Chapter 2: Cholinergic Pharmacology

Question 1

MOA of hemocholinum.

Answer 1

blocks uptake of choline

Question 2

MOA of botulinum toxin.

Answer 2

cleaves SNARE proteins involved in exocytosis of ACh

Question 3

Xerostomia definition and why is this caused? (what is defective)

Answer 3

dry mouth
salivary glands don’t produce enough saliva

Question 4

M1 and M3 correspond with what receptor pathway?

(what coupled pathway or second messenger pathway)

Answer 4

Gq coupled

increase phosphliase C > increase IP3, DAG, Ca2+

Question 5

M2 goes through what coupled receptor pathway?

(what second messenger pathway in other words)

Answer 5

Gi coupled

dec. adenylyl cyclase > dec cAMP

Question 6

Nn and Nm go through what G coupled receptor pathway?

Answer 6

trick question

no 2nd messengers

activation through opening of Na/K channels

Question 7

Stem to remember muscarinic agonist

Answer 7

“chol”

Question 8

Clinical use of bethanechol.

Answer 8

Rx: ileus (postop); urinary retention

Question 9

Use of methacholine.

Answer 9

Dx: bronchial hyperactivity (challenge test)

Question 10

Use of pilocarpine, cevimeline.

Answer 10

Rx: xerostomia, glaucoma (pilocarpine)

Question 11

Stem to help you remember indirect acting cholinomimetics.

Answer 11

stigmine

Question 12

Clinical use for edrophonium

Answer 12

Dx myasthenia gravis

Question 13

Benefits to edrophonium typically being used as a diagnostic tool?

Answer 13

short acting

Question 14

Clinical use of physostigmine?

Answer 14

Rx: glaucoma; antidote in atropine overdose

Question 15

Why can physostigmine be used for atropine overdose? (characteristics that make it suitable)

Answer 15

tertiary amine
very lipid soluble
(readily enters CNS)

Question 16

Neostigmine and pyridostigmine can be used for what?

Answer 16

ileus, urinary retention, myasthenia gravis, reversal of non depolarizing NM blockers

Question 17

Characteristics of neostigmine and pyridostigmine that do not make it suitable for atropine overdose?

Answer 17

Quaternary amine so cannot enter CNS

Question 18

Donepezil clinical use.

Answer 18

Rx - Alzheimers

Question 19

Rivastigmine clinical use.

Answer 19

RX - Alzheimers

Question 20

Organophosphate use. (Name some)

Answer 20

used as insecticides (malathion, parathion) and sarin ( nerve gas)

Question 21

Some properties of donepezil and rivastigmine that make them ideal for treating Alzeihmers?

Answer 21

lipid- solubility

Question 22

Way to remember difference between physostigmine and pyridostigmine.

Answer 22

“pyro burns down”

pyro below CNS and physo above so good for atropine overdose

Question 23

DUMBBEELSS acronym use?

Answer 23

clues to tell if someone has AChE inhibitor poisoning

Question 24

Use the proper acronym to be able to tell if someone has AChE inhibitor poisoning.

Answer 24

DUMBBEELSS

diarrhea
urination
miosis
bradycardia
bronchoconstriction
emesis
excitation (CNS/muscle)
lacrimation
salivation
sweating

Question 25

What is the most deadly S/E of AChE inhibitor poisoning?

Answer 25

paralysis of diaphragm

Question 26

Use of pralidoxime.

Answer 26

Reversal of irreversible AChE inhibitors

Question 27

What is the prototype of the muscarinic receptor antagonist class?

Answer 27

atropine

Question 28

What is the characteristic of atropine that makes it a good antidote for AChE inhibitors?

Answer 28

tertiary amine; readily enters CNS

Question 29

What plant atropine derived from?

Answer 29

atropa belladonna; Jimsonweed

Question 30

Muscarinic antagonist effects on eyes?

Answer 30

mydriasis and cycloplegia

Question 31

Pharamacologic effects of muscarinic receptor anatagonists? (name 2 or 3)

Answer 31

* decrease secretions (salivary, bronchiolar, sweat) * mydriasis and cyclopegia * hyperthermia (with resulting vasodilation) * tachycardia * sedation * urinary retention and constipation * Behavioral: excitation and hallucinations

Question 32

Name some classes of drugs with antimuscarinic properties.

Answer 32

antihistamine (particularly the 1st generation) tricyclic antidepressants antipsychotics quinidine amantadine meperidine

Question 33

Antidote for antimuscarinic drugs?

Answer 33

physostigmine

Question 34

Clinical use of atropine.

Answer 34

antispasmodic, antisecretory, management of AChE inhibitor OD, antidiarrheal, ophthalmology (but long action)

Question 35

Clinical use of tropicamide.

Answer 35

ophthalmology (topical)

Question 36

Clinical use of ipratropium, tiotropium. Also name some important properties to remember about these drugs. (Can they enter CNS) (How do they effect mucus viscosity)

Answer 36

asthma and COPD (inhalation) - no CNS entry, no change in mucous viscosity

Question 37

Stem to remember M blockers?

Answer 37

"trop"

Question 38

Scopolamine clinical use. Also S/E.

Answer 38

motion sickness causes sedation and short-term memory block

Question 39

Benztropine and trihexyphenidyl clinical use.

Answer 39

lipid-soluble (CNS entry) used in Parkinson-ism and in acute extrapyramidal symptoms induced by antipsychotics

Question 40

Clinical use of oxybutinin.

Answer 40

used in overactive bladder (urge incontinence

Question 41

What makes tropicamide a more useful drug in eye exams than atropine.

Answer 41

causes less sustained dilation of pupils because of its short half-life

Question 42

What are ganglion blockers also typically named?

Answer 42

nicotinic receptor antagonist

Question 43

What are 2 ganglion blockers not used today but that this chapter covered?

Answer 43

hexamethonium. and mecamylamine

Question 44

Ganglion blockers have what effect that can be useful?

Answer 44

they block reflexes

Question 45

Which receptors are stimulated for direct action on HR?

Answer 45

M2 and B1

Question 46

What receptors are stimulated for indirect effect on HR causing reflex Brady or tachy?

Answer 46

a1 (vasoconstriction) and B2 (vasodilation)