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Pharmacology -- Test #3 > Muscarinic Antagonists > Flashcards

Muscarinic Antagonists Flashcards

1
Q

Effects of M1, M3, and M5 activation?

A

Signal via intracellular Ca2+ increase and PKC activity

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2
Q

Effects of M2, M4 activation?

A

Signal via cAMP, decrease cAMP-dependent PK activity

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3
Q

Important sites of M1?

A

Present in CNS, sympathetic postganglionic, and presynaptic sites

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4
Q

Important sites of M3?

A

Smooth Muscle, Lungs, Eyes, Effector Cell Membranes

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5
Q

Important sites of M2?

A

Myocardium, Smooth Muscle, Presynaptic sites

slows the heart rate

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6
Q

Important sites of M4?

A

CNS

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7
Q

Primary clinical uses for anti-muscarinic drugs?

A

Ocular Exams
Incontinence
Irritable Bowel Syndrome

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8
Q

Use of anti-muscarinic drugs in ocular exams?

A

Inhibit ACh activation of M3 of pupillary constrictor–> Mydyriasis
Inhibit ACh on M3 in cilliary muscle –> Cycloplegia

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9
Q

What is cycloplegia

A

Loss of accomodation/regulation of lens thickness

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10
Q

Effects of anti-muscarinic drugs on incontinence?

A

Trigger bladder relaxation via blockage of the M3 receptor (which normally contracts the bladder), and M2 (indirectly), which would inhibit relaxation

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11
Q

use of anti-muscarinic drugs in treatment of IBS?

A

Induce GI tract intestinal paralysis

Reduce secretions

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12
Q

Name the anti-muscarinic drug used to treat IBS?

A

Mebeverine

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13
Q

Less popular uses for anti-muscarinic drugs?

A

COPD (can decrease secretions, dilate bronchioles)
Pre-Operative anti-secretor
Motion Sickness
Parkinson’s (as an adjunct to L-dopa)

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14
Q

What are the two types of muscarinic antagonists?

A

Those with a tertiary amine and those with a quaternary amine

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15
Q

Downside of muscarinic antagonists with a quaternary amine?

A

Solubility issues – only for GI or peripheral applications

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16
Q

Within the antagonist structure you can recognize which structure…

A

acetylcholine

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17
Q

How are tertiary amines muscarinic antagonists?

A

Ocular and CNS applications

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18
Q

Two common non-selective muscarinic antagonists?

A

Atropine and Scopolamine

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19
Q

Use of Atropine and Scopolamine?

A

Long duration of action

useful in treatment of GI/urinary conditions, COPD, and motion sickness

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20
Q

Atropine and Scopolamine. Who penetrates the CNS more?

A

Scopolamine

Thats why is can cause CNS side effects (ex. drowsiness)

21
Q

Uses of Scopolamine specifically?

A

Surgical amnesia

Motion sickness patch

22
Q

Problems with Scopolamine use?

A

Prolonged use can cause withdrawl effects upon termination of treatment

23
Q

How to treat Scopolamine withdrawl?

A

Anti-histamines

Leave the patch on to squeeze out meds over an extended period

24
Q

Indication for Tropicamide?

A

Cause cycloplegia and mydriasis with shorter duration than atropine. Allows for examination of the terminal ends of the optic nerve.

25
Q

What are the four types of urinary incontinence?

A

Stress Incontinence
Urge Incontinence
Outflow Incontinence
Functional Incontinence

26
Q

Important Information for Stress Incontinence?

A

Laxity of pelvic floor muscle
Associated with leak with cough/laugh, vaginal childbirth
Treat with adrenergic agonists

27
Q

Important information for Urge Incontinence?

A

Increased detrusor muscle activity (Overactive bladder)
Nocturia, small volume, increased frequency
Treat with anti cholinergics

28
Q

Important information about outflow incontinence?

A

Urinary retention secondary to obstruction or bladder atony
Nocturia, small volume, increased frequency
Treat with cholinergics (atony), alpha antagonists (obstruction)

29
Q

Cause of functional incontinence

A

Large volume intake

30
Q

Diabetic cystopathy can lead to what kind of incontinence?

A

Outflow incontinence

31
Q

Effect of gestational diabetes on bladder fxn?

A

damage to bladder sphincter

32
Q

leftover urine is a problem because it can lead to…

A

Increased urge and frequency

33
Q

Effect of muscarinic antagonists on urinary incontinence?

A

Suppress bladder contraction

Increase maximal urine volume that causes contraction

34
Q

Examples of M3 selective muscarinic antagonists in treating incontinence? Whats so cool about them?

A

Darifenacin and Solifenacin

Longer acting than oxybutiin

35
Q

Examples of M2/M3 selective muscarinic antagonists used in urinary incontinence? Whats so cool about them?

A

Tolterodine

Fewer Side Effects

36
Q

Example of an M1/M3 selective muscarinic antagonists used for urinary incontinence?

A

Oxybutynin

37
Q

What is Probanthine? When do you use it?

A

A quaternary aminemuscarinic antagonist used in treatment of GI spasms, peptic ulcers.

38
Q

Three examples of muscarinic antagonists used as anti-spasmodics.

A

Atropine
Dicyclomine
Hyoscyamine

39
Q

Who shouldn’t be taking muscarinic antagonist anti-spasmodic drugs?

A

Glaucoma patients

Long term use

40
Q

What drugs are used in muscarinic antagonist treatment of COPD?

A

IPRAtropium (short acting rescue inhaler)
TIOtropium (long acting daily inhaler)
LAMA (Long acting Musc. antagonists).

41
Q

muscarinic antagonist treatments of COPD are typically paired with…

A

beta-adrenergic agonists

42
Q

muscarinic antagonists used in treatment of Parkinsons?

A

Benztropine

Trihexyphenidyl

43
Q

What receptor do Benztropine and Trihexyphenidyl act on?

A

M1 Receptor

44
Q

Benztropine and Trihexyphenidyl are adjunct therapies paired with ______

A

L-dopa

45
Q

What do Benztropine and Trihexyphenidyl do to help Parkinson’s?

A

Improve the balance between dopaminergic and cholinergic neurotransmission

46
Q

List drug classes known to have anti-cholinergic activity

A

Anti-histamines
Anti-psychotics
Tricyclic Antidepressants
Anti-arrythmetics

47
Q

Nortriptyline is preferred the preferred TCA for the elderly. Why?

A

Mild/Moderate anti-cholinergic effects

48
Q

Four common contraindications for antimuscarinic drugs?

A

Open/Narrow Angle Glaucoma
Tachycardia
Ileus (Intestinal Obstruction)
Urinary Obstruction (causes benign prostatic hyperplasia)

Pharmacology -- Test #3 (13 decks)

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