Spiroshin
Spironolactone
Indication
Spironolactone is used in the treatment of heart failure, essential hypertension, edema associated with Hepatic Cirrhosis or Nephrotic Syndrome and Primary Hyper-aldosteronism.
Dosage and Administration
It should be taken with or without food.
Heart Failure:
Initially, 25 mg once daily. Patients who tolerate may have their dosage increased to 50 mg once daily as clinically indicated. Patients who develop hyperkalemia on 25 mg once daily may have their dosage reduced to 25 mg every other day.
Essential Hypertension:
The recommended initial daily dose is 25 to 100 mg in single or divided dose. Dosage can be titrated at two-week intervals.
Edema:
In patients with cirrhosis, initiate therapy in a hospital setting and titrate slowly. The recommended initial daily dosage is 100 mg of Spironolactone administered in either single or divided doses, but may range from 25 to 200 mg daily, When given as the sole agent for diuresis, administer for at ...
Primary Hyperaldosteronism:
Administer Spironolactone in doses of 100 to 400 mg daily in preparation for surgery. For patients who are considered unsuitable for surgery, Spironolactone can be used as long-term maintenance therapy at the lowest effective dosage determined for the individual patient.
Composition
Each film-coated tablet contains:
Spironolactone B.P ... 25 mg.
Description
Spironolactone, potassium sparing diuretic is 17-hydroxy- 7α-mercapto-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone acetate. Its molecular formula is C24H32O4S and molecular weight is 416.57.
Clinical Pharmacology
Spironolactone is an aldosterone receptor antagonist. It acts primarily through competitive binding of receptors at aldosterone-dependent sodium-potassium exchange channels in the distal convoluted renal tubule. Spironolactone causes increased amounts of sodium and water to be excreted, while potass...
Pharmacokinetics
The mean time to reach peak plasma concentration of spironolactone and the active metabolite, canrenone, in healthy volunteers is 2.6 and 4.3 hours, respectively. Food increased the bioavailability of spironolactone (as measured by AUC) by approximately 95.4%. Patients should establish a routine pat...
Contraindication
It is contraindicated in patients who have known hypersensitivity to spironolactone, hyperkalemia, Addison’s disease, acute renal insufficiency, significant renal compromise, anuria and concomitant use of eplerenone.
Precaution
Spironolactone should be used with caution in the elderly and/ or in patients with pre-existing impaired renal or hepatic function. Cautions is advised when driving or operating machinery until the response to initial treatment has been determined. Caution should be exercised in the management of pa...
Adverse Effects
Digestive: Gastric bleeding, ulceration, gastritis, nausea, vomiting, diarrhea and cramping.
Reproductive: Inability to achieve or maintain erection, irregular menses or amenorrhea, postmenopausal bleeding, breast and nipple pain.
Hematologic: Leukopenia (including agranulocytosis), thrombocytopenia.
Hypersensitivity: Fever, urticarial, maculopapular or erythematous cutaneous eruptions, anaphylactic reactions, vasculitis.
Metabolism: Hyperkalemia, electrolyte disturbances, hyponatremia, hypovolemia.
Musculoskeletal: Leg cramps.
Nervous system/ psychiatric: Changes in libido, confusion, lethargy, ataxia, dizziness, headache, drowsiness.
Renal: Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), drug rash with eosinophilia and systemic symptoms (DRESS), alopecia, pruritis.
Drug Interaction
Potassium containing drugs and Drugs known to cause hyperkalemia: Concomitant use of spironolactone with these drugs can increase potassium level and may lead to hyperkalemia. (Examples of drugs that can increase potassium include: ACEI, ARB, NSAIDs, trimethoprim, heparin and low molecular weight he...
Digoxin: Spironolactone may increase the half-life of digoxin. Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs may attenuate the natriuretic efficacy of diuretics due to inhibition of intra-renal synthesis of prostaglandins and have been shown to attenuate the diuretic effect of spironolacton...
Lithium: Spironolactone may reduce the renal clearance of lithium, thus increasing the risk of lithium toxicity. Monitor lithium levels periodically when concurrent administration.
Ammonium Chloride or Cholestyramine: Hyperkalemic metabolic acidosis has been reported in patients given spironolactone concurrently with ammonium chloride or cholestyramine.
Storage
Store below 30°C in cool and dry place. Protect from light and moisture. Keep out of reach and sight of children.
Presentation
10 x 10’s Blisters.