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Identification
NameOlmesartan
Accession NumberDB00275  (APRD00223)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Olmesartan is an antihypertensive agent, which belongs to the class of medications called angiotensin II receptor blockers. It is indicated for the treatment of high blood pressure and is marketed under the name Olmetec®. The FDA label includes a black-box warning of injury and death to the fetus, so women of child-bearing age need to be warned and take the necessary precautions. Olmesartan is also contraindicated in diabetes mellitus patients taking aliskiren.

Structure
Thumb
Synonyms
4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
4-(hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
External Identifiers
  • DE-092
  • RNH-6270
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Benicartablet, film coated20 mg/1oralbryant ranch prepack2002-04-25Not applicableUs
Benicartablet, film coated40 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-22Not applicableUs
Benicartablet, film coated20 mg/1oralDaiichi Sankyo, Inc.2002-04-25Not applicableUs
Benicartablet, film coated40 mg/1oralPhysicians Total Care, Inc.2003-08-06Not applicableUs
Benicartablet, film coated40 mg/1oralbryant ranch prepack2002-04-25Not applicableUs
Benicartablet, film coated20 mg/1oralREMEDYREPACK INC.2013-10-042016-04-05Us
Benicartablet, film coated40 mg/1oralPd Rx Pharmaceuticals, Inc.2002-04-25Not applicableUs
Benicartablet, film coated40 mg/1oralMed Health Pharma, LLC2012-02-02Not applicableUs
Benicartablet, film coated20 mg/1oralCardinal Health2002-04-25Not applicableUs
Benicartablet, film coated20 mg/1oralMed Health Pharma, LLC2012-02-02Not applicableUs
Benicartablet, film coated40 mg/1oralCardinal Health2002-04-25Not applicableUs
Benicartablet, film coated5 mg/1oralMed Health Pharma, LLC2012-02-02Not applicableUs
Benicartablet, film coated5 mg/1oralCarilion Materials Management2002-04-25Not applicableUs
Benicartablet, film coated20 mg/1oralCardinal Health2002-04-25Not applicableUs
Benicartablet, film coated5 mg/1oralDaiichi Sankyo, Inc.2002-04-25Not applicableUs
Benicartablet, film coated20 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-22Not applicableUs
Benicartablet, film coated40 mg/1oralDaiichi Sankyo, Inc.2002-04-25Not applicableUs
Benicartablet, film coated20 mg/1oralPhysicians Total Care, Inc.2004-01-30Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ErastapexNot Available
GolmeNot Available
OlmetecNot Available
WinBPNot Available
Brand mixtures
NameLabellerIngredients
AzorPhysicians Total Care, Inc.
Benicar HctLake Erie Medical & Surgical Supply DBA Quality Care Products LLC
TribenzorDaiichi Sankyo, Inc.
Salts
Name/CASStructureProperties
Olmesartan medoxomil
144689-63-4
Thumb
  • InChI Key: UQGKUQLKSCSZGY-UHFFFAOYSA-N
  • Monoisotopic Mass: 558.22268271
  • Average Mass: 558.595
DBSALT001815
Categories
UNII8W1IQP3U10
CAS number144689-24-7
WeightAverage: 446.5016
Monoisotopic: 446.206638728
Chemical FormulaC24H26N6O3
InChI KeyInChIKey=VTRAEEWXHOVJFV-UHFFFAOYSA-N
InChI
InChI=1S/C24H26N6O3/c1-4-7-19-25-21(24(2,3)33)20(23(31)32)30(19)14-15-10-12-16(13-11-15)17-8-5-6-9-18(17)22-26-28-29-27-22/h5-6,8-13,33H,4,7,14H2,1-3H3,(H,31,32)(H,26,27,28,29)
IUPAC Name
4-(2-hydroxypropan-2-yl)-2-propyl-1-({4-[2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-imidazole-5-carboxylic acid
SMILES
CCCC1=NC(=C(N1CC1=CC=C(C=C1)C1=C(C=CC=C1)C1=NN=NN1)C(O)=O)C(C)(C)O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as biphenyltetrazoles and derivatives. These are organic compounds containing a biphenyl attached to a tetrazole. A carbon atom of the biphenyl moiety is boned to a carbon or the nitrogen atom of the tetrazole moiety.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassTetrazoles
Direct ParentBiphenyltetrazoles and derivatives
Alternative Parents
Substituents
  • Biphenyltetrazole
  • Biphenyl
  • 1,2,4,5-tetrasubstituted imidazole
  • Phenylmethylamine
  • Benzenoid
  • N-substituted imidazole
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary alcohol
  • Imidazole
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of hypertension.
PharmacodynamicsOlmesartan is a specific angiotensin II type 1 (AT1) receptor antagonist, which blocks the blood pressure increasing effects of angiotensin II via the renin-angiotensin-aldosterone system (RAAS). During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering cardiovascular structure. Angiotensin II binds to two receptors: AT1 and AT2. AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II. Angiotensin receptor blockers (ARBs) are non-peptide competitive inhibitors of AT1. ARBs block the ability of angiotensin II to stimulate pressor and cell proliferative effects. Unlike ACE inhibitors, ARBs do not affect bradykinin-induced vasodilation. The overall effect of ARBs is a decrease in blood pressure.
Mechanism of actionOlmesartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Olmesartan is selective for AT1 and has a 12,500 times greater affinity for AT1 than the AT2 receptor. Also unlike the well-known ARB losartan, olmesartan does not have an active metabolite or possess uricosuric effects.
Related Articles
AbsorptionBioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
Volume of distribution

The volume of distribution is 17 L and olmesartan poorly crosses the blood brain barrier.

Protein bindingHighly bound to plasma proteins (99%) and does not penetrate red blood cells.
Metabolism

Olmesartan is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. There is virtually no further metabolism of olmesartan.

Route of eliminationOlmesartan is elminated unchanged in the urine (35% to 50%) and the remainder in the feces.
Half lifeThe half life is approximately 13 hours.
Clearance
  • Total plasma cl=1.3 L/h
  • Renal cl=0.6 L/h
ToxicityThe main symptoms of overdose include low blood pressure and fast heartbeat.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Olmesartan Action PathwayDrug actionSMP00163
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier-0.8719
Caco-2 permeable-0.6865
P-glycoprotein substrateSubstrate0.7247
P-glycoprotein inhibitor INon-inhibitor0.5917
P-glycoprotein inhibitor IIInhibitor0.6029
Renal organic cation transporterNon-inhibitor0.807
CYP450 2C9 substrateNon-substrate0.7429
CYP450 2D6 substrateNon-substrate0.8602
CYP450 3A4 substrateNon-substrate0.5149
CYP450 1A2 substrateNon-inhibitor0.782
CYP450 2C9 inhibitorInhibitor0.5816
CYP450 2D6 inhibitorNon-inhibitor0.8059
CYP450 2C19 inhibitorInhibitor0.6604
CYP450 3A4 inhibitorInhibitor0.7409
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8396
Ames testNon AMES toxic0.6203
CarcinogenicityNon-carcinogens0.6871
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6599 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9254
hERG inhibition (predictor II)Non-inhibitor0.6427
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Daiichi sankyo inc
  • Daiichi Sankyo
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral40 mg/1
Tablet, film coatedoral5 mg/1
Tablet, film coatedoral
Prices
Unit descriptionCostUnit
Benicar 5 mg tablet12.81USD tablet
Benicar hct 40-25 mg tablet4.93USD tablet
Benicar hct 40-12.5 mg tablet4.67USD tablet
Benicar hct 20-12.5 mg tablet3.94USD tablet
Benicar 40 mg tablet3.74USD tablet
Benicar 20 mg tablet2.97USD tablet
Olmetec 20 mg Tablet1.04USD tablet
Olmetec 40 mg Tablet1.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2061607 No1999-01-192012-02-20Canada
US5616599 Yes1996-10-252016-10-25Us
US6878703 Yes2002-05-192022-05-19Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point175-180 °CNot Available
logP5.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0105 mg/mLALOGPS
logP2.98ALOGPS
logP2.14ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)0.91ChemAxon
pKa (Strongest Basic)5.57ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area129.81 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity137.32 m3·mol-1ChemAxon
Polarizability47.46 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Lilach Hedvati, Gideon Pilarsky, “Preparation of olmesartan medoxomil.” U.S. Patent US20060069141, issued March 30, 2006.

US20060069141
General ReferencesNot Available
External Links
ATC CodesC09DA08C09CA08C09DX03C09DB02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (179 KB)
MSDSDownload (58.6 KB)
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Olmesartan.
AcebutololOlmesartan may increase the hypotensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Aceclofenac.
AcetazolamideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Acetazolamide.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Acetylsalicylic acid.
AdapaleneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Adapalene.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Olmesartan.
AlfuzosinAlfuzosin may increase the hypotensive activities of Olmesartan.
AliskirenOlmesartan may increase the hypotensive activities of Aliskiren.
AlprenololOlmesartan may increase the hypotensive activities of Alprenolol.
AmbrisentanOlmesartan may increase the hypotensive activities of Ambrisentan.
AmifostineOlmesartan may increase the hypotensive activities of Amifostine.
AmilorideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Amiloride.
AmlodipineOlmesartan may increase the hypotensive activities of Amlodipine.
AmobarbitalAmobarbital may increase the hypotensive activities of Olmesartan.
Amyl NitriteThe risk or severity of adverse effects can be increased when Olmesartan is combined with Amyl Nitrite.
AntipyrineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Antipyrine.
ApraclonidineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Apraclonidine.
ApremilastThe risk or severity of adverse effects can be increased when Olmesartan is combined with Apremilast.
ArdeparinArdeparin may increase the hyperkalemic activities of Olmesartan.
AripiprazoleAripiprazole may increase the hypotensive activities of Olmesartan.
AtenololOlmesartan may increase the hypotensive activities of Atenolol.
AzapropazoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Azapropazone.
AzelastineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Azelastine.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Olmesartan is combined with Azilsartan medoxomil.
BalsalazideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Balsalazide.
BarbitalBarbital may increase the hypotensive activities of Olmesartan.
BemiparinBemiparin may increase the hyperkalemic activities of Olmesartan.
BenazeprilOlmesartan may increase the hypotensive activities of Benazepril.
BendroflumethiazideOlmesartan may increase the hypotensive activities of Bendroflumethiazide.
BenmoxinBenmoxin may increase the hypotensive activities of Olmesartan.
BenoxaprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Benoxaprofen.
BepridilOlmesartan may increase the hypotensive activities of Bepridil.
BetaxololBetaxolol may increase the hypotensive activities of Olmesartan.
BethanidineBethanidine may increase the hypotensive activities of Olmesartan.
BimatoprostOlmesartan may increase the hypotensive activities of Bimatoprost.
BisoprololOlmesartan may increase the hypotensive activities of Bisoprolol.
BosentanOlmesartan may increase the hypotensive activities of Bosentan.
BretyliumOlmesartan may increase the hypotensive activities of Bretylium.
BrimonidineOlmesartan may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Olmesartan.
BromfenacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Bromfenac.
BumetanideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Bumetanide.
BupranololOlmesartan may increase the hypotensive activities of Bupranolol.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Olmesartan.
CanagliflozinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Canagliflozin.
CandesartanOlmesartan may increase the hypotensive activities of Candesartan.
CandoxatrilOlmesartan may increase the hypotensive activities of Candoxatril.
CaptoprilOlmesartan may increase the hypotensive activities of Captopril.
CaroxazoneCaroxazone may increase the hypotensive activities of Olmesartan.
CarprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Carprofen.
CarteololOlmesartan may increase the hypotensive activities of Carteolol.
CarvedilolOlmesartan may increase the hypotensive activities of Carvedilol.
CastanospermineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Castanospermine.
CelecoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Celecoxib.
CeliprololOlmesartan may increase the hypotensive activities of Celiprolol.
CertoparinCertoparin may increase the hyperkalemic activities of Olmesartan.
ChloroquineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Chloroquine.
ChlorothiazideOlmesartan may increase the hypotensive activities of Chlorothiazide.
ChlorthalidoneOlmesartan may increase the hypotensive activities of Chlorthalidone.
CilazaprilOlmesartan may increase the hypotensive activities of Cilazapril.
CiprofloxacinOlmesartan may increase the arrhythmogenic activities of Ciprofloxacin.
ClevidipineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Clevidipine.
ClonidineOlmesartan may increase the hypotensive activities of Clonidine.
ClonixinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Clonixin.
ColesevelamThe serum concentration of Olmesartan can be decreased when it is combined with Colesevelam.
CryptenamineOlmesartan may increase the hypotensive activities of Cryptenamine.
CyclosporineOlmesartan may increase the hyperkalemic activities of Cyclosporine.
CyclothiazideOlmesartan may increase the hypotensive activities of Cyclothiazide.
D-LimoneneThe risk or severity of adverse effects can be increased when Olmesartan is combined with D-Limonene.
DalteparinDalteparin may increase the hyperkalemic activities of Olmesartan.
DapagliflozinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Dapagliflozin.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Olmesartan.
DebrisoquinOlmesartan may increase the hypotensive activities of Debrisoquin.
DeserpidineOlmesartan may increase the hypotensive activities of Deserpidine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Dexmedetomidine.
DiazoxideDiazoxide may increase the hypotensive activities of Olmesartan.
DiclofenacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Diclofenac.
DiclofenamideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Diclofenamide.
DiflunisalThe risk or severity of adverse effects can be increased when Olmesartan is combined with Diflunisal.
DiltiazemOlmesartan may increase the hypotensive activities of Diltiazem.
DinutuximabThe risk or severity of adverse effects can be increased when Olmesartan is combined with Dinutuximab.
DipyridamoleThe risk or severity of adverse effects can be increased when Olmesartan is combined with Dipyridamole.
DorzolamideOlmesartan may increase the hypotensive activities of Dorzolamide.
DoxazosinOlmesartan may increase the hypotensive activities of Doxazosin.
DrospirenoneOlmesartan may increase the hyperkalemic activities of Drospirenone.
DroxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Droxicam.
DuloxetineOlmesartan may increase the orthostatic hypotensive activities of Duloxetine.
EfonidipineOlmesartan may increase the hypotensive activities of Efonidipine.
EltrombopagThe serum concentration of Olmesartan can be increased when it is combined with Eltrombopag.
EmpagliflozinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Empagliflozin.
EnalaprilOlmesartan may increase the hypotensive activities of Enalapril.
EnalaprilatOlmesartan may increase the hypotensive activities of Enalaprilat.
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Olmesartan.
EpirizoleThe risk or severity of adverse effects can be increased when Olmesartan is combined with Epirizole.
EplerenoneEplerenone may increase the hyperkalemic activities of Olmesartan.
EplerenoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Eplerenone.
EpoprostenolOlmesartan may increase the hypotensive activities of Epoprostenol.
EprosartanOlmesartan may increase the hypotensive activities of Eprosartan.
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Olmesartan.
Etacrynic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Etacrynic acid.
EtanerceptThe risk or severity of adverse effects can be increased when Olmesartan is combined with Etanercept.
EtodolacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Etodolac.
EtofenamateThe risk or severity of adverse effects can be increased when Olmesartan is combined with Etofenamate.
EtoricoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Etoricoxib.
Evening primrose oilThe risk or severity of adverse effects can be increased when Olmesartan is combined with Evening primrose oil.
exisulindThe risk or severity of adverse effects can be increased when Olmesartan is combined with exisulind.
FelodipineOlmesartan may increase the hypotensive activities of Felodipine.
FenbufenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Fenbufen.
FenoldopamOlmesartan may increase the hypotensive activities of Fenoldopam.
FenoprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Fenoprofen.
FloctafenineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Floctafenine.
FlunixinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Flunixin.
FlurbiprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Flurbiprofen.
FosinoprilOlmesartan may increase the hypotensive activities of Fosinopril.
FurazolidoneFurazolidone may increase the hypotensive activities of Olmesartan.
FurosemideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Furosemide.
GuanabenzOlmesartan may increase the hypotensive activities of Guanabenz.
GuanadrelGuanadrel may increase the hypotensive activities of Olmesartan.
GuanethidineOlmesartan may increase the hypotensive activities of Guanethidine.
GuanfacineOlmesartan may increase the hypotensive activities of Guanfacine.
HeparinHeparin may increase the hyperkalemic activities of Olmesartan.
HexamethoniumOlmesartan may increase the hypotensive activities of Hexamethonium.
HexobarbitalHexobarbital may increase the hypotensive activities of Olmesartan.
HMPL-004The risk or severity of adverse effects can be increased when Olmesartan is combined with HMPL-004.
HydracarbazineHydracarbazine may increase the hypotensive activities of Olmesartan.
HydralazineOlmesartan may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideOlmesartan may increase the hypotensive activities of Hydrochlorothiazide.
HydroflumethiazideOlmesartan may increase the hypotensive activities of Hydroflumethiazide.
IbuprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Ibuprofen.
IbuproxamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Ibuproxam.
IcatibantThe risk or severity of adverse effects can be increased when Olmesartan is combined with Icatibant.
IloprostIloprost may increase the hypotensive activities of Olmesartan.
IndapamideOlmesartan may increase the hypotensive activities of Indapamide.
IndenololOlmesartan may increase the hypotensive activities of Indenolol.
IndomethacinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Indomethacin.
IndoprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Indoprofen.
IndoraminOlmesartan may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Olmesartan.
IproniazidIproniazid may increase the hypotensive activities of Olmesartan.
IrbesartanOlmesartan may increase the hypotensive activities of Irbesartan.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Olmesartan.
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Olmesartan is combined with Isosorbide Dinitrate.
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Olmesartan is combined with Isosorbide Mononitrate.
IsoxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Isoxicam.
IsoxsuprineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Isoxsuprine.
IsradipineIsradipine may increase the hypotensive activities of Olmesartan.
KebuzoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Kebuzone.
KetoprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Ketorolac.
LabetalolOlmesartan may increase the hypotensive activities of Labetalol.
LacidipineOlmesartan may increase the hypotensive activities of Lacidipine.
LatanoprostOlmesartan may increase the hypotensive activities of Latanoprost.
LeflunomideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Leflunomide.
LercanidipineOlmesartan may increase the hypotensive activities of Lercanidipine.
LevobunololThe risk or severity of adverse effects can be increased when Olmesartan is combined with Levobunolol.
LevodopaOlmesartan may increase the orthostatic hypotensive activities of Levodopa.
LisinoprilOlmesartan may increase the hypotensive activities of Lisinopril.
LithiumThe serum concentration of Lithium can be increased when it is combined with Olmesartan.
LofexidineOlmesartan may increase the hypotensive activities of Lofexidine.
LornoxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Lornoxicam.
LosartanOlmesartan may increase the hypotensive activities of Losartan.
LoxoprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Loxoprofen.
LumiracoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Lumiracoxib.
MacitentanOlmesartan may increase the hypotensive activities of Macitentan.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Olmesartan is combined with Magnesium salicylate.
ManidipineOlmesartan may increase the hypotensive activities of Manidipine.
MannitolThe risk or severity of adverse effects can be increased when Olmesartan is combined with Mannitol.
MasoprocolThe risk or severity of adverse effects can be increased when Olmesartan is combined with Masoprocol.
MebanazineMebanazine may increase the hypotensive activities of Olmesartan.
MecamylamineOlmesartan may increase the hypotensive activities of Mecamylamine.
Meclofenamic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Meclofenamic acid.
Mefenamic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Meloxicam.
MesalazineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Mesalazine.
MetamizoleThe risk or severity of adverse effects can be increased when Olmesartan is combined with Metamizole.
MethazolamideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Methazolamide.
MethohexitalMethohexital may increase the hypotensive activities of Olmesartan.
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Olmesartan.
MethyldopaOlmesartan may increase the hypotensive activities of Methyldopa.
Methylene blueMethylene blue may increase the hypotensive activities of Olmesartan.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Olmesartan.
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Olmesartan.
MetipranololOlmesartan may increase the hypotensive activities of Metipranolol.
MetolazoneOlmesartan may increase the hypotensive activities of Metolazone.
MetoprololMetoprolol may increase the hypotensive activities of Olmesartan.
MibefradilOlmesartan may increase the hypotensive activities of Mibefradil.
MinaprineMinaprine may increase the hypotensive activities of Olmesartan.
MinoxidilOlmesartan may increase the hypotensive activities of Minoxidil.
MoclobemideMoclobemide may increase the hypotensive activities of Olmesartan.
MoexiprilOlmesartan may increase the hypotensive activities of Moexipril.
MolsidomineMolsidomine may increase the hypotensive activities of Olmesartan.
MoxonidineOlmesartan may increase the hypotensive activities of Moxonidine.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Olmesartan is combined with Mycophenolate mofetil.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Mycophenolic acid.
NabumetoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nabumetone.
NadololOlmesartan may increase the hypotensive activities of Nadolol.
NadroparinNadroparin may increase the hyperkalemic activities of Olmesartan.
NaftifineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Naftifine.
NaproxenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Naproxen.
NCX 4016The risk or severity of adverse effects can be increased when Olmesartan is combined with NCX 4016.
NebivololOlmesartan may increase the hypotensive activities of Nebivolol.
NepafenacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nepafenac.
NesiritideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nesiritide.
NialamideNialamide may increase the hypotensive activities of Olmesartan.
NicardipineOlmesartan may increase the hypotensive activities of Nicardipine.
NicorandilNicorandil may increase the hypotensive activities of Olmesartan.
NifedipineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nifedipine.
Niflumic AcidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Niflumic Acid.
NiguldipineOlmesartan may increase the hypotensive activities of Niguldipine.
NilvadipineOlmesartan may increase the hypotensive activities of Nilvadipine.
NimesulideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nimesulide.
NimodipineOlmesartan may increase the hypotensive activities of Nimodipine.
NisoldipineOlmesartan may increase the hypotensive activities of Nisoldipine.
NitrendipineOlmesartan may increase the hypotensive activities of Nitrendipine.
NitroglycerinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nitroglycerin.
NitroprussideOlmesartan may increase the hypotensive activities of Nitroprusside.
ObinutuzumabOlmesartan may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Olmesartan.
OlopatadineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Olopatadine.
OlsalazineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Olsalazine.
OmapatrilatOlmesartan may increase the hypotensive activities of Omapatrilat.
OrgoteinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Orgotein.
OxaprozinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Oxaprozin.
OxprenololOlmesartan may increase the hypotensive activities of Oxprenolol.
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Oxyphenbutazone.
PapaverineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Papaverine.
ParecoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Parecoxib.
PargylineOlmesartan may increase the hypotensive activities of Pargyline.
ParnaparinParnaparin may increase the hyperkalemic activities of Olmesartan.
PenbutololOlmesartan may increase the hypotensive activities of Penbutolol.
PentobarbitalPentobarbital may increase the hypotensive activities of Olmesartan.
PentoliniumOlmesartan may increase the hypotensive activities of Pentolinium.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Olmesartan.
PerindoprilOlmesartan may increase the hypotensive activities of Perindopril.
PhenelzinePhenelzine may increase the hypotensive activities of Olmesartan.
PheniprazinePheniprazine may increase the hypotensive activities of Olmesartan.
PhenobarbitalPhenobarbital may increase the hypotensive activities of Olmesartan.
PhenoxybenzamineOlmesartan may increase the hypotensive activities of Phenoxybenzamine.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Olmesartan.
PhentolamineOlmesartan may increase the hypotensive activities of Phentolamine.
PhenylbutazoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Phenylbutazone.
PimecrolimusThe risk or severity of adverse effects can be increased when Olmesartan is combined with Pimecrolimus.
PinacidilOlmesartan may increase the hypotensive activities of Pinacidil.
PindololOlmesartan may increase the hypotensive activities of Pindolol.
PirfenidoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Pirfenidone.
PirlindolePirlindole may increase the hypotensive activities of Olmesartan.
PiroxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Piroxicam.
PivhydrazinePivhydrazine may increase the hypotensive activities of Olmesartan.
PolythiazideOlmesartan may increase the hypotensive activities of Polythiazide.
PrazosinOlmesartan may increase the hypotensive activities of Prazosin.
PrimidonePrimidone may increase the hypotensive activities of Olmesartan.
PropacetamolThe risk or severity of adverse effects can be increased when Olmesartan is combined with Propacetamol.
PropranololOlmesartan may increase the hypotensive activities of Propranolol.
PTC299The risk or severity of adverse effects can be increased when Olmesartan is combined with PTC299.
QuetiapineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Quetiapine.
QuinaprilOlmesartan may increase the hypotensive activities of Quinapril.
QuinineQuinine may increase the hypotensive activities of Olmesartan.
RamiprilRamipril may increase the hypotensive activities of Olmesartan.
RasagilineRasagiline may increase the hypotensive activities of Olmesartan.
RemikirenRemikiren may increase the hypotensive activities of Olmesartan.
RescinnamineOlmesartan may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Olmesartan.
ResveratrolThe risk or severity of adverse effects can be increased when Olmesartan is combined with Resveratrol.
ReviparinReviparin may increase the hyperkalemic activities of Olmesartan.
RiociguatOlmesartan may increase the hypotensive activities of Riociguat.
RisperidoneOlmesartan may increase the hypotensive activities of Risperidone.
RituximabOlmesartan may increase the hypotensive activities of Rituximab.
RofecoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Rofecoxib.
SafrazineSafrazine may increase the hypotensive activities of Olmesartan.
SalicylamideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Salicylamide.
Salicylic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Salicylic acid.
SalsalateThe risk or severity of adverse effects can be increased when Olmesartan is combined with Salsalate.
SaprisartanOlmesartan may increase the hypotensive activities of Saprisartan.
SecobarbitalSecobarbital may increase the hypotensive activities of Olmesartan.
SelegilineSelegiline may increase the hypotensive activities of Olmesartan.
SelexipagOlmesartan may increase the hypotensive activities of Selexipag.
SeratrodastThe risk or severity of adverse effects can be increased when Olmesartan is combined with Seratrodast.
SildenafilSildenafil may increase the antihypertensive activities of Olmesartan.
SitaxentanOlmesartan may increase the hypotensive activities of Sitaxentan.
SotalolThe risk or severity of adverse effects can be increased when Olmesartan is combined with Sotalol.
SpiraprilOlmesartan may increase the hypotensive activities of Spirapril.
SpironolactoneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Spironolactone.
SRT501The risk or severity of adverse effects can be increased when Olmesartan is combined with SRT501.
SulfasalazineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Sulfasalazine.
SulindacThe risk or severity of adverse effects can be increased when Olmesartan is combined with Sulindac.
SuprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Suprofen.
TadalafilTadalafil may increase the antihypertensive activities of Olmesartan.
TelmisartanOlmesartan may increase the hypotensive activities of Telmisartan.
TemocaprilOlmesartan may increase the hypotensive activities of Temocapril.
TenoxicamThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tenoxicam.
TepoxalinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tepoxalin.
TerazosinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Terazosin.
TeriflunomideThe serum concentration of Olmesartan can be increased when it is combined with Teriflunomide.
TeriflunomideThe risk or severity of adverse effects can be increased when Olmesartan is combined with Teriflunomide.
TerlipressinOlmesartan may increase the hypotensive activities of Terlipressin.
ThiamylalThiamylal may increase the hypotensive activities of Olmesartan.
ThiopentalThiopental may increase the hypotensive activities of Olmesartan.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tiaprofenic acid.
TiboloneOlmesartan may increase the hypotensive activities of Tibolone.
TicrynafenOlmesartan may increase the hypotensive activities of Ticrynafen.
TimololOlmesartan may increase the hypotensive activities of Timolol.
TinzaparinTinzaparin may increase the hyperkalemic activities of Olmesartan.
TizanidineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tizanidine.
TolazolineOlmesartan may increase the hypotensive activities of Tolazoline.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tolfenamic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tolmetin.
ToloxatoneToloxatone may increase the hypotensive activities of Olmesartan.
TolvaptanTolvaptan may increase the hyperkalemic activities of Olmesartan.
TorasemideTorasemide may increase the hypotensive activities of Olmesartan.
TrandolaprilOlmesartan may increase the hypotensive activities of Trandolapril.
TranilastThe risk or severity of adverse effects can be increased when Olmesartan is combined with Tranilast.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Olmesartan.
TranylcypromineTranylcypromine may increase the hypotensive activities of Olmesartan.
TravoprostOlmesartan may increase the hypotensive activities of Travoprost.
TreprostinilOlmesartan may increase the hypotensive activities of Treprostinil.
TriamtereneThe risk or severity of adverse effects can be increased when Olmesartan is combined with Triamterene.
TrichlormethiazideOlmesartan may increase the hypotensive activities of Trichlormethiazide.
TrimazosinOlmesartan may increase the hypotensive activities of Trimazosin.
TrimethaphanOlmesartan may increase the hypotensive activities of Trimethaphan.
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Olmesartan.
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Olmesartan is combined with Trisalicylate-choline.
UdenafilUdenafil may increase the antihypertensive activities of Olmesartan.
UnoprostoneOlmesartan may increase the hypotensive activities of Unoprostone.
ValdecoxibThe risk or severity of adverse effects can be increased when Olmesartan is combined with Valdecoxib.
ValsartanValsartan may increase the hypotensive activities of Olmesartan.
VardenafilVardenafil may increase the antihypertensive activities of Olmesartan.
VerapamilThe risk or severity of adverse effects can be increased when Olmesartan is combined with Verapamil.
XylometazolineOlmesartan may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Olmesartan.
ZaltoprofenThe risk or severity of adverse effects can be increased when Olmesartan is combined with Zaltoprofen.
ZileutonThe risk or severity of adverse effects can be increased when Olmesartan is combined with Zileuton.
ZomepiracThe risk or severity of adverse effects can be increased when Olmesartan is combined with Zomepirac.
Food Interactions
  • Food does not affect the bioavailability of olmesartan.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
AGTR1
Uniprot ID:
P30556
Molecular Weight:
41060.53 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Koike H, Sada T, Mizuno M: In vitro and in vivo pharmacology of olmesartan medoxomil, an angiotensin II type AT1 receptor antagonist. J Hypertens Suppl. 2001 Jun;19(1):S3-14. [PubMed:11451212 ]
  3. Ochiai K, Hu Q, Lee J, Mansoor A, Liu J, Wang X, Gong G, Murakami Y, Ishibashi Y, Shimada T, Zhang J: Functional and bioenergetic consequences of AT1 antagonist olmesartan medoxomil in hearts with postinfarction LV remodeling. J Cardiovasc Pharmacol. 2006 May;47(5):686-94. [PubMed:16775509 ]
  4. Warner GT, Jarvis B: Olmesartan medoxomil. Drugs. 2002;62(9):1345-53; discussion 1354-6. [PubMed:12076183 ]
  5. Mire DE, Silfani TN, Pugsley MK: A review of the structural and functional features of olmesartan medoxomil, an angiotensin receptor blocker. J Cardiovasc Pharmacol. 2005 Nov;46(5):585-93. [PubMed:16220064 ]
  6. Kreutz R, Bolbrinker J, Huber M: Pharmacokinetics of olmesartan medoxomil plus hydrochlorothiazide combination in healthy subjects. Clin Drug Investig. 2006;26(1):29-34. [PubMed:17163232 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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
Molecular Weight:
174205.64 Da
References
  1. Weiss J, Sauer A, Divac N, Herzog M, Schwedhelm E, Boger RH, Haefeli WE, Benndorf RA: Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos. 2010 Mar;31(2-3):150-61. doi: 10.1002/bdd.699. [PubMed:20222053 ]
  2. Nakagomi-Hagihara R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, Ikeda T: OATP1B1, OATP1B3, and mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Dispos. 2006 May;34(5):862-9. Epub 2006 Feb 24. [PubMed:16501004 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Nakagomi-Hagihara R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, Ikeda T: OATP1B1, OATP1B3, and mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Dispos. 2006 May;34(5):862-9. Epub 2006 Feb 24. [PubMed:16501004 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Nakagomi-Hagihara R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, Ikeda T: OATP1B1, OATP1B3, and mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Dispos. 2006 May;34(5):862-9. Epub 2006 Feb 24. [PubMed:16501004 ]
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Drug created on June 13, 2005 07:24 / Updated on August 31, 2016 03:28