Neuronal nAChR agonist
Neuronal nicotinic acetylcholine receptor agonist
- ↑ dopamine, norepinephrine, serotonin, glutamate and GABA release
- If BBB-crossing:
- Reward-circuit activation → reinforcement
- Can enhance attention/cognition and alter sleep
- highest relevance at α4β2 subtype
- Neuroprotection (activation of α7 subtype)
- preclinical evidence
- intranasal varenicline (Tyrvaya) stimulates trigeminal–parasympathetic reflex → ↑ tear production
Drugs with this mechanism (7)
- Acetylcholine — Endogenous neurotransmitter at muscarinic and nicotinic receptors.
- Carbachol — Nonselective cholinergic agonist used in ophthalmology.
- Nicotine gum — The addictive alkaloid of tobacco; nicotinic agonist, available OTC for cessation.
- Nicotine inhaler — Nicotine-replacement device: absorbed mainly through mouth and throat; addresses cravings and the hand-to-mouth smoking ritual.
- Nicotine lozenge — Short-acting nicotine replacement for breakthrough cravings; oral irritation is common.
- Nicotine nasal spray — Fast-acting nicotine-replacement spray for breakthrough cravings during smoking cessation.
- Nicotine patch — Steady transdermal nicotine for smoking cessation; pair with a short-acting form for breakthrough craving.
Self-check
- How does intranasal varenicline increase tears?
Stimulates the trigeminal–parasympathetic reflex. - How strong is the evidence qualifier for α7-mediated neuroprotection here?
Preclinical evidence.
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