Spiros

Each tablet contains: Spironolactone USP.
Excipients q.s.

Pharmacology: Pharmacokinetics: Spironolactone is fairly rapidly absorbed from the gastrointestinal tract, the extent of absorption depending on particle size and formulation. Modern formulations are reported to provide bioavailability of about 90%. It is about 90% bound to plasma proteins. Spironolactone is metabolized extensively to a number of metabolites including canrenone and the sulfur-containing 7-thiomethyl spironolactone, both of which are pharmacologically active. The major metabolite may be 7-thiomethyl spironolactone, although it is uncertain to what extent the actions of spironolactone are dependent on the parent compound or its metabolites. Spironolactone is excreted mainly in the urine and also in feces, in the form of metabolites. Spironolactone or its metabolites may cross the placental barrier, and canrenone is distributed into breast milk.

For the management of heart failure, to treat refractory edema and in lower doses as an adjunct to standard therapy; For refractory edema-associated with cirrhosis of the liver or the nephrotic syndrome, and in ascites associated with malignancy; For the treatment of essential hypertension; For the diagnosis and treatment of primary aldosteronism.

Oedema: Initial dose of 100 mg daily by mouth, subsequently adjusted as necessary; some patients may require doses of up to 400 mg daily.
Hepatic cirrhosis with ascites and oedema: patients with a urinary sodium/potassium ratio greater than 1 may be given an initial dose of 100 mg daily; while patients with a ratio less than 1 may be given initial dose of 200 to 400 mg daily.
Hyperaldosteronism: 400 mg daily in the presumptive diagnosis of primary hyperaldosteronism; 100 to 400 mg daily for pre-operative management of hyperaldosteronism and in the lowest effective dosage for long term maintenance therapy in the absence of surgery.
Heart failure: In patients with severe heart failure, addition of spironolactone in a dose of 25 to 50 mg therapy with ACE Inhibitors and loop diuretics reduced the risk of death and hospitalization.
Hirsutism: 50 to 200 mg daily for idiopathic hirsutism or polycystic ovary syndrome preferably in combination with oral contraceptives.

Spironolactone is contraindicated in the following: Patients with anuria (patients are at greater risk of developing hyperkalemia).
Acute renal insufficiency, severe or rapidly progressing impairment of renal function (spironolactone may aggravate electrolyte imbalance and the risk of developing hyperkalemia is increased).
Hyperkalemia (spironolactone may further increase serum potassium concentrations).
Patients who are hypersensitive to spironolactone or any of the ingredients in the product.
Addison's disease.
Diabetes mellitus, especially in patients with confirmed or suspected renal insufficiency.
Diabetic nephropathy (increased risk of hyperkalemia. Spironolactone should be discontinued at least 3 days prior to a glucose tolerance test because of the risk of hyperkalemia).
Breast-feeding is contraindicated.

Patients receiving spironolactone therapy should be carefully evaluated for possible disturbances of fluid and electrolyte balance particularly in the elderly and in those with significant renal and hepatic impairment.
Hyperkalemia may occur in patients with impaired renal function or excessive potassium intake and can cause irregularities, which can be fatal. If hypernatremia occur, spironolactone should be discontinued, and if necessary, active measures taken to reduce the serum potassium levels to normal.
Reversibly increases in blood urea have been reported in association with spironolactone therapy, particularly in the presence of impaired renal function.
Reversible hyperchloremic metabolic acidosis, usually in association with hyperkalemia, has been reported to occur in some patients with decompensated cirrhosis even in the presence of normal renal function.
Caution should be taken in patients diagnosed with porphyria as Spironolactone is considered unsafe in these patients.
Care should be taken in patients suffering from menstrual abnormalities or breast enlargement.

Headache and drowsiness, gastrointestinal disturbances including cramps, and diarrhea; Ataxia, mental confusion and skin rashes; Gynecomastia (not uncommon) and in rare cases of breast enlargement may persist; Endocrine disorders including hirsutism, deepening of the voice, menstrual irregularities and impotence; transient increase in blood-urea-nitrogen concentrations may occur; mild acidosis; hyponatremia; Breast cancer, agranulocytosis, effects on electrolyte imbalance; increase serum-cholesterol concentrations; lichen-planus-like skin eruptions and chloasma-like pigmentation on the face.

ACE inhibitors decreases aldosterone production and they should not routinely be used with spironolactone, particularly in patients with marked renal impairment. Concomitant use of Spironolactone with ACE inhibitors may lead to severe hyperkalemia, particularly in patients with renal failure. Spironolactone may also have been an enhanced hypotensive effect when administered concomitantly with ACE inhibitors.
Anti-diabetics administration with chlorpropamide may increase risk of hyponatremia.
Co-administration of potassium sparring diuretics with ciclosporin may result in hyperkalemia. Avoid concurrent use of spironolactone and ciclosporin. If concurrent therapy is necessary monitor serum potassium levels.
Aspirin may reduce the diuretic effect of Spironolactone.
Sympathomimetics-Spironolactone reduces vascular responses to noradrenaline (norepinephrine); Caution should be exercised in management of individuals being subjected to regional or general anesthesia receiving therapy with spironolactone.
Estrogen: diuretic effect of Spironolactone antagonized by Estrogen.
Coumarins: in patients receiving oral anticoagulant therapy with warfarin, the prothrombin time ratio or INR (international normalized ratio) should be monitored with the addition and withdrawal of treatment with Spironolactone, and should be reassessed periodically during concurrent therapy. Adjustments of the warfarin dose may be necessary in order to maintain the desired level of anticoagulation.

Store at temperature not exceeding 30°, protected from light.

Diuretics

C03DA01 - spironolactone ; Belongs to the class of aldosterone antagonists. Used as potassium-sparing diuretics.

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