Sacubitrilat

Sacubitrilat is the active metabolite of sacubitril, a prodrug that is used in combination with valsartan to treat heart failure. Sacubitrilat is a neprilysin inhibitor, which means it blocks the action of an enzyme that breaks down certain peptides in the body. By inhibiting this enzyme, sacubitrilat increases the levels of these peptides, which can have beneficial effects on the cardiovascular system.

Pharmacology

Sacubitril is converted to sacubitrilat in the body by a process known as hydrolysis. This conversion is carried out by an enzyme called esterase. Once sacubitrilat is formed, it inhibits the enzyme neprilysin. Neprilysin is responsible for breaking down certain peptides, including natriuretic peptides, which are involved in regulating blood volume and blood pressure.

By inhibiting neprilysin, sacubitrilat increases the levels of natriuretic peptides. This leads to a number of effects, including dilation of the blood vessels, increased urine output, and decreased release of aldosterone. These effects can help to reduce the symptoms of heart failure.

Clinical Use

Sacubitril, in combination with valsartan, is used to treat heart failure. This combination is often used in patients who have not responded adequately to other treatments for heart failure. The combination of sacubitril and valsartan has been shown to reduce the risk of hospitalization and death in patients with heart failure.

Side Effects

The most common side effects of sacubitril/valsartan are low blood pressure, high potassium levels, and kidney problems. Other side effects can include dizziness, cough, and swelling of the face, lips, tongue, or throat.

See Also

• Heart failure
• Valsartan
• Neprilysin
• Natriuretic peptides

References

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