Generic
Sacubitril + Valsartan
39 brands available in the market
At a glance
Sacubitril + Valsartan is an ARNI (angiotensin receptor neprilysin inhibitor) used to reduce the risk of cardiovascular death and hospitalization in patients with chronic heart failure (NYHA class II-IV). It relaxes blood vessels and makes it easier for the heart to pump blood.
Description
Sacubitril + Valsartan is a combination of sacubitril (a neprilysin inhibitor) and valsartan (an angiotensin II receptor blocker). Sacubitril's active metabolite LBQ657 inhibits neprilysin, increasing natriuretic peptide levels, promoting natriuresis and vasodilation; valsartan blocks AT1 receptors, inhibiting vasoconstrictive and aldosterone-secreting effects of angiotensin II.
Indications
- Chronic heart failure (NYHA class II-IV) – reduce cardiovascular death and hospitalization
- Pediatric heart failure (≥1 year)
Therapeutic class
ARNI (Angiotensin Receptor Neprilysin Inhibitor)
Pharmacological class
Angiotensin Receptor Blocker + Neprilysin Inhibitor
Pharmacology
Sacubitril's active metabolite LBQ657 inhibits neprilysin, preventing degradation of natriuretic peptides (ANP, BNP), leading to vasodilation, natriuresis, and reduced plasma volume. Valsartan blocks angiotensin II type-1 receptors, inhibiting vasoconstriction and aldosterone secretion. This dual action reduces hemodynamic burden in heart failure.
Mechanism of action
Inhibits neprilysin to increase natriuretic peptides and blocks angiotensin II receptors to relax blood vessels.
Dosage
Adult Heart Failure:
- Starting: 49/51 mg twice daily
- Target maintenance: Double to 97/103 mg twice daily after 2-4 weeks (as tolerated)
- Reduced starting (not on ACEi/ARB, low dose, severe renal, moderate hepatic): 24/26 mg twice daily
Pediatric (≥1 year):
- <40 kg: 1.6→2.3→3.1 mg/kg
- 40-<50 kg: 24/26→49/51→49/51 mg
- ≥50 kg: 49/51→72/78→97/103 mg
Administration
- Take orally with or without food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as possible; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Angioedema
- Hypotension
- Impaired renal function
- Hyperkalemia
- Cough
- Dizziness
- Orthostatic hypotension
Precautions & warnings
- Do not use in patients with history of angioedema
- Do not use with ACE inhibitors (36-hour washout)
- Do not use with aliskiren in diabetic patients
- Not recommended in severe hepatic impairment (Child-Pugh C)
- Unsafe in pregnancy; avoid in lactation
Contraindications
- History of angioedema (ACEi or ARB-related)
- Concomitant use with ACE inhibitors (36-hour washout)
- Concomitant use with aliskiren in diabetic patients
- Hypersensitivity to any component
Drug interactions
- Dual RAAS blockade: Avoid with ACEi, aliskiren (in diabetes), or ARB
- Potassium-sparing diuretics: May increase serum potassium
- NSAIDs: Increased risk of renal impairment
- Lithium: Increased risk of lithium toxicity
Food interactions
Alcohol is unsafe with Sacubitril + Valsartan; consult your doctor.
Use in pregnancy
Use in Pregnancy: Unsafe during pregnancy; definite evidence of risk to the developing baby; use only in life-threatening situations; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited data suggests drug may pass into breast milk and harm the baby; consult your doctor.
Pediatric use
Indicated for pediatric patients ≥1 year of age
Geriatric use
No relevant pharmacokinetic differences in elderly (≥65 years) or very elderly (≥75 years)
Renal / hepatic impairment
Renal Impairment: Mild-moderate (eGFR ≥30): no dose adjustment; severe (eGFR <30): start 24/26 mg twice daily; consult your doctor.
Hepatic Impairment: Mild (Child-Pugh A): no dose adjustment; moderate (Child-Pugh B): start 24/26 mg twice daily; severe (Child-Pugh C): not recommended; consult your doctor.
Overdose effects
Overdose is most likely to cause hypotension; provide symptomatic treatment; unlikely to be removed by hemodialysis due to high protein binding.
Storage conditions
Store below 30°C in a dry place, protected from moisture; keep out of reach of children.
Chemical structure
Sacubitril + Valsartan