You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameBrimonidine
Accession NumberDB00484  (APRD00034)
TypeSmall Molecule
GroupsApproved
Description

Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. [Wikipedia] A topical gel formulation, marketed under the name Mirvaso, was FDA approved on August 2013 for the treatment of rosacea.

Structure
Thumb
Synonyms
5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline
Brimonidina
Brimonidine
Brimonidinum
Bromoxidine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alphaganliquid0.2 %ophthalmicAllergan Inc1997-12-02Not applicableCanada
Alphagan Psolution/ drops1.5 mg/mLophthalmicAllergan, Inc.2001-07-10Not applicableUs
Alphagan Psolution/ drops1.5 mg/mLophthalmicPhysicians Total Care, Inc.2002-10-16Not applicableUs
Alphagan Psolution0.15 %ophthalmicAllergan Inc2003-11-05Not applicableCanada
Alphagan Psolution/ drops1 mg/mLophthalmicPhysicians Total Care, Inc.2013-03-08Not applicableUs
Alphagan Psolution/ drops1 mg/mLophthalmicAllergan, Inc.2006-01-25Not applicableUs
Brimonidinesolution0.2 %ophthalmicPharmascience IncNot applicableNot applicableCanada
Brimonidine Ophthalmicsolution0.2 %ophthalmicPharmel IncNot applicableNot applicableCanada
Brimonidine Psolution0.15 %ophthalmicAa Pharma Inc2008-07-15Not applicableCanada
Brimonidine Tartratesolution1.5 mg/mLophthalmicSandoz Inc2010-10-02Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicPacific Pharma, Inc.2003-04-10Not applicableUs
Brimonidine Tartratesolution1.5 mg/mLophthalmicPhysicians Total Care, Inc.2009-12-22Not applicableUs
Brimonidine Tartrate Ophthalmic Solution 0.2%solution0.2 %ophthalmicAlcon Canada IncNot applicableNot applicableCanada
Dom-brimonidinesolution0.2 %ophthalmicDominion PharmacalNot applicableNot applicableCanada
Mirvasogel5 mg/gtopicalGalderma Laboratories, L.P.2013-08-23Not applicableUs
Onrelteagel0.33 %topicalGalderma Canada Inc2014-03-24Not applicableCanada
PMS-brimonidinesolution0.2 %ophthalmicPharmascience Inc2002-08-13Not applicableCanada
Ratio-brimonidinesolution0.2 %ophthalmicTeva Canada Limited2002-07-10Not applicableCanada
Sandoz Brimonidinesolution0.2 %ophthalmicSandoz Canada Incorporated2008-02-08Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-brimonidinesolution0.2 %ophthalmicApotex Inc2005-06-02Not applicableCanada
Brimonidinesolution/ drops2 mg/mLophthalmicAkorn, Inc.2006-09-07Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicSTAT Rx USA LLC2003-05-28Not applicableUs
Brimonidine Tartratesolution2 mg/mLophthalmicSandoz Inc2003-09-17Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicPhysicians Total Care, Inc.2011-07-25Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicREMEDYREPACK INC.2013-06-24Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mgophthalmicOsmotica Pharmaceutical Corp.2015-01-01Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicBausch & Lomb Incorporated2003-05-28Not applicableUs
Brimonidine Tartratesolution/ drops2 mg/mLophthalmicRegimed Medical2016-01-05Not applicableUs
Brimonidine Tartrate Ophthalmic Solution, 0.2%solution/ drops2 mg/mLophthalmicWestminster Pharmaceuticals, Llc2015-09-18Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Apo-brimonidine-timopApotex Inc
CombiganAllergan, Inc.
SimbrinzaAlcon Laboratories, Inc.
Salts
Name/CASStructureProperties
Brimonidine Tartrate
70359-46-5
Thumb
  • InChI Key: QZHBYNSSDLTCRG-LREBCSMRSA-N
  • Monoisotopic Mass: 441.028395916
  • Average Mass: 442.221
DBSALT000195
Categories
UNIIE6GNX3HHTE
CAS number59803-98-4
WeightAverage: 292.135
Monoisotopic: 291.011957992
Chemical FormulaC11H10BrN5
InChI KeyInChIKey=XYLJNLCSTIOKRM-UHFFFAOYSA-N
InChI
InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17)
IUPAC Name
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine
SMILES
BrC1=C(NC2=NCCN2)C=CC2=NC=CN=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinoxalines. These are compounds containing a quinoxaline moiety, a bicyclic heterocycle made up of a benzene ring fused to a pyrazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassQuinoxalines
Direct ParentQuinoxalines
Alternative Parents
Substituents
  • Quinoxaline
  • 2-bromoaniline
  • Benzenoid
  • Pyrazine
  • Aryl halide
  • Aryl bromide
  • Heteroaromatic compound
  • 2-imidazoline
  • Guanidine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organobromide
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationThe ophthalmic solution is indicated for patients with open-angle glaucoma or ocular hypertension to lower intraocular pressure. The topical gel is indicated for the treatment of persistent (nontransient) facial erythema of rosacea in adults 18 years or older.
PharmacodynamicsBrimonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.
Mechanism of actionBrimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. The topical gel reduces erythema through direct vasocontriction.
Related Articles
AbsorptionMinimal systemic absorption occurs after ocular insertion. When the topical gel was applied to adult patients with facial erythema associated with rosacea, the plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) were 46 ± 62 pg/mL and 417 ± 264 pg.hr/mL, respectively. These values were reached on Day 15 of treatment.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Metabolized primarily by the liver.

SubstrateEnzymesProduct
Brimonidine
2-oxobrimonidineDetails
Brimonidine
3-oxobrimonidine Details
Route of eliminationUrinary excretion is the major route of elimination of the drug and its metabolites.
Half life2 hours [ophthalmic solution]
ClearanceNot Available
ToxicityOral LD50 is 50 mg/kg in mice and 100 mg/kg in rats. Common adverse reactions of the topical gel formulation include erythema, flushing, skin burning sensation, and contact dermatitis.
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+0.978
Blood Brain Barrier+0.717
Caco-2 permeable+0.5435
P-glycoprotein substrateSubstrate0.7017
P-glycoprotein inhibitor INon-inhibitor0.5688
P-glycoprotein inhibitor IIInhibitor0.5951
Renal organic cation transporterInhibitor0.8266
CYP450 2C9 substrateNon-substrate0.8403
CYP450 2D6 substrateNon-substrate0.7533
CYP450 3A4 substrateNon-substrate0.5617
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.6898
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7044
Ames testNon AMES toxic0.8222
CarcinogenicityNon-carcinogens0.9446
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0196 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8093
hERG inhibition (predictor II)Non-inhibitor0.6711
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Allergan inc
  • Allergan
  • Akorn inc
  • Alcon inc
  • Alcon research ltd
  • Bausch and lomb pharmaceuticals inc
  • Sandoz canada inc
  • Teva parenteral medicines inc
  • Allergan, Inc
Packagers
Dosage forms
FormRouteStrength
Liquidophthalmic0.2 %
Solutionophthalmic0.15 %
Solution/ dropsophthalmic1 mg/mL
Solution/ dropsophthalmic1.5 mg/mL
Solutionophthalmic1.5 mg/mL
Solutionophthalmic2 mg/mL
Solution/ dropsophthalmic2 mg/mg
Solution/ dropsophthalmic2 mg/mL
Solutionophthalmic
Solution/ dropsophthalmic
Geltopical5 mg/g
Geltopical0.33 %
Solutionophthalmic0.2 %
Suspensionophthalmic
Suspension/ dropsophthalmic
Prices
Unit descriptionCostUnit
Alphagan P 15ml Bottle .15% 15ml Bottle228.5USD bottle
Brimonidine Tartrate 0.15% Solution 15ml Bottle218.5USD bottle
Alphagan P 0.1% Solution 15ml Bottle208.94USD bottle
Alphagan P 10ml Bottle .15% 10ml Bottle152.32USD bottle
Brimonidine Tartrate 0.15% Solution 10ml Bottle145.65USD bottle
Alphagan P 0.1% Solution 10ml Bottle143.97USD bottle
Alphagan P 5ml Bottle .15% 5ml Bottle79.52USD bottle
Brimonidine Tartrate 0.15% Solution 5ml Bottle72.85USD bottle
Brimonidine Tartrate 0.2% Solution 10ml Bottle67.85USD bottle
Brimonidine Tartrate 0.2% Solution 15ml Bottle56.88USD bottle
Brimonidine Tartrate 0.2% Solution 5ml Bottle33.96USD bottle
Brimonidine tartrate 0.15% drp29.82USD ml
Alphagan p 0.15% eye drops14.65USD ml
Alphagan p 0.1% drops13.85USD ml
Brimonidine 0.2% eye drop6.53USD ml
Alphagan 0.2 % Solution3.72USD ml
Apo-Brimonidine 0.2 % Solution2.08USD ml
Pms-Brimonidine 0.2 % Solution2.08USD ml
Ratio-Brimonidine 0.2 % Solution2.08USD ml
Sandoz Brimonidine 0.2 % Solution2.08USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2173974 No2006-05-022014-09-19Canada
CA2225626 No2002-09-032016-06-17Canada
US5424078 No1995-06-132012-06-13Us
US6316441 No1999-12-072019-12-07Us
US6562873 Yes2002-01-102022-01-10Us
US6627210 Yes2002-01-182022-01-18Us
US6641834 Yes2002-01-282022-01-28Us
US6673337 Yes2002-01-262022-01-26Us
US7030149 No2002-04-192022-04-19Us
US7265117 No2005-08-192025-08-19Us
US7320976 No2002-04-192022-04-19Us
US7323463 No2003-01-192023-01-19Us
US7439241 No2005-08-252025-08-25Us
US7642258 No2002-04-192022-04-19Us
US8053427 No2011-06-132031-06-13Us
US8133890 No2002-04-192022-04-19Us
US8163725 No2011-06-132031-06-13Us
US8231885 No2005-05-242025-05-24Us
US8354409 No2002-04-192022-04-19Us
US8410102 No2005-05-242025-05-24Us
US8426410 No2005-05-242025-05-24Us
US8513247 No2011-03-252031-03-25Us
US8513249 No2011-03-252031-03-25Us
US8748425 No2002-04-192022-04-19Us
US8858961 Yes2004-03-022024-03-02Us
US8859551 No2004-05-252024-05-25Us
US9044484 No2010-10-302030-10-30Us
US9295641 No2001-07-102021-07-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point207.5 °CNot Available
water solubilitySoluble (1.5 mg/mL)Not Available
logP1.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.154 mg/mLALOGPS
logP1.27ALOGPS
logP1.37ChemAxon
logS-3.3ALOGPS
pKa (Strongest Basic)8.32ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area62.2 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity68.49 m3·mol-1ChemAxon
Polarizability25.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesD11AX21S01EA05
AHFS Codes
  • 52:92.00
PDB EntriesNot Available
FDA labelDownload (517 KB)
MSDSDownload (20.9 KB)
Interactions
Drug Interactions
Drug
AcebutololBrimonidine may increase the antihypertensive activities of Acebutolol.
AcetaminophenBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Acetaminophen.
Acetylsalicylic acidBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Acetylsalicylic acid.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Brimonidine.
AlfentanilBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
AliskirenBrimonidine may increase the antihypertensive activities of Aliskiren.
AlprazolamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
AmilorideBrimonidine may increase the antihypertensive activities of Amiloride.
AmitriptylineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.
AmlodipineBrimonidine may increase the antihypertensive activities of Amlodipine.
AmobarbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
AmoxapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
AripiprazoleBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Aripiprazole.
AsenapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
AtenololBrimonidine may increase the antihypertensive activities of Atenolol.
AtropineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Atropine.
AzelastineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Azilsartan medoxomilBrimonidine may increase the antihypertensive activities of Azilsartan medoxomil.
BaclofenBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
BenazeprilBrimonidine may increase the antihypertensive activities of Benazepril.
BendroflumethiazideBrimonidine may increase the antihypertensive activities of Bendroflumethiazide.
BetaxololBrimonidine may increase the antihypertensive activities of Betaxolol.
BisoprololBrimonidine may increase the antihypertensive activities of Bisoprolol.
BrexpiprazoleBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.
BromazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Bromazepam.
BrompheniramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Brompheniramine.
BumetanideBrimonidine may increase the antihypertensive activities of Bumetanide.
BuprenorphineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Buspirone.
ButabarbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
ButalbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
ButethalButethal may increase the hypotensive activities of Brimonidine.
ButorphanolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
CaffeineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Caffeine.
CandesartanBrimonidine may increase the antihypertensive activities of Candesartan.
CaptoprilBrimonidine may increase the antihypertensive activities of Captopril.
CarbamazepineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Carbamazepine.
CarbidopaBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Carbidopa.
CarbinoxamineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Carbinoxamine.
CarisoprodolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Carisoprodol.
CarvedilolBrimonidine may increase the antihypertensive activities of Carvedilol.
CetirizineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cetirizine.
ChlordiazepoxideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Chlordiazepoxide.
ChlorothiazideBrimonidine may increase the antihypertensive activities of Chlorothiazide.
ChlorphenamineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Chlorphenamine.
ChlorpromazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Chlorpromazine.
ChlorthalidoneBrimonidine may increase the antihypertensive activities of Chlorthalidone.
ChlorzoxazoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
CilazaprilBrimonidine may increase the antihypertensive activities of Cilazapril.
ClemastineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clemastine.
ClevidipineBrimonidine may increase the antihypertensive activities of Clevidipine.
ClidiniumBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clidinium.
ClobazamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
ClofedanolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clofedanol.
ClomipramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clomipramine.
ClonazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clonazepam.
ClonidineBrimonidine may increase the antihypertensive activities of Clonidine.
ClorazepateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
ClozapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
CodeineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Codeine.
CyclizineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.
CyclobenzaprineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyclobenzaprine.
CyproheptadineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
DantroleneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Dantrolene.
DesfluraneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Desflurane.
DesipramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Desipramine.
DesloratadineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
DexbrompheniramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Dexbrompheniramine.
Dexchlorpheniramine maleateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Dexchlorpheniramine maleate.
DiazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
DifenoxinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
DigoxinBrimonidine may increase the bradycardic activities of Digoxin.
DihydrocodeineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Dihydrocodeine.
DiltiazemBrimonidine may increase the antihypertensive activities of Diltiazem.
DimenhydrinateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
DiphenhydramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Diphenhydramine.
DiphenoxylateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Diphenoxylate.
DoxazosinBrimonidine may increase the antihypertensive activities of Doxazosin.
DoxepinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
DuloxetineBrimonidine may increase the orthostatic hypotensive activities of Duloxetine.
EfavirenzBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.
EnalaprilBrimonidine may increase the antihypertensive activities of Enalapril.
EnalaprilatBrimonidine may increase the antihypertensive activities of Enalaprilat.
EntacaponeBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
EplerenoneBrimonidine may increase the antihypertensive activities of Eplerenone.
EprosartanBrimonidine may increase the antihypertensive activities of Eprosartan.
EsmololBrimonidine may increase the antihypertensive activities of Esmolol.
EstazolamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
EszopicloneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Eszopiclone.
Etacrynic acidBrimonidine may increase the antihypertensive activities of Ethacrynic acid.
EthanolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthosuximideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ethosuximide.
EthotoinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ethotoin.
EzogabineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ezogabine.
FelbamateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Felbamate.
FelodipineBrimonidine may increase the antihypertensive activities of Felodipine.
FentanylBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fentanyl.
FexofenadineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fexofenadine.
FlibanserinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.
FlunarizineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
FlupentixolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
FluphenazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fluphenazine.
FlurazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flurazepam.
Fluticasone PropionateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fluticasone Propionate.
FosinoprilBrimonidine may increase the antihypertensive activities of Fosinopril.
FosphenytoinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
FurosemideBrimonidine may increase the antihypertensive activities of Furosemide.
GabapentinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.
gabapentin enacarbilBrimonidine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Gamma Hydroxybutyric AcidBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Gamma Hydroxybutyric Acid.
GuanfacineBrimonidine may increase the antihypertensive activities of Guanfacine.
HaloperidolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Haloperidol.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Brimonidine.
HexobarbitalHexobarbital may increase the hypotensive activities of Brimonidine.
HydralazineBrimonidine may increase the antihypertensive activities of Hydralazine.
HydrochlorothiazideBrimonidine may increase the antihypertensive activities of Hydrochlorothiazide.
HydrocodoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydromorphoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
IloperidoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
ImipramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Imipramine.
IndapamideBrimonidine may increase the antihypertensive activities of Indapamide.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Brimonidine.
IrbesartanBrimonidine may increase the antihypertensive activities of Irbesartan.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Brimonidine.
IsofluraneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Isoflurane.
IsradipineBrimonidine may increase the antihypertensive activities of Isradipine.
KetamineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ketamine.
LabetalolBrimonidine may increase the antihypertensive activities of Labetalol.
LamotrigineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
LevetiracetamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.
LevocabastineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
LevocetirizineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
LevodopaBrimonidine may increase the orthostatic hypotensive activities of Levodopa.
LevorphanolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levorphanol.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Brimonidine.
LisinoprilBrimonidine may increase the antihypertensive activities of Lisinopril.
LoratadineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Loratadine.
LorazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
LosartanBrimonidine may increase the antihypertensive activities of Losartan.
LoxapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
LurasidoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
MannitolBrimonidine may increase the antihypertensive activities of Mannitol.
MaprotilineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
MecamylamineBrimonidine may increase the antihypertensive activities of Mecamylamine.
MeclizineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
MeprobamateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
MetaxaloneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
MethadoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methadone.
MethocarbamolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
MethohexitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MethotrimeprazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethsuximideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methsuximide.
MethyclothiazideBrimonidine may increase the antihypertensive activities of Methyclothiazide.
MethyldopaBrimonidine may increase the antihypertensive activities of Methyldopa.
MetolazoneBrimonidine may increase the antihypertensive activities of Metolazone.
MetoprololBrimonidine may increase the antihypertensive activities of Metoprolol.
MetyrosineBrimonidine may increase the sedative activities of Metyrosine.
MianserinThe therapeutic efficacy of Brimonidine can be decreased when used in combination with Mianserin.
MidazolamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Midazolam.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
MinoxidilBrimonidine may increase the antihypertensive activities of Minoxidil.
MirtazapineMirtazapine may decrease the antihypertensive activities of Brimonidine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Brimonidine.
MoexiprilBrimonidine may increase the antihypertensive activities of Moexipril.
MorphineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
NadololBrimonidine may increase the antihypertensive activities of Nadolol.
NalbuphineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Nalbuphine.
NebivololBrimonidine may increase the antihypertensive activities of Nebivolol.
NicardipineBrimonidine may increase the antihypertensive activities of Nicardipine.
NicorandilNicorandil may increase the hypotensive activities of Brimonidine.
NifedipineBrimonidine may increase the antihypertensive activities of Nifedipine.
NimodipineBrimonidine may increase the antihypertensive activities of Nimodipine.
NisoldipineBrimonidine may increase the antihypertensive activities of Nisoldipine.
NitrazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.
NitroprussideBrimonidine may increase the antihypertensive activities of Nitroprusside.
Nitrous oxideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Nitrous oxide.
NortriptylineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.
OlanzapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
OlmesartanBrimonidine may increase the antihypertensive activities of Olmesartan.
OlopatadineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
OrphenadrineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.
OxycodoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.
OxymorphoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
PaliperidoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
ParaldehydeBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Paroxetine.
PenbutololBrimonidine may increase the antihypertensive activities of Penbutolol.
PentazocineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pentazocine.
PentobarbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
PerindoprilBrimonidine may increase the antihypertensive activities of Perindopril.
PerphenazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Perphenazine.
PethidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Brimonidine.
PhenobarbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
PhenoxybenzamineBrimonidine may increase the antihypertensive activities of Phenoxybenzamine.
PhentolamineBrimonidine may increase the antihypertensive activities of Phentolamine.
PhenytoinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Phenytoin.
PimozideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
PindololBrimonidine may increase the antihypertensive activities of Pindolol.
PipotiazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pipotiazine.
PizotifenBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pizotifen.
PomalidomideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pomalidomide.
PramipexoleBrimonidine may increase the sedative activities of Pramipexole.
PrazosinBrimonidine may increase the antihypertensive activities of Prazosin.
PregabalinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.
PrimidoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Brimonidine.
ProchlorperazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Prochlorperazine.
PromazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Promazine.
PromethazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Promethazine.
PropofolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Propofol.
PropranololBrimonidine may increase the antihypertensive activities of Propranolol.
ProtriptylineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.
QuazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Quazepam.
QuetiapineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.
QuinaprilBrimonidine may increase the antihypertensive activities of Quinapril.
RamelteonBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.
RamiprilBrimonidine may increase the antihypertensive activities of Ramipril.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Brimonidine.
RemifentanilBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Remifentanil.
ReserpineBrimonidine may increase the antihypertensive activities of Reserpine.
RisperidoneBrimonidine may increase the hypotensive activities of Risperidone.
RopiniroleBrimonidine may increase the sedative activities of Ropinirole.
RotigotineBrimonidine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Brimonidine.
ScopolamineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Scopolamine.
Scopolamine butylbromideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Scopolamine butylbromide.
SecobarbitalBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Brimonidine.
SevofluraneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Sevoflurane.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
SotalolBrimonidine may increase the antihypertensive activities of Sotalol.
SpironolactoneBrimonidine may increase the antihypertensive activities of Spironolactone.
StiripentolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
SufentanilBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.
SuvorexantBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
TasimelteonBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Brimonidine.
TelmisartanBrimonidine may increase the antihypertensive activities of Telmisartan.
TemazepamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Temazepam.
TerazosinBrimonidine may increase the antihypertensive activities of Terazosin.
TetrabenazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
ThalidomideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Thioridazine.
ThiothixeneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
TiagabineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tiagabine.
TimololBrimonidine may increase the antihypertensive activities of Timolol.
TizanidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
TolcaponeBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
TopiramateBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Topiramate.
TorasemideBrimonidine may increase the antihypertensive activities of Torasemide.
TramadolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
TrandolaprilBrimonidine may increase the antihypertensive activities of Trandolapril.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Brimonidine.
TriamtereneBrimonidine may increase the antihypertensive activities of Triamterene.
TriazolamBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Triazolam.
TrifluoperazineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
TrimipramineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Trimipramine.
TriprolidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Triprolidine.
ValsartanBrimonidine may increase the antihypertensive activities of Valsartan.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Brimonidine.
VerapamilBrimonidine may increase the antihypertensive activities of Verapamil.
VigabatrinBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
ZaleplonBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
ZiconotideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
ZiprasidoneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Ziprasidone.
ZolpidemBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZonisamideBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zonisamide.
ZopicloneBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
ZuclopenthixolBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Rauly I, Ailhaud M, Wurch T, Pauwels PJ: alpha(2A)-adrenoceptor: G(alphai1) protein-mediated pertussis toxin-resistant attenuation of G(s) coupling to the cyclic AMP pathway. Biochem Pharmacol. 2000 Jun 15;59(12):1531-8. [PubMed:10799649 ]
  2. Wikberg-Matsson A, Simonsen U: Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. [PubMed:11481271 ]
  3. Meana JJ, Barturen F, Garro MA, Garcia-Sevilla JA, Fontan A, Zarranz JJ: Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease. J Neurochem. 1992 May;58(5):1896-904. [PubMed:1373179 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed:14610637 ]
  2. Bohmann C, Schollmeyer P, Rump LC: Methoxamine inhibits noradrenaline release through activation of alpha 1- and alpha 2-adrenoceptors in rat isolated kidney: involvement of purines and prostaglandins. Naunyn Schmiedebergs Arch Pharmacol. 1993 Mar;347(3):273-9. [PubMed:8097565 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed:14610637 ]
  2. Orito K, Kishi M, Imaizumi T, Nakazawa T, Hashimoto A, Mori T, Kambe T: alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70. [PubMed:11606316 ]
  3. Zhang W, Ordway GA: The alpha2C-adrenoceptor modulates GABA release in mouse striatum. Brain Res Mol Brain Res. 2003 Apr 10;112(1-2):24-32. [PubMed:12670699 ]
  4. Prinster SC, Holmqvist TG, Hall RA: Alpha2C-adrenergic receptors exhibit enhanced surface expression and signaling upon association with beta2-adrenergic receptors. J Pharmacol Exp Ther. 2006 Sep;318(3):974-81. Epub 2006 Jun 6. [PubMed:16757535 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xanthine dehydrogenase activity
Specific Function:
Oxidase with broad substrate specificity, oxidizing aromatic azaheterocycles, such as N1-methylnicotinamide and N-methylphthalazinium, as well as aldehydes, such as benzaldehyde, retinal, pyridoxal, and vanillin. Plays a key role in the metabolism of xenobiotics and drugs containing aromatic azaheterocyclic substituents. Participates in the bioactivation of prodrugs such as famciclovir, catalyz...
Gene Name:
AOX1
Uniprot ID:
Q06278
Molecular Weight:
147916.735 Da
References
  1. Acheampong AA, Chien DS, Lam S, Vekich S, Breau A, Usansky J, Harcourt D, Munk SA, Nguyen H, Garst M, Tang-Liu D: Characterization of brimonidine metabolism with rat, rabbit, dog, monkey and human liver fractions and rabbit liver aldehyde oxidase. Xenobiotica. 1996 Oct;26(10):1035-55. [PubMed:8905918 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on June 24, 2016 03:04