Today's article on lipid-lowering drugs commemorates a Japanese who is eligible for the Nobel Prize, Sho Endo.
Why commemorate him? There is only one reason, that is, he has made outstanding contributions to human lipid reduction, if you or your parents are taking statin lipid-lowering drugs such as: atorvastatin, rosuvastatin, etc., in fact, you should thank him, because the statin drugs that everyone takes are made by Akira Endo as the founder, this person is the discoverer of the world's first statin - mevastatin, known as the "father of statins". Unfortunately, he passed away three weeks ago at the age of 90, and his research results have had a profound effect on the prevention and treatment of cardiovascular and cerebrovascular diseases, not only saving the lives of tens of millions of patients around the world, but also bringing them a longer life and a better quality of life. Although mevastatin has never entered the market, Akira Endo's research contributions have undoubtedly laid a solid foundation for subsequent statin drug development.
Penicillin may be familiar to everyone, it is one of the greatest discoveries of the last century, and the second greatest discovery is statins, which can reduce bad cholesterol, inhibit vascular endothelial inflammatory response, treat and prevent cardiovascular and cerebrovascular related diseases, today I will re-sort out the advantages and disadvantages of statin drugs, and explain the applicable groups of drugs in plain language, I hope you will read patiently!
Illustration of 7 statins
There are three generations of statin descendants:
First generation: simvastatin, pravastatin, lovastatin
Second generation: fluvastatin
Third generation: atorvastatin, rosuvastatin, pitavastatin
Grandparents, fathers, and grandchildren have their own statins and differences, so let's take a look at them today.
- Lovastatin
Back in 1979, Professor Endo successfully extracted an active ingredient from Monascus monascus, and this discovery was subsequently transformed by Merck into the world's first commercial statin drug - lovastatin, and statin was born! It is the same as the drug Xuezhikang carefully developed in the early 90s in China, when japonica rice was used as a culture medium and inoculated with Monascus, and since then, China has also had a lipid-lowering "natural statin" --- Xuezhikang.
If you want to ask: which is better, lovastatin or hemolipid? Of course, it's good blood lipids! Because it is a Chinese medicine, because it is natural, because it has more medicinal ingredients, it is better absorbed! I'm sorry to digress, let's move on to lovastatin.
Truly! The first product produced lovastatin is often immature, a serious side effect is easy to cause liver damage, many people because of eating it aminotransferase inexplicably high, headache, dizziness and other symptoms are more common, as a lipophilic statin, lovastatin can not get rid of the characteristics of lipophilic drugs: fat-soluble statin affects the central nervous system, dizziness, headache, easy to penetrate the liver cell membrane, damage liver cells. Lovastatin metabolism mainly depends on the liver enzyme CYP3A4 system metabolism, and atorvastatin is a channel, so those who often eat atorvastatin are intolerant, and almost all of them are intolerant to lovastatin, of course, atorvastatin is a high-intensity statin, much more awesome than lovastatin, lovastatin is a low-intensity statin at best, which is more suitable for friends with mildly elevated blood lipids. Don't use it if you have a headache! If you have pain, fatigue, increased creatine kinase, or myolysis in a certain muscle of the body, do not use it, and if you drink alcohol for a long time, do not use it. If you want to use it, use Xuezhikang to replace lovastatin, maybe the side effects are milder.
- Simvastatin
Simvastatin, the lipid-lowering effect is not very strong, and the strength is rated as medium, but there are not a few applicants, and it is very suitable for friends who do not have high blood lipids! Simvastatin, also known as an "old qualification" statin, was launched in 1988 and was the second statin to be applied to the general public. Now the older generation of cardiologists love to use simvastatin, after all, up to now, the drug research has been sufficient, and any positive and negative effects can be announced to the public.
Simvastatin's poor lipid-lowering strength is actually directly related to the dosage, 10mg per day often does not reduce blood lipids well, and increasing the dose to 20mg or the maximum amount of 40mg may reduce the LDL level by about 6%-40%. Therefore, there are international regulations that any statin that does not reduce lipids by more than 40% will be classified as low- and medium-intensity statins.
Simvastatin is a bit like a "short-acting drug", but it is not a short-acting drug in the real sense, but after oral administration of this drug, the blood concentration is not very stable, and within a day, the lipid-lowering effect of the drug in the body is different, so in order to better reduce blood lipids, doctors often let you take simvastatin at night, so that the cholesterol synthesized mainly at night can be slowed down or stagnant, and simvastatin should have a lipid-lowering effect.
Simvastatin has many adverse reactions, most of the people who take this medicine have abnormal liver function, mainly because many people do not have the consciousness to check the liver and kidney function, and do not know that their liver and kidney indicators are high, if you do a physical examination every year, it is better, to focus on the two indicators of aspartate aminotransferase and alanine aminotransferase, although the increase does not mean liver damage, but if the aminotransferase is increased more than 3 times the normal value, it is necessary to pay attention to it, and it is a wise choice to stop the drug immediately.
Simvastatin may cause muscle damage, and creatine kinase (CK), which is an essential monitoring item for taking simvastatin, exceeds 5 times the upper limit of normal, and the drug is often discontinued. If you have severe myalgia, muscle weakness, and soy sauce-colored urination, then you are in trouble, be alert to the presence of rhabdomyolysis, stop the drug immediately and seek medical attention.
- Pravastatin
Although pravastatin has a mediocre lipid-lowering force, it has several advantages:
Minimal effect on blood sugar: Statins, which generally raise blood sugar, especially during long-term use, can indeed cause blood sugar to rise. Thankfully, pravastatin has an advantage in this regard. The risk of elevated blood sugar is almost non-existent.
It doesn't hurt the liver very much: pravastatin is metabolized through the liver and kidney organs, two pathways, one organ has a problem, and it can be compensated by the other organ, just like two water pipes, this faucet does not flow, the faucet will flow, and it can't be blocked at all, therefore, pravastatin is very friendly to the liver, and the requirements for the kidneys are not so strict.
Weak myoscopy: Muscle pain is particularly common when taking pravastatin, while soy sauce-colored urine and kidney damage are less likely to occur. The incidence of severe rhabdomyolysis is also low.
It has little effect on the nervous system: fat-soluble statins can penetrate the blood-brain barrier and cause symptoms such as insomnia, headache, dizziness, and poor memory, while pravastatin is a water-soluble statin, which does not enter the blood-brain barrier, so there is no need to worry about these side effects.
The combination of drugs is safe: we have an enzyme system in our liver called CYP3A4, which most drugs rely on for digestion. With this plug-in, the medicine we take can be accepted and utilized by the body. But the problem is that when we get older, the CYP3A4 ability in the body may become weaker, and the complexity of taking drugs will inevitably cause the drugs to accumulate in the body and bring trouble to the body. At this time, pravastatin is particularly friendly. Because it is not dependent on CYP3A4 in the metabolic process, the possibility of conflict with other drugs is greatly reduced, and the impact on the body is also small.
Although pravastatin has many advantages, it also has many disadvantages, mainly two points:
The effect of lowering blood lipids is average: pravastatin reduces the range of density lipoprotein by only about 30~50%, and at the moderate intensity level, when it is increased to a maximum of 40mg, it can only increase the lipid-lowering intensity by 6%. It can be said that some people with high blood lipids do not have a high attainment rate even if they use pravastatin, so doctors sometimes do not want to recommend this drug to lower lipids.
Short duration of action: there is a reductase enzyme in the liver, and pravastatin can inhibit it in order to lower lipids, however, the highest activity of this enzyme is at 0:00 in the morning. However, the half-life of pravastatin is about 2 hours, in order to inhibit this enzyme more vigorously and achieve the purpose of lowering lipids, pravastatin must be used at 10 o'clock before sleeping, which is really inconvenient for some people who love to forget.
- Fluvastatin
It is the first fully synthetic and only statin that is mainly metabolized by CYP2C9, and the chemical liquor blended is of course cheap, but the chemically made fluvastatin is not very cheap, but fortunately, it is well tolerated by most people, and in clinical trials, only 2% of people had to stop taking it because of side effects such as muscle pain, muscle wasting, and elevated liver aminotransferases.
There are several categories of people who are contraindicated for fluvastatin:
1. People with cholestasis and blocked bile ducts;
2. People with active liver disease such as gradual decline in labor ability, fatigue, poor appetite, etc.;
3. People who have continuously elevated liver enzymes that cannot find a trigger;
4. Pregnant people and women of childbearing age who do not use contraception are prohibited, because fetal development requires cholesterol and cannot be excessively lowered.
When choosing to take fluvastatin, the intensity of the medication needs to vary from person to person. If you feel that you can't tolerate the intense medication, don't push yourself up, and reduce the intensity of the treatment appropriately. It's important to start with a small dose!
Fluvastatin can also cause rhabdomyolysis and cause kidney failure, especially in people who are severely infected with pathogenic microorganisms, who have had major surgery, who have suffered severe trauma, who have severe metabolic endocrine and electrolyte disorders, renal insufficiency, dermatomyositis. It is recommended to temporarily stop fluvastatin and wait until it is critical.
Fluvastatin is kidney-friendly, and for those with mild to moderate renal insufficiency, you can take fluvastatin with confidence without adjusting the dosage. However, if kidney function is already severely impaired, then caution should be exercised.
People who have drunk too much alcohol or have liver problems should also be careful when using it. After all, fluvastatin is a drug, and it still has a slight effect on the liver. Children under the age of 18 do not need to consider fluvastatin.
- Atorvastatin
Atorvastatin can be said to be the most used statin, it is a star drug, it has saved too many lives, but also too many patients have been "devastated", in the experience to learn a lesson, we can draw the following 7 atorvastatin side effects, if you are also taking, you must pay attention:
1. Liver damage: Atorvastatin is mainly metabolized by the liver and may lead to elevated aminotransferases. Therefore, it should be used with caution in patients with pre-existing liver function abnormalities such as hepatitis, liver cirrhosis, and liver cancer, as well as patients with elevated aminotransferases due to alcohol abuse and other liver-damaging drugs. Liver function should be monitored regularly while taking the drug.
2. Elevated blood sugar: Atorvastatin may cause blood sugar to rise, increasing the risk of diabetes. Caution should be exercised in patients who already have diabetes or whose blood glucose is borderline, and consider statins that have less effect on blood glucose.
3. Muscle pain and rhabdomyolysis: Some patients may have muscle pain after using atorvastatin, and in severe cases, rhabdomyolysis may occur. In the event of such symptoms, prompt medical attention should be sought and discontinuation should be considered.
4. Affect fetal development and sexual function: Atorvastatin may affect fetal development, so pregnant women, lactating women and women of childbearing age should be contraindicated. In addition, male patients may also experience decreased sexual function.
5. Gastrointestinal reactions: Atorvastatin may cause gastrointestinal reactions, such as constipation, bloating, indigestion, etc. Patients with mild symptoms can continue to take the drug, and those with severe symptoms should consider changing the drug or adding a prokinetic drug.
6. Neurological problems: Some patients may have insomnia, nightmares and other neurological problems after using atorvastatin. For patients with severe symptoms, discontinuation or timing of the drug should be considered.
7. Allergic reactions: Patients who are allergic to atorvastatin should be contraindicated. Allergic reactions may manifest as severe symptoms such as dyspnea, shock, and syncope, and should be treated immediately if they occur.
- Rosuvastatin
Rosuvastatin and atorvastatin are good brothers, but sometimes some people are not suitable for atorvastatin and are suitable for rosuvastatin, and the two can be substituted for each other. Rosuvastatin's lipid-lowering power is on par with, or even surpasses, of atorvastatin. As a hydrophilic statin, rosuvastatin performs well in reducing side effects, and has the advantages of hydrophilic statins, which I have already talked about before, and I will not repeat them here. With proper medication, it can reduce blood levels of low-density lipoprotein cholesterol (LDL-C) by 25% to up to 50%.
1. Side effects:
1. Muscle pain
- Some patients experience muscle pain after taking the drug.
- If this side effect occurs, a creatine kinase test is required.
- If you are abnormally elevated, you may have rhabdomyolysis and you need to seek medical attention immediately and stop taking the drug if necessary.
2. Impaired renal function
- 90% of rosuvastatin is metabolized by the kidneys and can damage the kidneys.
- The impact is generally not significant in healthy people, but patients with severe renal dysfunction should be selected carefully.
3. Impaired liver function
- Although only 10% is metabolized by the liver, it may cause abnormal transaminases due to its action on the liver.
- If the aminotransferase elevation exceeds 3 times the normal high value, the drug should be adjusted under the guidance of a physician.
4. Other common side effects
- Compared to other statins, rosuvastatin has less significant side effects.
- It has a strong lipid-lowering effect and does not affect the function of the nervous system.
2. Precautions for taking rosuvastatin
1. Check after taking the medication
- After taking the drug for about 3 months, you need to check your blood lipids and liver function before you decide whether to continue.
2. Genetic and environmental factors
- Hyperlipidemia based on genetic factors, the possibility of stopping the drug is small, and it is recommended to reduce the dose appropriately to maintain it.
- For hyperlipidemia caused by dietary factors, the drug can be discontinued after improving lifestyle habits.
3. Drug reduction and drug withdrawal
- For the purpose of lowering lipids, you can try to reduce or stop the drug after the blood lipid is normal, but you need to recheck it regularly.
- People with secondary prevention of cardiovascular and cerebrovascular diseases are recommended to take it for life.
During the period of taking rosuvastatin, if you find side effects such as abnormal blood sugar, myalgia, liver function damage, kidney function damage, etc., you need to seek medical attention in time for adjustment.
Pitavastatin
Pitavastatin is a statin drug developed in Japan and launched in 2003 as a third-generation product. Don't look at this big white pill is not very famous, it can be used a lot, although pitavastatin is the last statin on the market, its lipid reduction is only above average at best.
Do you know? Cholesterol is one of the main culprits in hardening blood vessels, and pitavastatin is effective in lowering bad cholesterol (LDL-C) and triglycerides (TG) in the blood, while also helping to increase the level of high-density cholesterol (HDL-C). In particular, pitavastatin is more effective than other drugs in raising HDL-C.
The price of pitavastatin is a bit expensive, which may be one of the reasons why it is not used by many people. However, it has relatively few side effects, which is one of its advantages. It has a small effective dose that only needs to be eaten once a day, and the therapeutic doses are 1 mg, 2 mg, and 4 mg, respectively. In contrast, other statins come at much larger doses. This is because pitavastatin has a special property, that is, after it works in the liver, it is excreted through bile into the intestines, and then it is reabsorbed by the intestines and returned to the liver to continue working. This repeated cycle allows it to exert its therapeutic effect in only a small dose. Pitavastatin has very little or no effect on blood sugar. This is a boon for patients who are concerned that statins can trigger blood sugar problems.
Pitavastatin does not conflict with other drugs.
The incidence of side effects of pitavastatin is relatively low. While pitavastatin can also have side effects, it can cause elevated aminotransferases or muscle damage. But because of its smaller doses, the chances of these side effects are also lower.
Overall, pitavastatin, although not the most powerful statin, has a number of unique advantages, such as a small dose, low effect on blood sugar, less interaction with other medications, and a low incidence of side effects.
Summary:
The strongest lipid-lowering effect - rosuvastatin, atorvastatin
A statin that does not harm the kidneys - atorvastatin
Statins that do not harm the liver - rosuvastatin, pitavastatin
Statins that are not affected by time and food – atorvastatin, rosuvastatin, pitavastatin
Relatively small impact on muscles and nerves - pravastatin, pitavastatin
Statins suitable for the elderly - pravastatin, rosuvastatin
The cheapest statins – simvastatin, rosuvastatin, atorvastatin
Anti-aging statins – simvastatin, lovastatin, atorvastatin
Statins that do not affect blood sugar – pravastatin, pitavastatin
I hope that through this summary of statin drugs, you will be given some inspiration, thanks for watching! #头条首发挑战赛