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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyLevocabastine
Identification
- Name
- Levocabastine
- Accession Number
- DB01106 (APRD01069)
- Type
- Small Molecule
- Groups
- Approved
- Description
Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.
- Structure
Structure for DB01106 (Levocabastine)
- Synonyms
- Levocabastin
- Levocabastina
- Levocabastinum
- Product Ingredients
Ingredient UNII CAS InChI Key Levocabastine hydrochloride 124XMA6YEI 79547-78-7 OICFWWJHIMKBCD-VALQNVSPSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Livostin Eye Drops Solution / drops; Suspension 0.5 mg Ophthalmic Novartis 1995-12-31 2011-06-27 Canada 
Livostin Sus Nas 0.5mg/ml Spray; Suspension 0.5 mg Nasal Janssen Pharmaceuticals 1993-12-31 Not applicable Canada - International/Other Brands
- Livostin
- Categories
- UNII
- H68BP06S81
- CAS number
- 79516-68-0
- Weight
- Average: 420.528
Monoisotopic: 420.221306345 - Chemical Formula
- C26H29FN2O2
- InChI Key
- ZCGOMHNNNFPNMX-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[[email protected]@H]1CN(CC[[email protected]]1(C(O)=O)C1=CC=CC=C1)[[email protected]]1CC[[email protected]](CC1)(C#N)C1=CC=C(F)C=C1
Pharmacology
- Indication
As an ophthalmic for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis. Also used as a nasal spray for allergic rhinitis.
- Structured Indications
- Pharmacodynamics
Levocabastine 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 action
Levocabastine 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.
Target Actions Organism AHistamine H1 receptor antagonistHuman ANeurotensin receptor type 2 partial antagonistHuman - Absorption
After instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
Mostly unchanged. 10 to 20% is metabolized to the acylglucuronide of levocabastine.
- Route of elimination
- Not Available
- Half life
36 hours (after oral administration)
- Clearance
- Not Available
- Toxicity
Adverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Levocabastine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group 2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Levocabastine. Experimental, Illicit 3,4-Methylenedioxyamphetamine 3,4-Methylenedioxyamphetamine may decrease the sedative activities of Levocabastine. Experimental, Illicit 4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Levocabastine. Experimental, Illicit 7-Nitroindazole The risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Levocabastine. Experimental Acepromazine The risk or severity of adverse effects can be increased when Acepromazine is combined with Levocabastine. Approved, Vet Approved Aceprometazine The risk or severity of adverse effects can be increased when Aceprometazine is combined with Levocabastine. Approved Adipiplon The risk or severity of adverse effects can be increased when Adipiplon is combined with Levocabastine. Investigational Agomelatine The risk or severity of adverse effects can be increased when Agomelatine is combined with Levocabastine. Approved, Investigational Alaproclate The risk or severity of adverse effects can be increased when Levocabastine is combined with Alaproclate. Experimental Alfaxalone The risk or severity of adverse effects can be increased when Alfaxalone is combined with Levocabastine. Vet Approved Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Levocabastine. Approved, Illicit Allopregnanolone The risk or severity of adverse effects can be increased when Allopregnanolone is combined with Levocabastine. Investigational Alphacetylmethadol The risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Levocabastine. Experimental, Illicit Alphaprodine The risk or severity of adverse effects can be increased when Alphaprodine is combined with Levocabastine. Illicit Alprazolam The risk or severity of adverse effects can be increased when Alprazolam is combined with Levocabastine. Approved, Illicit, Investigational Amisulpride The risk or severity of adverse effects can be increased when Amisulpride is combined with Levocabastine. Approved, Investigational Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocabastine. Approved Amobarbital The risk or severity of adverse effects can be increased when Amobarbital is combined with Levocabastine. Approved, Illicit Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Levocabastine. Approved Amperozide The risk or severity of adverse effects can be increased when Amperozide is combined with Levocabastine. Experimental Amphetamine Amphetamine may decrease the sedative activities of Levocabastine. Approved, Illicit Aripiprazole The risk or severity of adverse effects can be increased when Aripiprazole is combined with Levocabastine. Approved, Investigational Articaine The risk or severity of adverse effects can be increased when Articaine is combined with Levocabastine. Approved Asenapine The risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine. Approved Azaperone The risk or severity of adverse effects can be increased when Azaperone is combined with Levocabastine. Vet Approved Azelastine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine. Approved Baclofen The risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine. Approved Barbital The risk or severity of adverse effects can be increased when Barbital is combined with Levocabastine. Illicit Benperidol The risk or severity of adverse effects can be increased when Benperidol is combined with Levocabastine. Investigational Benzocaine The risk or severity of adverse effects can be increased when Benzocaine is combined with Levocabastine. Approved Benzphetamine Benzphetamine may decrease the sedative activities of Levocabastine. Approved, Illicit Benzyl alcohol The risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Levocabastine. Approved Benzylpenicilloyl Polylysine Levocabastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent. Approved Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Levocabastine. Approved Brexpiprazole The risk or severity of adverse effects can be increased when Brexpiprazole is combined with Levocabastine. Approved Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved Bromazepam The risk or severity of adverse effects can be increased when Bromazepam is combined with Levocabastine. Approved, Illicit Bromisoval The risk or severity of adverse effects can be increased when Bromisoval is combined with Levocabastine. Experimental Bromperidol The risk or severity of adverse effects can be increased when Bromperidol is combined with Levocabastine. Investigational Brompheniramine The risk or severity of adverse effects can be increased when Brompheniramine is combined with Levocabastine. Approved Brotizolam The risk or severity of adverse effects can be increased when Brotizolam is combined with Levocabastine. Approved, Withdrawn Bupivacaine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Levocabastine. Approved, Investigational Buprenorphine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The risk or severity of adverse effects can be increased when Buspirone is combined with Levocabastine. Approved, Investigational Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Levocabastine. Approved, Illicit Butacaine The risk or severity of adverse effects can be increased when Butacaine is combined with Levocabastine. Vet Approved Butalbital The risk or severity of adverse effects can be increased when Butalbital is combined with Levocabastine. Approved, Illicit Butamben The risk or severity of adverse effects can be increased when Butamben is combined with Levocabastine. Approved Butethal The risk or severity of adverse effects can be increased when Butethal is combined with Levocabastine. Approved, Illicit Butorphanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Levocabastine. Approved, Illicit, Vet Approved Canertinib The risk or severity of adverse effects can be increased when Canertinib is combined with Levocabastine. Investigational Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Levocabastine. Approved, Investigational Carbinoxamine The risk or severity of adverse effects can be increased when Carbinoxamine is combined with Levocabastine. Approved Carfentanil The risk or severity of adverse effects can be increased when Carfentanil is combined with Levocabastine. Illicit, Vet Approved Carisoprodol The risk or severity of adverse effects can be increased when Carisoprodol is combined with Levocabastine. Approved Cetirizine The risk or severity of adverse effects can be increased when Cetirizine is combined with Levocabastine. Approved Chloral hydrate The risk or severity of adverse effects can be increased when Chloral hydrate is combined with Levocabastine. Approved, Illicit, Vet Approved Chlordiazepoxide The risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Levocabastine. Approved, Illicit Chlormezanone The risk or severity of adverse effects can be increased when Chlormezanone is combined with Levocabastine. Approved, Withdrawn Chloroprocaine The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Levocabastine. Approved Chlorphenamine The risk or severity of adverse effects can be increased when Chlorphenamine is combined with Levocabastine. Approved Chlorphentermine Chlorphentermine may decrease the sedative activities of Levocabastine. Illicit, Withdrawn Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Levocabastine. Approved, Vet Approved Chlorprothixene The risk or severity of adverse effects can be increased when Chlorprothixene is combined with Levocabastine. Approved, Withdrawn Chlorzoxazone The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Levocabastine. Approved Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levocabastine. Approved, Vet Approved Citalopram The risk or severity of adverse effects can be increased when Levocabastine is combined with Citalopram. Approved Clemastine The risk or severity of adverse effects can be increased when Clemastine is combined with Levocabastine. Approved Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Levocabastine. Approved Clobazam The risk or severity of adverse effects can be increased when Clobazam is combined with Levocabastine. Approved, Illicit clomethiazole The risk or severity of adverse effects can be increased when clomethiazole is combined with Levocabastine. Investigational Clomipramine The risk or severity of adverse effects can be increased when Clomipramine is combined with Levocabastine. Approved, Vet Approved Clonazepam The risk or severity of adverse effects can be increased when Clonazepam is combined with Levocabastine. Approved, Illicit Clonidine The risk or severity of adverse effects can be increased when Clonidine is combined with Levocabastine. Approved Clopenthixol The risk or severity of adverse effects can be increased when Clopenthixol is combined with Levocabastine. Experimental Clorazepate The risk or severity of adverse effects can be increased when Clorazepate is combined with Levocabastine. Approved, Illicit Clothiapine The risk or severity of adverse effects can be increased when Clothiapine is combined with Levocabastine. Experimental Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Levocabastine. Approved Cocaine The risk or severity of adverse effects can be increased when Cocaine is combined with Levocabastine. Approved, Illicit Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Levocabastine. Approved, Illicit Cyclizine The risk or severity of adverse effects can be increased when Cyclizine is combined with Levocabastine. Approved Cyclobenzaprine The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Levocabastine. Approved Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocabastine. Approved Dantrolene The risk or severity of adverse effects can be increased when Dantrolene is combined with Levocabastine. Approved Dapiprazole The risk or severity of adverse effects can be increased when Dapiprazole is combined with Levocabastine. Approved Dapoxetine The risk or severity of adverse effects can be increased when Levocabastine is combined with Dapoxetine. Investigational Deramciclane The risk or severity of adverse effects can be increased when Deramciclane is combined with Levocabastine. Investigational Desflurane The risk or severity of adverse effects can be increased when Desflurane is combined with Levocabastine. Approved Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Levocabastine. Approved Desloratadine The risk or severity of adverse effects can be increased when Desloratadine is combined with Levocabastine. Approved, Investigational Desvenlafaxine The risk or severity of adverse effects can be increased when Levocabastine is combined with Desvenlafaxine. Approved Detomidine The risk or severity of adverse effects can be increased when Detomidine is combined with Levocabastine. Vet Approved Dexbrompheniramine The risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Levocabastine. Approved Dexmedetomidine The risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Levocabastine. Approved, Vet Approved Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Levocabastine. Approved, Illicit Dextromoramide The risk or severity of adverse effects can be increased when Dextromoramide is combined with Levocabastine. Experimental, Illicit Dextropropoxyphene The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Levocabastine. Approved, Illicit, Withdrawn Dezocine The risk or severity of adverse effects can be increased when Dezocine is combined with Levocabastine. Approved Diazepam The risk or severity of adverse effects can be increased when Diazepam is combined with Levocabastine. Approved, Illicit, Vet Approved Diethyl ether The risk or severity of adverse effects can be increased when Diethyl ether is combined with Levocabastine. Experimental Diethylpropion Diethylpropion may decrease the sedative activities of Levocabastine. Approved, Illicit Difenoxin The risk or severity of adverse effects can be increased when Difenoxin is combined with Levocabastine. Approved, Illicit Dihydrocodeine The risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Levocabastine. Approved, Illicit Dihydroetorphine The risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Levocabastine. Experimental, Illicit Dihydromorphine The risk or severity of adverse effects can be increased when Dihydromorphine is combined with Levocabastine. Experimental, Illicit Dimenhydrinate The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Levocabastine. Approved Diphenhydramine The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Levocabastine. Approved Diphenoxylate The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Levocabastine. Approved, Illicit Dixyrazine The risk or severity of adverse effects can be increased when Dixyrazine is combined with Levocabastine. Experimental Doramectin The risk or severity of adverse effects can be increased when Doramectin is combined with Levocabastine. Vet Approved Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Levocabastine. Approved Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Vet Approved DPDPE The risk or severity of adverse effects can be increased when DPDPE is combined with Levocabastine. Investigational Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Illicit Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Vet Approved Drotebanol The risk or severity of adverse effects can be increased when Drotebanol is combined with Levocabastine. Experimental, Illicit Duloxetine The risk or severity of adverse effects can be increased when Levocabastine is combined with Duloxetine. Approved Dyclonine The risk or severity of adverse effects can be increased when Dyclonine is combined with Levocabastine. Approved Ecgonine The risk or severity of adverse effects can be increased when Ecgonine is combined with Levocabastine. Experimental, Illicit Ecopipam The risk or severity of adverse effects can be increased when Ecopipam is combined with Levocabastine. Investigational Efavirenz The risk or severity of adverse effects can be increased when Efavirenz is combined with Levocabastine. Approved, Investigational Eltanolone The risk or severity of adverse effects can be increased when Eltanolone is combined with Levocabastine. Investigational Enflurane The risk or severity of adverse effects can be increased when Enflurane is combined with Levocabastine. Approved, Vet Approved Entacapone The risk or severity of adverse effects can be increased when Entacapone is combined with Levocabastine. Approved, Investigational Escitalopram The risk or severity of adverse effects can be increased when Levocabastine is combined with Escitalopram. Approved, Investigational Estazolam The risk or severity of adverse effects can be increased when Estazolam is combined with Levocabastine. Approved, Illicit Eszopiclone The risk or severity of adverse effects can be increased when Eszopiclone is combined with Levocabastine. Approved Ethanol Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol. Approved Ethchlorvynol The risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Levocabastine. Approved, Illicit, Withdrawn Ethosuximide The risk or severity of adverse effects can be increased when Ethosuximide is combined with Levocabastine. Approved Ethotoin The risk or severity of adverse effects can be increased when Ethotoin is combined with Levocabastine. Approved Ethyl carbamate The risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Levocabastine. Withdrawn Ethyl chloride The risk or severity of adverse effects can be increased when Ethyl chloride is combined with Levocabastine. Experimental Ethyl loflazepate The risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Levocabastine. Approved, Illicit Ethylmorphine The risk or severity of adverse effects can be increased when Ethylmorphine is combined with Levocabastine. Approved, Illicit Etidocaine The risk or severity of adverse effects can be increased when Etidocaine is combined with Levocabastine. Approved Etifoxine The risk or severity of adverse effects can be increased when Etifoxine is combined with Levocabastine. Withdrawn Etizolam The risk or severity of adverse effects can be increased when Etizolam is combined with Levocabastine. Approved Etomidate The risk or severity of adverse effects can be increased when Etomidate is combined with Levocabastine. Approved Etoperidone The risk or severity of adverse effects can be increased when Levocabastine is combined with Etoperidone. Approved Etorphine The risk or severity of adverse effects can be increased when Etorphine is combined with Levocabastine. Illicit, Vet Approved Ezogabine The risk or severity of adverse effects can be increased when Ezogabine is combined with Levocabastine. Approved Felbamate The risk or severity of adverse effects can be increased when Felbamate is combined with Levocabastine. Approved Fencamfamine The risk or severity of adverse effects can be increased when Fencamfamine is combined with Levocabastine. Approved, Illicit, Withdrawn Fentanyl The risk or severity of adverse effects can be increased when Fentanyl is combined with Levocabastine. Approved, Illicit, Investigational, Vet Approved Fexofenadine The risk or severity of adverse effects can be increased when Fexofenadine is combined with Levocabastine. Approved Flibanserin The risk or severity of adverse effects can be increased when Flibanserin is combined with Levocabastine. Approved Fluanisone The risk or severity of adverse effects can be increased when Fluanisone is combined with Levocabastine. Experimental Fludiazepam The risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocabastine. Approved, Illicit Flunarizine The risk or severity of adverse effects can be increased when Flunarizine is combined with Levocabastine. Approved Flunitrazepam The risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocabastine. Approved, Illicit Fluoxetine The risk or severity of adverse effects can be increased when Levocabastine is combined with Fluoxetine. Approved, Vet Approved Flupentixol The risk or severity of adverse effects can be increased when Flupentixol is combined with Levocabastine. Approved, Withdrawn Fluphenazine The risk or severity of adverse effects can be increased when Fluphenazine is combined with Levocabastine. Approved Flurazepam The risk or severity of adverse effects can be increased when Flurazepam is combined with Levocabastine. Approved, Illicit Fluspirilene The risk or severity of adverse effects can be increased when Fluspirilene is combined with Levocabastine. Approved Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Levocabastine. Approved Fluvoxamine The risk or severity of adverse effects can be increased when Fluvoxamine is combined with Levocabastine. Approved, Investigational Fosphenytoin The risk or severity of adverse effects can be increased when Fosphenytoin is combined with Levocabastine. Approved Fospropofol The risk or severity of adverse effects can be increased when Fospropofol is combined with Levocabastine. Approved, Illicit Gabapentin The risk or severity of adverse effects can be increased when Gabapentin is combined with Levocabastine. Approved, Investigational Gabapentin Enacarbil The risk or severity of adverse effects can be increased when Gabapentin Enacarbil is combined with Levocabastine. Approved Gamma Hydroxybutyric Acid The risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Levocabastine. Approved, Illicit Gepefrine Gepefrine may decrease the sedative activities of Levocabastine. Experimental Gepirone The risk or severity of adverse effects can be increased when Gepirone is combined with Levocabastine. Investigational Glutethimide The risk or severity of adverse effects can be increased when Glutethimide is combined with Levocabastine. Approved, Illicit Guanfacine The risk or severity of adverse effects can be increased when Guanfacine is combined with Levocabastine. Approved, Investigational Halazepam The risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine. Approved, Illicit, Withdrawn Haloperidol The risk or severity of adverse effects can be increased when Haloperidol is combined with Levocabastine. Approved Halothane The risk or severity of adverse effects can be increased when Halothane is combined with Levocabastine. Approved, Vet Approved Heroin The risk or severity of adverse effects can be increased when Heroin is combined with Levocabastine. Approved, Illicit Hexobarbital The risk or severity of adverse effects can be increased when Hexobarbital is combined with Levocabastine. Approved Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Levocabastine. Approved, Investigational Hydrocodone Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone. Approved, Illicit Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Levocabastine. Approved, Illicit Hydroxyamphetamine Hydroxyamphetamine may decrease the sedative activities of Levocabastine. Approved Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved Iloperidone The risk or severity of adverse effects can be increased when Iloperidone is combined with Levocabastine. Approved Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Levocabastine. Approved Indalpine The risk or severity of adverse effects can be increased when Levocabastine is combined with Indalpine. Investigational, Withdrawn Indiplon The risk or severity of adverse effects can be increased when Indiplon is combined with Levocabastine. Investigational Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Levocabastine. Approved Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Levocabastine. Approved, Vet Approved Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with Levocabastine. Approved, Vet Approved Ketazolam The risk or severity of adverse effects can be increased when Ketazolam is combined with Levocabastine. Approved Ketobemidone The risk or severity of adverse effects can be increased when Ketobemidone is combined with Levocabastine. Approved Lamotrigine The risk or severity of adverse effects can be increased when Lamotrigine is combined with Levocabastine. Approved, Investigational Levetiracetam The risk or severity of adverse effects can be increased when Levetiracetam is combined with Levocabastine. Approved, Investigational Levobupivacaine The risk or severity of adverse effects can be increased when Levobupivacaine is combined with Levocabastine. Approved Levocetirizine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Levocabastine. Approved Levodopa The risk or severity of adverse effects can be increased when Levodopa is combined with Levocabastine. Approved Levomethadyl Acetate The risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Levocabastine. Approved Levomilnacipran The risk or severity of adverse effects can be increased when Levocabastine is combined with Levomilnacipran. Approved Levorphanol The risk or severity of adverse effects can be increased when Levorphanol is combined with Levocabastine. Approved Lidocaine The risk or severity of adverse effects can be increased when Lidocaine is combined with Levocabastine. Approved, Vet Approved Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Levocabastine. Approved, Investigational Lithium The risk or severity of adverse effects can be increased when Lithium is combined with Levocabastine. Approved Lofentanil The risk or severity of adverse effects can be increased when Lofentanil is combined with Levocabastine. Illicit Loprazolam The risk or severity of adverse effects can be increased when Loprazolam is combined with Levocabastine. Experimental Loratadine The risk or severity of adverse effects can be increased when Loratadine is combined with Levocabastine. Approved Lorazepam The risk or severity of adverse effects can be increased when Lorazepam is combined with Levocabastine. Approved Lormetazepam The risk or severity of adverse effects can be increased when Lormetazepam is combined with Levocabastine. Approved Loxapine The risk or severity of adverse effects can be increased when Loxapine is combined with Levocabastine. Approved Lurasidone The risk or severity of adverse effects can be increased when Lurasidone is combined with Levocabastine. Approved Magnesium Sulfate Magnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Vet Approved Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Levocabastine. Approved Mebicar The risk or severity of adverse effects can be increased when Mebicar is combined with Levocabastine. Experimental Meclizine The risk or severity of adverse effects can be increased when Meclizine is combined with Levocabastine. Approved Medazepam The risk or severity of adverse effects can be increased when Medazepam is combined with Levocabastine. Experimental Medetomidine The risk or severity of adverse effects can be increased when Medetomidine is combined with Levocabastine. Vet Approved Melatonin The risk or severity of adverse effects can be increased when Melatonin is combined with Levocabastine. Approved, Nutraceutical, Vet Approved Melperone The risk or severity of adverse effects can be increased when Melperone is combined with Levocabastine. Approved Mephedrone Mephedrone may decrease the sedative activities of Levocabastine. Investigational Mephentermine Mephentermine may decrease the sedative activities of Levocabastine. Approved Mepivacaine The risk or severity of adverse effects can be increased when Mepivacaine is combined with Levocabastine. Approved, Vet Approved Meprobamate The risk or severity of adverse effects can be increased when Meprobamate is combined with Levocabastine. Approved, Illicit Meptazinol The risk or severity of adverse effects can be increased when Meptazinol is combined with Levocabastine. Experimental Mesoridazine The risk or severity of adverse effects can be increased when Mesoridazine is combined with Levocabastine. Approved Metaxalone The risk or severity of adverse effects can be increased when Metaxalone is combined with Levocabastine. Approved Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Levocabastine. Approved Methadyl Acetate The risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Levocabastine. Approved, Illicit Methamphetamine Methamphetamine may decrease the sedative activities of Levocabastine. Approved, Illicit Methapyrilene The risk or severity of adverse effects can be increased when Methapyrilene is combined with Levocabastine. Withdrawn Methaqualone The risk or severity of adverse effects can be increased when Methaqualone is combined with Levocabastine. Illicit, Withdrawn Methocarbamol The risk or severity of adverse effects can be increased when Methocarbamol is combined with Levocabastine. Approved, Vet Approved Methohexital The risk or severity of adverse effects can be increased when Methohexital is combined with Levocabastine. Approved Methotrimeprazine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. Approved Methoxyflurane The risk or severity of adverse effects can be increased when Methoxyflurane is combined with Levocabastine. Approved, Vet Approved Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Levocabastine. Experimental Methsuximide The risk or severity of adverse effects can be increased when Methsuximide is combined with Levocabastine. Approved Methylecgonine The risk or severity of adverse effects can be increased when Methylecgonine is combined with Levocabastine. Experimental Methylphenobarbital The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Levocabastine. Approved Metyrosine Levocabastine may increase the sedative activities of Metyrosine. Approved Midazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine. Approved, Illicit Midomafetamine 3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Levocabastine. Experimental, Illicit Milnacipran The risk or severity of adverse effects can be increased when Levocabastine is combined with Milnacipran. Approved Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Investigational Mirtazapine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. Approved MMDA MMDA may decrease the sedative activities of Levocabastine. Experimental, Illicit Molindone The risk or severity of adverse effects can be increased when Molindone is combined with Levocabastine. Approved Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Levocabastine. Approved, Investigational Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved, Investigational Nalbuphine The risk or severity of adverse effects can be increased when Nalbuphine is combined with Levocabastine. Approved Nefazodone The risk or severity of adverse effects can be increased when Levocabastine is combined with Nefazodone. Approved, Withdrawn Nitrazepam The risk or severity of adverse effects can be increased when Nitrazepam is combined with Levocabastine. Approved Nitrous oxide The risk or severity of adverse effects can be increased when Nitrous oxide is combined with Levocabastine. Approved, Vet Approved Norflurane The risk or severity of adverse effects can be increased when Norflurane is combined with Levocabastine. Investigational Normethadone The risk or severity of adverse effects can be increased when Normethadone is combined with Levocabastine. Approved, Illicit Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Levocabastine. Approved Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Levocabastine. Approved, Investigational Olopatadine The risk or severity of adverse effects can be increased when Olopatadine is combined with Levocabastine. Approved Ondansetron The risk or severity of adverse effects can be increased when Ondansetron is combined with Levocabastine. Approved Opium The risk or severity of adverse effects can be increased when Opium is combined with Levocabastine. Approved, Illicit Orphenadrine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. Approved Osanetant The risk or severity of adverse effects can be increased when Osanetant is combined with Levocabastine. Investigational Oxazepam The risk or severity of adverse effects can be increased when Oxazepam is combined with Levocabastine. Approved Oxethazaine The risk or severity of adverse effects can be increased when Oxethazaine is combined with Levocabastine. Investigational Oxprenolol The risk or severity of adverse effects can be increased when Oxprenolol is combined with Levocabastine. Approved Oxybuprocaine The risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Levocabastine. Approved Oxycodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Levocabastine. Approved, Illicit, Investigational Oxymorphone The risk or severity of adverse effects can be increased when Oxymorphone is combined with Levocabastine. Approved, Investigational, Vet Approved Paliperidone The risk or severity of adverse effects can be increased when Paliperidone is combined with Levocabastine. Approved Paraldehyde Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. Approved Paroxetine The risk or severity of adverse effects can be increased when Levocabastine is combined with Paroxetine. Approved, Investigational Penfluridol The risk or severity of adverse effects can be increased when Penfluridol is combined with Levocabastine. Experimental Pentazocine The risk or severity of adverse effects can be increased when Pentazocine is combined with Levocabastine. Approved, Vet Approved Pentobarbital The risk or severity of adverse effects can be increased when Pentobarbital is combined with Levocabastine. Approved, Vet Approved Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved Perazine The risk or severity of adverse effects can be increased when Perazine is combined with Levocabastine. Investigational Perospirone The risk or severity of adverse effects can be increased when Perospirone is combined with Levocabastine. Approved Perphenazine The risk or severity of adverse effects can be increased when Perphenazine is combined with Levocabastine. Approved Pethidine The risk or severity of adverse effects can be increased when Pethidine is combined with Levocabastine. Approved Phenazocine The risk or severity of adverse effects can be increased when Phenazocine is combined with Levocabastine. Experimental Phenibut The risk or severity of adverse effects can be increased when Phenibut is combined with Levocabastine. Experimental Phenobarbital The risk or severity of adverse effects can be increased when Phenobarbital is combined with Levocabastine. Approved Phenoperidine The risk or severity of adverse effects can be increased when Phenoperidine is combined with Levocabastine. Experimental Phenoxyethanol The risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Levocabastine. Approved Phentermine Phentermine may decrease the sedative activities of Levocabastine. Approved, Illicit Phenytoin The risk or severity of adverse effects can be increased when Phenytoin is combined with Levocabastine. Approved, Vet Approved Pimozide The risk or severity of adverse effects can be increased when Pimozide is combined with Levocabastine. Approved Pipamperone The risk or severity of adverse effects can be increased when Pipamperone is combined with Levocabastine. Approved Pipotiazine The risk or severity of adverse effects can be increased when Pipotiazine is combined with Levocabastine. Approved Piritramide The risk or severity of adverse effects can be increased when Piritramide is combined with Levocabastine. Investigational Pizotifen The risk or severity of adverse effects can be increased when Pizotifen is combined with Levocabastine. Approved Pomalidomide The risk or severity of adverse effects can be increased when Pomalidomide is combined with Levocabastine. Approved Pramipexole Levocabastine may increase the sedative activities of Pramipexole. Approved, Investigational Pramocaine The risk or severity of adverse effects can be increased when Pramocaine is combined with Levocabastine. Approved Prazepam The risk or severity of adverse effects can be increased when Prazepam is combined with Levocabastine. Approved, Illicit Pregabalin The risk or severity of adverse effects can be increased when Pregabalin is combined with Levocabastine. Approved, Illicit, Investigational Prilocaine The risk or severity of adverse effects can be increased when Prilocaine is combined with Levocabastine. Approved Primidone The risk or severity of adverse effects can be increased when Primidone is combined with Levocabastine. Approved, Vet Approved Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Levocabastine. Approved, Investigational, Vet Approved Prochlorperazine The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Levocabastine. Approved, Vet Approved Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Levocabastine. Approved, Vet Approved Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Levocabastine. Approved Propanidid The risk or severity of adverse effects can be increased when Propanidid is combined with Levocabastine. Experimental Proparacaine The risk or severity of adverse effects can be increased when Proparacaine is combined with Levocabastine. Approved, Vet Approved Propofol The risk or severity of adverse effects can be increased when Propofol is combined with Levocabastine. Approved, Investigational, Vet Approved Propoxycaine The risk or severity of adverse effects can be increased when Propoxycaine is combined with Levocabastine. Approved Protriptyline The risk or severity of adverse effects can be increased when Protriptyline is combined with Levocabastine. Approved Proxibarbal The risk or severity of adverse effects can be increased when Proxibarbal is combined with Levocabastine. Experimental PSD502 The risk or severity of adverse effects can be increased when PSD502 is combined with Levocabastine. Investigational Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Levocabastine. Approved Quazepam The risk or severity of adverse effects can be increased when Quazepam is combined with Levocabastine. Approved, Illicit Quetiapine The risk or severity of adverse effects can be increased when Quetiapine is combined with Levocabastine. Approved Quinisocaine The risk or severity of adverse effects can be increased when Quinisocaine is combined with Levocabastine. Experimental Raclopride The risk or severity of adverse effects can be increased when Raclopride is combined with Levocabastine. Investigational Ramelteon The risk or severity of adverse effects can be increased when Ramelteon is combined with Levocabastine. Approved, Investigational Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Levocabastine. Approved Remoxipride The risk or severity of adverse effects can be increased when Remoxipride is combined with Levocabastine. Approved, Withdrawn Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Levocabastine. Approved Risperidone The risk or severity of adverse effects can be increased when Risperidone is combined with Levocabastine. Approved, Investigational Ritanserin The risk or severity of adverse effects can be increased when Ritanserin is combined with Levocabastine. Investigational Ritobegron Ritobegron may decrease the sedative activities of Levocabastine. Investigational Romifidine The risk or severity of adverse effects can be increased when Romifidine is combined with Levocabastine. Vet Approved Ropinirole Levocabastine may increase the sedative activities of Ropinirole. Approved, Investigational Ropivacaine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Levocabastine. Approved Rotigotine Levocabastine may increase the sedative activities of Rotigotine. Approved Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Levocabastine. Approved Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Levocabastine. Approved Secobarbital The risk or severity of adverse effects can be increased when Secobarbital is combined with Levocabastine. Approved, Vet Approved Sepranolone The risk or severity of adverse effects can be increased when Sepranolone is combined with Levocabastine. Investigational Sertindole The risk or severity of adverse effects can be increased when Sertindole is combined with Levocabastine. Approved, Withdrawn Sertraline The risk or severity of adverse effects can be increased when Levocabastine is combined with Sertraline. Approved Sevoflurane The risk or severity of adverse effects can be increased when Sevoflurane is combined with Levocabastine. Approved, Vet Approved Sodium oxybate Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved Stiripentol The risk or severity of adverse effects can be increased when Stiripentol is combined with Levocabastine. Approved Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Levocabastine. Approved, Investigational Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with Levocabastine. Approved Sultopride The risk or severity of adverse effects can be increased when Sultopride is combined with Levocabastine. Experimental Suvorexant Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. Approved Tandospirone The risk or severity of adverse effects can be increased when Tandospirone is combined with Levocabastine. Investigational Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine. Approved Tasimelteon The risk or severity of adverse effects can be increased when Tasimelteon is combined with Levocabastine. Approved Temazepam The risk or severity of adverse effects can be increased when Temazepam is combined with Levocabastine. Approved Tetrabenazine The risk or severity of adverse effects can be increased when Tetrabenazine is combined with Levocabastine. Approved Tetracaine The risk or severity of adverse effects can be increased when Tetracaine is combined with Levocabastine. Approved, Vet Approved Tetrahydropalmatine The risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Levocabastine. Investigational Tetrodotoxin The risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Levocabastine. Investigational Thalidomide Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide. Approved, Investigational, Withdrawn Thiamylal The risk or severity of adverse effects can be increased when Thiamylal is combined with Levocabastine. Approved, Vet Approved Thiopental The risk or severity of adverse effects can be increased when Thiopental is combined with Levocabastine. Approved, Vet Approved Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Levocabastine. Withdrawn Thiothixene The risk or severity of adverse effects can be increased when Thiothixene is combined with Levocabastine. Approved Tiagabine The risk or severity of adverse effects can be increased when Tiagabine is combined with Levocabastine. Approved Tiapride The risk or severity of adverse effects can be increased when Tiapride is combined with Levocabastine. Approved, Investigational Tiletamine The risk or severity of adverse effects can be increased when Tiletamine is combined with Levocabastine. Vet Approved Tilidine The risk or severity of adverse effects can be increased when Tilidine is combined with Levocabastine. Experimental Tizanidine The risk or severity of adverse effects can be increased when Tizanidine is combined with Levocabastine. Approved Tolcapone The risk or severity of adverse effects can be increased when Tolcapone is combined with Levocabastine. Approved, Withdrawn Topiramate The risk or severity of adverse effects can be increased when Topiramate is combined with Levocabastine. Approved Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Levocabastine. Approved, Investigational Trans-2-Phenylcyclopropylamine The risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Levocabastine. Experimental Tranylcypromine The risk or severity of adverse effects can be increased when Tranylcypromine is combined with Levocabastine. Approved Trazodone The risk or severity of adverse effects can be increased when Trazodone is combined with Levocabastine. Approved, Investigational Triazolam The risk or severity of adverse effects can be increased when Triazolam is combined with Levocabastine. Approved Tricaine methanesulfonate The risk or severity of adverse effects can be increased when Tricaine methanesulfonate is combined with Levocabastine. Vet Approved Trichloroethylene The risk or severity of adverse effects can be increased when Trichloroethylene is combined with Levocabastine. Experimental Trifluoperazine The risk or severity of adverse effects can be increased when Trifluoperazine is combined with Levocabastine. Approved Trifluperidol The risk or severity of adverse effects can be increased when Trifluperidol is combined with Levocabastine. Experimental Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Levocabastine. Approved, Vet Approved Trimipramine The risk or severity of adverse effects can be increased when Trimipramine is combined with Levocabastine. Approved Triprolidine The risk or severity of adverse effects can be increased when Triprolidine is combined with Levocabastine. Approved Valproic Acid The risk or severity of adverse effects can be increased when Valproic Acid is combined with Levocabastine. Approved, Investigational Venlafaxine The risk or severity of adverse effects can be increased when Levocabastine is combined with Venlafaxine. Approved Veralipride The risk or severity of adverse effects can be increased when Veralipride is combined with Levocabastine. Experimental Vigabatrin The risk or severity of adverse effects can be increased when Vigabatrin is combined with Levocabastine. Approved Vinyl ether The risk or severity of adverse effects can be increased when Vinyl ether is combined with Levocabastine. Experimental Vortioxetine The risk or severity of adverse effects can be increased when Vortioxetine is combined with Levocabastine. Approved Xenon The risk or severity of adverse effects can be increased when Xenon is combined with Levocabastine. Experimental Xylazine The risk or severity of adverse effects can be increased when Xylazine is combined with Levocabastine. Vet Approved Zaleplon The risk or severity of adverse effects can be increased when Zaleplon is combined with Levocabastine. Approved, Illicit, Investigational Ziconotide The risk or severity of adverse effects can be increased when Ziconotide is combined with Levocabastine. Approved Zimelidine The risk or severity of adverse effects can be increased when Levocabastine is combined with Zimelidine. Withdrawn Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Levocabastine. Approved Zolazepam The risk or severity of adverse effects can be increased when Zolazepam is combined with Levocabastine. Vet Approved Zolpidem Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem. Approved Zonisamide The risk or severity of adverse effects can be increased when Zonisamide is combined with Levocabastine. Approved, Investigational Zopiclone The risk or severity of adverse effects can be increased when Zopiclone is combined with Levocabastine. Approved Zotepine The risk or severity of adverse effects can be increased when Zotepine is combined with Levocabastine. Approved Zuclopenthixol The risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Levocabastine. Approved, Investigational - Food Interactions
- Not Available
References
- General References
- Not Available
- External Links
- KEGG Drug
- D01717
- ChemSpider
- 16736421
- BindingDB
- 50019405
- ChEBI
- 135679
- ChEMBL
- CHEMBL1615438
- Therapeutic Targets Database
- DAP000335
- PharmGKB
- PA164742988
- IUPHAR
- 1586
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Levocabastine
- ATC Codes
- R01AC02 — Levocabastine
- R01AC — Antiallergic agents, excl. corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- AHFS Codes
- 52:02.00 — Antiallergic Agents
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Rhinitis, Allergic, Perennial and Seasonal 2 3 Completed Treatment Rhinitis, Allergic, Perennial 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Novartis AG
- OMJ Pharmaceuticals
- Physicians Total Care Inc.
- Dosage forms
Form Route Strength Solution / drops; suspension Ophthalmic 0.5 mg Spray; suspension Nasal 0.5 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility >0.5 mg/mL Not Available logP 5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00347 mg/mL ALOGPS logP 4.56 ALOGPS logP 2.5 ChemAxon logS -5.1 ALOGPS pKa (Strongest Acidic) 3.71 ChemAxon pKa (Strongest Basic) 10.32 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 64.33 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 118.48 m3·mol-1 ChemAxon Polarizability 45.58 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9811 Blood Brain Barrier + 0.8388 Caco-2 permeable + 0.5747 P-glycoprotein substrate Substrate 0.7325 P-glycoprotein inhibitor I Inhibitor 0.5 P-glycoprotein inhibitor II Non-inhibitor 0.5682 Renal organic cation transporter Non-inhibitor 0.5526 CYP450 2C9 substrate Non-substrate 0.7708 CYP450 2D6 substrate Non-substrate 0.6679 CYP450 3A4 substrate Substrate 0.5153 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.8932 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9046 Ames test Non AMES toxic 0.7503 Carcinogenicity Non-carcinogens 0.9196 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.9608 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9404 hERG inhibition (predictor II) Inhibitor 0.625
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This 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.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Piperidines
- Sub Class
- Phenylpiperidines
- Direct Parent
- Phenylpiperidines
- Alternative Parents
- Piperidinecarboxylic acids / Aralkylamines / Fluorobenzenes / Cyclohexylamines / Aryl fluorides / Trialkylamines / Amino acids / Nitriles / Monocarboxylic acids and derivatives / Azacyclic compounds show 6 more
- Substituents
- Phenylpiperidine / Piperidinecarboxylic acid / Cyclohexylamine / Fluorobenzene / Aralkylamine / Halobenzene / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid show 22 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
Targets
- 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 catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- Uniprot Name
- Neurotensin receptor type 2
- Molecular Weight
- 45384.635 Da
References
- 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]
- 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]
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Drug created on June 13, 2005 07:24 / Updated on October 23, 2017 14:13