| Fact Table | |
|---|---|
| Formula | C24H29NO5 (sacubitril) / C24H29N5O3 (valsartan) |
| License | FDA approved (2015); EMA approved |
| Bioavailability | Sacubitril (as LBQ657): ~60%; Valsartan: ~23% |
| Legal status | Prescription only (Rx) |
| Chemical Name | Sacubitril: methyl (2S,4R)-5-biphenyl-4-yl-4-amino-2-methylpentanoate; Valsartan: (2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid |
| Elimination half-life | Sacubitril (LBQ657): ~11.5 hours; Valsartan: ~9.9 hours |
| Dosage (Strength) | Tablets: 24/26 mg, 49/51 mg, 97/103 mg (sacubitril/valsartan), twice daily |
| Pregnancy | Category D – Fetal toxicity; contraindicated in pregnancy |
| Brands | Entresto |
| Protein binding | Sacubitril/LBQ657: ~94–97%; Valsartan: ~95% |
| PubChem CID | Sacubitril: 16132621; Valsartan: 60846 |
| MedlinePlus | a615043 |
| ChEBI | Sacubitril: 83779; Valsartan: 9925 |
| ATC code | C09DX04 |
| DrugBank | DB09292 (sacubitril); DB00177 (valsartan) |
| KEGG | D10099 (sacubitril); D02368 (valsartan) |
| Routes of administration | By mouth (oral tablets) |
Entresto (sacubitril/valsartan) is a medication used to treat heart failure in adults and children. It combines two drugs that work together to help the heart pump more effectively. Sacubitril helps blood vessels relax by stopping the breakdown of natural substances in the body that widen the vessels. Valsartan helps prevent blood vessels from tightening, allowing blood to flow more easily. Together, these effects help reduce stress on the heart and reduce the risk of hospitalization or death in people with heart failure.
Entresto is taken by mouth twice daily, with or without food. The standard starting dose for adults with chronic heart failure is typically 49/51 mg (sacubitril/valsartan) twice daily, though some patients may begin at 24/26 mg twice daily. The dose can be doubled every 2 to 4 weeks as tolerated, with a target maintenance dose of 97/103 mg twice daily. In children, the dosage will depend on body weight.
It's important to take this medication at the same time each day. Do not stop taking Entresto without consulting a doctor.
The active ingredients in Entresto are sacubitril and valsarta
Avoid taking or using this medication if any of the following apply:
Common side effects of Entresto include:
These side effects are more common when starting treatment or adjusting the dose. Blood tests may be done regularly to monitor kidney function and potassium levels while on Entresto.
More serious side effects can occur, including angioedema, a severe allergic reaction that causes swelling of the face, lips, tongue, or throat and can be life-threatening. Kidney problems may worsen in some people and, in rare cases, lead to kidney failure. Seek immediate medical attention for trouble breathing, facial swelling, severe dizziness, or fainting.
What is Entresto used for?
Entresto is primarily used to treat heart failure with reduced ejection fraction (HFrEF). It helps improve the heart’s ability to pump blood efficiently, reduces the risk of cardiovascular death and hospitalization, and is often prescribed in place of ACE inhibitors or ARBs in appropriate patients.
How does Entresto work?
Entresto combines two medications: sacubitril, a neprilysin inhibitor that helps increase levels of beneficial peptides that relax blood vessels, and valsartan, an angiotensin II receptor blocker (ARB) that lowers blood pressure and reduces strain on the heart. Together, they improve heart function and outcomes in heart failure.
How should Entresto be taken?
Entresto is taken by mouth, usually twice a day, with or without food. The dosage is based on individual patient needs, kidney function, and previous use of ACE inhibitors or ARBs. It’s important to follow the prescribed schedule and not stop the medication without medical advice.
What are the common side effects of Entresto?
Common side effects include low blood pressure (hypotension), high potassium levels (hyperkalemia), dizziness, and kidney function changes. Some patients may also experience a dry cough. Side effects should be monitored regularly through lab tests and clinical evaluations.
Who should not take Entresto?
Entresto should not be used by patients with a history of angioedema related to ACE inhibitors or ARBs, those currently taking an ACE inhibitor (without a 36-hour washout period), or individuals with severe liver impairment. It is also not recommended during pregnancy due to the risk of harm to an unborn baby.
Can Entresto be used with other heart failure medications?
Yes, Entresto is often used alongside beta-blockers, diuretics, and mineralocorticoid receptor antagonists (like spironolactone) as part of guideline-directed therapy for heart failure. However, it should not be used with ACE inhibitors or other ARBs due to the risk of serious side effects.
Does Entresto affect blood pressure?
Yes, Entresto can lower blood pressure, which is part of how it helps the heart. However, this can sometimes lead to symptomatic hypotension, especially in older adults or those taking other blood pressure medications, so regular monitoring is essential.
What should I do if I miss a dose of Entresto?
If you miss a dose of Entresto, take it as soon as you remember. If it’s close to the time of your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at once to make up for a missed dose.
How long does it take for Entresto to start working?
Some benefits, such as improved blood pressure and reduced symptoms, may be noticed within a few weeks. However, full effects on heart function and hospitalization risk reduction are typically seen over several months of consistent use.
Is regular monitoring needed while taking Entresto?
Yes, patients on Entresto should have their kidney function, potassium levels, and blood pressure checked regularly. These tests help ensure the medication is working effectively and safely, especially when starting or adjusting the dose.
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A generic drug is a copy of the brand-name drug with the same dosage, safety, strength, quality, consumption method, performance, and intended use. Before generics become available on the market, the generic company must prove it has the same active ingredients as the brand-name drug and works in the same way and in the same amount of time in the body.
The only differences between generics and their brand-name counterparts is that generics are less expensive and may look slightly different (e.g., different shape or color), as trademark laws prevent a generic from looking exactly like the brand-name drug.
Generics are less expensive because generic manufacturers don't have to invest large sums of money to develop a drug. When the brand-name patent expires, generic companies can manufacture a copy of the brand-name and sell it at a substantial discount.