Product Information
Registration Status: ActiveINSPRA TABLET 50MG is approved to be sold in Singapore with effective from 2005-02-17. It is marketed by PFIZER PTE LTD, with the registration number of SIN13049P.
This product contains Eplerenone 50mg in the form of TABLET,-COATED. It is approved for ORAL use.
This product is manufactured by Pfizer Pharmaceuticals LLC
Pfizer Pharmaceuticals LLC Vega Baja in PUERTO RICO.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.
Indication
For improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.
Mechanism of Action
Eplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.
Pharmacokinetics
- Absorption
- The absolute bioavailability of eplerenone is unknown.
- Distribution
- * 43 to 90 L
- Metabolism
- Eplerenone is metabolized primarily by CYP3A4, however, no active metabolites have been identified in human plasma.
- Elimination
Clearance
* Apparent plasma cl=10 L/hr
Toxicity
The most likely symptoms of human overdosage would be anticipated to be hypotension or hyperkalemia. However, no cases of human overdosage with eplerenone have been reported.
Active Ingredient/Synonyms
Epoxymexrenone | Eplerenone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.