Pharm1E1 Cholinergic Agonists Flashcards Preview

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Flashcards in Pharm1E1 Cholinergic Agonists Deck (44):
1

muscarinic receptors
only in CNS?
inhibitory?
stimulatory?

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

2

M1 and M3 receptors are coupled to stimulatory ? proteins
-leads to an increase in ? and ?
-leads to an increase in intracellular ?

Gq/11 G-proteins
IP3, DAG
Ca2+

3

M2 receptors are coupled to inhibitory ? proteins
-inhibits production of ?
-leads to ? through the opening of K channels

Gi/G0
cAMP
hyperpolarization

4

nicotinic receptors are ?, ? channels
(muscarinic is 7 transmembrane G)

pentameric, ion

5

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

excitatory, postsynaptic

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 ?

reflex arcs

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

result in bradycardia, SA node, AV node

7

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

presynaptic nerve
Ach, NE

8

Nm receptors responds to both ? and ?

nicotine, acetylcholine

9

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

nicotine, depolarization blockade, flaccid paralysis

10

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

contraindications of choline esters

11

acetylcholine
bethanechol
carbechol
methacholine

choline esters

12

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

acetylCHOLine

13

longer lasting than Ach, more resistant to AchE
used to Dx bronchial airway hypersensitivity via bronchoconstriction

methaCHOLine (provoCHOLine)

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 ?

carbaCHOL
muscarinic receptors
nicotine (it can only bind here)

15

promotes urination, NONobstructive urinary retention
only choline ester given SYSTEMICALLY

bethaneCHOL (URecholine)

16

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

cholinomimetic alkaloids
nicotine
muscarine

17

muscarINE
pilocarpINE
nicotINE
vareniclINE

alkaloids

18

no clinical uses
psychodelic effect- amanita muscaria (mushroom)

muscarINE

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!

pilocarpINE

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

nicotine

21

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

vareneclINE

22

endothelium intact

vasodilation from release of nitric oxide

23

endothelium not intact

vasoconstriction

24

quarternary alcohols and carbamates are ?

reversible

25

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

irreversible
hundreds of hours, covalent
PAM (pralidoxime)

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 ?

blood pressure
hypotension

27

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

indirect acting reversible cholinesterase inhibitors

28

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

edrophonIUM

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

29

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

physoSTIGmine

30

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

neoSTIGmine

31

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

pyridoSTIGmine

32

Alzheimers disease Tx- 3

Aricept
COGnex
REMINyl

33

derived from daffodils

reminyl

34

PD w/ dementia
pseudo-irreversible

EXelon

35

used for MG
4-8 hours

mytelase

36

rarely used due to liver toxicity

COGnex

37

echothiphate
malathion & parathion
nerve agents (gases)

irreversible cholinesterase inhibitors- mostly pesticides

38

low lipid solubility
used in GLC

echothiophate

39

opthal drops for GLC

HUMORsol

40

treats lice

carbaCIDE

41

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

PAM, aging

42

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

malathion

43

NOT rapidly detoxified in vertebrate; more dangerous and not available

parathion

44

sarin
soman
tabun
VX

nerve agents- death from respiratory failure