Ch. 9 Cholinergic Flashcards Preview

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Flashcards in Ch. 9 Cholinergic Deck (78):
1

Hemicholinium-3

Blocks high-affinity transporter for choline and thereby prevents uptake of choline required for ACh synthesis
RESEARCH ONLY

2

Vesamicol

Blocks the ACh-H+ antiporter used to transport ACh into vesicles
RESEARCH ONLY

3

Botulinum toxin

Degrades synaptobrevin = prevents vesicle fusion on presynaptic membrane

4

Edrophonium

Inhibitor of ACh Degredation: Inhibits acetylcholinesterase (AChE) by binding to enzyme's active site

5

Neostigmine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

6

Pyridostigmine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

7

Ambenonium

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

8

Physostigmine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

9

Diisopropyl fluorophosphate

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site
organophosphate used as insecticide, nerve gas, former topical miotic medication

10

Tacrine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

11

Donepezil

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site

12

Rivastigmine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site
Also affects butyrylcholinesterase by forming a carbamoylate complex with the enzymes

13

Galantamine

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme's active site
Also acts as a nonpotentiating ligand of nicotinic receptors

14

Methacholine

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

15

Carbachol

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity
Cannot be used systemically

16

Bethanechol

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity
Almost completely selective for muscarinic receptors

17

Cevimeline

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

18

Pilocarpine

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

19

Succinylcholine

Nicotinic Receptor Agonist: Stimulate opening of nicotinic ACh receptor channel and produce depolarization of the cell membrane.
Persists at the neuroeffector junction and activates the nicotinic receptor channels continuously --> inactivation of voltage-gated Na+ channels = cannot open to support further APs
Short duration = DOC for paralysis during intubation.

20

Another name for action of succinylcholine

"Depolarizing blockade"

21

Atropine

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

22

Scopolamine

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

23

Pirenzepine

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

24

Methscopolamine

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

25

Glycopyrrolate

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

26

Ipratropium

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

27

Tiotropium

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

28

Oxybutynin

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

29

Propantheline

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

30

Terodiline

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

31

Fesoterodine

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

32

Trospium

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

33

Darifenacin

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective

34

Solifenacin

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective

35

Pancuronium

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
LONG ACTING

36

Tubocurarine

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
LONG ACTING

37

Vecuronium

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
INTERMEDIATE ACTING

38

Rocuronium

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
INTERMEDIATE ACTING

39

Mivacurium

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
SHORT ACTING

40

Trimethaphan

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
Administered when ganglionic blockade is desired - HTN acute aortic dissection

41

Mecamylamine

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade")
Administered when ganglionic blockade is desired - HTN acute aortic dissection

42

Types of cholinergic receptors

Muscarinic and Nicotinic

43

Muscarinic receptors are

G protein coupled receptors

44

Nicotinic Receptors are

ligand-gated ion channels

45

M1, M3, and M5 mAChR

Gq/11 --> PLC --> increased IP3 and DAG --> increased Ca2+ and increased PKC = excitatory

46

M2 and M4 mAChR

Beta/gamma of G protein --> inhibition of adenylyl cyclase and increased K+ channel opening = suppress cellular excitability

47

Location of M1

Autonomic ganglia = late excitatory postsynaptic potential
CNS = arousal, attention, analgesia

48

Location of M2

Heart:
- SA node = slowed spontaneous depolarization; hyperpolarization
- AV node = decrease conduction velocity
- Atrium = decrease refractory period, decrease contractile force
- Ventricle = slight decrease in contractility

49

Location of M3

Smooth muscle = contraction

50

Location of M4

CNS

51

Location of M5

CNS

52

Nicotinic receptors

Ligand-gated ion channels --> net inward Na+ depolarizing the cell
-Direct ligand-gated conductance
- requires binding of 2 ACh to 1 nAChR --> conformational change of 2 alpha subunits
2 alpha, 1 beta, 1 delta, 1 epsilon (mature skel m) OR 1 gamma (embryonic

53

Nicotinic Nm receptor Location

NMJ - skeletal muscle
- opening of Na+/K+ channels --> skeletal muscle contraction

54

Nicotinic Nn receptor location

Autonomic ganglia
- opening of Na+/K+ channels --> depolarization and firing of postganglionic neuron
Adrenal medulla
- opening of Na+/K+ channels --> secretion of catecholamines
CNS
- opening of Na+/K+ channels --> arousal, attention analgesia

55

2 cholinesterases

1. AChE - postsyn membrane
2. Butyrylcholinesterase (BuChE) secondary role, may be involved in path of Alzheimer's

56

Latency of mAChR

100 - 250 msec

57

Latency of nAChR

5 msec

58

Principle neurotransmitter at the NMJ that is released by alpha motor neurons --> binding of nicotinic receptors and motor end-plate depolarization

ACh
- extent of depolarization depends on QUANTITIY of ACh

59

Effect of Gaglionic Blockade on ARTERIOLES

(mainly adrenergic sympathetic tone) --> Vasodilation, increased peripheral blood flow, hypotension

60

Effect of Gaglionic Blockade on VEINS

(mainly adrenergic sympathetic tone) --> vasodilation, pooling of blood, decreased of venous return, decreased cardiac output

61

Effect of Gaglionic Blockade on HEART

(mainly parasymp cholinergic tone) --> tachycardia

62

Effect of Gaglionic Blockade on IRIS

mainly parasymp cholinergic tone --> Mydriasis (pupil dilation)

63

Effect of Gaglionic Blockade on CILIARY MUSCLE

mainly parasymp cholinergic tone --> cycloplegia (focused to far vision)

64

Effect of Gaglionic Blockade on GI TRACT

Mainly parasymp cholinergic tone --> decreased tone and motility; constipation; decreased secretions

65

Effect of Gaglionic Blockade on URINARY BLADDER

Mainly parasymp cholinergic ton --> urinary retention

66

Effect of Gaglionic Blockade on SALIVARY GLANDS

Mainly parasymp cholinergic tone --> xerostomia (dry mouth)

67

Effect of Gaglionic Blockade on SWEAT GLANDS

Mainly symp cholinergic tone --> Anhidrosis (absence of sweating)

68

Effects of ACh on VASCULATURE (endothelial cells)

Release of NO and vasodilation

69

Effects of ACh on EYE IRIS (pupillae sphincter muscle)

Contraction and miosis (constriction of pupil)

70

Effects of ACh on CILIARY MUSCLE

Contraction and accommodation for near vision

71

Effects of ACh on SALIVARY AND LACRIMAL GLANDS

Thin and watery secretions

72

Effects of ACh on BRONCHI

Constriction
Increased secretions

73

Effects of ACh on HEART

Bradycardia
Decreased conduction velocity
AV block at high doses
Slight decrease in contractility

74

Effects of ACh on GI TRACT

Increased Tone
Increased secretions
Relaxation of sphincters

75

Effects of ACh on URINARY BLADDER

Contraction of detrusor muscle
Relaxation of sphincter

76

Effects of ACh on SWEAT GLANDS

Diaphoresis (sweating)

77

Effects of ACh on REPRODUCTIVE TRACT, MALE

Erection

78

Effects of ACh on UTERUS

Variable