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Pharm Exam 3 > Muscarinic Antagonists > Flashcards

Muscarinic Antagonists Flashcards

1
Q

Anticholinergic drugs do what?

A

Antagonists that prevent acetylcholine signaling

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2
Q

Antimuscarinic acts where?

A

Post ganglionic neuroeffector junction to block parasympathetic autonomic discharge

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3
Q

Neuromuscular blocker acts where?

A

Neuromuscular junction to block acetylcholine signaling

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4
Q

Ganglionic blockers act where?

A

They act as antagonists at both parasympathetic and sympathetic autonomic ganglia

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5
Q

How do Muscarinic Receptors M1, M3, and M5 signal?

A

Via increase in intracellular Ca2+and PKC activity

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6
Q

Where is M1 located? (3)

A

CNS
Sympathetic postganglionic cells
Presynaptic sites

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7
Q

M3 locations? (3)

A

Smooth muscle
Lungs
Eyes effector cell membranes

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8
Q

M2 and M4 are activated how?

A

Signal via cAMP decreased and reduced cAMP-dependent PK activity

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9
Q

Where is M2 located? (3)

A

Myocardium
Smooth muscle
Presynaptic sites

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10
Q

Where is M4? (1)

A

CNS

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11
Q

Atropa Belladonna (deadly nightshade) gave us what?

A

Atropine

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12
Q

Belladonna causes what effect in the eyes?

A

Increase in pupil size

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13
Q

Antimuscarinic drug use in ocular exams? (2)

A

Mydyriasis (pupil dilation)

Cycloplegia (Loss of focus/regulation of lens thickness)

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14
Q

Which M receptor is being targeted in antimuscarinic drugs?

A

M3

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15
Q

How does Muscarinic antagonists affect incontinence?

A

Triggers bladder relaxation via M3 receptor which mediates contraction of bladder and M2 which inhibits relaxation

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16
Q

Drug used in irritable bowel syndrome to induce GI paralysis and reduce secretions?

A

Mebeverine

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17
Q

What other uses are listed for antimuscarinic drugs? (4)

A

COPD
Pre-Op Anti-Secretory
Motion Sickness
Parkinson’s disease

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18
Q

For COPD use what is the effect of muscarinic antagonists? (2)

A

Reduce secretions

Cause Bronchial dilation

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19
Q

In COPD use what would I combine antimuscarinic drugs with?

A

B-adrenergic agonist

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20
Q

What is the purpose of anti-muscarinic in treating Parkinson’s?

A

Adjunct to L-DOPA

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21
Q

What is the mechanism of Antimuscarinic drugs?

A

Competitive and reversible inhibition of muscarinic receptor activation by preventing the binding of Ach.

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22
Q

Two classes of antimuscarinic?

A 
Tertiary Amines (Atropine)
Quaternary Amines/Ammonium (Glycopyrrolate)
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23
Q

Main use for Tertiary amines?

A

Ocular and CNS applications

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24
Q

Main use of Quaternary Amines/Ammonium?

A

GI tract and peripheral application

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25
Q

What specific tertiary amine do you use for COPD?

A

Ipratropium

26
Q

Characteristics of tertiary amines? (2)

A

Can penetrate CNS

Non-selective antagonists

27
Q

Which tertiary amine is better for CNS penetration?

A

Scopolamine is better than Atropine

28
Q

What happens in low vs high doses of Scopolamine?

A

Low doses you get drowsiness

High doses you get hallucination

29
Q

Why is Scopolamine not for children?

A

Toxicity

30
Q

How do you give Scopolamine locally?

A

Patch form

31
Q

Why is Scopolamine useful in surgery and childbirth?

A

Can cause amnesia

32
Q

When Scopolamine treatment is stopped what effects can be seen?

A

Rebound effects which cause overstimulation of vestibular and reticular formation of the vomiting center

33
Q

Short acting tertiary amine used in optical applications?

A

Tropicamide (0.25 days)

34
Q

What does Tropicamide cause? (2)

A

Cycloplegia (loss of accommodation)

Mydriasis

35
Q

Types of Urinary Incontinence? (4)

A

Stress (Leak)
Urge (Nocturia)
Outflow (Retention secondary to obstruction)
Functional (Large volume intake)

36
Q

What do you treat stress incontinence with?

A

Adrenergic agonist

37
Q

What do you treat urge incontinence with?

A

Anti-cholinergics

38
Q

What do you treat outflow incontinence with?

A

Cholinergics for atony

alpha antagonists for obstruction

39
Q

Diabetic neuropathy can cause what two dysfunctions?

A

1) Diabetic bladder dysfunction

2) Diabetic cystopathy

40
Q

What is diabetic bladder dysfunction?

A

Overactive bladder leading to urge incontinence

41
Q

What is diabetic cystopathy?

A

Decreased bladder sensation, increased capacity leading to outflow incontinence

42
Q

How does pregnancy affect the bladder?

A

Increased weight from baby damages bladder sphincter

43
Q

Effect of Congestive heart failure on bladder?

A

Retention of water causes more water in body causes too much urine causes nocturia

44
Q

What do muscarinic antagonists do for urinary incontinence? (2)

A

Suppress involuntary bladder contraction

Increase maximal urine volume that causes involuntary bladder contraction

45
Q

Which muscle in the bladder does M2 handle?

A

Detrusor

46
Q

Benefit of M3 selective Darifenacin or Solifenacin in urinary incontinence?

A

Longer acting than oxybutinin

47
Q

Benefit of M2/M3 selective Tolterodine?

A

Fewer side effects than oxybutinin

48
Q

Downside of Tolterodine?

A

Too much/too long use can lead to acute urinary retention

49
Q

Quaternary amine probanthine used for what?

A

Gastric disorders such as GI spasms/peptic ulcers

50
Q

What restricts Probanthine from crossing the gut?

A

Charged Nitrogen

51
Q

What type of restricted is Probanthine?

A

Peripherally

52
Q

Main antispasmodics for irritable bowel syndrome? (3)

A

Atropine
Dicyclomine
Hyoscyamine

53
Q

Who do you avoid giving antispasmodics to?

A

Glaucoma patients

54
Q

Which muscarinic receptors mediate constriction of bronchial smooth muscle?

A

M3

So M3 antagonist will block Ach mediated constriction and open the airways

55
Q

M3 antagonists enhance what?

A

B-adrenergic agonists in COPD

56
Q

What is known as the “rescue inhaler”?

A

Ipratropium: short acting

57
Q

What is known as the daily inhaler?

A

Tiotropium: long acting

58
Q

What do tertiary amines for Parkinson’s act on?

A

CNS M1 receptors

59
Q

What is the preferred Tri-cyclic Anti-depressant in elderly to moderate anticholinergic effects ?

A

Nortriptyline (Aventyl, Pamelor)

60
Q

Important drug in treating Parkinson’s?

A

Trihexyphenldyl

61
Q

When do you not give anti muscarinic drugs? (4)

A

Glaucoma
Tachycardia
Intestinal obstruction
Urinary obstruction

Pharm Exam 3 (10 decks)

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