英文药名：Lipitor Tablets（Atorvastatin Calcium Hydrate） 中文药名：阿托伐他汀钙片 生产厂家：安斯泰来制药 リピトール錠5mg／リピトール錠10mg 治疗类别名称 HMG-CoA还原酶抑制剂 商標名 Lipitor Tablets 一般名 アトルバスタチンカルシウム水和物（Atorvastatin Calcium Hydrate） 化学名 Monocalcium bis｛（3R, 5R）-7-［2-（4-fluorophenyl）-5-（1-methylethyl）-3-phenyl-4-（phenylcarbamoyl）-1H -pyrrol-1-yl］-3,5-dihydroxyheptanoate｝trihydrate 構造式 分子式 C66H68CaF2N4O10?3H2O 分子量 1209.39 性状 阿托伐他汀钙水合物是一种白色至浅黄色的白色结晶粉末。这是非常易溶于甲醇，不溶于二甲亚砜，极微溶于水或乙醇（99.5）。它逐渐由轻变淡黄白色。 操作注意事项 注意： 该产品一直由内袋的高抗湿性召开质量。 药效药理 1. 药理作用 (1) 胆固醇合成的抑制作用 在衍生的HepG2细胞，阿托伐他汀和选择性和有竞争力的人肝癌细胞抑制HMG-CoA还原酶，在胆固醇的生物合成途径中的限速酶，和胆固醇的合成由乙酸以依赖于浓度的方式。口服阿托伐他汀此外，长抑制肝脏胆固醇的合成大鼠与同类药物相比。 (2) 高脂模型动物的降脂作用 1) 降胆固醇的作用 在胆固醇负荷兔和胆固醇负载迷你猪，阿托伐他汀通过口服给药降低血浆总胆固醇水平，它减少了LDL-胆固醇和血浆载脂蛋白B的值。 在LDL受体缺陷小鼠和WHHL兔，阿托伐他汀降低血浆总胆固醇和LDL-胆固醇的水平。 2) Hypotriglyceridemic的作用 在胆固醇装载小型猪和蔗糖负荷血症大鼠，阿托伐他汀降低血液甘油三酯的水平。 (3) 动脉硬化进展抑制作用 在胆固醇负荷内皮损伤兔和WHHL兔，阿托伐他汀降低动脉粥样硬化病变区域和血管壁的胆固醇含量。 (4) 代谢物的药理作用 在大鼠肝微粒，酰胺键位置的苯环的羟基化的4位是人类（M-1）和2位的主要代谢物的羟基化的（M-2）的1/2至阿托伐他汀它表明HMG-CoA还原酶抑制活性的相同的水平。 (5) 对脂蛋白代谢的作用 在HepG2细胞，阿托伐他汀降低一起细胞内胆固醇含量，增加肝脏LDL受体mRNA的表达水平和肝LDL受体的活性，减少了载脂蛋白B分泌和甘油三酯分泌。在正常的豚鼠，阿托伐他汀连同增加肝脏低密度脂蛋白受体活性，降低了载脂蛋白B分泌。在胆固醇负荷迷你猪，阿托伐他汀降低VLDL-载脂蛋白B的生产速度。在LDL受体缺陷小鼠，阿托伐他汀降低胆固醇分泌速率。在蔗糖负荷大鼠高甘油三酯血症，阿托伐他汀降低甘油三酯分泌率。 2. 作用机序 阿托伐他汀肝HMG-CoA还原酶是用于与代谢调节血液中的胆固醇选择性和竞争性抑制的量，一起具有活性的阿托伐他汀顺序相同的主要器官，抑制胆固醇的肝合成。其结果是，阿托伐他汀增加肝脏的LDL受体数目，并通过抑制脂蛋白的分泌来降低血液中的脂肪。此外，阿托伐他汀是改善血脂动力学，抑制动脉硬化的发展，由于高胆固醇血症。 适应病症： 杂合子家族性或非家族性高胆固醇血症和混合性高脂血症，也用于纯合子高胆固醇血症。 用法用量： 可在任何时间单剂量服用，进食或非进食时均可。起始剂量为10mg，qd，剂量范围为10～80mg·d-1。根据治疗目标和治疗反应采取个体化治疗方案。对肾功能不全患者，不必调整剂量. 包装规格 片： 10毫克 100片（10片×10） 500片（10片×50） 500粒（瓶） 700片（14片×50） 1000片（10片×100） 5毫克： 100片（10片×10） 500片（10片×50） 500片（瓶） 1000片（10片×100） http://www.info.pmda.go.jp/go/pack/2189015F1023_1_34/ 生产商：安斯泰来制药 营销联盟:辉瑞公司日本 Lipitor是一种治疗其总胆固醇升高，低密度脂蛋白胆固醇升高，载脂蛋白B升高和甘油三酯升高。在纯合子家族性高胆固醇血症患者，阿托伐他汀钙可与其他降脂疗法合用或单独使用（当无其他治疗手段时），以降低总胆固醇和低密度脂蛋白胆固醇。 Lipitor Tablets（Atorvastatin calcium hydrate） Lipitor Tablets 5mg（リピトール錠5mg） Brand name : Lipitor Tablets 5mg 　Active ingredient: Atorvastatin calcium hydrate 　Dosage form: pale pink tablet (φ: 5.6mm, thickness: 2.7mm) 　Print on wrapping: (Face) リピトール5mg, house-mark + 715, (Back) リピトール5mg, house-mark, company's name Lipitor Tablets 10mg（リピトール錠10mg） Brand name : Lipitor Tablets 10mg 　Active ingredient: Atorvastatin calcium hydrate 　Dosage form: white tablet (φ: 6.1mm, thickness: 2.7mm) 　Print on wrapping: (Face) リピトール10mg, house-mark + 716, (Back) リピトール10mg, house-mark, company's name Effects of this medicine This medicine prevents production of cholesterol in the liver, and thus lowers the cholesterol levels in the blood. It is usually used for the treatment of hypercholesterolaemia or familial hypercholesterolaemia. Before using this medicine, be sure to tell your doctor and pharmacist If you ever experienced any allergic reaction (itch, rash etc.) to any medicine. If you have liver or renal disorder. If you are pregnant or breastfeeding. If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> ?General dosage regimen: For hypercholesterolaemia: For adults, take 1 tablet (10mg of atorvastatin) at a time, once daily. The dosage may be adjusted according to the patient's age and symptoms. For severe patients, the dosage may be increased up to a maximum dose of 2 tablets (20 mg) per day. For familial hypercholesterolaemia: For adults, take 1 tablet (10mg of atorvastatin) at a time, once daily. The dosage may be adjusted according to the patient's age and symptoms. For severe patients, the dosage may be increased up to a maximum dose of 4 tablets (40mg) per day. In either case, strictly follow the instructions of your doctor/pharmacist. ?If you have missed a dose, take the missed dose as soon as possible before bedtime. DO NOT take double doses to make up for the missed dose. ?If you took too much of the medicine (more than ordered), check with your doctor/pharmacist. ?Do not stop taking the medicine without the instructions of your doctor. Precautions while taking this medicine Strictly follow the instructions on dietary/exercise therapy. Intake of grapefruit juice may enhance the effect of this medicine. Refrain from taking the medicine together with grapefruit juice. Possible adverse reactions to this medicine Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: stomach discomfort, itching, numbness of the fingers, loss of sleep, diarrhoea, heartburn, constipation, headache, general malaise, etc. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. muscle pain, feeling of weakness, reddish brown urine  [rhabdomyolysis, myopathy] ?queasiness/vomiting, general malaise, yellowing of the skin and the whites of the eyes  [hepatitis fulminant, hepatitis, hepatic function disorder, jaundice] pharynx pain/headache/heaviness of the head, general malaise, bleeding of nose/gums or under the skin  [agranulocytosis, pancytopenia, thrombocytopenia] fever, loss of appetite, red rash  [oculomucocutaneous syndrome, toxic epidermal necrosis, erythema multiforme] dry mouth, excessive drinking/urination, getting tired easily  [hyperglycaemia, diabetes mellitus] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information Keep out of the reach of infants and children. Store away from direct sunlight, heat and humidity. Discard the remainder. Do not store them. Astellas Pharama Inc.Internal Revised: 1/2011 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. http://www.info.pmda.go.jp/go/pack/2189015F1023_1_30/