Name: Cocaine (Various)
Class: CNS Stimulant (Indirect Sympathomimetic Agent)/Local Anesth (Ester)
Mechanism: Inhib. reuptake of catecholamines (DA, NE, 5HT) ® prolonged action. Local anesthetic properties from block of Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.
Absorption: : Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.
Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart
Metabolism.: Rapidly Metabolism. by plasma pseudocholinesterases. Med. duration of anesth action.
Toxicity/S.E.s: Fever, nausea, vomiting, confusion, headache. Neurosis, paranoia, frank psychosis. Tolerance, but not as strong as opiates. Acute toxicity ® hypertension, stroke, seizures, cardiac arrhythmias. Very strong psych. dependence. Mild physical dependence. W/drawal ® appetite, fatigue, depression.
Utility: Used in ENT surgery to produce local anesthesia, hemostasis, vasoconstriction. Crack = smokable version.
Special Features: Does not require concomitant application of a vasoconstrictor. Twice the potency of procaine. Produces elevation of mood, euphoria, self-esteem, energy, ¯ sense of fatigue. Moderate dose ® HR, BP.