氨氯地平:修订间差异
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* [[收縮壓和舒張壓低於90/60 mmHg]](Systolic and diastolic blood pressure below 90/60 mmHg) |
* [[收縮壓和舒張壓低於90/60 mmHg]](Systolic and diastolic blood pressure below 90/60 mmHg) |
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* [[主動脈瓣狹窄]](Aortic valve stenosis): 氨氯地平引起血管擴張,從而導致患者產生嚴重"主動脈瓣狹窄"進而造成心臟血液輸出量減少。 |
* [[主動脈瓣狹窄]](Aortic valve stenosis): 氨氯地平引起血管擴張,從而導致患者產生嚴重"主動脈瓣狹窄"進而造成心臟血液輸出量減少。 |
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==不良反應== |
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<!--Adverse side effects of the use of amlodipine may be:<ref>Source: [[Sandoz]] product information sheet</ref> |
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* Very often: [[peripheral edema]] in 8.3% of users, [[Fatigue (medical)|fatigue]] in 4.5% of users<ref>{{cite web |
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|author=[[Pfizer]] |
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|date=February 2006 |
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|url=http://www.norvasc.com/high-blood-pressure-medicine/index.asp |
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|title= Norvasc (amlodipine besylate): official site |
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|publisher=[http://www.pfizer.com/home/ Pfizer Inc.] |
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|location=[[New York City]], [[New York]] |
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|accessdate=20 July 2010| archiveurl= http://web.archive.org/web/20100724122632/http://www.norvasc.com/high-blood-pressure-medicine/index.asp| archivedate= 24 July 2010 <!--DASHBot-->| deadurl= no}}</ref> |
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* Often: [[dizziness]]; [[palpitations]]; [[muscle]]-, [[stomach]]- or [[headache]]; [[dyspepsia]]; or [[nausea]] - in one in 100 users |
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* Sometimes: [[blood]] disorders, development of [[breast]]s in [[man|men]] ([[gynecomastia]]), [[impotence]], [[Clinical depression|depression]], [[insomnia]], [[tachycardia]], or [[gingival enlargement]] - in one in 1,000 users |
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* Rarely: erratic [[behavior]], [[hepatitis]], [[jaundice]] - in one in 10,000 users |
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* Very rarely: [[hyperglycemia]], [[tremor]], [[Stevens–Johnson syndrome]] - in one in 100,000 users |
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The [[Acute (medicine)|acute]] oral [[toxicity]] ([[Median lethal dose|LD50]]) of amlodipine in [[Mouse|mice]] is 37 mg/kg.<ref name=Sciencelab>{{cite web |
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|author=Sciencelab.com, Inc. |
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|date=6 November 2008 |
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|url=http://www.sciencelab.com/xMSDS-Amlodipine_Besylate-9922908 |
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|title=Material Safety Data Sheet: Amlodipine Besylate |
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|publisher=[http://www.sciencelab.com/ ScienceLab.com] |
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|location=Houston, Texas |
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|accessdate=20 July 2010}}</ref>--> |
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===注意事項=== |
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* [[肝臟|肝]]功能不全者服用需注意。 |
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* [[妊娠]]婦女服用需注意。 |
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===Interactions === |
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* In patients with severe coronary artery disease, amlodipine can increase the frequency and severity of angina or actually cause a heart attack on rare occasions. This phenomenon usually occurs when first starting amlodipine, or at the time of dosage increase. {{Citation needed|date=October 2009}} |
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* Excessive lowering of blood pressure during initiation of amlodipine treatment can occur, especially in patients already taking another medication for lowering blood pressure. In rare instances, congestive heart failure has been associated with amlodipine, usually in patients already on a beta blocker. |
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* Amlodipine is primarily metabolyzed by the liver, via the [[cytochrome P450]] isoenzyme [[CYP3A4]].<ref name="Norvasc monograph">{{cite web |url=http://www.pfizer.ca/en/our_products/products/monograph/129 |title=Product Monograph:Norvasc |format=PDF |work= |year=2012 |publisher=Pfizer Canada Inc' |accessdate=2013-03-24}}</ref> As a result, serum levels can potentially be affected by drugs which [[enzyme inhibition|inhibit]] or [[enzyme activation|activate]] CYP3A4. Grapefruit juice can inhibit the [[cytochrome P450]] system,<ref name="Norvasc monograph"/> but the predicted interaction risk with amlodipine is low.<ref>{{cite journal | author=Bailey DG, Dresser G, and Arnold JMA | title=Grapefruit and Medication Interactions: Forbidden Fruit or Avoidable Consequences? | journal=Canadian Medical Association Journal | year=2012 | doi=10.1503/cmaj.120951}}</ref> |
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The most recent study indicates that long-term use (10 yrs) of calcium channel blockers to control hypertension lead to a 10 fold increase in risk to develop breast cancer.{{cn|date=August 2013}}--> |
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==製劑== |
==製劑== |
2014年1月22日 (三) 05:50的版本
臨床資料 | |
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AHFS/Drugs.com | Monograph |
MedlinePlus | a692044 |
核准狀況 |
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懷孕分級 |
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给药途径 | 口服(片劑/錠) |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | 64-90% |
药物代谢 | 肝臟 |
生物半衰期 | 30-50小時(1天至2天) |
排泄途徑 | 腎 |
识别信息 | |
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CAS号 | 88150-42-9 |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.102.428 |
化学信息 | |
化学式 | C20H25ClN2O5 |
摩尔质量 | 408.879 g/mol |
3D模型(JSmol) | |
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氨氯地平(Amlodipine 或 Amlodipine besylate、脈優錠(Norvasc)(輝瑞公司商標名)及其它學名藥))(可與苯磺酸(besylate)、甲磺酸酯(mesylate)或馬來酸(maleic acid)等形成組合藥劑)是一種作為抗高血压药和治療心絞痛之二氫吡啶(DHP)類的長效钙通道阻滞药(CCB)。「像其他鈣通道阻滯劑一樣,氨氯地平的作用是通過鬆弛在動脈壁的平滑肌,降低總外週阻力(total peripheral resistance)從而降低血壓;在心绞痛時,氨氯地平增加血液流向心肌」(儘管"DHP類鈣通道阻滯劑"對動脈而言更具選擇性、如比起心臟(心肌)的肌肉組織來看,像是"心肌钙通道"並無"二氫吡啶"類)。
醫療使用
禁忌
- 母乳餵養
- 心源性休克(Cardiogenic shock)
- 不穩定型心絞痛(Unstable angina)
- 收縮壓和舒張壓低於90/60 mmHg(Systolic and diastolic blood pressure below 90/60 mmHg)
- 主動脈瓣狹窄(Aortic valve stenosis): 氨氯地平引起血管擴張,從而導致患者產生嚴重"主動脈瓣狹窄"進而造成心臟血液輸出量減少。
不良反應
| deadurl= no}}</ref>
- Often: dizziness; palpitations; muscle-, stomach- or headache; dyspepsia; or nausea - in one in 100 users
- Sometimes: blood disorders, development of breasts in men (gynecomastia), impotence, depression, insomnia, tachycardia, or gingival enlargement - in one in 1,000 users
- Rarely: erratic behavior, hepatitis, jaundice - in one in 10,000 users
- Very rarely: hyperglycemia, tremor, Stevens–Johnson syndrome - in one in 100,000 users
The acute oral toxicity (LD50) of amlodipine in mice is 37 mg/kg.[3]-->
注意事項
製劑
對"氨氯地平"而言輝瑞公司的"脈優錠"(Norvasc)專利保護延續到2007年為止。總的專利到期至2007年以後截止。[4] 之後可容許多不同商標的學名藥(generic drug)。
商標名稱
氨氯地平在"學名藥"市場的各式商標名稱如列:
- Emadine 尼泊爾的Merck Kga'公司。
- Aforbes 菲律賓的Merck Inc.公司。
- Agen 捷克的Zentiva公司。
- Aken 墨西哥的"Kendrick Farmaceutica"公司。
- Amcard 孟加拉的"Apex Pharma Ltd"公司。
- Amdepin 印度的"Cadila Pharmaceuticals"公司。
- Amlod 在尼泊爾的商標名。
- Amdipin 哥倫比亞的"Laboratorios Lafrancol"公司。
- Amlodine 日本的"Dainippon Sumitomo Pharmaceuticals"公司。菲律賓InnoGen公司的分部門"Westfield Pharmaceuticals"。
- Amlodipin 在挪威的商標名。
- Amlodipine 5 印度尼西亞的"PT KALBE FARMA Tbk, Bekasi"公司。
- Amlodipin-Mepha 5/10 瑞典的"Mepha Pharma AG, Basel"公司。
- Amlong 印度的"Micro Labs"公司。
- Amlopin Lek公司。
- Amlopin 孟加拉的"The Acme Laboratories Ltd"公司。
- Amlopine 泰國的"Berlin (Thailand) Pharmaceutical Industry Co Ltd"公司。
- Amlostin 英國的"Discovery Pharmaceuticals"公司。
- Amlosun 孟加拉的"Sun Pharmaceutical (Bangladesh)"公司。
- Amlovas 印度的"Macleods Pharmaceuticals Ltd"公司。
- Amlovasc 英國的Dr. Reddy's Laboratories實驗室。
- Amlozek 波蘭的"Adamed"公司。
- Asomex 印度的Emcure Pharmaceuticals公司。
- Atecard-AM 印度的Alembic公司。
- Camlodin 孟加拉的"Square Pharmaceuticals Ltd"公司。
- Dailyvasc "Xeno Pharmaceuticals"公司。
- Hipril 在印度由"氨氯地平(每錠5 mg)"搭配"Lisinopril"之組合藥。
- Istin 在英國及愛爾蘭的商標名。
- Lama 印度加尔各答的"Square Pharmaceuticals Ltd"公司。
- Lodopin 巴基斯坦的"Merck Pakistan"公司。
- Lopin 孟加拉的"Edruc Ltd"公司。
- Lodip 尼泊爾的"TIME Pharmaceuticals"公司。
- Nelod 孟加拉的"The Kemiko Pharmaceuticals Ltd"公司。
- Nopidin 孟加拉的"Ad-din Pharmaceuticals Ltd"公司。
- Norvasc 北美洲的輝瑞公司商標名,其它如一些歐洲國家、中國、日本、台灣及巴基斯坦等國均用此商標名。
- Norvasc 澳大利亞的"Perivasc"公司及"Nordip"公司。
- Pharex Amlodipine 菲律賓的"PHAREX HealthCorp"公司。
- Tenox Krka公司。
參見
- 組合藥劑(combination drug)
- Amlodipine/valsartan
- Aliskiren/amlodipine
- Levamlodipine,為(S)-氨氯地平對映體。
- CVnor 10,為孟加拉"那瓦那"(Navana)藥品公司"氨氯地平"商標名。
- 药物英文名称列表
註釋
- ^ Wang, JG. A combined role of calcium channel blockers and angiotensin receptor blockers in stroke prevention. Vascular health and risk management. 2009, 5: 593–605. PMID 19688100.
- ^ Amlodipine Besylate. The American Society of Health-System Pharmacists. [3 April 2011].
- ^ Sciencelab.com, Inc. Material Safety Data Sheet: Amlodipine Besylate. Houston, Texas: ScienceLab.com. 6 November 2008 [20 July 2010].
- ^ Kennedy VB. Pfizer loses court ruling on Norvasc patent. MarketWatch. 22 March 2007.
外部鏈接
- Istin - Summary of Product Characteristics from the electronic Medicines Compendium
- U.S. National Library of Medicine: Drug Information Portal - Amlodipine
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