released soon. At present, HMG-CoA reductase inhibitor (statin drug) and fibrate drugs are mainstream in hyperlipidemia drug therapy, but ezetimibe is a drug having a different action mechanism from these existing drugs There will be new options for treatment of hyperlipemia in our country.
In the treatment of hypercholesterolemia, one of hyperlipemia, it is essential to inhibit the biosynthesis of cholesterol in vivo, or to inhibit the absorption of cholesterol from a meal or the like. Statin medicines, which are the mainstream of current high cholesterol therapy, are drugs that inhibit the biosynthesis of cholesterol mainly in the liver, whereas ezetimibe approved this time inhibits the absorption of cholesterol from the small intestine Improve hypercholesterolemia by doing it. Specifically, it has an action of inhibiting the "small intestinal cholesterol transporter" involved in absorption of cholesterol from the small intestine.
It is responsible for the sterol transport function and is present on the upper border membrane of the upper part of the small intestine. By inhibiting this, the same drug reduces the absorption of bile and dietary cholesterol by 54%. In addition, in data in Europe and the United States, even in cases where administration with statin drugs with different action mechanisms did not show sufficient effect with administration of statin drug alone, significant cholesterol lowering (LDL cholesterol lowering ) Effect has been recognized.
In addition to this, (1) it has indication of "homozygous sitosterolemia" which is not present in existing oral medicine, in addition to hypercholesterolemia, familial hypercholesterolemia, (2) Ezetimibe circulates through the intestinal tract and acts on the small intestine locally for a long time, so it can be administered once a day. (3) The major metabolic pathway is glucuronidation conjugation, it is not subject to metabolism involving the hepatic drug metabolizing enzyme cytochrome P450 in vivo, so there is little drug interaction - such as tablets are small and good compliance can be expected It has features. Ezetimibe has been approved in more than 90 countries in the world since it was launched in the United States in 2002 and has already been used for over 10 million patients.
In the future, ezetimibe is thought to be widely used in Japan as a new option in drug treatment of hyperlipidemia, but it is also a drug having a new mechanism of action that has never existed, and side effects etc. You will need to pay sufficient attention to it.
This transporter, which is the target of ezetimibe,
The occurrence rate of side effects in domestic clinical trials was 18.8%, and the main things were constipation, rash, diarrhea, abdominal pain, abdominal bloating feeling, nausea · vomiting. Laboratory test value abnormality was found at 12.1%, and γ-GTP increase, CK increase, ALT increase, etc. were reported. Also serious side effects include anaphylaxis, vascular neural edema, hypersensitivity including rash, rhabdomyolysis, and myopathy. Among these cases, statin drugs were administered mostly in cases where rhabdomyolysis occurred before administration of ezetimibe. At the present time, it is considered desirable to avoid combinations with fibrate drugs because it is not sufficiently confirmed its efficacy and safety.
产品特点及上市信息：
依泽替米贝是由Schering-Plough和Merck公司合作研制的新型胆固醇吸收抑制剂，于2002年10月被FDA批准上市。
Zetia是降脂药物近15年来的一大创新，是首个获准上市的胆固醇吸收抑制剂，它是200 |
