你很熟悉但卻不一定能準(zhǔn)確說出含義的80個詞匯猶大的親吻,海妖之歌The80stha

1、你很熟悉但卻不一定能準(zhǔn)確說出含義的80個詞匯 猶大的親吻，海妖之歌 (The 80 words that you are familiar with but don'tnecessarily know exactly what it means the kiss of judas, thesong of the siren)According to schering-plough? Products? LLCdrug nameGeneric name: yi-mbukCommodity name: yishi chun? EZETROL?English name: Ezetimibe?

2、 TabletsChinese pinyin: Yizhemaibu? Pian【composition 】According to fold the mabChemical name: 1 -(4 - phenyl) - 3 (R) - 3 -(4 - phenyl) -3 (S) - hydroxypropyl) to 4 (S) -(4 - hydroxyphenyl) - 2 - around organism (nitrogen heterocyclic butane) methadoneChemical formula:The INCLUDEPICTURE "C: Doc

3、uments and Settings Administrator Local Set tings Molecular formula: C24H21F2NO3Molecular weight: 4094【 traits 】 this product is white or whiteindicationPrimary hypercholesterolemiaThis product as an aid in the treatment of die t cont rol out side, independently or with HMG CoA reductase inhibitors

4、(statins) jointly applied in the treatment of primary (heterozygous familial or non familial) hypercholesterolemia, reduces total cholesterol (TC), low-density lipoprotein cholesterol (LDL - C), apolipoprotein B (Apo? B)Homozygous familial hypercholesterolemia (HoFH)This product with statins joint a

5、pplication, can be used as adjuvant therapy of other lipid-lowering therapy plasma separation displacement method (such as LDL - C), or on other lipid-lowering treatment is invalid to reduce HoFH the patient* s level of TC and LDL - C.Homozygotic sterolaemia (or phytosterinemia)As an adjuvant therap

6、y other than diet control, this product was used to reduce the level of sterol and phytosterol inpatients with homozygous family of homozygous families.Specification: 1Omgusage and dosagePatients should adhere to the proper low-fat diet during the treatment of this product.This product is recommende

7、d for a daily dose of lOmg, which can be used alone or in combination with statins This product may be taken at any time of the day, but may be taken on an empty stomach or with foodApplication of drugs in elderly patientsElderly patients do not need to adjust the doseThe use of drugs in childrenChi

8、ldren and adolescents aged more than 10 years: no need to adjust the dosageChildren less than 10 years old： do not recommend this productDrugs are used in patients with impaired liver functionPatients with mild liver dysfunction do not need to adjust the dose (child-pugh scores are 5 or 6) (see phar

9、macokinetics)Drugs are used in patients with impaired renal functionPatients with renal impairment do not need to adjust the dose.In combination with the cholic acidYou should take this product more than 2 hours before you take the gacin, or more than 4 hours after taking it.adverse reactionsIn 814

10、weeks of clinical study, 3366 patients a day aloneor with statins combined use of 10 mg, the resuIts show that the patients generally to this product is well tolerated, adverse reactions to mild and transient, the overall incidence of side effects similar to placebo, experimental group by adverse re

11、actions caused by the termination rate with the placebo groupIn patients with a single application (n = 1691), and in patients with statins (n = 1675), common (= 1/100,1/10) the adverse reactions associated with drugs are as follows:Apply this product alone: headache, abdominal pain, diarrheaCombine

12、d with statins: headache, fatigue; Abdominal pain, constipation, diarrhea, bloating, nausea; ALT elevation, AST elevation; Muscle pain.Laboratory indicators:In a controlled clinical study of the product alone, this product (0.5 %) and placebo (0. 3 %) resulted in a similar incidence of transaminase

13、(ALT and/or AST, 3 times greater than normal value) In the study of the combined application of this product and statins, the incidence of aminotransferase in patients with combined application and statins was 1.3%, and the incidence of the patients with statins alone was 0. 4 % However, the transam

14、inase was not clinically present and had nothing to do with the stasis of bile, and was reduced to normal after the interruption or continued treatmentThe increase of CPK (greater than 10 times the upper limit of normal value) resulting from the application of this product or the combined applicatio

15、n of statins is similar to that of a placebo or individual application of statinsAdverse reactions (ignoring causality) of the report after the product is listed: allergic reactions, including anaphylaxis, vascular neuroedema, rashes and urticaria; Joint pain; Muscle pain; CPK increases; Liver trans

16、aminase increased; Hepatitis; Thrombocytopenia; Pancreatitis; Vomiting; Gallstones Cholecystitis. Myopathy/rhabdomyolysis is very rare【taboo】Allergic to any component of this productPatients with active liver disease, or unexplained serum transaminase, continue to riseAll HMG 一 CoA reductase inhibit

17、ors are restricted to pregnant and lactating women When the drug is combined with these drugs for potential delivery possibilities, refer to the HMG CoA reductase inhibitor product label (see pregnant and lactating women)Note:Please refer to the instructions for the use of statins when this product

18、is combined with statins.Liver enzyme actionIn the control study of the combined application of this product and statins, serum transaminase was found to be increased continuously (three times the upper limit of the normal value) Therefore, when the product is combined with statins, the liver functi

19、on should be measured before treatment, and the statins should be referred to.Skeletai muscleIn clinical studies, compared to the control group (placebo or individual statins), the myopathy and rhabdomyolysis of the muscle were not found Myopathy and rhabdomyolysis are known adverse reactions to sta

20、tins and other lipid-lowering drugs 10 times this product cause CPK is greater than the upper limit of normal incidence was 0. 2%, the incidence of placebo was 0. 1%, the product with statins incidence was 0. 1%, incidence of 0. 4% with statins alone After this product has been listed, the case of m

21、yopathy and rhabdomyolysis has been reported(whether the myopathy and rhabdomyolysis are related to the drug is not clear. Most patients with rhabdomyolytic symptoms are taking statins before taking the product. However, when using this product and the drug associated with the known increase of the

22、risk of rhabdomyolysis, it is rare to report the case of rhabdomyolysis. All patients should be informed of the risk of myopathy and be told to report any unexplained myopathy, tenderness, or weakness If the patient is diagnosed or suspected of myopathy,This product should be discontinued immediatel

23、y and any of the statins that are being used The above symptoms and CPK level > 10ULN indicate the occurrence of myopathy.Hepatic insufficiencyIt is not recommended for these patients to apply this product (see pharmacodynamics), given that the influence of the long-term use of imbuteron in patie

24、nts with moderate or severe liver function is not clearBetty classCurrently, the safety and effectiveness of the combination of the present and bette classes have not been established, so the two drugs are not recommendedcyclosporineThis product should be used carefully during the use of cyclosporin

25、e. The concentration of cyclosporine should be monitored for patients receiving the combination of thisproduct and cyclosporine.anticoagulantsThe international standardized ratio (IXR) should be properly monitored when other coumarin anticoagulants or fluorinindione are used for the use of this prod

26、uct and the Chinese lawmedication for pregnant and lactating womenThere is no clinical data on pregnancy medication. Animal experiments show that the product has no direct or indirect adverse effects on pregnancy, embryo and fetal development, birth and birth However, pregnant women should still use

27、 this product carefully.In the study of rats in pregnancy, this product has not been deformed by the combined application of lovastatin,simvastatin, provastatin and atorvastatin. In the study of the pregnant rabbits, a small amount of bone deformity was observedThe study of rats found that ezetimibe

28、 was secreted from the breast of rats. It is not yet certain whether or not it can be produced by human breast milk, so unless it can be proved that its poten tial benefits out weigh the pot ential risks to infants, this product should not be used for breastfeeding women.Children，s medicationThe abs

29、orption and metabolism of this product in children and adolescents (10 ' 18 years old) is similar to that of adult patients. The pharmacokinetics of adolescents and adults were not different according to the plasma concentration of the total ezetimibe. No pharmacokinetic data for children under

30、10 years of age Clinical data of children and adolescents (9 to 17 years old) are limited to HoFH and the patients with the diseaseelderly patient medicationElderly patients (older than 65) were twice as likely to have been in the plasma concentration of their younger patients (18 to 45 years old) T

31、he reduction and safety of LDL - C after drug use were no significant difference between older and younger patients. Therefore, elderly patients need not adjust the dosagedrug interactionsThe preclinical study indicated that this product did not induce cytochrome P450 drug metabolism enzyme There wa

32、s no clinical pharmac ok i ne t i c interaction between the product and the known drugs that could be metabolized by cytochrome P450, 1A2, 2D6, 2C8, 2C9, 3A4, or n-acetylase.This product with dapsone, dextromethorphan, digoxin, oral contraceptive (ethinyl estradiol and acetylene connaught progestero

33、ne from left), glipizide, a sugar or midazolam drugs such as joint applications, not found this product affect the pharmacokinetics of the drugs Cimetidine does not affect the bioavailability of this product when it is used in combinationwith this productAntacid: taking antacids at the same time can

34、 reduce the absorption rate of the product without affecting its bioavailability This decrease in absorption rate is not clinically significantAnticholamine: at the same time, the use of anticholamine can decrease the average AUC about 55 % of the average AUC The enhancement effect may be reduced du

35、e to the interaction of the reduction of LDL - C by adding this product on the basis of the anticholamineCyclosporine: in one study, eight patients after renal transplantation of the creatinine clearance > 50 ml/min and stable in taking cyclosporine, single after taking 10 mg according to fold th

36、e mab, the average total according to fold the mab AUC value with another study (n = 17) compared to healthy population has increased 3. 4 times (from 2. 3 to 7.9 times) In another study, a kidney transplant patients with severe renal insufficiency (creatinine clearance of 13.2 ml/min / 1.73 m2) and

37、 accept a variety of medications, including cyclosporine, its total exposure levels in accordance with the folding mab increased 12 times compared with the control group In the second phase of 12 healthy subjects crossover study, a daily dose of 20 mg per 8 days, single dose used 100 mg of cyclospor

38、ine in 7 days, compared with the separate application of cyclosporine, AUC value is increased by an average of 15% (range is 10% + 51%)Bette： the addition of fenofibrate or gephirozi increased by 1. 5 times and 1. 7 times respectively, but this interaction had no clinical significance The safety and

39、 efficacy of the combination of ezetimibe and bette drugs has not been established The bette class can increase the concentration of cholesterol in bile, causing gallstones to occur In the dog，s preclinical study, it was found that this product can increase the cholesterol cont ent in bile Although

40、the relevance of the preclinical findings to humans is not known, it is not recommended that this product should be used in conjunction with the bette drugs prior to the studyStatins: the interaction between this product and atorvastatin, simvastatin, prostatin, lovastatin, fluvastatin and rivastati

41、n combined with no clinically significant pharmacokineticsAnticoagulants： the study of 12 healthy men showed that the combination of this product (lOmg/day) with warfarin or fluorindenadione did not significantly affect the bioavailability and clot ting time of the law After the product is listed, t

42、here is a report on the increase of international standardized ratio in patients who have been jointly used with China law. Most of these patients are also receiving other medicationsdrug overdoseIn the clinical study, 15 healthy subjects took 50mg daily for 14 consecutive days, and 18 patients with

43、 primary hypercholesterolemia were given 40mg daily for 56 days and were generally well toleratedThere were a few reports of overdoses, and most of the adverse reactions were not severe In drug overdose, symptomatic and supportive treatment should be carried outclinical researchPrimary hypercholeste

44、rolemiaaloneIn two multicenter, double-blind, placebo-controlled, 12week studies, 1719 patients with primary hypercholesterolemia were treated with 10 mg of this product per day. The resuIts showed that the experimental group was compared with the control group of TC, ldl-c, Apo. B, TG significantly

45、 decreased and increased HDL - C (see table 1 ) In patients with different age, sex, race, and basal ldl-c levels, ldl-c decreased with consistency This product has no effect on the plasma concentration of fat-soluble vitamins A, D and E; It had no effect on thrombin time;In the treatment of statins

46、, it was randomly added to the drug or a placebo.Application in baseline statins do not meet the LDL 一 C control standard of patients (about 82%), in the end of LDL - C control standard of patients in this group and placebo group were 72% and 19% respectively.This study showed that the addition of t

47、his product to the application of statins could significantly reduce the TC, ldl-c, Apo. B, TG plasma conce nt ration, and increased HDL 一 C plasma conce nt ration (see table 4). This product is similar to the effect of lowering ldl-c after combined application of statinsTable 4 The mean variation o

48、f each index of a after the combined drug regimen was accepted by patients with primary hypercholesterolemia (the average variation of the baseline comparison)treatmentN TC ldlc Apo? TGb HDL - C B are taking statins 390-2-4 + placebo (C - 6 mg/dl) - 3-3 + 1 are taking statins, the product 379-17 to

49、25 (- 36 mg/DLC) - 19-14 + 3 a to apply various statins: proportion of patients with 40% atorvastatin and simvastatin, 31% and 29% of other (pravastatin, fluorine cut statin, cut ting statins, the department of lovastatin)B to TG, the median of the change in the value of the baseline valueC) compare

50、d with baseline, the change in LDL 一 c (statin + n) was 138mg/dl, statin + placebo change of 139mg/d1.In a multicenter, double-blind, placebo-controlled, in a period of 14 weeks, 621 are taking atorvastatin and LDL - C is greater than 130 mg/dl in patients with primary hypercholesterolemia were rand

51、omly divided into two groups, one group treated with atorvastatin 20 mg a day, another group received daily atorvastatin 10 mg + 10 mg treatment(in the control index of patients who fail to meet the control target set ting of LDL - C is less than 100 mg/dl), single applica tion of atorvastatin in pa

52、tients with medication can be increased to 80 mg dose, the combined use of atorvastatin and patients, dosage of atorvastatin can improve to 40 mg. In this group, the average baseline ldlc was 187mg/dl, and 60% of the patients were heterozygous familial hypercholesterolemia (HeFH) At the end of the s

53、tudy, 7% of the patients in the individual drug group reached the control target, and the combined drug group reached the control target by 22% The difference was significant In week 4, there was a significant difference between the two groups of LDL - C (24 per cent) and 9 per cent alone. In these

54、patients, the effects of the control of ldl-c were also consistent with the results of the two different treatment regimensIn the design of a similar study, 100 patients treated with simvastatin 20 mg after LDL 一 C control target has not been achieved, it is divided into two groups, one group of sim

55、vastatin + 10 mg treatment, another group only accepted the simvastatin treatment. The results are similar to those of atorvastatin. For example, there was a significant difference in the target of ldl-c control (3 per cent of patients with simvastatin alone, and 27 per cent of patients with combine

56、d drugs) The average rate of LDL - C reduction was 11 per cent in patients alone and 24 per cent for patients with combined drugsHomozygous familial hypercholesterolemiaA used to evaluate the product in the homozygous familial hypercholesterolemia therapy effect of double-blind, randomized, the 12-w

57、eek study, 50 were diagnosed by clinical or genotype homozygous familial hypercholesterolemia patients selected, this group of patients with LDL 一 C not all exceptions, and have been accepted the atorvastatin (40 mg) or simvastatin treatment (40 mg). These patients were divided into three groups, on

58、e group receiving atorvastatin (40 mg) or simvastatin (80 mg), a set of accept the goods 10 mg + atorvastatin (40 mg) or simvastatin (40 mg), and a set of accept the goods 10 mg + atorvastatin (80 mg) or simvastatin (80 mg). The results are shown in table 5. The research results show that the product with atorvastatin (40 or 80 mg) or simvastatin (40 or 80 mg) combined with application, the effects of lowering LDL - C is superior to simvastatin and atorvastatin therapy alone (dose of 40 mg - 80 mg).Table 5 the mean variation of each index of the patients with homozygous