Among the “three highs,” high blood lipids have the highest incidence rate. In our country, about 40% of adults have elevated blood lipids. For the treatment of high blood lipids, it mainly relies on taking statins. Before taking statins, many doctors advise friends to take the medication before going to bed at night. Do all statins need to be taken orally before bed? Today, let’s talk about this issue.
How do statins treat high blood lipids?
In lipid profile tests, the main focus is on 4 indicators, including total cholesterol, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and triglycerides. Among these indicators, elevated low-density lipoprotein cholesterol poses the greatest harm to the body.
Low-density lipoprotein cholesterol directly damages the intima of arterial blood vessels, causing intimal inflammation. Subsequently, cholesterol deposits on the vessel wall, leading to atherosclerosis. Over time, atherosclerotic plaques form on the arterial wall, causing vascular narrowing, and even rupture, detachment, leading to critical complications such as heart disease and stroke.
Only 20% of cholesterol comes from food absorption; the remaining 80% is synthesized by the liver itself. This is why many friends who are not overweight and are mindful of their diet still find elevated cholesterol levels in lipid tests. Statins cannot prevent the absorption of cholesterol but can inhibit cholesterol synthesis in the liver.
Cholesterol synthesis in the liver involves the participation of HMG-CoA reductase. Statins mainly achieve the goal of inhibiting cholesterol synthesis by suppressing the activity of HMG-CoA reductase.
Why do doctors recommend taking statins before bedtime?
As mentioned earlier, cholesterol synthesis requires the involvement of HMG-CoA reductase. Statins mainly inhibit the activity of HMG-CoA reductase to suppress cholesterol synthesis. The activity of HMG-CoA reductase fluctuates within 24 hours, reaching its peak around midnight at 12 o’clock. This is one of the reasons why doctors recommend taking statins before bedtime.
Currently, there are a total of 7 statins used in clinical practice. These include simvastatin, pravastatin, lovastatin, fluvastatin, pitavastatin, atorvastatin, and rosuvastatin. Simvastatin, pravastatin, and lovastatin belong to the first generation of statins, with the earliest clinical application, while fluvastatin belongs to the second generation, and pitavastatin, atorvastatin, and rosuvastatin belong to the third generation, with relatively later clinical use.
The characteristics of the first and second-generation statins are a short half-life, approximately 4 hours. Therefore, when doctors first prescribe statins, they recommend taking the medication orally before bedtime to ensure that the drug is still within its half-life around 12 midnight, enhancing its efficacy. This is another reason why doctors recommend taking statins before bedtime.
Do all statins need to be taken orally before bedtime?
Not all statins need to be taken orally before bedtime. Third-generation statins are long-acting drugs. Among these, pitavastatin has a half-life of 11 hours, atorvastatin has a half-life of 14 hours, and rosuvastatin has a half-life of 19 hours. Among these three drugs, only pitavastatin, with a relatively short half-life of 11 hours, is recommended to be taken before bedtime; the other two third-generation statins can be taken at any time of the day.
Observant friends may notice that atorvastatin has a half-life of only 14 hours, which means that if taken in the morning, it does not cover until midnight. The same applies to rosuvastatin with a half-life of 19 hours. Why can they be taken at any time of the day?
Although the half-lives of atorvastatin and rosuvastatin are less than 24 hours, they can still be taken in the morning. By taking them in the morning, even though these drugs have passed their half-life by midnight, their metabolites still have the effect of inhibiting cholesterol synthesis, thus achieving the therapeutic purpose.
Therefore, for atorvastatin and rosuvastatin, they can be taken at any time of the day. Many doctors recommend taking them before bedtime because the habitual use of first and second-generation statins has accustomed them to this dosing schedule. However, for atorvastatin and rosuvastatin, taking them at any time does not adversely affect the efficacy of the drugs.
Summary
Among the 7 statins, aside from atorvastatin and rosuvastatin, it is recommended to take them before bedtime. This is because atorvastatin and rosuvastatin are long-acting lipid-lowering drugs with half-lives of over 14 hours, and their metabolites can still inhibit cholesterol synthesis. Therefore, they can be taken at any time of the day. For other statins, it is best to take them before bedtime because HMG-CoA reductase activity peaks around midnight, and taking the medication at night can effectively inhibit its activity and suppress cholesterol synthesis.
As for the question of whether all statins need to be taken orally before bedtime, let’s stop here for today. If you agree with Dr. Zhang’s viewpoint, feel free to like, comment, or share. Creating content is not easy, so your support is appreciated. If you have other questions or opinions, please leave a comment in the comment section. Good questions also inspire my creativity, and I look forward to your help. I am Dr. Zhang Wei, the exceptional doctor. Until next time.
References
[1] Baigent C, Keech A, Kearney PM, et al. Efficacy and safety of cholesterollowering treatment: prospective metaanalysis of data from 90, 056 participants in 14 randomised trials of statins[J]. Lancet, 2005, 366(9493): 12671278. DOI: 10.1016/S01406736(05)673941.
