Pharmacology - Autonomics I Flashcards Preview

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Flashcards in Pharmacology - Autonomics I Deck (118):
1

Postganglionic PS fibers release:

Aceytlcholine
"cholinergic"

2

Postganglionic symptathetic fibers generally release:

Norepinephrine
"adrenergic"

3

T/F: Not all postganglionic sympathetic fibers are adrenergic - other NTs can be used.

True

4

All preganglionic neurons, both sympathetic and parasympathetic, release:

ACh and stimulate nicotinic receptors on postganglionic neurons

5

All preganglionic neurons, both sympathetic and parasympathetic, release ACh and stimulate ______ receptors on postganglionic neurons.

Nicotinic

6

All postganglionic PS neurons release ACh and stimulate _____ ACh receptors on target tissues.

Muscarinic

7

Postganglionic symptathetic fibers to sweat glands release:

ACh

8

Postganglionic sympathetic fibers to renal vessels release:

Dopamine

9

____ blocks ACh and, when, injected, can locally inhibit muscle contraction.

Botulinim Toxin A

10

Drugs that block NE synthesis, storage or release, for example, guanethidine, are useful in several diseases like hyptertension, because they block _____ function

sympathetic, but NOT parasympathetic

11

What is the physiologic effect of cocaine?

To block NE uptake --> increase adrenergic transmission

12

Cholinoceptors include:

Muscarinic
Nicotinic

13

Where are M1 receptors found?

Location:
CNS
sympathetic PG neurons

Effects:
formation of IP3 and DAG
increased intracellular Ca
**same as M3 receptors (exocrine glands, CNS, vessels)
**same as M5 receptors (vascular endothelium esp cerebral vessels, CNS)

14

Where are M2 receptors found?

Location:
Myocardium
Smooth muscle
CNS

Effects:
open K channels
inhibit Adenyl cyclase
**same as M4 receptors (CNS)

15

Nicotinic receptors, both Nn (N2) and Nm (N1) have what effect?

Opening of Na and K channels, depolarization

16

Where are Nm (N1) receptors found?

Skeletal muscle neuromuscular end plates

17

What is the effect of Alpha 1 adrenergic receptors?

Effects:
Formation os IP3 and DAG
increased intracellular Ca

Location:
Postsynaptic effector cells esp smooth muscle

18

What is the effect of Alpha 2 (adrenoreceptors) receptors?

Effects:
Inhibition of adenyl cyclase
decreased cAMP

Location:
Presynaptic adrenergic nerve terminals,
platelets
lipocytes
smooth muscle

19

All beta (adrenoreceptors) receptors have what function?

stimulate AC
increase cAMP

all found in heart, beta-1 found most widespread in the body

20

All muscarinic receptors (M1-M5) are

GPCRs
M2, M4 --> Gi (decrease cAMP, hyperpolarize) --> inhibition of neurotransmitter release

M1, M3, M5 --> Gq (increase IP3 and DAG)

**enables ACh to have specific effects, depending on the receptor

21

Class: Bethanechol

Direct acting carbamic acid ester
cholinomimetic

22

MOA: Bethanechol

Direct-acting muscarinic cholinomimetic

23

Uses: Bethanechol

Post-operative and neurogenic ileus;
urinary retention (bowel and bladder smooth muscle ACh-innervated)

24

Side Effects: Bethanechol

SLUDGE
Salivation: stimulation of the salivary glands
Lacrimation: stimulation of the lacrimal glands
Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles
Diaphoresis
Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea
Emesis: Vomiting

25

Class: Pilocarpine

Direct acting non-ester alkaloid
cholinomimetic

26

MOA: Pilocarpine

Direct-acting muscarinic cholinomimetic

27

Uses: Pilocarpine

Glaucoma (ACh activates sphincter and ciliary muscles of eye)

28

Side Effects: Pilocarpine

SLUDGE
Salivation: stimulation of the salivary glands
Lacrimation: stimulation of the lacrimal glands
Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles
Diaphoresis
Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea
Emesis: Vomiting

29

Class: Cevimeline

Direct acting non-ester alkaloid
cholinomimetic

30

MOA: Cevimeline

Direct-acting muscarinic cholinomimetic

31

Uses: Cevimeline

Dry mouth/xerostomia (in, e.g., Sjogren's, post-radiation therapy; via increased salivation)

32

Side Effects: Cevimeline

SLUDGE
Salivation: stimulation of the salivary glands
Lacrimation: stimulation of the lacrimal glands
Urination: relaxation of the internal sphincter muscle of urethra, and contraction of the detrusor muscles
Diaphoresis
Gastrointestinal upset: Smooth muscle tone changes causing gastrointestinal problems, including diarrhea
Emesis: Vomiting

33

Class: Nicotine

Direct acting non-ester alkaloid
cholinomimetic

34

MOA: Nicotine

Direct-acting muscarinic cholinomimetic

35

Uses: Nicotine

Smoking cessation/reduces craving

36

Class: Physiostigmine

Indirect acting carbamate
cholinomimetic

37

MOA:
Physostigmine
Echothiophate

AChE inhibitor (short acting)

38

Uses:
Physostigmine
Echothiophate

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

39

Side Effects: Physostigmine

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

40

Class:
Muscarine
Pilocarpine
Cevimeline
Nicotine

Direct acting non-ester alkaloid
cholinomimetic

41

Uses:
Pilocarpine
Physostigmine
Echothiophate

Glaucoma

42

Class: Edrophonium

Indirect acting non-ester
cholinomimetic

43

MOA: Edrophonium

AChE inhibitor (v. short acting)

44

Uses:
Edrophonium
Pyridostigmine
Neostigmine

Myasthenia Gravis

45

Side Effects: Edrophonium

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

46

Class: Neostignmine

Indirect acting carbamate
cholinomimetic

47

Class:
Neostigmine
Physostigmine

Indirect acting carbamate

48

MOA: Neostigmine

AChE inhibitor (short acting)

49

Uses: Neostigmine

Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade

50

Side Effects: Neostigmine

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

51

Class: Muscarine

Direct acting non-ester alkaloid
cholinomimetic

52

MOA: Muscarine

Direct-acting muscarinic cholinomimetic

53

Side Effects: Muscarine

SLUDGE

54

Class: Donepezil

Indirect acting non-ester
cholinomimetic

55

MOA: Donepezil

AChE inhibitor

56

Uses: Donepezil

Alzheimer's (amplifies endogenous ACh in brain)

57

Side Effects: Donepezil

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

58

Class:
Donepezil
Edrophonium

Indirect acting non-ester
cholinomimetic

59

Side Effects:
Neostigmine
Physostigmine
Donepezil
Sarin
Edrophonium
Echothiophate
Pralidoxime

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

60

Side Effects:
Bethanechol
Muscarine
Pilocarpine
Cevimeline

SLUDGE

61

Class: Echothiophate

Indirect acting organophosphate
cholinomimetic

62

MOA: Echothiophate

AChE inhibitor (long acting)

63

Uses: Echothiophate

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

64

Side Effects: Echothiophate

SLUDGE
general increase in cholinergic neurotransmission;
paralysis

65

Class: Sarin

Very potent indirect acting organophosphate
cholinomimetic

66

MOA: Sarin

AChE inhibitor

67

Uses: Sarin

volatile nerve gas

68

Side Effects: Sarin

SLUDGE
general increase in cholinergic neurotransmission;
paralysis
DEATH

69

Class: Pralidoxime

Strong nucleophile
cholinomimetic

70

MOA: Pralidoxime

AChE inhibitor

71

Uses: Pralidoxime

Poisoning by nerve gas, insecticide

72

Class: Atropine

Tertiary amine antimuscarinic
cholinergic receptor inhibitor

73

Class:
Atropine
Scopolamine
Dicyclomine
Tropicamide
Tolterodine
Benztropine

Tertiary amine antimuscarinic
cholinergic receptor inhibitor

74

MOA: Atropine

Blocks muscarinic receptors

75

MOA:
Atropine
Scopolamine
Dicyclomine
Tropicamide
Tolterodine
Benztropine
Ipratroprium
Tiotropium

Blocks muscarinic receptors

76

Side Effects:
Atropine
Scopolamine
Dicyclomine
Tropicamide
Tolterodine
Benztropine
Ipratroprium
Tiotropium

General block of muscarinic functions

77

Uses:
Atropine
Tropicamide

To cause:
Mydriasis
Cycloplegia is paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation

*Tropicamide has a short half life

78

Uses: Scopolamine

Motion sickness

79

Uses: Dicyclomine

Reduce transient hypermotility of GI tract

80

Uses: Tolterodine

Treat transient cystitis;
postoperative bladder spasms;
incontinence

81

Uses: Benztropine

To prevent manifestations of Parkinson's disease

82

Class:
Ipatroprium
Tiotropium

Quarternary amine antimuscarinic
cholinergic receptor inhibitor

83

Uses:
Ipatroprium
Tiotropium

Bronchodilation in asthma or COPD

84

Class: Succinylcholine

Depolarizing blocker
cholinergic receptor inhibitor

85

MOA: Succinylcholine

Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation

86

Uses: Succinylcholine

Brief procedures (e.g., tracheal intubation, reset dislocated joints)

87

Side Effects:
Succinylcholine
Tubocurarine
Mivacurium

Respiratory paralysis;
disturbance of autonomic function

88

MOA:
Tubocurarine
Mivacarium

Blocks nicotinic (Nm) receptor

89

Class:
Tubocurarine
Mivacarium

Nondepolarizing blocker
cholinergic receptor inhibitor

90

Uses:
Tubocurarine
Mivacarium

Muscle relaxant for surgery w/o deep anesthesia

91

Class: Botulinum Toxin A

local paralytic

92

MOA: Botulinum Toxin A

Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25

93

Uses: Boltulinum Toxin A

Reduce frown lines and wrinkles;
achalasia;
strabismus;
oromandibular dystonia

94

Class:
Hexamethonium
Mecamylamine

Ganglionic blocker
cholinergic receptor inhibitor

95

MOA:
Hexamethonium
Mecamylamine

Blocks ganglionic (Nn) receptor and sympathetic tone

96

Uses:
Hexamethonium
Mecamylamine

Hypertensive crisis; "Bloodless" field surgery

97

Clinical Uses:
Ipratroprium
Tiotroprium

to cause bronchodilation in asthma and COPD

98

What kind of amine is atropine?

Tertiary - can interact with CNS AND peripheral muscarinic receptors well - good for nerve gas exposure

99

Mnemonic for atropine overdose

Dry as a bone - no glandular secretions
Blind as a bat - blockade of accomodation and excessive dilation
Red as a beet - atropine flush - dilation of cutaneous blood vessels AND inhibition of sweat glands (inhibition alpha-1 mediated vasoconstriction)
--also atropine fever from lack of sweating
Mad as a hatter - delirium - CNS

100

Atropine fever can be lethal in:

infants and small children
Sweat glands are sympathetic but utilize cholinergic post-ganglionic fibers
**symptom managament** to treat, do not use a cholinesterase inhibitor ie physostigmine

101

Prazosin

alpha-blocker
alpha-1 selective antagonist

102

Phenoxybenzamine

alpha-blocker
Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor)

103

Therapeutic Use: Prazosin

Raynaud's
BPH
Primary HTN

104

Therapeutic Use: Phenoxybenzamine

Pheochromocytoma, Raynaud's, frostbite

105

MOA Tyramine

Increases NE release
gets uptaken into cleft like NE

106

Best way to adrenergically increase HR:

Epinephrine
Beta-1 effects greater than NE

107

MOA Terbutaline

beta-2 selective agonist

Uses: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD; early labor

108

Glaucoma is treated with muscarinic agonists or antagonists?

muscarinic agonists, which facilitate the outflow of aqueous humor

109

An alpha agonist vasodilates or vasocontricts?

Vasoconstricts

110

Parasympathetic control of salivation is mediated by:

M3 receptors found in salivary glands; these receptors elevate calcium concentration and activate the secretory process.

111

T/F: Although MAO may contribute to the ultimate metabolism of NE, it does not assist in the termination of NE neurotransmission.

True

Termination of NE neurotransmission:
Uptake by non-neuronal cells.
Diffusion out of the synaptic cleft.
Uptake by neuron plasma membrane.

112

Phenylephrine MOA

alpha-1 agonist
decongestant
vasoconstriction → increase in total peripheral resistance → increase in blood pressure → activation of a baroreceptor response to decrease sympathetic outflow and increase parasympathetic outflow, resulting in a decrease in heart rate.

113

For prevention of migraines, consider:

Propranolol, methysergide, and calcium channel blockers have all been shown to be prophylactic in migraine therapy.

114

For treatment of an acute migraine, consider:

Ergotamine and the several “triptans” (e.g. sumatriptan [Imitrex]) are effective in the acute treatment of a migraine headache.

115

T/F: Activation of α2 receptors which are presynaptic can reduce subsequent release of norepinephrine from post-ganglionic fibers.

True

116

MOA Succinylcholine

Succinylcholine (diacetylcholine) activates Nm persistently because it is poorly hydrolyzed at the NMJ. This hyperactivation causes persistent depolarization at the endplate, blocking Nm function and leading to flaccid paralysis.

117

Side effects: Prazosin

Orthostatic HTN;
Tachycardia

118

How would metoprolol decrease renin release?

blocking beta receptors on juxtaglomerular apparatus cells