What is Cocaine's mechanism of action?

• A. Increases GABA release
• B. Mimics endorphins
• C. Blocks reuptake of dopamine, serotonin, and norepinephrine
• D. Blocks acetylcholine receptors

Answer: (C)

Cocaine increases synaptic levels of monoamines by blocking their reuptake transporters, especially dopamine, norepinephrine, and serotonin. By inhibiting DAT, dopamine stays in the synapse longer, enhancing reward signaling in pathways linked to addiction. Inhibiting NET raises sympathetic activity, contributing to tachycardia, hypertension, and pupil dilation. Inhibiting SERT adds to mood effects. This reuptake blockade is the primary mechanism behind cocaine’s reinforcing and stimulating effects.

Note that cocaine also has local anesthetic effects by blocking voltage-gated sodium channels, but that action is separate from its central monoamine reuptake blockade that drives its abuse potential.