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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)
* [[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。

==不良反應==
<!--Adverse side effects of the use of amlodipine may be:<ref>Source: [[Sandoz]] product information sheet</ref>
* Very often: [[peripheral edema]] in 8.3% of users, [[Fatigue (medical)|fatigue]] in 4.5% of users<ref>{{cite web
|author=[[Pfizer]]
|date=February 2006
|url=http://www.norvasc.com/high-blood-pressure-medicine/index.asp
|title= Norvasc (amlodipine besylate): official site
|publisher=[http://www.pfizer.com/home/ Pfizer Inc.]
|location=[[New York City]], [[New York]]
|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>
* Often: [[dizziness]]; [[palpitations]]; [[muscle]]-, [[stomach]]- or [[headache]]; [[dyspepsia]]; or [[nausea]] - in one in 100 users
* 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
* 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 (medicine)|acute]] oral [[toxicity]] ([[Median lethal dose|LD50]]) of amlodipine in [[Mouse|mice]] is 37&nbsp;mg/kg.<ref name=Sciencelab>{{cite web
|author=Sciencelab.com, Inc.
|date=6 November 2008
|url=http://www.sciencelab.com/xMSDS-Amlodipine_Besylate-9922908
|title=Material Safety Data Sheet: Amlodipine Besylate
|publisher=[http://www.sciencelab.com/ ScienceLab.com]
|location=Houston, Texas
|accessdate=20 July 2010}}</ref>-->

===注意事項===
* [[肝臟|肝]]功能不全者服用需注意。
* [[妊娠]]婦女服用需注意。
<!--
===Interactions ===
* 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}}
* 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.
* 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>

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}}-->


==製劑==
==製劑==

2014年1月22日 (三) 05:50的版本

氨氯地平
(Amlodipine)
臨床資料
AHFS/Drugs.comMonograph
MedlinePlusa692044
核准狀況
懷孕分級
  • : C
给药途径口服(片劑/錠)
ATC碼
法律規範狀態
法律規範
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
识别信息
  • (RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
CAS号88150-42-9  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.102.428 編輯維基數據鏈接
化学信息
化学式C20H25ClN2O5
摩尔质量408.879 g/mol
3D模型(JSmol英语JSmol
  • Clc1ccccc1C2C(=C(/N/C(=C2/C(=O)OCC)COCCN)C)\C(=O)OC
  • InChI=1S/C20H25ClN2O5/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21/h5-8,17,23H,4,9-11,22H2,1-3H3 checkY
  • Key:HTIQEAQVCYTUBX-UHFFFAOYSA-N checkY

氨氯地平(AmlodipineAmlodipine besylate、脈優(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

氨氯地平是用來治療高血壓[1]冠狀動脈性心臟病[2]

禁忌

不良反應

| deadurl= no}}</ref>

The acute oral toxicity (LD50) of amlodipine in mice is 37 mg/kg.[3]-->

注意事項

  • 功能不全者服用需注意。
  • 妊娠婦女服用需注意。

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:

參見

註釋

  1. ^ 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. 
  2. ^ Amlodipine Besylate. The American Society of Health-System Pharmacists. [3 April 2011]. 
  3. ^ Sciencelab.com, Inc. Material Safety Data Sheet: Amlodipine Besylate. Houston, Texas: ScienceLab.com. 6 November 2008 [20 July 2010]. 
  4. ^ Kennedy VB. Pfizer loses court ruling on Norvasc patent. MarketWatch. 22 March 2007. 

外部鏈接