Cholinergic

Question 1

carbachol

Answer 1

MOA: non selective Cholinergic Agonist
Indications: Glaucoma; mitosis,increased aqueous humor outflow
P’dynamics:
P’kinetics: topical; not broken down by AchE, long duration
Tox: Cholinergic (SLUDGE & DUMBBELSS)

Question 2

bethanechol

Answer 2

MOA: non selective muscarinic agonist
Indications: neurogenic illeus; urinary retention, GERD
P’dynamics: increase depressor tone + GI motility
Tox: Reflex tachycardia, bronchoconstriction, increased secretory (sweat, GI, Resp secretions)

Question 3

methacholine

Answer 3

MOA: non selective Muscarinic agonist
Indications: Dx asthma/bronchiole hyperactivity

inhaled only

Question 4

pilocarpine

Answer 4

MOA: non selective Muscaranic agonist
Indications: glaucoma, dry mouth/xerostomia, Sjogren syndrome, Head/neck cancer
Tox: Reflex tachycardia (vasodilation), bronchoconstriction, increased secretory (sweat, GI, Resp secretions)

Question 5

nicotine

Answer 5

MOA: Nicotinic agonist
Indications: smoking cessation, nicotine withdrawal
Tox: bronchospasm, dependence transference
considerations: gum, patch, nasal

Question 6

varenicline

Answer 6

MOA: Partial a2-b4 nicotinic agonist; inhibits nicotine’s ability to stimulate mesolimbic dopamine reward system
Indications: Smoking cessation
Tox: nausea, headache, insomnia, abnormal dreams
considerations: Oral

Question 7

edrophonium

Answer 7

MOA: Short acting AChE inhibitor
Indications: Myasthenia Gravis Dx
P'dynamics: Blocks AchE action
P'kinetics: short half life, 10-30 min duration
Tox: cholinergic reaction (DUMBBELS)

highly charged; won’t cross BBB

Question 8

neostigmine

Answer 8

MOA: Intermediate term AChE inhibitor; reversible
Indications: Myasthenia Gravis Dx
P’dynamics: increases Ach availability at post synaptic membrane receptors
Tox: cholinergic reactions
IV/IM/SC; doesn’t enter CNS

Question 9

physostigmine

Answer 9

MOA: Intermediate term AChE inhibitor; reversible
Indications: glaucoma, alzeheimers, Rx of CNS muscarinic side effects, atropine overdose, non-depolarizing neuromuscular blockade reversal
P’dynamics: indirectly stimulates N +M receptors
Tox: Cholinergic reaction
considerations: Crosses BBB; acts on CNS

Question 10

organophosphates

Answer 10

MOA:Long Acting AChE inhibitor
Indications: Insecticides + Nerve gas
P'dynamics: blocks AchE actions
P'kinetics:
Tox: Cholinergic symptoms

Question 11

echothiophate

Answer 11

MOA: irreversible AChE inhibitor
Indications: Glaucoma
P'dynamics: binds irreversibly to Ach binding site on AchE
P'kinetics: topical, long half life
Tox: lacrimation, stinging

Question 12

praladoxime

Answer 12

MOA: AChE reactivator
Indications: organophosphate poisoning
P’dynamics: binds inactivated AchE, accelerates reactivation
P’kinetics:
Tox: w/ atropine (hot, dry, mad, red, blind)
Interactions: enhances atropine toxicity
considerations: IV IM only

Question 13

atropine

Answer 13

MOA: non-selective muscarinic blocker
Indications: cholinergic syndrome, bradicardia, organophosphate poisoning, cardiac resuscitation
P’dynamics: prevents Ach activity, lowers muscle/gland activity controlled by parasympathetic
Tox: delirium, hallucinations, mydriasis, photophobia, cycloplegia, fever, anhydrosis, vessel dilation
Interactions: w/ 2-PAM,
considerations: CS; IM; IV; lipid soluble, crosses BBB

Question 14

scopolamine

Answer 14

MOA: non-selective Muscarinic blocker
Indications: motion sickness, amnestic; anti emetic; dilation of eye
P’dynamics: blocks M1 receptors preferentially
Tox: similar to atropine
considerations: transdermal; crosses BBB

Question 15

dicyclomine

Answer 15

MOA: non-selective Muscarinic blocker
Indications: irritable bowel
P'dynamics: relaxes smooth muscle, inhibits bradykinin/histamine induced bowel spasms
Tox: atropine like
considerations: oral

Question 16

methscopolamine

Answer 16

MOA: Muscarinic blocker
Indications: Peptic ulcer

Question 17

pirenzepine

Answer 17

MOA: Muscarinic blocker
Indications: Peptic ulcer

Question 18

propantheline

Answer 18

MOA: Muscarinic blocker
Indications: Peptic ulcer

Question 19

oxybutynin

Answer 19

MOA: Muscarinic blocker
Indications: Urgency and Bladder spasms

Question 20

glycopyrrolate

Answer 20

MOA: Muscarinic blocker
Indications: Urgency and Bladder spasms

Question 21

tropicamide

Answer 21

MOA: Muscarinic blocker
Indications: promydriatic

Question 22

homatropine

Answer 22

MOA: Muscarinic blocker
Indications: post eye surgery

Question 23

ipratropium

Answer 23

MOA: Muscarinic blocker, short acting
Indications: Asthma, COPD
P’dynamics: inhaled M3 antagonist

Tox: rare but atropine like effects

Question 24

tiotropium

Answer 24

MOA: Muscarinic blocker, long acting
Indications: Asthma, COPD
Indications: Asthma, COPD
P’dynamics: inhaled M3 antagonist

Tox: rare but atropine like effects

Question 25

succinylcholine

Answer 25

MOA: depolarizing nicotinic antagonist
Indications: surgical paralysis, RSI
P’dynamics: complete skeletal muscle relaxation; flaccid paralysis; initial stimulation not terminated, motor endplate depolarizes;
P’kinetics: NOT broken down by AchE
Tox: Rhabdomyolysis w/ hyperK in Duchene muscular dystrophy
Interactions:
considerations: only depolarizing agent in use; don’t use w/ AchE blockade; no reversal

Question 26

tubocurarine

Answer 26

MOA: Non- depolarizing nicotinic antagonist
Indications: surgical paralysis
P’dynamics: directly blocks nicotinic motor end plate; flaccid paralysis
P’kinetics:
Tox: resp failure, tachycardia, HTN, histamine release, ganglionic/muscarinic side effects
Interactions:
considerations: 30-60min duration; neostigmine to reverse

Question 27

pancuronium

Answer 27

MOA: Non- depolarizing nicotinic antagonist; reversible competitive inhibition; benzoisoquinolinium analogue
Indications: surgical paralysis, RSI
P’dynamics: antagonizes motor endplate AchRs

Tox: resp failure, tachycardia, HTN, histamine release, ganglionic/muscarinic side effects

considerations: 30-60min duration; neostigmine to reverse

Question 28

rocuronium

Answer 28

MOA: Non- depolarizing nicotinic antagonist; reversible competitive inhibition; benzoisoquinolinium analogue
Indications: surgical paralysis, RSI
P’dynamics: antagonizes motor endplate AchRs

Tox: resp failure, tachycardia, HTN, histamine release, ganglionic/muscarinic side effects

considerations: 30-60min duration; neostigmine to reverse

Question 29

cistracurium

Answer 29

MOA: Non- depolarizing nicotinic antagonist; reversible competitive inhibition; benzoisoquinolinium analogue
Indications: surgical paralysis
P’dynamics: antagonizes motor endplate AchRs

Tox: resp failure, tachycardia, HTN, histamine release, ganglionic/muscarinic side effects

considerations: 30-60min duration; neostigmine to reverse

Question 30

trimethaphan

Answer 30

MOA: NN ganglionic antagonist; non-depolarizing; reversible competitive inhibition
Indications: Emergency Hypertensive crisis, dissecting AA
P’dynamics:blocks SNS and PNS; non-depolarizing nicotinic Ach blocker
Tox: highly toxic, emergency only; orthostatic hypotension,
Short Acting IV
doesn’t cross BBB

Question 31

Botulinum toxin

Answer 31

MOA: Indirect Anticholinergic; inhibits
Indications: anti-wrinkle
P’dynamics: inhibits ACh release from nerve terminals; interferes w/ internal vesicle docking
Tox: botulism; distant spread => botulism symptoms (weakness, diplopia, ptosis, dysphagia etc)
local injections only

Question 32

Acetylcholine

Answer 32

MOA: Cholinergic agonist
Indications: glaucoma
P’dynamics:
P’kinetics:

Question 33

benztropine

Answer 33

MOA: Muscarinic blocker (M1 specificity) Histamine receptor blocker
Indications: Parkinson’s disease, dystonia, extrapyramidal symptoms
P’dynamics: centrally acting anticholinergic / antihistamine
Tox: Atropine like
Route: IV/IM