Sacubitril/valsartan can treat heart failure and lower blood pressure. What should you pay attention to when using it?

A friend of mine suffers from high blood pressure and heart problems, and the doctor gave him sacubitril-valsartan. He told Huazi that he was not familiar with this medicine. He knew that valsartan was a blood pressure medicine, but he was unfamiliar with sacubitril. What should he pay attention to when using it?

Hua Zi said that sacubitril-valsartan is a new drug, and it is the first angiotensin receptor neprilysin inhibitor (ARNI) to be marketed in the world. It was originally used to treat heart failure, but later it was found that it also has a good control effect on hypertension, so it was approved for the treatment of hypertension.

1. Special single co-crystal "compound drug"

When many people see the name of the drug "Sacubitril-Valsartan", they think it is a compound drug. This understanding is not wrong. After taking it, the two components of Sacubitril and Valsartan will be decomposed in the human body to take effect. However, Sacubitril-Valsartan is different from traditional compound drugs that are made by mixing two drugs into tablets. It is a single co-crystal drug made by mixing the two drugs in a molar ratio of 1:1.

This advanced process not only increases the stability of the drug, but also makes the bioavailability of valsartan higher in sacubitril/valsartan.

2. Sacubitril is a neprilysin inhibitor

There are natriuretic peptide systems in cardiac cells and vascular endothelial cells, which can counteract the effects of the renin-angiotensin-aldosterol system (RAAS). However, the natriuretic peptides produced by the human body are rapidly degraded by enkephalinase, with a half-life of only a few minutes.

Sacubitril can inhibit the activity of enkephalinase, enhance and prolong the effect of natriuretic peptides, strengthen the inhibition of RAAS, and exert antihypertensive and anti-heart failure effects.

Sacubitril can inhibit the degradation of bradykinin, and prils can also inhibit the degradation of bradykinin, so both can cause dry cough and angioedema, and adverse reactions increase when used together. Sacubitril and prils cannot be used together. If you have taken prils before, you need to switch to sacubitril-valsartan, and the medication must be taken at least 36 hours apart.

3. Valsartan is a RAAS inhibitor

Valsartan is an angiotensin 2 receptor antagonist that can inhibit the binding of angiotensin 2 to receptors on blood vessels, inhibit RAAS, and exert antihypertensive and anti-heart failure effects.

After valsartan and sacubitril form a single co-crystal drug, the bioavailability is greatly improved. In 50 mg of sacubitril-valsartan, there are 24 mg of sacubitril and 26 mg of valsartan, which is equivalent to 40 mg of valsartan.

When used to treat high blood pressure, attention should be paid to dose conversion. For example, if 40 mg of valsartan was originally enough to control blood pressure, 50 mg of sacubitril-valsartan can do the trick; if 80 mg of valsartan was originally taken, 100 mg of sacubitril-valsartan can be chosen.

4. Other matters needing attention

Sacubitril/valsartan is little affected by diet, and there is no strict restriction on the time of taking the medicine. Dry cough may occur during medication, but the symptoms are usually not severe. It is recommended to take the medicine consistently and do not stop the medicine without authorization. However, if angioedema occurs, stop the medicine immediately and seek medical attention.

Sacubitril/valsartan can cause increased blood potassium. Blood potassium needs to be measured before taking the medicine. If the blood potassium is greater than 5.4mmol/L, the medicine cannot be used. Blood potassium also needs to be monitored during medication.

Drugs that inhibit RAAS may cause renal failure, and when used in combination with nonsteroidal anti-inflammatory drugs, the risk of renal damage increases, so renal function monitoring is required during medication.

Sacubitril/valsartan cannot be used in combination with aliskiren; it may increase the adverse reactions of statins and caution should be exercised when used in combination with statins; it may aggravate the adverse reaction of hypotension caused by sildenafil and other PDE-5 inhibitors; and it may reduce the bioavailability of metformin.

In summary, sacubitril-valsartan can be used for heart failure and hypertension. When using it, it is important to note that it cannot be used at the same time as pril drugs, and the interval should be more than 36 hours; when used for hypertension treatment, attention should be paid to the dose conversion with valsartan; in addition, attention should be paid to adverse reactions and interactions with other drugs. Drugs should be used under the guidance of a doctor. If you have any questions about medication, please consult a doctor or pharmacist. I am pharmacist Huazi, welcome to follow me and share more health knowledge.