Spironolactone

When ATH:
C03DA01

Characteristic.

Kaliйsberegaющiй diuretic, competitive antagonist of aldosterone. The white crystalline powder. Practically insoluble in water, soluble in ethyl alcohol, easy insoluble in benzene and chloroform. Molecular weight - 416,57.

Pharmacological action.
Diuretic, Kalisberegate, antihypertensive.

Application.

Edema syndrome in patients with chronic heart failure, cirrhosis (particularly in the simultaneous presence of hypokalemia and hyperaldosteronism), nephrotic syndrome; essential hypertension in adults; ascites; diagnosis and treatment of primary hyperaldosteronism (Horse Syndrome); prevention of hypokalemia in the treatment of patients and saluretikami, receiving cardiac glycosides, myasthenia (adjuvant).

Contraindications.

Hypersensitivity, Addison's disease, acute or rapidly progressive renal failure, chronic renal failure with a significant decrease in the excretory function (Cl creatinine less than 10 ml / min), anurija, hyperkalemia, giponatriemiya, hypercalcemia.

Restrictions apply.

Reduced renal excretory function, abnormal liver function (increased sensitivity to changes in electrolyte balance), diabetes (especially diabeticheskaya nephropathy), predisposition to metabolic acidosis (when the effect of acidosis enhanced giperkaliemichesky spironolactone, spironolactone may contribute to the development of acidosis), menstrual irregularities and / or breast enlargement, OF блокада (may be increased due to the development of hyperkalemia).

Pregnancy and breast-feeding.

The use of spironolactone is contraindicated in the I trimester of pregnancy. In II and III trimester of pregnancy is possible only under strict conditions, if the effect of therapy outweighs the potential risk to the fetus.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding (canrenone - the active metabolite of spironolactone - passes into breast milk).

Side effects.

From the nervous system and sensory organs: dizziness, drowsiness, lethargy, slackness, headache, ataxia, confusion.

From the digestive tract: nausea, vomiting, diarrhea, spasms, kišečnaâ how, gastritis, ulceration and bleeding in the digestive tract, abnormal liver function.

With the genitourinary system: gynecomastia (usually reversible, in rare cases can persist after the abolition PM), breast pain, erectile dysfunction in men, reduced potency in men, menstrual disorders or amenorrhea, metrorrhagia, menopause, girsutizm, change of voice in women.

For the skin: makulopapulârnye or erythematous skin rashes, alopecia, hypertryhoz, itch, hives.

Other: leg cramps, benign Neoplasms of the breast, chest pain, leukopenia (incl. agranulocytosis), thrombocytopenia, electrolyte imbalance, hyperkalemia, increase in the blood urea nitrogen, creatinine, osteomalacia, drug fever.

Reported cases of breast cancer in men and women, treated with spironolactone, however, a causal relationship has not been established.

Cooperation.

The simultaneous use of indomethacin, ACE inhibitors, potassium supplements leads to the development of hyperkalemia. In order to avoid hyperkalemia not take spironolactone or amiloride together with triamterene. In simultaneous reception with carbenoxolone reduced therapeutic effect of spironolactone, tk. carbenoxolone causes sodium retention. Spironolactone reduces the vascular sensitivity to norepinephrine, that must be taken into account in general and local anesthesia in patients, treated with spironolactone. Aspirin reduces the diuretic effect of spironolactone. Spironolactone potentiates the effect of diuretics and antihypertensive drugs (together with the use of hypotensive dose of the past should be reduced by 50%), reduces the effect of anti indirect action (coumarin derivatives). Increases T_1/2, plasma levels of Digoxin toxicity (in their joint admission to be reduced dose or increase the interval between doses of Digoxin). The combination of spironolactone with triptorelin, buserelin, gonadorelin reinforces their effects.

Overdose.

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

Treatment: discontinuation of the drug, induction of vomiting, gastric lavage, symptomatic treatment of dehydration and disorders of fluid and electrolyte balance, hypotension, maintaining vital functions; in the case of hyperkalemia - a quick in / in a 20-50% solution of glucose and insulin - 0.25-0.5 units / g of glucose. Kaliyvyvodyaschie used diuretics and ion exchange resins. Perhaps hemodialysis. No specific antidote.

Dosing and Administration.

Inside. The mode set individually. Typical adult doses: 25-200 mg / day in single or divided doses; if necessary, increase the dose to 400 mg / day. Babies are usually given at the rate of 3 mg / kg / day, mono- or 2 admission, Dose selected individually.

Precautions.

Be wary appoint surgery on the background of local and general anesthetics, elderly patients (increased risk of hyperkalemia). There should be appointed spironolactone in conjunction with PM, causing gynecomastia. At doses above 100 mg / day often develop endocrine / anti-androgenic effects, manifest effect on the central nervous system and irritation of the gastrointestinal mucosa. During therapy should be carefully monitored electrolytes, the level of urea nitrogen, urea and creatinine in the blood (especially in elderly patients with impaired renal function and / or liver), regularly monitor the performance of BP. With the development of hyperkalemia should stop taking spironolactone. Avoid intake of excessive amounts of potassium, incl. exclude or limit food, rich in potassium (potatoes, apricots, raisins, tomato juice, etc.), and PM, containing potassium. In the treatment with spironolactone should avoid drinking. At the beginning of treatment with spironolactone drivers of vehicles and people, skills relate to the high concentration of attention, It should not be applied during work. When conducting tolerance test glucose tolerance in patients with diabetic nephropathy spironolactone should be abolished, at least, for 3 days before the test (due to the risk of severe hyperkalemia).

Cooperation