Sacubitril/valsartan
A tablet combining the neprilysin inhibitor sacubitril with the ARB valsartan, used to cut deaths and admissions in chronic heart failure.
Also called sacubitril and valsartan (US label name).
Drug card
- How it works
- Inhibiting neprilysin to boost natriuretic peptides, with AT1 receptor block
- Used for
- Chronic heart failure, to reduce deaths and admissions
- Heart failure in children aged one year and older
- Known for
- Low blood pressure
- Angioedema, more often in Black patients
- Fetal injury or death in pregnancy
- Its name
- -sartan means an angiotensin II receptor blocker (ARB); -tril, -trilat means a neprilysin (endopeptidase) inhibitor
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does sacubitril/valsartan work?
Sacubitril is a prodrug: esterases turn it into LBQ657 (sacubitrilat), which inhibits neprilysin and raises natriuretic peptide levels, so vessels widen and sodium is lost. Valsartan blocks the AT1 receptor, cancelling the rise in angiotensin II that neprilysin inhibition brings and reducing aldosterone release.
Uses
What is sacubitril/valsartan used for?
- Chronic heart failure, to reduce deaths and admissions
- Heart failure in children aged one year and older
Side effects
Side effects of sacubitril/valsartan
- Low blood pressureKnown for
- Angioedema, more often in Black patientsKnown forSerious
- Fetal injury or death in pregnancyKnown forSerious
- High potassiumSerious
- Cough
- Dizziness
- Kidney impairment or failureSerious
- Dizziness on standing and falls
- Rash, itching and anaphylaxisSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Never given with an ACE inhibitor: at least 36 hours must separate the two because of angioedema.
- Not combined with another ARB, since it already contains valsartan; aliskiren is contraindicated in diabetes.
- Stopped as soon as pregnancy is detected.
- Salt or volume depletion raises the risk of hypotension; kidney function and potassium are monitored.
Good to know: It replaces an ACE inhibitor or ARB rather than joining one; in a large heart failure trial it beat enalapril at preventing cardiovascular death or admission.
Remember it
A way to remember it
Keep the good peptides, block the bad hormone.
Sacubitril, through its active form, inhibits neprilysin so the natriuretic peptides that widen vessels and clear salt and water last longer; valsartan blocks the AT1 receptor so the angiotensin II that also builds up cannot constrict vessels or release aldosterone.
Written for biofideX
Its name
-sartan means angiotensin II receptor blocker (ARB)
Sartans block the AT1 receptor for angiotensin II. Valsartan is also half of sacubitril/valsartan, which adds a neprilysin inhibitor.
-tril, -trilat means neprilysin (endopeptidase) inhibitor
Sacubitril, given with valsartan, blocks neprilysin, which breaks down natriuretic peptides; its active form is sacubitrilat. One letter away from -pril (ACE inhibitors).
- Every drug name stem
Its class
Angiotensin receptor-neprilysin inhibitors
They pair a neprilysin inhibitor with an angiotensin receptor blocker. Blocking neprilysin slows the breakdown of natriuretic peptides, which widen vessels and help the kidney shed sodium and water. Neprilysin also breaks down angiotensin II, so the ARB is needed to block AT1 receptors and stop that extra angiotensin II from constricting vessels and releasing aldosterone.
Easily mixed up with angiotensin receptor blockers and ACE inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Heart failure, rhythm and angina
Sacubitril/valsartan is one of 10 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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