I. Lovastatin
1August 3, 9871,lovastatin was approved to be listed by the FDA of the United States, and it is the first statins listed in the world. After the listing, the sales were not ideal, and now the United States has withdrawn from the market. Although there are 4 dosage forms and more than 0 manufacturers in China, the sales volume is very small, and the sales volume of sample hospitals in 20 16 years is only about 2.3 million yuan. At present, there is no enterprise to evaluate the consistency of this variety (the state requires that generic drugs should be consistent with the quality and efficacy of the original drug). Specifically, the impurity spectrum is consistent, the stability is consistent, and the dissolution law in vivo and in vitro is consistent. ) It is very likely that lovastatin will also withdraw from the China market.
Second, pravastatin.
Pravastatin is a chemical structure modifier of lovastatin, which was first developed in Japan. 199 1 was approved by FDA to be listed in many countries in Europe and America, and was approved to be listed in China in 2004. Pravastatin is a hydrophilic statin derived from microorganisms, which is seldom metabolized by cytochrome P450 enzyme system in liver. It has the characteristics of fast oral absorption, low protein binding rate and few adverse reactions in the elderly.
Three. simvastatin
Simvastatin was developed by Merck, USA, and was approved by FDA in February of 199 1. Simvastatin is a drug for the treatment of primary hypercholesterolemia. Simvastatin 1997 was introduced to China from Merck. Simvastatin is a kind of drug that regulates blood lipid in recent years, and its utilization rate in hospitals has steadily increased.
Simvastatin is a fat-soluble substance, which is taken in the form of inactive lactone and converted into active acid in the body. Its content in liver tissue is high, and its activity in vivo is four times that of pravastatin, which can effectively prevent the development of atherosclerosis and the recurrence of heart disease, and reduce the risk of non-fatal myocardial infarction and myocardial revascularization. Simvastatin has a good market in Beijing and Shanghai.
Four. Fluvastatin
Fluvastatin is a second-generation fully synthetic lipid-regulating product, which was developed by Novartis in Switzerland. In February, it was approved by the FDA of the United States, 1993, 1, and listed in Britain and the United States the following year. Its patent will expire in June, 20 1 1. Novartis introduced this product to China on 1997, and it was protected by patent in China.
Fluvastatin is a water-soluble substance, 80% of which is metabolized after being absorbed in the body and excreted through the intestine, and its pharmacodynamics is 4.4 times that of lovastatin. The drug is not easy to penetrate the blood-brain barrier, has little influence on the central system, and has no tissue residue, so it is a drug for treating familial hyperlipidemia.
Verb (abbreviation of verb) Atorvastatin (hypolipidemic drug)
Atorvastatin is a newly synthesized selective HMG-CoA reductase inhibitor, which is recognized by the medical community as superior to natural microbial fermentation and semi-synthetic statins. When used by patients, the initial dose has excellent lipid-regulating rate. Atorvastatin is the most popular statin in China at present, but its clinical application is gradually limited due to its excessive dosage and many adverse reactions.
6.rosuvastatin
Rosuvastatin, known as "super statin", was first developed abroad with an initial dose of 20mg. Because of ethnic differences, 20mg statins abroad have great side effects on China people. In order to explore statins suitable for China people's physique, Lunan Pharmaceutical began to try to reduce the drug dosage to 5mg without affecting the therapeutic effect, which opened the precedent for statins to treat China. 5mg statin is developed according to the pharmacokinetics of China people, which is more suitable for the physique of China people. Its lipid-lowering effect is equivalent to atorvastatin 20mg, but the side effects are greatly reduced and the price is more favorable, which opens a new era of statin lipid-regulating.
Seven, pitavastatin
In August 2003, pitavastatin was developed and marketed in Japan. In 2008, 9 copies were put into the China market. So far, there is no large-scale experiment on pitavastatin, which is not very promising at home and abroad. On the other hand, price and self-financing are a big "soft rib". The lipid-lowering effect is also a big deficiency. When the maximum dose reached 4mg, the LDL-C level decreased by 465,438 0%, while the LDL-C levels of 20mg and 80mg rosuvastatin decreased by 55%.
Statins are dazzling in the market. Although they are all HGM-CoA reductase inhibitors, their safety and lipid-lowering effects are quite different due to structural differences. As the saying goes, a thousand miles a day. Therefore, to take statins specifically, we should follow the doctor's advice according to our physical condition.