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cocaine

N01BC01

Forms & Strengths

Topical solution: 4% (40 mg/mL)
Topical solution: 10% (100 mg/mL)

Adult Dosing

Topical mucous membrane anesthesia: 1.5 mg/kg (maximum 150 mg) of the 4% or 10% solution applied topically to the mucous membranes of the nasal, oral, and laryngeal cavities as needed for procedure.

Pediatric Dosing

Topical anesthesia: 0.5 mg/kg to 1.5 mg/kg (maximum 3 mg/kg total dose depending on age and procedure) applied topically to mucous membranes.

Indications

Local (topical) anesthesia of accessible mucous membranes of the nasal, oral, and laryngeal cavities.

Mechanism of Action

Inhibits presynaptic reuptake of norepinephrine, serotonin, and dopamine, leading to prolonged neurotransmitter presence in the synaptic cleft.
Blocks voltage-gated sodium channels, preventing the initiation and conduction of nerve impulses and producing local anesthesia.

Contraindications

Known hypersensitivity to cocaine or local anesthetics of the ester type
Topical administration in the eye (risk of corneal damage)
Use in patients with sepsis or severe inflammation at the application site

Adverse Reactions

Central nervous system stimulation: anxiety, restlessness, tremor, euphoria, seizures
Cardiovascular effects: hypertension, tachycardia, arrhythmias, myocardial ischemia, stroke
Local effects: nasal mucosal ulceration, tissue ischemia, perforation of the nasal septum with chronic use

Drug Interactions

Monoamine oxidase inhibitors (MAOIs): severe hypertensive crises and hyperpyrexia
Sympathomimetics and vasopressors: potentiates pressor response, risk of severe hypertension and coronary ischemia
Beta-blockers: unopposed alpha-adrenergic vasoconstriction leading to severe hypertension and reduced coronary blood flow

Curated Content: Needs Vetting Before Put to Clinical Use