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Identification
NameProcaine
Accession NumberDB00721  (APRD00650)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
DescriptionA local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).
Structure
Thumb
Synonyms
2-Diethylaminoethyl p-aminobenzoate
4-aminobenzoic acid 2-diethylaminoethyl ester
Novocaine
p-Aminobenzoic acid 2-diethylaminoethyl ester
Procaina
Procainum
Vitamin H3
β-(diethylamino)ethyl 4-aminobenzoate
β-(diethylamino)ethyl p-aminobenzoate
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Novocain 20 mg/mlSolution2 %InfiltrationHospira Healthcare Corporation2001-06-012012-08-03Canada
Novocain Liq 2%Liquid2 %InfiltrationSanofi Canada, Inc.1920-12-312001-08-10Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NovocainNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Procaine hydrochloride
51-05-8
Thumb
  • InChI Key: HCBIBCJNVBAKAB-UHFFFAOYSA-N
  • Monoisotopic Mass: 272.129155633
  • Average Mass: 272.771
DBSALT000551
Categories
UNII4Z8Y51M438
CAS number59-46-1
WeightAverage: 236.3101
Monoisotopic: 236.152477894
Chemical FormulaC13H20N2O2
InChI KeyMFDFERRIHVXMIY-UHFFFAOYSA-N
InChI
InChI=1S/C13H20N2O2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3
IUPAC Name
2-(diethylamino)ethyl 4-aminobenzoate
SMILES
CCN(CC)CCOC(=O)C1=CC=C(N)C=C1
Pharmacology
IndicationUsed as a local anesthetic primarily in oral surgery
Structured Indications Not Available
PharmacodynamicsProcaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine.
Mechanism of actionProcaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
TargetKindPharmacological actionActionsOrganismUniProt ID
Sodium channel protein type 10 subunit alphaProteinyes
inhibitor
HumanQ9Y5Y9 details
Glutamate receptor ionotropic, NMDA 3AProteinyes
antagonist
HumanQ8TCU5 details
5-hydroxytryptamine receptor 3AProteinyes
antagonist
HumanP46098 details
Sodium-dependent dopamine transporterProteinyes
inhibitor
HumanQ01959 details
Neuronal acetylcholine receptor subunit alpha-2Proteinunknown
antagonist
HumanQ15822 details
DNANucleotideunknown
binder
Humannot applicabledetails
Calcium-activated potassium channel subunit alpha-1Proteinunknown
binder
HumanQ12791 details
Phospholipase A2Protein groupunknownNot AvailableHumannot applicabledetails
LysophospholipaseProteinunknownNot AvailableHumannot applicabledetails
Monoamine oxidaseProtein groupunknownNot AvailableHumannot applicabledetails
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hydrolysis by plasma esterases to PABA

Route of eliminationWith normal kidney function, the drug is excreted rapidly by tubular excretion.
Half life7.7 minutes
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Procaine Action PathwayDrug actionSMP00402
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Procaine is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when Procaine is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Procaine is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Procaine is combined with Aceprometazine.Approved
adipiplonThe risk or severity of adverse effects can be increased when Procaine is combined with adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Procaine is combined with Agomelatine.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Procaine is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Procaine is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Procaine is combined with Alphacetylmethadol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Procaine.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Procaine is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Procaine is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Procaine is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Procaine is combined with Amperozide.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Procaine is combined with Aripiprazole.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Procaine is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Procaine is combined with Asenapine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Procaine is combined with Azaperone.Vet Approved
AzelastineProcaine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Procaine is combined with Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Procaine is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Procaine is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Procaine is combined with Benzyl alcohol.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Procaine is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Procaine is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Bromazepam.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Procaine is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Procaine is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Procaine.Approved, Investigational
BuprenorphineProcaine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Procaine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Procaine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Procaine is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Procaine is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Procaine is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Procaine.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Procaine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Procaine is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Procaine is combined with Carfentanil.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Procaine is combined with Carisoprodol.Approved
CetirizineThe risk or severity of adverse effects can be increased when Procaine is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Procaine is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Procaine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Procaine is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Procaine is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Procaine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Procaine is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Procaine is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Procaine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Procaine is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Procaine is combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Procaine is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Procaine is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Procaine is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Procaine is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Procaine is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Procaine.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Procaine.Approved
CocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Procaine.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Procaine is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Procaine is combined with Cyclobenzaprine.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Procaine is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Procaine is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Procaine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Dapoxetine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when Procaine is combined with deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Procaine is combined with Desflurane.Approved
DesipramineThe risk or severity of adverse effects can be increased when Procaine is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Procaine is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Procaine is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Procaine is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Procaine is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Procaine.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Procaine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Procaine.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Procaine is combined with Dezocine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Diazepam.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Procaine is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Procaine is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Procaine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Procaine is combined with Dihydromorphine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Procaine is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Procaine is combined with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Procaine is combined with Diphenoxylate.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Procaine is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Procaine is combined with Doxepin.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Procaine is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Procaine is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Procaine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Procaine is combined with Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Procaine is combined with ECGONINE METHYL ESTER.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Procaine is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Procaine is combined with Efavirenz.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Procaine.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Procaine is combined with Entacapone.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Procaine is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Procaine is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Procaine.Approved
EthanolProcaine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Procaine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Procaine is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Procaine is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Procaine is combined with Ethyl carbamate.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Procaine is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Procaine is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Procaine is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Procaine is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Procaine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Procaine is combined with Etorphine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Procaine is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Procaine is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Procaine is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Procaine is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Procaine is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Procaine is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Procaine is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Procaine is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Procaine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Procaine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Procaine is combined with Fluspirilene.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Procaine is combined with Fluticasone Propionate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Procaine.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Procaine is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Procaine is combined with Fospropofol.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Procaine is combined with Gabapentin.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Procaine is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Procaine is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Procaine is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Procaine is combined with Glutethimide.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Procaine is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Procaine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Procaine is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Procaine is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Hexobarbital.Approved
HyaluronidaseThe risk or severity of adverse effects can be increased when Hyaluronidase is combined with Procaine.Approved, Investigational
HydrocodoneProcaine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Procaine.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Procaine is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Procaine is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Procaine is combined with Isoflurane.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Procaine is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Procaine is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Ketobemidone.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Procaine is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Procaine is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Procaine is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Procaine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Procaine is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Procaine is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Procaine is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Procaine is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Procaine is combined with Levorphanol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Procaine.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Procaine is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Procaine is combined with Lofentanil.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Procaine is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Procaine.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Procaine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Procaine is combined with Lu AA21004.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Procaine is combined with Maprotiline.Approved
MeclizineThe risk or severity of adverse effects can be increased when Procaine is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Procaine is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Procaine is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Procaine is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Procaine is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Procaine.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Procaine is combined with Mesoridazine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Procaine is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Procaine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Procaine is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Procaine is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Procaine is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Procaine is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Procaine.Approved
MethotrimeprazineProcaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Procaine is combined with Methoxyflurane.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Procaine is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Methylphenobarbital.Approved
MetyrosineProcaine may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Procaine.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Procaine is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Investigational
MirtazapineProcaine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Procaine is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Procaine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Procaine is combined with Nalbuphine.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Procaine is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Procaine is combined with Nitrous oxide.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Procaine is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Procaine is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Procaine.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Procaine is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Procaine is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Procaine is combined with Opium.Approved, Illicit
OrphenadrineProcaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Procaine is combined with Osanetant.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Oxazepam.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Procaine is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Procaine is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Oxybuprocaine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Procaine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Procaine is combined with Oxymorphone.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Paliperidone.Approved
ParaldehydeProcaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Procaine.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Procaine.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved
PerazineThe risk or severity of adverse effects can be increased when Procaine is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Procaine is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Procaine is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Procaine.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Procaine is combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Procaine is combined with Phenoxyethanol.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Procaine is combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Procaine is combined with Pimozide.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Procaine is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Procaine is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Procaine is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Procaine is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Procaine is combined with Pomalidomide.Approved
PramipexoleProcaine may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Procaine.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Procaine is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Prilocaine.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Primidone.Approved, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Procaine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Procaine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Procaine is combined with Promethazine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Procaine is combined with Proparacaine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Procaine is combined with Propofol.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Procaine is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Procaine is combined with Protriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when Procaine is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Procaine is combined with Quetiapine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Procaine is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Procaine is combined with Ramelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Procaine is combined with Remifentanil.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Procaine.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Procaine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Procaine is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Procaine is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Procaine is combined with Romifidine.Vet Approved
RopiniroleProcaine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Procaine.Approved
RotigotineProcaine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Procaine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Procaine is combined with S-Ethylisothiourea.Experimental
Sage 547The risk or severity of adverse effects can be increased when Procaine is combined with Sage 547.Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Procaine is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Procaine.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Procaine is combined with Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Procaine is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Procaine is combined with Sevoflurane.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved
StiripentolThe risk or severity of adverse effects can be increased when Procaine is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Procaine.Approved, Investigational
SulfadiazineThe therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Procaine.Approved, Vet Approved
SulfamethoxazoleThe therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Procaine.Approved
SulfisoxazoleThe therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Procaine.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Procaine.Approved
SuvorexantProcaine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Procaine is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Procaine is combined with Tasimelteon.Approved
Technetium Tc-99m tilmanoceptProcaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Procaine.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Procaine is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Procaine is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Procaine is combined with Tetrodotoxin.Investigational
ThalidomideProcaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Procaine is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Procaine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Procaine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Procaine is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Procaine is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Procaine is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Procaine is combined with Tiletamine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Procaine is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Procaine is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Procaine is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Procaine.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Procaine is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Procaine is combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Procaine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Procaine is combined with Triazolam.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Procaine is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Procaine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Procaine is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Procaine is combined with Triprolidine.Approved
Uc1010The risk or severity of adverse effects can be increased when Procaine is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Procaine.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Procaine is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Procaine is combined with Vigabatrin.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Procaine is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Procaine is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Procaine is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Procaine is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Procaine.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Zolazepam.Vet Approved
ZolpidemProcaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Procaine is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Procaine is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Procaine is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Procaine is combined with Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceUS812554
General References
  1. Gentry CL, Lukas RJ: Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes. J Pharmacol Exp Ther. 2001 Dec;299(3):1038-48. [PubMed:11714893 ]
External Links
ATC CodesS01HA05N01BA52N01BA02C05AD05
AHFS Codes
  • 24:04.04.04
  • 72:00.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.1 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9747
Blood Brain Barrier+0.9533
Caco-2 permeable+0.6291
P-glycoprotein substrateSubstrate0.587
P-glycoprotein inhibitor INon-inhibitor0.9492
P-glycoprotein inhibitor IINon-inhibitor0.9884
Renal organic cation transporterNon-inhibitor0.684
CYP450 2C9 substrateNon-substrate0.8646
CYP450 2D6 substrateNon-substrate0.6643
CYP450 3A4 substrateNon-substrate0.6456
CYP450 1A2 substrateNon-inhibitor0.6308
CYP450 2C9 inhibitorNon-inhibitor0.9312
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9294
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7918
Ames testNon AMES toxic0.6165
CarcinogenicityNon-carcinogens0.6462
BiodegradationNot ready biodegradable0.9449
Rat acute toxicity2.5160 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8728
hERG inhibition (predictor II)Non-inhibitor0.6234
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Eli lilly and co
  • Consolidated pharmaceutical group inc
  • King pharmaceuticals inc
  • Parke davis div warner lambert co
  • Pfizer laboratories div pfizer inc
  • Hospira inc
  • Abraxis pharmaceutical products
  • Bel mar laboratories inc
  • Elkins sinn div ah robins co inc
  • Gd searle llc
  • Miles laboratories inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
SolutionInfiltration2 %
LiquidInfiltration2 %
Prices
Unit descriptionCostUnit
Novocain 10% ampul2.4USD ml
Novocain 1% ampul1.79USD ml
Procaine hcl crystals1.76USD g
Nesacaine-mpf 3% vial1.34USD ml
Nesacaine-mpf 2% vial1.28USD ml
Nesacaine 2% vial0.74USD ml
Nesacaine 1% vial0.72USD ml
Chloroprocaine 3% vial0.33USD ml
Chloroprocaine 2% vial0.26USD ml
Procaine hcl 2% vial0.15USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point61 °CPhysProp
water solubility9450 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.14AVDEEF,A (1997)
logS-1.4ADME Research, USCD
pKa8.05 (at 15 °C)PERRIN,DD (1965)
Predicted Properties
PropertyValueSource
Water Solubility6.81 mg/mLALOGPS
logP2.1ALOGPS
logP1.88ChemAxon
logS-1.5ALOGPS
pKa (Strongest Basic)8.96ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area55.56 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity70.3 m3·mol-1ChemAxon
Polarizability26.81 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-000i-9200000000-44eb49be9b2baedfebddView in MoNA
1D NMR13C NMR SpectrumNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzoic acid esters. These are ester derivatives of benzoic acid.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzoic acids and derivatives
Direct ParentBenzoic acid esters
Alternative Parents
Substituents
  • Benzoate ester
  • Aminobenzoic acid or derivatives
  • Benzylether
  • Substituted aniline
  • Benzoyl
  • Aniline
  • Primary aromatic amine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity
Specific Function:
Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
Gene Name:
SCN10A
Uniprot ID:
Q9Y5Y9
Molecular Weight:
220623.605 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 ]
  3. Brau ME, Vogel W, Hempelmann G: Fundamental properties of local anesthetics: half-maximal blocking concentrations for tonic block of Na+ and K+ channels in peripheral nerve. Anesth Analg. 1998 Oct;87(4):885-9. [PubMed:9768788 ]
  4. Katalymov LL: [The effect of inhibitors of sodium permeability (novocaine and tetrodotoxin) on the trace depolarization of myelinated nerve fibers]. Fiziol Zh Im I M Sechenova. 1995 Sep;81(9):127-33. [PubMed:8581044 ]
  5. Creveling CR, Bell ME, Burke TR Jr, Chang E, Lewandowski-Lovenberg GA, Kim CH, Rice KC, Daly JW: Procaine isothiocyanate: an irreversible inhibitor of the specific binding of [3H]batrachotoxinin-A benzoate to sodium channels. Neurochem Res. 1990 Apr;15(4):441-8. [PubMed:2167458 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein phosphatase 2a binding
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism (By similarity).
Gene Name:
GRIN3A
Uniprot ID:
Q8TCU5
Molecular Weight:
125464.07 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. Hahnenkamp K, Durieux ME, Hahnenkamp A, Schauerte SK, Hoenemann CW, Vegh V, Theilmeier G, Hollmann MW: Local anaesthetics inhibit signalling of human NMDA receptors recombinantly expressed in Xenopus laevis oocytes: role of protein kinase C. Br J Anaesth. 2006 Jan;96(1):77-87. Epub 2005 Nov 18. [PubMed:16299047 ]
  4. Nishizawa N, Shirasaki T, Nakao S, Matsuda H, Shingu K: The inhibition of the N-methyl-D-aspartate receptor channel by local anesthetics in mouse CA1 pyramidal neurons. Anesth Analg. 2002 Feb;94(2):325-30, table of contents. [PubMed:11812692 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Fan P, Weight FF: Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons. Neuropharmacology. 1994 Dec;33(12):1573-9. [PubMed:7539114 ]
  2. 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
yes
Actions
inhibitor
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T: Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn Schmiedebergs Arch Pharmacol. 2000 Feb;361(2):214-20. [PubMed:10685879 ]
  2. Wilcox KM, Kimmel HL, Lindsey KP, Votaw JR, Goodman MM, Howell LL: In vivo comparison of the reinforcing and dopamine transporter effects of local anesthetics in rhesus monkeys. Synapse. 2005 Dec 15;58(4):220-8. [PubMed:16206183 ]
  3. Kiyatkin EA, Brown PL: The role of peripheral and central sodium channels in mediating brain temperature fluctuations induced by intravenous cocaine. Brain Res. 2006 Oct 30;1117(1):38-53. Epub 2006 Sep 7. [PubMed:16956595 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 Da
References
  1. Wang H, Zhang Y, Li ST: The effect of local anesthetics on the inhibition of adult muscle-type nicotinic acetylcholine receptors by nondepolarizing muscle relaxants. Eur J Pharmacol. 2010 Mar 25;630(1-3):29-33. doi: 10.1016/j.ejphar.2009.12.028. Epub 2010 Jan 4. [PubMed:20045405 ]
6. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Villar-Garea A, Fraga MF, Espada J, Esteller M: Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res. 2003 Aug 15;63(16):4984-9. [PubMed:12941824 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Voltage-gated potassium channel activity
Specific Function:
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key ...
Gene Name:
KCNMA1
Uniprot ID:
Q12791
Molecular Weight:
137558.115 Da
References
  1. Benham CD, Bolton TB, Lang RJ, Takewaki T: The mechanism of action of Ba2+ and TEA on single Ca2+-activated K+ -channels in arterial and intestinal smooth muscle cell membranes. Pflugers Arch. 1985 Feb;403(2):120-7. [PubMed:2580269 ]
8. Phospholipase A2
Kind
Protein group
Organism
Human
Pharmacological action
unknown
References
  1. Kunze H, Nahas N, Traynor JR, Wurl M: Effects of local anaesthetics on phospholipases. Biochim Biophys Acta. 1976 Jul 20;441(1):93-102. [PubMed:952985 ]
9. Lysophospholipase
Kind
Protein
Organism
Human
Pharmacological action
unknown
References
  1. Kawashima Y, Nakagawa M, Suzuki Y, Uchiyama M: The relationship between chain elongation of palmitoyl-CoA and phospholipid content in rat liver microsomes. Biochim Biophys Acta. 1976 Aug 23;441(2):173-80. [PubMed:952986 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
General Function:
Serotonin binding
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine.
Components:
NameUniProt IDDetails
Amine oxidase [flavin-containing] AP21397 Details
Amine oxidase [flavin-containing] BP27338 Details
References
  1. MacFarlane MD: Procaine HCl (Gerovital H3): a weak, reversible, fully competitive inhibitor of monoamine oxidase. Fed Proc. 1975 Jan;34(1):108-10. [PubMed:1109354 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Perez-Guillermo F, Delgado EM, Vidal CJ: Inhibition of human serum and rabbit muscle cholinesterase by local anesthetics. Biochem Pharmacol. 1987 Nov 1;36(21):3593-6. [PubMed:3675616 ]
  2. Dorokhov KE, Grigorian GL: [Binding of reversible spin-labeled inhibitors with an butyrylcholinesterase active center]. Biofizika. 1986 Sep-Oct;31(5):746-51. [PubMed:3022829 ]
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Drug created on June 13, 2005 07:24 / Updated on October 27, 2016 09:57