Chemical: Drug
nifedipine

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



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 nifedipine

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP3A4 *1 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *18 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1042713 NC_000005.10:g.148826877G=, NC_000005.10:g.148826877G>A, NC_000005.9:g.148206440G=, NC_000005.9:g.148206440G>A, NG_016421.1:g.5285A=, NG_016421.1:g.5285A>G, NM_000024.5:c.46A=, NM_000024.5:c.46A>G, NP_000015.1:p.Arg16=, NP_000015.1:p.Arg16Gly, XM_005268382.1:c.46G=, XM_005268382.1:c.46G>A, XM_005268383.1:c.46G=, XM_005268383.1:c.46G>A, XP_005268439.1:p.Gly16=, XP_005268439.1:p.Gly16Arg, XP_005268440.1:p.Gly16=, XP_005268440.1:p.Gly16Arg, rs17287432, rs17334179, rs17334242, rs17721693, rs17839749, rs17846639, rs17859732, rs3182174, rs3729940, rs52812686, rs56964295
G > A
SNP
R16G
No VIP available No Clinical Annotations available VA
rs1042714 NC_000005.10:g.148826910G=, NC_000005.10:g.148826910G>C, NC_000005.9:g.148206473G=, NC_000005.9:g.148206473G>C, NG_016421.1:g.5318C=, NG_016421.1:g.5318C>G, NM_000024.5:c.79C=, NM_000024.5:c.79C>G, NP_000015.1:p.Gln27=, NP_000015.1:p.Gln27Glu, XM_005268382.1:c.79G=, XM_005268382.1:c.79G>C, XM_005268383.1:c.79G=, XM_005268383.1:c.79G>C, XP_005268439.1:p.Glu27=, XP_005268439.1:p.Glu27Gln, XP_005268440.1:p.Glu27=, XP_005268440.1:p.Glu27Gln, rs17287411, rs17287474, rs17334200, rs17640526, rs17845338, rs17858183, rs17859733, rs3182175, rs3729941, rs52793394, rs60374884
G > C
G > T
SNP
Q27E
No VIP available CA VA
rs1048101 NC_000008.10:g.26628028A>G, NC_000008.11:g.26770511A>G, NG_029395.1:g.99895T>C, NM_000680.2:c.1039T>C, NM_033302.2:c.1039T>C, NM_033303.3:c.1039T>C, NM_033304.2:c.1039T>C, NP_000671.2:p.Cys347Arg, NP_150645.2:p.Cys347Arg, NP_150646.3:p.Cys347Arg, NP_150647.2:p.Cys347Arg, XM_005273414.1:c.1039T>C, XM_005273414.3:c.1039T>C, XM_006716292.2:c.1039T>C, XM_006716293.2:c.1039T>C, XP_005273471.1:p.Cys347Arg, XP_006716355.1:p.Cys347Arg, XP_006716356.1:p.Cys347Arg, rs17425094, rs3188081, rs3729633, rs386513207, rs52806290, rs57898697
A > G
SNP
C347R
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 VA
rs1123617 NC_000018.10:g.45672918G>A, NC_000018.9:g.43252883G>A, NM_001242692.1:c.2248G>A, NM_007163.3:c.2248G>A, NP_001229621.1:p.Val750Ile, NP_009094.3:p.Val750Ile, XM_011526216.1:c.2248G>A, XM_011526217.1:c.2113G>A, XP_011524518.1:p.Val750Ile, XP_011524519.1:p.Val705Ile, rs2276315, rs386517691, rs52814222, rs59629208
G > A
SNP
V750I
No VIP available No Clinical Annotations available VA
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 No Clinical Annotations available VA
rs2106809 NC_000023.10:g.15618061A>G, NC_000023.11:g.15599938A>G, NG_012575.1:g.7132T>C, NM_021804.2:c.186+788T>C, XM_005274571.1:c.186+788T>C, XM_011545549.1:c.186+788T>C, XM_011545550.1:c.186+788T>C, XM_011545551.1:c.186+788T>C, XM_011545552.1:c.186+788T>C, rs59690101
A > G
SNP
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
rs3745009 NC_000018.10:g.45682394G>A, NC_000018.9:g.43262359G>A, NM_001242692.1:c.2638G>A, NM_007163.3:c.2638G>A, NP_001229621.1:p.Ala880Thr, NP_009094.3:p.Ala880Thr, XM_011526216.1:c.2638G>A, XM_011526217.1:c.2503G>A, XP_011524518.1:p.Ala880Thr, XP_011524519.1:p.Ala835Thr, rs52819242, rs58066525
G > A
SNP
A880T
No VIP available No Clinical Annotations available VA
rs3918242 NC_000020.10:g.44635976C>T, NC_000020.11:g.46007337C>T, NG_011468.1:g.3430C>T, NM_004994.2:c.-1590C>T
C > T
SNP
No VIP available No Clinical Annotations available VA
rs4986910 NC_000007.13:g.99358524A>G, NC_000007.14:g.99760901A>G, NG_008421.1:g.28285T>C, NM_001202855.2:c.1331T>C, NM_017460.5:c.1334T>C, NP_001189784.1:p.Met444Thr, NP_059488.2:p.Met445Thr, XM_011515841.1:c.1427T>C, XM_011515842.1:c.1424T>C, XP_011514143.1:p.Met476Thr, XP_011514144.1:p.Met475Thr, rs386597005, rs60835115
A > G
SNP
M444T
No VIP available No Clinical Annotations available VA
rs4986913 NC_000007.13:g.99358459G>A, NC_000007.14:g.99760836G>A, NG_008421.1:g.28350C>T, NM_001202855.2:c.1396C>T, NM_017460.5:c.1399C>T, NP_001189784.1:p.Pro466Ser, NP_059488.2:p.Pro467Ser, XM_011515841.1:c.1492C>T, XM_011515842.1:c.1489C>T, XP_011514143.1:p.Pro498Ser, XP_011514144.1:p.Pro497Ser, rs386597007
G > A
SNP
P466S
No VIP available CA VA
rs4987161 NC_000007.13:g.99366081A>G, NC_000007.14:g.99768458A>G, NG_008421.1:g.20728T>C, NM_001202855.2:c.566T>C, NM_017460.5:c.566T>C, NP_001189784.1:p.Phe189Ser, NP_059488.2:p.Phe189Ser, XM_011515841.1:c.566T>C, XM_011515842.1:c.566T>C, XP_011514143.1:p.Phe189Ser, XP_011514144.1:p.Phe189Ser
A > G
SNP
F189S
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
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
Trade Names
  • Adalat
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  • Adalat 20
  • Adalat 5
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  • Macorel
  • Megalat
  • Myogard
  • N1fedilat
  • Nedipin
  • Nicardia
  • Nifangin
  • Nifar
  • Nifdemin
  • Nifebene
  • Nifecard
  • Nifecor
  • Nifedepat
  • Nifedicor
  • Nifedin
  • Nifedine
  • Nifedipine Retard
  • Nifedipres
  • Nifedirex LP
  • Nifelan
  • Nifelat
  • Nifelat Q
  • Nifelate
  • Nifensar XL
  • Nificard
  • Nifidine
  • Nifipen
  • Niphedipine
  • Orix
  • Oxcord
  • Pidilat
  • Procardia
  • Procardia XL
  • Sepamit
  • Tibricol
  • Zenusin
Brand Mixture Names

PharmGKB Accession Id

PA450631

Type(s):

Drug

Description

Nifedipine has been formulated as both a long- and short-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, nifedipine 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. Nifedipine is used to treat hypertension and chronic stable angina.

Source: Drug Bank

Indication

For the management of vasospastic angina, chronic stable angina, hypertension, and Raynaud's phenomenon. May be used as a first line agent for left ventricular hypertrophy and isolated systolic hypertension (long-acting agents).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Nifedipine 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 inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. The vasodilatory effects of nifedipine result in an overall decrease in blood pressure.

Source: Drug Bank

Pharmacology

Nifedipine, the prototype of the dihydropyridine class of calcium channel blockers (CCBs), is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, nifedipine binds directly to inactive 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 nifedipine additional arterial selectivity. At therapeutic sub-toxic concentrations, nifedipine has little effect on cardiac myocytes and conduction cells. By blocking the calcium channels, Nifedipine inhibits the spasm of the coronary artery and dilates the systemic arteries, results in a increase of myocardial oxygen supply and a decrease in systemic blood pressure.

Source: Drug Bank

Food Interaction

Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nifedipine and may cause toxicity. Avoid grapefruit products while on this medication.|Avoid alcohol.|Take with low fat meal.|Avoid natural licorice.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic metabolism via cytochrome P450 system. Predominantly metabolized by CYP3A4, but also by CYP1A2 and CYP2A6 isozymes.

Source: Drug Bank

Protein Binding

92-98%

Source: Drug Bank

Absorption

Rapidly and fully absorbed following oral administration.

Source: Drug Bank

Half-Life

2 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include dizziness, drowsiness, nausea, severe drop in blood pressure, slurred speech, and weakness. LD 50=494 mg/kg (orally in mice); LD 50=1022 mg/kg (orally in rats)

Source: Drug Bank

Route of Elimination

Nifedipine is extensively metabolized to highly water-soluble, inactive metabolites accounting for 60 to 80% of the dose excreted in the urine. The remainder is excreted in the feces in metabolized form, most likely as a result of biliary excretion.

Source: Drug Bank

Chemical Properties

Chemical Formula

C17H18N2O6

Source: Drug Bank

Isomeric SMILES

CC1=C(C(C(=C(N1)C)C(=O)OC)c2ccccc2N(=O)=O)C(=O)OC

Source: OpenEye

Canonical SMILES

COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-]

Source: Drug Bank

Average Molecular Weight

346.3346

Source: Drug Bank

Monoisotopic Molecular Weight

346.116486318

Source: Drug Bank

SMILES

COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC

Source: Drug Bank

InChI String

InChI=1S/C17H18N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8,15,18H,1-4H3

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

PharmGKB contains no curated pathways for this drug. If you would like to volunteer to work on a pathway, please let us know.

External Pathways

Links to non-PharmGKB pathways.

  1. cadmium induces dna synthesis and proliferation in macrophages - (BioCarta via Pathway Interaction Database)

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
CACNA1C (source: Drug Bank)
CACNA1D (source: Drug Bank)
CACNA1H (source: Drug Bank)
CACNA1S (source: Drug Bank)
CACNA2D1 (source: Drug Bank)
CACNB2 (source: Drug Bank)
CALM3 (source: Drug Bank)
KCNA1 (source: Drug Bank)

Drug Interactions

Interaction Description
cimetidine - nifedipine Increases the effect of the calcium channel blocker (source: Drug Bank)
cimetidine - nifedipine Cimetidine increases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
cisapride - nifedipine Increases the effect and toxicity of nifedipine (source: Drug Bank)
cisapride - nifedipine Increases the effect and toxicity of nifedipine (source: Drug Bank)
cyclosporine - nifedipine Increased risk of gingivitis (source: Drug Bank)
cyclosporine - nifedipine Increased risk of gingivitis (source: Drug Bank)
imatinib - nifedipine Imatinib increases the effect and toxicity of nifedipine (source: Drug Bank)
imatinib - nifedipine Imatinib increases the effect and toxicity of nifedipine (source: Drug Bank)
melatonin - nifedipine Melatonin can possibly decrease the effect of nifedipine (source: Drug Bank)
melatonin - nifedipine Melatonin can possibly decrease the effect of nifedipine (source: Drug Bank)
nifedipine - amobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - amobarbital The barbiturate, amobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - aprobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - aprobarbital The barbiturate, aprobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - butabarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - butabarbital The barbiturate, butabarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - butalbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - butalbital The barbiturate, butalbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - butethal The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - butethal The barbiturate, butethal, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - cimetidine Cimetidine increases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - cimetidine Cimetidine increases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - cisapride Cisapride increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - cisapride Cisapride increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - cyclosporine Increased risk of gingivitis (source: Drug Bank)
nifedipine - cyclosporine Increased risk of gingivitis (source: Drug Bank)
nifedipine - ginseng Ginseng increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - ginseng Ginseng increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - heptabarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - heptabarbital The barbiturate, heptabarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - hexobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - hexobarbital The barbiturate, hexobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - imatinib Imatinib increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - imatinib Imatinib increases the effect and toxicity of nifedipine (source: Drug Bank)
nifedipine - melatonin Melatonin can possibly decrease the effect of nifedipine (source: Drug Bank)
nifedipine - melatonin Melatonin can possibly decrease the effect of nifedipine (source: Drug Bank)
nifedipine - methohexital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - methohexital The barbiturate, methohexital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - methylphenobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - methylphenobarbital The barbiturate, methylphenobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - pentobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - pentobarbital The barbiturate, pentobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - phenobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - phenobarbital The barbiturate, phenobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - primidone The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - primidone The barbiturate, primidone, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - quinidine Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
nifedipine - quinidine Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
nifedipine - quinidine Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
nifedipine - quinupristin Synercid increases the effect of ziprasidone (source: Drug Bank)
nifedipine - quinupristin Synercid increases the effect of ziprasidone (source: Drug Bank)
nifedipine - rifampin Rifampin decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - rifampin Rifampin decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - secobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - secobarbital The barbiturate, secobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
nifedipine - tacrolimus Nifedipine increases serum levels of tacrolimus (source: Drug Bank)
nifedipine - tacrolimus Nifedipine increases serum levels of tacrolimus (source: Drug Bank)
nifedipine - talbutal The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
nifedipine - talbutal The barbiturate, talbutal, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
phenobarbital - nifedipine The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
phenobarbital - nifedipine The barbiturate, phenobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
primidone - nifedipine The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
primidone - nifedipine The barbiturate, primidone, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
quinidine - nifedipine Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
quinidine - nifedipine Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
quinupristin - nifedipine Synercid increases the effect of ziprasidone (source: Drug Bank)
rifampin - nifedipine Rifampin decreases the effect of the calcium channel blocker (source: Drug Bank)
rifampin - nifedipine Rifampin decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
tacrine - nifedipine The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Nifedipine, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Nifedipine is initiated, discontinued or if the dose is changed. (source: Drug Bank)
telithromycin - nifedipine Telithromycin may reduce clearance of Nifedipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nifedipine if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
thiopental - nifedipine The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nifedipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nifedipine if Thiopental is initiated, discontinued or dose changed. (source: Drug Bank)
thiopental - nifedipine The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nifedipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nifedipine if Thiopental is initiated, discontinued or dose changed. (source: Drug Bank)
tipranavir - nifedipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nifedipine. Monitor for changes in Nifedipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed. (source: Drug Bank)
tizanidine - nifedipine Nifedipine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. (source: Drug Bank)
treprostinil - nifedipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. (source: Drug Bank)
voriconazole - nifedipine Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nifedipine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nifedipine 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 nifedipine: 25

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Nifedipine pharmacokinetics are influenced by CYP3A5 genotype when used as a preterm labor tocolytic. American journal of perinatology. 2013. Haas David M, 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
Matrix metalloproteinase-9 polymorphisms affect plasma MMP-9 levels and antihypertensive therapy responsiveness in hypertensive disorders of pregnancy. The pharmacogenomics journal. 2011. Palei A C T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, 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
eNOS haplotypes affect the responsiveness to antihypertensive therapy in preeclampsia but not in gestational hypertension. The pharmacogenomics journal. 2010. Sandrim V C, 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 CA VA No VIP available No VIP available
Arg347Cys polymorphism of alpha1A-adrenoceptor gene is associated with blood pressure response to nifedipine GITS in Chinese hypertensive patients. Journal of human genetics. 2009. Zhang Yan, 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
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Polymorphisms of ACE2 gene are associated with essential hypertension and antihypertensive effects of Captopril in women. Clinical pharmacology and therapeutics. 2007. Fan X, 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
Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. The Journal of pharmacology and experimental therapeutics. 2007. Faucette Stephanie R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic polymorphisms of the urea transporter gene are associated with antihypertensive response to nifedipine GITS. Methods and findings in experimental and clinical pharmacology. 2007. Hong X, 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 CA VA No VIP available No VIP available
Recombinant CYP3A4*17 is defective in metabolizing the hypertensive drug nifedipine, and the CYP3A4*17 allele may occur on the same chromosome as CYP3A5*3, representing a new putative defective CYP3A haplotype. The Journal of pharmacology and experimental therapeutics. 2005. Lee Su-Jun, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Acute effects of nifedipine administration in pulmonary haemodynamics and oxygen delivery during exercise in patients with chronic obstructive pulmonary disease: implication of the angiotensin-converting enzyme gene polymorphisms. Clinical physiology and functional imaging. 2004. Kanazawa Hiroshi, 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
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug metabolism and disposition: the biological fate of chemicals. 2003. Patki Kiran C, 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
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, 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
Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug metabolism and disposition: the biological fate of chemicals. 2001. Drocourt 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
The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics. 2001. Zhang J, 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
CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity. Clinical pharmacology and therapeutics. 2000. Sata 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
SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes & development. 1998. Blumberg B, 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
Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proceedings of the National Academy of Sciences of the United States of America. 1998. Bertilsson G, 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
Prediction of patient responses to antihypertensive drugs using genetic polymorphisms: investigation of renin-angiotensin system genes. Journal of hypertension. 1996. Dudley C, 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
Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. The Journal of pharmacology and experimental therapeutics. 1994. Shimada T, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0378-3475-01
DrugBank:
DB01115
ChEBI:
7565
KEGG Compound:
C07266
KEGG Drug:
D00437
PubChem Compound:
4485
PubChem Substance:
172894
46505103
IUPHAR Ligand:
2514
Drugs Product Database (DPD):
2235898
BindingDB:
50000778
ChemSpider:
4330
Therapeutic Targets Database:
DAP000529
FDA Drug Label at DailyMed:
62069120-e894-42fd-8927-f1d74e449ca6

Clinical Trials

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

No trials found.

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Sources for PharmGKB drug information: DrugBank, PubChem.