Drug List 1: cholinergic agonists & antagonists Flashcards
Benthanechol
Direct, non-selective Muscarinic agonist (cholinergic ag.)
Ind: atonic/neurogenic bladder or ileus, megacolon* (*off-label)
Mech: stimulate intestinal motility & urination (via M3 R)
SE: DUMBBELSS
Acetylcholine
Direct, non-selective m/nAChR agonist (cholinergic ag.)
Ind: temporary miosis during eye surgery
(cataracts, keratoplasty, etc.)
Effect: +M3 –> miosis & accommodation
(rapid, short duration bc of AChE metabolism)
SE: DUMBBELSS
Carbachol
Direct, non-selective m/nAChR agonist (cholinergic ag.)
Ind: suppress IOP after cataract surgery, chronic open-angle glaucoma
Mech: lower intraocular P (+M3 –> miosis & accomodation)
SE: DUMBBELSS
Cevimeline
Direct, non-selective Muscarinic AChR agonist (cholinergic ag.)
Ind: Sjögren’s syndrome
Effects: stimulate gland secretion via M3 R (sweat, tears, saliva)
SE: DUMBBELSS, & many others
Pilocarpine
Direct, non-selective mAChR agonist (cholingergic ag)
Ind: primary glaucoma (#1) - emergency lower IOP or chronic mgmt, Sjögren’s syndrome
Mech: lower intraocular P (+ M3 –> miosis & accomodation), stimulate gland secretion
SE: DUMBBELSS
Echothiophate
Class: cholinergic agonist Indirect, AChE inhibitor *irreversible* Ind: chronic open-angle glaucoma Mech: reduce intraocular P (long-lasting bc irreversible) SE: DUMBBELSS
Edrophonium
Class: cholinergic agonist
Mech: indirect, AChE inhibitor (reversible, short acting)
–> potentiate levels of ACh @ NMJ
Ind: Myasthenia Gravis (Dx and assess Tx), reverse NMJ blockade
Effects: transient increase in muscle strength
(*will not see if too much Tx w/ neostigmine)
SE: DUMBBELSS
Neostigmine
Class: Cholinergic agonist
Indirect, AChE inhibitor (reversible)
Ind: atonic/neurogenic bladder and ileus, megacolon* (off-label), long-term Tx myasthenia gravis, reverse NMJ blockade
Mech: stimulate intestinal motility and urination (+M3 R), increase muscle strength (–> potentiate levels of ACh @ NMJ)
SE: DUMBBELSS
Physostigmine
Class: cholinergic agonist
Mech: indirect, AChE inhibitor (reversible)
–> potentiate levels of ACh @ NMJ and CNS
Ind: anti-cholinergic overdose (treat CNS symptoms)
Effects: stimulate peripheral and CNS cholinergic signaling
*MORE distribution to CNS than neostigmine!
SE: convulsions, DUMBBELSS
Pralidoxime
Class: organophosphate antidote (NOT a cholinergic agonist)
Mech: displace organophosphate prior to chem. changes (“AChE aging”)
Ind: organophosphate poisoning (in pesticides, nerve gases, etc.)
Effects: reactivate AChE if given before aging
SE: –
atropine
Mech: muscarinic antagonist (cholinergic antag.)
Ind: Cyclogplegia for eye exam (esp. young children), cholinergic overdose, GI hypermotility/incontinence
Effects: Mydriasis & cyclogplegia (-M3 –l circular/ciliary mm.), inhibits voiding/secretions (relax detrussor, constrict sphincter)
SE: Blind/dry/hot/red/mad, trigger latent glaucoma
*hypERthermia esp. in children!
Contraindications: glaucoma (increase IOP = bad)
ipratropium
class: cholinergic antagonist
mech: Muscarinic antagonist
Ind: COPD (1st line), asthma (w/ or instead of beta agonist)
Effects: bronchodilation (No CNS effects bc inhaled) & decrease mucus secretion (both -M3)
SE: blind/dry
scopolamine
class: cholinergic antagonist
mech: Muscarinic antagonist (blocks mACh Receptor)
Ind: motion sickness, sedative/amnestic in surgery,
Effects: amnesia/sedation, anti-emesis, HIGH CNS absorption!
SE: blind/dry/hot/red/mad, drowsiness
Contraindications: glaucoma
mecamylamine
class: cholinergic antagonist
Mech: non-depolarizing nicotinic antagonist (ganglia)
Ind: rare… anti-nicotine craving, moderate/severe HTN (if unmanageable on other meds)
Effects: block symp. output to CV system –> vasodilation, decrease BP
SE: Many
Trimethaphan
class: cholinergic antagonist
mech: non-depolarizing nicotinic antagonist (ganglia)
Ind: rare… controlled hypotension during surgery, HTN emergency
Effects: block symp. output to CV system –> vasodilation, decrease BP rapid onset of action
SE: many
