ANS Pharmacology Flashcards

1
Q

norepinephrine

A

a and B agonist

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2
Q

epinephrine

A

B1, B2, a1 agonist

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3
Q

isoproterenol

A

B1, B2, a1 agonist
more selective for B1, 2 than endogenous epinephrine

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4
Q

albuterol

A

B2 agonist

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5
Q

acetylcholine

A

nicotinic and muscarinic agonist

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6
Q

pilocarpine

A

muscarinic agonist

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7
Q

nicotine

A

nicotinic agonist

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8
Q

organophosphate pesticides

A

cholinesterase inhibitor

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9
Q

atropine

A

muscarinic antagonist

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10
Q

characteristics of synaptic transmission

A
  1. rapid
  2. polarized
  3. cholinergic
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11
Q

adrenergic receptors

A

presynaptic neuron releases norepinephrine

alpha 1, 2
beta 1, 2, 3

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12
Q

cholinergic receptors

A

presynaptic neuron releases acetylcholine

nicotinic
muscarinic 1, 2, 3, 4, 5

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13
Q

neuropeptidergic

A

presynaptic neuron releases neuropeptides

calcitonin gene related peptide
tachykinins
vasoactive intestinal peptide
nitric oxide

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14
Q

are adrenergic receptors ionotropic or metabotropic

A

metabotropic (G protein coupled)

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15
Q

a1 receptors

A

Gq protein coupled
excitatory
stimulate PLC –> IP3 + DAG –> increase Ca2+
expressed at postsynaptic sites

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16
Q

a2 receptors

A

Gi protein coupled
inhibitory
inhibit AC –> decrease cAMP
expressed at presynaptic sites

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17
Q

B receptors

A

Gs protein coupled
excitatory
stimulate AC –> increase cAMP

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18
Q

where are B1 receptors most commonly found

A

heart

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19
Q

where are B2 receptors most commonly found

A

most other tissues

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20
Q

where are B3 receptors most commonly found

A

detrusor muscle
adipocytes

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21
Q

what receptors is norepinephrine selective for

A

B1 and a1

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22
Q

what receptors is epinephrine selective for

A

B1 and B2

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23
Q

what receptors is isoprotenerol selective for

A

B1 and B2 (with much higher B selectivity over a than epi)

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24
Q

are muscarinic receptors ionotropic or metabotropic

A

metabotropic

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25
Q

M1, M3, M5 receptors

A

Gq protein coupled
excitatory
stimulate PLC –> IP3 + DAG –> increase Ca2+

26
Q

M2, M4 receptors

A

Gi protein coupled
inhibitory
inhibit AC –> decrease cAMP

27
Q

are nicotinic receptors ionotropic or metabotropic

A

ionotropic

ligand gated ion channels with different subtypes expressed at different effectors

28
Q

somatic neuron pathways

A

monosynaptic with no ganglion

CNS –> efferent –> ACh –> n-AChR on effector

29
Q

effectors of somatic nervous system

A

skeletal muscle

30
Q

autonomic neuron pathways

A

polysynaptic; involve ganglion

31
Q

parasympathetic neuron pathway

A

long preganglionic, short postganglionic

CNS –> pregang –> ACh –> n-AChR on postgang –> ACh –> m-AChR on effector

32
Q

what are the effectors of parasympathetic nervous system

A

cardiac muscle
smooth muscle
glands

33
Q

sympathetic synaptic neuron pathway

A

short preganglionic, long postganglionic

CNS –> pregang –> ACh –> n-AChR on postgang –> NE –> adrenergic receptor on effector

34
Q

what are the effectors of sympathetic nervous system

A

cardiac muscle
smooth muscle
glands
eccrine sweat glands
adrenal medulla

35
Q

sympathetic non-synaptic neuron pathway

A

CNS –> pregang –> ACh –> n-AChR in adrenal medulla –> Epi –> bloodstream –> adrengeric receptor on effector

36
Q

targets of the autonomic nervous system

A
  1. exocrine glands
  2. cardiac muscle
  3. smooth muscle
37
Q

receptors on cardiac muscle

A

B1: (sympathetic) increase HR and contractility

M2: (parasympathetic) decrease HR and contractility

38
Q

receptors on smooth muscle

A

a1: contraction
B2: relaxation
M: contraction

39
Q

sympathetic innervation of blood vessels

A

synaptic a1 receptors: vasoconstriction

non-synaptic B2 receptors: vasodilation
- lower affinity for NE than a1 receptors
- activated by epi in circulation
- expressed on skeletal muscle vasculature

40
Q

autonomic dominance

A

in muscles that are innervated by both sympathetic and parasympathetic fibers - one will be dominant over net effects on the muscle under certain conditions

41
Q

autonomic dominance in pupil diameter

A

radial muscle: dilates the pupil; controlled by sympathetic
circular muscle: constricts the pupil; controlled by parasympathetic

normal conditions: parasympathetic dominant
light conditions: parasympathetic (M3) dominant
dim conditions: sympathetic (a1) dominant

42
Q

cross talk

A

collateral branches of neurons will inhibit ongoing activity of opposing pathway

43
Q

detrusor muscle

A

surrounds the bladder

parasympathetic (M3) –> contraction –> urinary release

sympathetic (B3) –> relaxation –> urinary retention

44
Q

why does sympathetic innervation cause relaxation and parasympathetic innervation cause contraction in urinary muscles?

A

sympathetic B3 receptors use Gs protein –> increase cAMP –> activates PKA –> phosphorylates myosin –> decreases contraction

parasympathetic M3 receptors use Gi protein –> decrease cAMP –> inhibits PKA –> dephosphorylates myosin –> increases contraction

45
Q

internal urethral sphincter muscle

A

surrounds the urethral orifice at junction with bladder

sympathetic (a1) –> contraction –> urinary retention

46
Q

external urethral sphincter

A

skeletal muscle under voluntary control

47
Q

sympathomimetic drugs

A

a/b adrenergic agonists

direct agonists: a1, B1, B2
direct antagonists: presynaptic a2
indirect: PDE inhibitors

48
Q

sympatholytic

A

a/b adrenergic antagonists

direct antagonists: a1, B1, B2
direct agonists: presynaptic a2
indirect: decrease availability of NE

49
Q

parasympathomimetic

A

nicotinic and muscarinic agonists

direct agonists: ACh-like compounds
direct antagonists: presynaptic M2
indirect: cholinesterase inhibitors

50
Q

parasympatholytic

A

nicotinic and muscarinic antagonists

direct antagonists: nAChR and mAChR
direct agonists: presynaptic M2
indirect: botulism toxin; decreases ACh release at NMJ

51
Q

asthma

A

episodic, reversible bronchoconstriction caused by identifiable triggers

52
Q

effects of asthmatic attacks

A
  1. mucus hypersecretion into the lumen of the bronchi
  2. airway inflammation
  3. airway hyperreactivity (increased muscle tone around bronchi)
53
Q

cause of asthma

A

neurologic dysfunction - the nerves innervating the muscle around airways are abnormal

the muscle itself is NORMAL

54
Q

parasympathetic innervation of the airways

A

ACh –> n-AChR on postgang –> ACh –> M2, M3 on airway

results in bronchoconstriction

55
Q

auto-inhibition mechanism of airways

A

M2 receptors on presynaptic side of the pre and post ganglionic fibers

M2 –> Gi protein –> inhibitory to synapse

56
Q

parasympathetic regulatory mechanisms for sympathetic pathways

A

M2 receptors located on airway

M2 –> Gi protein –> decrease cAMP –> promotes contraction

57
Q

is sympathetic or parasympathetic innervation dominant in the airways

A

parasympathetic

maintains muscle tone

58
Q

sympathetic innervation of the airways

A

ACh –> n-AChR on postgang –> NE –> B2 receptors on airway

results in bronchodilation
B2 –> Gs protein –> increase cAMP –> inhibits contraction –> relaxation

59
Q

sympathetic regulatory mechanisms for parasympathetic pathways

A

collateral cross talk

uses B2 receptors on parasympathetic ganglia

60
Q

indirect B2 agonists

A

phosphodiesterase inhibitors

inhibiting PDE –> cAMP persists –> relaxation