What is the mechanism of action of spironolactone?
Mechanism of action: Aldactone (spironolactone) is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule.
How does spironolactone come?
It comes as an oral tablet and an oral suspension. Spironolactone oral tablet is available as the brand-name drug Aldactone and as a generic drug.
What is the pharmacokinetics of spironolactone?
12.3 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. Effect of food: Food increased the bioavailability of spironolactone (as measured by AUC) by approximately 95.4%.
What is the main ingredient in spironolactone?
Spironolactone oral tablets contain 25 mg, 50 mg, or 100 mg of the aldosterone antagonist spironolactone, 17‑ hydroxy-7α-mercapto-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone acetate, which Spironolactone is practically insoluble in water, soluble in alcohol, and freely soluble in benzene and in chloroform.
Does spironolactone inhibit 5 alpha reductase?
Spironolactone inhibits 5-alpha reductase weakly. Unfortunately, finasteride does not reduce sebum production and is not effective in the treatment of acne.
How is aldosterone activated?
The release of aldosterone from the adrenal glands is regulated via the renin-angiotensin II-aldosterone system. This system is initially activated via a decrease in the mean arterial blood pressure to increase the blood pressure.
Which is a aldosterone blocking agent?
Aldosterone antagonists are diuretics or “water pills.” They may also be called aldosterone receptor blockers. Aldosterone antagonists include: Eplerenone (Inspra) Spirinolactone (Aldactone)
Is spironolactone a prodrug?
Spironolactone has a very short biological half-life and is considered to be a prodrug; hence, its active metabolites are responsible for most of its pharmacodynamics.
Where is spironolactone metabolized?
Spironolactone
| Clinical data | |
|---|---|
| Metabolism | Liver, others: • Deacetylation via CES • S-Oxygenation via FOM • S-Methylation via TMT • Dethioacetylation • Hydroxylation via CYP3A4 • Lactone hydrolysis via PON3) |
| Metabolites | 7α-TS , 7α-TMS , 6β-OH-7α-TMS , canrenone, others (All three active) |
What type of diuretic is spironolactone?
Spironolactone is a potassium-sparing diuretic (water pill). It prevents your body from absorbing too much salt and keeps your potassium levels from getting too low. This medicine is also used to treat or prevent hypokalemia (low potassium levels in the blood).
How does spironolactone inhibit androgen?
It works by binding to the AR and displacing androgens like testosterone and DHT from the receptor, thereby reducing its activation by these hormones.
What does 5 alpha reductase do?
The SRD5A2 gene provides instructions for making an enzyme called steroid 5-alpha reductase 2. This enzyme is involved in processing androgens, which are hormones that direct male sexual development. Specifically, the enzyme is responsible for a chemical reaction that converts the hormone testosterone to DHT.
How is aldosterone synthesized?
Active steroids are produced by conversion of cholesterol to pregnenolone then to progesterone in the pathway. The synthesis of aldosterone then involves the activities of three cytochrome P450 enzymes in the mitochondria and endoplasmic reticulum in cells of the outer, zona glomerulosa, of the adrenal glands.
What stimulates aldosterone production?
The major factors stimulating aldosterone production and release by the zona glomerulosa are angiotensin II and the serum potassium concentration.
How does spironolactone increase aldosterone?
Spironolactone, an aldosterone receptor antagonist, can raise plasma renin levels. K-wasting diuretics (Non-K-sparing diuretics, such as thiazides, induce renal potassium losses and reduce plasma potassium concentrations, leading to decreased aldosterone secretion.)
Which is active metabolite of spironolactone?
Canrenone-the principal active metabolite of spironolactone? – PMC.
Is spironolactone a mineralocorticoid?
Spironolactone and eplerenone are both mineralocorticoid-receptor antagonists. These compounds block both the epithelial and nonepithelial actions of aldosterone, with the latter assuming increasing clinical relevance.
Is spironolactone potassium-sparing?
Does spironolactone have active metabolites?
Spironolactone reaches a maximum concentration in 2.6 hours and an active metabolite (canrenone) reaches a maximum concentration in 4.3 hours.