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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

25
Administration of Scopolamine
- patch | - 1.5mg patch will deliver 1mg over 3days transdermally
26
Scopolamine not recommended for
- for children or the elderly due to toxicity
27
Withdrawal from scopolamine
- 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
Symptoms of withdrawal from scopolamine
nausea headache blurred vision
29
Treatment options for withdrawal of scopolamine
- bonine(mezcline) is antihistamine | - dramamine
30
Shortacting tertiary amines
Tropicamide(0.25day) | Homatropine(1-3day)
31
Effect of tropicamide
used in optical applications causes cycloplegia and mydriasis shorter duration than atropine
32
Cycloplegia description
paralysis of the ciliary muscle of the eye, resulting in loss of accommodation
33
Muscarinic antagonists commonly used for
dilation of pupil for eye exams
34
Types of urinary incontinence
stress urge outflow functional
35
Stress incontinence description
laxity of pelvic floor muscle leak with cough or laughing history of vaginal childbirth treat with adrenergic agonist
36
Urge incontinence description
increased detrusor muscle activity(overactive bladder) nocturia, small volume, increased frequency treat with anticholinergics
37
Outflow incontinence description
urinary retention secondary to obstruction or bladder anatomy nocturia, small volume, increased frequency treat with cholinergics(atony), alpha antagonists(obs.)
38
Functional incontinence description
due to large volume intake
39
Diabetes effect on incontinence
- overweight and pressure on bladder - diabetic neuropathy 1. diabetic bladder dysfunction: overactive bladder: urge 2. 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
Muscarinic antagonist for urinary incontinence; tertiary amines
suppress involuntary bladder contraction | increase maximal urine volume
41
M3 selective for urinary incontinence
Darifenacin, Solifenacin | longer acting than oxybutinin
42
M2/M3 selective for urinary incontinence
Tolterodine | fewer side effects than oxybutinin
43
M1/M3 selective for urinary incontinence
Oxybutinin | ER or patch with dry mouth side effect
44
Quarternary amines used for GI disorders
Probanthine used to treat gastric disorders(GI spasm, peptic ulcers) charged N makes crossing gut difficult peripherally restricted
45
Antispasmotics for IBS
Atropine - Saltropine Dicyclomine - Bentyl Hyoscyamine - Levsin
46
Contraindications for antispasmotics
glaucoma | long term/continuous use
47
M3 receptors and bronchial smooth muscle action
M3 receptors mediate constriction of bronchial smooth muscle.
48
M3 antigonist function on bronchial smooth muscle
block Ach-mediated constriction and open the airways
49
M3 antagonist and COPD
- 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
Ipratropium description
- short acting, rescue inhaler
51
Tiotropium description
- long acting, daily inhaler
52
Tertiary amines used for Parkinson's disease
- 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
Antipsychotics drugs with anticholinergic activity
``` chlorpromazine - thorazine clozapine - Clozaril mesoridazine - serentil olanzapine - zyprexa promazine - sparine quetiapine - seroquel thioridazine - mellaril ```
54
Tricyclic antidepressants with anticholinergic activity
``` amitriptyline - elavil desipramine - norpramin doxepin - sinequan imipramine - tofranil nortriptyline - aventyl, pamelor ```
55
Antiarrythmics with anticholinergic activity
discopyramide - norpace procainamide - pronestyl quinidine - quinaglute, quinidex
56
Antihistamine with anticholinergic activity
azatadine - optimine chlorpheniramine - chlortrimeton clemastine - tavist diphenydramine - tylenol, sominex, benadryl
57
Contraindications for antimuscarinic drugs
- open/narrow angle glaucoma - tachycardia; increase HR - ileus obstruction - urinary obstruction

Pharm - Autonomics (3 decks)

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