Alisartan and Mesartan, the "newcomers" in the sartan class of drugs, what are their characteristics?

A friend left a message to Huazi, saying that among the sartan drugs, he found two less familiar sartans, Alisartan and Mesartan. What are their characteristics? It seems that not many people use them?

Hua Zi said that Alisartan and Mesartan are both newly launched sartan drugs, and both are prodrugs that need to be absorbed and metabolized by the human body to release active ingredients before they can play a blood pressure-lowering role. Compared with the previously launched sartan "predecessors", they have the characteristics of lower adverse reactions and stronger efficacy.

1. Alisartan independently developed in my country

Most antihypertensive drugs are developed by foreign pharmaceutical companies and then copied by Chinese pharmaceutical companies after the patent protection period expires. Alisartan, on the other hand, is an antihypertensive drug independently developed by China and launched in China in 2013. It is the "little brother" of the sartan drug family.

The reference prototype for the development of Alisartan was "Losartan" . After taking it, it will be metabolized by hydrolases in the human body and release 5-carboxylic acid losartan (EXP-3174) to exert its pharmacological effects. Losartan will also release EXP-3174 in the human body. In this respect, the two drugs are similar.

However, losartan needs to be metabolized by the liver, while allisartan is metabolized by gastrointestinal hydrolases and does not require liver metabolism. This can reduce the liver burden of hypertensive patients and has fewer interactions when used in combination with other drugs .

In clinical application, Alisartan, like losartan, can be used to treat mild and moderate hypertension. Moreover, it can promote uric acid excretion while lowering blood pressure , so it is suitable for hypertensive patients with hyperuricemia.

The antihypertensive effect of losartan lasts for a short time, and taking it once a day may not achieve stable blood pressure reduction for 24 hours. However, the antihypertensive effect of allisartan lasts for a longer time, and taking it once a day can produce a stable blood pressure reduction effect .

2. Asartan, the “strongest drug in history”

Asartan potassium was launched in the United States in 2011, but it was not launched in China until 2021. It is a new member of the sartan drug family. Sartan drugs rely on binding to angiotensin 2 receptors (AT1 receptors) to exert their effects, and the affinity with AT1 receptors determines the duration and intensity of the action of sartan drugs.

After entering the human body, lasartan will quickly release azilsartan to exert a blood pressure lowering effect . Azilsartan has multiple and irreversible binding sites with AT1, which can exert a long-lasting and stable blood pressure lowering effect. Compared with azilsartan, lasartan has a different chemical structure. lasartan releases more active ingredients than azilsartan and has a stronger effect.

Commonly used antihypertensive drugs can reduce blood pressure by about 10 mmHg per tablet, while each tablet of sartan can reduce blood pressure by up to 15 mmHg, which is better than existing sartan drugs and even other types of antihypertensive drugs. Therefore, sartan is also known as the "strongest" antihypertensive drug in history .

Like other sartans, sartan has the function of protecting the heart and kidneys. Moreover, due to its powerful and long-lasting effects, its organ-protective effect is stronger than that of other sartans.

Sartan drugs have a low overall adverse reaction rate, and mesartan has the same safety as other sartans. Therefore, mesartan has stronger antihypertensive and organ protection effects, and no increase in adverse reactions, making it a new choice in antihypertensive treatment .

3. Limitations of drug costs and long-term safety

From the perspective of pharmacological mechanisms and clinical trial results, Alisartan and Mesartan have surpassed their predecessors and are more suitable for the treatment of hypertension. However, there are two reasons why they are not widely used in clinical practice:

One is that the cost of medication is too high . After centralized state procurement, the cost of classic sartan drugs has been reduced to only a few cents per tablet. However, Alisartan and Mesartan were launched later and are more expensive, which most patients cannot afford.

Second, long-term safety remains to be observed . Classic sartan drugs have been on the market for a long time, and their pharmacological effects and adverse reactions have been studied more thoroughly and are more reliable. Doctors have formed a habit of using drugs and generally do not easily change drugs. New drugs require long-term observation of long-term safety, which also affects their use.

In summary, Alisartan and Mesartan are both "newcomers" in the sartan family of drugs. Both are prodrugs that require biotransformation after entering the human body to release active ingredients to exert their effects. Compared with traditional sartan drugs, the new drugs have significantly improved duration and intensity of action, and lower adverse reactions, but they are more expensive and their long-term safety needs to be observed, which limits their use.

Drugs must 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.