The “old” simvastatin does not have a strong lipid-lowering effect, so why is it still being used?

When Huazi was explaining statins, he said that atorvastatin and rosuvastatin were strong statins, and other statins were medium-acting statins. A patient asked Huazi, his doctor asked him to use simvastatin, but since the lipid-lowering effect was not good, why should he use it?

Hua Zi said that the principle of drug selection is not to choose the "strongest" but to choose the "most suitable". When doctors choose statins, they usually decide based on the patient's initial blood lipid level. If it is not very high, then a medium-acting statin will do the job.

1. “Old” Simvastatin

In the statin family, simvastatin is a "veteran". The first statin to be marketed was lovastatin, which was launched in 1987. Simvastatin is based on lovastatin, with slight structural changes. It was launched in 1988 and is the second statin to be marketed.

Because it was launched early, simvastatin has been studied more and more thoroughly for its efficacy and adverse reactions. Many doctors used simvastatin as their first statin and have used it for a long time, forming a habit of taking it. Therefore, they prefer simvastatin when choosing statins.

2. Simvastatin: Still in good shape

Although simvastatin was developed and marketed relatively early, its efficacy is well recognized. It can effectively inhibit hydroxymethylglutaryl coenzyme A reductase (the enzyme that synthesizes cholesterol), reduce the levels of total cholesterol and low-density lipoprotein cholesterol, and can be used for the treatment of hyperlipidemia and anti-atherosclerosis.

The level of low-density lipoprotein cholesterol (LDL-C) is an indicator of the efficacy of statins. For people with "three highs" such as high blood pressure, high blood lipids, and high blood sugar, if they want to prevent the occurrence of cardiovascular and cerebrovascular diseases, they need to control LDL-C below 2.6mmol/L; for people who have already suffered cerebral infarction, myocardial infarction, and coronary heart disease, if they want to prevent the recurrence of the disease, they need to control LDL-C below 1.8mmol/L.

3. What should you pay attention to when using simvastatin

Simvastatin should be taken starting from 10 mg per day. After one month of taking it, blood lipids should be rechecked. If the target is not reached, the dose can be increased to 20 mg. The maximum dose is 40 mg per day. Doubling the dose of statins can only reduce LDL-C levels by 6%. The maximum dose of simvastatin can reduce LDL-C levels by about 40%. If the initial LDL-C level is high, or if the patient is insensitive to simvastatin after taking the drug, it is recommended to choose a strong statin.

The peak blood concentration of simvastatin is reached in about 4 hours after oral administration, and the human body's cholesterol is mainly synthesized at night, so simvastatin has the strongest lipid-lowering effect when taken before bed.

4. Adverse Reactions of Simvastatin

Taking simvastatin may affect liver function and cause an increase in transaminase (AST, ALT), but this does not usually mean liver damage and can be restored after stopping the medication. Pay attention to monitoring liver function during medication. If the transaminase increases by more than 3 times the normal value, the medication should be stopped. If it does not exceed 3 times the normal value, the medication can be continued.

Simvastatin may cause muscle damage. Monitor creatine kinase (CK) during medication. If it exceeds 5 times the upper limit of normal, stop taking the drug. If severe muscle pain and fatigue occur during medication, accompanied by soy sauce-colored urine, rhabdomyolysis is likely to occur. Stop taking the drug immediately and seek medical attention.

Simvastatin is metabolized by the liver enzyme CYP3A4. Many drugs are metabolized by this pathway. When used in combination with other drugs, simvastatin metabolism may be slowed down, and accumulation may cause side effects. Therefore, when other drugs are needed, you need to consult a doctor or pharmacist to determine whether there is an interaction. Grapefruit will inhibit the activity of CYP3A4, so you should avoid eating grapefruit during medication.

People who suffer from multiple chronic diseases and need to take other medications for a long time can choose statins that have fewer interactions with other drugs, such as pravastatin, pitavastatin, and rosuvastatin.

To sum up, simvastatin is an "old" statin. Although it was launched on the market earlier, it has definite efficacy and is still a widely used lipid-lowering drug today.

When choosing a drug, you don't need to pursue the strongest effect, but rather the most suitable one. Using the drug under the guidance of a doctor is the correct choice.

I am pharmacist Huazi. Welcome to follow me and share more health knowledge.