• Esteratic local anesthetic agent
• Blocks voltage-gated sodium channels and inhibits depolarization, initiation, and conduction of nerve impulses
• Blocks neuronal reuptake of norepinephrine resulting in CNS stimulation, tachycardia, hypertension, and vasoconstriction
• Blocks neuronal reuptake of dopamine and serotonin in the midbrain, with resulting euphoria and arousal

• Local anesthetic with vasoconstrictor activity, used on mucosal surfaces of the respiratory tract for otorhinolaryngology procedures and bronchoscopy
• Used in combination with other agents (tetracaine-adrenaline-cocaine) for the repair of minor head and neck lacerations
• Commonly abused CNS stimulant in the US (National Institute of Drug Abuse NIDA)

1 minute when applied to mucosa, peak effect in 5 minutes

Serum half-life of cocaine is 30-90 minutes

• Non-enzymatic hydrolysis to benzoylecgonine, via hepatic esterases, or plasma pseudocholinesterases to ecgonine methylester, and minimal amounts by CYP3A4 to norcocaine, all of which are active and excreted in urine
• Benzoylecgonine has the highest concentration in urine and can be detected for 2-3 days after exposure

Hypertension, tachycardia, dysrhythmias, myocardial ischemia, CNS stimulation, euphoria, hallucinations, paranoia, seizures, fever, agitation, restlessness, tremor, stroke, mydriasis, rhinitis, tachypnea, vasculitis, Raynaud's phenomenon