Cholinergic Drugs

Question 1

4 choline esters

Answer 1

Acetylcholine
Methacholine
Carbachol
Bethanechol

Question 2

Choline ester properties

Answer 2

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

Question 3

Muscarinic or nicotinic:

Acetylcholine

Answer 3

Both

Question 4

Muscarinic or nicotinic:

Methacholine

Answer 4

Muscarinic

Question 5

Muscarinic or nicotinic:

Carbachol

Answer 5

Both, more nicotinic

Question 6

Muscarinic or nicotinic:

Bethanechol

What about it?

Answer 6

Muscarinic

Specifically affects urinary/GU system

Question 7

4 alkaloids

Answer 7

Nicotine
Muscarine
Pilocarpine
Lobeline

Question 8

Are alkaloids charged or uncharged?

Answer 8

Uncharged (absorbed into CNS) EXCEPT muscarine

Question 9

Muscarinic or nicotinic:

Pilocarpine?

Answer 9

Muscarinic

Question 10

Muscarinic or nicotinic:

Lobeline

Answer 10

Nicotinic

Question 11

Danger of muscarine

Answer 11

Can cross BBB and be highly toxic (poison mushrooms)

Question 12

MoA of indirect cholinergic agonists

Answer 12

AChE inhibitors

Question 13

3 groups of AChE inhibitors

Answer 13

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

Question 14

Miosis during surgery

Answer 14

Acetylcholine, Carbachol, Pilocarpine

Question 15

Urinary retention treatment

Answer 15

Bethanechol

Question 16

Glaucoma treatment

Does what?

Answer 16

Carbachol, Pilocarpine

Contraction of ciliary body, fascilitating outflow of aqueous humor

Question 17

Xerostomia treatment (dry mouth)

Answer 17

Cevimeline, Pilocarpine

Question 18

Varenicline

Answer 18

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

Question 19

Side effects of Varenicline

Answer 19

Neuropsychiatric symptoms - suicide

Question 20

GI uses for cholinergic agonists

Answer 20

Post-operative ileus
Congenital megacolon
Esophageal reflux

Question 21

SLUDGE

Answer 21

Muscarinic stimulant toxicity

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

Question 22

Use for anti-nicotinic antagonists

Answer 22

Skeletal muscle relaxants

Question 23

Uses for anti-muscarinic antagonists

Answer 23

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

Question 24

Prototypical muscarinic antagonist

Answer 24

Atropine

Question 25

General function of anticholinergics

Answer 25

Increase sympathetics

Question 26

Parkinson's disease (CNS disorders)

Answer 26

Tertiary amines - benztropine, trihexyphenidyl, procyclidine Antimuscarinics - reduce tremors due to loss of dopaminergic neurons in substantia nigra

Question 27

Motion sickness

Answer 27

Scopolamine

Question 28

Anesthesia

Answer 28

Atropine - block vagal responses for visceral surgery | W/ neostigmine to block parasympathetic effects

Question 29

Must dilate eye for surgery. What to use?

Answer 29

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

Question 30

Asthma, COPD

Answer 30

``` Ipratropium, Tiotropium Muscarinic antagonists (inhalation) ```

Question 31

Lomotil

Answer 31

Atropine + opiate (diphenoxylate) | Antidiarrheal, discourages abuse of opiate

Question 32

Urinary urgency treatment

Answer 32

Darifenacin, solifenacin, tolterodine | Selective M3 antagonists w/o major side effects

Question 33

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

Answer 33

Atropine + pralidoxime (cholinesterase regenerator)

Question 34

Contraindications for anticholinergics

Answer 34

Glaucoma Prostatic hyperplasia Acid-peptic disease

Question 35

Contraindications for muscarinic agonists

Answer 35

Asthma Hyperthyroid Coronary insufficiency Acid-peptic disease

Question 36

Nicotinic poisoning causes

Answer 36

Tobacco | Insecticides

Question 37

Acute nicotinic toxicity

Answer 37

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

Question 38

Treating nicotinic toxicity

Answer 38

Atropine + Diazepam (anti-convulsant)

Question 39

Charged AChE inhibitors

Answer 39

Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium

Question 40

Uncharged AChE inhibitors

Answer 40

Physostigmine, donepezil, galantamine, rivastigmine, tacrine

Question 41

3 classes of cholinesterase inhibitors (+ examples)

Answer 41

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

Question 42

Oxybutynin

Answer 42

M3 selective antagonist (w/ bad side effects) | Better to use Darifenacin, Solifenacin, Tolterodine

Question 43

Fixing depolarized skeletal muscle block

Answer 43

Neostigmine (AChE inhibitor) + atropine/glycopyrrolate