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Q3 Pharm Cholinergics > Cholinergic Agonists/Antagonists > Flashcards

Cholinergic Agonists/Antagonists Flashcards

(69 cards)

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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
Stim of N receptors in ganglion results in: symp effects parasymp effects
symp = HTN, tachycardia, vagal bradycardia parasymp = N/V, diarrhea, urination
26
Nicotine toxicity results in? (4)
vomiting CNS stim = convulsions, coma, resp arrest skeletal mm depol = paralysis HTN, arrhythmia
27
Tx for nicotine toxicity?
atropine = ↓ parasymp by blocking M receptors anticonvulsants respiratory assistance
28
Varenicline (Chantix) is what? Used for what? S/E?
part agonist of N rec in brain ↓ nicotine craving N/V, gas, constipation sleep and psych disturb
29
Cholinesterase Inhibitors do what?
↑ time ACh available to stim receptors
30
4 types of Cholinesterase Inhibitors?
1) neostigmine (Prostigmin) 2) physostigmine (Eserine) 3) edrophonium (Tensilon) 4) organophosphates
31
Neostigmine inhibits AChE how?
binds -> slows AchE
32
Carbamates inhibit AChE how?
covalent bond -> slows AchE
33
Edrophonium inhibition of AChE?
reversible short acting (5 min) injected no CNS penetration
34
Organophosphate inhibition of AChE?
become irreversible w/ aging | long lasting
35
Pralidoxime (2-PAM) is?
strong nucleophile, effective at NMJ, no CNS, prevents aging of enz so use to counteract organophosphates
36
AChE Inhibitors effects on: CNS Eye GI, Bladder Respiratory
CNS = ↑ alertness, memory toxic: convulsions, resp arrest Eye = miosis, near vision GI, Bladder = stim, diarr, urination Respiratory = salivation, secretions, bronchoconstriction
37
AChE Inhibitors effects on cardiovascular?
All ganglia activated: parasym dominates bradycardia, ↓ contraction force, ↓ CO little effect on BP (no cholinergic innerv)
38
AChE Inhibitors effects on NMJ: low dose high dose
low = ↑ ACh action, ↑ mm strength high = twitched, fasiculations, paralysis
39
Neostigmine (Prostigmin) effects on AChE?
``` last 4 hrs no brain absorp ↑ bladder motility reverse NM blockade post surgery tx myasthenia gravis ```
40
Edrophonium (Tensilon) used for what?
1) diagnose myasthenia gravis (immediate improvement of sxs = + result) 2) monitor AChE inhibitor tx (will ↓ strength if dose too high)
41
Echothinophate is? Used for?
organophosphate AChE inhibitor very long acting eyedrops to ↓ intraocular pressure of narrow-angle glaucoma
42
Glaucome tx
direct agonists cholinesterase inhibitors direct/AChE inhibitor combos
43
Myasthenia Gravis
autoimmune dx, antibodies ↓ # of N receptors, causes mm weakness w/ use, small mm of head most effected (e.g. eye)
44
AChE inhibitor toxicity results?
``` SLUDGE: Salivation Lacrimation Urination Defecation Gastric distress Emesis ``` NM stim followed by paralysis
45
Tx for organophosphate AChE inhibitor poisoning? (4)
atropine 2-PAM w/i 4 hrs diazepam respiration support
46
Atropine effects? 0.5 mg 1 mg 2 mg 5 mg 10 mg
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
Muscarinic Antagonist (antichol) drugs method of action? Prototype drug?
bind M receptor, displacing ACh Atropine
48
Scopolamine method of action? Administration? Effects on CNS? Used for?
binds M receptors, displaces ACh patch euphoria, amnesia, drowsiness hallucination, coma motion sickness
49
Opthamology M antag drug for dilation?
Tropicamide (6 hrs)
50
M antagonist drug effects on cardiovas?
↓ tone = tachycardia M2 receptors blocked = ↑ NE little effect on babies/elderly cuz vagal tone is low
51
M antagonists drug effects on eye?
``` ↓ tone pupil dilates lens flattens (can;t focus) phtotphobia dry eyes ```
52
M antagonist drug effects on respiration?
reverse bronchoconstriction best for COPD or acute asthma attack
53
M antagonist drug effects on GI?
↓ motility and secretions ↓ tone antispasmodic
54
M antagonist drug effects on bladder?
↓ motility
55
M antagonist drug effects on secretions?
↓ sweat, saliva and tears | dry eyes, mouth
56
Use of M Antagonists for Opthamology? Prototype?
eye dilation for exam cycloplegia (IOM paralysis) tropicamide
57
Use of M Antagonists for cardiac?
↓ bradycardia reverse heart block Atropine used post MI
58
Ipatropium (Atrovent) is what drug type? Used for?
M antagonist COPD, acute asthma
59
Tolterodine (Detrol) is what drug type? Used for?
M antagonist (M3) overactive bladder
60
Oxybutynin (Ditropan) is what drug type? Used for?
M antagonist bladder spasm post surgery
61
Contraindications for M Antagonists?
narrow angle glaucoma (↑ IO pressure) | benign prostate hyperplasia (↑ urine difficulties)
62
Atropine overdose signs?
dry as bone blind as bat red as beet mad as hatter
63
Neuromuscular Blockers do what?
block nicotinic receptors on skeletal mm
64
Non-depolarizing NM blockers mode of action? Administered? Reverse effect w/ what? Used for?
reversible competitor for ACh receptors IV AChE Inhibitors (↑ ACh) mm relax in surgery
65
Depolarizing NM blocker action?
temp paralysis of extremities, face/neck, respiration Can results in hyperkalemia = MI
66
Depolarizing NM blocker prototype drug?
succinylcholine
67
Contraindications for succinylcholine?
``` < 8yo soft tissue damage/burns nontraumatic rhadbomylosis quad or paraplegia MD ```
68
NM blockers enhanced by what drugs?
anesthetics aminoglycoside antibiotics TCN Ca2+ channel blockers
69
Ganglion Receptor Blocker mode of action?
block nicotine receptors in all auto ganglia, non-depol competitive antagonist, ↓ total output of ANS

Q3 Pharm Cholinergics (7 decks)

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