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Direct-acting cholinergic receptor agonists
- Pilocarpine - used to treat glaucoma
- Bethanechol - used to treat urinary dysfunction
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Indirect-acting cholinesterase inhibitors
- short duration of action (.5-.8 hours)
- used to treat Alzheimer's
- Donepezil (Aricept)
- Galantamine (Razadyne)
- Rivastigmine (Excelon)
- Tacrine (Cognex)
- Edrophonium (used to test for myasthenia gravis)
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Irreversible cholinesterase inhibitors
- >100 hours
- used to treat glaucoma
- Echothiophate
- Demecarium bromide
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Uses for irreversible cholinesterase inhibitors
- eyes - glaucoma
- GI tract - postoperative atony
- urinary tract - neurogenic urinary bladder
- neuromuscular junction - Myasthenia gravis, curare-induced neuromuscular paralysis
- heart - supraventricular tachydysrhythmia
- antimuscarinic intoxication - due to overdose of muscarinic receptor antagonists or tricyclic antidepressants
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Toxicity of direct and indirect-acting cholinergic agonists
- bronchoconstriction
- salivation
- lacrimation
- urination
- diarrhea
- nausea
- vomiting
- sweating
- cutaneous vasodilation
- neuromuscular nicotinic receptors (indirect-acting)
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Cholinergic receptor antagonists
- block parasympathetic nerves
- enables sympathetic nerves to exert their end-organ effects
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Nicotine receptor partial agonist
- Chantix, varenicline
- works by blocking the pleasant effects of nicotine achieved from smoking on the brain
- use: smoking cessation with education and counseling
- potential adverse behavioral effects: hostility, agitation, depression, suicidal thoughts
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