Cocaine

alkaloid · nervous · cardiovascular · Intranasal · IV · Inhaled · Oral

Cocaine, an alkaloid. Tropane alkaloid from coca; blocks the dopamine, norepinephrine, and serotonin transporters (DAT/NET/SERT), raising… Oral half-life 0.8 h.

Tropane alkaloid from coca; blocks the dopamine, norepinephrine, and serotonin transporters (DAT/NET/SERT), raising synaptic monoamines for a short, intense euphoric stimulation. Also a local anesthetic via voltage-gated sodium-channel blockade plus vasoconstriction. Short half-life drives compulsive redosing; cardiovascular toxicity (arrhythmia, MI, stroke).

PubChem CID 446220. DAT/NET/SERT Ki + plasma t½ (~0.7–1.5 h) deferred to enrichment pass.

Pharmacokinetics

• Intranasal — t½ 1.3 h · F 80% · Vd 189 L
• Oral — t½ 48 min · Vd 189 L
• IV — t½ 1.3 h · F 100% · Vd 189 L
• Inhaled — t½ 1.1 h · Vd 189 L