Cocaine

Drug Class: Central nervous system stimulant, local anesthetic (ester type)

Overview

Cocaine is a potent central nervous system stimulant and local anesthetic derived from the coca plant. It has high abuse potential and is classified as a Schedule II controlled substance in the United States. While it has limited medical use as a topical anesthetic in certain surgical procedures, its recreational use is illegal in most countries, including Jordan.

Mechanism of Action

Cocaine acts primarily by blocking the reuptake of neurotransmitters (dopamine, norepinephrine, and serotonin) at presynaptic nerve terminals, leading to increased concentrations in the synaptic cleft. This results in prolonged stimulation of postsynaptic receptors. It also acts as a local anesthetic by blocking voltage-gated sodium channels, inhibiting nerve impulse conduction.

Indications

  • Topical anesthesia for mucous membranes in specific surgical procedures (e.g., nasal, laryngeal, or ophthalmic surgery). Note: Medical use is highly restricted and not common.

Dosage

Medical use: Applied topically as a solution (typically 1-10% concentration) in controlled clinical settings. Dosage is minimal and based on the procedure. Recreational use is illegal and not standardized.

Black Box Warning

Warning: Cocaine has a high potential for abuse. It should only be used under strict medical supervision in controlled settings. Recreational use is associated with severe health risks, including sudden death.

Contraindications

  • Hypersensitivity to cocaine or other ester-type local anesthetics
  • Patients with severe cardiovascular disease
  • History of substance abuse
  • Concurrent use with monoamine oxidase inhibitors (MAOIs)
  • Use in children
  • Application to infected or traumatized mucous membranes

Side Effects

  • Cardiovascular: Tachycardia, hypertension, arrhythmias, chest pain, myocardial infarction
  • CNS: Euphoria, anxiety, agitation, paranoia, hallucinations, seizures, headache
  • Psychiatric: Dependence, addiction, psychosis
  • Gastrointestinal: Nausea, vomiting
  • Other: Nasal septum perforation (with intranasal use), hyperthermia, rhabdomyolysis, sudden death

Interactions

  • MAOIs: Risk of hypertensive crisis
  • Other stimulants (e.g., amphetamines): Increased cardiovascular and CNS effects
  • Beta-blockers: Paradoxical hypertension
  • Alcohol: Formation of cocaethylene, increasing toxicity
  • Antidepressants (e.g., SSRIs): Increased serotonin syndrome risk