Pharm1E1 Cholinergic Agonists Flashcards

1
Q

muscarinic receptors
only in CNS?
inhibitory?
stimulatory?

A

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

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2
Q

M1 and M3 receptors are coupled to stimulatory ? proteins

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

Gq/11 G-proteins
IP3, DAG
Ca2+

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3
Q

M2 receptors are coupled to inhibitory ? proteins

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

Gi/G0
cAMP
hyperpolarization

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4
Q

nicotinic receptors are ?, ? channels

muscarinic is 7 transmembrane G

A

pentameric, ion

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5
Q

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

A

excitatory, postsynaptic

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6
Q

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 ?

A

reflex arcs

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

result in bradycardia, SA node, AV node

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7
Q

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

A

presynaptic nerve

Ach, NE

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8
Q

Nm receptors responds to both ? and ?

A

nicotine, acetylcholine

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9
Q

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

A

nicotine, depolarization blockade, flaccid paralysis

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10
Q

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

A

contraindications of choline esters

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11
Q

acetylcholine
bethanechol
carbechol
methacholine

A

choline esters

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12
Q

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

A

acetylCHOLine

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13
Q

longer lasting than Ach, more resistant to AchE

used to Dx bronchial airway hypersensitivity via bronchoconstriction

A

methaCHOLine (provoCHOLine)

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14
Q

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 ?

A

carbaCHOL
muscarinic receptors
nicotine (it can only bind here)

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15
Q

promotes urination, NONobstructive urinary retention

only choline ester given SYSTEMICALLY

A

bethaneCHOL (URecholine)

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16
Q

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

A

cholinomimetic alkaloids
nicotine
muscarine

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17
Q

muscarINE
pilocarpINE
nicotINE
vareniclINE

A

alkaloids

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18
Q

no clinical uses

psychodelic effect- amanita muscaria (mushroom)

A

muscarINE

19
Q

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!

A

pilocarpINE

20
Q

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

A

nicotine

21
Q

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

A

vareneclINE

22
Q

endothelium intact

A

vasodilation from release of nitric oxide

23
Q

endothelium not intact

A

vasoconstriction

24
Q

quarternary alcohols and carbamates are ?

A

reversible

25
Q

organophosphates are ?

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

irreversible
hundreds of hours, covalent
PAM (pralidoxime)

26
Q

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

A

blood pressure

hypotension

27
Q
edrophonIUM
physosSTIGmine
neoSTIGmine
Aricept
COGnex
REMINyl
EXelon (rivaSTIGmine)
pyridoSTIGmine
ambenonIUM
HUMORsol
carbaCIDE (carbaryl)
A

indirect acting reversible cholinesterase inhibitors

28
Q

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

A

edrophonIUM

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

29
Q

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

A

physoSTIGmine

30
Q

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

A

neoSTIGmine

31
Q

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

A

pyridoSTIGmine

32
Q

Alzheimers disease Tx- 3

A

Aricept
COGnex
REMINyl

33
Q

derived from daffodils

A

reminyl

34
Q

PD w/ dementia

pseudo-irreversible

A

EXelon

35
Q

used for MG

4-8 hours

A

mytelase

36
Q

rarely used due to liver toxicity

A

COGnex

37
Q

echothiphate
malathion & parathion
nerve agents (gases)

A

irreversible cholinesterase inhibitors- mostly pesticides

38
Q

low lipid solubility

used in GLC

A

echothiophate

39
Q

opthal drops for GLC

A

HUMORsol

40
Q

treats lice

A

carbaCIDE

41
Q

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

A

PAM, aging

42
Q

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

A

malathion

43
Q

NOT rapidly detoxified in vertebrate; more dangerous and not available

A

parathion

44
Q

sarin
soman
tabun
VX

A

nerve agents- death from respiratory failure