Eplerenone CAS 107724-20-9
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- Appearance: White powder
- Assay: 99. 0%min
- Stock: In stock
- Sample: Available
- Zhishang Chemical: Eplerenone Suppiler
Eplerenone: The Complete Guide
Eplerenone for Sale
Basic Info of Eplerenone
(7α,11α,17α)-9,11-Epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylicacidγ-lactoneMethylester; Eplerenone cas 107724-20-9
Pharmaceuticals, pesticides, dye intermediates; Pharmaceutical raw materials
What is Eplerenone?
Eplerenone is utilized alone or in mix with various other drugs to treat hypertension. Eplerenone comes from a course of medicines called mineralocorticoid receptor villains. It works by blocking the activity of aldosterone, an all-natural compound in the body that can elevate blood pressure.
Eplerenone, an aldosterone receptor villain similar to spironolactone, has been revealed to create continual boosts in plasma renin and product aldosterone, which is consistent with the unfavorable governing comments of hindering aldosterone on renin secretion. The resulting rise in plasma renin activity and also aldosterone distributing degrees did not conquer the effects of eplerenone. Compared to its binding to recombinant human glucocorticoid, progesterone and also androgen receptors, eplerenone uniquely binds to recombinant human mineralocorticoid receptors.
Eplerenone is a new type of careful aldosterone receptor antagonist. It was approved by the State Fda for professional application in 2002. The pure product is white or white like crystal, and its aldosterone antagonistic effect is more powerful than spironolactone, and its fondness for androgen and progesterone receptors is very low. The adverse responses are little. It has a certain result on the therapy of hypertension, cardiac arrest and myocardial infarction, with less negative reactions and excellent resistance, It is a good substitute for spironolactone. For serious hypertension that can not be controlled by multiple antihypertensive drugs, the enhancement of eplerenone can dramatically lower blood pressure, particularly systolic high blood pressure. With angiotensin converting enzyme prevention (ACEI) and β The mix of receptor blockers can enhance the lifestyle as well as decrease the death of individuals with serious cardiac arrest as well as coronary infarction.
- Eplerenone selectively acts on aldosterone receptors and is highly selective for mineralocorticoid receptors, but has less effect on androgen and progesterone receptors, and its affinity for mineralocorticoids is 15-20% of that of spironolactone. It has a 500-fold smaller affinity for androgen and progesterone receptors than spironolactone, so there are fewer sex hormone-related adverse reactions.
- Eplerenone can reduce hypertension C, because aldosterone may play an important role in the pathophysiological process of obesity hypertension, so eplerenone also has a good antihypertensive effect on diet-induced obesity-related hypertension; In addition, eplerenone can significantly reduce glomerular ultrafiltration, thereby reducing proteinuria in hypertensive patients, and this renoprotective effect is more pronounced in hypertensive patients with diabetes.
- Eplerenone is not an inhibitor of CYP1A2, CYP3A4, CYP2C19, CYP2C9, or CYP2D6, and does not inhibit diclofenac, methylphenidate, losartan, amiodarone, dexamethasone, phenytoin, phenacetin, Dextromethorphan, metoprolol, tolbutamide, amlodipine, astemizole, cisapride, diazepam, 17-ethinyl estradiol, fluoxetine, lovastatin, methylprednisone Metabolism of drugs such as dragon, midazolam, nifedipine, glyburide and warfarin.
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Application of Eplerenone
- Heart failure: The EPHESUS trial showed that for patients with left ventricular ejection fraction (LVEF) < 40% and heart failure within 3 to 14 days after myocardial infarction, the addition of EPL on the basis of standard treatment can reduce 15 % of all-cause deaths, 17% of the primary composite endpoint (cardiovascular death or hospitalization for a cardiovascular event), and 21% of sudden cardiac death (SCD). For patients with a history of hypertension after acute myocardial infarction, heart failure, and LVEF ≤ 40%, the addition of EPL significantly reduced all-cause mortality, combined primary endpoints, and SCD. In patients without a history of hypertension, EPL reduced HF hospitalizations but did not reduce mortality or other end points. Hospitalization for hypertension is a risk factor for cardiovascular death, and EPL reduces the risk of hospitalization for hypertension in people without a history of hypertension. Because the use of EPL early (3-7 days) after acute myocardial infarction can reduce the primary composite end-point event by 24% and SCD by 34%. However, if EPL was used again for ≥ 7 days, the effect of improving the prognosis was not obvious.
- Hypertension: For patients with mild to moderate hypertension, the blood pressure reduction in the spironolactone 50 mg bid group was greater than that in the EPL 50 mg bid or 100 mg qd group. In patients with hypertension caused by primary aldosteronism, the antihypertensive effect of spironolactone is also better than that of EPL. For hypertensive patients ≥ 50 years old, EPL (50-200 mg/d) and the calcium antagonist amlodipine (2.5-10 mg/d) have similar systolic blood pressure lowering effects. For patients with grade 1 and 2 hypertension, EPL (50-200 mg/d) and the ACEI drug enalapril (10-40 mg/d) are equally effective in the long-term control of SBP and DBP. In black hypertensive patients, EPL was more effective in reducing SBP than the ARB drug losartan, which was not observed in whites. EPL has similar antihypertensive effect on blacks and whites. In patients with high renin hypertension, the antihypertensive effect of EPL is similar to that of losartan. In patients with low renin hypertension, EPL is more effective than losartan in antihypertensive effect. For hypertensive patients who are poorly controlled by ARB alone, adding EPL (50-100 mg·d) for 8 weeks can further enhance the effect of reducing SBP and DBP. For elderly hypertensive patients with poor control of ACEI or ARB, the addition of low-dose (25-50 mg/d, mean 37.5 mg) EPL can effectively reduce SBP and DBP for an average of 24 hours. However, EPL has poor antihypertensive effect in children with hypertension.
Preparation of Eplerenone
A preparation method of eplerenone. The method includes the following steps:
- 17α-hydroxy-3-keto-γ-lactone-pregnant-4,9(11) in a solvent, in the presence of a side reaction inhibitor, in a trichloroacetonitrile, an oxidant and a phosphate buffer system -diene-7α, 21-dicarboxylate methyl ester IV carries out double bond selective epoxidation to prepare eplerenone crude product, the reaction formula is as follows:
- The eplerenone crude product is recrystallized to obtain the eplerenone fine product.