Crestor延缓动脉粥样硬化的进展
据美联社3月25日新闻报道，阿斯利康公司的降胆固醇药物Crestor可以延缓心脏病和中风发作的危险性较低人群颈动脉肥厚的进程，但是它没有像研究人员事先预想的那样可以逆转肥厚。
动脉壁的肥厚是斑块形成的前兆，而动脉斑块可以导致心脏病和中风的发作。Crestor起初被批准用于降低有害胆固醇的水平，但是阿斯利康希望美国药品管理局同意修改这种产品的说明书，以使它能够被用于改善动脉粥样硬化。
就药物本身来说，关于Crestor的新研究可能并不支持Crestor和其它的他汀类药物在心脏病和心血管疾病低危险人群中的更广泛的应用。但是对这个人群的进一步的研究又支持了使用范围的扩大。
威克森林大学医学院心脏病学家John Crouse在美国心脏病学会年会的新闻采访中说：“在我们的研究中，这种药物不仅能延缓疾病的进展，而且能使疾病彻底停滞下来。”这项研究的结果今天就已经公布了，而且它还在网上的«美国医学会杂志»上发表了。
但是这项研究的结果仍然没有像去年的ACC会议上公布的Crestor研究结果那样令人瞩目。那项研究是在有心脏病体征且处于心脏病和中风发作高危状态的人群中进行的。在这些病人中Crestor部分逆转了冠状动脉的斑块形成。
    Crestor战略发展主管James Blasetto说，阿斯利康已经把两个研究的资料呈交给食品和药品管理局，并且希望在年底知道它们是否能够修改说明书上药物在动脉粥样硬化方面的应用。
去年的研究帮助Crestor在2006年的销售额上涨了60％并且超过了二十亿美元。Crestor和另一种上升势头很猛的降胆固醇药物Vytorin（默克公司和先灵葆雅公司联合推出的一种新药）从降胆固醇药物市场的老大――辉瑞公司的立普妥手中抢走了不少的份额，而立普妥是世界上最畅销的药物，它去年的销售额总共达到一百二十九亿美元。这些制药公司在激烈的竞争中都争相展示自己新的临床数据来证明各自产品的优越性。
这项称为Meteor的新的Crestor研究是由阿斯利康资助的，它给予那些冠心病危险性相对较低的人高剂量的此药，而这些人通过超声检查证明有一些颈动脉的肥厚。通常医生都不会给这些低危人群开他汀类药物。
984位参与者服用了Crestor或安慰剂，然后进行随访的超声检查以确定颈动脉壁厚度的变化。在实验中病人们随访了接近两年。
在安慰剂组，颈动脉壁每年增厚了约0.013毫米。在Crestor组却有了0.0014毫米的变薄，但是在统计学上不足以证明有逆转。然而，Crestor组与安慰剂组的差异足以证明Crestor能够显著延缓疾病的进展。
研究还发现Crestor可以导致LDL的49％的降低，还有HDL的8％的升高。
这项研究中最常见的副作用包括了肌肉痛和背痛，但是Crestor组和安慰剂组中这些事件的发生率没有明显的差异。
迄今为止还没有资料证实Crestor能够降低死亡，心脏病发作和其它心血管事件的发生率。而阿斯利康正在进行这类实验来确定结果。

美国FDA批准阿斯利康畅销降脂药Crestor的扩适应症，即用于那些胆固醇水平正常或略高的人士，作预防药物至此，Crestor可用于那些在临床上未发现冠心病迹象的人士，以减少中风、心肌梗塞和接受冠状动脉血管再造术的风险。
这次Crestor扩大适应症通过批准的依据是该药项名为Jupiter的临床试验。结果显示，与安慰剂对照组相比较，受试者用药后心脏病发作的风险降低54%，中风风险降低48%，需要接受冠状动脉再造术的风险降低46%。
需提醒的是，某些适用人群刚开始药物治疗时会增加心血管疾病风险，如年纪偏大（男性50岁以上，女性60岁以上）、高敏C反应蛋白水平增高或存在某项心血管高危因素（如患有高血压或抽烟）等。

学名: Rosuvastatin Calcium (瑞舒伐他汀)

商品牌子名: Crestor (冠脂妥)

药物制造商: AstraZeneca

药理: Rosuvastatin是一种具有选择性、竞争性的HMG-CoA还原酶抑制剂(他汀)，对胆固醇生物合成的限速酶HMG-CoA还原酶有竞争性的抑制作用，使LDL(坏胆固醇)合成减少，同时提升HDL(好胆固醇),因而有改善血脂水平的作用。

用途:
1.适用于经饮食控制和其它非药物治疗仍不能适当控制血脂异常的原发性高胆固醇血症（IIa型，包括杂合子家族性高胆固醇血症）或混合型血脂异常症（IIb型） 。
2.适用于家族性高胆固醇血症的患者，作为饮食控制和其他降脂措施的辅助治疗，或在这些方法不适时使用。

剂量:
每日一次，每次10毫克。亚洲人起始剂量为5mg。
如有必要，可在治疗4周后调整剂量至每日一次，每次20毫克。
对心血管疾病危险性高而20毫克不能达到治疗目标的严重高胆固醇血症（特别是在那些家族性高胆固醇血症）患者，可考虑将剂量加倍至40毫克，并应对他们进行定期监测。

用药禁忌:活性肝病、肝酵素持续高水平、严重的肾功能损害、肌病、同时使用cyclosporin抗排斥药的病人、孕妇、哺乳期妇女。
用药注意:蛋白尿、肌痛、有肌病/横纹肌溶解诱发因素的患者(如肾功能损害、甲状腺机能减退、酒精滥用、年龄>70岁等) ,同时服用ketoconazole, spironolactone, cimetidine等可降低steroid hormone的药物的人士。同时服用华法林(Warfarin)，需要监测INR指数。曾患肝病人士，如肝酵素过高，有可能需要降低药物剂量或停药。

常见副作用:头痛、头晕、便秘、恶心、腹泻、腹痛、肌痛、乏力。
其他副作用:肌病和横纹肌溶解、血管神经性水肿、蛋白尿、瘙痒、皮疹和荨麻疹

药物相互作用: Cyclosporin, gemfibrozil,与rosuvastatin合用可增加rosuvastatin血液中含量。 Rosuvastatin与warfarin合用可加强warfarin作用。 Rosuvastatin与口服避孕药/激素替代治疗(HRT)合用可增加贺尔蒙在血液中含量。 Rosuvastatin与gemfibrozil, fenofibrate, nicotinic acid合用可增加患肌病的机会。

病患者及家属注意事项:
1.可在一天中的任何时候服用
2.可在进食时或空腹时服用
3.如服用后有肌痛情况,请立即求诊

【原产地英文商品名】CRESTOR 20mg/tab 30tabs/box
【原产地英文药品名】ROSUVASTATIN CALCIUM
【中文参考商品译名】冠脂妥 20毫克/片 30片/盒
【中文参考药品译名】瑞舒伐他汀钙
【生产厂家中文参考译名】阿斯利康
【生产厂家英文名】AstraZeneca 

 
Crestor

Generic Name: rosuvastatin (roe SOO va sta tin)
Brand Names: Crestor

What is Crestor?
Crestor is in a group of drugs called HMG CoA reductase inhibitors, or "statins." Rosuvastatin reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

Crestor is used to lower cholesterol and triglycerides (types of fat) in the blood.

Crestor is also used to lower the risk of stroke, heart attack, and other heart complications in people with diabetes, coronary heart disease, or other risk factors

Crestor is used in adults and children who are at least 10 years old.

Crestor may also be used for other purposes not listed in this medication guide.

Important information about Crestor
You should not take Crestor if you are allergic to rosuvastatin, if you are pregnant or breast-feeding, or if you have liver disease. Stop taking this medication and tell your doctor right away if you become pregnant.

Before taking Crestor, tell your doctor if you have ever had liver or kidney disease, diabetes, or a thyroid disorder, if you are of Chinese descent, or if you drink more than 2 alcoholic beverages daily.

In rare cases, Crestor can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Avoid eating foods that are high in fat or cholesterol. Crestor will not be as effective in lowering your cholesterol if you do not follow a cholesterol-lowering diet plan.

Avoid drinking alcohol. It can raise triglyceride levels and may increase your risk of liver damage.

There are many other drugs that can increase your risk of serious medical problems if you take them together with Crestor. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.

Crestor is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

Before taking Crestor
You should not take Crestor if you are allergic to rosuvastatin, if you are pregnant or breast-feeding, or if you have liver disease.

If you have any of these other conditions, you may need to adjust your dose of Crestor or have special tests:
history of liver disease;
history of kidney disease;
diabetes;
a thyroid disorder; or
if you drink more than 2 alcoholic beverages daily.

People of Asian descent may absorb rosuvastatin at a higher rate than other people. Make sure your doctor knows if you are Asian. You may need a lower than normal starting dose.

In rare cases, Crestor can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. This condition may be more likely to occur in older adults and in people who have kidney disease or poorly controlled hypothyroidism (underactive thyroid).

Tell your doctor about all other medications you use. Certain other drugs can increase your risk of serious muscle problems, and it is very important that your doctor knows if you are using any of them:
amiodarone (Cordarone, Pacerone);
danazol (Danocrine);
gemfibrozil (Lopid), fenofibric acid (Fibricor, Trilipix), or fenofibrate (Antara, Fenoglide, Lipofen, Lofibra, Tricor, Triglide);
antibiotics such as clarithromycin (Biaxin), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin), or telithromycin (Ketek);
antifungal medications such as fluconazole (Diflucan), itraconazole (Sporanox), or ketoconazole (Extina, Ketozole, Nizoral, Xolegal);
heart or blood pressure medication such as diltiazem (Cartia, Cardizem) or verapamil (Calan, Covera, Isoptin, Verelan);
HIV medications such as atazanavir (Reyataz), ritonavir (Norvir), lopinavir/ritonavir (Kaletra), saquinavir (Invirase), and others;
medicines that contain niacin (Advicor, Niaspan, Niacor, Simcor, Slo-Niacin, and others); ordrugs that weaken your immune system, such as steroids, cancer medicine, or medicines used to prevent organ transplant rejection, such as cyclosporine (Gengraf, Neoral, Sandimmune), sirolimus (Rapamune), or tacrolimus (Prograf).

FDA pregnancy category X. Crestor can harm an unborn baby or cause birth defects. Do not take Crestor if you are pregnant. Stop taking this medication and tell your doctor right away if you become pregnant. Use effective birth control to avoid pregnancy while you are taking Crestor. Rosuvastatin may pass into breast milk and could harm a nursing baby. Do not breast-feed while you are taking Crestor.

How should I take Crestor?
Take Crestor exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Crestor is usually taken once a day, with or without food. Take the medicine at the same time each day. Your doctor may occasionally change your dose to make sure you get the best results.

You may need to stop using Crestor for a short time if you have:
uncontrolled seizures;
an electrolyte imbalance (such as high or low potassium levels in your blood);
severely low blood pressure;
a severe infection or illness;
dehydration; or
surgery or a medical emergency.

To be sure Crestor is helping your condition and is not causing harmful effects, your blood will need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.

Crestor is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

You may need to take Crestor on a long-term basis for the treatment of high cholesterol. Store at room temperature away from moisture, heat, and light.

What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Crestor?
Avoid using antacids without your doctor's advice. Use only the type of antacid your doctor recommends, and do not take it within 2 hours after taking Crestor. Some antacids can make it harder for your body to absorb Crestor.

Avoid eating foods that are high in fat or cholesterol. Crestor will not be as effective in lowering your cholesterol if you do not follow a cholesterol-lowering diet plan.

Avoid drinking alcohol. It can raise triglyceride levels and may increase your risk of liver damage.

Grapefruit and grapefruit juice may interact with Crestor and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor. Do not increase or decrease the amount of grapefruit products in your diet without first talking to your doctor.

Crestor side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Crestor: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking Crestor and call your doctor at once if you have any of these serious side effects:
unexplained muscle pain, tenderness, or weakness;
fever, unusual tiredness, and dark colored urine;
swelling, weight gain, urinating less than usual or not at all; or
nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Less serious Crestor side effects may include:
headache;
mild muscle pain;
joint pain;
constipation;
mild nausea; or
stomach pain or indigestion.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Crestor?
Before taking Crestor, tell your doctor about all other medicines you are using, especially:
birth control pills;
cimetidine (Tagamet);
a blood thinner such as warfarin (Coumadin);
spironolactone (Aldactone, Aldactazide);
any other "statin" medication such as atorvastatin (Lipitor, Caduet), fluvastatin (Lescol), lovastatin (Altoprev, Mevacor), pravastatin (Pravachol), or simvastatin (Zocor, Simcor, Vytorin).

This list is not complete and other drugs may interact with Crestor. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?
Your pharmacist can provide more information about Crestor.

What does my medication look like?
Rosuvastatin is available with a prescription under the brand name Crestor. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.

Crestor 5 mg - yellow, round, film-coated tablets
Crestor 10 mg - pink, round, film-coated tablets
Crestor 20 mg - pink, round, film-coated tablets
Crestor 40 mg - pink, oval, film-coated tablets

Every effort has been made to ensure that the information provided is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects.