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Identification
NameCyclizine
Accession NumberDB01176  (APRD00061)
TypeSmall Molecule
GroupsApproved
DescriptionA histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935)
Structure
Thumb
Synonyms
(+-)-1-Diphenylmethyl-4-methylpiperazine
(±)-1-diphenylmethyl-4-methylpiperazine
(N-Benzhydryl)(n'-methyl)diethylenediamine
1-(Diphenylmethyl)-4-methylpiperazine
1-Benzhydryl-4-methylpiperazin
Ciclizina
Cyclizine
Cyclizinum
N-Benzhydryl-N'-methylpiperazine
N-methyl-N'-benzhydrylpiperazine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Marzine Inj 50mg/mlLiquid50 mgIntramuscular; IntravenousGlaxo Wellcome Inc.1988-12-311998-07-30Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CyclivertTablet25 mg/25mgOralLaser Pharmaceuticals, LLC2011-11-01Not applicableUs
Unapproved/Other Products Not Available
International Brands
NameCompany
EmoquilNot Available
MarezineNot Available
MarzineGlaxoSmithKline
ValoidGlaxoSmithKline
Brand mixtures
NameLabellerIngredients
Megral TabsGlaxo Wellcome Inc.
Salts
Name/CASStructureProperties
Cyclizine chloride
Thumb
  • InChI Key: UKPBEPCQTDRZSE-UHFFFAOYSA-N
  • Monoisotopic Mass: 302.154976453
  • Average Mass: 302.842
DBSALT000399
Cyclizine hydrochloride
ThumbNot applicableDBSALT001535
Cyclizine lactate
ThumbNot applicableDBSALT001182
Categories
UNIIQRW9FCR9P2
CAS number82-92-8
WeightAverage: 266.3807
Monoisotopic: 266.178298714
Chemical FormulaC18H22N2
InChI KeyUVKZSORBKUEBAZ-UHFFFAOYSA-N
InChI
InChI=1S/C18H22N2/c1-19-12-14-20(15-13-19)18(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18H,12-15H2,1H3
IUPAC Name
1-(diphenylmethyl)-4-methylpiperazine
SMILES
CN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1
Pharmacology
IndicationFor prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo (dizziness caused by other medical problems).
Structured Indications
PharmacodynamicsCyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.
Mechanism of actionVomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.
TargetKindPharmacological actionActionsOrganismUniProt ID
Histamine H1 receptorProteinyes
antagonist
HumanP35367 details
Estrogen sulfotransferaseProteinunknown
inhibitor
HumanP49888 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine.

Route of eliminationNot Available
Half life20 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Cyclizine is combined with 1,1,1,2 Tetrafluoroethane.Investigational
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Cyclizine.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Cyclizine.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Cyclizine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Cyclizine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Cyclizine.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Cyclizine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Cyclizine.Approved
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Cyclizine.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Cyclizine.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Cyclizine.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Cyclizine.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Cyclizine.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Cyclizine.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Cyclizine.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Cyclizine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Cyclizine.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Cyclizine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Cyclizine.Experimental
AmphetamineAmphetamine may decrease the sedative activities of Cyclizine.Approved, Illicit
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Cyclizine.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Cyclizine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyclizine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Cyclizine.Vet Approved
AzelastineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Cyclizine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyclizine.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Cyclizine.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Cyclizine is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Cyclizine.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Cyclizine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Cyclizine.Approved
Benzylpenicilloyl PolylysineCyclizine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Cyclizine.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Cyclizine is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Cyclizine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Cyclizine.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Cyclizine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Cyclizine.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Cyclizine.Approved, Investigational
BuprenorphineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Cyclizine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Cyclizine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Cyclizine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Cyclizine.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Cyclizine.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Cyclizine.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Cyclizine.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Cyclizine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Cyclizine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Cyclizine.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Cyclizine.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Cyclizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Cyclizine.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Cyclizine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Cyclizine.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Cyclizine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Cyclizine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Cyclizine.Illicit, Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Cyclizine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Cyclizine.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Cyclizine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Cyclizine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Cyclizine is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Cyclizine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Cyclizine.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Cyclizine.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Cyclizine.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Cyclizine.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Cyclizine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Cyclizine.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Cyclizine.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Cyclizine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Cyclizine.Approved, Illicit
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Cyclizine.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Cyclizine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Cyclizine is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Cyclizine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Dapoxetine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Cyclizine.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Cyclizine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Cyclizine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Cyclizine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Cyclizine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Cyclizine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Cyclizine.Approved, Vet Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Cyclizine.Approved, Illicit
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Cyclizine.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Cyclizine.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Cyclizine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Cyclizine.Approved, Illicit, Vet Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Cyclizine.Approved, Illicit
DifenoxinThe risk or severity of adverse effects can be increased when Cyclizine is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Cyclizine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Cyclizine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Cyclizine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Cyclizine.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Cyclizine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Cyclizine.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Cyclizine.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Cyclizine.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Cyclizine.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Cyclizine.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Cyclizine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Cyclizine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Cyclizine.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Cyclizine is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Cyclizine.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Cyclizine.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Cyclizine.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Cyclizine is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Cyclizine.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Cyclizine.Approved
EthanolCyclizine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Cyclizine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Cyclizine.Approved
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Cyclizine.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Cyclizine.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Cyclizine.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Cyclizine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Cyclizine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Cyclizine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Cyclizine.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Cyclizine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Cyclizine is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Cyclizine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Cyclizine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Cyclizine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Cyclizine.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Cyclizine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Cyclizine is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Cyclizine.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Cyclizine.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Cyclizine.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Cyclizine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Cyclizine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Cyclizine.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Cyclizine.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Cyclizine.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Cyclizine is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Cyclizine.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Cyclizine.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Cyclizine is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Cyclizine.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Cyclizine is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Cyclizine.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Cyclizine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyclizine.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Cyclizine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Cyclizine.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Cyclizine.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Cyclizine.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Cyclizine.Approved, Investigational
HydrocodoneCyclizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Cyclizine.Approved, Illicit
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Cyclizine.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Cyclizine is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Cyclizine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Cyclizine.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Cyclizine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Cyclizine.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Cyclizine.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Cyclizine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Cyclizine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Cyclizine.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Cyclizine.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Cyclizine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Cyclizine.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Cyclizine.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Cyclizine.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Cyclizine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Cyclizine.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Cyclizine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Lu AA21004 is combined with Cyclizine.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Cyclizine.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Cyclizine.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Cyclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Cyclizine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Cyclizine.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Cyclizine.Approved
MephedroneMephedrone may decrease the sedative activities of Cyclizine.Investigational
MephentermineMephentermine may decrease the sedative activities of Cyclizine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Cyclizine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Cyclizine.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Cyclizine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Cyclizine.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Cyclizine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Cyclizine.Approved, Illicit
MethamphetamineMethamphetamine may decrease the sedative activities of Cyclizine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Cyclizine.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Cyclizine.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Cyclizine.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Cyclizine.Approved
MethotrimeprazineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Cyclizine.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Cyclizine.Approved
MetyrosineCyclizine may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyclizine.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Cyclizine is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Investigational
MirtazapineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MMDAMMDA may decrease the sedative activities of Cyclizine.Experimental, Illicit
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Cyclizine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Cyclizine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Cyclizine.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Cyclizine is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Cyclizine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Cyclizine.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Cyclizine.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Cyclizine.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Cyclizine.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Cyclizine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Cyclizine.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Cyclizine.Approved, Illicit
OrphenadrineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Cyclizine.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Cyclizine.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Cyclizine.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Cyclizine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Cyclizine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Cyclizine.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Cyclizine.Approved
ParaldehydeCyclizine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Cyclizine.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Cyclizine.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
PerazineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Cyclizine.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Cyclizine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Cyclizine.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Cyclizine.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Cyclizine.Approved
PhenterminePhentermine may decrease the sedative activities of Cyclizine.Approved, Illicit
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Cyclizine.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Cyclizine.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Cyclizine.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Cyclizine is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Pomalidomide.Approved
PramipexoleCyclizine may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Cyclizine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Cyclizine.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Cyclizine.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Cyclizine is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Cyclizine.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Cyclizine.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Cyclizine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Cyclizine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Cyclizine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Cyclizine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Cyclizine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Cyclizine.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Cyclizine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Cyclizine.Approved
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Cyclizine.Investigational
PseudoephedrinePseudoephedrine may decrease the sedative activities of Cyclizine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Cyclizine.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Cyclizine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Cyclizine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Cyclizine.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Cyclizine.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Cyclizine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Cyclizine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Cyclizine is combined with Ritanserin.Investigational
RitobegronRitobegron may decrease the sedative activities of Cyclizine.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Cyclizine.Vet Approved
RopiniroleCyclizine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Cyclizine.Approved
RotigotineCyclizine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyclizine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Cyclizine.Experimental
Sage 547The risk or severity of adverse effects can be increased when Cyclizine is combined with Sage 547.Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Cyclizine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Cyclizine.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Cyclizine.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Cyclizine.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
StiripentolThe risk or severity of adverse effects can be increased when Cyclizine is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Cyclizine.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Cyclizine.Approved
SuvorexantCyclizine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Cyclizine.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Cyclizine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Cyclizine.Investigational
ThalidomideCyclizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Cyclizine.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Cyclizine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Cyclizine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Cyclizine.Approved
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Cyclizine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Cyclizine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Cyclizine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Cyclizine.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Cyclizine.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cyclizine.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Cyclizine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Cyclizine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Cyclizine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Cyclizine.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Cyclizine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Cyclizine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Cyclizine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Cyclizine.Approved
Uc1010The risk or severity of adverse effects can be increased when Cyclizine is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Cyclizine.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Cyclizine.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Cyclizine.Approved
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Cyclizine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Cyclizine.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Cyclizine is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Cyclizine.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Cyclizine.Vet Approved
ZolpidemCyclizine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Cyclizine.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Cyclizine.Approved
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Cyclizine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Cyclizine.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Food may reduce irritation.
  • Take without regard to meals.
References
Synthesis Reference

Baltzly, R. and Castillo, J.C.; U.S. Patent 2,630,435; March 3,1953; assigned to Burroughs
Wellcome & Co. (U.S.A.) Inc.

General ReferencesNot Available
External Links
ATC CodesR06AE03R06AE53
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.4 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9674
Blood Brain Barrier+0.9813
Caco-2 permeable+0.8023
P-glycoprotein substrateSubstrate0.8071
P-glycoprotein inhibitor INon-inhibitor0.7583
P-glycoprotein inhibitor IINon-inhibitor0.981
Renal organic cation transporterInhibitor0.7875
CYP450 2C9 substrateNon-substrate0.829
CYP450 2D6 substrateSubstrate0.6312
CYP450 3A4 substrateNon-substrate0.6591
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9676
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9438
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9071
Ames testNon AMES toxic0.9308
CarcinogenicityNon-carcinogens0.9667
BiodegradationNot ready biodegradable0.983
Rat acute toxicity2.3937 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6672
hERG inhibition (predictor II)Non-inhibitor0.5073
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral25 mg/25mg
LiquidIntramuscular; Intravenous50 mg
TabletOral
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point105.5-107.5Baltzly, R. and Castillo, J.C.; U.S. Patent 2,630,435; March 3,1953; assigned to Burroughs Wellcome & Co. (U.S.A.) Inc.
water solubility1000 mg/L (at 25 °C)MERCK INDEX (1996); less than
logP3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0752 mg/mLALOGPS
logP3.55ALOGPS
logP3.55ChemAxon
logS-3.5ALOGPS
pKa (Strongest Basic)8.51ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity84.93 m3·mol-1ChemAxon
Polarizability31.53 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Aralkylamine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Piperazine
  • 1,4-diazinane
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

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 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. Leza JC, Lizasoain I, Lorenzo P: H1- and H2-histamine receptor blockers and opiate analgesia in mice. Methods Find Exp Clin Pharmacol. 1990 Dec;12(10):671-8. [PubMed:1983158 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sulfotransferase activity
Specific Function:
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of estradiol and estrone. May play a role in the regulation of estrogen receptor activity by metabolizing free estradiol. Maximally sulfates beta-estradiol and estrone at concentrations of 20 nM. Also sulfates dehydroepiandrosterone, pregnenolone, ethinylestradiol, equalen...
Gene Name:
SULT1E1
Uniprot ID:
P49888
Molecular Weight:
35126.185 Da
References
  1. Bamforth KJ, Dalgliesh K, Coughtrie MW: Inhibition of human liver steroid sulfotransferase activities by drugs: a novel mechanism of drug toxicity? Eur J Pharmacol. 1992 May 1;228(1):15-21. [PubMed:1397064 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23