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PHRM 825 > Cholinergic Agonists > Flashcards

Cholinergic Agonists Flashcards

1
Q

m1 receptor tissue

A

postganglionic

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2
Q

m1 receptor response

A

depolarization

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3
Q

m2 receptor tissue

A

heart

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4
Q

m2 receptor response

A

inhibition

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5
Q

m3 receptor tissue

A

smooth muscles, exocrine glands, endothelium

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6
Q

m3 receptor response

A

contraction, secretion, relaxation

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7
Q

which receptor does acetylcholine have the highest affinity for?

A

muscarinic

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8
Q

acetylcholine biosynthesis

A

choline into nerve terminal
acetylcholine + choline
transported into storage vesicle by VAT
Ca goes up in cell, vesicles fuse and ACh released (this can be blocked by botox)
ACh binds to receptors and is terminated by AChE

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9
Q

muscarinic agonist heart effects

A

M2 leads to decrease in HR, conduction, and force

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10
Q

muscarinic agonist exocrine glands effect

A

M3 increase in secretion (tears, saliva, sweat)

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11
Q

muscarinic agonist smooth muscle effect

A

M3 increase in contraction

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12
Q

muscarinic agonist sphincter effect

A

M3 relaxation

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13
Q

muscarinic agonist CNS effects

A

M1 tremor, hypothermia, increased locomotor activity, improved cognition

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14
Q

direct acting cholinergic receptors structure

A

esters (like acetylcoa)

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15
Q

chemical modifications to direct acting cholinergic agonist

A

add beta methyl, add carbamate

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16
Q

modification effect on activity and sensitivity to AChE

A

beta methyl increse muscarinic decrease nicotinic, adding either will decrease sensitivity to AChE

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17
Q

what are alkaloids

A

natural product, stereochemistry, selective

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18
Q

pilocarpine target

A

muscarinic agonist

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19
Q

pilocarpine use

A

for dry mouth (xerostemia/sjorgens), promote sweating, urination, salivation, glaucoma (increase outflow)

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20
Q

why are antimuscarinic drugs contraindicated in glaucoma?

A

STRONG side effects

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21
Q

methacholine

A

muscarinic agonist
provocative test for hyperactive airways

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22
Q

carbachol

A

muscarinic agonist
ocular (surgery, glaucoma)

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23
Q

bethanechol

A

muscarinic agonist
GI stimulation, treatment of urinary retention

24
Q

PSNS side effects

A

diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating

25
Q

PSNS cautions

A

asthma, COPD, coronary insufficiency, peptic ulcer

26
Q

nicotinic receptor structure

A

ionotropic (Na ion channels)

27
Q

nicotinic receptor neurotransmitters

A

acetylcholine and nicotine

28
Q

nicotinic receptors location in body

A

Nm: skeletal muscle endplate
Nn: autonomic ganglia, brain (CNS)

29
Q

nicotine effects

A

alerting, dopamine release (addictive), hypertension, tachycardia, seizures

30
Q

varenicline (Chantix)

A

nicotinic partial agonist
produces low amounts dopamine and blocks nicotine binding
EFFECTIVE but side effect suicide (boxed warning)

31
Q

types of cholinesterases

A

acetylcholinesterase, plasma cholinesterase

32
Q

acetylcholinesterase location and selectivity

A

synapses, ACh selective

33
Q

plasma cholinesterase location and selectivity

A

plasma (non neuronal), ACh, succinylcholine, local anesthetics

34
Q

acetylcholinesterase activity esteric and anionic site

A

esteric site = acetyl , anionic site = choline
serine attaches to acetyl, choline released
water nuc attacks acetyl and then releases it
enzyme is reactivated!

35
Q

AChE inhibitors general structure

A

quarternary ammonium alcohol or carbamate, organophosphate

36
Q

edrophonium

A

reversible and noncovalent
Myasthenia Gravis

37
Q

AChE inhibitors carbamates

A

reversible and covalent
more slowly hydrolyzed than ACh
carbamates just chills for a sec

38
Q

pyridostigmine

A

reversible and noncovalent
treatment MG, potential nerve gas exposure

39
Q

neostigmine

A

reversible and covalent
treatment MG, post op urinary retention

40
Q

what is a problem with AChE inhibitors?

A

exessive cholinergic receptor activation

41
Q

AChE inhibitors organophosphates

A

irreversible, covalent, longer acting, most are toxic

42
Q

echothiophate

A

organophosphate irreversible covalent
originally for glaucoma, not used now

43
Q

sarin

A

organophosphate irreversible covalent
nerve gases

44
Q

malathion/diazinon

A

organophosphate irreversible covalent
insecticide
rapidly inactivated in mammals

45
Q

malathion biotransformation in insects vs adults

A

insects: cyp450 converts s to o to become toxic
mammals: esterase hydrolyzes functional group to become inactive

46
Q

aging effect organophosphates

A

bind covalently to serine, functional group dealkylated, water can not hydrolyze the remaining group (this is irreversible aging)

47
Q

aging antidote

A

2-PAM

48
Q

2-PAM

A

antidote for pesticide or nerve poisoning, effective if given quick before aging occurs
hydrolyzes the organophosphate
combined with atropine

49
Q

Alzheimer’s Disease

A

loss of cholinergic neurons in the brain

50
Q

donepezil

A

symptoms of Alzheimers
does not slow progression of disease
binds anionic site

51
Q

rivastigmine

A

symptoms Alzhemiers
reversible carbamate
loses effectiveness as disease progresses

52
Q

galantamine

A

symptoms alzhemiers
reversible competitive inhibitor
loses effectiveness as disease progresses

53
Q

memantamine

A

symptoms alzheimers
may slow progression!!

54
Q

SLUD

A

salivation, lacrimation, urination, defecfation

55
Q

cholinergic side effects treatment

A

atropine (2PAM if irreversible)

56
Q

physostigmine

A

antimuscarinic poisioning

PHRM 825 (24 decks)

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