Muscarinic Agonists And Antagonists From Goodman & Gilmans Ch. 7 (Dr. William Messer's Class)

Front 1

Are muscarinic agonists/antagonists highly selective?

Back 1

No, they have very low selectivity

Front 2

What receptors are Pirenzepine selective for?

Back 2

M1 and M4

Front 3

What receptors are Otenzapad selective for?

Back 3

M2 and M4

Front 4

What receptors are Darifenacin selective for?

Back 4

M3

Front 5

What happened to Xanomeline when it moved from in vitro experiments to in vivo experiments?

Back 5

When it was in vitro, it was selective for M1 and M4 receptors, but that selectivity was lost in vivo, most likely due to metabolism.

Front 6

What are the four effects exerted by acetylcholine in the cardiovascular system?

Back 6

Vasodilation, decrease in cardiac rate, decrease in rate of conduction, and decrease in force of cardiac contractions.

Front 7

What type of effect is a decrease in cardiac rate?

Back 7

negative chronotropic

Front 8

What type of effect is a decrease in rate of conduction?

Back 8

Negative dromotropic

Front 9

What type of effect is a decrease in force of cardiac contractions?

Back 9

Negative inotropic effect

Front 10

What type of dose of acetylcholine produces a transient drop in blood pressure?

Back 10

intravenous

Front 11

Is an intravenous dose of acetylcholine enough to elicit bradycardia or block conduction?

Back 11

no, a larger dose is required.

Front 12

What types of cardiovascular beds does acetylcholine produce vasodilation in?

Back 12

all of them, but effects may be mediated by local production of nitric oxide.

Front 13

What is the pathway for production of NO from acetylcholine?

Back 13

Acetylcholine binds to M3 receptors on vascular endothelial cells, which activate the Gq-PLC-IP3 pathway, leading to Ca-calmodulin-dependent activation of endothelial NO synthase.

Front 14

How does acetylcholine slow the heart rate?

Back 14

It decreases the rate of spontaneous depolarizations from the SA node and increases repolarizing of the K current.

Front 15

How does acetylcholine decrease the strength of atrial contractions?

Back 15

it decreases cAMP and Ca channel activity

Front 16

What effect does acetylcholine have on gastrointestinal and urinary tracts?

Back 16

Vagal input to the GI tract increases tone, contractility and secretion, while parasympathetic activation causes detrusor muscle contraction, increased voiding pressure, and ureter peristalsis.

Front 17

What is more effective- acetylcholine, or muscarinic agonists?

Back 17

Muscarinic agonists -- acetylcholine has limited perfusion of visceral organs and is hydrolyzed rapidly.

Front 18

What are some muscarinic agonists that are related esters to acetylcholine?

Back 18

Methacoline, Carbamylcholine, and bethanechol

Front 19

What are some natural products that are muscarinic agonists?

Back 19

Muscarine, pilocarpine, and arecoline

Front 20

Compare Acetylcholine, methacholine, carbachol, and bethanechol.

Back 20

Acetylcholine and methacholine are acetyl esters, while carbachol and bethanechol are carbamyl esters. Acetycholine is unstable and nonselective, while methacholine is more stable than Ach and selective for muscarinic vs. nicotinic. Carbachol and bethanechol are both resistant to hydrolysis and selective for muscarinic receptors.

Front 21

Where was muscarine found and what type of receptors is it selective for?

Back 21

It was isolated from the muschroom Amanita muscaria and is selective for muscarinic receptors

Front 22

Where was pilocarpine found and what effects does it have?

Back 22

It is derived from the south American shrub of the genus pilocarpus and chewing the plant leaves results in salivation, pupil constriction, salivation, and diaphoresis (sweat)

Front 23

Where was arecoline found, what receptors does it activate, and what is a characteristic of the compound in the body?

Back 23

it is isolated from betel nuts (Areca catechu) and it activates both muscarinic and nicotinic receptors, and it has a short half-life in vivo

Front 24

What are some synthetic compounds and some of their qualities?

Back 24

McN-A-343 is a M1 agonist, and activates sympathetic ganglia selectively, while Oxotremorine is an agonist that activates M2 and M4 receptors

Front 25

List all known Muscarinic Agonists

Back 25

Acetylcholine, Nicotine, Xanomeline, Methacholine, carbamycholine, bethanechol, muscarine, pilocarpine, arecholine, McN-A-343, Oxotremorine, Cevimeline

Front 26

List all known Muscarinic Antagonists

Back 26

Atropine, Scopalomine, hyoscaymine, homatropine, methylatropine, methscopalomine, Ipratropium, tiotropium, tolterodine, trospium, Oxybutynin, Darifenicen, Dolifenicen, Favoxate, Cyclopentolate, Tropicamide, Benztropine, Procyclidine, Biperidin, Trihexyphenidyl

Front 27

What do muscarninic agonists do in the cardiovascular system?

Back 27

Decrease heart rate, force of contraction, and rate of conduction, and they vasodialate.

Front 28

What do muscarninic agonists do in the GI tract and genito-urinary tract?

Back 28

They tend to encourage pressure, motility and voiding of these tracts.

Front 29

What do muscarninic agonists do as far as secretions go?

Back 29

They increase almost all types of secretions, including sweating.

Front 30

What do muscarninic agonists do in the lungs?

Back 30

They bronchio-constrict.

Front 31

What do muscarninic agonists do in the CNS?

Back 31

THey may be used to treat Alzheimer's or schizophrenia.

Front 32

What do muscarninic agonists do in the eye?

Back 32

They reduce intraocular pressure.

Front 33

What are the natural muscarinic antagonists?

Back 33

Atropine, Scopolamine, Hyoscyamine

Front 34

What is the semi-synthetic muscarinic antagonist?

Back 34

Homatropine

Front 35

What are the quaternarily derived muscarinic antagonists?

Back 35

Methylatropine, Methscopalomine, Homatropine, Ipratropium, Tiotropium

Front 36

Do muscarinic antagonists bind to muscarinic receptors in the same (or different) fassion as acetylcholine?

Back 36

Same (similar)

Front 37

What do muscarinic antagonists do in the cardiovascular system?

Back 37

They increase heart rate, force of contraction, and rate of contraction, and they vasoconstrict.

Front 38

What do muscarinic antagonists do in the GI and G-U tracts?

Back 38

They basically inhibit secretions, motility and the pressure that is normally there to void these tracts.

Front 39

What do muscarinic antagonists do as far as secretions are concerned?

Back 39

They generally inhibit all secretions, including sweating.

Front 40

What do muscarinic antagonists do in the lungs?

Back 40

They bronchio-dialate.

Front 41

What do muscarinic antagonists do in the CNS?

Back 41

Produce restlessness, hallucinations, and dellerium.

Front 42

What conditions may muscarinic antagonists be suited to treat therapeutically?

Back 42

Motion sickness, and Prkinson's disease

Front 43

What do muscarinic antagonists do in the eyes?

Back 43

They inhibit the muscles, resulting in dialation, and they increase intraocular pressure.

Front 44

Is it true or untrue that atropine has a significant impact in the cardiovascular system when administered alone?

Back 44

Untrue (False)

Front 45

How are the tertiary amines (which are muscarinic antagonists) best absorbed?

Back 45

From the GI tract namely, but has limited absorption from skin.

Front 46

How are the quaternary amines (which are muscarinic antagonists) best absorbed?

Back 46

Inhalation.