Lasilactona

Furosemide:

• Pharmacological action
• Pharmacokinetics
• Why is Lasilactona prescribed?
• Dosage and administration
• Lasilactona (Furosemide) side effects, adverse reactions
• Lasilactona contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Lasilactona drug interactions
• Lasilactona in case of emergency / overdose
• Lasilactona (Furosemide) reviews

Pharmacological action

Lasilactona is a loop diuretic. This medication violates the reabsorption of sodium and chlorine in the large segment of the ascending loop of Henle. Due to increasing separation of sodium ions occurs secondary (indirect osmotically bound water) increased excretion of water and increased secretion of potassium ions in the distal renal tubule. Simultaneously increased excretion of calcium and magnesium ions.

Lasilactona (Furosemide) has secondary effects caused by the release of neurotransmitters and intrarenal redistribution of intrarenal blood flow. On the background of a course of treatment does not occur the weakening effect.

When heart failure Lasilactona (Furosemide) quickly leads to a reduction of preload on the heart through the expansion of large veins. This drug exerts the hypotensive effect due to increased excretion of sodium chloride and reduction reactions of vascular smooth muscle to vasoconstrictor effects and by decreasing the BCC. Effect of Lasilactona (Furosemide) after IV injection occurs in 5-10 minutes; after oral administration within 30-60 minutes, a maximum of the action is after 1-2 hours, the duration of effect is 2-3 hours (if reduced kidney function - up to 8 hours).

Lasilactona (Furosemide) reduces the incidence of atrial natriuretic factor in the plasma, causing vasoconstriction.

Diuretic effect develops in 3-4 minutes after IV injection and lasts 1-2 h; after oral taking - 20-30 minutes, lasts up to 4 hours.

Pharmacokinetics

After oral administration absorption of Lasilactona (Furosemide) is 60-70%. In severe kidney disease or chronic heart failure, extent of absorption is reduced.

V_d is 0.1 L / kg. Binding to plasma proteins (mainly albumin) is 95-99%. Lasilactona (Furosemide) metabolized in the liver. Excreted by the kidneys is 88% with bile - 12%. T_1/2 in patients with normal renal function and liver is 0.5-1.5 h. When anuria T_1/2 can be increased up to 1.5-2.5 h, with concomitant renal and liver failure - up to 11-20 hours.

Why is Lasilactona prescribed?

Edematous syndrome of different genesis, including in chronic heart failure II-III stage, liver cirrhosis (portal hypertension syndrome), nephrotic syndrome. Pulmonary edema, cardiac asthma, cerebral edema, eclampsia, conducting forced diuresis, severe hypertension, some forms of hypertensive crisis, hypercalcemia.

Dosage and administration

Dosing regimen set individually, depending on the evidence, the clinical situation, the patient's age. The treatment dosing regimen is adjusted depending on the value of diuretic response and the dynamics of the patient.

When Lasilactona administered orally an initial dose for adults is 20-80 mg / day, further, if necessary, the dose gradually increased to 600 mg / day. For children a single dose is 1-2 mg / kg.

The maximum oral dose for children is 6 mg / kg.

For IV jet or IM administration the dose for adults is 20-40 mg 1 time / day, in some cases - 2 times / day. For children the starting daily dosage for parenteral use is 1 mg / kg.

Lasilactona (Furosemide) side effects, adverse reactions

Cardiovascular system: decreased blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decreased BCC.

CNS and peripheral nervous system: dizziness, headache, myasthenia gravis, calf muscle cramps (tetany), paresthesia, apathy, weakness, fatigue, lethargy, drowsiness, confusion.

Senses: blurred vision and hearing.

Digestive system: anorexia, dry mouth, thirst, nausea, vomiting, constipation or diarrhea, cholestatic jaundice, pancreatitis (acute).

Urogenital system: oliguria, acute urinary retention (in patients with prostatic hypertrophy), interstitial nephritis, hematuria, reduced potency.

Hemopoietic system: leucopenia, thrombocytopenia, agranulocytosis, aplastic anemia.

Water and electrolyte metabolism: hypovolemia, dehydration (the risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, chloropenia, hypocalcemia, hypomagnesemia, metabolic alkalosis.

Metabolism: hypovolemia, hypokalemia, hyponatremia, chloropenia, hypokalemic metabolic alkalosis (as a result of these violations - hypotension, dizziness, dry mouth, thirst, arrhythmias, muscle weakness, cramps), hyperuricemia (with the possible aggravation of gout), hyperglycemia.

Allergic reactions: purpura, urticaria, exfoliative dermatitis, erythema multiforme exudative, vasculitis, necrotizing vasculitis, pruritus, chills, fever, photosensitivity, anaphylactic shock.

Other: for optional IV injections - thrombophlebitis, renal calcinosis in preterm infants.

Lasilactona contraindications

Acute glomerulonephritis, stenosis of the urethra, obstruction of urinary tract stones, acute renal failure with anuria, hypokalemia, alkalosis, precomatose state, severe hepatic failure, hepatic coma and precoma, diabetic coma, hyperglycemic coma, hyperuricemia, gout, decompensated mitral or aortic stenosis, hypertrophic obstructive cardiomyopathy, increased central venous pressure (greater than 10 mm Hg), hypotension, acute myocardial infarction, pancreatitis, impaired water-electrolyte metabolism (hypovolemia, hyponatremia, hypokalemia, chloropenia, hypocalcemia, hypomagnesemia), digitalis toxicity, increased sensitivity to Lasilactona (Furosemide).

Using during pregnancy and breastfeeding

In pregnancy, the use of Lasilactona is only possible within a short time only, when the intended use of therapy to the mother justifies the potential risk to the fetus.

As Lasilactona (Furosemide) may be excreted in breast milk and to suppress lactation, if necessary use during lactation, a breastfeeding should be discontinued.

Category effects on the fetus by FDA - C.

Special instructions

With careful use Lasilactona (Furosemide) with prostatic hyperplasia, SLE, hypoproteinemia (risk of ototoxicity), diabetes (impaired glucose tolerance), stenosing atherosclerosis of cerebral arteries on the background of long-term therapy cardiac glycosides, elderly patients with severe atherosclerosis, pregnancy (especially first half), during lactation.

Before the treatment by Lasilactona (Furosemide) it should be compensated for electrolyte disturbances. During treatment with Lasilactona (Furosemide) it is necessary to control blood pressure, electrolytes and glucose in the blood serum, liver and kidney function.

For the prevention of hypokalemia there is expedient to combine Lasilactona (Furosemide) with potassium-sparing diuretics. With the simultaneous administration of Lasilactona (Furosemide) and hypoglycemic agents it may be require dose adjustment of the latter.

There is not recommended to mix a solution of Lasilactona (Furosemide) in the same syringe with any other drugs.

Lasilactona drug interactions

Aminoglycosides, ethacrynic acid and cisplatin increases ototoxicity of this medication (especially when impaired renal function). Lasilactona (Furosemide) increases the danger of kidney damage with amphotericin B. if prescribed high doses of salicylates increases the risk of salicylism (competitive renal excretion), cardiac glycosides - hypokalemia and related arrhythmias, corticosteroids - an electrolyte imbalance. Lasilactona (Furosemide) reduces muscle relaxant activity of tubocurarine, potentiates the effect of succinylcholine. This drug reduces the renal clearance (and increases the likelihood of intoxication) lithium. Under the influence of Lasilactona (Furosemide) increases the effect of ACE inhibitors and antihypertensive agents, warfarin, diazoxide, theophylline, attenuated - antidiabetic drugs, norepinephrine. Sucralfate and indomethacin (by inhibiting the synthesis of PG, the level of violations of plasma renin and aldosterone excretion) reduce the effectiveness of Lasilactona (Furosemide) Atlantic Laboratories. Probenecid increases the concentration of this medicine in serum (blocking excretion).

Lasilactona in case of emergency / overdose

Symptoms: hypovolemia, dehydration, haemoconcentration expressed hypotension, reduction of BCC, collapse, shock, cardiac arrhythmias and conduction (including AV block, ventricular fibrillation), acute renal failure with anuria, thrombosis, thromboembolism, drowsiness, confusion, flaccid paralysis, apathy.

Treatment: correction of water and electrolyte balance and acid-base balance, supplementation of BCC, symptomatic therapy, the maintenance of vital functions. The specific antidote is unknown.

Spironolactone:

• Pharmacological action
• Pharmacokinetics
• Why is Lasilactona prescribed?
• Dosage and administration
• Lasilactona (Spironolactone) side effects, adverse reactions
• Lasilactona contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Lasilactona drug interactions
• Lasilactona in case of emergency / overdose
• Lasilactona (Spironolactone) reviews

Pharmacological action

Lasilactona is a potassium, magnesium sparing diuretic. This medication is a competitive antagonist of aldosterone on the effect on distal nephron (competes for binding sites on cytoplasmic protein receptors, reduces the synthesis of permeases in the aldosterone-sensitive part of collecting tubules and distal tubules), increases the excretion of Na+, Cl- and water and reduces the excretion of K+ and urea, reduces the titratable acidity of urine. Increased diuresis causes a hypotensive effect, which is unstable. The hypotensive effect is not dependent on the level of renin in the blood plasma and is not revealed in normal blood pressure.

The diuretic effect is seen at 2-5 days of treatment.

Pharmacokinetics

After oral administration Lasilactona (Spironolactone) absorbed from the gastrointestinal tract, the absorption is 90%. This drug metabolized in the liver, the major active metabolite is canrenone. T_1/2 is 13-24 hours. This medicine derived primarily by the kidneys, some is excreted in the bile.

Why is Lasilactona prescribed?

Edema in congestive heart failure, cirrhosis of the liver (especially in the simultaneous presence of hypokalemia and hyperaldosteronism), in the nephrotic syndrome.

Swelling in the II and III trimester of pregnancy.

Hypertension, including with aldosterone producing adrenal adenoma (in combination therapy).

Primary hyperaldosteronism. Aldosterone produced adrenal adenoma (long-term maintenance therapy with contraindications to surgery or in case of refusal from it). Diagnosis of hyperaldosteronism.

Hypokalemia and its prevention in the treatment of saluretics.

Polycystic ovary syndrome, premenstrual syndrome.

Dosage and administration

The dosage regimen is set individually depending on the severity of violations of water-electrolyte metabolism and hormonal status.

In cases of edema - 100-200 mg / day in 2-3 recepts (usually in combination with the "loop" and / or thiazide diuretic) daily for 14-21 days. The correction of dose should be based on the values of potassium in the plasma. If necessary, repeat it every 10-14 days. In marked hyperaldosteronism and a reduced content of plasma potassium - 300 mg in 2-3 recepts.

Lasilactona (Spironolactone) side effects, adverse reactions

Digestive system: nausea, vomiting, abdominal pain, gastritis, ulcers and bleeding in the gastrointestinal tract, intestinal colic, diarrhea or constipation.

CNS: dizziness, drowsiness, lethargy, headache, lethargy, ataxia.

Metabolism: increased concentrations of urea, hypercreatininemia, hyperuricemia, impaired water-salt metabolism and KSCHR (metabolic acidosis or hypochloremic alkalosis).

Hematopoietic system: megaloblastosis, agranulocytosis, thrombocytopenia.

Endocrine system: in long-term use - gynecomastia, erectile dysfunction in men; women - dysmenorrhea, amenorrhea, metrorrhagia, menopause, hirsutism, deepening voice, breast tenderness, breast carcinoma.

Allergic reactions: urticaria, papular makulopapular and erythematous rash, drug fever, pruritus.

Other: muscle cramps, reduced potency.

Lasilactona contraindications

Addison's disease, hyperkalemia, hypercalcemia, hyponatremia, chronic renal failure, anuria, hepatic failure, diabetes mellitus with confirmed or suspected renal disease, diabetic nephropathy, I trimester of pregnancy, metabolic acidosis, menstrual disorders or breast enlargement, hypersensitivity to Lasilactona (Spironolactone).

Using during pregnancy and breastfeeding

There is no data on adverse effects of Lasilactona on pregnancy and fetal development.

However, in the I trimester of pregnancy this medication is contraindicated, in II and III trimester can be used for prescription. If necessary to use during lactation it should be considered that with breast milk in small amounts canrenone (metabolite of Lasilactona (Spironolactone)) excretes.

Category of the fetus by FDA - C.

Special instructions

Use Lasilactona (Spironolactone) cautiously in AV block (the possibility of strengthening due to the development of hyperkalemia), decompensated cirrhosis, surgery, taking drugs that cause gynecomastia, while taking local and general anesthetics in elderly patients.

Against the background of Lasilactona (Spironolactone) it should not be given medications containing potassium and other diuretics that cause potassium retention in the body. Patients should avoid using this drug with carbenoxolone, causing sodium retention.

In the period of treatment should be periodic determination of electrolytes and urea in the blood.

If taking of Lasilactona (Spironolactone) in combination with other diuretics or antihypertensive the dose of latters is recommended to be reduced.

In the application of this medicatio in conjunction with digoxin it may be necessary to reduce both the saturation and maintenance dose of the latter.

Lasilactona drug interactions

When this drug applied simultaneously with:

- antihypertensive drugs potentiated the hypotensive effect of Lasilactona (Spironolactone).

- ACE inhibitors may develop hyperkalemia (especially in patients with impaired renal function), as ACE inhibitors reduce the content of aldosterone, resulting in a delay of potassium in the body against the removal of potassium restriction.

- preparations of potassium and other potassium-sparing diuretics, salt substitutes and food supplements containing potassium may develop hyperkalemia.

- salicylates decreases the diuretic effect of Lasilactona (Spironolactone) due to blockade of canrenone excretion by the kidneys.

- decreases hypoprothrombinemic effect of oral anticoagulants.

- digitoxin may gain as well as reducing the effects of digitoxin.

- Lasilactona (Spironolactone) inhibits the excretion of digoxin by the kidneys, and probably reduce its volume of distribution. This may cause an increased concentration of digoxin in plasma.

- candesartan, losartan, eprosartan is a risk of hyperkalemia.

- cholestyramine it been described a case of hypochloremic alkalosis.

- lithium carbonate may increase the concentration of lithium in blood plasma.

- norepinephrine may decrease the sensitivity of vessels to noradrenaline.

- amplified effect triptorelin, buserelin, gonadorelin. Indomethacin and mefenamic acid inhibit the excretion of canrenone by kidneys.

Lasilactona in case of emergency / overdose

Symptoms: nausea, vomiting, drowsiness, dizziness, confusion, leg cramps, skin rash, diarrhea, dehydration may, disruption of water and electrolyte balance.

Treatment: discontinuation of the drug, induction of vomiting, gastric lavage, symptomatic treatment of dehydration and disorders of water and electrolyte balance, arterial hypotension, maintenance of vital functions; in the case of hyperkalemia - fast IV injection of 20-50% solution of glucose and insulin - 0.25-0.5 units / g of glucose. Used diuretics, and potassium carve ion exchange resins. Perhaps hemodialysis. There is no specific antidote for Lasilactona (Spironolactone) Quality Pharmaceutical Laboratory.