Spironolactone
Spironolactone is a potassium-sparing diuretic. Spironolactone is a synthetic 17-spirolactone steroid that is competititive antagonist of aldosterone. Spironolactone is used as an antihypertensive agent. It frequently is used to treat ascites associated with cirrhosis and also has been used as a diagnostic aid for primary hyperaldosteronism. Spironolactone is a poor agent for treating hypertension or generalized edema, although its effects can be additive with thiazide diuretics. It was approved by the FDA in 1960.
Primary Characteristics
It is of Synthetic origin and belongs to Steroid.
It belongs to Aldosterone antagonist pharmacological group on the basis of mechanism of action and also classified in Diuretic Potassium Sparing pharmacological group.
Molecular Weight: 416.1 · pKa: not relevant · Solubility in Water: Insoluble · Solubility in Alcohol: 1 in 80 · Non-proprietary name: Spironolactone.
Pharmacokinetics
Absorption: Spironolactone has an oral bioavailability is 103%.
Distribution: Spironolactone has a plasma protein binding is 98 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 1.3 +/- 0.3 hr.
Advertisement
Indications
Spironolactone is primarily indicated in conditions like All forms of epilepsy, Congestive heart failure, Electrolyte disorder, For prophylaxis in pregnancy, Hirsutism, Hyperaldoesteronism, Hypertension, Myoclonus, Nephrotic syndrome, Oedema, Oedema and ascites in cirrhosis of the liver, Parkinson's disease; drug-induced extrapyramidal symptoms, Primary hyperaldosteronism, Tobacco amblyopia and leber's optic atrophy.
Contraindications
Spironolactone is contraindicated in conditions like Renal failure, Hyperkalaemia.
Dosage
Spironolactone's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 75 mg | 75 mg | Every 24h | PO | |
| Paediatric Dosage (20kg) | ||||
| 1.25 mg/kg | 1.25 mg/kg | Every 12h | Oral | - |
| Neonatal Dosage (3kg) | ||||
| 1.25 mg/kg | 1.25 mg/kg | Every 12h | Oral | - |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Spironolactone in overdosage may give rise to further complications which include Gynacomastia , Impotence , Loss of libido , Menstrual irregularities .
Spironolactone produces potentially life-threatening effects which include Agranulocytosis, Eosinophilia , Peptic ulceration, Hematemesis. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Spironolactone are Diarrhea, Drowsiness, Dizziness, Mental confusion.
Spironolactone is known to cause more or less tolerable side effects which are usually transient. These include Ataxia, Drowsiness, Headache, Mental confusion.
Warnings / Precautions
Interference in Pathology
Spironolactone may interfere in the diagnosis of Fluorometric Test for measuring Plsasma Cortisol & Corticosteroids , Immunoassay for Serum Digoxin Levels , Zimmerman reaction for 17-Ketosteroids and 17-Ketogenic Steroids , Porter-Silber Reaction for Urinary 17-OH-Corticosteroids .
Available Brands
Storage Conditions
Drug Classification
- 1.16.3 — Potassium sparing diuretics