英文药名: Actonel (Risedronate Sodium Tablets)
中文药名: 利塞膦酸钠片
药品名称和成分
通用名称： 利塞膦酸钠片
英文名称： Risedronate Sodium Tablets
本品主要成份为利塞膦酸钠
化学名称： 2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物。
适应症
本品用于治疗和预防绝经后妇女的骨质疏松症。
用法用量
口服用药，需至少餐前30分钟直立位服用，一杯（200ml左右）清水送服，服药后30分钟内不宜卧床。用量为一日一次，一次5mg（一片）。
如果您有任何疑问，请遵医嘱。
不良反应
1、消化系统 可引起上消化道紊乱，表现为吞咽困难、食道炎、食道或胃溃疡，还可以引起腹泻、腹痛、恶心、便秘等；其他如流感样综合征、头痛、头晕、皮疹、关节痛等。
禁忌
以下患者禁用
1、已知对本品过敏者；
2、低钙血症患者；
3、30分钟内难以坚持站立或端坐位者。
孕妇及哺乳期妇女用药
孕妇用药的安全有效性尚未确立，除非疾病本身对母子的危害性更大并无其他更安全药物替代时，才在妊娠期使用本品。
本品对哺乳婴儿有严重的不良反应，哺乳期妇女应停药或停止哺乳。
儿童用药
儿童用药的安全有效性尚未确立。
老年患者用药
临床试验资料表明，老年人和年轻人在服用本品时无安全性和有效性上的差异，但不排除老年人个体对本品具有高敏性。
注意事项
1、服药后2小时内，避免食用高钙食品（例如牛奶或奶制品）以及服用补钙剂或含铝、镁等的抗酸药物。
2、不宜与阿司匹林或非甾体抗炎药同服。
3、重度肾功能损害者慎用本品。
4、饮食中钙、维生素D摄入不足者，应加服这些药品。
5、勿嚼碎或吸吮本品。
药物相互作用
没有有关本品特殊的药物间相互作用的报道。本品不被代谢，也不诱导或抑制肝细胞色素酶P450。
钙剂/抗酸剂 本品与钙剂、抗酸剂以及含二价阳离子的口服制剂同服，会影响本品的吸收。
激素替代治疗 如运用得当，本品可与激素联合使用。
阿司匹林/非甾体抗炎药
在5700名病人参加的本品III期临床试验中，31％病人服用阿司匹林，其中24％为规律服用，48％的病人服用了非甾体类抗炎药，其中21％为规律服用，结果显示服用阿司匹林/非甾体抗炎药的病人中，上消化道不良反应的发生率，本品组（24.5%）与安慰剂组（24.8%）相似。
H2－受体阻滞剂和质子泵抑制剂 在上述同一试验中，21%病人服用了H2－受体阻滞剂和质子泵抑制剂，这些病人中，上消化道副反应的发生率，本品组与安慰剂组相似。
药物过量
过量使用可能会引起血钙、磷下降，还会出现低血钙症状。牛奶或含钙的抗酸剂可以减少本品的吸收，洗胃可以清除未吸收的药物，静脉注射钙制剂，可减轻低血钙症状。
药理毒理
药理作用：
利塞膦酸钠能够与骨中羟磷灰石结合，具有抑制骨吸收的作用。在细胞水平，本品抑制破骨细胞。破骨细胞通常存在于骨表面上，但不具有明显的吸收活性。对大鼠、狗、小猪进行组织形态测定，发现本品可减少骨转换（活化频率，即骨组织重构部位被活化的速率）和骨再塑部位的吸收。
动物试验提示，本品可抑制骨质疏松模型大鼠和小型猪的破骨细胞，抑制骨吸收。大鼠和小猪分别经口给予本品（按体表面积折算，剂量分别为人用剂量5mg/m2的4和25倍，计算方法下同），骨量和骨生物力学强度呈剂量依赖性增加，骨密度的增加与骨生物力学强度呈现正相关，对骨结构和骨矿化无明显影响。狗经口给予本品（剂量分别为人用剂量的0.35～1.4倍），可促进骨更新单元水平上的骨平衡。狗经口给予本品1mg/kg/天（约为人用剂量的5倍），可延迟骨折愈合。这种作用与其他二膦酸盐化合物相似，但在0.1mg/kg/天的剂量下不发生。大鼠本品治疗后对骨骼进行组织检查，结果在高剂量（5mg/kg/天，皮下注射）下也没有影响骨矿化，也未出现骨软化。
毒理研究
遗传毒性：本品在沙门氏伤寒菌及大肠杆菌体外回复突变试验（Ames试验）、哺乳动物细胞基因突变试验（CHO/HPRT）、大鼠肝细胞程序外DNA合成试验、大鼠骨髓细胞微核试验中未见基因毒性。CHO细胞染色体裂变试验中，浓度达到细胞毒水平时（>675mcg/ml，存活率6%～7%）出现阳性结果，但在细胞存活率达29％的剂量水平时，未发现染色体损伤。
生殖毒性：雌性大鼠经口给予本品16mg/kg/天（按体表面积折算，相当于人用剂量30mg/天的5.2倍，下同），排卵受到抑制；剂量为7mg/kg/天（相当于人用剂量的2.3倍），着床减少。雄性大鼠经口给予本品40mg/kg/天，可见睾丸和附睾萎缩、炎性细胞浸润；大鼠连续13周经口给予本品16mg/kg/天，也可见睾丸萎缩；犬连续13周经口给予本品8mg/kg/天（相当于人用剂量的8倍），可见中度至重度的精子生成障碍。这些变化随给药剂量的增加和给药时间延长而趋严重。
妊娠期大鼠经口给予本品，剂量≥16mg/kg/天（相当于人用剂量的5.2倍）时，胎鼠成活率降低；在80mg/kg/天的剂量下，胎仔体重下降；在7.1mg/kg/天剂量下，见胸骨或颅骨骨化数明显增高；在≥16mg/kg/天剂量下，胸骨未骨化或骨化不完全均明显增加；在≥3.2mg/kg/天剂量下，可见胚胎腭裂发生率下降，但该发现与临床的相关性尚不清楚。妊娠家兔经口给予本品，剂量达10mg/kg/天（相当于人用剂量的6.7倍）时，未发现对胚胎骨化产生影响，但14窝中有1窝流产，另外1窝早产分娩。
与其他二膦酸类化合物类似，大鼠在交配期与妊娠期给药，剂量低至3.2mg/kg/天（相当于人用剂量的1倍）可致亲代动物分娩期低血钙症和死亡。此外，本品能在大鼠乳汁中分泌。
致癌性：在104周的致癌研究中，大鼠经口给予本品达24mg/kg/天，未发现明显因药物引起的肿瘤。试验中，雄鼠高剂量组（24mg/kg/天）因毒性反应较大，于第93周时停止试验。在大鼠80周的致癌研究中，本品给药剂量达32mg/kg/天时未发现明显因药物引起的肿瘤。
药代动力学
据文献报道，本品的药代动力学特点如下：
吸收:本品口服后由上消化道迅速吸收，血药浓度达峰时间（Tmax）约为服药后1小时，在一定剂量范围内（单剂量给药：2.5～30mg、多剂量给药：2.5～5mg），吸收呈剂量依赖性。连续用药57天内可达到稳态血浆浓度。利塞膦酸钠片的平均绝对口服生物利用度为0.63%（90%置信限：0.54％～0.75％），与食物同服时生物利用度降低。与空腹给药相比，早餐前半小时或晚餐后2小时给药，吸收减少55％；早餐前1小时给药，吸收减少30％。本品在早餐前至少30分钟给药是有效的。
分布:人体平均稳态分布容积为6.3L/kg。人血浆蛋白结合率约为24%。给大鼠和狗静脉注射单剂量14C标记的本品，吸收量的大约60%分布到骨组织，其余随尿液排出，软组织分布极少，大鼠经多次灌胃后，大约有0.001%～0.01%的本品分布到软组织。
代谢: 本品在体内无明显代谢。
清除
口服给药后，吸收量的约一半在24小时内随尿排出，未吸收的药物以原型随粪便排出。其平均肾清除率为105ml/分，与肌酐清除率之间呈线性关系，而无剂量依赖性。终末半衰期（t1/2）达480h，代表本品从骨组织的解离速率。
特殊人群的药代动力学
儿童: 本品尚未在18岁以下患者中进行药代动力学研究。
性别: 本品的口服生物利用度和药代动力学基本上没有性别差异。
老年: 老年患者（＞60岁）和年轻患者具有相似的生物利用度，因此老年患者不需调整剂量。
肾功能不全:本品主要以原形经肾排泄。与肾功能正常的人相比，肌酐清除率约为30ml/分的患者，本品的肾清除率约减少70%。严重肾功能损害（肌酐清除率＜30ml/分）的患者慎用本品。肌酐清除率≥30ml/分的患者不需要调整剂量。
肝功能不全: 尚未在肝功能损害的患者中评价过本品的安全性和有效性。
贮藏
密封，凉暗（避光并不超过20℃）处保存。请置于儿童不易拿到处。
Actonel
Generic Name: risedronate (rih SED ro nayt)
Brand Names: Actonel
What is Actonel?
Actonel is in a group of medicines called bisphosphonates (bis FOS fo nayts). It alters the cycle of bone formation and breakdown in the body. It slows bone loss while increasing bone mass, which may prevent bone fractures.
Actonel is used to treat or prevent osteoporosis in men and women. Actonel is also used to treat Paget's disease of bone.
Actonel may also be used for other purposes not listed.
Important information about Actonel
Do not take an Actonel tablet if you cannot sit upright or stand for at least 30 minutes. Actonel can cause serious problems in the stomach or esophagus (the tube that connects
your mouth and stomach). You will need to stay upright for at least 30 minutes after taking this medication.
Take the Actonel tablet first thing in the morning, at least 30 minutes before you eat or drink anything or take any other medicine.
Take each dose with a full glass (6 to 8 ounces) of water. Use only plain water (not mineral water) when taking an Actonel tablet.
For at least the first 30 minutes after taking an Actonel tablet, do not lie down or recline; do not eat or drink anything other than plain water; and do not take any other
medicines including vitamins, calcium, or antacids.
Some people using medicines similar to Actonel have developed bone loss in the jaw, also called osteonecrosis of the jaw.
Symptoms of this condition may include jaw pain, swelling, numbness, loose teeth, gum infection, or slow healing after injury or surgery involving the gums. You may be more likely to develop osteonecrosis of the jaw if you have cancer or have been treated with chemotherapy, radiation, or steroids. Other conditions associated with osteonecrosis of the jaw include blood clotting disorders, anemia (low red blood cells), and pre-existing dental problems.
Actonel is only part of a complete program of treatment that may also include diet changes, exercise, and taking calcium and vitamin supplements. Follow your diet, medication, and exercise routines very closely.

What should I discuss with my healthcare provider before taking Actonel?
Do not take an Actonel tablet if you cannot sit upright or stand for at least 30 minutes. Actonel can cause serious problems in the stomach or esophagus (the tube that connects
your mouth and stomach). You will need to stay upright for at least 30 minutes after taking this medication.
You should not take Actonel if you are allergic to risedronate, or if you have low levels of calcium in your blood (hypocalcemia), or a problem with the movement of muscles in your esophagus.
To make sure you can safely take Actonel, tell your doctor if you have any of these other conditions:
low blood calcium (hypocalcemia);
a vitamin D deficiency;
kidney disease; or an ulcer in your stomach or esophagus.
Some people using medicines similar to Actonel have developed bone loss in the jaw, also called osteonecrosis of the jaw.
Symptoms of this condition may include jaw pain, swelling, numbness, loose teeth, gum infection, or slow healing after injury or surgery involving the gums.
You may be more likely to develop osteonecrosis of the jaw if you have cancer or have been treated with chemotherapy, radiation, or steroids. Other conditions associated with
osteonecrosis of the jaw include blood clotting disorders, anemia (low red blood cells), and dental surgery or pre-existing dental problems.
FDA pregnancy category C. Actonel may be harmful to an unborn baby.
Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether Actonel passes into breast milk or if it could harm a nursing baby. Do
not use this medication without telling your doctor if you are breast-feeding a baby.
How should I take Actonel?
Take Actonel exactly as it was prescribed for you. Do not use the medication in larger amounts or for longer than recommended by your doctor.
Follow the directions on your prescription label.
Actonel tablets come in different strengths (number of milligrams per pill). Some tablets are taken once each day or once each week. The stronger tablets may be taken only 1 or 2
times each month. Your dosing schedule will depend on the tablet strength your doctor has prescribed.
If you change tablet strengths, you may also need to change your schedule.
Follow the directions on your prescription label.
Your dosing schedule will depend on the tablet strength your doctor has prescribed. If you change tablet strengths, you may also need to change your schedule. Follow the directions on your prescription label.
Take the Actonel tablet first thing in the morning, at least 30 minutes before you eat or drink anything or take any other medicine.
If you take an Actonel tablet only once a week, take it on the same day each week and always first thing in the morning.
Take each Actonel tablet with a full glass (6 to 8 ounces) of water. Use only plain water (not mineral water) when taking an Actonel tablet. Do not crush, chew, or suck the Actonel tablet. Swallow the pill whole.
After taking an Actonel tablet, carefully follow these instructions:Do not lie down or recline for at least 30 minutes after taking Actonel.
Do not eat or drink anything other than plain water.
Do not take any other medicines including vitamins, calcium, or antacids for at least 30 minutes after taking Actonel. It may be best to take your other medicines at a different time of the day.
Talk with your doctor about the best dosing schedule for your other medicines.
To be sure this medication is helping your condition, your bone mineral density will need to be tested on a regular basis. Visit your doctor regularly.
Actonel is only part of a complete program of treatment that may also include diet changes, exercise, and taking calcium and vitamin supplements. Follow your diet, medication, and exercise routines very closely.
Store Actonel tablets at room temperature away from moisture and heat.            
What happens if I miss a dose?
If you take Actonel tablets once daily: If you forget to take this medicine first thing in the morning, do not take it later in the day. Wait until the following morning to take the medicine and skip the missed dose. Do not take two (2) tablets in one day.
If you take Actonel tablets once a week, or once or twice per month:
If you forget to take Actonel on your scheduled day, take it first thing in the morning on the day after you remember the missed dose.
Then return to your regular weekly schedule on your chosen dose day. Do not take two (2) tablets in one day.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Drink a full glass of milk and call your local poison control center or emergency room right away. Do not make yourself vomit and do not lie down.
Overdose symptoms may include nausea, heartburn, stomach pain, diarrhea, muscle cramps, numbness or tingling, tight muscles in your face, seizure (convulsions), irritability, and unusual thoughts or behavior.
What should I avoid while taking Actonel?
Avoid taking any other medicines including vitamins, calcium, or antacids for at least 30 minutes after taking an Actonel tablet. Some medicines can make it harder for your body to absorb risedronate. Do not lie down for at least 30 minutes after you take an Actonel tablet.
Actonel side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Actonel: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using Actonel and call your doctor at once if you have a serious side effect such as:
chest pain;
difficulty or pain when swallowing;
pain or burning under the ribs or in the back;
new or worsening heartburn;
severe joint, bone, or muscle pain; or
jaw pain, numbness, or swelling.
Less serious Actonel side effects may include:
mild stomach pain or upset stomach;
diarrhea, constipation;
mild joint or back pain; or
headache.
This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.
What other drugs will affect Actonel?
Before using Actonel, tell your doctor if you also use aspirin or other NSAIDs (non-steroidal anti-inflammatory drugs) such as celecoxib (Celebrex), diclofenac (Voltaren), diflunisal (Dolobid), ibuprofen (Motrin, Advil), indomethacin, ketoprofen (Orudis), ketorolac (Toradol), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others.
This list is not complete and other drugs may interact with Actonel. 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 Actonel.
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States
and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy.
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. Multum does not assume any responsibility for any aspect of
healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist. 
附件：
2010111019100434.pdf

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注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
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产地国家: 美国
原产地英文商品名:
ACTONEL 75mg/tab 2tabs/ disp pack
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 75毫克/片 2片/板装
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT

---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
ACTONEL 35mg/tab 4tabs/disp  pack
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 35毫克/片 4片/板装
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT

---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
ACTONEL 30mg/tab 10tabs/box
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 30毫克/片 10片/盒
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT
---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
ACTONEL 150mg/tab 6tabs/disp  pack
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 150毫克/片 6片/板装
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT

---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
ACTONEL 150mg/tab 6tabs/disp  pack
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 150毫克/板装
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT

---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
ACTONEL 5mg/tab 30tabs/box
原产地英文药品名:
RISEDRONATE SODIUM
中文参考商品译名:
ACTONEL 5毫克/片 30片/盒
中文参考药品译名:
利塞膦酸钠
中文参考化合物名称:
2-(3-吡啶基)-1-羟基乙烷-1，1-双膦酸单钠盐二倍半水合物
生产厂家中文参考译名:
WARNER CHILCOTT
生产厂家英文名:
WARNER CHILCOTT