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Identification
NameMethotrimeprazine
Accession NumberDB01403
TypeSmall Molecule
GroupsApproved
Description

A phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)

Structure
Thumb
Synonyms
(-)-(2R)-3-(2-Methoxy-10H-phenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
(-)-10-(3-(Dimethylamino)-2-methylpropyl)-2-methoxyphenothiazine
2-Methoxytrimeprazine
Levomepromazina
Levomepromazine
Levomepromazinum
Methotrimeprazine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Methoprazinetablet2 mgoralAa Pharma Inc1998-07-20Not applicableCanada
Methoprazinetablet50 mgoralAa Pharma Inc1998-07-20Not applicableCanada
Methoprazinetablet25 mgoralAa Pharma Inc1998-07-20Not applicableCanada
Methoprazinetablet5 mgoralAa Pharma Inc1998-07-20Not applicableCanada
Methotrimeprazine-2tablet2 mgoralPro Doc Limitee1999-05-102009-07-23Canada
Methotrimeprazine-25tablet25 mgoralPro Doc Limitee1999-05-122011-07-27Canada
Methotrimeprazine-5tablet5 mgoralPro Doc Limitee1999-05-122011-07-27Canada
Methotrimeprazine-50tablet50 mgoralPro Doc Limitee1999-05-102011-07-27Canada
Nov Meprazine Tab 50mgtablet50 mgoralNovopharm Limited1996-12-312005-08-10Canada
Novo Meprazine Tab 25mgtablet25 mgoralNovopharm Limited1996-12-31Not applicableCanada
Novo Meprazine Tab 5mgtablet5 mgoralNovopharm Limited1995-07-17Not applicableCanada
Nozinan 5mg Tabtablet5 mgoralSanofi Aventis Canada Inc1958-12-312007-07-18Canada
Nozinan 5mg/mlsolution5 mgoralSanofi Aventis Canada Inc1966-12-312006-07-28Canada
Nozinan Inj 25mg/mlsolution25 mgintramuscular; intravenousSanofi Aventis Canada Inc1958-12-31Not applicableCanada
Nozinan Liq 40mg/mldrops; liquid40 mgoralAventis Pharma Inc1963-12-312005-08-01Canada
Nozinan Tab 25mgtablet25 mgoralSanofi Aventis Canada Inc1958-12-312007-07-18Canada
Nozinan Tab 2mgtablet2 mgoralAventis Pharma Inc1958-12-312005-08-01Canada
Nozinan Tab 50mgtablet50 mgoralSanofi Aventis Canada Inc1958-12-312007-07-18Canada
PMS-methotrimeprazinetablet50 mgoralPharmascience Inc1997-10-20Not applicableCanada
PMS-methotrimeprazinetablet25 mgoralPharmascience Inc1997-10-20Not applicableCanada
PMS-methotrimeprazinetablet5 mgoralPharmascience Inc1997-10-20Not applicableCanada
Riva-meprazine 25mg Tabletstablet25 mgoralLaboratoire Riva Inc1999-11-222003-07-28Canada
Riva-meprazine 50mg Tabletstablet50 mgoralLaboratoire Riva Inc1999-11-222003-07-28Canada
Riva-meprazine 5mg Tabletstablet5 mgoralLaboratoire Riva Inc1999-11-222003-07-28Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LevopromeNot Available
NeurocilNot Available
NosinanNot Available
NozinanNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII9G0LAW7ATQ
CAS number60-99-1
WeightAverage: 328.472
Monoisotopic: 328.16093409
Chemical FormulaC19H24N2OS
InChI KeyInChIKey=VRQVVMDWGGWHTJ-CQSZACIVSA-N
InChI
InChI=1S/C19H24N2OS/c1-14(12-20(2)3)13-21-16-7-5-6-8-18(16)23-19-10-9-15(22-4)11-17(19)21/h5-11,14H,12-13H2,1-4H3/t14-/m1/s1
IUPAC Name
[(2R)-3-(2-methoxy-10H-phenothiazin-10-yl)-2-methylpropyl]dimethylamine
SMILES
COC1=CC2=C(SC3=C(C=CC=C3)N2C[[email protected]](C)CN(C)C)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiazines
Sub ClassPhenothiazines
Direct ParentPhenothiazines
Alternative Parents
Substituents
  • Phenothiazine
  • Alkyldiarylamine
  • Diarylthioether
  • Anisole
  • Alkyl aryl ether
  • Benzenoid
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder.
PharmacodynamicsMethotrimeprazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)
Mechanism of actionMethotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role.
Related Articles
AbsorptionMethotrimeprazine has an incomplete oral bioavailability, because it undergoes considerable first-pass-metabolism in the liver. Oral bioavailability is approximately 50 to 60%.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety.

Route of eliminationNot Available
Half lifeApproximately 20 hours.
ClearanceNot Available
ToxicitySymptoms of overdose include convulsions, spastic movements, and coma.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9857
Blood Brain Barrier+0.9935
Caco-2 permeable+0.6694
P-glycoprotein substrateSubstrate0.6805
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IIInhibitor0.8571
Renal organic cation transporterNon-inhibitor0.5132
CYP450 2C9 substrateNon-substrate0.7511
CYP450 2D6 substrateSubstrate0.5363
CYP450 3A4 substrateSubstrate0.6056
CYP450 1A2 substrateInhibitor0.6953
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.5432
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5633
Ames testNon AMES toxic0.5562
CarcinogenicityNon-carcinogens0.9182
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5064 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.932
hERG inhibition (predictor II)Inhibitor0.8488
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral2 mg
Tabletoral25 mg
Tabletoral5 mg
Solutionoral5 mg
Solutionintramuscular; intravenous25 mg
Drops; liquidoral40 mg
Tabletoral50 mg
Prices
Unit descriptionCostUnit
Nozinan 25 mg/ml3.6USD ml
Apo-Methoprazine 50 mg Tablet0.4USD tablet
Apo-Methoprazine 25 mg Tablet0.27USD tablet
Apo-Methoprazine 5 mg Tablet0.1USD tablet
Apo-Methoprazine 2 mg Tablet0.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility20 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.68HANSCH,C ET AL. (1995)
logS-4.22ADME Research, USCD
pKa9.19SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.00525 mg/mLALOGPS
logP4.84ALOGPS
logP4.25ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)9.42ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area15.71 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity99.83 m3·mol-1ChemAxon
Polarizability36.77 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
MSMass Spectrum (Electron Ionization)splash10-056r-9356000000-bb17e4980980d336d337View in MoNA
References
Synthesis Reference

Christian Berger, “Process for preparing levomepromazine hydrogen maleate.” U.S. Patent US4798895, issued January 17, 1989.

US4798895
General References
  1. Link [Link]
External Links
ATC CodesN05AA02
AHFS Codes
  • 28:16.08.24
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Methotrimeprazine.
AclidiniumAclidinium may increase the anticholinergic activities of Methotrimeprazine.
AlfentanilAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Methotrimeprazine.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Methotrimeprazine.
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Methotrimeprazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
AmisulprideThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Methotrimeprazine.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Methotrimeprazine.
AmphetamineMethotrimeprazine may decrease the stimulatory activities of Amphetamine.
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
AtomoxetineThe serum concentration of Atomoxetine can be increased when it is combined with Methotrimeprazine.
AzelastineMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
BenzphetamineMethotrimeprazine may decrease the stimulatory activities of Benzphetamine.
Botulinum Toxin Type AMethotrimeprazine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BMethotrimeprazine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Methotrimeprazine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
BromocriptineThe therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Bromocriptine.
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
BuprenorphineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Methotrimeprazine.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methotrimeprazine.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Methotrimeprazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Methotrimeprazine.
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CathinoneMethotrimeprazine may decrease the stimulatory activities of Cathinone.
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Methotrimeprazine.
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Cimetropium BromideMethotrimeprazine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Methotrimeprazine.
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Methotrimeprazine.
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Methotrimeprazine.
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Methotrimeprazine.
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Methotrimeprazine.
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Methotrimeprazine.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DextroamphetamineMethotrimeprazine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Methotrimeprazine.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Methotrimeprazine.
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DofetilideMethotrimeprazine may increase the QTc-prolonging activities of Dofetilide.
DonepezilDonepezil may increase the central neurotoxic activities of Methotrimeprazine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Methotrimeprazine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Methotrimeprazine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Methotrimeprazine.
EfavirenzEfavirenz may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Methotrimeprazine.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Methotrimeprazine.
EluxadolineMethotrimeprazine may increase the activities of Eluxadoline.
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Methotrimeprazine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Methotrimeprazine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methotrimeprazine.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Methotrimeprazine.
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
EthanolMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Methotrimeprazine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methotrimeprazine.
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Methotrimeprazine.
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Methotrimeprazine.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Methotrimeprazine.
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
gabapentin enacarbilgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
GalantamineGalantamine may increase the central neurotoxic activities of Methotrimeprazine.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Methotrimeprazine.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Methotrimeprazine.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Methotrimeprazine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Glucagon recombinant.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Methotrimeprazine.
GoserelinMethotrimeprazine may increase the QTc-prolonging activities of Goserelin.
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
HydrocodoneHydrocodone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
HydromorphoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Methotrimeprazine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Methotrimeprazine.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Methotrimeprazine.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Methotrimeprazine.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Methotrimeprazine.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Methotrimeprazine.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Methotrimeprazine.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Methotrimeprazine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Methotrimeprazine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Methotrimeprazine.
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Methotrimeprazine.
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LeuprolideMethotrimeprazine may increase the QTc-prolonging activities of Leuprolide.
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Methotrimeprazine.
LevorphanolLevorphanol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methotrimeprazine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Methotrimeprazine.
LisdexamfetamineMethotrimeprazine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Methotrimeprazine.
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Methotrimeprazine.
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Methotrimeprazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Methotrimeprazine.
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MequitazineThe serum concentration of Mequitazine can be increased when it is combined with Methotrimeprazine.
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Methotrimeprazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Methotrimeprazine.
MethamphetamineMethotrimeprazine may decrease the stimulatory activities of Methamphetamine.
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Methotrimeprazine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Methotrimeprazine.
MetyrosineMethotrimeprazine may increase the sedative activities of Metyrosine.
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Methotrimeprazine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Methotrimeprazine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MirabegronThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Mirabegron.
MirtazapineMirtazapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Methotrimeprazine.
MorphineMorphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Methotrimeprazine.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Methotrimeprazine.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Methotrimeprazine.
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Methotrimeprazine.
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
OrphenadrineMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
OxycodoneOxycodone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
OxymorphoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ParaldehydeMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Paroxetine.
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Methotrimeprazine.
PhendimetrazineMethotrimeprazine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Methotrimeprazine.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PhentermineMethotrimeprazine may decrease the stimulatory activities of Phentermine.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Methotrimeprazine.
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PorfimerMethotrimeprazine may increase the photosensitizing activities of Porfimer.
Potassium ChlorideMethotrimeprazine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Methotrimeprazine.
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Methotrimeprazine.
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Methotrimeprazine.
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Methotrimeprazine.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Methotrimeprazine.
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Methotrimeprazine.
PyrimethamineThe serum concentration of Methotrimeprazine can be increased when it is combined with Pyrimethamine.
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Methotrimeprazine.
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
RamosetronMethotrimeprazine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Methotrimeprazine.
RemifentanilRemifentanil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Methotrimeprazine.
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
RivastigmineRivastigmine may increase the central neurotoxic activities of Methotrimeprazine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Methotrimeprazine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methotrimeprazine.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methotrimeprazine.
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Scopolamine butylbromideScopolamine butylbromide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Methotrimeprazine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Methotrimeprazine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Methotrimeprazine.
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
StiripentolStiripentol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
SufentanilSufentanil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
SulpirideThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Methotrimeprazine.
SuvorexantMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Tacrine.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Methotrimeprazine resulting in a loss in efficacy.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Methotrimeprazine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Methotrimeprazine.
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TetrabenazineThe serum concentration of Tetrabenazine can be increased when it is combined with Methotrimeprazine.
ThalidomideMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Methotrimeprazine.
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TiotropiumMethotrimeprazine may increase the anticholinergic activities of Tiotropium.
TizanidineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Methotrimeprazine.
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Methotrimeprazine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Methotrimeprazine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Methotrimeprazine.
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Methotrimeprazine.
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Methotrimeprazine.
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Methotrimeprazine.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Methotrimeprazine.
VerteporfinMethotrimeprazine may increase the photosensitizing activities of Verteporfin.
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Methotrimeprazine.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Methotrimeprazine.
VortioxetineThe serum concentration of Vortioxetine can be increased when it is combined with Methotrimeprazine.
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Methotrimeprazine.
ZolpidemZolpidem may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Food Interactions
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  3. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD5
Uniprot ID:
P21918
Molecular Weight:
52950.5 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  2. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  2. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  2. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  2. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  2. Hals PA, Hall H, Dahl SG: Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12. [PubMed:2899826 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  3. Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K: Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. [PubMed:6149771 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  3. Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K: Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. [PubMed:6149771 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
  2. Dahl SG, Hough E, Hals PA: Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding. Biochem Pharmacol. 1986 Apr 15;35(8):1263-9. [PubMed:2870716 ]
  3. Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K: Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. [PubMed:6149771 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Green B, Pettit T, Faith L, Seaton K: Focus on levomepromazine. Curr Med Res Opin. 2004 Dec;20(12):1877-81. [PubMed:15701205 ]
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Drug created on July 10, 2007 12:38 / Updated on September 16, 2013 17:14