You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameCimetidine
Accession NumberDB00501  (APRD00568)
TypeSmall Molecule
GroupsApproved
Description

A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
1-Cyano-2-methyl-3-(2-(((5-methyl-4-imidazolyl)methyl)thio)ethyl)guanidineNot AvailableNot Available
2-Cyano-1-methyl-3-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)guanidineNot AvailableNot Available
CimetagNot AvailableNot Available
CimetidinGermanINN
CimetidinaSpanishINN
CimétidineFrenchINN
CimetidinumLatinINN
N-Cyano-n'-methyl-n''-(2-([(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl)ethyl)guanidineNot AvailableNot Available
N''-cyano-N-methyl-n'-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidineNot AvailableNot Available
Tagamet hb 200Not AvailableNot Available
UlcerfenNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cimetidinetablet, film coated300 mgoralTeva Pharmaceuticals USA Inc2003-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralTeva Pharmaceuticals USA Inc2004-02-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated800 mgoralTeva Pharmaceuticals USA Inc2003-12-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated200 mgoralMylan Pharmaceuticals Inc.1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralMylan Pharmaceuticals Inc.1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralMylan Pharmaceuticals Inc.1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated800 mgoralMylan Pharmaceuticals Inc.1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet400 mgoralLiberty Pharmaceuticals, Inc.2010-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralSTAT Rx USA LLC1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralSTAT Rx USA LLC2010-05-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated800 mgoralSTAT Rx USA LLC2010-05-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet300 mgoralRebel Distributors Corp1998-12-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet400 mgoralRebel Distributors Corp2010-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralAidarex Pharmaceuticals LLC2004-02-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralAv Kare, Inc.2013-07-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet400 mgoralREMEDYREPACK INC.2010-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet400 mgoralREMEDYREPACK INC.2011-07-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralREMEDYREPACK INC.2013-05-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralREMEDYREPACK INC.2014-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralPhysicians Total Care, Inc.1994-06-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralPhysicians Total Care, Inc.1994-07-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated800 mgoralPhysicians Total Care, Inc.1994-05-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralPd Rx Pharmaceuticals, Inc.2011-05-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidine Hydrochloridesolution300 mg/5mLoralMorton Grove Pharmaceuticals, Inc.1997-03-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated800 mgoralbryant ranch prepack2003-12-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralbryant ranch prepack2010-10-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralbryant ranch prepack2003-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Good Sense Heartburn Relieftablet200 mgoralbryant ranch prepack2002-12-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralDispensing Solutions, Inc.2010-05-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated200 mgoralCarilion Materials Management1994-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated300 mgoralCarilion Materials Management2003-11-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralCarilion Materials Management2004-02-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidinetablet, film coated400 mgoralPreferred Pharmaceuticals, Inc2011-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Good Sense Heartburn Relieftablet200 mgoralL. Perrigo Company2002-12-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Tagamet HBtablet200 mgoralGlaxo Smith Kline Consumer Healthcare Lp2010-03-192015-09-30Us 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cimetidine acid reducertablet200 mgoralWalgreen Company2001-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Acid Reducertablet200 mgoralRite Aid Corporation2005-07-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Good Neighbor Pharmacy Heartburn Relieftablet200 mgoralAmerisource Bergen2000-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Topcare Heartburn Relieftablet200 mgoralTopco Associates LLC2000-02-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Leader Heartburn Relieftablet200 mgoralCardinal Health2000-02-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Equaline Acid Reducertablet200 mgoralSupervalu Inc2004-09-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heartburn Relieftablet200 mgoralMeijer Distribution Inc2000-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Equate Cimetidinetablet200 mgoralWal Mart Stores Inc2006-09-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Sunmark Heartburn Relief acid reducertablet200 mgoralMc Kesson2003-09-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Smart Sense Acid Reducertablet200 mgoralKmart Corporation2000-01-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heartburn Relieftablet200 mgoralFamily Dollar Services Inc2000-09-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Dg Health Heartburn Relieftablet200 mgoralDolgencorp, LLC2010-03-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Heartburn Relieftablet200 mgoralCVS Pharmacy2000-01-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Tagamettablet200 mgoralMedtech Products Inc.2012-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
International Brands
NameCompany
CimetagJulphar
Tagamet HB200GlaxoSmithKline
UlcedineNot Available
UlcerfenFinadiet
UlcimetFarmasa
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cimetidine Hydrochloride
70059-30-2
Thumb
  • InChI Key: QJHCNBWLPSXHBL-UHFFFAOYSA-N
  • Monoisotopic Mass: 288.092392971
  • Average Mass: 288.8
DBSALT000287
Categories
CAS number51481-61-9
WeightAverage: 252.339
Monoisotopic: 252.115715232
Chemical FormulaC10H16N6S
InChI KeyAQIXAKUUQRKLND-UHFFFAOYSA-N
InChI
InChI=1S/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)
IUPAC Name
(Z)-1-cyano-2-methyl-3-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
SMILES
C\N=C(\NCCSCC1=C(C)NC=N1)NC#N
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as imidazoles. These are compounds containing an imidazole ring, which is an aromatic five-member ring with two nitrogen atoms at positions 1 and 3, and three carbon atoms.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassImidazoles
Direct ParentImidazoles
Alternative Parents
Substituents
  • Heteroaromatic compound
  • Imidazole
  • Guanidine
  • Azacycle
  • Dialkylthioether
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Sulfenyl compound
  • Carboximidamide
  • Thioether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Imine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
PharmacodynamicsCimetidine is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. It is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Cimetidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Cimetidine include an increase in gastric bacterial flora such as nitrate-reducing organisms.
Mechanism of actionCimetidine binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity.
AbsorptionRapid 60-70%
Volume of distributionNot Available
Protein binding15-20%
Metabolism

Hepatic

Route of eliminationThe principal route of excretion of cimetidine is the urine.
Half life2 hours
ClearanceNot Available
ToxicitySymptoms of overdose include nausea, vomiting, diarrhea, increased saliva production, difficulty breathing, and a fast heartbeat.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9855
Blood Brain Barrier-0.6782
Caco-2 permeable-0.6358
P-glycoprotein substrateSubstrate0.7887
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterInhibitor0.7233
CYP450 2C9 substrateNon-substrate0.8048
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5795
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 substrateNon-inhibitor0.907
CYP450 2D6 substrateNon-inhibitor0.9231
CYP450 2C19 substrateInhibitor0.5773
CYP450 3A4 substrateNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9575
Ames testNon AMES toxic0.837
CarcinogenicityNon-carcinogens0.9579
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.7341 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7983
hERG inhibition (predictor II)Non-inhibitor0.8745
Pharmacoeconomics
Manufacturers
  • Glaxosmithkline
  • Apotex inc
  • Contract pharmacal corp
  • Dava pharmaceuticals inc
  • Endo pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lek pharmaceuticals d d
  • Mylan pharmaceuticals inc
  • L perrigo co
  • Perrigo co
  • Pliva inc
  • Roxane laboratories inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Hospira inc
  • Luitpold pharmaceuticals inc
  • Teva parenteral medicines inc
  • Actavis mid atlantic llc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Hi tech pharmacal co inc
  • Novex pharma
  • Pharmaceutical assoc inc div beach products
  • Teva pharmaceuticals usa
  • Wockhardt eu operations (swiss) ag
Packagers
Dosage forms
FormRouteStrength
Solutionoral300 mg/5mL
Tabletoral200 mg
Tabletoral300 mg
Tabletoral400 mg
Tablet, film coatedoral200 mg
Tablet, film coatedoral300 mg
Tablet, film coatedoral400 mg
Tablet, film coatedoral800 mg
Prices
Unit descriptionCostUnit
Cimetidine 800 mg tablet2.7USD tablet
Tagamet 400 mg tablet2.51USD tablet
Cimetidine 150 mg/ml vial1.67USD ml
Cimetidine powder1.48USD g
Cimetidine 400 mg tablet1.44USD tablet
Tagamet 300 mg tablet1.28USD tablet
Cimetidine 300 mg tablet0.93USD tablet
Cimetidine 200 mg tablet0.46USD tablet
Cimetidine HCl 300 mg/5ml Solution0.38USD ml
Tagamet hb 200 mg tablet0.37USD tablet
Apo-Cimetidine 800 mg Tablet0.27USD tablet
Mylan-Cimetidine 800 mg Tablet0.27USD tablet
Acid reducer 200 mg tablet0.21USD tablet
Apo-Cimetidine 600 mg Tablet0.18USD tablet
Mylan-Cimetidine 600 mg Tablet0.18USD tablet
Novo-Cimetine 600 mg Tablet0.18USD tablet
Nu-Cimet 600 mg Tablet0.18USD tablet
Apo-Cimetidine 400 mg Tablet0.14USD tablet
Mylan-Cimetidine 400 mg Tablet0.14USD tablet
Novo-Cimetine 400 mg Tablet0.14USD tablet
Nu-Cimet 400 mg Tablet0.14USD tablet
Apo-Cimetidine 200 mg Tablet0.09USD tablet
Apo-Cimetidine 300 mg Tablet0.09USD tablet
Mylan-Cimetidine 300 mg Tablet0.09USD tablet
Novo-Cimetine 300 mg Tablet0.09USD tablet
Nu-Cimet 300 mg Tablet0.09USD tablet
Heartburn relief 200 mg tablet0.08USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point142 °CPhysProp
water solubility9380 mg/L (at 25 °C)MCFARLAND,JW ET AL. (2001)
logP0.40HANSCH,C ET AL. (1995)
logS-1.35ADME Research, USCD
Caco2 permeability-5.89ADME Research, USCD
pKa6.8TOMLINSON,E & HAFKENSCHEID,TL (1986)
Predicted Properties
PropertyValueSource
Water Solubility0.816 mg/mLALOGPS
logP0.44ALOGPS
logP-0.11ChemAxon
logS-2.5ALOGPS
pKa (Strongest Acidic)13.38ChemAxon
pKa (Strongest Basic)6.91ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area88.89 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity70.32 m3·mol-1ChemAxon
Polarizability27.47 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10 KB)
SpectraMS1D NMR
References
Synthesis Reference

Saburo Uchikuga, Tomoyasu Tashiro, Yasuko Osawa, “Process for preparing the H.sub.2 -receptor antagonist cimetidine.” U.S. Patent US4413129, issued March, 1972.

US4413129
General Reference
  1. Michnovicz JJ, Galbraith RA: Cimetidine inhibits catechol estrogen metabolism in women. Metabolism. 1991 Feb;40(2):170-4. Pubmed
External Links
ATC CodesA02BA01
AHFS Codes
  • 56:28.12
PDB EntriesNot Available
FDA labelDownload (420 KB)
MSDSDownload (73.4 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolMay enhance the anticoagulant effect of Vitamin K Antagonists.
AgomelatineCYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine.
AlfentanilCimetidine may increase the serum concentration of Alfentanil.
AminophyllineMay decrease the metabolism of Theophylline Derivatives.
AmiodaroneCimetidine may increase the serum concentration of Amiodarone.
AmitriptylineMay decrease the metabolism of Tricyclic Antidepressants.
AmlodipineCimetidine may increase the serum concentration of Calcium Channel Blockers.
AmoxapineMay decrease the metabolism of Tricyclic Antidepressants.
AmrinoneCimetidine may increase the serum concentration of Calcium Channel Blockers.
AripiprazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of ARIPiprazole.
AtazanavirH2-Antagonists may decrease the serum concentration of Atazanavir.
AtorvastatinMay enhance the adverse/toxic effect of Cimetidine. Specifically, there is a theoretical potential for enhanced effects on reducing endogenous steroid activity.
AvanafilCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Avanafil.
BepridilCimetidine may increase the serum concentration of Calcium Channel Blockers.
BosentanCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosentan.
BosutinibCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosutinib.
BromazepamCimetidine may increase the serum concentration of Bromazepam.
BupropionMay increase the serum concentration of OCT2 Substrates.
CapecitabineCimetidine may increase serum concentrations of the active metabolite(s) of Capecitabine. Specifically, concentrations of fluorouracil may be increased.
CarbamazepineCimetidine may increase the serum concentration of CarBAMazepine. The serum carbamazepine concentration might return to normal within one week of starting cimetidine.
CarmustineMay enhance the myelosuppressive effect of Carmustine.
CarvedilolCimetidine may increase the serum concentration of Carvedilol.
CefditorenH2-Antagonists may decrease the serum concentration of Cefditoren.
CefpodoximeH2-Antagonists may decrease the absorption of Cefpodoxime. Separate oral doses by at least 2 hours.
CefuroximeH2-Antagonists may decrease the absorption of Cefuroxime. Separate oral doses by at least 2 hours.
ChlorpropamideMay increase the serum concentration of Sulfonylureas.
CilostazolCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
CisaprideCimetidine may increase the serum concentration of Cisapride.
CitalopramMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
ClomipramineMay decrease the metabolism of Tricyclic Antidepressants.
ClopidogrelCYP2C19 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Clopidogrel.
ClozapineMay increase the serum concentration of CloZAPine.
CodeineCYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine.
ColchicineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Colchicine.
DabrafenibH2-Antagonists may decrease the serum concentration of Dabrafenib.
DalfampridineCimetidine may increase the serum concentration of Dalfampridine.
DapoxetineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dapoxetine.
DasatinibH2-Antagonists may decrease the absorption of Dasatinib.
DelavirdineH2-Antagonists may decrease the serum concentration of Delavirdine.
DesipramineMay decrease the metabolism of Tricyclic Antidepressants.
DexmethylphenidateH2-Antagonists may increase the absorption of Dexmethylphenidate. Specifically, H2-antagonists may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption.
DiltiazemMay increase the serum concentration of Calcium Channel Blockers.
DofetilideMay increase the serum concentration of Dofetilide. This is likely via inhibition of dofetilide renal tubular secretion (primarily) and inhibition of dofetilide metabolism.
DomperidoneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Domperidone.
DronabinolCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dronabinol.
EliglustatCYP2D6 Inhibitors (Moderate) may increase the serum concentration of Eliglustat.
EpirubicinMay increase the serum concentration of EPIrubicin.
EplerenoneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eplerenone.
ErlotinibH2-Antagonists may decrease the serum concentration of Erlotinib.
EscitalopramCimetidine may increase the serum concentration of Escitalopram.
EverolimusCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Everolimus.
FelodipineCimetidine may increase the serum concentration of Calcium Channel Blockers.
FentanylCYP3A4 Inhibitors (Moderate) may increase the serum concentration of FentaNYL.
FesoterodineCYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s) of Fesoterodine.
FloxuridineMay increase serum concentrations of the active metabolite(s) of Floxuridine. Specifically, concentrations of fluorouracil may be increased.
FlunarizineCimetidine may increase the serum concentration of Calcium Channel Blockers.
FluoxetineMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
FluvoxamineMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
FosamprenavirH2-Antagonists may decrease the serum concentration of Fosamprenavir. Cimetidine may also inhibit the metabolism of the active metabolite amprenavir, making its effects on fosamprenavir/amprenavir concentrations difficult to predict.
FosphenytoinMay enhance the adverse/toxic effect of Fosphenytoin-Phenytoin. Cimetidine may increase the serum concentration of Fosphenytoin-Phenytoin.
GabapentinCimetidine may increase the serum concentration of Calcium Channel Blockers.
GefitinibH2-Antagonists may decrease the serum concentration of Gefitinib.
GliclazideMay increase the serum concentration of Sulfonylureas.
GlimepirideMay increase the serum concentration of Sulfonylureas.
GlipizideMay increase the serum concentration of Sulfonylureas.
GlyburideMay increase the serum concentration of Sulfonylureas.
HalofantrineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Halofantrine.
HydrocodoneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Hydrocodone.
IfosfamideCYP3A4 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Ifosfamide.
ImatinibCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Imatinib.
ImipramineMay decrease the metabolism of Tricyclic Antidepressants.
IndinavirH2-Antagonists may decrease the serum concentration of Indinavir.
IsradipineMay increase the serum concentration of Calcium Channel Blockers.
ItraconazoleH2-Antagonists may decrease the serum concentration of Itraconazole.
IvacaftorCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ivacaftor.
LamotrigineCimetidine may increase the serum concentration of Calcium Channel Blockers.
LedipasvirH2-Antagonists may decrease the serum concentration of Ledipasvir.
LercanidipineCimetidine may increase the serum concentration of Calcium Channel Blockers.
LomitapideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lomitapide.
LurasidoneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lurasidone.
Magnesium SulfateCimetidine may increase the serum concentration of Calcium Channel Blockers.
MebendazoleCimetidine may increase the serum concentration of Mebendazole.
MetforminMay increase the serum concentration of MetFORMIN.
MethylphenidateH2-Antagonists may increase the absorption of Methylphenidate. Specifically, H2-antagonists may interfere with the normal release of drug from the extended-release capsules (Ritalin LA brand), which could result in both increased absorption (early) and decreased delayed absorption.
MetoprololCYP2D6 Inhibitors may increase the serum concentration of Metoprolol.
MoclobemideCimetidine may decrease the metabolism of Moclobemide.
NebivololCYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nebivolol.
NelfinavirH2-Antagonists may decrease the serum concentration of Nelfinavir. Concentrations of the active M8 metabolite may also be reduced.
NicardipineCimetidine may increase the serum concentration of Calcium Channel Blockers.
NicotineMay increase the serum concentration of Nicotine.
NifedipineMay increase the serum concentration of Calcium Channel Blockers.
NilotinibH2-Antagonists may decrease the serum concentration of Nilotinib.
NimodipineMay increase the serum concentration of Calcium Channel Blockers.
NisoldipineMay increase the serum concentration of Calcium Channel Blockers.
NitrendipineCimetidine may increase the serum concentration of Calcium Channel Blockers.
NortriptylineMay decrease the metabolism of Tricyclic Antidepressants.
OxycodoneCYP3A4 Inhibitors (Moderate) may enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Moderate) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite Oxymorphone may also be increased.
ParoxetineMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
PazopanibH2-Antagonists may decrease the serum concentration of PAZOPanib.
PentoxifyllineCimetidine may increase the serum concentration of Pentoxifylline.
PerhexilineCimetidine may increase the serum concentration of Calcium Channel Blockers.
PhenytoinMay enhance the adverse/toxic effect of Fosphenytoin-Phenytoin. Cimetidine may increase the serum concentration of Fosphenytoin-Phenytoin.
PimecrolimusCYP3A4 Inhibitors (Moderate) may decrease the metabolism of Pimecrolimus.
PimozideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
PirfenidoneCYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pirfenidone.
PosaconazoleH2-Antagonists may decrease the serum concentration of Posaconazole.
PramipexoleMay increase the serum concentration of Pramipexole.
PraziquantelCimetidine may increase the serum concentration of Praziquantel.
PrenylamineCimetidine may increase the serum concentration of Calcium Channel Blockers.
ProcainamideCimetidine may decrease the excretion of Procainamide.
ProcaineMay decrease the excretion of Procainamide.
PropafenoneCimetidine may increase the serum concentration of Propafenone.
ProtriptylineMay decrease the metabolism of Tricyclic Antidepressants.
QuinidineCimetidine may increase the serum concentration of QuiNIDine.
QuinineMay increase the serum concentration of QuiNINE.
RanolazineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ranolazine.
RilpivirineH2-Antagonists may decrease the serum concentration of Rilpivirine.
RisedronateCimetidine may increase the serum concentration of Calcium Channel Blockers.
RivaroxabanCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Rivaroxaban. This warning is more specifically for drugs that are inhibitors of both CYP3A4 and P-glycoprotein. For erythromycin, refer to more specific erythromycin-rivaroxaban monograph recommendations.
RoflumilastCimetidine may increase serum concentrations of the active metabolite(s) of Roflumilast. Cimetidine may increase the serum concentration of Roflumilast.
SalmeterolCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Salmeterol.
SaquinavirH2-Antagonists may increase the serum concentration of Saquinavir.
SaxagliptinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Saxagliptin.
SertralineMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
SimeprevirCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Simeprevir.
SuvorexantCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Suvorexant.
TamoxifenCYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites.
TamsulosinCimetidine may increase the serum concentration of Tamsulosin.
TeriflunomideMay increase the serum concentration of OAT3 Substrates.
TheophyllineMay decrease the metabolism of Theophylline Derivatives.
ThioridazineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
TolazamideMay increase the serum concentration of Sulfonylureas.
TolbutamideMay increase the serum concentration of Sulfonylureas.
TolvaptanCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tolvaptan.
TrabectedinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Trabectedin.
TramadolCYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects.
TrimipramineMay decrease the metabolism of Tricyclic Antidepressants.
UlipristalCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ulipristal.
VareniclineH2-Antagonists may increase the serum concentration of Varenicline.
VerapamilCimetidine may increase the serum concentration of Calcium Channel Blockers.
VilazodoneMay decrease the metabolism of Selective Serotonin Reuptake Inhibitors.
VismodegibH2-Antagonists may decrease the serum concentration of Vismodegib.
ZaleplonCimetidine may decrease the metabolism of Zaleplon.
ZolmitriptanMay increase the serum concentration of ZOLMitriptan.
ZopicloneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Zopiclone.
ZuclopenthixolCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Best effect when taken with food.
  • Limit caffeine intake.

Targets

1. Histamine H2 receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Histamine H2 receptor P25021 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Hernandez-Munoz R, Montiel-Ruiz C, Vazquez-Martinez O: Gastric mucosal cell proliferation in ethanol-induced chronic mucosal injury is related to oxidative stress and lipid peroxidation in rats. Lab Invest. 2000 Aug;80(8):1161-9. Pubmed
  3. Kuint J, Linder N, Reichman B: Hypoxemia associated with cimetidine therapy in a newborn infant. Am J Perinatol. 1996 Jul;13(5):301-3. Pubmed
  4. Takahashi HK, Watanabe T, Yokoyama A, Iwagaki H, Yoshino T, Tanaka N, Nishibori M: Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol. 2006 Aug;70(2):450-3. Epub 2006 May 24. Pubmed

Enzymes

1. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

3. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed
  4. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed
  5. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed
  6. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed
  7. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed

4. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Wang DS, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y: Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther. 2002 Aug;302(2):510-5. Pubmed
  4. Wang DS, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y: Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther. 2002 Aug;302(2):510-5. Pubmed

5. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 11B1, mitochondrial

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 11B1, mitochondrial P15538 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

11. Dimethylaniline monooxygenase [N-oxide-forming] 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Dimethylaniline monooxygenase [N-oxide-forming] 3 P31513 Details

References:

  1. Cashman JR: Human flavin-containing monooxygenase: substrate specificity and role in drug metabolism. Curr Drug Metab. 2000 Sep;1(2):181-91. Pubmed
  2. Cashman JR, Park SB, Berkman CE, Cashman LE: Role of hepatic flavin-containing monooxygenase 3 in drug and chemical metabolism in adult humans. Chem Biol Interact. 1995 Apr 28;96(1):33-46. Pubmed
  3. Hai X, Adams E, Hoogmartens J, Van Schepdael A: Enantioselective in-line and off-line CE methods for the kinetic study on cimetidine and its chiral metabolites with reference to flavin-containing monooxygenase genetic isoforms. Electrophoresis. 2009 Apr;30(7):1248-57. Pubmed

12. Dimethylaniline monooxygenase [N-oxide-forming] 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Dimethylaniline monooxygenase [N-oxide-forming] 1 Q01740 Details

References:

  1. Hai X, Adams E, Hoogmartens J, Van Schepdael A: Enantioselective in-line and off-line CE methods for the kinetic study on cimetidine and its chiral metabolites with reference to flavin-containing monooxygenase genetic isoforms. Electrophoresis. 2009 Apr;30(7):1248-57. Pubmed
  2. Cashman JR: Human flavin-containing monooxygenase: substrate specificity and role in drug metabolism. Curr Drug Metab. 2000 Sep;1(2):181-91. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. Pubmed
  2. Lentz KA, Polli JW, Wring SA, Humphreys JE, Polli JE: Influence of passive permeability on apparent P-glycoprotein kinetics. Pharm Res. 2000 Dec;17(12):1456-60. Pubmed
  3. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. Pubmed
  4. van der Sandt IC, Blom-Roosemalen MC, de Boer AG, Breimer DD: Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines. Eur J Pharm Sci. 2000 Sep;11(3):207-14. Pubmed
  5. Ito T, Yano I, Tanaka K, Inui KI: Transport of quinolone antibacterial drugs by human P-glycoprotein expressed in a kidney epithelial cell line, LLC-PK1. J Pharmacol Exp Ther. 1997 Aug;282(2):955-60. Pubmed
  6. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. Pubmed

2. Solute carrier family 22 member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 2 O15244 Details

References:

  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. Pubmed
  2. Motohashi H, Uwai Y, Hiramoto K, Okuda M, Inui K: Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Eur J Pharmacol. 2004 Oct 25;503(1-3):25-30. Pubmed
  3. Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun. 2002 Aug 23;296(3):644-50. Pubmed
  4. Urakami Y, Okuda M, Masuda S, Saito H, Inui KI: Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs. J Pharmacol Exp Ther. 1998 Nov;287(2):800-5. Pubmed
  5. Okuda M, Urakami Y, Saito H, Inui K: Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes. Biochim Biophys Acta. 1999 Mar 4;1417(2):224-31. Pubmed
  6. Pan BF, Sweet DH, Pritchard JB, Chen R, Nelson JA: A transfected cell model for the renal toxin transporter, rOCT2. Toxicol Sci. 1999 Feb;47(2):181-6. Pubmed
  7. Dudley AJ, Bleasby K, Brown CD: The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK cell monolayers. Br J Pharmacol. 2000 Sep;131(1):71-9. Pubmed
  8. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  9. Grundemann, D., Liebich, G., Kiefer, N., Koster, S. & Schomig, E. Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol 56, 1-10 (1999). Pubmed

3. Solute carrier family 22 member 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 1 O15245 Details

References:

  1. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM: Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun;51(6):913-21. Pubmed
  2. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. Pubmed
  3. Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun. 2002 Aug 23;296(3):644-50. Pubmed
  4. Zhang L, Dresser MJ, Chun JK, Babbitt PC, Giacomini KM: Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A). J Biol Chem. 1997 Jun 27;272(26):16548-54. Pubmed
  5. Urakami Y, Okuda M, Masuda S, Saito H, Inui KI: Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs. J Pharmacol Exp Ther. 1998 Nov;287(2):800-5. Pubmed
  6. Okuda M, Urakami Y, Saito H, Inui K: Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes. Biochim Biophys Acta. 1999 Mar 4;1417(2):224-31. Pubmed
  7. Jonker JW, Wagenaar E, Mol CA, Buitelaar M, Koepsell H, Smit JW, Schinkel AH: Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene. Mol Cell Biol. 2001 Aug;21(16):5471-7. Pubmed
  8. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed
  9. Wang, D.S. et al. Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther 302, 510-515 (2002). Pubmed

4. Solute carrier family 22 member 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 3 O75751 Details

References:

  1. Grundemann D, Schechinger B, Rappold GA, Schomig E: Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter. Nat Neurosci. 1998 Sep;1(5):349-51. Pubmed
  2. Wu X, Huang W, Ganapathy ME, Wang H, Kekuda R, Conway SJ, Leibach FH, Ganapathy V: Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. Am J Physiol Renal Physiol. 2000 Sep;279(3):F449-58. Pubmed
  3. Kekuda R, Prasad PD, Wu X, Wang H, Fei YJ, Leibach FH, Ganapathy V: Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta. J Biol Chem. 1998 Jun 26;273(26):15971-9. Pubmed
  4. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. Pubmed

5. Solute carrier family 22 member 5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 5 O76082 Details

References:

  1. Wu X, Prasad PD, Leibach FH, Ganapathy V: cDNA sequence, transport function, and genomic organization of human OCTN2, a new member of the organic cation transporter family. Biochem Biophys Res Commun. 1998 May 29;246(3):589-95. Pubmed
  2. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. Pubmed
  3. Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. Pubmed

6. Bile salt export pump

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Bile salt export pump O95342 Details

References:

  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. Pubmed

7. Solute carrier family 22 member 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

References:

  1. Jung KY, Takeda M, Kim DK, Tojo A, Narikawa S, Yoo BS, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001 Sep 21;69(18):2123-35. Pubmed
  2. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed
  3. Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol. 2002 May;61(5):982-8. Pubmed
  4. Burckhardt BC, Brai S, Wallis S, Krick W, Wolff NA, Burckhardt G: Transport of cimetidine by flounder and human renal organic anion transporter 1. Am J Physiol Renal Physiol. 2003 Mar;284(3):F503-9. Epub 2002 Nov 12. Pubmed

8. Solute carrier family 22 member 8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

References:

  1. Jung KY, Takeda M, Kim DK, Tojo A, Narikawa S, Yoo BS, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001 Sep 21;69(18):2123-35. Pubmed
  2. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed
  3. Motohashi H, Uwai Y, Hiramoto K, Okuda M, Inui K: Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Eur J Pharmacol. 2004 Oct 25;503(1-3):25-30. Pubmed
  4. Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. Pubmed
  5. Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. Pubmed
  6. Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol. 2002 May;61(5):982-8. Pubmed
  7. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. Pubmed
  8. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. Pubmed
  9. Bakhiya A, Bahn A, Burckhardt G, Wolff N: Human organic anion transporter 3 (hOAT3) can operate as an exchanger and mediate secretory urate flux. Cell Physiol Biochem. 2003;13(5):249-56. Pubmed
  10. Tahara H, Kusuhara H, Chida M, Fuse E, Sugiyama Y: Is the monkey an appropriate animal model to examine drug-drug interactions involving renal clearance? Effect of probenecid on the renal elimination of H2 receptor antagonists. J Pharmacol Exp Ther. 2006 Mar;316(3):1187-94. Epub 2005 Nov 16. Pubmed
  11. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. Pubmed

9. Multidrug and toxin extrusion protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug and toxin extrusion protein 1 Q96FL8 Details

References:

  1. Lai Y, Sampson KE, Balogh LM, Brayman TG, Cox SR, Adams WJ, Kumar V, Stevens JC: Preclinical and clinical evidence for the collaborative transport and renal secretion of an oxazolidinone antibiotic by organic anion transporter 3 (OAT3/SLC22A8) and multidrug and toxin extrusion protein 1 (MATE1/SLC47A1). J Pharmacol Exp Ther. 2010 Sep 1;334(3):936-44. Epub 2010 Jun 2. Pubmed

10. Solute carrier family 22 member 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 4 Q9H015 Details

References:

  1. Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A: Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther. 1999 May;289(2):768-73. Pubmed
  2. Wu X, George RL, Huang W, Wang H, Conway SJ, Leibach FH, Ganapathy V: Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim Biophys Acta. 2000 Jun 1;1466(1-2):315-27. Pubmed

11. Solute carrier family 22 member 11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed

12. Solute carrier family 22 member 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 7 Q9Y694 Details

References:

  1. Kobayashi Y, Ohshiro N, Shibusawa A, Sasaki T, Tokuyama S, Sekine T, Endou H, Yamamoto T: Isolation, characterization and differential gene expression of multispecific organic anion transporter 2 in mice. Mol Pharmacol. 2002 Jul;62(1):7-14. Pubmed
  2. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. Pubmed

Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11