PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
nifedipine

2D structure

Overview

Trade Names: Adalat; Adalat 10; Adalat 20; Adalat 5; Adalat CC; Adalat CR; Adalat Crono; Adalat Ft; Adalat Gits; Adalat Gits 30; Adalat LA; Adalat LP; Adalat Oros; Adalat PA; Adalat Retard; Adalate; Adapine; Adapress; Alat; Aldipin; Alfadal; Alonix; Alonix S; Alpha-Nifedipine Retard; Angipec; Anifed; Anpine; Apo-Nifed; Aprical; Bonacid; Calcibloc; Calcigard; Calcilat; Camont; Cardifen; Cardilat; Cardionorm; Chronadalate; Chronadalate Lp; Citilat; Coracten; Coral; Cordafen; Cordaflex; Cordalat; Cordicant; Cordilan; Cordipin; Corinfar; Corotrend; Corynphar; Depin; Dignokonstant; Dilafed; Dilcor; Dipinkor; Duranifin; Ecodipi; Ecodipin; Ecodipin E; Fedcor; Fedcor Retard; Fenamon; Fenamon Sr; Fenihidin; Fenihidine; Glopir; Hadipin; Hexadilat; Introcar; Kordafen; 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
PharmGKB Accession Id: PA450631

Description

A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. PubChem (source: Drug Bank)

Indication

For the management of vasospastic angina, chronic stable angina and hypertension. (source: Drug Bank)

ATC Therapeutic Category

  • C08CA:Dihydropyridine derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Nifedipine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular 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. (source: Drug Bank)

Pharmacology

Nifedipine, the prototype of the dihydropyridine class of calcium-channel antagonists, is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. Nifedipine is used to treat Prinzmetal's angina, hypertension, and other vascular disorders such as Raynaud's phenomenon. 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 Interactions

Avoid alcohol.
Avoid natural licorice.
Avoid taking with grapefruit juice.
Take with low fat meal. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. (source: Drug Bank)

Protein Binding

92-98% (source: Drug Bank)

Absorption

Rapidly and fully absorbed following oral administration. (source: Drug Bank)

Toxicity

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

Isomeric SMILES Code:

CC1=C(C(C(=C(N1)C)C(=O)OC)c2ccccc2N(=O)=O)C(=O)OC (source: Drug Bank)

In-Depth Annotations (In-Depth Annotation)

  1. rs4987161 at chr7:99204017 in CYP3A, CYP3A4
    Defining variant for CYP3A4*17, defective in metabolizing the hypertensive drug nifedipine in vitro; exhibited lower turnover numbers than wild-type for testosterone and chlorpyrifos in vitro.
    Variant Name:
    CYP3A4:F189S; CYP3A4:670 T>C; CYP3A4:189 Phe>Ser; CYP3A4*17
    Related Drugs:
    nifedipine
    Evidence:
    http://www.pharmgkb.org/.../haplotype.jsp#ImportantHaplotypeInformationforCYP3A4-3

Curated Annotations (Curated Annotation)

  1. rs699 at chr1:228912417 in AGT
    The AGT:Met235Thr variant was not associated with response to antihypertensives in a study of 97 hypertensive British individuals.
    Variant Name:
    AGT M235T, AGT:Met235Thr
    Related Drugs:
    atenolol, lisinopril, nifedipine
    Related Diseases:
    Hypertension
    Evidence:
    PMID:8728305
  2. rs1123617 at chr18:41506881 in SLC14A2
    In a Chinese population, this SNP was significantly associated with blood pressure response to nifedipine treatment.
    Variant Name:
    SLC14A2:Val227Ile
    Related Drugs:
    nifedipine
    Related Diseases:
    Hypertension
    Evidence:
    PMID:17344938
  3. rs3745009 at chr18:41516357 in SLC14A2
    In a Chinese population, this SNP was significantly associated with blood pressure response to nifedipine treatment.
    Variant Name:
    SLC14A2:Ala357Thr
    Related Drugs:
    nifedipine
    Related Diseases:
    Hypertension
    Evidence:
    PMID:17344938
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ACE
  • CO
  • PD
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
ACE2
  • CO
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
AGT
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
CACNA1C
  •   
  • PD
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2B6
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  •   
  •   
  •   
Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
  •   
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
NOS3
  •   
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available No genotype data No literature annotations Not annotated
SLC14A2
  •   
  •   
  •   
  •   
  •   
Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
CACNA2D1 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
  •   
  •   
  •   
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
amobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
aprobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
butabarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
butalbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
butethal Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
cimetidine Uncurated Annotation Cimetidine increases the effect of the calcium channel blocker (source: Drug Bank)
cisapride Uncurated Annotation Cisapride increases the effect and toxicity of nifedipine (source: Drug Bank)
cyclosporine Uncurated Annotation Increased risk of gingivitis (source: Drug Bank)
ginseng Uncurated Annotation Ginseng increases the effect and toxicity of nifedipine (source: Drug Bank)
heptabarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
hexobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
imatinib Uncurated Annotation Imatinib increases the effect and toxicity of nifedipine (source: Drug Bank)
melatonin Uncurated Annotation Melatonin can possibly decrease the effect of nifedipine (source: Drug Bank)
methohexital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
methylphenobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
pentobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
phenobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
primidone Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
quinidine Uncurated Annotation Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
quinidine Uncurated Annotation Decreased quinidine effect, increased nifedipine effect (source: Drug Bank)
quinupristin Uncurated Annotation Synercid increases the effect of ziprasidone (source: Drug Bank)
rifampin Uncurated Annotation Rifampin decreases the effect of the calcium channel blocker (source: Drug Bank)
secobarbital Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
tacrolimus Uncurated Annotation Nifedipine increases serum levels of tacrolimus (source: Drug Bank)
talbutal Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Gestational hypertension
  •   
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Hypertension
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Pre-Eclampsia
  •   
  • PD
  •   
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

  1. In vivo and in vitro characterization of variants
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • PD
    • PK
    • FA
    Submitted by Mary Relling, PharmD involving CYP3A, CYP3A4, CYP3A5, NR1I2, , midazolam, nifedipine, rifampin and troleandomycin

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance
  2. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01115
ChEBI ID:
7565
KEGG Compound ID:
C07266
KEGG Drug ID:
D00437
PubChem Compound ID:
4485
PubChem Substance ID:
172894
IUPHAR Ligand ID:
2514

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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