Chemical: Drug
amlodipine

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.


1. FDA Label for amlodipine

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Cardiomyopathies
    • Warnings section
    • source: PHONT
  • Cardiovascular Diseases
    • Indications & usage section
    • source: PHONT
  • Coronary Disease
    • Indications & usage section
    • source: PHONT
  • Death
    • Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Diabetes Mellitus
    • Indications & usage section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Heart Failure
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Hypertension
    • Indications & usage section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Myocardial Infarction
    • Indications & usage section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Stroke
    • Indications & usage section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for amlodipine

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
No VIP available No Clinical Annotations available VA
rs10494366 NC_000001.10:g.162085685G>T, NC_000001.11:g.162115895G>T, NG_015979.1:g.51105G>T, NM_001164757.1:c.106-38510G>T, NM_014697.2:c.106-38510G>T, XR_922217.1:n.884-1993C>A, XR_922219.1:n.713-1993C>A, XR_922221.1:n.713-9147C>A, rs59845656
G > T
SNP
No VIP available CA No Variant Annotations available
rs11122576 NC_000001.10:g.230846679T>C, NC_000001.11:g.230710933T>C, NG_008836.1:g.8658A>G, NM_000029.3:c.-3-80A>G, rs58482950, rs59792559
T > C
SNP
No VIP available CA VA
rs12143842 NC_000001.10:g.162033890C>T, NC_000001.11:g.162064100C>T, rs59411707
C > T
SNP
rs1799752 NC_000017.10:g.61565890_61565891insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NC_000017.10:g.61565890_61565891insG, NC_000017.11:g.63488529_63488530insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NC_000017.11:g.63488529_63488530insG, NG_011648.1:g.16457_16458insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NG_011648.1:g.16457_16458insG, NM_000789.3:c.2306-119_2306-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NM_000789.3:c.2306-119_2306-118insG, NM_001178057.1:c.584-119_584-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NM_001178057.1:c.584-119_584-118insG, NM_152830.2:c.584-119_584-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, NM_152830.2:c.584-119_584-118insG, XM_005257110.1:c.1757-119_1757-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, XM_005257110.1:c.1757-119_1757-118insG, XM_006721737.2:c.644-119_644-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, XM_006721737.2:c.644-119_644-118insG
- > ATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC
- > G
indel
No VIP available CA No Variant Annotations available
rs200148 NC_000006.11:g.143345696G>A, NC_000006.12:g.143024559G>A, NR_038987.1:n.595-2606C>T, rs61230468, rs629392
G > A
SNP
No VIP available No Clinical Annotations available VA
rs2032582 NC_000007.13:g.87160618A>C, NC_000007.13:g.87160618A>T, NC_000007.14:g.87531302A>C, NC_000007.14:g.87531302A>T, NG_011513.1:g.186947T>A, NG_011513.1:g.186947T>G, NM_000927.4:c.2677T>A, NM_000927.4:c.2677T>G, NP_000918.2:p.Ser893Ala, NP_000918.2:p.Ser893Thr, rs10228331, rs2229106, rs386553610, rs57135550, rs9641018
A > C
SNP
S893A
No VIP available No Clinical Annotations available VA
rs2238032 NC_000012.11:g.2222732T>G, NC_000012.12:g.2113566T>G, NG_008801.2:g.147781T>G, NM_000719.6:c.50-1658T>G, NM_001129827.1:c.50-1658T>G, NM_001129829.1:c.50-1658T>G, NM_001129830.1:c.50-1658T>G, NM_001129830.2:c.50-1658T>G, NM_001129831.1:c.50-1658T>G, NM_001129832.1:c.50-1658T>G, NM_001129833.1:c.50-1658T>G, NM_001129834.1:c.50-1658T>G, NM_001129835.1:c.50-1658T>G, NM_001129836.1:c.50-1658T>G, NM_001129837.1:c.50-1658T>G, NM_001129838.1:c.50-1658T>G, NM_001129839.1:c.50-1658T>G, NM_001129840.1:c.50-1658T>G, NM_001129841.1:c.50-1658T>G, NM_001129842.1:c.50-1658T>G, NM_001129843.1:c.50-1658T>G, NM_001129844.1:c.50-1658T>G, NM_001129846.1:c.50-1658T>G, NM_001167623.1:c.50-1658T>G, NM_001167624.2:c.50-1658T>G, NM_001167625.1:c.50-1658T>G, NM_199460.3:c.50-1658T>G, XM_005253765.1:c.140-1658T>G, XM_005253766.1:c.50-1658T>G, XM_005253767.1:c.50-1658T>G, XM_005253768.1:c.50-1658T>G, XM_005253769.1:c.50-1658T>G, XM_005253770.1:c.50-1658T>G, XM_005253771.1:c.50-1658T>G, XM_005253772.1:c.50-1658T>G, XM_005253773.1:c.50-1658T>G, XM_005253774.1:c.50-1658T>G, XM_005253775.1:c.50-1658T>G, XM_005253776.1:c.50-1658T>G, XM_005253777.1:c.50-1658T>G, XM_005253778.1:c.50-1658T>G, XM_005253779.1:c.50-1658T>G, XM_005253780.1:c.50-1658T>G, XM_005253781.1:c.50-1658T>G, XM_005253782.1:c.50-1658T>G, XM_005253783.1:c.50-1658T>G, XM_005253784.1:c.50-1658T>G, XM_005253785.1:c.50-1658T>G, XM_005253786.1:c.50-1658T>G, XM_005253787.1:c.50-1658T>G, XM_006719017.1:c.140-1658T>G, XM_011521018.1:c.-1069-1658T>G, XM_011521020.1:c.140-1658T>G, XM_011521021.1:c.50-1658T>G, XM_011521022.1:c.50-1658T>G, XM_011521023.1:c.50-1658T>G
T > G
SNP
No VIP available No Clinical Annotations available VA
rs2239050 NC_000012.11:g.2447414G>C, NC_000012.12:g.2338248G>C, NG_008801.2:g.372463G>C, NM_000719.6:c.478-110728G>C, NM_001129827.1:c.478-110728G>C, NM_001129829.1:c.478-110728G>C, NM_001129830.1:c.478-110728G>C, NM_001129830.2:c.478-110728G>C, NM_001129831.1:c.478-110728G>C, NM_001129832.1:c.478-110728G>C, NM_001129833.1:c.478-110728G>C, NM_001129834.1:c.478-110728G>C, NM_001129835.1:c.478-110728G>C, NM_001129836.1:c.478-110728G>C, NM_001129837.1:c.478-110728G>C, NM_001129838.1:c.478-110728G>C, NM_001129839.1:c.478-110728G>C, NM_001129840.1:c.478-110728G>C, NM_001129841.1:c.478-110728G>C, NM_001129842.1:c.478-110728G>C, NM_001129843.1:c.478-110728G>C, NM_001129844.1:c.478-110728G>C, NM_001129846.1:c.478-110728G>C, NM_001167623.1:c.478-110728G>C, NM_001167624.2:c.478-110728G>C, NM_001167625.1:c.478-110728G>C, NM_199460.3:c.478-110728G>C, XM_005253765.1:c.568-110728G>C, XM_005253766.1:c.487-110728G>C, XM_005253767.1:c.487-110728G>C, XM_005253768.1:c.487-110728G>C, XM_005253769.1:c.487-110728G>C, XM_005253770.1:c.487-110728G>C, XM_005253771.1:c.487-110728G>C, XM_005253772.1:c.487-110728G>C, XM_005253773.1:c.487-110728G>C, XM_005253774.1:c.487-110728G>C, XM_005253775.1:c.487-110728G>C, XM_005253776.1:c.487-110728G>C, XM_005253777.1:c.487-110728G>C, XM_005253778.1:c.487-110728G>C, XM_005253779.1:c.487-110728G>C, XM_005253780.1:c.487-110728G>C, XM_005253781.1:c.487-110728G>C, XM_005253782.1:c.487-110728G>C, XM_005253783.1:c.487-110728G>C, XM_005253784.1:c.487-110728G>C, XM_005253785.1:c.487-110728G>C, XM_005253786.1:c.487-110728G>C, XM_005253787.1:c.487-110728G>C, XM_006719017.1:c.568-110728G>C, XM_011521018.1:c.-641-110728G>C, XM_011521020.1:c.568-110728G>C, XM_011521021.1:c.478-110728G>C, XM_011521022.1:c.478-110728G>C, XM_011521023.1:c.478-110728G>C, rs56640547, rs57375424
G > C
SNP
No VIP available No Clinical Annotations available VA
rs2239128 NC_000012.11:g.2757769T>C, NC_000012.12:g.2648603T>C, NG_008801.2:g.682818T>C, NM_000719.6:c.3945+96T>C, NM_001129827.1:c.4089+96T>C, NM_001129829.1:c.3945+96T>C, NM_001129830.1:c.3945+96T>C, NM_001129830.2:c.3945+96T>C, NM_001129831.1:c.4029+96T>C, NM_001129832.1:c.4005+96T>C, NM_001129833.1:c.3945+96T>C, NM_001129834.1:c.3945+96T>C, NM_001129835.1:c.3945+96T>C, NM_001129836.1:c.3997-3037T>C, NM_001129837.1:c.3913-3037T>C, NM_001129838.1:c.3913-3037T>C, NM_001129839.1:c.3907-3037T>C, NM_001129840.1:c.3945+96T>C, NM_001129841.1:c.3945+96T>C, NM_001129842.1:c.3945+96T>C, NM_001129843.1:c.3945+96T>C, NM_001129844.1:c.3936+96T>C, NM_001129846.1:c.3913-3037T>C, NM_001167623.1:c.3945+96T>C, NM_001167624.2:c.3945+96T>C, NM_001167625.1:c.3913-3037T>C, NM_199460.3:c.4089+96T>C, XM_005253765.1:c.4239+96T>C, XM_005253766.1:c.4098+96T>C, XM_005253767.1:c.3922-3037T>C, XM_005253768.1:c.4098+96T>C, XM_005253769.1:c.3954+96T>C, XM_005253770.1:c.3954+96T>C, XM_005253771.1:c.3954+96T>C, XM_005253772.1:c.4038+96T>C, XM_005253773.1:c.4014+96T>C, XM_005253774.1:c.3954+96T>C, XM_005253775.1:c.3954+96T>C, XM_005253776.1:c.3954+96T>C, XM_005253777.1:c.4006-3037T>C, XM_005253778.1:c.3922-3037T>C, XM_005253779.1:c.3922-3037T>C, XM_005253780.1:c.3916-3037T>C, XM_005253781.1:c.3954+96T>C, XM_005253782.1:c.3954+96T>C, XM_005253783.1:c.3954+96T>C, XM_005253784.1:c.3954+96T>C, XM_005253785.1:c.3954+96T>C, XM_005253786.1:c.3945+96T>C, XM_005253787.1:c.3922-3037T>C, XM_005253788.1:c.1851+96T>C, XM_006719017.1:c.4035+96T>C, XM_011521017.1:c.3189+96T>C, XM_011521018.1:c.2634+96T>C, XM_011521019.1:c.744+96T>C, XM_011521020.1:c.4110+96T>C, XM_011521021.1:c.3945+96T>C, XM_011521022.1:c.3945+96T>C, XM_011521023.1:c.4020+96T>C, rs58064366
T > C
SNP
No VIP available CA VA
rs2246709 NC_000007.13:g.99365719A>G, NC_000007.14:g.99768096A>G, NG_008421.1:g.21090T>C, NM_001202855.2:c.670+258T>C, NM_017460.5:c.670+258T>C, XM_011515841.1:c.670+258T>C, XM_011515842.1:c.670+258T>C, rs56901335
A > G
SNP
No VIP available CA VA
rs2740574 NC_000007.13:g.99382096C>T, NC_000007.14:g.99784473C>T, NG_008421.1:g.4713G>A, NM_001202855.2:c.-392G>A, NM_017460.5:c.-392G>A, XM_011515841.1:c.-392G>A, XM_011515842.1:c.-392G>A, rs3176920, rs36231114, rs59393892
C > T
SNP
No VIP available CA VA
rs4291 NC_000017.10:g.61554194T>A, NC_000017.11:g.63476833T>A, NG_011648.1:g.4761T>A, NM_000789.3:c.-262T>A, XM_005257110.1:c.-717T>A
T > A
SNP
No VIP available CA VA
rs5065 NC_000001.10:g.11906068A>G, NC_000001.11:g.11846011A>G, NG_012926.1:g.6773T>C, NM_006172.3:c.454T>C, NP_006163.1:p.Ter152Arg, NR_037806.1:n.1479+245A>G, rs1130764, rs17413194, rs17856153, rs198363, rs3189984, rs57081035
A > G
SNP
*152R
No VIP available No Clinical Annotations available VA
rs5443 NC_000012.11:g.6954875C>T, NC_000012.12:g.6845711C>T, NG_009100.1:g.10501C>T, NM_001297571.1:c.822C>T, NM_002075.3:c.825C>T, NP_001284500.1:p.Ser274=, NP_002066.1:p.Ser275=, NW_003871083.2:g.47295C>T, XM_005253679.1:c.825C>T, XM_005253680.1:c.822C>T, XM_005253681.1:c.702-6C>T, XM_005277751.1:c.825C>T, XM_005277752.1:c.822C>T, XM_005277753.1:c.702-6C>T, XM_011520953.1:c.825C>T, XM_011520954.1:c.822C>T, XM_011521027.1:c.*1818G>A, XM_011521028.1:c.*1818G>A, XM_011521029.1:c.*2036G>A, XM_011521030.1:c.*1969G>A, XP_005253736.1:p.Ser275=, XP_005253737.1:p.Ser274=, XP_005277808.1:p.Ser275=, XP_005277809.1:p.Ser274=, XP_011519255.1:p.Ser275=, XP_011519256.1:p.Ser274=, rs2230334, rs3138516, rs57419337, rs6489738
C > T
SNP
S274S
rs776746 NC_000007.13:g.99270539C>T, NC_000007.14:g.99672916T>C, NG_007938.1:g.12083G=, NG_007938.1:g.12083G>A, NM_000777.4:c.219-237A>G, NM_000777.4:c.219-237G>A, NM_001190484.2:c.219-237A>G, NM_001190484.2:c.219-237G>A, NM_001291829.1:c.-253-1A>G, NM_001291829.1:c.-253-1G>A, NM_001291830.1:c.189-237A>G, NM_001291830.1:c.189-237G>A, NR_033807.2:n.717-1A>G, NR_033807.2:n.717-1G>A, NR_033808.1:n.689-1G>A, NR_033809.1:n.581-237G>A, NR_033810.1:n.689-1G>A, NR_033811.1:n.321-1G>A, NR_033812.1:n.321-1G>A, XM_005250169.1:c.189-237G>A, XM_005250170.1:c.-357-1G>A, XM_005250171.1:c.-253-1G>A, XM_005250172.1:c.-254G>A, XM_005250173.1:c.-331-237G>A, XM_005250198.1:c.806-4288C>T, XM_006715859.2:c.219-237A>G, XM_011515843.1:c.-254A>G, XM_011515844.1:c.-229-237A>G, XM_011515845.1:c.-463-1A>G, XM_011515846.1:c.-331-237A>G, XM_011515847.1:c.-571-1A>G, XR_927383.1:n.344-237A>G, XR_927402.1:n.1466+48736T>C, rs10361242, rs11266830, rs386613022, rs58244770
C > T
SNP
No VIP available No Clinical Annotations available VA
rs877087 NC_000015.10:g.33582074T>C, NC_000015.9:g.33874275T>C, NM_001036.4:c.1573+431T>C, NM_001243996.2:c.1573+431T>C, XM_005254587.1:c.1573+431T>C, XM_005254588.1:c.1573+431T>C, XM_011521880.1:c.1573+431T>C, rs111190022, rs17236203, rs58291053
T > C
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Amlodipine Benzenesulfonate
  • Amlodipine Besilate
  • Amlodipine Besylate
  • Amlodipine Free Base
  • Amlodipino [Spanish]
  • Amlodipinum [Latin]
Trade Names
  • Amlocard
  • Amlodis
  • Amvaz
  • Coroval
  • Lipinox
  • Lotrel
  • Norvasc
Brand Mixture Names
  • Lotrel (amlodipine + benazepril)

PharmGKB Accession Id

PA448388

Type(s):

Drug

Description

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.

Source: Drug Bank

Indication

For the treatment of hypertension and chronic stable angina.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

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.

Source: Drug Bank

Pharmacology

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.

Source: Drug Bank

Food Interaction

Grapefruit down regulates post-translational expression of CYP3A4, the major metabolizing enzyme of amlodipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of amlodipine and may cause toxicity. Avoid grapefruit products while on this medication.|Take without regard to meals.|Avoid natural licorice.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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

Source: Drug Bank

Protein Binding

97.5%

Source: Drug Bank

Absorption

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.

Source: Drug Bank

Half-Life

30-50 hours

Source: Drug Bank

Toxicity

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.

Source: Drug Bank

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.

Source: Drug Bank

Chemical Properties

Chemical Formula

C20H25ClN2O5

Source: Drug Bank

Isomeric SMILES

CCOC(=O)C1=C(NC(=C(C1c2ccccc2Cl)C(=O)OC)C)COCCN

Source: OpenEye

Canonical SMILES

CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC

Source: Drug Bank

Average Molecular Weight

408.876

Source: Drug Bank

Monoisotopic Molecular Weight

408.145199627

Source: Drug Bank

SMILES

CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC

Source: Drug Bank

InChI String

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

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
CA1 (source: Drug Bank )
CACNA1B (source: Drug Bank )
CACNA1C (source: Drug Bank )
CACNA1D (source: Drug Bank )
CACNA1S (source: Drug Bank )
CACNA2D1 (source: Drug Bank )
CACNA2D3 (source: Drug Bank )
CACNB2 (source: Drug Bank )
CACNG1 (source: Drug Bank )

Drug Interactions

Interaction Description
amlodipine - diltiazem Diltiazem increases the effect and toxicity of amlodipine (source: Drug Bank )
amlodipine - diltiazem Diltiazem increases the effect and toxicity of amlodipine (source: Drug Bank )
amlodipine - quinupristin This combination presents an increased risk of toxicity (source: Drug Bank )
diltiazem - amlodipine Increases the effect and toxicity of amlodipine (source: Drug Bank )
diltiazem - amlodipine Increases the effect and toxicity of amlodipine (source: Drug Bank )
quinupristin - amlodipine This combination presents an increased risk of toxicity (source: Drug Bank )
tacrine - amlodipine 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. (source: Drug Bank )
telithromycin - amlodipine 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. (source: Drug Bank )
thiopental - amlodipine 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. (source: Drug Bank )
thiopental - amlodipine 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. (source: Drug Bank )
tipranavir - amlodipine 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. (source: Drug Bank )
tizanidine - amlodipine Amlopidine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. (source: Drug Bank )
treprostinil - amlodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. (source: Drug Bank )
voriconazole - amlodipine 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. (source: Drug Bank )

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to amlodipine: 26

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Influence of G-protein beta-Polypeptide 3 C825T Polymorphism on Antihypertensive Response to Telmisartan and Amlodipine in Chinese Patients. Chinese medical journal. 2016. Zhang Zan-Lin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A new adverse drug reaction - Schamberg's disease caused by amlodipine administration - a case report. British journal of clinical pharmacology. 2015. Schetz Daria, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mechanisms and assessment of statin-related muscular adverse effects. British journal of clinical pharmacology. 2014. Moßhammer Dirk, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic effects of 'candidate gene complexes' on stroke in the GenHAT study. Pharmacogenetics and genomics. 2014. Sørensen Izel F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Adoption of a clinical pharmacogenomics implementation program during outpatient care-initial results of the University of Chicago "1,200 Patients Project". American journal of medical genetics. Part C, Seminars in medical genetics. 2014. O'Donnell Peter H, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
The effects of angiotensinogen gene polymorphisms on cardiovascular disease outcomes during antihypertensive treatment in the GenHAT study. Frontiers in pharmacology. 2014. Do Anh N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Amlodipine - Not a Significant Contributor to Clopidogrel Non-Response?. Heart (British Cardiac Society). 2013. Kreutz Rolf P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
RYR3 gene polymorphisms and cardiovascular disease outcomes in the context of antihypertensive treatment. The pharmacogenomics journal. 2012. Lynch A I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
STK39 variation predicts the ambulatory blood pressure response to losartan in hypertensive men. Hypertension research : official journal of the Japanese Society of Hypertension. 2012. Donner Kati M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic association of hypertension candidate genes with fasting glucose in the GenHAT Study. Journal of hypertension. 2010. Irvin Marguerite R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Tacrolimus nephrotoxicity: beware of the association of diarrhea, drug interaction and pharmacogenetics. Pediatric nephrology (Berlin, Germany). 2010. Leroy Sandrine, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP3A4 and CYP3A5 polymorphisms and blood pressure response to amlodipine among African-American men and women with early hypertensive renal disease. American journal of nephrology. 2010. Bhatnagar Vibha, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Dihydropyridines: evaluation of their current and future pharmacological applications. Drug discovery today. 2009. Edraki Najmeh, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of cytochrome P450 3A5*3 genotype on the stereoselective pharmacokinetics of amlodipine in healthy subjects. Chirality. 2009. Kim Kyoung-Ah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Medicinal Chemistry of Drugs used in Diabetic Cardiomyopathy. Current medicinal chemistry. 2009. Adeghate E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Renin-angiotensin system and alpha-adducin gene polymorphisms and their relation to responses to antihypertensive drugs: results from the GENRES study. American journal of hypertension. 2009. Suonsyrjä Timo, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A common NOS1AP genetic polymorphism is associated with increased cardiovascular mortality in users of dihydropyridine calcium channel blockers. British journal of clinical pharmacology. 2009. Becker Matthijs L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic association of the NPPA T2238C genetic variant with cardiovascular disease outcomes in patients with hypertension. JAMA : the journal of the American Medical Association. 2008. Lynch Amy I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Antihypertensive therapy, the alpha-adducin polymorphism, and cardiovascular disease in high-risk hypertensive persons: the Genetics of Hypertension-Associated Treatment Study. The pharmacogenomics journal. 2007. Davis B R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Effect of ABCB1 (MDR1) haplotypes derived from G2677T/C3435T on the pharmacokinetics of amlodipine in healthy subjects. British journal of clinical pharmacology. 2007. Kim Kyoung-Ah, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effect of CYP3A5*3 genotype on the pharmacokinetics and pharmacodynamics of amlodipine in healthy Korean subjects. Clinical pharmacology and therapeutics. 2006. Kim Kyoung-Ah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
CACNA1C polymorphisms are associated with the efficacy of calcium channel blockers in the treatment of hypertension. Pharmacogenomics. 2006. Bremer Troy, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetic association of the angiotensin-converting enzyme insertion/deletion polymorphism on blood pressure and cardiovascular risk in relation to antihypertensive treatment: the Genetics of Hypertension-Associated Treatment (GenHAT) study. Circulation. 2005. Arnett Donna K, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
53808-0200-1
DrugBank:
DB00381
ChEBI:
2668
KEGG Compound:
C06825
PubChem Compound:
2162
PubChem Substance:
193166
46507214
Drugs Product Database (DPD):
878936
ChemSpider:
2077
Therapeutic Targets Database:
DAP000139
FDA Drug Label at DailyMed:
a10fa641-ac6b-466d-bcba-31c678a74be8

Clinical Trials

These are trials that mention amlodipine and are related to either pharmacogenetics or pharmacogenomics.

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NURSA Datasets

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No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.