Pharm1E1 Cholinergic Agonists

Question 1

muscarinic receptors
only in CNS?
inhibitory?
stimulatory?

Answer 1

M4, M5
M2, M4 (M2 decreases effects on heart)
M1, M3, M5

Question 2

M1 and M3 receptors are coupled to stimulatory ? proteins

• leads to an increase in ? and ?
• leads to an increase in intracellular ?

Answer 2

Gq/11 G-proteins
IP3, DAG
Ca2+

Question 3

M2 receptors are coupled to inhibitory ? proteins

• inhibits production of ?
• leads to ? through the opening of K channels

Answer 3

Gi/G0
cAMP
hyperpolarization

Question 4

nicotinic receptors are ?, ? channels

muscarinic is 7 transmembrane G

Answer 4

pentameric, ion

Question 5

both Nn and Nm mediate fast ? ? potentials resulting in the activation of the post synaptic cell

Answer 5

excitatory, postsynaptic

Question 6

direct effects of muscarinic agonists on the CV system can be altered through ?
EX: IV infusion of a low dose of Ach will cause a drop in blood pressure that is detected by ?, resulting in an ?
-a larger dose of Ach will ? due to a slowed firing rate w/in the ? and a decreased conduction velocity of the ?

Answer 6

reflex arcs

baroreceptors, increase in SNS stimulation on the heart- increase HR- reflex tachycardia

result in bradycardia, SA node, AV node

Question 7

muscarinic agonists on the ? terminals decrease the release of ? or ?

Answer 7

presynaptic nerve

Ach, NE

Question 8

Nm receptors responds to both ? and ?

Answer 8

nicotine, acetylcholine

Question 9

continued exposure to a nonhydrolyzable agonist like ? will lead to ? and eventually a ?

Answer 9

nicotine, depolarization blockade, flaccid paralysis

Question 10

hyperthyroidism, asthma, CAD (hypotension), acid peptic disorders (increased gastric secretion), obstructive urinary retention

Answer 10

contraindications of choline esters

Question 11

acetylcholine
bethanechol
carbechol
methacholine

Answer 11

choline esters

Question 12

only high IV doses for short term effects
reduce postop IOP
last about 20 min
used in sweat spot test for diabetics

Answer 12

acetylCHOLine

Question 13

longer lasting than Ach, more resistant to AchE

used to Dx bronchial airway hypersensitivity via bronchoconstriction

Answer 13

methaCHOLine (provoCHOLine)

Question 14

is mostly NICOTINIC (other esters are M3)
increase in skeletal muscle activation
limit to opthalmic applications
IF YOU GIVE ATROPINE- it will block ? and you will see all of the effects of ?

Answer 14

carbaCHOL
muscarinic receptors
nicotine (it can only bind here)

Question 15

promotes urination, NONobstructive urinary retention

only choline ester given SYSTEMICALLY

Answer 15

bethaneCHOL (URecholine)

Question 16

CAN cross BBB
some are highly soluble and readily absorbed i.e. ?
some are quarternary amines and less readily absorbed i.e.?

Answer 16

cholinomimetic alkaloids
nicotine
muscarine

Question 17

muscarINE
pilocarpINE
nicotINE
vareniclINE

Answer 17

alkaloids

Question 18

no clinical uses

psychodelic effect- amanita muscaria (mushroom)

Answer 18

muscarINE

Question 19

initial, acute treatment of open angle GLC
sjogren’s syndrome- xerostomia
reverses mydratic actions
rapid miosis
dont use in IOP that are >45 because it can close the angle further!

Answer 19

pilocarpINE

Question 20

increase HR, secretions of NE&Epi
increase tone and motility of GI
(both PNS and SNS b/c it’s nicotinic)
clinically used as a smoking cessation agent

Answer 20

nicotine

Question 21

ALSO NICOTINIC
partial agonist at neuronal nicotinic receptors
neuropsychiatric changes i.e. agitation, depressed mood, suicidal thoughts

Answer 21

vareneclINE

Question 22

endothelium intact

Answer 22

vasodilation from release of nitric oxide

Question 23

endothelium not intact

Answer 23

vasoconstriction

Question 24

quarternary alcohols and carbamates are ?

Answer 24

reversible

Question 25

organophosphates are ? - last ? due to the ? bonding - if given early enough- ? (cholinesterase regenerator) can treat patients suffering from organophosphate poisoning

Answer 25

irreversible hundreds of hours, covalent PAM (pralidoxime)

Question 26

moderate doses of cholinesterase inhibitors (indirect) will reduce HR/CO and increase ?, BUT large/toxic doses will result in marked bradycardia, reduced CO and ?

Answer 26

blood pressure | hypotension

Question 27

``` edrophonIUM physosSTIGmine neoSTIGmine Aricept COGnex REMINyl EXelon (rivaSTIGmine) pyridoSTIGmine ambenonIUM HUMORsol carbaCIDE (carbaryl) ```

Answer 27

indirect acting reversible cholinesterase inhibitors

Question 28

Dx of myasthenia gravis- increase in muscle strength is positive assesses the long term anticholinesterase therapy used in MG (pryidoSTIGmine) short DOA

Answer 28

edrophonIUM *decrease in muscle strength would indicate that they have been exposed to an anticholinesterase insecticide; driven from stimulation to depolarizing inhibition

Question 29

antidote for anti-muscarinic toxicity miosis, accomodation, decrease in IOP nonobstructive paralytic ileus, postop atony of bladder

Answer 29

physoSTIGmine

Question 30

MG post-op bladder retention REVERSES anaesthesia by reversing NM blockade

Answer 30

neoSTIGmine

Question 31

MG gravis FIRST LINE Tx NM blockade reversal **prophylactic Tx of NERVE GAS

Answer 31

pyridoSTIGmine

Question 32

Alzheimers disease Tx- 3

Answer 32

Aricept COGnex REMINyl

Question 33

derived from daffodils

Answer 33

reminyl

Question 34

PD w/ dementia | pseudo-irreversible

Answer 34

EXelon

Question 35

used for MG | 4-8 hours

Answer 35

mytelase

Question 36

rarely used due to liver toxicity

Answer 36

COGnex

Question 37

echothiphate malathion & parathion nerve agents (gases)

Answer 37

irreversible cholinesterase inhibitors- mostly pesticides

Question 38

low lipid solubility | used in GLC

Answer 38

echothiophate

Question 39

opthal drops for GLC

Answer 39

HUMORsol

Question 40

treats lice

Answer 40

carbaCIDE

Question 41

organophosphate poisoning can be treated with ? (nucleophile) via regenerating the enzyme if given before ? occurs

Answer 41

PAM, aging

Question 42

rapidly metabolized by birds and mammals to non-toxic metabolites but not insects or fish

Answer 42

malathion

Question 43

NOT rapidly detoxified in vertebrate; more dangerous and not available

Answer 43

parathion

Question 44

sarin soman tabun VX

Answer 44

nerve agents- death from respiratory failure