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Neuro > FINISHED Cholinergic drugs > Flashcards

FINISHED Cholinergic drugs Flashcards

1
Q

Why does acetylcholine have virtually no therapeutic applications?

A

Actions are diffuse, hydrolysis is rapid

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2
Q

What are cholinomimetics?

A

Cholinergic agonists - acetylcholine derivatives that are more selective and have prolonged actions

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3
Q

Bethanechol, methacholine, and pilocarpine belong to which class of cholinergic drugs?

A

Muscarinic agonists

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4
Q

What are the three primary therapeutic uses of bethanechol?

A

Post operative abdominal distension, gastric atony, non-obstructive urinary retention

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5
Q

What is the primary therapeutic use of methacholine?

A

Diagnosis of asthma

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6
Q

What are the two primary therapeutic uses of pilocarpine?

A

Xerostomia, initial treatment of glaucoma

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7
Q

Why are bethanechol and pilocarpine therapeutically useful muscarinic agonists?

A

Resistant to cholinesterases, limited or no nicotinic activity

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8
Q

How does bethanechol treat post-operative abdominal distension and gastric atony?

A

Increases contractile force in smooth muscle throughout the GI tract

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9
Q

How does bethanechol treat non-obstructive urinary retention?

A

Increases smooth muscle contractions of the bladder body

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10
Q

How does pilocarpine treat xerostomia?

A

Facilitates lacrimal and salivary secretions

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11
Q

How does pilocarpine treat acute glaucoma attacks?

A

Contraction of ciliary muscle relaxes of suspensory ligaments of the lens, allowing it to become more convex and shift forward slightly; decrease intraocular pressure by widening the Canal of Schlemm, which increases drainage of aqueous humor

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12
Q

What are the two contraindications to therapeutic uses of muscarinic agonists?

A

Asthma (increase bronchial secretion and stimulate bronchial smooth muscle constriction) and peptic ulcer disease (increase acid secretion)

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13
Q

What are some potential side effects of muscarinic agonists?

A

Sweating, abdominal cramps, difficulty in visual accommodation, excess salivation

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14
Q

Atropine, scopolamine, ipratropium, prienzipine, and oxybutynin are examples of which class of cholinergic drugs?

A

Muscarinic receptor antagonists

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15
Q

How does atropine affect heart rate at high and low doses?

A

Slight cardiac slowing at low doses, increased heart rate at higher doses

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16
Q

What is atropine’s action on pupillary response?

A

Blocks muscarinic acetylcholine receptors on the sphincter pupillae causing relaxation and pupillary dilation

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17
Q

What is the major difference between pirenzipine and other muscarinic receptor antagonists?

A

Pirenzipine has some selectivity for M1, while all other muscarinic receptor antagonists have no selectivity for specific receptor subtypes

18
Q

What was pirenzipine historically used to treat?

A

Peptic ulcers

19
Q

What are the therapeutic uses of atropine?

A

Irritable bowel syndrome (reduce GI tract tone and motility), inducing mydriasis for ophthalmologic exams, treatment of organophosphate poisoning

20
Q

What are the therapeutic uses of oxybutynin?

A

Mild cystitis (in conjunction with antibiotics), bladder spasm

21
Q

What are the therapeutic uses of ipratropium?

A

COPD and asthma (minimal inhibition of mucociliary clearance, inefficient absorption from GI tract minimizes systemic effects

22
Q

What are the therapeutic uses of scopolamine?

A

Motion sickness prophylaxis

23
Q

What effects does nicotine have on the autonomic nervous system at high and low doses?

A

Stimulation of ANS at low doses, initial stimulation followed by longer-lasting transmission blockade at higher doses

24
Q

What effects does nicotine have on skeletal neuromuscular junctions at high and low doses?

A

Stimulation of NMJ at low doses, initial stimulation followed by rapidly developing paralysis at higher doses

25
Q

What effects does nicotine have on the central nervous system at high and low doses?

A

Stimulant at low doses, stimulation followed by central paralysis and chemoreceptor trigger zone stimulation (vomiting) at higher doses

26
Q

Hexamethonium belongs to what class of cholinergic drugs?

A

Ganglionic blocker (nicotinic antagonist)

27
Q

What are the current and historical therapeutic uses of hexamethonium?

A

Historically used for hypertension, some current specific uses in CV regulation

28
Q

Tubocuararine belongs to what class of cholinergic drugs?

A

Neuromuscular non-depolarizing blocker (nicotinic antagonist)

29
Q

Succinylcholine belongs to what class of cholinergic drugs?

A

Depolarizing blockers

30
Q

What are the current and historical therapeutic uses of tubocuararine?

A

Historically used as an adjunct to anesthetics (now replaced with safer alternatives)

Just for funsies: also treatment of tetanus, and black widow spider bites.

31
Q

What is the mechanism of action of succinylcholine?

A

Open nicotinic channels, which causes initial repetitive excitation, then depolarization while nicotinic channels remain open causing flaccid paralysis

32
Q

Don’t forget about botox

A

cool

33
Q

What are the three classes of acetylcholinesterase inhibitors?

A

Quaternary alcohols, carbamate esters, organophosphates

34
Q

What is the approximate duration of action for the different classes of acetylcholinesterase inhibitors?

A

Quaternary alcohols - a few minutes
Carbamate esters - a few hours
Organophosphates - a reeeeeaaaalllllyyyy long time

35
Q

What is aging in relation to organophosphates?

A

An acetylcholinesterase enzyme that has been irreversibly inactivated by the long-term binding of an organophosphate

36
Q

Edrophonium belongs to which class of cholinergic drugs?

A

Quaternary alcohols (acetylcholinesterase inhibitors)

37
Q

Neostigmine, physostigmine, and pyridostigmine belong to which class of cholinergic drugs?

A

Carbamate esters (acetylcholinesterase inhibitors)

38
Q

Malathion, parathion, and echothiophate belong to which class of cholinergic drugs?

A

Organophosphates (acetylcholinesterase inhibotors)

39
Q

What are the five common therapeutic uses of anticholinesterase agents?

A

Myasthenia gravis, urinary bladder atony, paralytic ileus, glaucoma, muscarinic antagonist poisoning

40
Q

Which cholinergic drug is used to differentiate between myasthenic weakness and cholinergic crisis?

A

Edrophonium (cholinergic crisis if causes further weakness, myasthenic weakness if improves muscle strength)

41
Q

What are the three possible causes of acetylcholinesterase inhibitor toxicity?

A

Side effects of cholinesterase inhibitor therapy, accidental exposure (insecticides, etc.), biological warfare

42
Q

What are the four methods of prophylaxis/treatment of acetylcholinesterase inhibitor toxicity?

A

Pyridostigmine (binds reversibly to AChE and protects from irreversible binding agents), high doses of atropine, pralidoxime (must be applied before aging), artificial respiration and anticonvulsants

Neuro (11 decks)

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