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PHARM Exam 2 > Cholinergic Agonists & Antagonists > Flashcards

Cholinergic Agonists & Antagonists Flashcards

1
Q

Muscarinic Agonist Prototype

A

Acetylcholine

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2
Q

Acetylcholine - Pharmacokinetics

A

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

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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

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4
Q

Acetylcholine effects on cardiac system

A

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

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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

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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

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7
Q

Acetylcholine (drug) adverse effects

A

bradycardia, hypotension

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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

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9
Q

What is the prototype ester?

A

bethanechol

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10
Q

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

A

resistant to hydrolysis by cholinersterases

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11
Q

Bethanechol effect on smooth muscle

A

increases contraction of bladder and GI tract

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12
Q

Bethanechol - Therapeutic Uses

A

postop and postpartum urinary retention

GERD and gastric atony

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13
Q

The two types of esters

A

Bethanechol - prototype

methacholine - other

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14
Q

Prototype Alkaloid

A

Pilocarpine

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15
Q

Action of Pilocarpine

A

partial agonist of all muscarinic receptors

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16
Q

Pilocarpine - Admin/Use

A

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

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17
Q

Pilocarpine - therapeutic uses

A

xerostomia

wide-angle glaucoma

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18
Q

Alkaloid, selective M3 agonist

A

Cevimeline

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19
Q

Cevimeline affinity for cardiac M2 receptors

A

low

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20
Q

Cevimeline is usually prescribed for…

A

Sjogren’s Syndrome

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21
Q

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

A

Cevimeline

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22
Q

Toxicity indications for muscarinic agonists

A

sweating
hypotension
GI effects

23
Q

Contraindications for muscarinic agonists

A

hyperthyroidism
asthma
peptic ulcer

24
Q

Muscarinic agonist antidotes

A

atropine

epinephrine

25
Q

Muscarinic Antagonist Prototype

A

atropine

26
Q

Chemical classification of atropine

A

belladonna alkaloid

27
Q

Atropine - MOA

A

competitive blockade of muscarinic receptors

  • produces opposing effect of muscarinic receptor
  • super high doses –> nicotinic blockade too
  • no muscarinic selectivity
28
Q

Atropine - Pharmacokinetics

A

cross BBB

blocks receptors in blood vessels, sweat glands, and CNS

29
Q

Tissue Response is oral dose-dependent

A

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
Q

Atropine - CNS effects

A

low dose - mild excitation

toxic dose - hallucinations, delirium resembling psychosis

31
Q

Atropine - Ocular effects

A

mydriasis - photophobia

cycloplegia - blurred near vision

32
Q

Atropine - CV effects

A

heart - tachy, result of blocking vagal impulses

circulation - no effect @ normal dose, flushing reaction

33
Q

Atropine - respiratory effects

A

decreased bronchial secretions

relaxed bronchial smooth muscle

34
Q

Atropine - GI effects

A

inhibit salivation
reduced tone/motility
partial reduction in gastric acid secretion

35
Q

Atropine - therapeutic use

A

pre-op: reduce secretions
brady/AV block: cardiac resuscitation
mydriasis/cycloplegia (but, long duration of action)
AChE inhibitor poisoning: muscarinic effects

36
Q

Atropine - Adverse effects

A

dry mouth, blurred vision, photophobia, tachy, GI distress, hot/dry skin, urinary retention, confusion

37
Q

Atropine - Contraindication

A

prostatic hypertrophy and narrow-angle glaucoma

38
Q

Atropine - antidote

A

physostigmine: elevates synaptic concentration of agonist ACh

39
Q

Scopolamine

A

muscarinic antagonist

40
Q

Scopolamine - CNS penetrance

A

scopolamine better at CNS penetration than atropine

41
Q

Scopolamine - uses

A

sedative with euphoric effects

suppress emesis/motion sickness, blocks M receptors in vestibular apparatus

42
Q

Scopolamine - admin route

A

transdermal

43
Q

Ipratropium bromide drug classification

A

muscarinic antagonist

44
Q

Ipratropium bromide - characteristics

A

quaternary amine

dose NOT cross BBB

45
Q

Ipratropium bromide - therapeutic use

A

bronchodilator for COPD/asthma

46
Q

ipratropium bromide - admin route

A

inhalation, therefore minimal systemic effects

47
Q

Tropicamide - drug classification

A

muscarinic antagonist

48
Q

tropicamide - action

A

used for eye surgeries and causes mydriasis and cycloplegia (SHORT DURATION OF ACTION)

49
Q

Tolterodine - drug classification

A

muscarinic antagonist

50
Q

Tolterodine - receptor target & use

A

non-selective muscarinic antagonist

treats OAB

51
Q

Tolterodine - MOA

A

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
Q

Tolterodine - Efficacy

A

modest, takes up to 4 weeks to reach full efficacy

effective in ~30% of patients & anti-ACh side effects limit dose escalation

53
Q

What is a major concern associated with Tolterodine?

A

CNS-related anticholinergic effects, esp. problematic in cognitively-impaired geriatric patients

PHARM Exam 2 (4 decks)

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