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Identification
NameLevocabastine
Accession NumberDB01106  (APRD01069)
TypeSmall Molecule
GroupsApproved
DescriptionLevocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.
Structure
Thumb
Synonyms
Levocabastin
Levocabastina
Levocabastinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Livostin Eye Dropsdrops; suspension0.5 mgophthalmicNovartis Pharmaceuticals Canada Inc1995-12-312011-06-27Canada
Livostin Sus Nas 0.5mg/mlsuspension; spray0.5 mgnasalJanssen Inc1993-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LivostinNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Levocabastine hydrochloride
79547-78-7
Thumb
  • InChI Key: OICFWWJHIMKBCD-VALQNVSPSA-N
  • Monoisotopic Mass: 456.1979841
  • Average Mass: 456.99
DBSALT001442
Categories
UNIIH68BP06S81
CAS number79516-68-0
WeightAverage: 420.528
Monoisotopic: 420.221306345
Chemical FormulaC26H29FN2O2
InChI KeyZCGOMHNNNFPNMX-KYTRFIICSA-N
InChI
InChI=1S/C26H29FN2O2/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)/t19-,23-,25-,26-/m1/s1
IUPAC Name
(3S,4R)-3-methyl-4-phenyl-1-[(1s,4s)-4-cyano-4-(4-fluorophenyl)cyclohexyl]piperidine-4-carboxylic acid
SMILES
C[C@@H]1CN(CC[C@]1(C(O)=O)C1=CC=CC=C1)[[email protected]]1CC[C@](CC1)(C#N)C1=CC=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassPhenylpiperidines
Direct ParentPhenylpiperidines
Alternative Parents
Substituents
  • Phenylpiperidine
  • Piperidinecarboxylic acid
  • Cyclohexylamine
  • Fluorobenzene
  • Aralkylamine
  • Halobenzene
  • Aryl fluoride
  • Aryl halide
  • Monocyclic benzene moiety
  • Benzenoid
  • Amino acid or derivatives
  • Amino acid
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid derivative
  • Carboxylic acid
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carbonitrile
  • Nitrile
  • Organooxygen compound
  • Hydrocarbon derivative
  • Organic nitrogen compound
  • Amine
  • Carbonyl group
  • Organic oxygen compound
  • Cyanide
  • Organic oxide
  • Organohalogen compound
  • Organofluoride
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationAs an ophthalmic for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis. Also used as a nasal spray for allergic rhinitis.
PharmacodynamicsLevocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. Both histamine and antigens induced conjunctivitis can be inhibited by levocabastine. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa.
Mechanism of actionLevocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
Related Articles
AbsorptionAfter instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Mostly unchanged. 10 to 20% is metabolized to the acylglucuronide of levocabastine.

Route of eliminationNot Available
Half life36 hours (after oral administration)
ClearanceNot Available
ToxicityAdverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.
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+0.9811
Blood Brain Barrier+0.8388
Caco-2 permeable+0.5747
P-glycoprotein substrateSubstrate0.7325
P-glycoprotein inhibitor IInhibitor0.5
P-glycoprotein inhibitor IINon-inhibitor0.5682
Renal organic cation transporterNon-inhibitor0.5526
CYP450 2C9 substrateNon-substrate0.7708
CYP450 2D6 substrateNon-substrate0.6679
CYP450 3A4 substrateSubstrate0.5153
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9046
Ames testNon AMES toxic0.7503
CarcinogenicityNon-carcinogens0.9196
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9608 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9404
hERG inhibition (predictor II)Inhibitor0.625
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Drops; suspensionophthalmic0.5 mg
Suspension; spraynasal0.5 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility>0.5 mg/mLNot Available
logP5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00347 mg/mLALOGPS
logP4.56ALOGPS
logP2.5ChemAxon
logS-5.1ALOGPS
pKa (Strongest Acidic)3.71ChemAxon
pKa (Strongest Basic)10.32ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area64.33 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity118.48 m3·mol-1ChemAxon
Polarizability45.58 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 ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR01AC02S01GX02
AHFS Codes
  • 52:02.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Levocabastine.
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Levocabastine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Levocabastine.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Levocabastine.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Levocabastine.
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Levocabastine.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Levocabastine.
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Levocabastine.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Levocabastine.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Levocabastine.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Levocabastine.
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Levocabastine.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocabastine.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Levocabastine.
AmoxapineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Levocabastine.
AmphetamineAmphetamine may decrease the sedative activities of Levocabastine.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Levocabastine.
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Levocabastine.
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine.
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Levocabastine.
AzelastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Levocabastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Levocabastine.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Levocabastine.
BenzphetamineBenzphetamine may decrease the sedative activities of Levocabastine.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Levocabastine.
Benzylpenicilloyl PolylysineLevocabastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Levocabastine.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Levocabastine is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
BrimonidineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Levocabastine.
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Levocabastine.
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Levocabastine.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Levocabastine.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Levocabastine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Levocabastine.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Levocabastine.
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Levocabastine.
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Levocabastine.
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Levocabastine.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Levocabastine.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Levocabastine.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Levocabastine.
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Levocabastine.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Levocabastine.
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Levocabastine.
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Levocabastine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Levocabastine.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Levocabastine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Levocabastine.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Levocabastine.
ChlorphenamineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Chlorphenamine.
ChlorphentermineChlorphentermine may decrease the sedative activities of Levocabastine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Levocabastine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Levocabastine.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Levocabastine.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Levocabastine.
CitalopramThe risk or severity of adverse effects can be increased when Levocabastine is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Levocabastine.
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Levocabastine.
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Levocabastine.
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Levocabastine.
ClomipramineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Levocabastine.
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Levocabastine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Levocabastine.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Levocabastine.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Levocabastine.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Levocabastine.
CyclizineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Levocabastine.
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocabastine.
DantroleneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Levocabastine.
DapoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Dapoxetine.
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Levocabastine.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Levocabastine.
DesipramineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Levocabastine.
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Levocabastine.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Levocabastine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Levocabastine.
DextroamphetamineDextroamphetamine may decrease the sedative activities of Levocabastine.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Levocabastine.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Levocabastine.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Levocabastine.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Levocabastine.
DifenoxinThe risk or severity of adverse effects can be increased when Levocabastine is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Levocabastine.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Levocabastine.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Levocabastine.
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Levocabastine.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Levocabastine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Levocabastine.
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Levocabastine.
DoxepinThe risk or severity of adverse effects can be increased when Levocabastine is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
DoxylamineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Levocabastine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Levocabastine.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Levocabastine.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Levocabastine.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Levocabastine.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Levocabastine.
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Levocabastine.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Levocabastine.
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Levocabastine.
EscitalopramThe risk or severity of adverse effects can be increased when Levocabastine is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Levocabastine.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Levocabastine.
EthanolLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Levocabastine.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Levocabastine.
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Levocabastine.
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Levocabastine.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Levocabastine.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Levocabastine.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Levocabastine.
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Levocabastine.
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Levocabastine.
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Levocabastine.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Levocabastine.
EtoperidoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Levocabastine.
EzogabineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Levocabastine.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Levocabastine.
FenfluramineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Levocabastine.
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Levocabastine.
FlibanserinThe risk or severity of adverse effects can be increased when Levocabastine is combined with Flibanserin.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocabastine.
FlunarizineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocabastine.
FluoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Levocabastine.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Levocabastine.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Levocabastine.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Levocabastine.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Levocabastine.
FluvoxamineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Levocabastine is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levocabastine.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Levocabastine.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Levocabastine is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Levocabastine.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Levocabastine.
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Levocabastine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Levocabastine.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Levocabastine.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Levocabastine.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Levocabastine.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Levocabastine.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Levocabastine.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Levocabastine.
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Levocabastine.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
HydroxyzineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Levocabastine.
IndalpineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Levocabastine.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Levocabastine.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Levocabastine.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Levocabastine.
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Levocabastine.
LevetiracetamThe risk or severity of adverse effects can be increased when Levocabastine is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Levocabastine is combined with Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Levocabastine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levocabastine is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Levocabastine.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Levocabastine.
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Levocabastine.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Levocabastine.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Levocabastine.
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Levocabastine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Levocabastine.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Levocabastine.
Lu AA21004The risk or severity of adverse effects can be increased when Levocabastine is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Levocabastine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Levocabastine is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Levocabastine.
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Levocabastine.
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Levocabastine.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Levocabastine.
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Levocabastine.
MephentermineMephentermine may decrease the sedative activities of Levocabastine.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Levocabastine.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Levocabastine.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Levocabastine.
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Levocabastine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Levocabastine.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Levocabastine.
MethamphetamineMethamphetamine may decrease the sedative activities of Levocabastine.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Levocabastine.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Levocabastine.
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Levocabastine.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Levocabastine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Levocabastine.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Levocabastine.
MethsuximideThe risk or severity of adverse effects can be increased when Levocabastine is combined with Methsuximide.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Levocabastine.
MetyrosineLevocabastine may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine.
MilnacipranThe risk or severity of adverse effects can be increased when Levocabastine is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
MirtazapineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Levocabastine.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Levocabastine.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Levocabastine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.
NabiloneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Levocabastine.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Levocabastine.
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Levocabastine.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Levocabastine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Levocabastine.
OlanzapineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Levocabastine.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Levocabastine.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Levocabastine.
OrphenadrineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Levocabastine.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Levocabastine.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Levocabastine.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Levocabastine.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Levocabastine.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Levocabastine.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Levocabastine.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Levocabastine.
ParaldehydeLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with Levocabastine.
ParoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Levocabastine.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Levocabastine.
PerampanelThe risk or severity of adverse effects can be increased when Levocabastine is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Levocabastine.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Levocabastine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Levocabastine.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Levocabastine.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Levocabastine.
PhenterminePhentermine may decrease the sedative activities of Levocabastine.
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Levocabastine.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Levocabastine.
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Levocabastine.
PipotiazineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Levocabastine is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Levocabastine is combined with Pomalidomide.
PramipexoleLevocabastine may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Levocabastine.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Levocabastine.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Levocabastine.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Levocabastine.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Levocabastine.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Levocabastine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Levocabastine.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Levocabastine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Levocabastine.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Levocabastine.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Levocabastine.
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Levocabastine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Levocabastine.
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Levocabastine.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Levocabastine.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Levocabastine.
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Levocabastine.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Levocabastine.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Levocabastine.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Levocabastine.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Levocabastine.
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Levocabastine.
RopiniroleLevocabastine may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Levocabastine.
RotigotineLevocabastine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levocabastine.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Levocabastine.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Levocabastine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Levocabastine.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Levocabastine.
SertralineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Levocabastine.
Sodium oxybateThe risk or severity of adverse effects can be increased when Sodium oxybate is combined with Levocabastine.
StiripentolThe risk or severity of adverse effects can be increased when Levocabastine is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Levocabastine.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Levocabastine.
SuvorexantThe risk or severity of adverse effects can be increased when Levocabastine is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Levocabastine is combined with Tapentadol.
TasimelteonThe risk or severity of adverse effects can be increased when Levocabastine is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Levocabastine.
TetrabenazineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Tetrabenazine.
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Levocabastine.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Levocabastine.
ThalidomideLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Levocabastine.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Levocabastine.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Levocabastine.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Levocabastine.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Levocabastine.
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Levocabastine.
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Levocabastine.
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Levocabastine.
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Levocabastine.
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Levocabastine.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Levocabastine.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Levocabastine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Levocabastine.
TrazodoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Levocabastine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Levocabastine.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Levocabastine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Levocabastine.
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Levocabastine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Levocabastine.
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Levocabastine.
VilazodoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Levocabastine.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Levocabastine.
ZiconotideThe risk or severity of adverse effects can be increased when Levocabastine is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Levocabastine.
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Levocabastine.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Levocabastine.
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Levocabastine.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Levocabastine.
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Levocabastine.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Levocabastine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial antagonist
General Function:
G-protein coupled receptor activity
Specific Function:
Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
NTSR2
Uniprot ID:
O95665
Molecular Weight:
45384.635 Da
References
  1. Richard F, Barroso S, Martinez J, Labbe-Jullie C, Kitabgi P: Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2. Mol Pharmacol. 2001 Dec;60(6):1392-8. [PubMed:11723247 ]
  2. Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D: Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 1996 May 20;386(2-3):91-4. [PubMed:8647296 ]
  3. Botto JM, Guillemare E, Vincent JP, Mazella J: Effects of SR 48692 on neurotensin-induced calcium-activated chloride currents in the Xenopus oocyte expression system: agonist-like activity on the levocabastine-sensitive neurotensin receptor and absence of antagonist effect on the levocabastine insensitive neurotensin receptor. Neurosci Lett. 1997 Feb 28;223(3):193-6. [PubMed:9080465 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 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. Sugimoto Y, Iba Y, Ishizawa K, Suzuki G, Kamei C: Effects of levocabastine on lipid mediator release from guinea pig lung fragments. Acta Med Okayama. 1999 Dec;53(6):271-4. [PubMed:10631382 ]
  3. Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D: Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 1996 May 20;386(2-3):91-4. [PubMed:8647296 ]
  4. Yamada M, Yamada M, Lombet A, Forgez P, Rostene W: Distinct functional characteristics of levocabastine sensitive rat neurotensin NT2 receptor expressed in Chinese hamster ovary cells. Life Sci. 1998;62(23):PL 375-80. [PubMed:9627096 ]
  5. Betancur C, Canton M, Burgos A, Labeeuw B, Gully D, Rostene W, Pelaprat D: Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain. Eur J Pharmacol. 1998 Feb 5;343(1):67-77. [PubMed:9551716 ]
  6. Akiyoshi M, Shigeoka T, Torii S, Maki E, Enomoto S, Takahashi H, Hirano F: [Pharmacological and clinical properties of levocabastine hydrochloride (eye drop and nasal spray), a selective H1 antagonist]. Nihon Yakurigaku Zasshi. 2002 Mar;119(3):175-84. [PubMed:11915520 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23