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Pharm - Autonomics > Muscarinic Antagonists > Flashcards

Muscarinic Antagonists Flashcards

1
Q

Muscarinic Receptors: Antimuscarinic receptor

A

acts at the postganglionic neuroeffector junction to block parasympathetic autonomic discharge

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2
Q

Nicotinic Receptors: Neuromuscular Block

A

act at the neuromuscular junction to block AcH signaling

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3
Q

Nicotinic Receptors: Ganglionic Blockers

A

act as antagonists at both parasympathetic and sympathetic autonomic ganglia

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4
Q

M1, M3, M5 action

A

signal via intracellular Ca2+ increase and PKC activity

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5
Q

M1(Galphaq) site

A

CNS, sympathetic postganglionic and presynaptic sites

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6
Q

M3(Galpha) site:

A

smooth muscle, lungs, eyes effector cell membranes

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7
Q

M2, M4 action

A

signal via cAMP decrease and reduced cAMP-dependent PK activity

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8
Q

M2(Galphai) site:

A

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

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9
Q

M4(Galphai) site:

A

located in the CNS

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10
Q

Atropine description

A
  • muscarinic antagonist isolated from aorta belladonna

- increased pupil size

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11
Q

Ocular exams and antimuscarinic drug

A

Mydyriasis: pupil dilation; inhibit Ach action on M3 receptor in pupillary constrictor muscle.

Cycloplegia: loss of focus/regulation of lens thickness; inhibit Ach action on M3 receptor in ciliary muscle

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12
Q

Incontinence and antimuscarinic drug

A
  • Bladder relaxation via M3 receptor which mediates contraction of the bladder
  • M2 receptor(indirectly) inhibits relaxation
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13
Q

IBS and antimuscarinic drug

A
  • induce GI tract intestinal paralysis(antispasmodic agents)
  • reduce secretions
  • Mebeverine
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14
Q

COPD and antimuscarinic drugs

A
  • reduce secretions, cause bronchial dilation

- in combination with a Beta-adrenergic agonist

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15
Q

Preoperative antisecretory and antimuscarinic drugs

A
  • used with inhalant anesthetics to reduce accumulations of secretions(salivary, mucous membranes of rest. tract)
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16
Q

Two other uses for antimuscarinic drugs

A
  • motion sickness

- parkinson disease; as an adjunct to L-DOPA

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17
Q

Mechanisms of antimuscarinic drugs

A
  • competitive and reversible inhibition of muscarinic receptor activation by preventing binding of Ach
  • two general classes based on their structure
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18
Q

Tertiary amines of antimuscarinic drugs

A
  • mainly used in ocular and CNS applications
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19
Q

Quaternary amines/ammonium of antimuscarinic drugs

A
  • mainly used in GI tract and peripheral applications
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20
Q

Long lasting tertiary amines

A
  • atropine and scopolamine
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21
Q

Description of long lasting tertiary amines

A
  • nonselective antagonists

- tertiary compounds can penetrate CNS

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22
Q

Scopolamine description

A
  • naturally occurring
  • CNS penetration better than atropine
  • drowsiness(low doses) or hallucinations(high doses)
  • side effects include confusion, dilated pupils, tachycardia
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23
Q

Scopolamine uses

A
  • motion sickness

- reduce nausea

24
Q

Side effects of scopolamine

A
  • amnesia
25
Q

Administration of Scopolamine

A
  • patch

- 1.5mg patch will deliver 1mg over 3days transdermally

26
Q

Scopolamine not recommended for

A
  • for children or the elderly due to toxicity
27
Q

Withdrawal from scopolamine

A
  • receptor sites are sensitized over time
  • cholinergic neurotransmitters are accumulated
  • rebound effects when scopolamine is stopped, causing overstimulation of vestibular nuclei and reticular formation
28
Q

Symptoms of withdrawal from scopolamine

A

nausea
headache
blurred vision

29
Q

Treatment options for withdrawal of scopolamine

A
  • bonine(mezcline) is antihistamine

- dramamine

30
Q

Shortacting tertiary amines

A

Tropicamide(0.25day)

Homatropine(1-3day)

31
Q

Effect of tropicamide

A

used in optical applications
causes cycloplegia and mydriasis
shorter duration than atropine

32
Q

Cycloplegia description

A

paralysis of the ciliary muscle of the eye, resulting in loss of accommodation

33
Q

Muscarinic antagonists commonly used for

A

dilation of pupil for eye exams

34
Q

Types of urinary incontinence

A

stress
urge
outflow
functional

35
Q

Stress incontinence description

A

laxity of pelvic floor muscle
leak with cough or laughing
history of vaginal childbirth
treat with adrenergic agonist

36
Q

Urge incontinence description

A

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

37
Q

Outflow incontinence description

A

urinary retention secondary to obstruction or bladder anatomy
nocturia, small volume, increased frequency
treat with cholinergics(atony), alpha antagonists(obs.)

38
Q

Functional incontinence description

A

due to large volume intake

39
Q

Diabetes effect on incontinence

A
  • overweight and pressure on bladder
  • diabetic neuropathy
    1. diabetic bladder dysfunction: overactive bladder: urge
    1. diabetic cystopathy: decreased bladder sensation, increased capacity: outflow
  • gestational diabetes; increased baby weight; damage to bladder sphincter
  • CHF; retain water; create too much urine at night; nocturia
  • constipation common in diabetes
  • leftover urine can cause UTI; increase urge and frequency
40
Q

Muscarinic antagonist for urinary incontinence; tertiary amines

A

suppress involuntary bladder contraction

increase maximal urine volume

41
Q

M3 selective for urinary incontinence

A

Darifenacin, Solifenacin

longer acting than oxybutinin

42
Q

M2/M3 selective for urinary incontinence

A

Tolterodine

fewer side effects than oxybutinin

43
Q

M1/M3 selective for urinary incontinence

A

Oxybutinin

ER or patch with dry mouth side effect

44
Q

Quarternary amines used for GI disorders

A

Probanthine
used to treat gastric disorders(GI spasm, peptic ulcers)
charged N makes crossing gut difficult
peripherally restricted

45
Q

Antispasmotics for IBS

A

Atropine - Saltropine
Dicyclomine - Bentyl
Hyoscyamine - Levsin

46
Q

Contraindications for antispasmotics

A

glaucoma

long term/continuous use

47
Q

M3 receptors and bronchial smooth muscle action

A

M3 receptors mediate constriction of bronchial smooth muscle.

48
Q

M3 antigonist function on bronchial smooth muscle

A

block Ach-mediated constriction and open the airways

49
Q

M3 antagonist and COPD

A
  • used as inhalant drug for COPD, asthma

- less effective as a mono therapy, but enhances the therapeutic effect of beta-adrenergic agonists in COPD

50
Q

Ipratropium description

A
  • short acting, rescue inhaler
51
Q

Tiotropium description

A
  • long acting, daily inhaler
52
Q

Tertiary amines used for Parkinson’s disease

A
  • action through CNS M1 receptor
  • used as an adjunct therapy with LDOPA in PD patients
  • improve balance between dopaminergic and cholinergic neurotransmission
  • disruption of Ache => increase Ach, decrease DA
  • treat extrapyramidal side effects of antipsychotics
53
Q

Antipsychotics drugs with anticholinergic activity

A 
chlorpromazine - thorazine
clozapine - Clozaril
mesoridazine - serentil
olanzapine - zyprexa
promazine - sparine
quetiapine - seroquel
thioridazine - mellaril
54
Q

Tricyclic antidepressants with anticholinergic activity

A 
amitriptyline - elavil
desipramine - norpramin
doxepin - sinequan
imipramine - tofranil
nortriptyline - aventyl, pamelor
55
Q

Antiarrythmics with anticholinergic activity

A

discopyramide - norpace
procainamide - pronestyl
quinidine - quinaglute, quinidex

56
Q

Antihistamine with anticholinergic activity

A

azatadine - optimine
chlorpheniramine - chlortrimeton
clemastine - tavist
diphenydramine - tylenol, sominex, benadryl

57
Q

Contraindications for antimuscarinic drugs

A
  • open/narrow angle glaucoma
  • tachycardia; increase HR
  • ileus obstruction
  • urinary obstruction

Pharm - Autonomics (3 decks)

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