SPRANONE 25
-
Chemical Name:
Eplerenone -
Therapeutic Category:
Cardiovascular drugs -
Pharmacologic Category:
Selective Aldosterone Blocker -
Pharmaceutical Form:
Tablets -
Composition:
Eplerenone 25mg
SPRANONE
Film Coated Tablets
Eplerenone
1.PHARMACOLOGY:
Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, a component of the rennin-angiotensin-aldosterone-sytem (RAAS).
Eplerenone has been shown to produce sustained increases in rennin and aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on rennin secretion. Eplerenone selectively binds to mineralcorticoid receptors.
2.PHARMACOKINETICS:
Absorption and distribution: Absorption is not affected by food, and the mean peak plasma concentrations of Eplerenoe are reached approximately 1.5 hours following oral administration. The plasma protein binding of Eplerenone is about 50% and it is primarily bound to alpha 1 - acid glycoproteins.
Metabolism and excretion: Eplerenone metabolism is primarily mediated via CYP3A4. Less than 5% of an Eplerenone dose is recovered as unchanged drug in the urine and feces. Following a single oral dose of radio labeled drug, approximately 32% of the dose was excreted in the feces and approximately 67% was excreted in the urine. The elimination half-life of Eplerenone is approximately 4 to 6 hours. The apparent plasma clearance is approximately 10 L/hr.
3.INDICATIONS:
Spranone is indicated to improve survival of stable patients with left ventricular systolic dysfunction and clinical evidence of congestive heart failure post-myocardial infarction.
Spranone is indicated for the treatment of hypertension, maybe use alone or in combination with other antihypertensive agents.
4.CONTRAINDICATIONS:
Spranone is contraindicated in all patients with the following:
- Serum potassium > 5.5mEq/L at initiation.
- Creatinine clearance ≤ 30 mL/min.
- Concomitant use with the following potent CYP3A4 inhibitors: Ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir and nelfinavir.
SPRANONE is also contra indicated for the treatment of hypertension in patients with the following:
-Type 2 diabetes with microalbuminuria.
- Creatinine clearance < 50 mL/min.
- Concomitant use of potassium supplements or potassium sparing diuretics (amiloride, spironolactone, or triamterene).
5.WARNINGS & PRECAUTIONS:
- Hyperkalemia in patients treated for hypertension.
- Hyperkalemia in patients treated for congestive heart failure post-myocardial infarction.
The principal risk of SPRANONE is hyperkalemia. Hyperkalemia can cause serious, sometimes fatal, arrhythmias. Patients who develop hyperkalemia (>5.5 mEq/L) may still benefit from SPRANONE with proper dose adjustment.
Patients with CHF post MI who have serum creatinine levels > 2.0 mg/dL (males) or > 1.8 mg/dL (females) or creatinine clearance ≤ 50mL/min should be treated with caution.
Diabetic patients with CHF post MI, including those with proteinuria, should also be treated with caution.
6.Pregnancy & Lactation:
Pregnancy Category B - There are no adequate and well-controlled studies in pregnant women. SPRANONE should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers: The concentration of Eplerenone in human breast milk after oral administration is unknown, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
7.SIDE EFFECTS :
Side effects may include: Chest pain, dizziness, headache, high cholesterol and triglyceride levels, increased blood potassium levels, increased risk for heart attack, kidney problems.
8.DRUG INTERACTIONS:
Drug – drug interaction studies were conducted with a 100 mg dose of eplerenone. Eplerenone is metabolized primarily by CYP3A4. A potent inhibitor of CYP3A4 (ketocnazole) caused increased exposure of about 5-fold while less potent CYP3A4 inhibitors (erythromycin, saquinavir, verapamil and fluconazole) gave approximately 2-fold increases. Grapefruit juice caused only a small increase (about 25 %) in exposure.
No significant changes in eplerenone pharmacokinetics were observed when eplerenone was administered with aluminium and magnesium-containing antacids.
9.DOSAGE AND ADMINSTRATION:
Congestive heart failure post-myocardial infarction:
The recommended dose of Spranone is 50 mg once daily. Treatment should be initiated at 25 mg once daily preferably within 4 weeks as tolerated by the patient. Spranone may be administered with or without food.
Hypertension:
Spranone may be used alone or in combination with other antihypertensive agents. The recommended starting dose of Spranone is 50 mg administered once daily. The full therapeutic effect of Spranone is apparent within 4 weeks. In patients with an inadequate blood pressure response to 50 mg once daily the dosage of Spranone should be increased to 50 mg twice daily.
10.PACKAGING & COMPOSITION:
- SPRANONE 25 – Film Coated Tablets: A pack of 10, 20 or 30 film coated tablets in Alu/Alu blister. Each f.c.tablet contains Eplerenone 25mg.
- SPRANONE 50 – Film Coated Tablets: A pack of 10, 20 or 30 film coated tablets in Alu/Alu blister. Each f.c.tablet contains Eplerenone 50mg.
11.STORAGE CONDITIONS:
Store SPRANONE – Film Coated Tablets at temperature between (15-30)°C.
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