API

COCAINE HYDROCHLORIDE

Drug classification

Local anesthetics (ester-type local anesthetic)

Dosage form

SOLUTION;NASAL

API strength per dosage

4%

Dose

Adults: Apply 160 mg (4 mL of 4% solution) intranasally per procedure; maximum 200 mg. Safety and efficacy in pediatric patients have not been established. Use with caution in elderly and those with cardiovascular disease; adjust dose as needed.

Mechanism of action

Inhibits presynaptic reuptake of norepinephrine, dopamine, and serotonin by blocking their respective transporters (NET, DAT, SERT), and blocks voltage-gated sodium channels (Nav), resulting in local anesthesia and vasoconstriction.

Indications

Topical anesthesia of the mucous membranes of the nasal cavities, diagnostic procedures and surgeries on or through the nasal cavities in adults.

Side effects

Hypertension, tachycardia, arrhythmias, myocardial infarction, seizures, CNS stimulation, anxiety, tremor, headache, nasal mucosal damage, epistaxis, respiratory depression, hypersensitivity reactions.

Pregnancy category

Precautions

Contraindications

Hypersensitivity to cocaine or ester-type local anesthetics, severe hypertension, thyrotoxicosis, known or suspected pheochromocytoma, acute coronary syndrome, narrow-angle glaucoma, history of seizures.