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Q3 Pharm Cholinergics > Cholinergic Agonists/Antagonists > Flashcards

Cholinergic Agonists/Antagonists Flashcards

1
Q

ACh stimulates what two types of receptors?

A

muscarinic

nicotinic

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2
Q

Muscarinic (M) Receptors found in what organs? (6)

A 
(parasymp)
eye
GI
Bladder
salivary glands
sweat glands
heart
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3
Q

Muscarinic Receptors respond to what?

A

muscarine

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4
Q

M1, M3 2ndary messengers?

A

Gq -> DAG -> ↑ Ca2+ (excitatory)

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5
Q

M2 2ndary messenger?

A

Gi -> ↓ AC (inhibitory)

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6
Q

Nicotinic Receptors found where?

A

brain
adrenal medulla
autonomic ganglia
neuromuscular jxn

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7
Q

Nicotinic Receptors respond to?

A

nicotine

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8
Q

N receptor 2ndary messenger?

A

Na+ Ion channels (excitatory)

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9
Q

Example of Direct-Acting agonists?

A

muscarinic agonists stim muscarinic receptors

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10
Q

Example of Inderect-Acting agonists?

A

Cholinesterase inhibitors ↓ ACh breakdown

Ѧ stims M and nicotinic receptors longer

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11
Q

Direct Agonists? (6)

A 
ACh
Methacholine
Carbachol
Bethanechol
Pilocarpine
Nicotine
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12
Q

Which direct agonists are cholinergic agonists?

A

ACh

Bethanechol

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13
Q

Properties of ACh vs Bethanechol?

A

ACh:
stim M and nicotinic receptors
hydrolyzed by AChE

Bethanechol:
stim M recpetors
resists AChE
doesn’t enter brain

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14
Q

Which direct agonists are muscarinic agonists?

A

Muscarine

Pilocarpine

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15
Q

What 2 kinds of receptors are extra sensitive to pilocarpine?

A

sweat

salivary

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16
Q

Bethanechol has the most affect on what? (2)

A

bladder

GI

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17
Q

Side Effects of Muscarinic Agonists? (8)

A 
salivation/tears
N/V
diarrhea
HA
visual disturbances
bronchospasm
bradycardia
shock
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18
Q

Tx for mushroom poisoning (muscarine)?

A

atrophine (antagonist)

albuterol

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19
Q

Contraindications for muscarine (3)

A

1) asthma/COPD (bronchoconstriction)
2) peptic ulcer (↑ acid prdxn)
3) bowel obstruction (↑ peristalsis)

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20
Q

Nicotinic (N) receptors are located on what kind of proteins?

A

ligand-gated Na+ channels

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21
Q

Nicotinic receptors are found where? (3)

A

1) autonomic ganglia (Nn)
2) skeletal mm (Nm)
3) brain (Nn)

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22
Q

N recpetors are rapidly what?

A

desensitized to nicotine

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23
Q

Stim of N receptors in brain results in:

low doses

high doses

toxic doses

A

low doses = ↑ alertness/attention

high doses = tremor, emesis, ↑ respiration

toxic = convulsions

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24
Q

Stim of N receptors in ganglion activates symp or parasymp?

A

activate BOTH

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25
Q

Stim of N receptors in ganglion results in:

symp effects

parasymp effects

A

symp = HTN, tachycardia, vagal bradycardia

parasymp = N/V, diarrhea, urination

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26
Q

Nicotine toxicity results in? (4)

A

vomiting
CNS stim = convulsions, coma, resp arrest
skeletal mm depol = paralysis
HTN, arrhythmia

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27
Q

Tx for nicotine toxicity?

A

atropine = ↓ parasymp by blocking M receptors

anticonvulsants

respiratory assistance

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28
Q

Varenicline (Chantix) is what?

Used for what?

S/E?

A

part agonist of N rec in brain

↓ nicotine craving

N/V, gas, constipation
sleep and psych disturb

29
Q

Cholinesterase Inhibitors do what?

A

↑ time ACh available to stim receptors

30
Q

4 types of Cholinesterase Inhibitors?

A

1) neostigmine (Prostigmin)
2) physostigmine (Eserine)
3) edrophonium (Tensilon)
4) organophosphates

31
Q

Neostigmine inhibits AChE how?

A

binds -> slows AchE

32
Q

Carbamates inhibit AChE how?

A

covalent bond -> slows AchE

33
Q

Edrophonium inhibition of AChE?

A

reversible
short acting (5 min)
injected
no CNS penetration

34
Q

Organophosphate inhibition of AChE?

A

become irreversible w/ aging

long lasting

35
Q

Pralidoxime (2-PAM) is?

A

strong nucleophile,
effective at NMJ,
no CNS,
prevents aging of enz so use to counteract organophosphates

36
Q

AChE Inhibitors effects on:

CNS

Eye

GI, Bladder

Respiratory

A

CNS = ↑ alertness, memory
toxic: convulsions, resp arrest

Eye = miosis, near vision

GI, Bladder = stim, diarr, urination

Respiratory = salivation, secretions, bronchoconstriction

37
Q

AChE Inhibitors effects on cardiovascular?

A

All ganglia activated: parasym dominates

bradycardia, ↓ contraction force, ↓ CO

little effect on BP (no cholinergic innerv)

38
Q

AChE Inhibitors effects on NMJ:

low dose

high dose

A

low = ↑ ACh action, ↑ mm strength

high = twitched, fasiculations, paralysis

39
Q

Neostigmine (Prostigmin) effects on AChE?

A 
last 4 hrs
no brain absorp
↑ bladder motility
reverse NM blockade post surgery
tx myasthenia gravis
40
Q

Edrophonium (Tensilon) used for what?

A

1) diagnose myasthenia gravis (immediate improvement of sxs = + result)
2) monitor AChE inhibitor tx (will ↓ strength if dose too high)

41
Q

Echothinophate is?

Used for?

A

organophosphate AChE inhibitor
very long acting

eyedrops to ↓ intraocular pressure of narrow-angle glaucoma

42
Q

Glaucome tx

A

direct agonists
cholinesterase inhibitors
direct/AChE inhibitor combos

43
Q

Myasthenia Gravis

A

autoimmune dx,
antibodies ↓ # of N receptors,
causes mm weakness w/ use,
small mm of head most effected (e.g. eye)

44
Q

AChE inhibitor toxicity results?

A 
SLUDGE:
Salivation
Lacrimation
Urination
Defecation
Gastric distress
Emesis

NM stim followed by paralysis

45
Q

Tx for organophosphate AChE inhibitor poisoning? (4)

A

atropine
2-PAM w/i 4 hrs
diazepam
respiration support

46
Q

Atropine effects?

0.5 mg

1 mg

2 mg

5 mg

10 mg

A

0.5 mg = dry mouth, ↓ sweat

1 mg = ↑ HR, thirsty

2 mg = blurred vision, tachycard, palp

5 mg = ф urine, hot/dry

10 mg = rapid/weak pulse, ataxia, coma

47
Q

Muscarinic Antagonist (antichol) drugs method of action?

Prototype drug?

A

bind M receptor, displacing ACh

Atropine

48
Q

Scopolamine method of action?

Administration?

Effects on CNS?

Used for?

A

binds M receptors, displaces ACh

patch

euphoria, amnesia, drowsiness
hallucination, coma

motion sickness

49
Q

Opthamology M antag drug for dilation?

A

Tropicamide (6 hrs)

50
Q

M antagonist drug effects on cardiovas?

A

↓ tone = tachycardia
M2 receptors blocked = ↑ NE

little effect on babies/elderly cuz vagal tone is low

51
Q

M antagonists drug effects on eye?

A 
↓ tone
pupil dilates
lens flattens (can;t focus)
phtotphobia
dry eyes
52
Q

M antagonist drug effects on respiration?

A

reverse bronchoconstriction

best for COPD or acute asthma attack

53
Q

M antagonist drug effects on GI?

A

↓ motility and secretions
↓ tone
antispasmodic

54
Q

M antagonist drug effects on bladder?

A

↓ motility

55
Q

M antagonist drug effects on secretions?

A

↓ sweat, saliva and tears

dry eyes, mouth

56
Q

Use of M Antagonists for Opthamology?

Prototype?

A

eye dilation for exam
cycloplegia (IOM paralysis)

tropicamide

57
Q

Use of M Antagonists for cardiac?

A

↓ bradycardia
reverse heart block

Atropine used post MI

58
Q

Ipatropium (Atrovent) is what drug type?

Used for?

A

M antagonist

COPD, acute asthma

59
Q

Tolterodine (Detrol) is what drug type?

Used for?

A

M antagonist (M3)

overactive bladder

60
Q

Oxybutynin (Ditropan) is what drug type?

Used for?

A

M antagonist

bladder spasm post surgery

61
Q

Contraindications for M Antagonists?

A

narrow angle glaucoma (↑ IO pressure)

benign prostate hyperplasia (↑ urine difficulties)

62
Q

Atropine overdose signs?

A

dry as bone
blind as bat
red as beet
mad as hatter

63
Q

Neuromuscular Blockers do what?

A

block nicotinic receptors on skeletal mm

64
Q

Non-depolarizing NM blockers mode of action?

Administered?

Reverse effect w/ what?

Used for?

A

reversible competitor for ACh receptors

IV

AChE Inhibitors (↑ ACh)

mm relax in surgery

65
Q

Depolarizing NM blocker action?

A

temp paralysis of extremities, face/neck, respiration

Can results in hyperkalemia = MI

66
Q

Depolarizing NM blocker prototype drug?

A

succinylcholine

67
Q

Contraindications for succinylcholine?

A 
< 8yo
soft tissue damage/burns
nontraumatic rhadbomylosis
quad or paraplegia
MD
68
Q

NM blockers enhanced by what drugs?

A

anesthetics
aminoglycoside antibiotics
TCN
Ca2+ channel blockers

69
Q

Ganglion Receptor Blocker mode of action?

A

block nicotine receptors in all auto ganglia,
non-depol competitive antagonist,
↓ total output of ANS

Q3 Pharm Cholinergics (7 decks)

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