Kruse - Cholinergic Agonists/Antagonists Flashcards Preview

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Flashcards in Kruse - Cholinergic Agonists/Antagonists Deck (101)
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1

Cholinesterase hydrolyzes at what rates?

ACh > methacholine > carbachol = bethanechol

2

ACh mimetics act on receptors by:

-Direct acting mAChR and nAChR stimulants
-Indirect cholinesterase inhibitors

3

Two types of direct acting cholinergic agonists

1. Choline esters
2. Akaloids

4

Choline ester names

ACh, carbachol, bethanechol

5

Alkaloid names

Muscarine, nictoine, policarpine

6

Choline ester:
Absoprtion -
Distribution -

Choline ester:
Absorption - poorly absorbed in CNS (quaternary ammonium groups)
Distribution - poorly distributed in CNS

7

Choline ester metabolism location

Metabolism - hydrolyzed by cholinesterase in GI

8

choline ester less active when given ___

PO

9

Alkaloid
Absorption -

Absorption - well absorbed from most sites (i.e. noctine thru skin)

10

muscarine (mushroom) ingestion is (toxic or not) and goes to what location

Toxic
Enters brain

11

Alkaloid metabolism

Kidney excretion >> acidification of urine accelerates clearance

12

Choline ester = Type of molecule = absorbed well?
Alkaloid = Type of molecule = absorbed well?

Choline ester = charged quaternary amine = not well absorbed
Alkaloid = uncharged tertiary amine = well absorbed

13

M1 location

nerves

14

M2 location

HEART, nerves, smooth muscle

15

M3 location

glands, smooth muscle, endothelium

16

M4 location

CNS

17

M5 location

CNS

18

Nm

skeletal muscle NMJ

19

Nn

postG cell body, dendrites, CNS

20

Gq M recetors
IP3, DAG

M1,3,5

21

Gi M receptors
Inhibit cAMP

M2, 4

22

Type of receptor and its action on skeletal muscle

nAChR
muscle contraction

23

ParaS effect of...

decrease/contract everything, except:
Dilation of aa and vv.
Stimulation of bronchial glands
Detrusor contraction; trigone and sphincter relaxation
Sweat, salivary, lacrimal, naspharyngeal secretion

24

ParaS eye - contraction of relaxation of iris sphincter and ciliary mm?

contraction to:
increase aqueous humor >> Schlemm >> ant chamber drainage

25

What are all cardiac actions mediated by?

M2 mAChR

26

PS innervation is less in ventricle or atria?

ventricles (so less physiological effect when activated)

27

Muscarinic agonists release what form endothelial cells to relax smooth muscle around blood vessels?

Endothelium Derived Relaxing Factor (EDFR)

28

EDFR is largely ___, which activates ___, and ___cGMP in smooth muscle.
Overall effect of this is: ____

NO >> activates...
GC >>
increases cGMP>>
Overall: to relax smooth muscle

29

Small doses of ACh = ____ effect on CV
Large doses of ACh = ____ effect on CV

small = vasodilation = decrease BP and increased HR
large = bradycardia and decrease AV node conduction + hypOTension

30

GI:
M__ mACHR required for direct activation of smooth muscle relaxation
M__ mAChR reduces cAMP = reduces relaxation (increased contraction)

M2
M3