Cholinergic Drugs Flashcards Preview

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Flashcards in Cholinergic Drugs Deck (43)
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1
Q

4 choline esters

A

Acetylcholine
Methacholine
Carbachol
Bethanechol

2
Q

Choline ester properties

A

Charged
Poorly distributed to CNS
Metabolized by acetylcholinesterase (to some degree)

3
Q

Muscarinic or nicotinic:

Acetylcholine

A

Both

4
Q

Muscarinic or nicotinic:

Methacholine

A

Muscarinic

5
Q

Muscarinic or nicotinic:

Carbachol

A

Both, more nicotinic

6
Q

Muscarinic or nicotinic:

Bethanechol

What about it?

A

Muscarinic

Specifically affects urinary/GU system

7
Q

4 alkaloids

A

Nicotine
Muscarine
Pilocarpine
Lobeline

8
Q

Are alkaloids charged or uncharged?

A

Uncharged (absorbed into CNS) EXCEPT muscarine

9
Q

Muscarinic or nicotinic:

Pilocarpine?

A

Muscarinic

10
Q

Muscarinic or nicotinic:

Lobeline

A

Nicotinic

11
Q

Danger of muscarine

A

Can cross BBB and be highly toxic (poison mushrooms)

12
Q

MoA of indirect cholinergic agonists

A

AChE inhibitors

13
Q

3 groups of AChE inhibitors

A
  1. Alcohols - reversible
  2. Carbamic acid esters - reversible but longer
  3. Organophosphates - irreversible (covalent)
14
Q

Miosis during surgery

A

Acetylcholine, Carbachol, Pilocarpine

15
Q

Urinary retention treatment

A

Bethanechol

16
Q

Glaucoma treatment

Does what?

A

Carbachol, Pilocarpine

Contraction of ciliary body, fascilitating outflow of aqueous humor

17
Q

Xerostomia treatment (dry mouth)

A

Cevimeline, Pilocarpine

18
Q

Varenicline

A

Smoking cessation
Partial agonist for neuronal nicotinic receptors
Reduced but not eliminated dopamine release
Reduce cravings and withdrawal

19
Q

Side effects of Varenicline

A

Neuropsychiatric symptoms - suicide

20
Q

GI uses for cholinergic agonists

A

Post-operative ileus
Congenital megacolon
Esophageal reflux

21
Q

SLUDGE

A

Muscarinic stimulant toxicity

Salivation, Lacrimation, Urination, Dehydration, GI issues (diarrhea), Emesis (vomiting)

22
Q

Use for anti-nicotinic antagonists

A

Skeletal muscle relaxants

23
Q

Uses for anti-muscarinic antagonists

A

Block parasympathetic effects of CNS, heart, nerves, SM, glands, endothelium

24
Q

Prototypical muscarinic antagonist

A

Atropine

25
Q

General function of anticholinergics

A

Increase sympathetics

26
Q

Parkinson’s disease (CNS disorders)

A

Tertiary amines - benztropine, trihexyphenidyl, procyclidine

Antimuscarinics - reduce tremors due to loss of dopaminergic neurons in substantia nigra

27
Q

Motion sickness

A

Scopolamine

28
Q

Anesthesia

A

Atropine - block vagal responses for visceral surgery

W/ neostigmine to block parasympathetic effects

29
Q

Must dilate eye for surgery. What to use?

A

Alpha-1 agonist rather than anticholinergic - shorter-acting with less side effects

30
Q

Asthma, COPD

A
Ipratropium, Tiotropium
Muscarinic antagonists (inhalation)
31
Q

Lomotil

A

Atropine + opiate (diphenoxylate)

Antidiarrheal, discourages abuse of opiate

32
Q

Urinary urgency treatment

A

Darifenacin, solifenacin, tolterodine

Selective M3 antagonists w/o major side effects

33
Q

Treatment for cholinergic poisoning (insecticides, wild mushrooms, nerve gasses)

A

Atropine + pralidoxime (cholinesterase regenerator)

34
Q

Contraindications for anticholinergics

A

Glaucoma
Prostatic hyperplasia
Acid-peptic disease

35
Q

Contraindications for muscarinic agonists

A

Asthma
Hyperthyroid
Coronary insufficiency
Acid-peptic disease

36
Q

Nicotinic poisoning causes

A

Tobacco

Insecticides

37
Q

Acute nicotinic toxicity

A

Convulsions, skeletal muscle depolarization blockade (paralysis), respiratory paralysis, HTN, cardiac arrhythmias

38
Q

Treating nicotinic toxicity

A

Atropine + Diazepam (anti-convulsant)

39
Q

Charged AChE inhibitors

A

Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium

40
Q

Uncharged AChE inhibitors

A

Physostigmine, donepezil, galantamine, rivastigmine, tacrine

41
Q

3 classes of cholinesterase inhibitors (+ examples)

A
  1. Alcohols (edrophonium)
  2. Carbamic acid esters (neostigmine, pysostigmine, pyridostigmine)
  3. Organophosphates (Echothiophate, parathion, malathion, sarin, soman, tabun)
42
Q

Oxybutynin

A

M3 selective antagonist (w/ bad side effects)

Better to use Darifenacin, Solifenacin, Tolterodine

43
Q

Fixing depolarized skeletal muscle block

A

Neostigmine (AChE inhibitor) + atropine/glycopyrrolate