Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

PHARM Exam 2 > Cholinergic Agonists & Antagonists > Flashcards

Cholinergic Agonists & Antagonists Flashcards

(53 cards)

Start Studying
1
Q

Muscarinic Agonist Prototype

A

Acetylcholine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Acetylcholine - Pharmacokinetics

A

(+) charge, does not cross BBB
short duration of action
non-selective

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Acetylcholine effects on vascular system

A

vasodilation - stimulate M3 receptors on vascular endothelium, releases NO, diffuses into vascular smooth muscle cells, causing relaxation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Acetylcholine effects on cardiac system

A

(-) chronotropic effect (m2 mediated)
(-) inotropic effect (calcium mediated)
(-) conduction velocity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

In the presence of atropine, ACh-induced stimulation of sympathetic ganglia can be observed as…

A

atropine selectively inhibits muscarinic receptors, so we see vasoconstriction and increased HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Effect of ACh for ophthalmic use

A

produces rapid and complete miosis

ciliary muscle contraction –> open trabecular meshwork –> increase aqueous humor to reduce IOP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Acetylcholine (drug) adverse effects

A

bradycardia, hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

General properties of all synthetic choline esters/cholinomimetic alkaloids

A

more selective and prolonged action than ACh
esters do NOT cross BBB, alkaloids do
used for bladder disorders, xerostomia, and diagnosis of bronchial hyperreactivity, and ophthalmic indications

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the prototype ester?

A

bethanechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

How is the action of bethanechol prolonged (compared to ACh)?

A

resistant to hydrolysis by cholinersterases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Bethanechol effect on smooth muscle

A

increases contraction of bladder and GI tract

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Bethanechol - Therapeutic Uses

A

postop and postpartum urinary retention

GERD and gastric atony

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

The two types of esters

A

Bethanechol - prototype

methacholine - other

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Prototype Alkaloid

A

Pilocarpine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Action of Pilocarpine

A

partial agonist of all muscarinic receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Pilocarpine - Admin/Use

A

topical admin - miosis and blurred vision of distant objects, and fall in IOP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Pilocarpine - therapeutic uses

A

xerostomia

wide-angle glaucoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Alkaloid, selective M3 agonist

A

Cevimeline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Cevimeline affinity for cardiac M2 receptors

A

low

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Cevimeline is usually prescribed for…

A

Sjogren’s Syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Longer duration and fewer side-effects, pilocarpine or cevimeline?

A

Cevimeline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Toxicity indications for muscarinic agonists

Study These Flashcards
A

sweating
hypotension
GI effects

23
Q

Contraindications for muscarinic agonists

Study These Flashcards
A

hyperthyroidism
asthma
peptic ulcer

24
Q

Muscarinic agonist antidotes

Study These Flashcards
A

atropine

epinephrine

25
Muscarinic Antagonist Prototype
atropine
26
Chemical classification of atropine
belladonna alkaloid
27
Atropine - MOA
competitive blockade of muscarinic receptors - produces opposing effect of muscarinic receptor - super high doses --> nicotinic blockade too - no muscarinic selectivity
28
Atropine - Pharmacokinetics
cross BBB | blocks receptors in blood vessels, sweat glands, and CNS
29
Tissue Response is oral dose-dependent
Very low dose - salivary & bronchial secretions suppressed low dose - mydriasis, cycloplegia, tachycardia medium - tone/motility of GI tract and bladder reduced high - gastric acid secretions partially reduced
30
Atropine - CNS effects
low dose - mild excitation | toxic dose - hallucinations, delirium resembling psychosis
31
Atropine - Ocular effects
mydriasis - photophobia | cycloplegia - blurred near vision
32
Atropine - CV effects
heart - tachy, result of blocking vagal impulses | circulation - no effect @ normal dose, flushing reaction
33
Atropine - respiratory effects
decreased bronchial secretions | relaxed bronchial smooth muscle
34
Atropine - GI effects
inhibit salivation reduced tone/motility partial reduction in gastric acid secretion
35
Atropine - therapeutic use
pre-op: reduce secretions brady/AV block: cardiac resuscitation mydriasis/cycloplegia (but, long duration of action) AChE inhibitor poisoning: muscarinic effects
36
Atropine - Adverse effects
dry mouth, blurred vision, photophobia, tachy, GI distress, hot/dry skin, urinary retention, confusion
37
Atropine - Contraindication
prostatic hypertrophy and narrow-angle glaucoma
38
Atropine - antidote
physostigmine: elevates synaptic concentration of agonist ACh
39
Scopolamine
muscarinic antagonist
40
Scopolamine - CNS penetrance
scopolamine better at CNS penetration than atropine
41
Scopolamine - uses
sedative with euphoric effects | suppress emesis/motion sickness, blocks M receptors in vestibular apparatus
42
Scopolamine - admin route
transdermal
43
Ipratropium bromide drug classification
muscarinic antagonist
44
Ipratropium bromide - characteristics
quaternary amine | dose NOT cross BBB
45
Ipratropium bromide - therapeutic use
bronchodilator for COPD/asthma
46
ipratropium bromide - admin route
inhalation, therefore minimal systemic effects
47
Tropicamide - drug classification
muscarinic antagonist
48
tropicamide - action
used for eye surgeries and causes mydriasis and cycloplegia (SHORT DURATION OF ACTION)
49
Tolterodine - drug classification
muscarinic antagonist
50
Tolterodine - receptor target & use
non-selective muscarinic antagonist | treats OAB
51
Tolterodine - MOA
unclear... believed to inhibit detrusor muscle contraction during filling increase bladder capacity and decrease sensation of urgency (blocks basal release of ACh during bladder filling)
52
Tolterodine - Efficacy
modest, takes up to 4 weeks to reach full efficacy | effective in ~30% of patients & anti-ACh side effects limit dose escalation
53
What is a major concern associated with Tolterodine?
CNS-related anticholinergic effects, esp. problematic in cognitively-impaired geriatric patients

PHARM Exam 2 (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions