➔ block nicotinic receptors in autonomic ganglia (clusters of neurons that relay signals between the CNS and organs in the sympathetic and parasympathetic systems)
➔ result: loss of autonomic tone ◇ orthostatic hypotension ◇ impaired reflex responses
➔ weak antagonist at α4β2 nAChRs
➔ reduces nicotine-induced dopamine release
Drugs with this mechanism (12)
Bupropion hydrobromide ER — Extended-release bupropion hydrobromide for depression; same active drug in a different salt.
Bupropion — NDRI antidepressant; activating, weight- and sex-neutral, but lowers the seizure threshold.
Dextromethorphan — OTC cough suppressant; NMDA antagonist and sigma-1 agonist, dissociative in overdose.
Dextrorphan — Dextromethorphan's active metabolite; the NMDA antagonism behind both the dissociative effect and the abuse potential.
Bupropion XL 450 mg — Bupropion XL as a single 450 mg tablet, for patients stabilized at the maximum dose.
Hexamethonium — Ganglionic nicotinic blocker of historical interest.
Mecamylamine — Ganglionic nicotinic blocker; studied as a smoking-cessation adjunct.
Memantine — NMDA antagonist for moderate-to-severe Alzheimer dementia; well tolerated.
Memantine XR — Extended-release NMDA antagonist for moderate-to-severe Alzheimer disease.
Bupropion SR — Sustained-release NDRI; activating and sexually sparing, but seizure-limited.
Bupropion XL — Longest-release NDRI; activating and usually sexually sparing.
Bupropion SR (smoking cessation) — Sustained-release bupropion for smoking cessation; nonnicotine aid with antidepressant activity.