Cocaine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

Canada: Cocaine.

Drug combinations

Chemistry

Cocaine Hydrochloride: C~17~H~21~NO~4~ HCl. Mw: 339.81. (1) 8-Azabicyclo[3.2.1]octane-2-carboxylic acid, 3-(benzoyloxy)-8-methyl-, methyl ester, hydrochloride, [1R-(exo,exo)]-; (2) Methyl 3β-hydroxy-1αH,5αH-tropan-2β-carboxylate, benzoate (ester) hydrochloride. CAS-53-21-4; CAS-50-36-2 (cocaine).

Pharmacologic Category

EENT Preparations; Local Anesthetics. (ATC-Code: N01BC01; R02AD03; S01HA01; S02DA02).

Mechanism of action

Blocks both the initiation and conduction of nerve impulses by decreasing permeability of neuronal membrane to sodium ions, which inhibits depolarization and blocks conduction. Interferes with the uptake of norepinephrine by adrenergic nerve terminals producing vasoconstriction. A type I antiarrhythmic.

Therapeutic use

Topical anesthesia for mucous membranes.

Pregnancy and lactiation implications

It is unknown whether the drug can cause fetal harm. Cocaine hydrochloride should be used during pregnancy only when clearly needed. It is not known if cocaine is distributed into milk.

Unlabeled use

Contraindications

Hypersensitivity to cocaine or any component of the topical solution. Ophthalmologic anesthesia (causing sloughing of the corneal epithelium). Pregnancy (nonmedicinal use).

Warnings and precautions

Use with caution in cardiovascular disease. Use with caution in history of cocaine abuse. In patients being treated for cardiovascular complication of cocaine abuse, avoid β-blockers for treatment. Use with caution in acutely ill or debilitated patients. Use with caution in the elderly and children. For topical use only. Use caution in severely traumatized mucosa and sepsis in the region of the proposed application.

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