Week 8 - Chapter 14 (Muscarinic Agonists and Antagonists) Flashcards

1
Q

Anhidrosis

A

a deficiency or absence of sweat

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2
Q

Anticholinergic drugs

A

Subtypes: muscarinic, nicotinicN, and nicotinicM

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3
Q

Belladonna Alkaloids

A

examples: atropine, hyoscyamine, and scopolamine

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4
Q

Cholinergic durgs

A

agents that influence the activity of cholinergic receptors. Most of these drugs act directly at cholinergic receptors, where they either mimic or block the actions of acetylcholine.

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5
Q

Muscarinic Agonist

A

bind to muscarinic receptors and thereby cause receptor activation. Since nearly all muscarinic receptors are associated with the parasympathetic nervous system, responses to muscarinic agonists closely resemble those produced by stimulation of parasympathetic nerves. Accordingly, muscarinic agonists are also known as parasympathomimetic agents. (Bethanechol)

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6
Q

Muscarinic Antagonist

A

competitively block the actions of acetylcholine at muscarinic receptors. Because the majority of muscarinic receptors are located on structures innervated by parasympathetic nerves, the muscarinic antagonists are also known as parasympatholytic drugs. Additional names for these agents are antimuscarinic drugs, muscarinic blockers, and anticholinergic drugs. (Atropine)

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7
Q

Parasympatholytic Drugs

A

muscarinic antagonists

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8
Q

Parasympathomimetic Agents

A

muscarinic agonists

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9
Q

Xerostomia

A

dry mouth

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10
Q

OAB

A

Overactive bladder akaurgency incontinence, detrusor instability, and sometimes “can’t-hold-it-anymore” incontinence. four major symptoms: urinary urgency, nocturia, Urinary frequency, urge incontinence.

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11
Q

M1 Receptor Location

A

Salivary glands and CNS (brain)

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12
Q

M1 Receptor Activation Response

A

salivation and enhanced cognition

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13
Q

M1 Receptor Blockade Response

A

dry mouth, Confusion, hallucinations

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14
Q

M2 Receptor Location

A

Heart

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15
Q

M2 Receptor Activation Response

A

Bradycardia

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16
Q

M2 Receptor Blockade Response

A

Tachycardia

17
Q

M3 Receptor Location

A
  • Salivary glands,
  • Bladder: detrusor,
  • GI smooth muscle
  • Eyes: Iris sphincter,
  • Eyes: Ciliary muscle,
  • Eyes: Lacrimal gland.
18
Q

M3 Receptor Activation Response

A
  • Salivation,
  • Bladder Contraction of detrusor (increased pressure),
  • GI: Increased smooth muscle tone and motility,
  • Eye: Puple constriction, Ciliarry muscle contraction (Vision - accommodation), Tearing
19
Q

M3 Receptor Blockade Response

A
  • Dry mouth,
  • Bladder Relaxation (decreased pressure),
  • Decreased GI tone and motility (constipation),
  • Eye: Relaxation of Iris sphincter (mydriasis), Relaxation of ciliary muscle (blurred vision), Dry eyes
20
Q

Atropine Category

A

muscarinic antagonist

21
Q

Atropine Use

A

Pre-anesthesia medication (help stimulate baroreceptors during surgery),

  • Disorders of the eye
  • Bradycardia
  • Diverticulitis (Intestinal hypertonicity and hypermotility)
  • Muscarinic agonist poisoning
  • Peptic ulcer disease
  • Asthma
  • Biliary colic
22
Q

Atropine mechanism of action

A

Atropine produces its effects through competitive blockade at muscarinic receptors. Like all other receptor antagonists, atropine has no direct effects of its own.

23
Q

Atropine adverse effects

A
  • Xerostomia (dry mouth)
  • Blurred vision and photophobia
  • Elevation of intraocular pressure
  • Urinary retention
  • Constipation
  • Anhidrosis
  • Tachycardia
  • Asthma (it can cause thickening of secretions)
24
Q

Darifenacin Category

A

anticholinergic agents

25
Q

Darifenacin Use

A

treatment of OAB while having no effect on M1 receptors in the brain or M2 receptors in the heart

26
Q

Darifenacin Mechanism of action

A

M3 selectivity anticholinergic agent.

27
Q

Darifenacin adverse effects

A
  • Dry mouth (most common)
  • Constipation is also common.
  • Others include dyspepsia (indigestion), gastritis, and headache.
28
Q

Bethanechol Category

A

muscarinic agonists

29
Q

Bethanechol Use

A

Urinary retention and investigational GI uses

30
Q

Bethanechol Mechanism of action

A

The drug binds reversibly to muscarinic cholinergic receptors to cause activation. At therapeutic doses, bethanechol acts selectively at muscarinic receptors, having little or no effect on nicotinic receptors, either in ganglia or in skeletal muscle.

31
Q

Bethanechol adverse effects

A
  • Cardiovascular system: Hypotension
  • Gastrointestinal system: Increased tone and motility
  • Exacerbation of asthma
  • Dysrhythmias in patients with hyperthyroidism (MEMORIZE) - Because patients with hyperthyroidism are sensitive to sympathetic activation of beta1 receptors (baroreceptor reflex)
32
Q

Muscarinic Receptors Location

A

-Heart: Bradycardia
-Exocrine glands: Increased sweating, salivation, bronchial secretions, and secretion of gastric acid
-Smooth muscles
>Contraction in lung (constriction)
>Gastrointestinal tract (increased tone/motility)
>Bladder (contraction of detrusor & relaxation of trigon and sphincter)
>Vascular (relaxation, vasodilation, and hypotension)
>Eye (pupillary constriction and ciliary contraction)

33
Q

NicotinicN Receptors Location

A

All ganglia of the autonomic nervous system

34
Q

NicotinicM Receptors Location

A

Neuromuscular junctions (NMJs)

35
Q

Muscarinic Receptors Effects

A

Many, including:
↓ Heart rate
↑ Gland secretion
Smooth muscle contraction

36
Q

NicotinicN Receptors Effects

A

Promotes ganglionic transmission

37
Q

NicotinicN Receptors Effects

A

Skeletal muscle contraction

38
Q

Toxicology of Muscarinic Antagonists

Symptoms include:

A
  • Dry mouth
  • Blurred vision
  • Photophobia
  • Hyperthermia
  • Central nervous system effects
  • Hot, dry, and flushed skin