Clinical and pharmacological group: & nbsp
Diuretics
Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
Minimal chemist's assortment
АТХ:C.03.D.A Aldosterone antagonists
C.03.D.A.01 Spironolactone
Pharmacodynamics:Competitive antagonist of deoxycorticosterone and aldosterone in the cortical section of the collecting tubules and in the final segment of the distal tubules. For the manifestation of antagonism, a greater concentration of spironolactone than aldosterone is required in 2-10 thousand times. Competing with aldosterone for binding sites on cytoplasmic mineralocorticoid receptors. Inhibits aldosterone-regulated exchange of sodium ions on potassium ions in collecting tubes and distal tubules.It inhibits reabsorption of sodium ions through the apical membrane of renal epithelial cells due to inhibition of sodium channel synthesis ENaC. Increases urinary excretion of sodium, chlorine and water ions, reduces secretion and excretion of potassium (potassium-sparing effect), magnesium, urea and increases their concentration in the blood. Reduces the titratable acidity of urine. Has a moderate long-lasting diuretic effect and a weak antihypertensive effect. The diuretic effect after taking multiple doses is shown on the 2nd-5th day and persists for 2-3 days after discontinuation.
Pharmacokinetics:Pharmacokinetics
After oral administration, up to 99% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 2-4 hours. The connection with plasma proteins is 90%.
The therapeutic effect develops 2-5 days after the beginning of the admission and lasts for several days. Metabolism in the liver. One of the metabolites - canrenone (50% in the proportion of all metabolites) exhibits antialdosterone action.
The half-life is 13-24 hours. Elimination is mostly kidney and feces.
Indications:Used for swelling associated with excessive production of mineralocorticoids (including II and III trimesters of pregnancy), with hypertonic disease and in combination with diuretics that cause hypokalemia, to correct the mineral balance in the body.
IV.E20-E35.E26 Hyperaldosteronism
IV.E70-E90.E87.6 Hypokalemia
XI.K70-K77.K74 Fibrosis and cirrhosis of the liver
IX.I10-I15.I10 Essential [primary] hypertension
IX.I10-I15.I15 Secondary Hypertension
XVIII.R50-R69.R60 Edema, not elsewhere classified
IX.I30-I52.I50.0 Congestive heart failure
Contraindications:Addison's disease, hyponatremia, hyperkalemia, anuria, severe renal failure.
Individual intolerance.
Carefully:Atrioventricular blockade, cirrhosis, dysmenorrhea, advanced age.
Pregnancy and lactation:Recommendations for FDA - Category C. Used in II and III trimesters of pregnancy, is contraindicated in I trimester of pregnancy and during lactation - penetrates into breast milk.
Dosing and Administration:Use in children
Newborns, by mouth: 1-2 mg / kg / day in 1-2 divided doses;
1 month - 12 years: 1-3 mg / kg / day in 1-2 doses, up to 9 mg / kg / day in the resistant form of ascites;
12-18 years old: 50-100 mg / kg / day in 1-2 divided doses, the maximum daily dose is 400 mg.
Adults
Inside 50-100 mg / day, with edematic syndrome up to 300 mg / day in 1-2 divided doses. Correction of the dose is based on the content of potassium ions in the blood plasma.
The highest daily dose: 400 mg.
The highest single dose: 150 mg.
Side effects:Central and peripheral nervous system: drowsiness, dizziness, inhibition, ataxia.
The system of hematopoiesis: agranulocytosis, thrombocytopenia, megaloblastosis.
Cardiovascular system: hyperkalemia.
Digestive system: nausea, diarrhea, vomiting.
Musculoskeletal system: muscle spasms.
Reproductive system: decreased potency, gynecomastia, menstrual cycle disorders.
Allergic reactions.
Overdose:Hyperkalemia, drowsiness, confusion.
Treatment is symptomatic.
Interaction:Reduces the effects of anticoagulants with simultaneous application.
Increased risk of hyperkalemia with simultaneous use with ACE inhibitors, potassium-containing drugs, cyclosporine.
Acetylsalicylic acid reduces the secretion of sodium and canrenone, weakens the diuretic effect.
Increases the risk of toxic effects of lithium and digoxin.
Special instructions:Monitoring the content of potassium ions in blood plasma.
When treating spironolactone, alcohol and potassium-rich foods should be excluded from the ration: dried apricots, potatoes, raisins, tomato juice.
It is not recommended to take the drug to people whose profession requires concentration.