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Block 5 > Pharm - Lecture 9 - Cholinergic - muscarinic agonists/antagonists + acetylchoinsterase inhib. > Flashcards

Pharm - Lecture 9 - Cholinergic - muscarinic agonists/antagonists + acetylchoinsterase inhib. Flashcards

1
Q

Which drugs are Muscarinic Receptor agonists?

A

Bethanechol

Pilocarpine

Acetylcholine (not bolded)

Muscarine (not bolded)

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2
Q

Which drugs are Choline esters? (2)

A

Acetylcholine (not bolded)

Bethanechol

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3
Q

What are the uses of Bethanechol?

Route of administration?

A

Used for urinary retention in the absence of obstruction
(post-op urinary retention, diabetic neuropthy, bladder disorders)

Route of administration: Oral or subcutanious

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4
Q

What drugs are naturally occuring alkaloids? (2)

A

Muscarine (not bolded)

Pilocarpine

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5
Q

How is Pilocarpine used?

A

1) orally to treat xerostamia (dry mouth)
2) Opthalmically: miotic agent - to treat wide angle glaucoma and emergency treatment of narrow angle glaucoma

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6
Q

How are Muscarinic receptor agonists adminstered?

Why?

A

Orally or subcutaniously: can’t administer by IV because it would cause hypotension

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7
Q

What does SLUDGE stand for?

A

Salivation

Lacrimation

Urination

Defecation

Gastrointestinal upset

Emesis

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8
Q

What are the side effects of muscarinic receptor agonists?

A

SLUDGE (salivation, lacrimatnio, urination, defecation, gastrointestinal upset, emesis (vomiting)

also: hypotension, bradycardia, difficulty with visual accomodation (blurred vision)

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9
Q

What drug blocks the toxicity of muscarinic receptor agonists?

A

atropine

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10
Q

What patients should muscarinic receptor agonists be used with caution? (3)

A

Asthma and COPD

Urinary or GI obstruction

Cardiovascular disease (bradycardia, hypotension, hyperthyroidism)

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11
Q

Why should you be careful about using muscarinic receptor agonists on patients with cardiovascular diseases?

A

may precipitate atrial fibrillation

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12
Q

Which drugs are acetylcholinesterase inhibitors? (5)

A

anticholinesterase agents:

Edrophonium

Physostigmine

Neostigmine

Sarin (nerve gas)

Malathion (insecticide)

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13
Q

How does Edrophonium bind? What is it’s onset and duration of action?

Can it penetrate CNS?

A

Truly reversible competitive enzyme inhibitor: non-covalent binding

Rapid onset and short duration of action (minutes)

Can’t penetrate CNS

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14
Q

What are the uses of Edrophonium? (3)

A

1) diagnosis of myasthenia gravis
2) distinguish cholinergic crisis from myasthenic crisis
3) reversal of paralysis by competitive neuromusclar blocking drugs

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15
Q

How is Physostigmine used?

A

1) wide angle glaucoma
2) toxicity by antimuscarinic drug poisoning

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16
Q

How does Physostigmine treat antimuscarinic drug poisoning?

A

Because Physostigmine is lipophilic, it can travel into the brain directly to treat this toxicity

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17
Q

How is Neostigmine used?

A

1) treatment of myasthenia gravis (oral)
2) prevention and treatment of post-operative atony of gut and bladder (oral)
3) reversal of paralysis by competitive neuromuscular blocking drugs (i.v.)

Has no CNS effects

18
Q

Why is malathion a relativly safe insecticide?

A

Because it is rapidly detoxified in higher organisms

19
Q

What is the cause of the side effects of acetylcholinesterase inhibitors?

A

results from activation of muscarinic and nicotinic receptors in both the periphery and CNS

20
Q

What are the side effects of REVERSIBLE acetylcholinesterase inhibitors? (4)

A

SLUDGE

hypotension, bradycardia, difficulty with visual accommodation

21
Q

What are the side effects of IRREVERSIBLE acetylcholinesterase inhibitors?

A

Same as reversible inhibitors and addisionally:

Medullary respiratory center depression

Muscle paralysis due to depolorazing neuromuscular junction blockade

Death due to respiratory failure

22
Q

What are antidotes for acetylcholinesterase inhibitor toxicity? (2)

A

1) atropine (muscarinic receptor antagonist)
2) pralidoxime (reactivates acetylcholinesterase - must treat within 2-3 hours)

23
Q

What are the effects of Muscarinic receptor antagonists? (5)

A

1) relax iris sphincter and cilary muscles (mydriasis and paralysis of accommodation)
2) relax non-vascular smooth muscle (airways, GI tract, urinary bladder)
3) inhibit exocrine gland secretion (sweat, salivary, lacrimal, intestinal, mucosal glands)
4) increase Heart Rate
5) CNS effects: low dose produces sedation

high dose produces: excitement, delirium, agitation, toxic psychosis

24
Q

What drugs are muscarinic receptor antagonists? (7)

2 alkaloids

1 semi-synthetic alkaloid

4 synthetics

A

Atropine (alkaloid)

Scopolamine (alkaloid)

Ipratropium (semi-synthetic alkaloid)

Tropicamide (synthetic)

Oxybutynin (synthetic)

Darifenacin (synthetic)

Glycopyrrolate (synthetic)

25
Q

What are the cardiac uses of Atropine? (2)

A

Used to treat bradycardia:

1) MI
2) syncope associated with hyperactive carotid sinus reflex

26
Q

What are the opthalmic uses of Atropine?

A

mydriasis (dialation and cylcoplegia (paralysis of accoomadation)

27
Q

What is the duration of action of Atropine? (opthalmically)

A

7-10 days opthalmically

28
Q

How is Atropine used in anesthesia?

A

block responses to vagal reflexes induced by surgery of visceral organs

29
Q

What types of toxicities is Atropine used for?

A

Anticholinesterase or muscarinic toxicity

30
Q

How is Scopolamine used?

A

Used as a transdermal patch to teat motion sickness and vestibular disease

(greater CNS penetration and more prominent CNS effects)

31
Q

How is Ipratropium used?

Via inhalation?

via nasal spray?

Does it penetrate CNS?

A

Inhaled: Treatement of COPD - reduces bronical secretions and constriction

Nasal spray: treatment of rhinorrhae associated with common cold

doesn’t penetrate CNS

32
Q

How is Tropicamide used?

What is the onset and duration of action?

A

Opthalmic solution to produce mydriasis and cycloplegia

Onset of action: fast (20-40 minutes)

duration: short (4-6 hours)

33
Q

How is Oxybutynin used?

A

Overactive bladder and incontinence

34
Q

What types of side effects is Oxybutynin known for?

A

high incidence of anti-muscarinic side effects:

Mostly zerostomia but also blurred vision, constipation and drowsiness and confussion

35
Q

What receptor is Darifenacin specific for?

A

M3

36
Q

What is Glycopyrrolate used for?

A

used to block parasympathomimetic effects during reversal of neuromusclar blockade with anticholinesterase agents

37
Q

What are the side effects of Muscaranic antagonists? (5)

A

1) hot as a hare (no sweating)
2) dry as a bone (dry mouth, dry hot skin, no sweating)
3) red as a beat (excessive heat and no sweating)
4) blind as a bat (mydriasis, cycloplegia, blurred vision)
5) drowsiness (CNS action)

38
Q

When at a toxic dose, what side effect is added for muscuranic antagonists?

A

“mad as a hatter”

ataxia, restlessness, excitement, hallucinations, delirium, coma

39
Q

What is physostigmine used for?

A

Muscaranic antagonist toxicity

40
Q

What patients should you be careful with when giving muscuranic antagonists? (3)

A

1) Glaucomoa - could increase intraocular pressure
2) prostatic hypertrophy - increase difficulty voiding
3) tachycardia (ex. angina pectoris)

41
Q

What is the mechanism of substrate inhibitors of acetylcholinesterase compared to non-substrate inhibitors?

A

Substrate inhibitors: bind as a substrate for acetylcholinesterase and is metabolized way slower than acetylcholine

Non-substrate inhibitor: blocks site of action for acetylcholinesterase

Block 5 (23 decks)

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