storage conditions:

Store at a temperature of no higher than 30 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014865 / 01

Date of registration:01.11.2008

The owner of the registration certificate:Sanofi India LimitedSanofi India Limited India

Manufacturer: & nbsp

SANOFI INDIA, Limited India

Information update date: & nbsp16.11.2015

Illustrated instructions

Instructions

Lasix® (Lasix®)