Identification
- Summary
Nifedipine is a dihydropyridine calcium channel blocker indicated for the management of several subtypes of angina pectoris, and hypertension.
- Brand Names
- Adalat, Afeditab CR, Nifediac, Nifedical, Procardia
- Generic Name
- Nifedipine
- DrugBank Accession Number
- DB01115
- Background
Nifedipine, or BAY a 1040, is a first generation dihydropyridine L-type calcium channel blocker, similar to nicardipine.3,10,11,13 Nifedipine was developed by Bayer and first described in the literature, along with other dihydropyridines, in 1972.11,12 Since nifedipine's development, second and third generation dihydropyridines have been developed with slower onsets and longer durations of action.10 The most popular of the third generation dihydropyridines is amlodipine.10
Nifedipine was granted FDA approval on 31 December 1981.13
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Nifedipine (DB01115)
- Weight
- Average: 346.3346
Monoisotopic: 346.116486318 - Chemical Formula
- C17H18N2O6
- Synonyms
- 4-(2'-Nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsäuredimethylester
- Nifedipine
- Nifedipino
- Nifedipinum
- External IDs
- BAY A 1040
Pharmacology
- Indication
Nifedipine capsules are indicated to treat vasospastic angina and chronic stable angina.13 Extended release tablets are indicated to treat vasospastic angina, chronic stable angina, and hypertension.14,15
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Achalasia ••• ••••• Used in combination to treat Anal fissures Combination Product in combination with: Lidocaine (DB00281) ••• ••• ••••• Management of Chronic stable angina pectoris •••••••••••• •••••• •••••••••••• ••••••• ••••••• •••••••• ••••••• Management of Hypertension •••••••••••• ••••••• •••••••• ••••••• Treatment of Hypertensive emergency ••• ••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Nifedipine is an inhibitor of L-type voltage gated calcium channels that reduces blood pressure and increases oxygen supply to the heart.1 Immediate release nifedipine's duration of action requires dosing 3 times daily.13 Nifedipine dosing is generally 10-120mg daily.13 Patients should be counselled regarding the risk of excessive hypotension, angina, and myocardial infarction.13
- Mechanism of action
Nifedipine blocks voltage gated L-type calcium channels in vascular smooth muscle and myocardial cells.1 This blockage prevents the entry of calcium ions into cells during depolarization, reducing peripheral arterial vascular resistance and dilating coronary arteries.1 These actions reduce blood pressure and increase the supply of oxygen to the heart, alleviating angina.1
Target Actions Organism AVoltage-dependent L-type calcium channel subunit alpha-1C inhibitorHumans AVoltage-dependent L-type calcium channel subunit alpha-1D inhibitorHumans AVoltage-dependent L-type calcium channel subunit beta-2 inhibitorHumans UNuclear receptor subfamily 1 group I member 2 agonistHumans UCalmodulin inhibitorHumans UVoltage-dependent L-type calcium channel subunit alpha-1S inhibitorHumans UPotassium voltage-gated channel subfamily D member 3 inhibitorHumans UVoltage-dependent T-type calcium channel inhibitorHumans - Absorption
Sublingual dosing leads to a Cmax of 10ng/mL, with a Tmax of 50min, and an AUC of 25ng*h/mL.9 Oral dosing leads to a Cmax of 82ng/mL, with a Tmax of 28min, and an AUC of 152ng*h/mL.9
Nifedipine is a Biopharmaceutics Classification System Class II drug, meaning it has low solubility and high intestinal permeability.8 It is almost completely absorbed in the gastrointestinal tract but has a bioavilability of 45-68%, partly due to first pass metabolism.3,8
- Volume of distribution
The steady state volume of distribution of nifedipine is 0.62-0.77L/kg and the volume of distribution of the central compartment is 0.25-0.29L/kg.3
- Protein binding
Nifedipine is 92-98% protein bound in serum.13 Nifedipine is 97±12% bound in a 40g/L solution of pure albumin.2 Nifedipine is 51.4±5.9% protein bound in a 50mg/100mL solution of alpha-1-acid glycoprotein, and 75.5±3.5% protein bound in a 150mg/mL solution.2
- Metabolism
Nifedipine is predominantly metabolized by CYP3A4.1,8,13,14,15 Nifedipine is predominantly metabolized to 2,6-dimethyl-4-(2-nitrophenyl)-5-methoxycarbonyl-pyridine-3-carboxylic acid, and then further metabolized to 2-hydroxymethyl-pyridine carboxylic acid.6 Nifedipine is also minorly metabolized to dehydronifedipine.7
Hover over products below to view reaction partners
- Route of elimination
Nifedipine is 60-80% recovered in the urine as inactive water soluble metabolites, and the rest is eliminated in the feces as metabolites.14
- Half-life
The terminal elimination half life of nifedipine is approximately 2 hours.3,8
- Clearance
The total body clearance of nifedipine is 450-700mL/min.3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The oral LD50 in rats is 1022mg/kg and in mice is 202mg/kg.16
Patients experiencing an overdose may present with hypotension, sinus node dysfunction, atrioventricular node dysfunction, and reflex tachycardia.4,5 Overdose may be managed by monitoring cardiovascular and respiratory function; elevating extremities; and administering vasopressors, fluids, and calcium infusions.13
- Pathways
Pathway Category Nifedipine Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Nifedipine which could result in a higher serum level. Abaloparatide The risk or severity of adverse effects can be increased when Nifedipine is combined with Abaloparatide. Abametapir The serum concentration of Nifedipine can be increased when it is combined with Abametapir. Abatacept The metabolism of Nifedipine can be increased when combined with Abatacept. Abiraterone The serum concentration of Nifedipine can be increased when it is combined with Abiraterone. - Food Interactions
- Avoid excessive or chronic alcohol consumption.
- Avoid grapefruit products. 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 natural licorice.
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Adapine / Afeditab / Coracten / Nifecard / Nifecor / Nifedical / NifedicalXL / Nifedipres
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Adalat Capsule 5 mg Oral Bayer 1997-01-07 2005-07-27 Canada 
Adalat - Cap 10mg Capsule 10 mg Oral Bayer 1982-12-31 2005-07-27 Canada Adalat Cap 10mg Capsule 10 mg Oral Miles Canada Inc. Pharmaceutical Division 1982-12-31 2000-08-01 Canada Adalat Cap 5mg Capsule 5 mg Oral Miles Canada Inc. Pharmaceutical Division 1986-12-31 2000-08-01 Canada Adalat CC Tablet, film coated 30 mg/1 Oral Bayer 1993-04-21 2017-12-10 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Afeditab CR Tablet, film coated, extended release 30 mg/1 Oral Carilion Materials Management 2002-11-01 Not applicable US 
Afeditab CR Tablet, film coated, extended release 60 mg/1 Oral bryant ranch prepack 2002-11-01 2010-05-01 US Afeditab CR Tablet, film coated, extended release 30 mg/1 Oral Actavis Pharma, Inc. 2002-11-01 2019-01-31 US 
Afeditab CR Tablet, film coated, extended release 60 mg/1 Oral Aphena Pharma Solutions Tennessee, Inc. 2002-11-01 Not applicable US Afeditab CR Tablet, film coated, extended release 60 mg/1 Oral Actavis Pharma, Inc. 2002-11-01 2018-11-30 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Adalat XL Plus Nifedipine (30 mg) + Acetylsalicylic acid (81 mg) Kit; Tablet, delayed release; Tablet, extended release Oral Bayer 2008-07-24 2014-07-18 Canada Adalat XL Plus Nifedipine (20 mg) + Acetylsalicylic acid (81 mg) Kit; Tablet, delayed release; Tablet, extended release Oral Bayer 2008-07-24 2014-07-18 Canada Adalat XL Plus Nifedipine (60 mg) + Acetylsalicylic acid (81 mg) Kit; Tablet, delayed release; Tablet, extended release Oral Bayer 2008-07-24 2014-07-18 Canada BELNIF Nifedipine (15 mg/1) + Metoprolol tartrate (50 mg/1) Capsule, extended release Oral 2018-10-01 2021-09-15 Germany 
BETA - NICARDIA CAPSULE Nifedipine (20 mg) + Atenolol (50 mg) Capsule Oral SINGAPORE PHARMACEUTICAL PRIVATE LIMITED 2003-08-14 Not applicable Singapore 
Categories
- ATC Codes
- C08CA55 — Nifedipine, combinations
- C08CA — Dihydropyridine derivatives
- C08C — SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- C08GA — Calcium channel blockers and diuretics
- C08G — CALCIUM CHANNEL BLOCKERS AND DIURETICS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- C08CA — Dihydropyridine derivatives
- C08C — SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Agents causing hyperkalemia
- Antiarrhythmic agents
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Beta blocking agents and calcium channel blockers
- Bradycardia-Causing Agents
- BSEP/ABCB11 Inhibitors
- BSEP/ABCB11 Substrates
- Calcium Channel Blockers
- Calcium Channel Blockers (Dihydropyridine)
- Calcium Channel Blockers and Diuretics
- Calcium-Regulating Hormones and Agents
- Cardiovascular Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2A6 Substrates
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dihydropyridine Derivatives
- Dihydropyridines
- Drugs that are Mainly Renally Excreted
- Hypotensive Agents
- Membrane Transport Modulators
- Moderate Risk QTc-Prolonging Agents
- Negative Inotrope
- OATP1B1/SLCO1B1 Inhibitors
- P-glycoprotein inducers
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Pyridines
- QTc Prolonging Agents
- Reproductive Control Agents
- Selective Calcium Channel Blockers With Mainly Vascular Effects
- Tocolytic Agents
- Vasodilating Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridines and derivatives
- Sub Class
- Hydropyridines
- Direct Parent
- Dihydropyridinecarboxylic acids and derivatives
- Alternative Parents
- Nitrobenzenes / Nitroaromatic compounds / Dicarboxylic acids and derivatives / Vinylogous amides / Enoate esters / Methyl esters / Amino acids and derivatives / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Enamines show 6 more
- Substituents
- Allyl-type 1,3-dipolar organic compound / Alpha,beta-unsaturated carboxylic ester / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / C-nitro compound / Carbonyl group / Carboxylic acid derivative show 23 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- dihydropyridine (CHEBI:7565)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- I9ZF7L6G2L
- CAS number
- 21829-25-4
- InChI Key
- HYIMSNHJOBLJNT-UHFFFAOYSA-N
- InChI
- 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
- IUPAC Name
- 3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
- SMILES
- COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC
References
- Synthesis Reference
Hiroitsu Kawata, Tadayoshi Ohmura, Katsuhiko Yano, Mikio Matsumura, Saburo Higuchi, Yoshiaki Soeishi, "Nifedipine-containing solid preparation composition." U.S. Patent US4412986, issued November, 1976.
US4412986- General References
- Khan KM, Patel J, Schaefer TJ: Nifedipine . [Article]
- Otto J, Lesko LJ: Protein binding of nifedipine. J Pharm Pharmacol. 1986 May;38(5):399-400. doi: 10.1111/j.2042-7158.1986.tb04598.x. [Article]
- Chung M, Reitberg DP, Gaffney M, Singleton W: Clinical pharmacokinetics of nifedipine gastrointestinal therapeutic system. A controlled-release formulation of nifedipine. Am J Med. 1987 Dec 21;83(6B):10-4. doi: 10.1016/0002-9343(87)90630-9. [Article]
- Herrington DM, Insley BM, Weinmann GG: Nifedipine overdose. Am J Med. 1986 Aug;81(2):344-6. doi: 10.1016/0002-9343(86)90276-7. [Article]
- Whitebloom D, Fitzharris J: Nifedipine overdose. Clin Cardiol. 1988 Jul;11(7):505-6. doi: 10.1002/clc.4960110714. [Article]
- Raemsch KD, Sommer J: Pharmacokinetics and metabolism of nifedipine. Hypertension. 1983 Jul-Aug;5(4 Pt 2):II18-24. doi: 10.1161/01.hyp.5.4_pt_2.ii18. [Article]
- Waller DG, Renwick AG, Gruchy BS, George CF: The first pass metabolism of nifedipine in man. Br J Clin Pharmacol. 1984 Dec;18(6):951-4. doi: 10.1111/j.1365-2125.1984.tb02569.x. [Article]
- Nader AM, Quinney SK, Fadda HM, Foster DR: Effect of Gastric Fluid Volume on the In Vitro Dissolution and In Vivo Absorption of BCS Class II Drugs: a Case Study with Nifedipine. AAPS J. 2016 Jul;18(4):981-8. doi: 10.1208/s12248-016-9918-x. Epub 2016 Apr 22. [Article]
- van Harten J, Burggraaf K, Danhof M, van Brummelen P, Breimer DD: Negligible sublingual absorption of nifedipine. Lancet. 1987 Dec 12;2(8572):1363-5. doi: 10.1016/s0140-6736(87)91258-x. [Article]
- Wang AL, Iadecola C, Wang G: New generations of dihydropyridines for treatment of hypertension. J Geriatr Cardiol. 2017 Jan;14(1):67-72. doi: 10.11909/j.issn.1671-5411.2017.01.006. [Article]
- Godfraind T: Discovery and Development of Calcium Channel Blockers. Front Pharmacol. 2017 May 29;8:286. doi: 10.3389/fphar.2017.00286. eCollection 2017. [Article]
- Vater W, Kroneberg G, Hoffmeister F, Saller H, Meng K, Oberdorf A, Puls W, Schlossmann K, Stoepel K: [Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)]. Arzneimittelforschung. 1972 Jan;22(1):1-14. [Article]
- FDA Approved Drug Products: Procardia Nifedipine Oral Capsules [Link]
- FDA Approved Drug Products: Procardia XL Nifedipine Oral Extended Release Tablets [Link]
- FDA Approved Drug Products: Adalat CC Nifedipine Oral Extended Release Tablets [Link]
- Cayman Chemical: Nifedipine MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0015247
- KEGG Drug
- D00437
- KEGG Compound
- C07266
- PubChem Compound
- 4485
- PubChem Substance
- 46505103
- ChemSpider
- 4330
- BindingDB
- 50101817
- 7417
- ChEBI
- 7565
- ChEMBL
- CHEMBL193
- ZINC
- ZINC000085205448
- Therapeutic Targets Database
- DAP000529
- PharmGKB
- PA450631
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- C5U
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Nifedipine
- PDB Entries
- 6jp5
- FDA label
- Download (206 KB)
- MSDS
- Download (74.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Hypertension in Pregnancy / Post Partum Pre-eclampsia 1 4 Completed Basic Science Coronavirus Disease 2019 (COVID‑19) / Myocarditis Allergic / Renal Dialysis / Severe Acute Respiratory Syndrome-related Coronavirus / Vaccines / Viral Infections 1 4 Completed Basic Science Hypertension 1 4 Completed Basic Science Premature Births 1 4 Completed Prevention Atrial Fibrillation 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Actavis Group
- Amerisource Health Services Corp.
- Apotheca Inc.
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- Bayer Healthcare
- Biovail Pharmaceuticals
- Bryant Ranch Prepack
- Cardinal Health
- Caremark LLC
- Catalent Pharma Solutions
- Comprehensive Consultant Services Inc.
- Coupler Enterprises Inc.
- Dept Health Central Pharmacy
- DHHS Program Support Center Supply Service Center
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Elan Pharmaceuticals Inc.
- Eurand Pharmaceuticals Inc.
- Gavis Pharmaceuticals LLC
- Giant Food Inc.
- Goldline Laboratories Inc.
- Greenstone LLC
- H.E. Butt Grocery Co.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- International Laboratories Inc.
- Ivax Pharmaceuticals
- IVC Industries Inc.
- Kaiser Foundation Hospital
- LeaderPharma
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Mason Distributors
- Mckesson Corp.
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Novopharm Ltd.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pfizer Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacy Service Center
- Pharmedix
- Physicians Total Care Inc.
- Prasco Labs
- Pratt Pharmaceuticals
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Qualitest
- Rebel Distributors Corp.
- Redpharm Drug
- Remedy Repack
- Resource Optimization and Innovation LLC
- RP Scherer Canada Inc.
- Sandhills Packaging Inc.
- Schering Corp.
- Schwarz Pharma Inc.
- Southwood Pharmaceuticals
- Talbert Medical Management Corp.
- Teva Pharmaceutical Industries Ltd.
- Tya Pharmaceuticals
- UDL Laboratories
- United Research Laboratories Inc.
- Va Cmop Dallas
- Vangard Labs Inc.
- Warrick Pharmaceuticals Corp.
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Capsule Oral Tablet, coated Oral Tablet, delayed release Oral 60 mg Capsule, coated Oral 10 mg Tablet, film coated Oral 30 mg/1 Tablet, film coated Oral 60 mg/1 Tablet, film coated Oral 90 mg/1 Tablet, extended release Oral 30 mg Tablet, extended release Oral 60 mg Tablet Oral 30 MG Tablet Oral 60 MG Tablet, film coated Oral 60 mg Tablet, coated Oral 20 mg Tablet Oral 10 mg Tablet, film coated Oral Kit; tablet, delayed release; tablet, extended release Oral Tablet Oral 25.000 mg Cream Rectal Spray Sublingual 5 mg/spray Capsule, coated Oral 20 mg Tablet, film coated Oral 40 mg Tablet, extended release Oral Capsule Oral 10.0000 mg Capsule, extended release Oral Capsule Oral 50 mg Solution Oral 20 MG/ML Tablet, film coated Oral 30 mg Tablet, film coated, extended release Oral 90 mg/1 Capsule Oral 20 MG Solution / drops Oral 20 MG/ML Tablet, film coated Oral 20 mg Tablet, extended release Oral 40 MG Tablet Oral 20 mg Capsule, liquid filled Oral 10 mg Tablet, coated Oral 30 MG Tablet, coated Oral 60 MG Capsule, extended release Oral Capsule Oral 10 mg/1 Capsule Oral 20 mg/1 Capsule, liquid filled Oral 10 mg/1 Capsule, liquid filled Oral 20 mg/1 Powder Not applicable 1 g/1g Tablet Oral 30 mg/1 Tablet, extended release Oral 30 mg/1 Tablet, extended release Oral 60 mg/1 Tablet, extended release Oral 90 mg/1 Tablet, film coated, extended release Oral 30 mg/1 Tablet, film coated, extended release Oral 60 mg/1 Tablet, extended release Oral 10 mg / srt Tablet, extended release Oral 20 mg / srt Capsule, coated Oral 100 mg Capsule, liquid filled Oral 20 mg Capsule, extended release Oral 30 mg Capsule, extended release Oral 3000000 mg Tablet, coated Oral 10 mg Tablet, extended release Oral 20 mg Tablet, film coated Oral 10 mg Capsule Oral 10.000 mg Capsule Oral Tablet Oral Tablet Oral 30.00 mg Capsule Oral 5 mg / cap Tablet, extended release Oral 10 mg Spray Sublingual 5 mg Capsule Oral 20 mg/1mL Capsule Oral 10 mg / cap Capsule, extended release Oral 60 mg Capsule Oral 5 mg Capsule Oral 10 mg Capsule, extended release Oral 20 mg - Prices
Unit description Cost Unit Nifedipine powder 15.3USD g Procardia XL 90 mg 24 Hour tablet 4.77USD tablet Procardia xl 90 mg tablet 4.58USD tablet Procardia xl 60 mg tablet 4.43USD tablet Procardia XL 60 mg 24 Hour tablet 4.13USD tablet Adalat CC 90 mg 24 Hour tablet 3.5USD tablet Adalat cc 90 mg tablet 3.37USD tablet Adalat CC 60 mg 24 Hour tablet 2.99USD tablet Adalat cc 60 mg tablet 2.87USD tablet NIFEdipine CR Osmotic 90 mg 24 Hour tablet 2.66USD tablet Nifediac cc 90 mg tablet 2.57USD tablet Nifedipine er 90 mg tablet 2.56USD tablet Procardia xl 30 mg tablet 2.56USD tablet Procardia XL 30 mg 24 Hour tablet 2.39USD tablet NIFEdipine CR Osmotic 60 mg 24 Hour tablet 2.38USD tablet Nifedipine er 60 mg tablet 2.29USD tablet Afeditab cr 60 mg tablet 2.24USD tablet Nifediac cc 60 mg tablet 2.17USD tablet Adalat CC 30 mg 24 Hour tablet 1.81USD tablet NIFEdipine 20 mg capsule 1.74USD capsule Adalat cc 30 mg tablet 1.61USD tablet Adalat Xl 60 mg Extended-Release Tablet 1.41USD tablet NIFEdipine CR Osmotic 30 mg 24 Hour tablet 1.35USD tablet Adalat Xl 20 mg Extended-Release Tablet 1.34USD tablet Adalat Xl 30 mg Extended-Release Tablet 1.34USD tablet Nifedipine er 30 mg tablet 1.32USD tablet Afeditab cr 30 mg tablet 1.26USD tablet Mylan-Nifedipine Extended Release 60 mg Extended-Release Tablet 1.18USD tablet Procardia 10 mg capsule 1.17USD capsule Nifediac cc 30 mg tablet 1.15USD tablet NIFEdipine 10 mg capsule 0.97USD capsule Apo-Nifed 10 mg Capsule 0.51USD capsule Apo-Nifed 5 mg Capsule 0.39USD capsule Coral calcium plus 1500 mg caplet 0.13USD caplet Coral calcium 1000 mg caplet 0.09USD caplet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5264446 No 1993-11-23 2010-11-23 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 172-174 °C PhysProp water solubility Insoluble FDA Label logP 2.20 MASUMOTO,K ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.0177 mg/mL ALOGPS logP 2.49 ALOGPS logP 1.82 Chemaxon logS -4.3 ALOGPS pKa (Strongest Acidic) 16.94 Chemaxon pKa (Strongest Basic) -6.6 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 107.77 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 91.16 m3·mol-1 Chemaxon Polarizability 33.89 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9073 Blood Brain Barrier - 0.9536 Caco-2 permeable + 0.7853 P-glycoprotein substrate Non-substrate 0.5089 P-glycoprotein inhibitor I Inhibitor 0.8771 P-glycoprotein inhibitor II Inhibitor 0.7902 Renal organic cation transporter Non-inhibitor 0.9182 CYP450 2C9 substrate Non-substrate 0.7776 CYP450 2D6 substrate Non-substrate 0.5726 CYP450 3A4 substrate Substrate 0.705 CYP450 1A2 substrate Inhibitor 0.9106 CYP450 2C9 inhibitor Non-inhibitor 0.6122 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.6715 CYP450 3A4 inhibitor Inhibitor 0.796 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.9013 Ames test Non AMES toxic 0.6973 Carcinogenicity Non-carcinogens 0.5412 Biodegradation Not ready biodegradable 0.9675 Rat acute toxicity 2.5425 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.863 hERG inhibition (predictor II) Non-inhibitor 0.903
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-00n0-1195000000-7e4e6770da078dff666a LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS splash10-0v4i-1691000000-c4842fe2c3070d6e90dd MS/MS Spectrum - , positive LC-MS/MS splash10-0v4i-1691000000-c4842fe2c3070d6e90dd Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 187.5191675 predictedDarkChem Lite v0.1.0 [M-H]- 185.8429675 predictedDarkChem Lite v0.1.0 [M-H]- 180.0825 predictedDeepCCS 1.0 (2019) [M+H]+ 187.5979675 predictedDarkChem Lite v0.1.0 [M+H]+ 186.0972675 predictedDarkChem Lite v0.1.0 [M+H]+ 184.09636 predictedDeepCCS 1.0 (2019) [M+Na]+ 187.2331675 predictedDarkChem Lite v0.1.0 [M+Na]+ 185.8507675 predictedDarkChem Lite v0.1.0 [M+Na]+ 192.91142 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1C
- Uniprot ID
- Q13936
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1C
- Molecular Weight
- 248974.1 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Morel N, Buryi V, Feron O, Gomez JP, Christen MO, Godfraind T: The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits. Br J Pharmacol. 1998 Nov;125(5):1005-12. [Article]
- Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Mol Pharmacol. 2009 Feb;75(2):407-14. doi: 10.1124/mol.108.049981. Epub 2008 Nov 24. [Article]
- Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity involved sa node cell action potential
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1D
- Uniprot ID
- Q01668
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1D
- Molecular Weight
- 245138.75 Da
References
- Bell DC, Butcher AJ, Berrow NS, Page KM, Brust PF, Nesterova A, Stauderman KA, Seabrook GR, Nurnberg B, Dolphin AC: Biophysical properties, pharmacology, and modulation of human, neuronal L-type (alpha(1D), Ca(V)1.3) voltage-dependent calcium currents. J Neurophysiol. 2001 Feb;85(2):816-27. [Article]
- Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Mol Pharmacol. 2009 Feb;75(2):407-14. doi: 10.1124/mol.108.049981. Epub 2008 Nov 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB2
- Uniprot ID
- Q08289
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-2
- Molecular Weight
- 73579.925 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
- Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
- Gene Name
- NR1I2
- Uniprot ID
- O75469
- Uniprot Name
- Nuclear receptor subfamily 1 group I member 2
- Molecular Weight
- 49761.245 Da
References
- Krasowski MD, Ai N, Hagey LR, Kollitz EM, Kullman SW, Reschly EJ, Ekins S: The evolution of farnesoid X, vitamin D, and pregnane X receptors: insights from the green-spotted pufferfish (Tetraodon nigriviridis) and other non-mammalian species. BMC Biochem. 2011 Feb 3;12:5. doi: 10.1186/1471-2091-12-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Titin binding
- Specific Function
- Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
- Gene Name
- CALM1
- Uniprot ID
- P0DP23
- Uniprot Name
- Calmodulin
- Molecular Weight
- 16837.47 Da
References
- Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1S
- Uniprot ID
- Q13698
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1S
- Molecular Weight
- 212348.1 Da
References
- Peterson BZ, Catterall WA: Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore. Mol Pharmacol. 2006 Aug;70(2):667-75. Epub 2006 May 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated...
- Gene Name
- KCND3
- Uniprot ID
- Q9UK17
- Uniprot Name
- Potassium voltage-gated channel subfamily D member 3
- Molecular Weight
- 73450.53 Da
References
- Bett GC, Rasmusson RL: Modification of K+ channel-drug interactions by ancillary subunits. J Physiol. 2008 Feb 15;586(4):929-50. Epub 2007 Dec 20. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Scaffold protein binding
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Components:
References
- Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [Article]
- Godfraind T: Discovery and Development of Calcium Channel Blockers. Front Pharmacol. 2017 May 29;8:286. doi: 10.3389/fphar.2017.00286. eCollection 2017. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Foti RS, Rock DA, Wienkers LC, Wahlstrom JL: Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Drug Metab Dispos. 2010 Jun;38(6):981-7. doi: 10.1124/dmd.110.032094. Epub 2010 Mar 4. [Article]
- Pelkonen O, Maenpaa J, Taavitsainen P, Rautio A, Raunio H: Inhibition and induction of human cytochrome P450 (CYP) enzymes. Xenobiotica. 1998 Dec;28(12):1203-53. [Article]
- Galetin A, Clarke SE, Houston JB: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach. Drug Metab Dispos. 2002 Dec;30(12):1512-22. [Article]
- Ramachandran SD, Vivares A, Klieber S, Hewitt NJ, Muenst B, Heinz S, Walles H, Braspenning J: Applicability of second-generation upcyte(R) human hepatocytes for use in CYP inhibition and induction studies. Pharmacol Res Perspect. 2015 Oct;3(5):e00161. doi: 10.1002/prp2.161. Epub 2015 Aug 10. [Article]
- Wrighton SA, Ring BJ: Inhibition of human CYP3A catalyzed 1'-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine. Pharm Res. 1994 Jun;11(6):921-4. doi: 10.1023/a:1018906614320. [Article]
- Flockhart Table of Drug Interactions [Link]
- FDA Approved Drug Products: Procardia XL Nifedipine Oral Extended Release Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Ma B, Prueksaritanont T, Lin JH: Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [Article]
- Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO: Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. J Pharmacol Exp Ther. 1993 Apr;265(1):401-7. [Article]
- ADALAT® XL® (Nifedipine extended-release tablets) Product Monograph [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56501.005 Da
References
- ADALAT® XL® (Nifedipine extended-release tablets) Product Monograph [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO: Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. J Pharmacol Exp Ther. 1993 Apr;265(1):401-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- Curator comments
- One in vitro study indicates that nifedipine induces CYP2B6 while another indicates that it does not demonstrate any induction of this enzyme. Clinical correlation of this enzyme action is known.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Drocourt L, Pascussi JM, Assenat E, Fabre JM, Maurel P, Vilarem MJ: Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metab Dispos. 2001 Oct;29(10):1325-31. [Article]
- Ramachandran SD, Vivares A, Klieber S, Hewitt NJ, Muenst B, Heinz S, Walles H, Braspenning J: Applicability of second-generation upcyte(R) human hepatocytes for use in CYP inhibition and induction studies. Pharmacol Res Perspect. 2015 Oct;3(5):e00161. doi: 10.1002/prp2.161. Epub 2015 Aug 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Ma B, Prueksaritanont T, Lin JH: Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30. [Article]
- Drocourt L, Pascussi JM, Assenat E, Fabre JM, Maurel P, Vilarem MJ: Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metab Dispos. 2001 Oct;29(10):1325-31. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Patki KC, Von Moltke LL, Greenblatt DJ: In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug Metab Dispos. 2003 Jul;31(7):938-44. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Otto J, Lesko LJ: Protein binding of nifedipine. J Pharm Pharmacol. 1986 May;38(5):399-400. doi: 10.1111/j.2042-7158.1986.tb04598.x. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
- Otto J, Lesko LJ: Protein binding of nifedipine. J Pharm Pharmacol. 1986 May;38(5):399-400. doi: 10.1111/j.2042-7158.1986.tb04598.x. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
- Gene Name
- ABCC3
- Uniprot ID
- O15438
- Uniprot Name
- Canalicular multispecific organic anion transporter 2
- Molecular Weight
- 169341.14 Da
References
- Teng S, Jekerle V, Piquette-Miller M: Induction of ABCC3 (MRP3) by pregnane X receptor activators. Drug Metab Dispos. 2003 Nov;31(11):1296-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Takara K, Sakaeda T, Tanigawara Y, Nishiguchi K, Ohmoto N, Horinouchi M, Komada F, Ohnishi N, Yokoyama T, Okumura K: Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. Eur J Pharm Sci. 2002 Aug;16(3):159-65. [Article]
- Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Payen L, Sparfel L, Courtois A, Vernhet L, Guillouzo A, Fardel O: The drug efflux pump MRP2: regulation of expression in physiopathological situations and by endogenous and exogenous compounds. Cell Biol Toxicol. 2002;18(4):221-33. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
- Stieger B: Role of the bile salt export pump, BSEP, in acquired forms of cholestasis. Drug Metab Rev. 2010 Aug;42(3):437-45. doi: 10.3109/03602530903492004. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55