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Identification
NamePromazine
Accession NumberDB00420  (APRD00358)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

A phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. Promazine is not approved for use in the United States.

Structure
Thumb
Synonyms
10-(3-(Dimethylamino)propyl)phenothiazine
Frenil
N-(3-Dimethylaminopropyl)phenothiazine
N-Dimethylamino-1-methylethyl thiodiphenylamine
N,N-dimethyl-3-(10H-phenothiazin-10-yl)-propan-1-amine
Promazin
Promazina
Promazina
Promazine
Promazinum
External Identifiers
  • A 145
  • RP 3276
  • Wy 1094
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Promazine HCl Inj 50mg/mlliquid50 mgintramuscular; intravenousAbbott Laboratories, Limited1981-12-312008-06-06Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CombelenNot Available
PrazinePliva
SparineNot Available
TalofenAbbott
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Promazine Hydrochloride
53-60-1
Thumb
  • InChI Key: JIVSXRLRGOICGA-UHFFFAOYSA-N
  • Monoisotopic Mass: 320.111397079
  • Average Mass: 320.88
DBSALT000147
Categories
UNIIO9M39HTM5W
CAS number58-40-2
WeightAverage: 284.419
Monoisotopic: 284.13471934
Chemical FormulaC17H20N2S
InChI KeyInChIKey=ZGUGWUXLJSTTMA-UHFFFAOYSA-N
InChI
InChI=1S/C17H20N2S/c1-18(2)12-7-13-19-14-8-3-5-10-16(14)20-17-11-6-4-9-15(17)19/h3-6,8-11H,7,12-13H2,1-2H3
IUPAC Name
dimethyl[3-(10H-phenothiazin-10-yl)propyl]amine
SMILES
CN(C)CCCN1C2=CC=CC=C2SC2=CC=CC=C12
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
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed as an adjunct for short term treatment of moderate and severe psychomotor agitation. Also used to treat agitation or restlessness in the elderly.
PharmacodynamicsPromazine belongs to a group of medications known as the phenothiazine antipsychotics. It acts by blocking a variety of receptors in the brain, particularly dopamine receptors. Dopamine is involved in transmitting signals between brain cells. When there is an excess amount of dopamine in the brain it causes over-stimulation of dopamine receptors. These receptors normally act to modify behaviour and over-stimulation may result in psychotic illness. Promazine hydrochloride blocks these receptors and stops them becoming over-stimulated, thereby helping to control psychotic illness. Promazine has weak extrapyramidal and autonomic side effects which lead to its use in the elderly, for restless or psychotic patients. Its anti-psychotic effect is also weaker and it is not useful in general psychiatry.
Mechanism of actionPromazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine.
Related Articles
AbsorptionAbsorption may be erratic and peak plasma concentrations show large interindividual differences.
Volume of distributionNot Available
Protein binding94%
Metabolism

Hepatic, primarily to N-desmethylpromazine and promazine sulfoxide.

SubstrateEnzymesProduct
Promazine
Promazine 5-sulfoxideDetails
Promazine
N-DesmethylpromazineDetails
Promazine
Not Available
3-HydroxypromazineDetails
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySide effects include: extrapyramidal symptoms, drowsiness, weight gain, dry mouth, constipation, endocrine effects (such as gynaecomastia and menstrual disturbance), sensitivity to sunlight and haemolytic anaemia.
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+0.9718
Blood Brain Barrier+0.987
Caco-2 permeable+0.8813
P-glycoprotein substrateSubstrate0.7933
P-glycoprotein inhibitor IInhibitor0.6857
P-glycoprotein inhibitor IIInhibitor0.6352
Renal organic cation transporterInhibitor0.7561
CYP450 2C9 substrateNon-substrate0.7526
CYP450 2D6 substrateSubstrate0.9334
CYP450 3A4 substrateSubstrate0.5578
CYP450 1A2 substrateInhibitor0.8935
CYP450 2C9 inhibitorNon-inhibitor0.9483
CYP450 2D6 inhibitorInhibitor0.9622
CYP450 2C19 inhibitorNon-inhibitor0.798
CYP450 3A4 inhibitorNon-inhibitor0.9166
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6784
Ames testNon AMES toxic0.9176
CarcinogenicityNon-carcinogens0.9545
BiodegradationNot ready biodegradable0.9921
Rat acute toxicity2.9416 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9662
hERG inhibition (predictor II)Inhibitor0.7828
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Wyeth ayerst laboratories
  • Watson laboratories inc
  • Baxter healthcare corp anesthesia critical care
  • Apothecon sub bristol myers squibb co
  • Apothecon inc div bristol myers squibb
  • Bristol myers squibb co
Packagers
Dosage forms
FormRouteStrength
Liquidintramuscular; intravenous50 mg
Prices
Unit descriptionCostUnit
Chlorpromazine 25 mg/ml amp8.04USD ml
Chlorpromazine 200 mg tablet1.05USD tablet
Chlorpromazine Hcl 25 mg/ml0.88USD ml
Chlorpromazine 100 mg tablet0.39USD tablet
Novo-Chlorpromazine 100 mg Tablet0.35USD tablet
Chlorpromazine 10 mg tablet0.32USD tablet
Chlorpromazine 50 mg tablet0.3USD tablet
Novo-Chlorpromazine 50 mg Tablet0.21USD tablet
Novo-Chlorpromazine 25 mg Tablet0.18USD tablet
Chlorpromazine 25 mg tablet0.17USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point< 25 °CPhysProp
boiling point203-210 °C at 3.00E-01 mm HgPhysProp
water solubility14.2 mg/L (at 24 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.55HANSCH,C ET AL. (1995)
logS-4.3ADME Research, USCD
pKa9.36SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0207 mg/mLALOGPS
logP4.63ALOGPS
logP3.93ChemAxon
logS-4.1ALOGPS
pKa (Strongest Basic)9.2ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity88.95 m3·mol-1ChemAxon
Polarizability32.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (9.05 KB)
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
MSMass Spectrum (Electron Ionization)splash10-0a4i-9430000000-708a7cbef8d61ce76846View in MoNA
References
Synthesis Reference

DrugSyn.org

US2519886
General References
  1. Cubala WJ, Jakuszkowiak-Wojten K, Burkiewicz A, Wronska A: Promazine in the treatment of delusional parasitosis. Psychiatr Danub. 2011 Jun;23(2):198-9. [PubMed:21685861 ]
External Links
ATC CodesN05AA03
AHFS Codes
  • 28:16.08.24
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (75.4 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Promazine can be increased when it is combined with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Promazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Promazine.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Promazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
AmisulprideThe risk or severity of adverse effects can be increased when Promazine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Promazine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Promazine.
AmphetaminePromazine may decrease the stimulatory activities of Amphetamine.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Promazine.
AzelastinePromazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Promazine.
BenzphetaminePromazine may decrease the stimulatory activities of Benzphetamine.
Botulinum Toxin Type APromazine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BPromazine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Promazine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Promazine.
BromocriptineThe therapeutic efficacy of Promazine can be decreased when used in combination with Bromocriptine.
BuprenorphinePromazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Promazine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promazine.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Promazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
CathinonePromazine may decrease the stimulatory activities of Cathinone.
CimetropiumPromazine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Promazine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Promazine.
CobicistatThe serum concentration of Promazine can be increased when it is combined with Cobicistat.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Promazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Promazine.
DarunavirThe serum concentration of Promazine can be increased when it is combined with Darunavir.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Promazine.
DesmopressinThe risk or severity of adverse effects can be increased when Promazine is combined with Desmopressin.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Promazine.
DextroamphetaminePromazine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Promazine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Promazine.
DofetilidePromazine may increase the QTc-prolonging activities of Dofetilide.
DonepezilDonepezil may increase the central neurotoxic activities of Promazine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Promazine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Promazine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Promazine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Promazine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Promazine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Promazine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Promazine.
EluxadolinePromazine may increase the activities of Eluxadoline.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Promazine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Promazine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Promazine.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Promazine.
EthanolPromazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Promazine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Promazine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Promazine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Promazine.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Promazine.
GalantamineGalantamine may increase the central neurotoxic activities of Promazine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Promazine is combined with Glucagon recombinant.
GoserelinGoserelin may increase the QTc-prolonging activities of Promazine.
HaloperidolPromazine may increase the QTc-prolonging activities of Haloperidol.
HydrocodonePromazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Promazine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Promazine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Promazine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Promazine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Promazine.
IvabradineIvabradine may increase the QTc-prolonging activities of Promazine.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Promazine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Promazine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Promazine.
LisdexamfetaminePromazine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Promazine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Promazine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Promazine.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Promazine 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 Promazine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Promazine.
MequitazinePromazine may increase the arrhythmogenic activities of Mequitazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Promazine.
MethamphetaminePromazine may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Promazine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Promazine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Promazine.
MetyrosinePromazine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Promazine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Promazine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Promazine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Promazine.
MirabegronThe risk or severity of adverse effects can be increased when Promazine is combined with Mirabegron.
MirtazapinePromazine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Promazine.
MorphinePromazine may increase the hypotensive activities of Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Promazine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Promazine.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Promazine.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Promazine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Promazine.
OctreotideOctreotide may increase the QTc-prolonging activities of Promazine.
OrphenadrinePromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PanobinostatThe serum concentration of Promazine can be increased when it is combined with Panobinostat.
ParaldehydePromazine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Promazine is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Promazine can be decreased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Promazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Promazine.
PhendimetrazinePromazine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Promazine.
PhenterminePromazine may decrease the stimulatory activities of Phentermine.
PorfimerPromazine may increase the photosensitizing activities of Porfimer.
Potassium ChloridePromazine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Promazine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Promazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Promazine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Promazine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Promazine.
PyrimethamineThe serum concentration of Promazine can be increased when it is combined with Pyrimethamine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Promazine.
RamosetronPromazine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Promazine.
RitonavirThe metabolism of Promazine can be decreased when combined with Ritonavir.
RivastigmineRivastigmine may increase the central neurotoxic activities of Promazine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Promazine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Promazine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Promazine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Promazine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Promazine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Promazine.
SulpirideThe risk or severity of adverse effects can be increased when Promazine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Promazine.
SuvorexantPromazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Promazine 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 Promazine resulting in a loss in efficacy.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Promazine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Promazine.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Promazine.
ThalidomidePromazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThiopentalThe risk or severity of adverse effects can be increased when Promazine is combined with Thiopental.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Promazine.
TiclopidineThe metabolism of Promazine can be decreased when combined with Ticlopidine.
TiotropiumPromazine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Promazine is combined with Topiramate.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Promazine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Promazine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Promazine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Promazine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Promazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Promazine.
Valproic AcidThe serum concentration of Valproic Acid can be increased when it is combined with Promazine.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Promazine.
VerteporfinPromazine may increase the photosensitizing activities of Verteporfin.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Promazine.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Promazine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Promazine.
ZolpidemPromazine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Govitrapong P, Chagkutip J, Turakitwanakan W, Srikiatkhachorn A: Platelet 5-HT(2A) receptors in schizophrenic patients with and without neuroleptic treatment. Psychiatry Res. 2000 Sep 25;96(1):41-50. [PubMed:10980325 ]
  4. Govitrapong P, Mukda S, Turakitwanakan W, Dumrongphol H, Chindaduangratn C, Sanvarinda Y: Platelet serotonin transporter in schizophrenic patients with and without neuroleptic treatment. Neurochem Int. 2002 Oct;41(4):209-16. [PubMed:12106771 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. 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:
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23