Cocaine

NERVOUS SYSTEM

Key facts

Cocaine is an ofp drug catalogued in DrugCentral. It was first approved by the YEAR INTRODUCED in 1860. DrugCentral lists 24 molecular targets, including SLC6A3, Slc6a3 and Slc6a4. Recorded indications include Local anesthesia.

• Approval status: ofp (first approved 1860 by the YEAR INTRODUCED).
• Molecular targets: SLC6A3, Slc6a3, Slc6a4 and SLC6A3 (24 listed in DrugCentral).
• Indications: Local anesthesia.
• ATC code: N01BC01 (Esters of benzoic acid).
• Molecular formula: C17H21NO4; molecular weight 303.36 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Local anesthesia

Contraindications (7)

• Acute disease of cardiovascular system
• Breastfeeding (mother)
• Conduction disorder of the heart
• Disorder of mucous membrane
• Epilepsy
• Hypertensive urgency
• Thyrotoxicosis

Mechanism & targets

Molecular targets (24)

Target	Gene	Action	Activity
Sodium-dependent dopamine transporter	SLC6A3	inhibitor	Ki 7.50
Sodium-dependent dopamine transporter	Slc6a3	unknown	Ki 7.49
Sodium-dependent serotonin transporter	Slc6a4	unknown	Ki 7.35
Dopamine transporter	SLC6A3	unknown	IC50 7.19
Dopamine transporter	SLC6A3	unknown	IC50 7.02
Transporter	Slc6a2	unknown	Ki 6.97
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 6.92
Sodium-dependent dopamine transporter	Slc6a3	unknown	IC50 6.70
5-hydroxytryptamine receptor 3A	HTR3A	unknown	Ki 5.71
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 5.68
Histamine H1 receptor	HRH1	unknown	Ki 5.67
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.57
Sodium- and chloride-dependent GABA transporter 1	SLC6A1	unknown	IC50 5.50
Transporter	NET	unknown	Ki 5.50
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 5.47
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 5.14
Kappa-type opioid receptor	OPRK1	unknown	IC50 5.10
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 5.05
Serotonin 3 receptor (5HT3)	HTR3B|HTR3A	antagonist	Ki 4.80
Sodium channel alpha subunits; brain (Types I, II, III)	SCN1A|SCN2A|SCN3A	unknown	IC50 4.31

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1860-01-01	YEAR INTRODUCED	—	—

ATC classification

ATC code	Therapeutic hierarchy
N01BC01	NERVOUS SYSTEM › ANESTHETICS › ANESTHETICS, LOCAL › Esters of benzoic acid
R02AD03	RESPIRATORY SYSTEM › THROAT PREPARATIONS › THROAT PREPARATIONS › Anesthetics, local
S01HA01	SENSORY ORGANS › OPHTHALMOLOGICALS › LOCAL ANESTHETICS › Local anesthetics
S02DA02	SENSORY ORGANS › OTOLOGICALS › OTHER OTOLOGICALS › Analgesics and anesthetics

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug abuse	18621.7
Substance use disorder	6187.5
Toxicity to various agents	5920.8
Drug use disorder	4580.0
Miosis	2164.9
Coma	2156.3
Drug dependence	1874.4
Intentional product misuse	1581.6
Cardio-respiratory arrest	1555.2
Poisoning	1548.7
Substance abuse	1498.7
Completed suicide	1433.7

Chemical structure

• Molecular formula: C₁₇H₂₁NO₄
• Molecular weight: 303.36 g/mol
• CAS number: 50-36-2
• InChIKey: ZPUCINDJVBIVPJ-LJISPDSOSA-N
• PubChem CID: 446220

COC(=O)[C@@H]1[C@H]2CC[C@@H](C[C@@H]1OC(=O)C1=CC=CC=C1)N2C

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cocaine used for?

DrugCentral lists the following indications for Cocaine: Local anesthesia.

How does Cocaine work?

Its molecular targets in DrugCentral include SLC6A3 (inhibitor), Slc6a3, Slc6a4 and SLC6A3.

When was Cocaine first approved?

Cocaine was first approved by the YEAR INTRODUCED in 1860.

What is the chemical formula of Cocaine?

Cocaine has the molecular formula C17H21NO4 and a molecular weight of 303.36 g/mol.

Sources

• DrugCentral drug card 723 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL370805 — compound record and bioactivity
• PubChem CID 446220 — chemical identifiers
• DrugBank DB00907 — drug record
• FDA UNII I5Y540LHVR — substance identity
• UniProt Q01959 (SLC6A3) — target protein
• UniProt P31645 (SLC6A4) — target protein
• UniProt P46098 (HTR3A) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt P35367 (HRH1) — target protein
• UniProt P23975 (SLC6A2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.