Product Name: Spironolactone
Common Brand Names: Aldactone
Pharmaceutical Category: Cardio / Blood Pressure / Cholesterol
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There is an additional general information about this medication active ingredient spironolactone:
Spironolactone 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.
After oral administration Spironolactone absorbed from the gastrointestinal tract, the absorption is 90%. This drug metabolized in the liver, the major active metabolite is canrenone. T1/2 is 13-24 hours. This medicine derived primarily by the kidneys, some is excreted in the bile.
Why is Spironolactone 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 (rare - 300 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.
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.
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 spironolactone.
Using during pregnancy and breastfeeding
There is no data on adverse effects of Spironolactone 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 spironolactone) excretes.
Category of the fetus by FDA - C.
Use 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 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 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.
Spironolactone drug interactions
When this drug applied simultaneously with:
- antihypertensive drugs potentiated the hypotensive effect of 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 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.
- 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.
Spironolactone 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 Spironolactone.