You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameAzelastine
Accession NumberDB00972  (APRD00813)
TypeSmall Molecule
GroupsApproved
Description

Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis.

Structure
Thumb
Synonyms
4-(P-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone
Azelastina
Azelastinum
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Astelinspray, metered137 ug/1nasalMeda Pharmaceuticals Inc.1996-11-152016-11-30Us 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Astelinspray, metered137 ug/1nasalPhysicians Total Care, Inc.2004-05-25Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Asteprospray, metered205.5 ug/1nasalMeda Pharmaceuticals Inc.2009-10-12Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridesolution/ drops.5 mg/mLintraocularWallace Pharmaceuticals Inc.2010-10-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/1nasalWallace Pharmaceuticals Inc.2010-07-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered205.5 ug/1nasalWallace Pharmaceuticals Inc.2015-04-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered205.5 ug/1nasalPerrigo New York Inc2015-04-09Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Optivarsolution/ drops.5 mg/mLintraocularMeda Pharmaceuticals Inc.2000-05-22Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Azelastine HCl Nasalspray205.5 ug/1nasalPerrigo New York Inc2014-05-09Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/1nasalRoxane Laboratories, Inc.2014-10-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/1nasalApotex Corp.2010-03-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridesolution/ drops.5 mg/mLintraocularApotex Corp.2009-12-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/1nasalPhysicians Total Care, Inc.2011-06-28Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/.137mLnasalBreckenridge Pharmaceutical, Inc.2015-07-29Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridesolution/ drops.5 mg/mLintraocularSun Pharma Global FZE2010-05-31Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered137 ug/1nasalSun Pharma Global FZE2012-05-24Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridesolution/ drops.5 mg/mLintraocularSandoz Inc2013-03-21Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Azelastine Hydrochloridespray, metered205.5 ug/1nasalApotex Corp.2014-07-07Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
DymistaMeda Pharmaceuticals Inc.
Salts
Name/CASStructureProperties
Azelastine Hydrochloride
79307-93-0
Thumb
  • InChI Key: YEJAJYAHJQIWNU-UHFFFAOYNA-N
  • Monoisotopic Mass: 417.137467851
  • Average Mass: 418.359
DBSALT000013
Categories
CAS number58581-89-8
WeightAverage: 381.898
Monoisotopic: 381.160790112
Chemical FormulaC22H24ClN3O
InChI KeyInChIKey=MBUVEWMHONZEQD-UHFFFAOYSA-N
InChI
InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3
IUPAC Name
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
SMILES
CN1CCCC(CC1)N1N=C(CC2=CC=C(Cl)C=C2)C2=CC=CC=C2C1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phthalazinones. These are compounds containing a phthalazine bearing a ketone group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassPhthalazines
Direct ParentPhthalazinones
Alternative Parents
Substituents
  • Phthalazinone
  • Pyridazinone
  • Halobenzene
  • Chlorobenzene
  • Azepane
  • Benzenoid
  • Pyridazine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactam
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis.
PharmacodynamicsAzelastine is a relatively selective histamine H1 antagonist, which inhibits the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. It has some affinity to H2 receptors. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine. Azelastine may also inhibit the accumulation and degranulation of eosinophils at the site of allergic inflammation.
Mechanism of actionAzelastine competes with histamine for the H1-receptor sites on effector cells and acts as an antagonist by inhibiting the release of histamine and other mediators involved in the allergic response.
AbsorptionAbsorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
Volume of distribution
  • 14.5 L/kg
Protein bindingIn-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively.
Metabolism

Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.

SubstrateEnzymesProduct
Azelastine
DesmethylazelastineDetails
Route of eliminationApproximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system.
Half lifeElimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine).
Clearance
  • 0.5 L/h/kg [symptomatic patients]
ToxicityNot Available
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+1.0
Blood Brain Barrier+0.982
Caco-2 permeable-0.5102
P-glycoprotein substrateSubstrate0.7034
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.9563
Renal organic cation transporterInhibitor0.6812
CYP450 2C9 substrateNon-substrate0.7501
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.8204
CYP450 1A2 substrateInhibitor0.6371
CYP450 2C9 inhibitorNon-inhibitor0.8114
CYP450 2D6 inhibitorNon-inhibitor0.568
CYP450 2C19 inhibitorNon-inhibitor0.6934
CYP450 3A4 inhibitorNon-inhibitor0.5902
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7266
Ames testNon AMES toxic0.6567
CarcinogenicityNon-carcinogens0.878
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0597 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7885
hERG inhibition (predictor II)Inhibitor0.7391
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Apotex inc richmond hill
  • Sun pharma global fze
  • Meda pharmaceuticals inc
  • Meda pharmaceuticals meda pharmaceuticals inc
  • Apotex inc
  • Meda pharmaceuticals
Packagers
Dosage forms
FormRouteStrength
Spray, meterednasal137 ug/1
Spray, meterednasal205.5 ug/1
Spraynasal205.5 ug/1
Spray, meterednasal137 ug/.137mL
Spray, meterednasal
Spray, metered dosenasal
Solution/ dropsintraocular.5 mg/mL
Prices
Unit descriptionCostUnit
Optivar 0.05% Solution 6ml Bottle120.26USD bottle
Astelin 137 mcg/spray Solution 30ml Bottle117.27USD bottle
Azelastine HCl 0.05% Solution 6ml Bottle108.23USD bottle
Optivar 0.05% drops19.27USD ml
Azelastine hcl 0.05% drops17.35USD ml
Astelin 137 mcg nasal spray3.71USD ml
Astepro 137 mcg nasal spray3.61USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States51641941994-05-012011-05-01
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point225 °C (hydrochloride salt)Not Available
water solubilitySparingly soluble (hydrochloride salt)Not Available
logP4.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0092 mg/mLALOGPS
logP3.81ALOGPS
logP4.04ChemAxon
logS-4.6ALOGPS
pKa (Strongest Basic)8.88ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area35.91 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity110.52 m3·mol-1ChemAxon
Polarizability41.54 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

Yutaka Morita, Noritoshi Koyama, Shigemitsu Ohsawa, “Methods employing stable preparation containing azelastine hydrochloride.” U.S. Patent US6117864, issued December, 1990.

US6117864
General References
  1. Horak F: Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Ther Clin Risk Manag. 2008 Oct;4(5):1009-22. Pubmed
  2. Bernstein JA: Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Curr Med Res Opin. 2007 Oct;23(10):2441-52. Pubmed
External Links
ATC CodesR01AC03R06AX19S01GX07
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (17.5 KB)
MSDSDownload (36.8 KB)
Interactions
Drug Interactions
Drug
AcetaminophenAcetaminophen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Acetylsalicylic acidAcetylsalicylic acid may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AclidiniumAclidinium may increase the anticholinergic activities of Azelastine.
AlfentanilAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AmitriptylineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AmoxapineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AmphetamineAmphetamine may decrease the sedative activities of Azelastine.
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AtropineAtropine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Benzylpenicilloyl PolylysineAzelastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Azelastine.
Botulinum Toxin Type AAzelastine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BAzelastine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrexpiprazoleBrexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BuprenorphineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BuspironeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ButalbitalButalbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CaffeineCaffeine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CarbidopaCarbidopa may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CathinoneCathinone may decrease the sedative activities of Azelastine.
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Cimetropium BromideAzelastine may increase the anticholinergic activities of Cimetropium Bromide.
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClidiniumClidinium may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClofedanolClofedanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClomipramineClomipramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CodeineCodeine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CyclobenzaprineCyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DesipramineDesipramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DexbrompheniramineDexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DifenoxinDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DihydrocodeineDihydrocodeine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DiphenoxylateDiphenoxylate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DoxepinDoxepin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EfavirenzEfavirenz may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EluxadolineAzelastine may increase the activities of Eluxadoline.
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FentanylFentanyl may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
gabapentin enacarbilgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Azelastine is combined with Glucagon recombinant.
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Azelastine.
HydrocodoneHydrocodone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
HydromorphoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
IloperidoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ImipramineImipramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Azelastine.
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Azelastine.
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LevocabastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LevodopaLevodopa may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LevorphanolLevorphanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MaprotilineMaprotiline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MethadoneMethadone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MethotrimeprazineMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MetyrosineAzelastine may increase the sedative activities of Metyrosine.
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MirabegronThe risk or severity of adverse effects can be increased when Azelastine is combined with Mirabegron.
MirtazapineMirtazapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
MorphineMorphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
NelfinavirThe serum concentration of Azelastine can be increased when it is combined with Nelfinavir.
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
NortriptylineNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
OrphenadrineAzelastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
OxycodoneOxycodone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
OxymorphoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ParaldehydeAzelastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Azelastine is combined with Paroxetine.
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PethidinePethidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PimozidePimozide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Potassium ChlorideAzelastine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleAzelastine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Azelastine.
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Azelastine.
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PromethazinePromethazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ProtriptylineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
RamosetronAzelastine may increase the activities of Ramosetron.
RemifentanilRemifentanil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
RopiniroleAzelastine may increase the sedative activities of Ropinirole.
RotigotineAzelastine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Azelastine.
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Scopolamine butylbromideScopolamine butylbromide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Azelastine.
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
StiripentolStiripentol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
SufentanilSufentanil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Azelastine.
SuvorexantSuvorexant may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TacrineThe therapeutic efficacy of Azelastine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TetrabenazineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ThalidomideAzelastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThioridazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TiotropiumAzelastine may increase the anticholinergic activities of Tiotropium.
TizanidineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TramadolTramadol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Azelastine.
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TrimipramineTrimipramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Azelastine.
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZolpidemZolpidem may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Food InteractionsNot Available

Targets

1. Histamine H1 receptor

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Histamine H1 receptor P35367 Details

References:

  1. Casale TB: The interaction of azelastine with human lung histamine H1, beta, and muscarinic receptor-binding sites. J Allergy Clin Immunol. 1989 Apr;83(4):771-6. Pubmed
  2. Conde Hernandez DJ, Palma Aqilar JL, Delgado Romero J: Comparison of azelastine nasal spray and oral ebastine in treating seasonal allergic rhinitis. Curr Med Res Opin. 1995;13(6):299-304. Pubmed
  3. Antepara I, Jauregui I, Basomba A, Cadahia A, Feo F, Garcia JJ, Gonzalo MA, Luna I, Rubio M, Vazquez M: [Investigation of the efficacy and tolerability of azelastine nasal spray versus ebastine tablets in patients with seasonal allergic rhinitis] Allergol Immunopathol (Madr). 1998 Jan-Feb;26(1):9-16. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  5. Horak F: Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Ther Clin Risk Manag. 2008 Oct;4(5):1009-22. Pubmed
  6. Bernstein JA: Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Curr Med Res Opin. 2007 Oct;23(10):2441-52. Pubmed
  7. Golden SJ, Craig TJ: Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. J Am Osteopath Assoc. 1999 Jul;99(7 Suppl):S7-12. Pubmed

Enzymes

1. Cytochrome P450 1A2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2D6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C19

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 1A1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

6. Cytochrome P450 3A5

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

7. Cytochrome P450 2C9

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2C8

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

9. Cytochrome P450 2A6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

References:

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

10. Cytochrome P450 2B6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

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

11. Cytochrome P450 2E1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

References:

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

Transporters

1. Multidrug resistance protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. Pubmed
  2. Hu YP, Robert J: Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies. Biochem Pharmacol. 1995 Jul 17;50(2):169-75. Pubmed

Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12