Identification

Name
Procaine
Accession Number
DB00721  (APRD00650, DB05342)
Type
Small Molecule
Groups
Approved, Investigational, Vet Approved
Description

A 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). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients (Clinical Trial NCT00299897.

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
Product Ingredients
IngredientUNIICASInChI Key
Procaine hydrochloride95URV01IDQ51-05-8HCBIBCJNVBAKAB-UHFFFAOYSA-N
Procaine nitrateT824SI1PU16192-92-3XUXYDJABBYUMRY-UHFFFAOYSA-N
Procaine phosphateA18LHT9ZXJ54812-66-7NPBISBZNYVWJOL-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Novocain 20 mg/mlSolution2 %InfiltrationHospira, Inc.2001-06-012012-08-03Canada
Novocain Liq 2%Liquid2 %InfiltrationSanofi1920-12-312001-08-10Canada
International/Other Brands
Novocain
Categories
UNII
4Z8Y51M438
CAS number
59-46-1
Weight
Average: 236.3101
Monoisotopic: 236.152477894
Chemical Formula
C13H20N2O2
InChI Key
MFDFERRIHVXMIY-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

Indication

Used as a local anesthetic primarily in oral surgery

Structured Indications
Not Available
Pharmacodynamics

Procaine 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 action

Procaine 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.

TargetActionsOrganism
ASodium channel protein type 10 subunit alpha
inhibitor
Human
AGlutamate receptor ionotropic, NMDA 3A
antagonist
Human
A5-hydroxytryptamine receptor 3A
antagonist
Human
ASodium-dependent dopamine transporter
inhibitor
Human
UNeuronal acetylcholine receptor subunit alpha-2
antagonist
Human
UDNA
binder
Human
UCalcium-activated potassium channel
binder
Human
UPhospholipase A2Not AvailableHuman
ULysophospholipaseNot AvailableHuman
UMonoamine oxidaseNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hydrolysis by plasma esterases to PABA

Route of elimination

With normal kidney function, the drug is excreted rapidly by tubular excretion.

Half life

7.7 minutes

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Procaine Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
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
AlaproclateThe risk or severity of adverse effects can be increased when Procaine is combined with Alaproclate.Experimental
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 Alfentanil is combined with Procaine.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Procaine is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Procaine is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Procaine is combined with Alphaprodine.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 Amobarbital is combined with Procaine.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 Aripiprazole is combined with Procaine.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 Asenapine is combined with Procaine.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
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
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 Bromazepam is combined with Procaine.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Procaine is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Procaine is combined with Bromperidol.Investigational
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
CanertinibThe risk or severity of adverse effects can be increased when Procaine is combined with Canertinib.Investigational
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
ClopenthixolThe risk or severity of adverse effects can be increased when Procaine is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Procaine.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Procaine is combined with Clothiapine.Experimental
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 Cyclobenzaprine is combined with Procaine.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 Desflurane is combined with Procaine.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 Diazepam is combined with Procaine.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Procaine is combined with Diethyl ether.Experimental
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 Dihydrocodeine is combined with Procaine.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 Diphenhydramine is combined with Procaine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Procaine.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Procaine is combined with Dixyrazine.Experimental
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
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
EltanoloneThe risk or severity of adverse effects can be increased when Procaine is combined with Eltanolone.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 Estazolam is combined with Procaine.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 chlorideThe risk or severity of adverse effects can be increased when Procaine is combined with Ethyl chloride.Experimental
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 Fentanyl is combined with Procaine.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
FluanisoneThe risk or severity of adverse effects can be increased when Procaine is combined with Fluanisone.Experimental
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 Flupentixol is combined with Procaine.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 Gabapentin is combined with Procaine.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 Gamma Hydroxybutyric Acid is combined with Procaine.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
IndiplonThe risk or severity of adverse effects can be increased when Procaine is combined with Indiplon.Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Procaine.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Procaine.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 Levorphanol is combined with Procaine.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
LoprazolamThe risk or severity of adverse effects can be increased when Procaine is combined with Loprazolam.Experimental
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
LormetazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Lormetazepam.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Procaine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Procaine.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
MebicarThe risk or severity of adverse effects can be increased when Procaine is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Procaine is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Procaine is combined with Medazepam.Experimental
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
MeptazinolThe risk or severity of adverse effects can be increased when Procaine is combined with Meptazinol.Experimental
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
MethylecgonineThe risk or severity of adverse effects can be increased when Procaine is combined with Methylecgonine.Experimental
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 Nalbuphine is combined with Procaine.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 Nitrazepam is combined with Procaine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Procaine.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Procaine is combined with Norflurane.Investigational
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 Oxazepam is combined with Procaine.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Procaine is combined with Oxethazaine.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 Oxymorphone is combined with Procaine.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Procaine.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
PenfluridolThe risk or severity of adverse effects can be increased when Procaine is combined with Penfluridol.Experimental
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 Perphenazine is combined with Procaine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Procaine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Procaine is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Procaine is combined with Phenibut.Experimental
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Procaine.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Procaine is combined with Phenoperidine.Experimental
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 Pimozide is combined with Procaine.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
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
PropanididThe risk or severity of adverse effects can be increased when Procaine is combined with Propanidid.Experimental
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 Propofol is combined with Procaine.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
ProxibarbalThe risk or severity of adverse effects can be increased when Procaine is combined with Proxibarbal.Experimental
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 Quazepam is combined with Procaine.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Procaine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Procaine is combined with Quinisocaine.Experimental
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 Remifentanil is combined with Procaine.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 Risperidone is combined with Procaine.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
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
SepranoloneThe risk or severity of adverse effects can be increased when Procaine is combined with Sepranolone.Investigational
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 Sevoflurane is combined with Procaine.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
SultoprideThe risk or severity of adverse effects can be increased when Procaine is combined with Sultopride.Experimental
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
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Procaine is combined with Tetrahydropalmatine.Investigational
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.Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Procaine.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.Approved, Investigational
TiletamineThe risk or severity of adverse effects can be increased when Procaine is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Procaine is combined with Tilidine.Experimental
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 Triazolam is combined with Procaine.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Procaine is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Procaine is combined with Trichloroethylene.Experimental
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Procaine.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Procaine is combined with Trifluperidol.Experimental
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
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
VeraliprideThe risk or severity of adverse effects can be increased when Procaine is combined with Veralipride.Experimental
VigabatrinThe risk or severity of adverse effects can be increased when Procaine is combined with Vigabatrin.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Procaine is combined with Vinyl ether.Experimental
VortioxetineThe risk or severity of adverse effects can be increased when Procaine is combined with Vortioxetine.Approved
XenonThe risk or severity of adverse effects can be increased when Procaine is combined with Xenon.Experimental
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 Zaleplon is combined with Procaine.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 Zopiclone is combined with Procaine.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 Zuclopenthixol is combined with Procaine.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference
US812554
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
Human Metabolome Database
HMDB14859
KEGG Drug
D08422
KEGG Compound
C07375
PubChem Compound
4914
PubChem Substance
46507724
ChemSpider
4745
BindingDB
64452
ChEBI
8430
ChEMBL
CHEMBL569
Therapeutic Targets Database
DAP000296
PharmGKB
PA451110
IUPHAR
4291
Guide to Pharmacology
GtP Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Procaine
ATC Codes
S01HA05 — ProcaineN01BA52 — Procaine, combinationsN01BA02 — ProcaineC05AD05 — Procaine
AHFS Codes
  • 24:04.04.04
  • 72:00.00
PDB Entries
Not Available
FDA label
Not Available
MSDS
Download (73.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentOsteomyelitis1
1, 2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2Not Yet RecruitingTreatmentNasopharyngeal Neoplasms / Vesicular Stomatitis1
2Unknown StatusTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2Unknown StatusTreatmentHuman Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableRecruitingPreventionArterial Hypotension1

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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)61 °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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-000i-9200000000-44eb49be9b2baedfebdd
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-000i-0090000000-7c7d7173da9393c2d059
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-0910000000-279febfbe258e2ce2807
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0uk9-0900000000-997e743a0702a7a5b54f
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00di-2900000000-39c6b968e8d17c932e10
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00dl-9700000000-157dc94224e66c932ae8
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-0w29-0900000000-050d794abd6d3a7e685d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01w0-1940000000-d4d5195f000d2d633df7
13C NMR Spectrum1D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzoic acid esters. These are ester derivatives of benzoic acid.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
Benzoic acid esters
Alternative Parents
Aminobenzoic acids and derivatives / Benzoyl derivatives / Aniline and substituted anilines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Primary amines / Organopnictogen compounds / Organooxygen compounds
show 2 more
Substituents
Aminobenzoic acid or derivatives / Benzoate ester / Benzoyl / Aniline or substituted anilines / Amino acid or derivatives / Tertiary aliphatic amine / Tertiary amine / Carboxylic acid ester / Carboxylic acid derivative / Monocarboxylic acid or derivatives
show 10 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
tertiary amino compound, substituted aniline, benzoate ester (CHEBI:8430)

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 acro...
Gene Name
SCN10A
Uniprot ID
Q9Y5Y9
Uniprot Name
Sodium channel protein type 10 subunit alpha
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 ...
Gene Name
GRIN3A
Uniprot ID
Q8TCU5
Uniprot Name
Glutamate receptor ionotropic, NMDA 3A
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-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
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
Uniprot Name
Sodium-dependent dopamine transporter
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
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-2
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 activati...
Gene Name
KCNMA1
Uniprot ID
Q12791
Uniprot Name
Calcium-activated potassium channel subunit alpha-1
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...

Components:
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
Uniprot Name
Cholinesterase
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]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:43