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Pharmacology Test #3 > Muscarinic Antagonists > Flashcards

Muscarinic Antagonists Flashcards

1
Q

Antimuscarinic

A

acts at the post-ganglionic neuroeffector junction to block parasympathetic autonomic discharge

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2
Q

Neuromuscular blocker

A

acts at the neuromuscular junction to block acetylcholine signaling

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3
Q

Ganglionic blockers

A

act as antagonists at both parasympathetic and sympathetic autonomic ganglia

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4
Q

M1, M3 and M5 receptors signal via

A

intracellular Ca2+ increase and PKC activity

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5
Q

M2 and M4 receptors signal via

A

cAMP decrease and reduced cAMP-dependent PK activity

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6
Q

M1 (G alpha q) receptors are located where?

A

CNS, sympathetic postganglionic cells and presynaptic sites

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7
Q

M3 (G alpha q) receptors are located where?

A

smooth muscle, lungs, eyes, effector cell membranes

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8
Q

M2 (G alpha I) receptors are located where?

A

myocardium, smooth muscle, and presynaptic sites (K+ channel linked = slow heart rate)

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9
Q

M4 (G alpha I) receptors are located where?

A

in the CNS

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10
Q

Atropa belladonna

A

deadly nightshade

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11
Q

Primary clinical uses for antimuscarinic drugs

A

ocular exams, incontinence, irritable bowel syndrome

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12
Q

Secondary clinical uses for antimuscarinic drugs

A

COPD, pre-operative anti-secretory, motion sickness, Parkinson’s disease

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13
Q

Antimuscarinic drug use in ocular exams

A

mydyriasis (pupil dilation): inhibits Ach action on M3 receptors in pupillar constrictor muscles
cycloplegia (loss of focus/lens thickness): inhibits Ach action of M3 receptors in the ciliary muscles

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14
Q

Antimuscarinic drug use for incontinence

A

bladder relaxation: inhibits M3 receptors (mediate contraction of the bladder) and M2 receptors (which inhibit relaxation)

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15
Q

Antimuscarinic drug use for irritable bowel syndrome

A

induces GI tract intestinal paralysis and reduces secretions

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16
Q

Mebeverine

A

antimuscarinic drug used for IBS

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17
Q

Antimuscarinic drug use in COPD

A

reduces secretions, causes bronchial dilation in combination with a beta-adrenergic agonist

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18
Q

Antimuscarinic drug use pre-operative (anti-secretory)

A

used with inhalant anesthetics to reduce accumulations of secretions (salivary, mucous membranes of respiratory tract)

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19
Q

Long lasting tertiary amines

A

atropine and scopolamine

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20
Q

Atropine and Scopolamine are used to treat

A

GI/urinary conditions, COPD, motion sickness, adjuct for Parkinson’s

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21
Q

Side effets of Scopolamine

A

drowsiness (low dose) or hallucinations (high doses)
confusion, dilated pupils, tachycardia
can cause amnesia

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22
Q

What happens when scopolamine treatment is stopped suddenly

A

rebound effects - causing an overstimulation of the vesitubular nuclei and the reticular formation of the vomiting center (nausea, headache, and blurred vision)

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23
Q

Scopolamine can be specifically used for

A

motion sickness and reducing nausea (scopolamine patch)

24
Q

How can the withdrawal symptoms of scopolamine be alleviated

A

using anti-histamines or leaving the scopolamine patch on for a longer time to “squeeze out” the last bit of scopolamine over a prolonged time

25
Q

Tropicamide is primarily used for

A

eye exams

26
Q

What does tropicamide cause

A

cycloplegia and mydriasis

27
Q

Why would you want to dilate the pupil when evaluating a patient with glaucoma?

A

a dilated pupil enables examination of the terminal ends of the optical nerve and the nerves at the terminus are thinner and the first to be damaged by glaucoma

28
Q

Types of urinary incontinence

A

Stress incontinence, urge incontinence, outflow incontinence, functional incontinence

29
Q

Stress incontinence

A

laxity of pelvic floor muscle, leaks with cough or laughing, history of vaginal childbirth

30
Q

Treat stress incontinence with

A

adrenergic agonists

31
Q

Urge incontinence

A

increased detrusor muscle activity (overactive bladder), nocturia, small volume, increased frequency

32
Q

Treat urge incontinence with

A

anti-cholinergics

33
Q

Outflow incontinence

A

urinary retention secondary to obstruction or bladder atony, nocturia, small volume, increased frequency

34
Q

Treat outflow incontinence with

A

cholinergics (atony) or alpha antagonists (obstruction)

35
Q

Functional incontinence

A

due to large volume intake

36
Q

How can gestational diabetes cause incontinence

A

gestational diabetes -> increased baby weight -> damage to bladder sphincter

37
Q

How can congestive heart failure cause incontinence

A

CHF -> retain water -> create too much urine at night -> nocturia

38
Q

How are muscarinic antagonists used to treat urinary incontinence

A

by relaxing the obtrusor muscle in the bladder and increasing maximal bladder volume

39
Q

What kind of muscarinic receptors does the bladder contain?

A

both M2 and M3 receptors

40
Q

Prolonged use of muscarinic antagonists for urinary incontinency may lead to

A

acute urinary retention

41
Q

M3 selective muscarinic antagonists used for urinary incontinence

A

Darifenacin and Solifenacin

42
Q

M2/M3 selective muscarinic antagonist used for urinary incontinence

A

Tolterodine

43
Q

M1/M3 selective muscarinic antagonist used for urinary incontinence

A

Oxybutynin (dry mouth is a common side effect)

44
Q

Probanthine

A

used to treat gastric disorders (GI spasms, peptic ulcers), peripherally restricted

45
Q

Antispasmotics are used for?

A

irritable bowel syndrome

46
Q

Name 3 antispasmotics

A

Atropine, Dicyclomine, Hyoscyamine

47
Q

When should you avoid using antispasmotics?

A

avoid in glaucoma patients and avoid long term/continuous use

48
Q

How do M3 antagonists work in COPD?

A

M3 receptors mediate constriction of bronchial smooth muscle so M3 antagonists will block Ach-mediated constriction and open the airways

49
Q

muscarinic antagonists used for COPD

A

“-tropium”

Ipratropium, Tiotropium

50
Q

Ipratropium

A

short acting, rescue inhaler for COPD

51
Q

Tiotropium

A

long acting, daily inhaler for COPD

52
Q

Muscarinic antagonists for the management of COPD and asthma are more effect when?

A

when co-administered with a beta2 blocker

53
Q

Drug classes known to contain drugs with anti-cholinergic activity

A

anti-histamines, anti-psychotics, TCA’s and anti-arrythmics

54
Q

Tricyclic anti-depressant choice for the elderly

A

Nortryptaline because it only has mild-moderate anti-cholinergic effects

55
Q

Common contraindications for anti-muscarinic drugs

A

open/narrow angle glaucoma, tachycardia, ileus (intestinal obstruction), urinary obstruction (BPH)

Pharmacology Test #3 (13 decks)

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