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cocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
local anaesthetics	723	50-36-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cocaine cocain benzoylmethylecgonine cocaine hydrochloride cocaine HCl	An 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. Molecular weight: 303.36 Formula: C17H21NO4 CLOGP: 2.57 LIPINSKI: 0 HAC: 5 HDO: 0 TPSA: 55.84 ALOGS: -1.78 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cocaine
cocain
benzoylmethylecgonine
cocaine hydrochloride
cocaine HCl

An 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.

Molecular weight: 303.36
Formula: C17H21NO4
CLOGP: 2.57
LIPINSKI: 0
HAC: 5
HDO: 0
TPSA: 55.84
ALOGS: -1.78
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	57 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.95 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	32 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1.60 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.76 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.12 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1860	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug abuse	3772.94	80.52	947	5245	71571	63411259
Toxicity to various agents	1709.94	80.52	697	5495	246553	63236277
Completed suicide	854.13	80.52	368	5824	145305	63337525
Cardio-respiratory arrest	692	80.52	248	5944	59711	63423119
Respiratory arrest	621.90	80.52	197	5995	32448	63450382
Cardiac arrest	508.20	80.52	224	5968	92321	63390509
Death	354.86	80.52	291	5901	374090	63108740
Intentional product misuse	275.22	80.52	129	6063	60788	63422042
Substance abuse	256.38	80.52	65	6127	4742	63478088
Poisoning deliberate	222.58	80.52	70	6122	11148	63471682

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug abuse	8289.54	50.96	2572	12211	96524	34845624
Toxicity to various agents	2439.91	50.96	1319	13464	199043	34743105
Intentional product misuse	767.38	50.96	377	14406	45234	34896914
Drug dependence	726.31	50.96	300	14483	23917	34918231
Coma	575.43	50.96	311	14472	45367	34896781
Cardio-respiratory arrest	556.94	50.96	325	14458	54948	34887200
Poisoning	475.93	50.96	183	14600	12043	34930105
Respiratory arrest	468.41	50.96	231	14552	27812	34914336
Miosis	441.19	50.96	162	14621	9373	34932775
Substance abuse	433.48	50.96	151	14632	7490	34934658

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug abuse	12023.23	55.11	3411	16620	159280	79565077
Toxicity to various agents	3843.69	55.11	1923	18108	419617	79304740
Cardio-respiratory arrest	1176.25	55.11	563	19468	107947	79616410
Intentional product misuse	1052.95	55.11	501	19530	94664	79629693
Respiratory arrest	1020.42	55.11	422	19609	57128	79667229
Completed suicide	1008.34	55.11	674	19357	245093	79479264
Drug dependence	913.40	55.11	354	19677	40415	79683942
Cardiac arrest	733.27	55.11	484	19547	171612	79552745
Poisoning	650.47	55.11	243	19788	25029	79699328
Miosis	644.55	55.11	214	19817	15575	79708782

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FDA Adverse Event Reporting System (Pediatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sudden infant death syndrome	17.98	15.80	3	3	53	89733

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Pharmacologic Action:

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Source	Code	Description
ATC	N01BC01	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Esters of benzoic acid
ATC	R02AD03	RESPIRATORY SYSTEM THROAT PREPARATIONS THROAT PREPARATIONS Anesthetics, local
ATC	S01HA01	SENSORY ORGANS OPHTHALMOLOGICALS LOCAL ANESTHETICS Local anesthetics
ATC	S02DA02	SENSORY ORGANS OTOLOGICALS OTHER OTOLOGICALS Analgesics and anesthetics
CHEBI has role	CHEBI:35337	analeptic
CHEBI has role	CHEBI:35524	sympathomimetic
CHEBI has role	CHEBI:35640	adrenergic uptake inhibitors
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:36333	local anesthetics
CHEBI has role	CHEBI:38633	sodium channel blockers

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Local anesthesia	indication	386761002
Conduction disorder of the heart	contraindication	44808001
Epilepsy	contraindication	84757009	DOID:1826
Thyrotoxicosis	contraindication	90739004	DOID:7997
Disorder of mucous membrane	contraindication	95351003
Acute disease of cardiovascular system	contraindication	128487001
Breastfeeding (mother)	contraindication	413712001
Hypertensive urgency	contraindication	443482000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.27	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10016407	Feb. 7, 2037	METHOD OF ADMINISTERING A LOCAL ANESTHETIC PRIOR TO PERFORMING A DIAGNOSTIC OR SURGICAL PROCEDURE ON A SUBJECT WITH HEPATIC OR RENAL IMPAIRMENT
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10149843	Feb. 7, 2037	METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10149843	Feb. 7, 2037	METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10413505	Feb. 7, 2037	METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10420760	Feb. 7, 2037	METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10857095	Feb. 7, 2037	METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10894012	Feb. 7, 2037	METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10933060	Feb. 7, 2037	METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10973811	Feb. 7, 2037	METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT
4%	GOPRELTO	GENUS LIFESCIENCES	N209963	Dec. 14, 2017	RX	SOLUTION	NASAL	10987347	Feb. 7, 2037	METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
4%	NUMBRINO	CODY LABS INC	N209575	Jan. 10, 2020	RX	SOLUTION	NASAL	Jan. 10, 2023	NEW PRODUCT

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	INHIBITOR	Ki	7.50	CHEMBL	IUPHAR
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	5.05	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.14	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.92	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.57	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	5.68	WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	5.67	WOMBAT-PK
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.47	WOMBAT-PK
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		Ki	5.71	WOMBAT-PK
Sodium- and chloride-dependent GABA transporter 1	Transporter	P30531	SC6A1_HUMAN		IC50	5.50	WOMBAT-PK

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External reference:

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ID	Source
CCA	PDB_CHEM_ID
001369	NDDF
001370	NDDF
14816004	SNOMEDCT_US
2286	IUPHAR_LIGAND_ID
2653	RXNORM
387085005	SNOMEDCT_US
4017521	VANDF
4019690	VUID
4019690	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
cocaine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	64950-362	SOLUTION	40 mg	NASAL	NDA AUTHORIZED GENERIC	35 sections
cocaine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	64950-362	SOLUTION	40 mg	NASAL	NDA AUTHORIZED GENERIC	35 sections
cocaine hydrochloride nasal	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1971	SOLUTION	40 mg	TOPICAL	NDA authorized generic	30 sections
cocaine hydrochloride nasal	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1971	SOLUTION	40 mg	TOPICAL	NDA authorized generic	30 sections
cocaine hydrochloride nasal	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1971	SOLUTION	40 mg	TOPICAL	NDA authorized generic	30 sections
GOPRELTO	HUMAN PRESCRIPTION DRUG LABEL	1	64950-359	SOLUTION	40 mg	NASAL	NDA	35 sections
GOPRELTO	HUMAN PRESCRIPTION DRUG LABEL	1	64950-359	SOLUTION	40 mg	NASAL	NDA	35 sections
NUMBRINO	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1961	SOLUTION	40 mg	NASAL	NDA	30 sections
NUMBRINO	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1961	SOLUTION	40 mg	NASAL	NDA	30 sections

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