Neuronal nAChR antagonist
Neuronal nicotinic acetylcholine receptor antagonist
- If BBB-crossing: α4β2 blockade reduces nicotine reward
- Ganglionic blockade → ↓ blood pressure
- 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 (10)
- 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 — Active dextromethorphan metabolite; NMDA antagonism drives dissociation and abuse potential.
- Bupropion XL 450 mg — Single 450 mg bupropion XL tablet for patients stabilized at the maximum dose.
- 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.
Self-check
- What is required for α4β2 blockade to reduce nicotine reward?
BBB penetration. - Why can nicotinic ganglionic blockade cause orthostatic hypotension?
Loss of autonomic tone and impaired reflex responses.
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