Important safety information

Clinical use:

  • ENTRESTO® should be administered in combination with other heart failure therapies, in place of an ACEi or ARB.

  • ENTRESTO® should be initiated, and up-titration conducted, by a physician experienced with the treatment of heart failure.

  • No dosage adjustment is required in patients over 65 years. However, ENTRESTO® has been studied in a limited number of patients above the age of 80 years. Caution is required in these patients.

  • The safety and efficacy of ENTRESTO® in pediatric patients (<18 years of age) has not been established.

Contraindications:

  • Recent symptomatic hypotension prior to initiation of treatment with ENTRESTO® (sacubitril/valsartan)

  • Concomitant use with any drug formulation containing an ACEi, due to potential enhanced risk of angioedema. ENTRESTO® must not be administered until at least 36 hours have elapsed following discontinuation of ACEi therapy.

  • Known history of angioedema related to previous ACEi or ARB therapy

  • History of hereditary or idiopathic angioedema

  • As for any formulation containing an ACEi or ARB, use of ENTRESTO® together with aliskiren-containing drugs is contraindicated in patients with diabetes mellitus, whether Type 1 or 2, or in patients with moderate to severe renal impairment, i.e., eGFR <60 mL/min/1.73 m2.

  • Pregnant and nursing women

  • Hypersensitivity to the active substances, sacubitril or valsartan, or to any of the excipients

Most serious warnings and precautions:

Use in pregnancy: When used in pregnancy, ARBs can cause injury to or even death of the developing fetus. When pregnancy is detected, ENTRESTO® should be discontinued as soon as possible.

Use of ACEi: ENTRESTO® must not be initiated until at least 36 hours have elapsed following discontinuation of ACEi therapy due to the risk of angioedema. If treatment with ENTRESTO® is stopped, ACEi therapy must not be initiated until 36 hours after the last dose of ENTRESTO®.

NT-proBNP monitoring: Due to the action of sacubitril on BNP levels, only NT-proBNP may be a suitable biomarker for the monitoring of heart failure patients treated with ENTRESTO®.

Use of medications known to raise serum potassium levels: Caution should be exercised when co-administering ENTRESTO® with medications known to raise serum potassium levels (e.g., potassium-sparing diuretics, potassium supplements).

Other relevant warnings and precautions:

  • ENTRESTO® should not be administered with any other drug formulation containing an ARB.

  • Caution when co-administering ENTRESTO® with direct renin inhibitors such as aliskiren.

  • Angioedema: Caution is recommended in patients with a prior history of any angioedema and in black patients.

  • Symptomatic hypotension: ENTRESTO® is not recommended in patients with systolic blood pressure <100 mmHg at the time of treatment initiation.

  • Hyperkalemia: Measure serum potassium before instituting ENTRESTO®, and during treatment, as appropriate, taking into account the patient’s predisposition to develop hyperkalemia.
    Patients with serum potassium >5.2 mmol/L prior to initiation of treatment with ENTRESTO® have not been studied. Careful monitoring of serum potassium is recommended in patients with severe renal impairment, diabetes mellitus, hypoaldosteronism, or a high potassium intake in their diet.

  • Decreases in renal function in susceptible individuals. Closely monitor serum creatinine, and down-titrate or interrupt ENTRESTO® in patients who develop a clinically significant decrease in renal function. Before initiation of therapy and during treatment, assess renal function, as appropriate.

  • Caution in patients with renal artery stenosis, if ENTRESTO® is to be used. Careful monitoring of renal function should be carried out.

  • Advising women of child-bearing potential to use contraception during treatment with ENTRESTO® and for one (1) week after their last dose.

  • Nursing women: Because of the potential risk for adverse drug reactions in breastfed newborns, a decision should be made whether to abstain from breast-feeding or to discontinue ENTRESTO® while breast-feeding, taking into account the importance of ENTRESTO® to the mother.

  • A starting dose of 24 mg sacubitril/26 mg valsartan twice daily is recommended in patients with moderate hepatic impairment (Child-Pugh B).
    ENTRESTO® is not recommended in patients with severe hepatic impairment (Child-Pugh C).

  • ENTRESTO® is not recommended in patients with severe renal impairment (eGFR <30 mL/min/1.73 m2).

For more information:

Please consult the Product Monograph at www.novartis.ca/EntrestoMonograph for important information relating to adverse reactions, drug interactions, and dosing information which have not been discussed in this piece. The Product Monograph is also available by calling 1-800-363-8883 or via medinfo.canada@novartis.com.

References:

  • 1.

    ENTRESTO® Product Monograph. Novartis Pharmaceuticals Canada Inc. July 13, 2021.

  • 2.

    Novartis Data on File – First and only. 2021.

  • 3.

    McDonald M, et al. CCS/CHFS Heart Failure Guidelines Update: Defining a new pharmacologic standard of care for heart failure with reduced ejection fraction. Can J Cardiol 2021;37(4):531-546.

  • 4.

    McMurray JJ, et al. Angiotensin-neprilysin inhibition versus enalapril in heart failure. N Engl J Med 2014;371:993-1004.

  • 5.

    Novartis Data on File – PARADIGM. 2020.

  • 6.

    Packer M, McMurray JJ, Desai AS et al. Angiotensin receptor neprilysin inhibition compared with enalapril on the risk of clinical progression in surviving patients with heart failure. Circulation 2015;131:54-61.

  • 7.

    Desai AS, McMurray JJ, Packer M et al. Effect of the angiotensin-receptor-neprilysin inhibitor LCZ696 compared with enalapril on mode of death in heart failure patients. Eur Heart J 2015;36(30):1990-7.

  • 8.

    Volpe M, et al. The natriuretic peptides system in the pathophysiology of heart failure: From the molecular basis to treatment. Clin Sci (Lond). 2016;130(2):57-77.

  • 9.

    Fielitz J, et al. Neutral endopeptidase is activated in cardiomyocytes in human aortic valve stenosisand heart failure. Circulation. 2002;105:286-289.