Cholinergic Agents

Front 1

Botulinum toxin

Back 1

Degrades synaptobrevin; prevents release of ACh

Front 2

Ganglionic effect and neuromuscular end plate effect

Back 2

Prolonged nicotinic receptor occupancy leads to loss of firing from postganglionic neuron; as a result the muscle cell relaxes

Front 3

Nicotinic N-type receptor

Back 3

Postganglionic cell body, dendrites, presynaptic cholinergic terminals

Opens sodium and potassium channels; depolarizes cell

Front 4

Nicotinic M-type receptor

Back 4

Neuromuscular end plates


Opens sodium and potassium channels; depolarizes cell

Front 5

M1 receptor

Back 5

CNS neurons, sympathetic postganglionic neurons, presynaptic sites

Formation of IP3 and DAG lead to increased intracellular calcium

Front 6

M2 receptor

Back 6

Myocardium, smooth muscle, some presynaptic sites

Opens potassium channels; inhibits adenylyl cyclase

Front 7

M3 receptor

Back 7

Exocrine glands, smooth muscle, vessels

Formation of IP3 and DAG lead to increased intracellular calcium

Front 8

Acetylcholine

Back 8

-choline ester
-rapid hydrolysis by cholinesterase
-not used therapeutically

Front 9

Methacholine

Back 9

-choline ester
-less susceptible to hydrolysis than ACh
-used to diagnose asthma

Front 10

Carbachol

Back 10

-choline ester
-topical miotic agent to treat glaucoma

Front 11

Bethanechol

Back 11

-choline ester
-resistant to hydrolysis
-promote GI and urinary tract motility
-muscarinic receptor selective

Front 12

Muscarine

Back 12

-quarternary amine; poorly absorbed
-toxicity treated with atropine

Front 13

Pilocarbine

Back 13

-tertiary amine (not hydrolyzed by AChE)
-miotic agent

Front 14

Atropine

Back 14

-muscarinic receptor antagonist
-well absorbed from gut
-dry as a bone, blind as a bat, red as a beet, mad as a hatter

Front 15

Scopalamine

Back 15

-atropine analogue
-significant CNS effects (sedation)
-Prevent/treat motion sickness
-chemotherapy nausea

Front 16

Benztropine

Back 16

-muscarinic receptor antagonist
-adjunct in therapy for Parkinson's

Front 17

Tolterodine

Back 17

-M3 selective antagonist
-urinary incontence

Front 18

Ipratropium

Back 18

-muscarinic receptor antagonist
-inhaled for asthma, COPD

Front 19

Tropicamide

Back 19

-muscarinic receptor antagonist
-shorter duration; used for ophthalmologic examination

Front 20

Nicotine

Back 20

-acute toxicity; fatal dose is 40mg
-readily absorbed

Front 21

Trimethaphan

Back 21

-ganglion-blocking nicotinic receptor antagonist
-hypertensive emergencies and dissecting aortic aneurysm

Front 22

Tubocuranine

Back 22

-non-depolarizing NMJ blocker
-isoquinoline derivative
-block channel in closed position

Front 23

Pancuronium

Back 23

-non-depolarizing NMJ blocker
-steroid derivative
-block channel in closed position

Front 24

Succinylcholine

Back 24

-agonist/antagonis effects
-opens channel, causing depolarization
-less susceptible to hydrolysis, so channel remains open

Front 25

Edrophonium

Back 25

-simple alcohol AChE inhibitor
-diagnostic test for myasthenia gravis or Eaton-Lambert syndrome

Front 26

Neostigmine

Back 26

-carbamate AChE inhibitor
-permanent charge; doesn't enter CNS
-treatment for MG, ileus, reversal of neuromuscular blockade

Front 27

Pyridostigmine

Back 27

-carbamate AChE inhibitor
-permanent charge; doesn't enter CNS
-treatment for MG

Front 28

Physostigmine

Back 28

-carbamate AChE inhibitor
-well-absorbed; enters CNS
-treatment for glaucoma, reversal of neuromuscular blockade

Front 29

Echothiophate

Back 29

polar; not well absorbed
organophosphate
Used for glaucoma
Treat toxicity with pralidoxime

Front 30

Thiophosphate insecticides

Back 30

Organophosphate
well-absorbed; lipid soluble
Converted to active oxygen analog
May undergo aging after phosphorylation
Pralidoxime may reverse phosphorylation bond

Front 31

Trimethaphan

Back 31

-ganglion-blocking nicotinic receptor antagonist
-hypertensive emergencies and dissecting aortic aneurysm

Front 32

Tubocuranine

Back 32

-non-depolarizing NMJ blocker
-isoquinoline derivative
-block channel in closed position

Front 33

Pancuronium

Back 33

-non-depolarizing NMJ blocker
-steroid derivative
-block channel in closed position

Front 34

Succinylcholine

Back 34

-agonist/antagonis effects
-opens channel, causing depolarization
-less susceptible to hydrolysis, so channel remains open

Front 35

Edrophonium

Back 35

-simple alcohol AChE inhibitor
-diagnostic test for myasthenia gravis or Eaton-Lambert syndrome

Front 36

Neostigmine

Back 36

-carbamate AChE inhibitor
-permanent charge; doesn't enter CNS
-treatment for MG, ileus, reversal of neuromuscular blockade

Front 37

Pyridostigmine

Back 37

-carbamate AChE inhibitor
-permanent charge; doesn't enter CNS
-treatment for MG

Front 38

Physostigmine

Back 38

-carbamate AChE inhibitor
-well-absorbed; enters CNS
-treatment for glaucoma, reversal of neuromuscular blockade

Front 39

Echothiophate

Back 39

polar; not well absorbed
organophosphate
Used for glaucoma
Treat toxicity with pralidoxime

Front 40

Thiophosphate insecticides

Back 40

Organophosphate
well-absorbed; lipid soluble
Converted to active oxygen analog
May undergo aging after phosphorylation
Pralidoxime may reverse phosphorylation bond

Front 41

Tacrine, donepezil, rivastigmine, galantamine

Back 41

anticholinesterase inhibitors
treat mild to moderate Alzheimer's
modest results