Generic Name: Sacubitril 49mg + Valsartan 51mg Company Name: Novartis(Bangladesh) Limited
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Indications of Entresto 100
This combination is advised to reduce the risk of cardiovascular mortality and heart failure hospitalization in patients with chronic heart failure (NYHA Classes II–IV) and a decreased ejection fraction.
This combination is typically administered in conjunction with other heart failure therapies rather than an ACE inhibitor or other ARB.
Pharmacology
The neutral endopeptidase enkephalinase, which normally cleaves natriuretic peptides like atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide, is inhibited by sacubitril's active metabolite, LBQ657 (CNP). Under atrial and ventricular pressure, ANP and BNP are released, activating subsequent receptors and causing vasodilation, natriuresis, and diuresis. Other vasodilators and vasoconstrictor peptides like angiotensin I and II, endothelin 1, and amyloid beta protein are degraded by enkephalinase under normal circumstances. Therefore, the inhibition of neprilysin results in increased levels of vasoconstrictor hormones like angiotensin II as well as increased concentration and decreased degradation of endogenous natriuretic peptides. (However, it can cause angiotensin II to block its receptors, prevent vasoconstriction, and result in a decrease in vascular resistance when used in conjunction with valsartan.
Valsartan is an oral medication that belongs to a class of drugs called angiotensin receptor blockers (ARB). It is a specific orally active angiotensin II antagonist that acts on the AT1 subtype. The binding of angiotensin to its receptors causes blood vessels to narrow (vasoconstriction), which leads to increased blood pressure (hypertension). Valsartan blocks angiotensin II receptors. By blocking the effects of angiotensin, valsartan dilates blood vessels and lowers blood pressure without affecting pulse rate. The affinity of valsartan for the AT1 receptor is much greater than that of the AT2 receptor (about 20,000 times). It does not bind to or block other hormone receptors or ion channels that are known to be important for cardiovascular regulation. Elevated peptide levels are the cardiovascular and renal effects of sacubitril. As a result, enkephalinase typically breaks down these peptides.
Angiotensin receptor blockers are a class of drugs that includes the oral medication valsartan (ARB). It is a particular angiotensin II antagonist that is orally active and targets the AT1 subtype. Vasoconstriction, which occurs as a result of angiotensin II binding to its receptors, raises blood pressure (hypertension). A blocker of angiotensin II receptors is valsartan. Valsartan relaxes blood vessels and lowers blood pressure without slowing the heart rate by blocking the effects of angiotensin. Valsartan has a much higher affinity for the AT1 receptor than the AT2 receptor (about 20,000 times). Other hormone receptors and ion channels that are well-known to be crucial for controlling cardiovascular function are not bound to or blocked by it.
Dosage & Administration
Contraindications
Side Effects of Entresto 50
Pregnancy & Lactation
Pregnancy: Inform female patients of reproductive age about the risks of using this combination while pregnant. Discuss treatment choices with women who are thinking about starting a family. Instruct patients to notify their doctors as soon as they get pregnant.
Lactation: There is no evidence on whether sacubitril/valsartan is present in human milk, the effects on a breastfed newborn, or the impact on milk production. Rat milk contains sacubitril/valsartan. Because of the risk of significant adverse effects in breastfed infants from exposure to sacubitril/valsartan, tell a nursing mother that breastfeeding is not recommended while she is on the drug.
Precautions & Warnings
Signs and symptoms of angioedema and hypotension should be observed
Storage Conditions
Store at room temperature between 20°C to 25°C. Protect from moisture.
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