Company InfoNewsInvestor InformationResearchDevelopmentCareersBusiness DevelopmentResourcesDrugs databaseBack to the home pageSearch  
Drugs database
Drugs A-Z

Brands A-Z

Drugs by categories

Drugs by manufacturer

Drugs by packager

Antibiotics for sale

Online Viagra bestellen in Nederland

Home / Drugs / Starting with A / Amlodipine

Amlodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, amlodipine prevents calcium-dependent myocyte contraction and vasoconstriction. A second proposed mechanism for the drug’s vasodilatory effects involves pH-dependent inhibition of calcium influx via inhibition of smooth muscle carbonic anhydrase. Some studies have shown that amlodipine also exerts inhibitory effects on voltage-gated N-type calcium channels. N-type calcium channels located in the central nervous system may be involved in nociceptive signaling and pain sensation. Amlodipine is used to treat hypertension and chronic stable angina.
CategoriesAntihypertensive Agents
Vasodilator Agents
Calcium Channel Blockers
ManufacturersSynthon pharmaceuticals inc
Actavis totowa llc
Alkem laboratories ltd
Amneal pharmaceuticals ny llc
Apotex inc
Aurobindo pharma ltd
Caraco pharmaceutical laboratories ltd
Dr reddys laboratories ltd
Gedeon richter usa inc
Genpharm inc
Glenmark generics ltd
Invagen pharmaceuticals inc
Lek pharmaceuticals dd
Lupin ltd
Matrix laboratories ltd
Mutual pharmacal co
Mylan laboratories inc
Orchid healthcare
Ranbaxy laboratories ltd
Roxane laboratories inc
Teva pharmaceuticals usa inc
Torrent pharmaceuticals ltd
Upsher smith laboratories inc
Vintage pharmaceuticals llc
Watson laboratories inc
Wockhardt ltd
World gen llc
Zydus pharmaceuticals usa inc
Pfizer inc
Dr reddys laboratories inc
PackagersActavis Group
Advanced Pharmaceutical Services Inc.
Amerisource Health Services Corp.
Amneal Pharmaceuticals
Apotex Inc.
AQ Pharmaceuticals Inc.
Arrow Pharm Malta Ltd.
A-S Medication Solutions LLC
Aurobindo Pharma Ltd.
Beijing Second Pharmaceutical Co. Ltd.
Blu Pharmaceuticals LLC
Breckenridge Pharmaceuticals
Bryant Ranch Prepack
Cadila Healthcare Ltd.
Camber Pharmaceuticals Inc.
Caraco Pharmaceutical Labs
Cardinal Health
Chemical Works Of Gedeon Richter Ltd.
Cobalt Pharmaceuticals Inc.
Comprehensive Consultant Services Inc.
Corepharma LLC
Coupler Enterprises Inc.
Dept Health Central Pharmacy
Direct Dispensing Inc.
Direct Pharmaceuticals Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Doctor Reddys Laboratories Ltd.
Glenmark Generics Ltd.
Greenstone LLC
H.E. Butt Grocery Co.
Heartland Repack Services LLC
InvaGen Pharmaceuticals Inc.
Kaiser Foundation Hospital
Lake Erie Medical and Surgical Supply
Letco Medical Inc.
Lupin Pharmaceuticals Inc.
Major Pharmaceuticals
Medisca Inc.
Medvantx Inc.
Murfreesboro Pharmaceutical Nursing Supply
Neuman Distributors Inc.
Norwich Pharmaceuticals Inc.
Novartis AG
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
PD-Rx Pharmaceuticals Inc.
Pfizer Inc.
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Promius Pharma
Rebel Distributors Corp.
Redpharm Drug
Remedy Repack
Roxane Labs
Sandhills Packaging Inc.
Secan Pharmaceuticals Inc.
Solco Healthcare US LLC
Southwood Pharmaceuticals
Stat Rx Usa
Stat Scripts LLC
Synthon Pharmaceuticals Inc.
Teva Pharmaceutical Industries Ltd.
Torrent Pharmaceuticals
Tya Pharmaceuticals
UDL Laboratories
US Pharmaceutical Group
USL Pharma Inc.
Va Cmop Dallas
Vangard Labs Inc.
Warner Lambert Company LLC
Wockhardt Ltd.
Zydus Pharmaceuticals
SynonymsAmlodipine Benzenesulfonate
Amlodipine Besilate
Amlodipine Besylate
Amlodipine Free Base
Amlodipino [Spanish]
Amlodipinum [Latin]


For the treatment of hypertension and chronic stable angina.


Amlodipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. It was widely accepted that DHP CCBs target L-type calcium channels, the major channel in muscle cells that mediate contraction; however, some studies have indicated that amlodipine also binds to and inhibits N-type calcium channels (see references in Targets section). Similar to other DHP CCBs, amlodipine binds directly to inactive L-type calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives amlodipine additional arterial selectivity. At therapeutic sub-toxic concentrations, amlodipine has little effect on cardiac myocytes and conduction cells.

mechanism of action

Amlodipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of amlodipine result in an overall decrease in blood pressure. Amlodipine is a long-acting CCB that may be used to treat mild to moderate essential hypertension and exertion-related angina (chronic stable angina). Another possible mechanism is that amlodipine inhibits vascular smooth muscle carbonic anhydrase I activity causing cellular pH increases which may be involved in regulating intracelluar calcium influx through calcium channels.


Gross overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to an including shock with fatal outcome have been reported.


Hepatic. Metabolized extensively (90%) to inactive metabolites via the cytochrome P450 3A4 isozyme.


Amlodipine is slowly and almost completely absorbed from the gastrointestinal tract. Peak plasma concentrations are reached 6-12 hour following oral administration. Its estimated bioavailability is 64-90%. Absorption is not affected by food.

half life

30-50 hours

route of elimination

Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine.

drug interactions

Diltiazem: Diltiazem may increase the serum concentration of amlodipine. Concomitant therapy will result in additive hypotensive effects. Monitor for changes in the hypotensive effect of amlodipine if diltiazem is initiated, discontinued or dose changed.

Quinupristin: This combination presents an increased risk of toxicity

Tacrine: The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Amlopidine, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Amlopidine is initiated, discontinued or if the dose is changed.

Telithromycin: Telithromycin may reduce clearance of Amlopidine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Amlopidine if Telithromycin is initiated, discontinued or dose changed.

Thiopental: The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Amlodipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Amlodipine if Thiopental is initiated, discontinued or dose changed.

Tipranavir: Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Amlopidine. Monitor for changes in Amlopidine therapeutic and toxic effects if Tipranavir is initiated, discontinued or dose changed.

Tizanidine: Amlopidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Voriconazole: Voriconazole may increase the serum concentration of amlodipine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amlodipine if voriconazole is initiated, discontinued or dose changed.