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Identification
NameCocaine
Accession NumberDB00907  (APRD00080)
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionAn alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. [PubChem]
Structure
Thumb
Synonyms
(-)-Cocaine
(−)-cocaine
[1R-(Exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid, methyl ester
2-Methyl-3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester)
Benzoylmethylecgonine
beta-Cocain
Cocain
Cocaina
Cocaine
Cocainum
Kokain
L-Cocain
L-Cocaine
Methyl [1R-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
Methyl benzoylecgonine
Neurocaine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cocaine Hydrochloride Top Sol 40mg/mlLiquid40 mgTopicalSandoz Canada Incorporated1992-12-31Not applicableCanada
Cocaine Hydrochloride Topical Sol 10%Liquid100 mgTopicalSandoz Canada Incorporated1992-12-31Not applicableCanada
PMS-cocaine Hydrochloride Topical Sol 4%Liquid40 mgTopicalPharmascience Inc1997-03-17Not applicableCanada
PMS-cocaine Hydrochloride Topical Sol 10%Liquid100 mgTopicalPharmascience Inc1995-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cocaine HydrochlorideSolution40 mg/mLTopicalLannett Company, Inc.2008-12-01Not applicableUs
Cocaine HydrochlorideSolution100 mg/mLTopicalLannett Company, Inc.2008-12-01Not applicableUs
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cocaine hydrochloride
ThumbNot applicableDBSALT001521
Categories
UNIII5Y540LHVR
CAS number50-36-2
WeightAverage: 303.3529
Monoisotopic: 303.147058165
Chemical FormulaC17H21NO4
InChI KeyZPUCINDJVBIVPJ-LJISPDSOSA-N
InChI
InChI=1S/C17H21NO4/c1-18-12-8-9-13(18)15(17(20)21-2)14(10-12)22-16(19)11-6-4-3-5-7-11/h3-7,12-15H,8-10H2,1-2H3/t12-,13+,14-,15+/m0/s1
IUPAC Name
methyl (1R,2R,3S,5S)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
SMILES
[H][C@]12CC[C@]([H])([[email protected]]([[email protected]](C1)OC(=O)C1=CC=CC=C1)C(=O)OC)N2C
Pharmacology
IndicationFor the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.
Structured Indications Not Available
PharmacodynamicsCocaine is a local anesthetic indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.
Mechanism of actionCocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. Cocaine is the only local anesthetic with vasoconstrictive properties. This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system. Cocaine binds differentially to the dopamine, serotonin, and norepinephrine transport proteins and directly prevents the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. Its effect on dopamine levels is most responsible for the addictive property of cocaine.
TargetKindPharmacological actionActionsOrganismUniProt ID
Sodium-dependent dopamine transporterProteinyes
inhibitor
HumanQ01959 details
Sodium-dependent noradrenaline transporterProteinyes
inhibitor
HumanP23975 details
Sodium-dependent serotonin transporterProteinyes
inhibitor
HumanP31645 details
Sodium channel protein type 5 subunit alphaProteinyes
inhibitor
HumanQ14524 details
Sodium channel protein type 11 subunit alphaProteinunknown
inhibitor
HumanQ9UI33 details
Sodium channel protein type 10 subunit alphaProteinunknown
inhibitor
HumanQ9Y5Y9 details
Muscarinic acetylcholine receptor M1Proteinunknown
antagonist
HumanP11229 details
Muscarinic acetylcholine receptor M2Proteinunknown
antagonist
HumanP08172 details
Related Articles
AbsorptionCocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine. In the presence of alcohol, a further active metabolite, cocaethylene is formed, and is more toxic then cocaine itself.

SubstrateEnzymesProduct
Cocaine
norcocaineDetails
Cocaine
Not Available
BenzoylecgonineDetails
Cocaine
Not Available
CocaethyleneDetails
Route of eliminationNot Available
Half life1 hour
ClearanceNot Available
ToxicityIntense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD50 = 96 mg/kg
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Cocaine Action PathwayDrug actionSMP00395
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 Cocaine is combined with 1,1,1,2 Tetrafluoroethane.Investigational
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Cocaine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when Cocaine is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Cocaine is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Cocaine is combined with Aceprometazine.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Cocaine.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Cocaine.Approved
adipiplonThe risk or severity of adverse effects can be increased when Cocaine is combined with adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Cocaine is combined with Agomelatine.Approved, Investigational
AjmalineThe metabolism of Ajmaline can be decreased when combined with Cocaine.Approved
AlfaxaloneThe risk or severity of adverse effects can be increased when Cocaine is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Cocaine.Approved, Illicit
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Cocaine.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Cocaine.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Cocaine is combined with Alphacetylmethadol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Cocaine.Approved, Illicit, Investigational
AlprenololThe metabolism of Alprenolol can be decreased when combined with Cocaine.Approved, Withdrawn
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Cocaine.Approved, Withdrawn
AmiodaroneThe metabolism of Cocaine can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Cocaine is combined with Amisulpride.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Cocaine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Cocaine is combined with Amobarbital.Approved, Illicit
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Cocaine.Approved
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Cocaine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Cocaine is combined with Amperozide.Experimental
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Cocaine.Approved, Illicit
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Cocaine.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Cocaine.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Cocaine.Approved
AprepitantThe serum concentration of Cocaine can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Cocaine.Approved
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Cocaine.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Cocaine.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Cocaine.Approved
ArticaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Cocaine is combined with Asenapine.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Cocaine.Approved, Withdrawn
AtazanavirThe metabolism of Cocaine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Atomoxetine can be increased when it is combined with Cocaine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Azaperone.Vet Approved
AzelastineCocaine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Cocaine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Cocaine is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Cocaine is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Cocaine is combined with Benperidol.Investigational
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Cocaine.Approved
BenzocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Benzocaine.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Cocaine.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Cocaine.Approved, Withdrawn
BetaxololThe metabolism of Betaxolol can be decreased when combined with Cocaine.Approved
BexaroteneThe serum concentration of Cocaine can be decreased when it is combined with Bexarotene.Approved, Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Cocaine.Approved
BoceprevirThe metabolism of Cocaine can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Bortezomib can be decreased when combined with Cocaine.Approved, Investigational
BosentanThe serum concentration of Cocaine can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Cocaine.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Bromazepam.Approved, Illicit
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Cocaine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Cocaine is combined with Brotizolam.Approved, Withdrawn
BufuralolThe metabolism of Bufuralol can be decreased when combined with Cocaine.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Cocaine.Approved, Investigational
BuprenorphineCocaine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Cocaine.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Cocaine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Cocaine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Cocaine is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Cocaine is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Cocaine is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Cocaine.Approved, Illicit, Vet Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Cocaine.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Cocaine.Approved
CarbamazepineThe metabolism of Cocaine can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Cocaine is combined with Carfentanil.Illicit, Vet Approved
CariprazineThe metabolism of Cariprazine can be decreased when combined with Cocaine.Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Cocaine is combined with Carisoprodol.Approved
CarteololThe metabolism of Carteolol can be decreased when combined with Cocaine.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Cocaine.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Cocaine.Approved, Vet Approved
CeritinibThe serum concentration of Cocaine can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cocaine is combined with Cetirizine.Approved
CevimelineThe metabolism of Cevimeline can be decreased when combined with Cocaine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Cocaine is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Cocaine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Chloroprocaine.Approved
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Cocaine.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Cocaine.Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Cocaine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Cocaine is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Cocaine.Approved
CilostazolThe metabolism of Cilostazol can be decreased when combined with Cocaine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Cocaine.Approved, Vet Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Cocaine.Approved
CitalopramThe metabolism of Citalopram can be decreased when combined with Cocaine.Approved
ClarithromycinThe metabolism of Cocaine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Cocaine can be decreased when combined with Clemastine.Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Cocaine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Cocaine is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Cocaine is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Cocaine is combined with clomethiazole.Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Cocaine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Clonazepam.Approved, Illicit
ClonidineThe metabolism of Clonidine can be decreased when combined with Cocaine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Cocaine.Approved, Illicit
ClotrimazoleThe metabolism of Cocaine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Cocaine.Approved
CobicistatThe metabolism of Cocaine can be decreased when combined with Cobicistat.Approved
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Cocaine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Cocaine can be decreased when combined with Crizotinib.Approved
CyclizineThe risk or severity of adverse effects can be increased when Cocaine is combined with Cyclizine.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Cocaine.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Cocaine.Approved, Investigational
CyclosporineThe metabolism of Cocaine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Cocaine is combined with Cyproheptadine.Approved
DabrafenibThe serum concentration of Cocaine can be decreased when it is combined with Dabrafenib.Approved
DantroleneThe risk or severity of adverse effects can be increased when Cocaine is combined with Dantrolene.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Cocaine.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Cocaine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Cocaine is combined with Dapoxetine.Investigational
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Cocaine.Approved, Investigational
DarunavirThe metabolism of Cocaine can be decreased when combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Cocaine.Approved
DasatinibThe serum concentration of Cocaine can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Cocaine.Approved
DeferasiroxThe serum concentration of Cocaine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Delavirdine can be decreased when combined with Cocaine.Approved
deramciclaneThe risk or severity of adverse effects can be increased when Cocaine is combined with deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Cocaine is combined with Desflurane.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Cocaine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Cocaine is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Cocaine is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Detomidine.Vet Approved
DexamethasoneThe serum concentration of Cocaine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Cocaine is combined with Dexbrompheniramine.Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Cocaine.Approved, Illicit, Withdrawn
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Cocaine.Approved, Vet Approved
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Cocaine.Approved
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Cocaine.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Cocaine.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Cocaine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Cocaine.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Cocaine is combined with Dezocine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Cocaine.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Cocaine is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Cocaine.Approved, Illicit
DihydroergotamineThe metabolism of Cocaine can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Cocaine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Cocaine is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Cocaine.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Cocaine is combined with Dimenhydrinate.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Cocaine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Cocaine is combined with Diphenoxylate.Approved, Illicit
DolasetronThe metabolism of Dolasetron can be decreased when combined with Cocaine.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Cocaine.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Cocaine.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Cocaine.Approved
DoramectinThe risk or severity of adverse effects can be increased when Cocaine is combined with Doramectin.Vet Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Cocaine.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Cocaine.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Cocaine.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Cocaine.Approved, Investigational
DoxycyclineThe metabolism of Cocaine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Cocaine is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Illicit
DronedaroneThe metabolism of Dronedarone can be decreased when combined with Cocaine.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Cocaine is combined with Drotebanol.Experimental, Illicit
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Cocaine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Cocaine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Cocaine is combined with Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Cocaine is combined with ECGONINE METHYL ESTER.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Cocaine is combined with Ecopipam.Investigational
EfavirenzThe serum concentration of Cocaine can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Cocaine.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Cocaine.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Cocaine.Approved, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Cocaine.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Cocaine.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Cocaine is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Cocaine can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Cocaine.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Cocaine.Approved, Investigational
ErythromycinThe metabolism of Cocaine can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Cocaine.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Cocaine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Cocaine.Investigational
EstazolamThe risk or severity of adverse effects can be increased when Cocaine is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Cocaine.Approved
EthanolCocaine 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 Cocaine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Cocaine is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Cocaine is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Cocaine is combined with Ethyl carbamate.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Cocaine is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Cocaine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Cocaine is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Cocaine is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Cocaine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Etoperidone.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Cocaine.Approved, Investigational
EtorphineThe risk or severity of adverse effects can be increased when Cocaine is combined with Etorphine.Illicit, Vet Approved
EtravirineThe serum concentration of Cocaine can be decreased when it is combined with Etravirine.Approved
EzogabineThe risk or severity of adverse effects can be increased when Cocaine is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Cocaine is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Cocaine.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cocaine.Approved
FexofenadineThe risk or severity of adverse effects can be increased when Cocaine is combined with Fexofenadine.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Cocaine.Approved, Investigational
FlecainideThe metabolism of Flecainide can be decreased when combined with Cocaine.Approved, Withdrawn
FlibanserinThe risk or severity of adverse effects can be increased when Cocaine is combined with Flibanserin.Approved
FluconazoleThe metabolism of Cocaine can be decreased when combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Fludiazepam.Approved, Illicit
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Cocaine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Cocaine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Cocaine.Approved, Withdrawn
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Cocaine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Cocaine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Cocaine is combined with Fluspirilene.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Cocaine is combined with Fluticasone Propionate.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Cocaine.Approved
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Cocaine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Cocaine.Approved, Investigational
FosamprenavirThe metabolism of Cocaine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Cocaine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Cocaine can be increased when combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Cocaine is combined with Fospropofol.Approved, Illicit
Fusidic AcidThe serum concentration of Cocaine can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Cocaine is combined with Gabapentin.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Cocaine is combined with gabapentin enacarbil.Approved
GalantamineThe metabolism of Galantamine can be decreased when combined with Cocaine.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Cocaine is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GefitinibThe metabolism of Gefitinib can be decreased when combined with Cocaine.Approved, Investigational
GepironeThe risk or severity of adverse effects can be increased when Cocaine is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Cocaine is combined with Glutethimide.Approved, Illicit
GranisetronThe metabolism of Granisetron can be decreased when combined with Cocaine.Approved, Investigational
GuanfacineThe risk or severity of adverse effects can be increased when Cocaine is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Cocaine.Approved, Illicit, Withdrawn
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Cocaine.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Cocaine.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Cocaine.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Cocaine is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Cocaine is combined with Hexobarbital.Approved
HyaluronidaseThe risk or severity of adverse effects can be increased when Hyaluronidase is combined with Cocaine.Approved, Investigational
HydrocodoneCocaine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Cocaine.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Cocaine.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Cocaine.Approved
IdelalisibThe serum concentration of Cocaine can be increased when it is combined with Idelalisib.Approved
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Cocaine.Approved
ImatinibThe metabolism of Imatinib can be decreased when combined with Cocaine.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Cocaine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Cocaine is combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Cocaine can be decreased when combined with Indinavir.Approved
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Cocaine.Approved
Ioflupane I-123Cocaine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.Approved
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Cocaine.Approved
IsavuconazoniumThe metabolism of Cocaine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Cocaine.Approved, Vet Approved
IsradipineThe metabolism of Cocaine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Cocaine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cocaine can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Cocaine.Approved
KetamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Cocaine is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Ketobemidone.Approved
KetoconazoleThe metabolism of Cocaine can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Cocaine.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Cocaine is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Cocaine is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Cocaine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Cocaine is combined with Levocetirizine.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Cocaine.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Cocaine is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Cocaine.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Cocaine.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Cocaine.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Cocaine.Approved
LithiumThe risk or severity of adverse effects can be increased when Cocaine is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Cocaine is combined with Lofentanil.Illicit
LomustineThe metabolism of Lomustine can be decreased when combined with Cocaine.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Cocaine.Approved
LopinavirThe metabolism of Cocaine can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Cocaine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Cocaine.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Cocaine.Approved
LovastatinThe metabolism of Cocaine can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Cocaine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Cocaine is combined with Lu AA21004.Investigational
LuliconazoleThe serum concentration of Cocaine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Cocaine can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Vet Approved
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Cocaine.Approved
MeclizineThe risk or severity of adverse effects can be increased when Cocaine is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Cocaine is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Melperone.Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Cocaine.Investigational, Withdrawn
MepivacaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Cocaine.Approved, Illicit
MequitazineThe serum concentration of Mequitazine can be increased when it is combined with Cocaine.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Cocaine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Cocaine is combined with Metaxalone.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Cocaine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Cocaine is combined with Methadyl Acetate.Approved, Illicit
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Cocaine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Cocaine is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Cocaine is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Cocaine.Approved
MethotrimeprazineCocaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Cocaine.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Cocaine is combined with Methsuximide.Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Cocaine.Approved, Investigational
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Cocaine.Approved
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Cocaine.Approved, Illicit, Withdrawn
MetoclopramideThe metabolism of Metoclopramide can be decreased when combined with Cocaine.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Cocaine.Approved, Investigational
MetyrosineCocaine may increase the sedative activities of Metyrosine.Approved
MexiletineThe metabolism of Mexiletine can be decreased when combined with Cocaine.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Cocaine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Cocaine.Approved, Illicit
MifepristoneThe serum concentration of Cocaine can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Cocaine is combined with Milnacipran.Approved
MinaprineThe metabolism of Minaprine can be decreased when combined with Cocaine.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Investigational
MirabegronThe metabolism of Mirabegron can be decreased when combined with Cocaine.Approved
MirtazapineCocaine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Cocaine can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Cocaine.Approved
ModafinilThe serum concentration of Cocaine can be decreased when it is combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Molindone.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Cocaine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Investigational
NafcillinThe serum concentration of Cocaine can be decreased when it is combined with Nafcillin.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Cocaine.Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Cocaine.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Cocaine.Approved, Investigational
NefazodoneThe metabolism of Cocaine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Cocaine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Cocaine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Cocaine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Cocaine.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Cocaine.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Cocaine.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Cocaine.Approved
NilotinibThe metabolism of Cocaine can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Nitrazepam.Approved
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Cocaine.Approved, Vet Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Cocaine is combined with Nitrous oxide.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Normethadone.Approved, Illicit
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Cocaine.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Cocaine.Approved, Investigational
OlaparibThe metabolism of Cocaine can be decreased when combined with Olaparib.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Cocaine is combined with Olopatadine.Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Cocaine.Approved
OpiumThe risk or severity of adverse effects can be increased when Cocaine is combined with Opium.Approved, Illicit
OrphenadrineCocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Cocaine is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Cocaine can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Cocaine.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Cocaine is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Cocaine.Approved
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Cocaine.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Cocaine.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Cocaine can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Paliperidone.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Cocaine.Approved, Investigational
ParaldehydeCocaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe metabolism of Paroxetine can be decreased when combined with Cocaine.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Cocaine.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Cocaine.Approved
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Cocaine.Approved, Vet Approved
PentobarbitalThe metabolism of Cocaine can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved
PerazineThe risk or severity of adverse effects can be increased when Cocaine is combined with Perazine.Investigational
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Cocaine.Approved
PerospironeThe risk or severity of adverse effects can be increased when Cocaine is combined with Perospirone.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Cocaine.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Cocaine.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Cocaine.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Cocaine.Approved, Withdrawn
PhenobarbitalThe metabolism of Cocaine can be increased when combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Cocaine is combined with Phenoxyethanol.Approved
PhenytoinThe metabolism of Cocaine can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cocaine.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Cocaine.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Cocaine is combined with Pipamperone.Approved
PiperazineThe metabolism of Piperazine can be decreased when combined with Cocaine.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Cocaine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Cocaine is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Cocaine is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Cocaine is combined with Pomalidomide.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Cocaine.Approved
PosaconazoleThe metabolism of Cocaine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleCocaine may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Cocaine.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Cocaine is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Cocaine.Approved
PrimidoneThe metabolism of Cocaine can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideThe metabolism of Procainamide can be decreased when combined with Cocaine.Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Cocaine.Approved, Investigational, Vet Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Cocaine.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Cocaine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Cocaine.Approved, Vet Approved
PromethazineThe metabolism of Promethazine can be decreased when combined with Cocaine.Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Cocaine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Cocaine.Approved, Vet Approved
PropofolThe metabolism of Propofol can be decreased when combined with Cocaine.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Propoxycaine.Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Cocaine.Approved, Investigational
ProtriptylineThe metabolism of Protriptyline can be decreased when combined with Cocaine.Approved
PSD502The risk or severity of adverse effects can be increased when Cocaine is combined with PSD502.Investigational
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Cocaine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Quazepam.Approved, Illicit
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Cocaine.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Cocaine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Cocaine is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Cocaine is combined with Ramelteon.Approved, Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Cocaine.Approved
RanolazineThe metabolism of Cocaine can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Cocaine.Approved
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Cocaine.Approved, Withdrawn
repinotanThe metabolism of repinotan can be decreased when combined with Cocaine.Investigational
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Cocaine.Approved
RifabutinThe metabolism of Cocaine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Cocaine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cocaine can be increased when combined with Rifapentine.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Cocaine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Cocaine is combined with Ritanserin.Investigational
RitonavirThe metabolism of Cocaine can be decreased when combined with Ritonavir.Approved, Investigational
RomifidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Romifidine.Vet Approved
RopiniroleCocaine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Cocaine.Approved
RotigotineCocaine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cocaine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Cocaine is combined with S-Ethylisothiourea.Experimental
Sage 547The risk or severity of adverse effects can be increased when Cocaine is combined with Sage 547.Investigational
SaquinavirThe metabolism of Cocaine can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Cocaine.Approved, Vet Approved
SertindoleThe metabolism of Sertindole can be decreased when combined with Cocaine.Approved, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Cocaine.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Cocaine is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Sildenafil can be decreased when combined with Cocaine.Approved, Investigational
SiltuximabThe serum concentration of Cocaine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Cocaine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Cocaine.Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved
SparteineThe metabolism of Sparteine can be decreased when combined with Cocaine.Experimental
St. John's WortThe serum concentration of Cocaine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Cocaine can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Cocaine.Approved, Investigational
SulfisoxazoleThe metabolism of Cocaine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Cocaine.Approved
SuvorexantCocaine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Cocaine resulting in a loss in efficacy.Approved
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Cocaine.Approved, Investigational
TandospironeThe risk or severity of adverse effects can be increased when Cocaine is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Cocaine is combined with Tasimelteon.Approved
Technetium Tc-99m tilmanoceptCocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Cocaine.Investigational, Withdrawn
TelaprevirThe metabolism of Cocaine can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Cocaine can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Cocaine.Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Cocaine.Withdrawn
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Cocaine.Investigational
TetrabenazineThe serum concentration of Tetrabenazine can be increased when it is combined with Cocaine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Cocaine is combined with Tetrodotoxin.Investigational
ThalidomideCocaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Theophylline can be decreased when combined with Cocaine.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Cocaine is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Cocaine.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Cocaine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Cocaine is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Cocaine is combined with Tiapride.Investigational
TiclopidineThe metabolism of Ticlopidine can be decreased when combined with Cocaine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tiletamine.Vet Approved
TimololThe metabolism of Timolol can be decreased when combined with Cocaine.Approved
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Cocaine.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Cocaine.Approved, Investigational
TizanidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tizanidine.Approved
TocilizumabThe serum concentration of Cocaine can be decreased when it is combined with Tocilizumab.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Cocaine is combined with Tolcapone.Approved, Withdrawn
TolterodineThe metabolism of Tolterodine can be decreased when combined with Cocaine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Cocaine is combined with Topiramate.Approved
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Cocaine.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Cocaine.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Cocaine is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Cocaine.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Cocaine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Cocaine.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Cocaine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Cocaine.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Cocaine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Triprolidine.Approved
Uc1010The risk or severity of adverse effects can be increased when Cocaine is combined with Uc1010.Investigational
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Cocaine.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Cocaine.Approved, Investigational
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Cocaine.Approved
VerapamilThe metabolism of Cocaine can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Cocaine is combined with Vigabatrin.Approved
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Cocaine.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Cocaine.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Cocaine.Approved, Investigational
VoriconazoleThe metabolism of Cocaine can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe serum concentration of Vortioxetine can be increased when it is combined with Cocaine.Approved
XylazineThe risk or severity of adverse effects can be increased when Cocaine is combined with Xylazine.Vet Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Cocaine.Approved, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Cocaine.Approved
ZaleplonThe risk or severity of adverse effects can be increased when Cocaine is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Cocaine is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Cocaine is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Cocaine can be decreased when combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Cocaine is combined with Zolazepam.Vet Approved
ZolpidemCocaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Cocaine is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Cocaine is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Cocaine is combined with Zotepine.Approved
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Cocaine.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Nobuyuki Shigetoh, Hiroshi Nakayama, Jinsei Miyazaki, Tadayasu Mitsumata, “Labelling colors for detecting cocaine or methamphetamine, method of preparing the same and detector for cocaine or methamphetamine.” U.S. Patent US5571727, issued October, 1981.

US5571727
General References
  1. Siegel RK, Elsohly MA, Plowman T, Rury PM, Jones RT: Cocaine in herbal tea. JAMA. 1986 Jan 3;255(1):40. [PubMed:3940302 ]
  2. Volkow ND, Wang GJ, Fischman MW, Foltin R, Fowler JS, Franceschi D, Franceschi M, Logan J, Gatley SJ, Wong C, Ding YS, Hitzemann R, Pappas N: Effects of route of administration on cocaine induced dopamine transporter blockade in the human brain. Life Sci. 2000 Aug 11;67(12):1507-15. [PubMed:10983846 ]
  3. Dimitrijevic N, Dzitoyeva S, Manev H: An automated assay of the behavioral effects of cocaine injections in adult Drosophila. J Neurosci Methods. 2004 Aug 30;137(2):181-4. [PubMed:15262059 ]
  4. Uz T, Akhisaroglu M, Ahmed R, Manev H: The pineal gland is critical for circadian Period1 expression in the striatum and for circadian cocaine sensitization in mice. Neuropsychopharmacology. 2003 Dec;28(12):2117-23. [PubMed:12865893 ]
  5. McClung CA, Sidiropoulou K, Vitaterna M, Takahashi JS, White FJ, Cooper DC, Nestler EJ: Regulation of dopaminergic transmission and cocaine reward by the Clock gene. Proc Natl Acad Sci U S A. 2005 Jun 28;102(26):9377-81. Epub 2005 Jun 20. [PubMed:15967985 ]
External Links
ATC CodesN01BC01S01HA01R02AD03S02DA02
AHFS Codes
  • 52:16.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (104 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8644
Blood Brain Barrier+0.8805
Caco-2 permeable+0.7654
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor IInhibitor0.8168
P-glycoprotein inhibitor IINon-inhibitor0.893
Renal organic cation transporterInhibitor0.6182
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6856
CYP450 1A2 substrateNon-inhibitor0.8627
CYP450 2C9 inhibitorNon-inhibitor0.9341
CYP450 2D6 inhibitorNon-inhibitor0.5614
CYP450 2C19 inhibitorNon-inhibitor0.9383
CYP450 3A4 inhibitorNon-inhibitor0.9237
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9408
Ames testNon AMES toxic0.7437
CarcinogenicityNon-carcinogens0.9585
BiodegradationNot ready biodegradable0.5319
Rat acute toxicity2.6387 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8463
hERG inhibition (predictor II)Non-inhibitor0.8042
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
SolutionTopical100 mg/mL
SolutionTopical40 mg/mL
LiquidTopical40 mg
LiquidTopical100 mg
Prices
Unit descriptionCostUnit
Cocaine hydrochloride powder68.44USD g
Cocaine 10% solution10.68USD ml
Cocaine 4% solution6.22USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point98 °CPhysProp
water solubility1800 mg/L (at 22 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.30HANSCH,C ET AL. (1995)
logS-2.23ADME Research, USCD
pKa8.61 (at 15 °C)MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility5.03 mg/mLALOGPS
logP1.97ALOGPS
logP2.28ChemAxon
logS-1.8ALOGPS
pKa (Strongest Basic)8.85ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area55.84 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity81.16 m3·mol-1ChemAxon
Polarizability32.36 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (2.96 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
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
  • Tropane alkaloid
  • Piperidinecarboxylic acid
  • Benzylether
  • Benzoyl
  • N-alkylpyrrolidine
  • Piperidine
  • Dicarboxylic acid or derivatives
  • Methyl ester
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

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. Wilson JM, Levey AI, Bergeron C, Kalasinsky K, Ang L, Peretti F, Adams VI, Smialek J, Anderson WR, Shannak K, Deck J, Niznik HB, Kish SJ: Striatal dopamine, dopamine transporter, and vesicular monoamine transporter in chronic cocaine users. Ann Neurol. 1996 Sep;40(3):428-39. [PubMed:8797532 ]
  2. Kim DI, Schweri MM, Deutsch HM: Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. J Med Chem. 2003 Apr 10;46(8):1456-64. [PubMed:12672245 ]
  3. Rothman RB, Baumann MH, Dersch CM, Appel J, Houghten RA: Discovery of novel peptidic dopamine transporter ligands by screening a positional scanning combinatorial hexapeptide library. Synapse. 1999 Sep 1;33(3):239-46. [PubMed:10420171 ]
  4. Carrera MR, Meijler MM, Janda KD: Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004 Oct 1;12(19):5019-30. [PubMed:15351386 ]
  5. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Galli A, DeFelice LJ, Duke BJ, Moore KR, Blakely RD: Sodium-dependent norepinephrine-induced currents in norepinephrine-transporter-transfected HEK-293 cells blocked by cocaine and antidepressants. J Exp Biol. 1995 Oct;198(Pt 10):2197-212. [PubMed:7500004 ]
  2. Burchett SA, Bannon MJ: Serotonin, dopamine and norepinephrine transporter mRNAs: heterogeneity of distribution and response to 'binge' cocaine administration. Brain Res Mol Brain Res. 1997 Oct 3;49(1-2):95-102. [PubMed:9387868 ]
  3. Zhao Y, Sun L: Perinatal cocaine exposure reduces myocardial norepinephrine transporter function in the neonatal rat. Neurotoxicol Teratol. 2004 May-Jun;26(3):443-50. [PubMed:15113605 ]
  4. Carrera MR, Meijler MM, Janda KD: Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004 Oct 1;12(19):5019-30. [PubMed:15351386 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Patkar AA, Berrettini WH, Hoehe M, Thornton CC, Gottheil E, Hill K, Weinstein SP: Serotonin transporter polymorphisms and measures of impulsivity, aggression, and sensation seeking among African-American cocaine-dependent individuals. Psychiatry Res. 2002 Jun 1;110(2):103-15. [PubMed:12057823 ]
  2. Barker EL, Moore KR, Rakhshan F, Blakely RD: Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter. J Neurosci. 1999 Jun 15;19(12):4705-17. [PubMed:10366604 ]
  3. Corey JL, Quick MW, Davidson N, Lester HA, Guastella J: A cocaine-sensitive Drosophila serotonin transporter: cloning, expression, and electrophysiological characterization. Proc Natl Acad Sci U S A. 1994 Feb 1;91(3):1188-92. [PubMed:8302852 ]
  4. Carrera MR, Meijler MM, Janda KD: Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004 Oct 1;12(19):5019-30. [PubMed:15351386 ]
  5. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function:
This protein 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 Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
References
  1. Antzelevitch C: Brugada syndrome. Pacing Clin Electrophysiol. 2006 Oct;29(10):1130-59. [PubMed:17038146 ]
  2. Satish OS, Yeh KH, Wen MS: Brugada syndrome--an update. Chang Gung Med J. 2005 Feb;28(2):69-76. [PubMed:15880981 ]
  3. Wright SN, Wang SY, Xiao YF, Wang GK: State-dependent cocaine block of sodium channel isoforms, chimeras, and channels coexpressed with the beta1 subunit. Biophys J. 1999 Jan;76(1 Pt 1):233-45. [PubMed:9876137 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity
Specific Function:
This protein 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. It is a tetrodotoxin-resistant sodium channel isoform. Also involved, with ...
Gene Name:
SCN11A
Uniprot ID:
Q9UI33
Molecular Weight:
204919.66 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Carrera MR, Meijler MM, Janda KD: Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004 Oct 1;12(19):5019-30. [PubMed:15351386 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Carrera MR, Meijler MM, Janda KD: Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004 Oct 1;12(19):5019-30. [PubMed:15351386 ]
  2. Sharkey J, Ritz MC, Schenden JA, Hanson RC, Kuhar MJ: Cocaine inhibits muscarinic cholinergic receptors in heart and brain. J Pharmacol Exp Ther. 1988 Sep;246(3):1048-52. [PubMed:3047364 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Ladona MG, Gonzalez ML, Rane A, Peter RM, de la Torre R: Cocaine metabolism in human fetal and adult liver microsomes is related to cytochrome P450 3A expression. Life Sci. 2000 Dec 15;68(4):431-43. [PubMed:11205892 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Grundemann D, Koster S, Kiefer N, Breidert T, Engelhardt M, Spitzenberger F, Obermuller N, Schomig E: Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. J Biol Chem. 1998 Nov 20;273(47):30915-20. [PubMed:9812985 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23