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12 Cards in this Set

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Acetylcholine
Direct-Acting Cholinergic Agonists

Nicotinic and muscarinic effects (acts at all cholinergic synapses)

Rapidly hydrolyzed if given systemically

Used topically for miosis induction during ophthalmic surgery
Methacholine
Direct-Acting Cholinergic Agonists

Primarily muscarinic with minimal nicotinic effects

More slowly hydrolyzed – greater duration of action

Administered by inhalation as a test for bronchial hyperactivity
Bethanechol
Direct-Acting Cholinergic Agonists

Primarily muscarinic effects

Resistant to hydrolysis – prolonged activity

Used to treat urinary retention

Oral administration can cause palpitations from vasodilation-
induced reflex tachycardia
Carbachol
Direct-Acting Cholinergic Agonists

Nicotinic and muscarinic effects – also stimulates ACh release

Resistant to hydrolysis

Used topically during ophthalmic surgery and to treat glaucoma
Pilocarpine
Direct-Acting Cholinergic Agonists

Primarily muscarinic effects

Resistant to hydrolysis

Used to treat dry mouth (xerostomia) and glaucoma

Oral administration can cause palpitations from vasodilation-
induced reflex tachycardia
Cevimeline
Direct-Acting Cholinergic Agonists

Primarily muscarinic effects

Resistant to hydrolysis

Used to treat dry mouth (xerostomia) in Sjogren’s syndrome
Nicotine
Direct-Acting Cholinergic Agonists

Nicotine interacts with nicotine receptors throughout the body

Autonomic ganglia, neuromuscular junction and in the brain

Low doses stimulate, high doses inhibit.
Its actions are complex and frequently unpredictable because of the
multiple target sites

Peripheral effects include ↑ HR, ↑ BP, ↑ GI tone and motility

CNS: stimulation, tremors, respiration, emetic effects

Nicotine is highly toxic (10 mg in children)!
Edrophonium
Short-Acting Cholinesterase Inhibitors

A competitive inhibitor

Does not cross the blood-brain barrier

Very short duration of action (10-20 min)

Used to diagnose myasthenia gravis
Echothiophate
Long-Acting Cholinesterase Inhibitors

Treatment of Glaucoma
Antidotes for AChE inhibitor poisoning
Atropine blocks the muscarinic effects of the excess Ach
Given to troops when entering areas believed to have chemical weapons

2-PAM is effective only if given within a few hours after exposure to the organophosphate
It can break the “irreversible” bond, liberating the AChE, but not after the bond “ages”
Scopolamine
Muscarinic Antagonists

Greater CNS effects than atropine

Produces drowsiness and can induce amnesia and psychotic behavior

Used to treat motion sickness (patch) and for preop sedation
Ipratropium
Muscarinic Antagonists

Poor CNS penetration

Used for the treatment COPD and asthma