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氨氯地平片|Norvasc OD(Amlodipine Tablets)

2014-08-17 16:39:05  作者:新特药房  来源:互联网  浏览次数:256  文字大小:【】【】【
简介: 络活喜(苯磺酸氨氯地平片)属片剂。具有抗动脉粥样硬化作用,长期应用于冠心病患者可显著减少心血管事件。可以治疗高血压。络活喜(Norvasc)   络活喜(苯磺酸氨氯地平片)是截止目前为止世界处方量最 ...
络活喜(苯磺酸氨氯地平片)属片剂。具有抗动脉粥样硬化作用,长期应用于冠心病患者可显著减少心血管事件。可以治疗高血压。
络活喜(Norvasc)   
络活喜(苯磺酸氨氯地平片)是截止目前为止世界处方量最大的治疗高血压的品牌药物。1990年以来,它在全球的使用已超过400亿个病人治疗日。该药品的成功得益于其杰出的疗效,起效和缓、作用持久平稳、每日一次的方便剂量、24小时稳定控制高血压和心绞痛以及极佳的安全性和耐受性。
最新的临床研究结果显示,络活喜还具有抗动脉粥样硬化作用,长期应用于冠心病患者可显著减少心血管事件和操作的总和并显著减少冠心病相关的医疗费用。
【别名】阿洛地平、络活喜 、氨氯地平、苯磺酸氨氯地平   
【外文名】Amiodipine Besylate ,Istin, Norvasc
【作用与用途】
本品为钙离子拮抗剂,阻滞心肌和血管平滑肌细胞外钙离子经细胞膜的钙离子通道进入细胞。直接舒张血管平滑肌,具有抗高血压作用,本品缓解心绞痛是通过扩张外周小动脉,使外周阻力降低,从而降低心肌耗氧量,另外扩张正常和缺血区的冠状动脉及冠状小动脉,使冠状动脉痉挛病人的心肌供氧量增加。用于治疗高血压、稳定型心绞痛和缺血性心脏病。
【药理毒理】
药理作用
苯磺酸氨氯地平是二氢吡啶类钙拮抗剂(钙离子拮抗剂或慢通道阻滞剂)。心肌和平滑肌的收缩依赖于细胞外钙离子通过特异性离子通道进入细胞。本品选择性抑制钙离子跨膜进入平滑肌细胞和心肌细胞,对平滑肌的作用大于心肌。其与钙通道的相互作用决定于它和受体位点结合和解离的渐进性速率,因此药理作用逐渐产生。
本品是外周动脉扩张剂,直接作用于血管平滑肌,降低外周血管阻力,从而降低血压。治疗剂量下,体外实验可观察到负性肌力作用,但在整体动物实验中未见。本品不影响血浆钙浓度。15项随机双盲、安慰剂对照的临床试验证实了本品的抗高血压作用。
轻中度高血压患者每日服药一次,可以24小时降低卧位和立位血压,长期使用不引起心率或血浆儿茶酚胺显著改变。
降压效果平稳。
降压效果和剂量相关,降压幅度与治疗前血压相关,中度高血压者(舒张压105-114mmHg)的疗效比轻度高血压者(舒张压90-104mmHg)高,血压正常者服药后没有明显作用。本品降低舒张压的作用在老年人和年轻人中相似,降低收缩压的作用对老年人更强。
本品缓解心绞痛的准确机制尚不明确,但可能在运动时,本品通过降低外周阻力(后负荷)减少心脏做功和心率血压乘积,减少心肌氧需,治疗劳力型心绞痛;通过抑制钙离子、肾上腺素、5-羟色胺和血栓素A2引起的冠状动脉和小动脉收缩,恢复缺血区血供治疗自发性心绞痛。8项临床试验中5项显示,本品显著延长运动诱发劳力型心绞痛的时间;部分研究显示本品延长ST段下降1mm的时间,并减少心绞痛发作频率。
该作用具有持续性,并且不显著影响血压和心率。在一项50例自发性心绞痛患者中进行临床试验显示,本品每周可以减少4次心绞痛发作(安慰剂每周减少1次)。心功能正常的患者服用本品后测定静息和运动状态下血流动力学,心脏射血分数有所增加,但对dP/dt或左室舒张末压/容积无显著影响。治疗剂量下,本品单独使用或与-阻滞剂合用,均不引起负性肌力作用。
一项安慰剂对照研究中,697例心功能II/III级(NYHA)的心衰患者用药8-12周后,运动耐量检查、NYHA分级、症状和左室射血分数均未显示心衰有加重的迹象。(另一项安慰剂对照的长期生存试验,1153名心功能III/IV级心衰病人,在常规治疗基础上随机加用本品或安慰剂,结果显示各种原因的死亡率和心源性发病率,氨氯地平组为39%,安慰剂组为42%。)本品不影响窦房结功能和房室传导。高血压或心绞痛患者合用本品和-阻滞剂,未发现心电图异常。
本品不改变心绞痛患者的心电图,不加重房室传导阻滞。肾功能正常的高血压患者用药后,肾血管阻力降低、肾小球滤过率和肾血流增加,但滤过分数或尿蛋白不变。毒理作用致癌、致突变和致畸以每日0.5、1.25和2.5mg/kg的剂量,大鼠和小鼠连续喂食氨氯地平两年,未证实有致癌性。
最高剂量已达到了小鼠的最大耐受量,但大鼠尚未达到(以临床最大推荐剂量10mg为基础计算mg/m2)。基因和染色体水平均未揭示有药物相关的致突变性。雄性大鼠在交配前64天、雌性大鼠在交配前14天开始给予氨氯地平,每日10mg/kg(8倍于人类最大推荐剂量),不影响生殖能力。
妊娠大鼠和兔子在主要器官形成期给予氨氯地平10mg/kg(8倍和23倍于人类最大推荐剂量),未发现有致畸性和其它胚胎毒性。但是大鼠交配前14天开始,直至整个交配期和妊娠期给予10mg/kg的氨氯地平,导致幼仔的体型明显减小(约50%),宫内死亡数量明显增加(约5倍),同时延长妊娠时间和分娩时程。毒性小鼠和大鼠分别单剂给予氨氯地平高达40mg/kg和100mg/kg,可以导致死亡。狗单剂服用4mg/kg或更高剂量将导致明显的外周血管扩张和低血压。
【药代动力学】
本品口服后吸收完全但缓慢,6-12小时达到峰浓度。单次口服5mg,血药峰值为3.0ng/ml;单次口服10mg,血药峰值为5.9ng/ml。绝对生物利用度为64%-90%,不受饮食影响。循环中的药物约95%以上与血浆蛋白结合,分布容积为21L/kg。持续用药后7-8天达到稳态血药浓度。本品以二室模型的方式从血浆中消除,在肝脏广泛代谢为无药理活性的代谢产物(90%)。终末半衰期(t1/2?)健康者约为35小时,高血压病人延长为50小时,老年人65小时,肝功受损者60小时,肾功能不全者不受影响。本品10%以原型、60%以代谢物的形式从尿中排出,20%-25%从胆汁或粪便排出。本品不被血液透析清除。肾功能不全对本品的药代动力学特点没有显著影响。老年患者和肝功能不全患者对本品的清除率降低,药时曲线下面积(AUC)约增加40%-60%。中重度心衰患者的AUC升高幅度相似。
【用法】
治疗高血压和心绞痛的初始剂量为5mg,每日一次。根据患者的临床反应,可将剂量增加,最大可增至10mg,每日一次。   
本品与噻嗪类利尿剂,β-受体阻滞剂和血管紧张素转换酶抑制剂合用时不需调整剂量。   
通常口服起始剂量为5mg,每日一次,最大不超过10mg,每日一次。瘦小者、体质虚弱者、老年患者或肝功能受损者从2.5mg,每日一次开始用药;合用其它抗高血压药者也从此剂量开始用药。用药剂量根据个体需要进行调整,调整期应不少于7-14天,以便医生充分评估患者对该剂量的反应。但在临床有保障的前提下,可以加快调整速度。治疗心绞痛的推荐剂量是5-10mg,老年患者或肝功能受损者需减量。
【不良反应】
本品在10mg/日的剂量范围内有良好的耐受性,大多数不良反应是轻中度的。本品因不良反应而停药的仅为1.5%,与安慰剂没有明显差别(约1%)。
最常见的不良反应是头痛和水肿。发生率1%的剂量相关性不良反应如下:
水肿、头晕、潮红和心悸。与剂量关系不明确,但发生率超过1.0%的不良反应如下:头痛、疲倦、恶心、腹痛和嗜睡。
以上不良反应中,水肿、潮红、心悸和嗜睡在女性中的发生率超过男性。以下不良事件发生率?1%但0.1%,与药物的因果关系不明确:一般:过敏反应,虚弱,背痛,潮热,不适,疼痛,僵硬,体重增加;心血管:心律失常(包括心动过速、心动过缓或房颤),胸痛,低血压,外周缺血,昏厥,体位性头晕,体位性低血压和脉管炎;中枢和外周神经系统:感觉减退,外周神经病,感觉异常,震颤,眩晕;胃肠道:厌食症,便秘,消化不良,吞咽困难,腹泻,胃胀气,胰腺炎,呕吐,牙龈增生;骨骼肌系统:关节痛,关节炎,肌肉痛性痉挛,肌痛;精神:性功能障碍,失眠,紧张,抑郁,梦魇,焦虑,人格解体;皮肤及附属物:血管性水肿,红斑,搔痒,皮疹,斑丘疹;特殊感觉:视觉异常,结膜炎,复视,眼痛,耳鸣;泌尿系统:尿频,排尿障碍,夜尿;自主神经系统:口干,盗汗;代谢和营养:高血糖,口渴;造血系统:白细胞减少症,紫癜,血小板减少症。
以下不良事件的发生率0.1%:心衰,脉搏不规则,期外收缩,皮肤变色,风疹,皮肤干燥,皮肤炎,脱发,肌肉无力,颤搐,共济失调,张力过高,偏头痛,皮肤冷湿,淡漠,激动,健忘,胃炎,食欲增加,稀便,咳嗽,鼻炎,排尿困难,多尿,嗅觉到错,味觉颠倒,视觉调节失常,眼干燥症。其它偶发反应如心肌梗死和心绞痛则不能分辨是药物作用还是疾病状态。常规实验室检查项目没有明显变化,未发现血钾、血糖、甘油三脂、总胆固醇、高密度脂蛋白(HDL)、尿酸、血尿素氮或肌酐出现有意义的变化。药物上市后,用药人群中偶有男性乳腺发育的报道,但与药物的因果关系不明;部分病例中黄疸和肝酶升高(常伴有胆汁淤积和肝炎)较严重,需要住院治疗。
【禁忌】
对二氢吡啶类钙拮抗剂过敏者。
【注意事项】
1.心绞痛和/或心肌梗死:
罕见。有严重的阻塞性冠状动脉疾病的患者,在开始应用钙通道拮抗剂治疗或加量时,会出现心绞痛发作频率、时程和/或严重性上升,或发展为急性心肌梗死,机制不明。
2.低血压:
由于本品逐渐产生扩血管作用,口服一般很少出现急性低血压。但本品与其它外周扩血管药物合用时仍需谨慎,特别是对于有严重主动脉瓣狭窄的病人。
3.心力衰竭患者:
钙通道阻滞剂应慎用于心衰患者。
4.肝功能不全患者:
严重肝功能不全患者应慎用本品。
5.肾功能衰竭患者:
肾衰患者的起始剂量可以不变。
6.停用?-阻滞剂:
本品对突然停用-阻滞剂所产生的反跳症状没有保护作用。因此,停用?-阻滞剂仍需逐渐减量。
7.本品在梗阻性肺病、代偿良好的心力衰竭、外周血管疾病、糖尿病和脂质异常疾病的病人中可以安全使用。
【孕妇及哺乳期妇女用药】
对孕妇用药缺乏相应的研究资料,但根据动物试验结果,本品只在非常必要时方可用于孕妇。尚不知本品能否通过乳汁分泌,服药的哺乳期妇女应中止哺乳。
【儿童用药】
儿童的安全性和有效性尚未确定。
【老年患者用药】
临床研究未证实老年人对该药的反应与年轻人不同,但考虑到老年人多有肝肾功能和心功能减退,并伴有其它疾病和相应的药物治疗,一般起始用药采用剂量范围的下限。老年人对本品的清除率降低,药时曲线(AUC)增加约40%-60%,也需采用较低的起始剂量。
【药物相互作用】
⑴西米替丁、葡萄柚汁、致酸剂:合用时不改变本品的药代动力学。
⑵阿伐他汀、地高辛、乙醇:本品不影响它们的药代动力学。
⑶昔多芬:原发性高血压患者单剂服用昔多芬(伟哥?)对本品的药代动力学没有影响。两药合用时独立产生降压效应。
⑷华法令:本品不改变华法令的凝血酶原作用时间。
⑸地高辛、苯妥因和华法令:与本品合用对血浆蛋白结合率没有影响。
⑹麻醉药:吸入烃类与本品合用可引起低血压。
⑺非甾体类抗炎药:尤其吲哚美辛可减弱本品的降压作用。
⑻-阻滞剂:与本品合用耐受性良好,但可引起过度低血压,罕见加重心力衰竭。
⑼雌激素:合用可引起体液潴留而增高血压。
⑽磺吡酮:合用可增加本品的蛋白结合率,产生血药浓度变化。
⑾锂:合用可引起神经中毒,出现恶心、呕吐、腹泻、共济失调、震颤和/或麻木,需慎重。
⑿拟交感胺:可减弱本品降压作用。
⒀舌下硝酸甘油和长效硝酸酯制剂:与本品合用可加强抗心绞痛效应。虽未报告有反跳作用,但停药时应在医生指导下逐渐减量。
⒁噻嗪类利尿药、ACEI、地高辛、华法令、抗生素和口服降糖药:可与本品安全合用。
【药物过量】
药物过量可导致外周血管过度扩张,引起低血压,还可能出现反射性心动过速。发生药物过量后,必须监测血压,同时进行心脏和呼吸监测。一旦发生低血压,则采取支持疗法,包括抬高肢体和根据需要扩容。如果这些手段无效,在循环血容量和尿量允许的情况下可以考虑给予升压剂(如去氧肾上腺素)。静脉给予葡萄糖酸钙有助于逆转钙拮抗作用。由于本品与血浆蛋白高度结合,透析处理没有作用。
【贮藏】
遮光、密封保存
Norvasc
Generic Name: amlodipine (am LOE di peen)
Brand Names: Norvasc
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What is Norvasc?
Norvasc is in a group of drugs called calcium channel blockers. It dilates blood vessels and slows the heart to reduce blood pressure and the pain of angina.
Norvasc is used to treat high blood pressure (hypertension) or angina (chest pain caused by lack of oxygen in the heart muscle due to clogged arteries).
Norvasc may also be used for other purposes not listed here.
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Important information about Norvasc
Before taking Norvasc, tell your doctor if you have congestive heart failure or liver disease.
Avoid drinking alcohol while taking Norvasc. Alcohol can further lower your blood pressure and may increase some of the side effects of Norvasc.
If you are being treated for high blood pressure, keep using this medication even if you feel fine.
You may need to use blood pressure medication for the rest of your life.
Norvasc is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications.
Follow your diet, medication, and exercise routines very closely.
Tell your doctor about all other heart or blood pressure medications you are taking.
Your chest pain may become worse when you first start taking Norvasc or when your dose is increased. Call your doctor if your chest pain is severe or ongoing.
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Before taking Norvasc
You should not take Norvasc if you are allergic to amlodipine.
If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before taking Norvasc, tell your doctor if you have:
congestive heart failure; or
liver disease.
If you are also taking a beta-blocker drug (such as Blocadren, Corgard, Inderal, Normodyne, Tenormin, Toprol, Trandate, Zebeta, and others) do not suddenly stop using the beta-blocker without first talking to your doctor. You may need to use less and less before you stop the medication completely. Stopping a beta-blocker too quickly
can cause serious heart problems that will not be prevented by Norvasc.
FDA pregnancy category C. Norvasc 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 Norvasc 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.
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How should I take Norvasc?
Take Norvasc exactly as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended. Follow the directions on your prescription label.
Norvasc is usually taken once daily. Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Your chest pain may become worse when you first start taking Norvasc or when your dose is increased.
Call your doctor if your chest pain is severe or ongoing.
Norvasc is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications.
Follow your diet, medication, and exercise routines very closely.
If you are being treated for high blood pressure, keep using this medication even if you feel fine.
High blood pressure often has no symptoms, so you may not know when your blood pressure is high.
You may need to use blood pressure medication for the rest of your life.
Store Norvasc at room temperature away from moisture, heat, and light.
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What happens if I miss a dose?
Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.
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What happens if I overdose?
Seek emergency medical attention if you think you have taken too much of this medication.
Overdose symptoms may include warmth or tingly feeling, severe dizziness, and fainting.
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What should I avoid while taking Norvasc?
Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.
Avoid drinking alcohol while taking Norvasc. Alcohol can further lower your blood pressure and may increase some of the side effects of Norvasc.
---------------------------------------------------------------------
Norvasc side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:
feeling like you might pass out;
swelling in your hands, ankles, or feet;
chest pain;
slow, fast, or pounding heartbeats;
easy bruising or bleeding, unusual weakness;
numbness, burning, pain, or tingly feeling; or
jaundice (yellowing of your skin or eyes).
Less serious Norvasc side effects may include:
headache;
drowsiness, depression, nervousness;
dizziness, spinning sensation;
warmth or redness under your skin;
nausea, vomiting, stomach pain, loss of appetite;
diarrhea, constipation;
urinating more than usual;
sleep problems (insomnia);
strange dreams;
mild skin rash or itching;
joint or muscle pain;
dry mouth, thirst, increased sweating; or
weight changes.
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 Norvasc?
Tell your doctor about all other heart or blood pressure medications you are taking.
There may be other drugs that can interact with Norvasc. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.
--------------------------------------------------------------------
Where can I get more information?
Your pharmacist can provide more information about Norvasc 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
The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects.
---------------------------------------------------------------           
产地国家: 日本
原产地英文商品名:
Norvasc OD 0.25mg 100 film-tablets
原产地英文药品名:
Amlodipine
中文参考商品译名:
络活喜OD 0.25毫克/片 100片/盒
中文参考药品译名:
氨氯地平
生产厂家中文参考译名:
诺华
生产厂家英文名:
Novartis
---------------------------------------------------------------
产地国家: 日本
原产地英文商品名:
Norvasc OD 5mg 100 film-tablets
原产地英文药品名:
Amlodipine
中文参考商品译名:
络活喜OD 5毫克/片 100片/盒
中文参考药品译名:
氨氯地平
生产厂家中文参考译名:
诺华

责任编辑:admin


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