Sacvin Tablets 24mg/26mg (Sacubitril , Valsartan) PharmEvo

Used For

Heart Failure

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.

Dosage

The recommended starting dose of Sacubitril + Valsartan is one tablet of 49mg + 51mg twice daily.The dose of Sacubitril + Valsartan should be doubled after 2 to 4 weeks to the target maintenance dose of one tablet of 97mg + 103mg twice daily, as tolerated by the patient. Starting dose for some populations : A starting dose of (Sacubitril + Valsartan) one tablet of 24mg + 26mg taken twice daily is recommended for patients not currently taking an ACE inhibitor or an ARB or patients previously taking low doses of these agents. A starting dose of Sacubitril + Valsartan of one tablet of 24mg + 26mg taken twice daily should be considered for patients who have risk factors for hypotension, including patients = 75 years old and patients with low systolic blood pressure (SBP =100 to 110 mmHg). The dose of Sacubitril + Valsartan should be doubled every 2-4 weeks to the target dose of one tablet of Sacubitril + Valsartan 97mg + 103 mg twice daily, as tolerated by the patient. Always consult your doctor or pharmacist for dose adjustments.

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

Sacubitril + valsartan may cause angioedema. If angioedema occurs, discontinue sacubitril + valsartan immediately, provide appropriate therapy and monitor for airway compromise. Sacubitril + valsartan should not be used in patients with a known history of angioedema related to previous ACE inhibitor or ARB therapy.

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.
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.

3. ) Caution should be exercised when initiating sacubitril + valsartan in patients with NYHA functional classification IV due to limited clinical experience in this population.

Pregnancy category

Always consult your physician before using any medicine.

Storage (YES/NO)

Store this medicine at room temperature, away from direct light and heat.