Pharmacology- Cholinergic Agonists And Antagonists

Front 1

Bethanechol (Duvoid)

Back 1

DC: Cholinergic Agonist (Choline Esterase)
Route:
MOA: Acts at MUSCARINIC receptors to contract detrusor muscle of urinary bladder, usually enough to initiate micturition, Increase GI motility
Uses: Disorders association with decreased parasympathetic tone (GI and Urinary excretion)
CI: Asthma, Hyperthyroidism
SE: SLUD (Salivation, Lacrimation, Urination, Defecation)
Note:

Front 2

Pilocarpine (Pilocar)

Back 2

DC: Cholinergic Agonist (Natural Alkaloid)
Route:
MOA: Reduce IOP by acting at the M1/M3 receptors of the constrictor pupilae
Uses: Acute and Chronic Glaucoma to reduce IOP, Counteract the effects of atropine, Treat dry mouth (Xerostomia)
CI: Asthma, Hyperthyroidism
SE: Systemic effects (if it crosses conjunctiva), SLUD (Salivation, Lacrimation, Urination, Defecation)
Note:

Front 3

Cevimeline (Evoxac)

Back 3

DC: Cholinergic Agonist (M1/M3 specific agonist)
Route:
MOA: Works on the M3 receptor in salivary glands
Uses: Treatment of Xerostomia, Enhance lacrimal secretions
CI: Asthma, Hyperthyroidism
SE: SLUD (Salivation, Lacrimation, Urination, Defecation)
Note: Fewer side effects than pilocarpine

Front 4

Atropine

Back 4

DC: Cholinergic Antagonist (Belladona Alkaloid)
Route:
MOA: Attaches to the muscarinic receptor at target organ
Uses: Mydriasis, Cycloplegia, Antispasmotic, Treat organophosphate poisoning, Suppress respiratory secretions
CI:
SE: Dose related (Hallucinations, delirium, rapid HR, palpitations)
Note:

Front 5

Scopolamine

Back 5

DC: Cholinergic Antagonist (Belladona Alkaloid)
Route:
MOA:
Uses: Prophylactic for motion sickness, Adjunct in anesthesia to produce sedation and amnesia
CI:
SE: CNS depression
Note: Crosses BBB easier than Atropine

Front 6

Ipratropium Bromide (Atrovent)

Back 6

DC: Cholinergic Antagonist (Synthetic derivative)
Route:
MOA: Blocks muscarinic receptors and reduces bronchoconstriction mediated by parasympathetic system
Uses: Used in asthma and COPD to cause bronchodilation
CI: BPH
SE: Slows voiding, Constipation, Mydriasis, Confusion, Blurred vision
Note:

Front 7

Tiotropium Bromide (Spiriva)

Back 7

DC: Cholinergic Antagonist (Synthetic Derivative)
Route:
MOA:
Uses: COPD and Asthma (more bronchoselective)
CI: BPH
SE: Slows voiding, Constipation, Mydriasis, Confusion, Blurred vision
Note: Greater affinity for M1/M3 than M2

Front 8

Tolterodine (Detrol)

Back 8

DC: Cholinergic Antagonist (Synthetic Derivative)
Route:
MOA: Blocks M3 receptors (postsynaptic) on detrusor muscle reducing parasympathetic mediated contraction of the bladder, Blocks M2 receptors on presynaptic sympathetic terminals enhancing sympathetic B2 mediated relaxation of the detrusor
Uses: Treatment of overactive bladder
CI: BPH
SE: Slows voiding, Constipation, Mydriasis, Confusion, Blurred vision
Note:

Front 9

Succinylcholine

Back 9

DC: Nicotinic Antagonist (NMJ blocker)
Route:
MOA: Phase 1- causes membrane depolarization resulting in an initial discharge that produces transient fasciculations followed by flaccid paralysis, Phase 2- membrane repolarizes but receptor is desensitized to the effect of acetylcholine
Uses: Prevent actions of acetylcholine
CI:
SE: Muscle pain, Malignant hyperthermia
Note:

Front 10

Edrophonium
Physostigmine
Pyridostigmine
Ambenonium
Ecothiophate
Isofluorophate

Back 10

DC: AChE Inhibitors
Route:
MOA: Inhibit acetylcholinesterase and prolong/enhance actions of acetylcholine
Uses: Myasthenia Gravis, Hypotonia of Bladder and GI, Glaucoma
CI:
SE:
Note:

Front 11

Physostigmine

Back 11

DC: AChE Inhibitor
Route:
MOA: Inhibit acetylcholinesterase and prolong/enhance actions of acetylcholine at the NMJ
Uses: Glaucoma, Antidote for atropine overdose
CI:
SE: Convulsions, Bradycardia, Muscle paralysis
Note:

Front 12

Neostigmine

Back 12

DC: AChE Inhibitor
Route:
MOA: Inhibit acetylcholinesterase and prolong/enhance actions of acetylcholine at the NMJ
Uses:
CI:
SE: Hypotension, Cholinergic crisis, Muscle paralysis
Note: