Uperio Tablets 100Mg (1 Strip = 14 Tablets) Specification
Requires Prescription (YES/NO)
Yes
Generics
Sacubitril , Valsartan
How it works
Sacubitril + valsartan inhibits neprilysin (neutral endopeptidase; NEP) , the active metabolite of the prodrug sacubitril and blocks the angiotensin II type-1 (AT1) receptor via valsartan. The cardiovascular and renal effects of sacubitril + valsartan in heart failure patients are attributed to the increased levels of peptides that are degraded by neprilysin, such as natriuretic peptides (NPs) and the simultaneous inhibition of the effects of angiotensin II by valsartan. NPs exert their effects by activating membrane bound guanylyl cyclase coupled receptors, resulting in increased concentrations of the second messenger cyclic guanosine monophosphate (cGMP), which could result in vasodilation, natriuresis and diuresis, increased glomerular filtration rate and renal blood flow, inhibition of renin and aldosterone release, reduction ofsympathetic activity and antihypertrophic and antifibrotic effects. Valsartan inhibits the effects of angiotensin II by selectively blocking the AT1 receptor and also inhibits angiotensin II-dependent aldosterone release. This prevents sustained activation of the renin-angiotensin-aldosterone system that would result in vasoconstriction, renal sodium and fluid retention, activation of cellular growth and proliferation and subsequent maladaptive cardiovascular remodeling.
Usage And Safety
Dosage
Sacubitril , Valsartan
Side Effects
Very Common : Hyperkalemia, hypotension and renal impairment.Common : Anemia, hypokalemia, hypoglycemia, dizziness, headache, syncope, vertigo, orthostatic hypotension, cough, diarrhea, nausea, gastritis, renal failure (renal failure, acute renal failure), fatigue and asthenia.Uncommon : Hypersensitivity, dizziness postural, pruritus, rash and angioedema.
Drug Interactions
Angiotensin Receptor Blockers , OATP1B1 and OATP1B3 substrates, e.g. statins , PDE5 inhibitors including sildenafil , potassium-sparing diuretics (triamterene, amiloride), mineralocorticoid antagonists (e.g. spironolactone, eplerenone), potassium supplements, salt substitutes containing potassium or other agents (such as heparin) , Non-steroidal anti-inflammatory agents (NSAIDs), including selective cyclooxygenase-2 (COX-2) inhibitors , Lithium , OATP1B1, OATP1B3, OAT3 (e.g. rifampicin, ciclosporin), OAT1 (e.g. tenofovir, cidofovir) or MRP2 (e.g. ritonavir) , Metformin HCl.
Indication
Sacubitril + Valsartan is indicated in adult patients for treatment of symptomatic chronic heart failure with reduced ejection fraction. Sacubitril + Valsartan is usually administered in conjunction with other heart failure therapies, in place of an ACE inhibitor or other ARB.
When not to Use
Sacubitril + Valsartan is contraindicated in patients with:• Hypersensitivity to the active substance, sacubitril, valsartan or to any of the excipient of the product.• Concomitant use with ACE inhibitors. Sacubitril + Valsartan must not be administered until 36 hours after discontinuing ACE inhibitor therapy.• Known history of angioedema related to previous ACE inhibitor or ARB therapy.• Hereditary or idiopathic angioedema.• Concomitant use with aliskiren-containing medicinal products in patients with diabetes mellitus or in patients with renal impairment (eGFR <60 ml/min/1.73 m2 ).• Severe hepatic impairment, biliary cirrhosis and cholestasis.• Second and third trimester of pregnancy
Warnings
Warning 1
Sacubitril + valsartan lowers blood pressure and may cause symptomatic hypotension. Patients with an activated renin-angiotensin system, such as volume- and/or salt-depleted patients (e.g., those being treated with high doses of diuretics), are at greater risk. Correct volume or salt depletion prior to administration of sacubitril + valsartan or start at a lower dose. If hypotension occurs, consider dose adjustment of diuretics, concomitant antihypertensive drugs and treatment of other causes of hypotension (e.g., hypovolemia). If hypotension persists despite such measures, reduce the dosage or temporarily discontinue sacubitril + valsartan.
Warning 2
Through its actions on the RAAS, hyperkalemia may occur with sacubitril + valsartan. Monitor serum potassium periodically and treat appropriately, especially in patients with risk factors for hyperkalemia such as severe renal impairment, diabetes, hypoaldosteronism or a high potassium diet. Dosage reduction or interruption of sacubitril + valsartan may be required.
Warning 3
Caution should be exercised when initiating sacubitril + valsartan in patients with NYHA functional classification IV due to limited clinical experience in this population.
