1. Cholinergics

Question 1

Cholinomimetics - Available Drugs

Answer 1

Cholinergic Agonists:

• Bethanchol
• Carbechol
• Pilocarpine
• Methacholine

Cholinesterase Inhibitors:

• Neostigmine
• Pyridostigmine
• Edrophonium
• Physostigmine
• Echothiophate
• Donepezil

Question 2

Cholinergic Agonists - Available Drugs

Answer 2

• Bethanchol
• Carbechol
• Pilocarpine
• Methacholine

Question 3

Bethanechol - MOA

Answer 3

Cholinergic agonist

• Activate Bowel and Bladder smooth muscle
• Resistant to AChE

“BETHANY, CALL (Bethanechol) me if you want to activate your Bowels and Bladder”

Question 4

Bethanechol - Clinical Use

Answer 4

Postoperative and neurogenic ileus and urinary retention.

Question 5

Carbachol - MOA

Answer 5

Cholinergic agonist
- Exact mimic of ACh

“CARBon copy of ACh”

Question 6

Carbachol - Clinical Use

Answer 6

Glaucoma, pupillary contraction, relief of intraocular pressure

Question 7

Pilocarpine - MOA

Answer 7

Cholinergic agonist

• Contracts ciliary muscle of eye - open angle
• Contracts pupillary sphincter - narrow angle
• Resistant to AChE

Question 8

Pilocarpine - Clinical Use

Answer 8

Potent stimulator of sweat, tears, and saliva

“You CRY, DROOL, and SWEAT on your PILOw”

Question 9

Methacholine - MOA

Answer 9

Cholinergic agonist

• Short acting
• Stimulates muscarinic receptors in the airway then inhaled.

Question 10

Methacholine - Clinical Use

Answer 10

Challenge test for diagnosis of asthma

Question 11

Cholinergic Agonists - Toxicities

Answer 11

Exacerbation of COPD, asthma, and peptic ulcers when given to susceptible patients.

Question 12

Cholinesterase Inhibitors - Available Drugs

Answer 12

• Neostigmine
• Pyridostigmine
• Edrophonium
• Physostigmine
• Echothiophate
• Donepezil

Question 13

Neostigmine - MOA

Answer 13

Cholinesterase Inhibitor

• Increase endogenous ACh
• No CNS penetration

“NEO (no) CNS penetration”

Question 14

Neostigmine - Clinical Use

Answer 14

• Postoperative and neurogenic ileus and urinary retention.
• Myasthenia Gravis
• Postoperative reversal of neuromuscular junction blockade

Question 15

Pyridostigmine - MOA

Answer 15

Cholinesterase inhibitor

• Increase endogenous ACh
• Increase strength
• No CNS penetration
• Long acting

Question 16

Pyridostigmine - Clinical Use

Answer 16

Myasthenia Gravis

“pyRIDostigmine gets RID of Myasthenia Gravis”

Question 17

Edrophonium - MOA

Answer 17

Cholinesterase inhibitor

- Increase endogenous ACh

Question 18

Edrophonium - Clinical Use

Answer 18

Extremely short acting

• Diagnosis of myasthenia Gravis
• Tenselon Test

Question 19

Physostigmine - MOA

Answer 19

Cholinesterase inhibitor

- Increase endogenous ACh

Question 20

Physostigmine - Clinical Use

Answer 20

Glaucoma
- Crosses BBB
Atropine overdose

“PHYsostigmine PHYxes atropine overdose”

Question 21

Echothiophate - MOA

Answer 21

Cholinesterase inhibitor

- Increase endogenous ACh

Question 22

Echothiophate - Clinical Use

Answer 22

Glaucoma

Question 23

Donepezil - MOA

Answer 23

Cholinesterase inhibitor

- Increase endogenous ACh

Question 24

Donepezil - Clinical Use

Answer 24

Alzheimer’s disease

Question 25

Cholinesterase Inhibitors - Toxicities

Answer 25

Exacerbation of COPD, asthma, and peptic ulcers in susceptible patients. Poisoning seen with irreversible AChE inhibitors --> Organophosphates - insecticides --> Often seen in farmers - Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation. "DUMBBELSS" - Antidote is Atropine (ACh antagonist) + Pralidoxime (regenerates AChE)

Question 26

Muscarinic Antagonists - Available Drugs

Answer 26

``` Atropine Homatropine Tropicamide Benztropine Scopolamine Ipratropium Oxybutynin Glycopyrrolate Methscopolamine Pirenzepine Propantheline ```

Question 27

Muscarinic Antagonists Used on the Eye

Answer 27

Atropine Homatropine Tropicamide

Question 28

Muscarinic Antagonists Used on the Eye - Clinical Use

Answer 28

Produce mydriasis and cycloplegia | Atropine, Homatropine, Tropicamide

Question 29

Muscarinic Antagonists Used on the Heart

Answer 29

Atropine

Question 30

Muscarinic Antagonists Used on the Heart - Clinical Use

Answer 30

Treat bradycardia --> Increase HR | Atropine

Question 31

Muscarinic Antagonists Used on the CNS

Answer 31

Benztropine | Scopolamine

Question 32

Muscarinic Antagonists Used on the CNS - Clinical Use

Answer 32

Benztropine - Parkinson's disease - "PARK my BENZ" Scopolamine - Motion sickness

Question 33

Muscarinic Antagonists Used on the Genitourinary System

Answer 33

Oxybutynin | Glycopyrrolate

Question 34

Muscarinic Antagonists Used on the Genitourinary System - Clinical Use

Answer 34

Reduce urgency in mild cystitis and reduce bladder spasms | Oxybutynin, Glycopyrrolate

Question 35

Muscarinic Antagonists Used on the Respiratory System

Answer 35

Ipratropium

Question 36

Muscarinic Antagonists Used on the Respiratory System - Clinical Use

Answer 36

- Asthma - COPD (IPRAtropium) "I PRAy I can breathe soon"

Question 37

Muscarinic Antagonists Used on the GI System

Answer 37

Methscopolamine Pirenzepine Propantheline

Question 38

Muscarinic Antagonists Used on the GI System - Clinical Use

Answer 38

Peptic ulcer treatment | Methscopolamine, Pirenzepine, Propantheline

Question 39

Atropine - MOA

Answer 39

Muscarinic antagonist

Question 40

Atropine - Clinical Use

Answer 40

Antidote for Organophosphate (irreversible AChE inhibitor)(DUMBBELSS) poisoning - Increase pupil dilation, cycloplegia - Increase HR

Question 41

Atropine - Toxicities

Answer 41

- Increase body temp. due to decreased sweating - Rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation "Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter" - Can cause acute angle closure glaucoma in elderly - Can cause urinary retention in men with prostatic hyperplasia - Can cause hyperthermia in infants