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Inventory of three generations of seven "statin" lipid-lowering drugs, some of which are not necessarily available on the instructions

Inventory of three generations of seven "statin" lipid-lowering drugs, some of which are not necessarily available on the instructions

With the improvement of people's living standards, there are more and more people with high blood lipids, and high blood lipids are the "culprits" of many diseases.

In previous articles, we have also mentioned that in addition to dietary adjustment and appropriate exercise, hyperlipidemia also requires medication when necessary. (Click on the blue word to see if high blood lipids are eaten?) What dietary tips can help control blood lipids? )

Today we will talk in detail about the treatment of high blood lipid drugs, a very important class of drugs - statins.

Inventory of three generations of seven "statin" lipid-lowering drugs, some of which are not necessarily available on the instructions

Statin drugs mainly by inhibiting the synthesis of cholesterol in the body to achieve the purpose of regulating blood lipids, is the "boss" in the regulation of blood lipid drugs, occupying 93% of the "Jiangshan" of drugs that regulate blood lipids.

According to the time-to-market classification of statins, it can be mainly divided into three generations and seven drugs.

First generation: simvastatin, pravastatin, lovastatin.

Second generation: fluvastatin, rosuvastatin, atorvastatin.

The third generation: pitvastatin.

Although they all achieve the purpose of lowering blood lipids by inhibiting cholesterol synthesis, they have different characteristics, as shown in the following figure:

Inventory of three generations of seven "statin" lipid-lowering drugs, some of which are not necessarily available on the instructions

For example, lipophilic drugs are easy to distribute to fat and liver, the better the lipophilicity, the better the hypolipidemic effect, but correspondingly, the stronger the myotoxicity and hepatotoxicity;

Hydrophilic drugs are easily distributed to the kidneys and have a greater burden on the kidneys.

As shown in the figure above, pravastatin is not metabolized by liver drug enzymes, so it is more friendly to patients with hepatic insufficiency.

Pravastatin and rosuvastatin are very water soluble, and the amount of medicine that enters the liver and muscles is very small, which means that their myotoxicity is relatively weak.

However, due to its good water solubility and wide distribution in the kidneys, it is not recommended to use pravastatin and rosuvastatin in patients with renal insufficiency.

According to the intensity of action, water solubility, fat solubility and other characteristics, the lipid-lowering effects of these seven commonly used statins are also strong or weak.

Inventory of three generations of seven "statin" lipid-lowering drugs, some of which are not necessarily available on the instructions

In addition to the ability to lower blood lipids is strong and weak, drug toxicity is also strong and weak, in the selection of statin drugs can not only look at the effect of lipid reduction, but also comprehensive consideration of adverse reactions.

Therefore, in actual clinical practice, doctors need to comprehensively consider the patient's situation and choose suitable statins for treatment.

In previous articles, we popularized two drugs, rosuvastatin calcium tablets and atorvastatin calcium tablets, and click on the blue word to review.

01 Take statins appropriately, remembering early, appropriate, long-term

Early stage: If there are dyslipidemia or atherosclerotic plaques, the sooner you take the better, the benefit of early drug intervention can reach 3 times that of advanced drug intervention.

Appropriate amount: Be sure to reduce the blood lipids to less than half, and increase the ratio of HDL to apolipoprotein A.

Long-term: blood lipids on the lining of arteries, the formation of atherosclerosis or plaque takes about 30-40 years, a very large time span.

The smoother and more neat the vascular lining, without inflammation, ulcers and other lesions, blood lipids are not easy to deposit in the vascular lining.

Therefore, the smoothness and softness of the vascular lining is very important, and taking the drug irregularly will damage the vascular lining.

And the formation of plaques at any time has the risk of disease, the time of action of the drug is limited, after stopping the drug lipids will rise again, so to take statin drugs for a long time and regularly, can not eat the last meal and forget the next meal.

02 Take statins and avoid tobacco, alcohol and grapefruit

In addition to paying attention to the adjustment of daily diet, patients with hyperlipidemia should also pay attention to the effects of diet on statins.

For example, smoking and drinking alcohol will have an impact on the efficacy of statins, especially drinking, alcohol will inhibit the hypolipidemic effect of statins and increase drug toxicity, so patients taking statins should quit smoking and alcohol.

In addition, patients with hyperlipidemia know that they should eat more vegetables and fruits, but there is one exception, which is grapefruit.

After grapefruit juice enters the human body, it is metabolized by the CYP3A4 enzyme in the liver, and many statin drugs are also metabolized by the CYP3A4 enzyme, and they will compete with each other.

Grapefruit juice affects statin metabolism, statin metabolism can not be metabolized out will accumulate in the body, increasing the toxicity of the drug.

Therefore, while taking statins, it is necessary to avoid eating grapefruit or drinking grapefruit juice.

References: Medical Microvision Official Website - Zhang Shige Chief Pharmacist "Safe Use of Statins" Medical Microvision Official Website - Liu Wenxian Chief Physician "Hyperlipidemia (Hyperlipidemia)"

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