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Pharm Exam 3 > 4 - Muscarinic Antagonists > Flashcards

4 - Muscarinic Antagonists Flashcards

1
Q

Antimuscarinic agents act where

A

postganglionic neuroeffector junction

block Psy discharge

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2
Q

Nicotinic receptor blocker types (and site of action)

A
  1. NM blocker = act at NMJ to block Ach signaling
  2. Ganglionic blocker = act as antagonists at Psy and Sy ganglia
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3
Q

Muscaric receptors are all

A

GPCR

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4
Q

Two types of Ach regulated GPCR and their general mechanisms

A

M 1,3,5 = Signal via intracellular Ca++ increase and Protein Kinase C activity

M 2+4 = SIgnal via cAMP decrease and reducced cAMP-dependent protein kinase activity

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5
Q

Type and location of M1

A

(Gaq)

CNS

Sy Post ganglionic cells and presynaptic sites

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6
Q

Type and location of M3

A

(Gaq)

  • Sm. muscle
  • Lungs
  • eyes
  • effector cell membranes
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7
Q

Type and location of M2

A

(Gai)

Myocardium

Sm muscle

Presynaptic sites (K+ channel linked = slow HR)

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8
Q

Type and location of M4

A

(Gai)

CNS

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9
Q

Ocular exams: Conditions and causes

A

Mydyriasis (dil) = inhibit Ach action on M3 receptor in constrictor muscle

Cycloplegia (loss of focus/reg of lens thickness) = Inhibit Ach on M3 receptor on ciliary muscle

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10
Q

Primary clinical uses for antimuscarinics

A

Ocular exams (mydyriasis, Cycloplegia)

Incontinence (bladder relaxation)

IBS (induce GI paralysis)

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11
Q

Antimuscarinic effect on bladder

A

Relaxation = via M3 (bladder contraction mediator) and M2 (indirectly…inhibits relaxation)

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12
Q

GI effects of antimuscarinics (for IBS)

A

Induce GIT paralysis

Reduce secretion

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13
Q

Antimuscarinic agent for IBS

A

Mebeverine

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14
Q

Other uses for antimuscarinics

A

COPD (bronchodilate and reduce secretions)

Pre-op anti secretory

Motion sickeness

Parkinsons

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15
Q

MOA of antimuscarinic

A

competitive and reversible inhibition of muscarinic receptor activation

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16
Q

Two classes of antimuscarinics

A

Tertiary amines (atropine, used in ocullar and CNS)

Quaternary amines (Glyopyrrolate, used in GI and peripheral applications)

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17
Q

Long lasting tertiary amines

A

Atropine

Scopolamine

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18
Q

Atropine and Scopolamine are…

A

Non-selective (hit M1-M5)

Tertiary compounds that penetrate the CNS

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19
Q

Long lasting Tertiary amines (Atropine / Scopolamine) are used for

A

GI

Urinary

COPD (Ipratropium)

Motion sickness

Adjunct to LDOPA therapy

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20
Q

Naturally occuring tertiary amine

A

Scopolamine

(CNS penetration is better than atropine)

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21
Q

Scopolamine Sides

A

Drowsiness (low dose)

Hallucination (high dose)

Confusion

Dilated pupils

Tachycardia

22
Q

Scopolamine used for

A

Motion sickness/nausea

23
Q

Scopolamine may cause

A

amnesia (surgical use)

24
Q

Scopolamine dose

A

1mg over 3 days transdermal

25
Q

Scopolamine not recommended for…

A

kids or elderly (toxicity)

26
Q

effect of Scopolamine discontinuation

A

Withdrawal because receptor sites are sensitized

Cholinergic NT’s accumulate

–> Overstimulation of vestibular nuclei and reticular formation of the emetic center

27
Q

Tx for scopolamine withdrawal

A
  • Meclizine (anti-histamine)
  • Diphenhydramine + 8-chlorotheophylline (=dramamine)
28
Q

Short acting tertiary amine

A

Tropicamide

Causes cycloplegia and mydriasis

(duration = .25 days)

29
Q

Stress incontinence

A

Laxity of pelvic floor muscle

Treat with adrenergics

30
Q

Urge incontinence

A

Increased detrusor activity (overactive bladder)

Nocturia

Treat with Anticholinergics

31
Q

Outflow incontinence

A

Urinary retention secondary to obstruction or bladder atony

(nocturia, increased frequency)

Treat atony with cholinergics

Treat obstruction with alpha antagonists

32
Q

Functional incontinence

A

Due to large volume intake

33
Q

Mechanisms for incontinence from Diabetes

A

Overweight

Diabetic neuropathy (either overactive/urge incontinence or Cystopathy where sensatation is decreased)

Gestational diabetes = sphincter damage

CHF = water retention

34
Q

Leftover urine can cause ___

A

UTI

Increase urge and frequency

35
Q

Bladder receptors include _______, which are targets for _____

A

M3/M2

Tolteridine

36
Q

Receptor on urethra

A

alpha1

37
Q

Receptor on Ext. Urethral sphincter

A

Nicotinic

38
Q

effect of muscarinic antagonists on urinary incontinence

A

Suppress involuntary bladder contraction

Increase threshold/maximal urine volume that causes involuntary bladder contraction

39
Q

M3 selective agents

A

Darifenacin, Solifenacin

Longer acting than oxybutinin

40
Q

M2/3 selective agents

A

Tolterodine

Fewer sides than oxybutinin

41
Q

M1/3 selective

A

Oxybutinin

ER or patch, xerostomia common side effect

42
Q

Probanthine used for __________

Pharmacodynamics?

A

GI spasms and peptic ulcers

Charged N makes crossing gut difficult

Peripherally restricted

43
Q

Anti spasmotics =

Avoid in whom?

A

Atropine, Dicyclomine, Hyoscyamine

Avoid in glaucoma patients, avoid long term use

(causes constipation and difficulty urinating)

44
Q

(COPD)

M3 receptors mediate ________

(effect of blocking?)

A

constriction of bronchial smooth muscle

(therefore M3 antagonist will block Ach-mediated constriction and open airways)

45
Q

M3 antagonist is less effective _________

A

as a monotherapy

46
Q

“-tropium”

Short and long acting examples

A

Ipra = short acting (rescue inhaler)

Tio = long acting (daily inhaler)

47
Q

T1/2 of LAMA

A

5-6 days

48
Q

Tertiary amines use for Parkinsons–

MOA

Use

A

Action through CNS M1 receptor

Adjunct with LDOPA

Treats extrapyramidal sides of antipsychotics

49
Q

Drug catergories with anticholinergic activity

A

anti-psychotics

tricyclics

antiarrythmics

anti-histamines

50
Q

Common Contraindications for antimuscarinics

A
  • Worsen open/narrow angle glaucoma
  • Tachycardia
  • Ileus (intestinal obstruction) - further reduce GI fxn
  • Urinary obstruction (BPH)

Pharm Exam 3 (11 decks)

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