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
M1, M3, M5 receptors
Gq protein coupled excitatory stimulate PLC --> IP3 + DAG --> increase Ca2+
26
M2, M4 receptors
Gi protein coupled inhibitory inhibit AC --> decrease cAMP
27
are nicotinic receptors ionotropic or metabotropic
ionotropic ligand gated ion channels with different subtypes expressed at different effectors
28
somatic neuron pathways
monosynaptic with no ganglion CNS --> efferent --> ACh --> n-AChR on effector
29
effectors of somatic nervous system
skeletal muscle
30
autonomic neuron pathways
polysynaptic; involve ganglion
31
parasympathetic neuron pathway
long preganglionic, short postganglionic CNS --> pregang --> ACh --> n-AChR on postgang --> ACh --> m-AChR on effector
32
what are the effectors of parasympathetic nervous system
cardiac muscle smooth muscle glands
33
sympathetic synaptic neuron pathway
short preganglionic, long postganglionic CNS --> pregang --> ACh --> n-AChR on postgang --> NE --> adrenergic receptor on effector
34
what are the effectors of sympathetic nervous system
cardiac muscle smooth muscle glands eccrine sweat glands adrenal medulla
35
sympathetic non-synaptic neuron pathway
CNS --> pregang --> ACh --> n-AChR in adrenal medulla --> Epi --> bloodstream --> adrengeric receptor on effector
36
targets of the autonomic nervous system
1. exocrine glands 2. cardiac muscle 3. smooth muscle
37
receptors on cardiac muscle
B1: (sympathetic) increase HR and contractility M2: (parasympathetic) decrease HR and contractility
38
receptors on smooth muscle
a1: contraction B2: relaxation M: contraction
39
sympathetic innervation of blood vessels
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
autonomic dominance
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
autonomic dominance in pupil diameter
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
cross talk
collateral branches of neurons will inhibit ongoing activity of opposing pathway
43
detrusor muscle
surrounds the bladder parasympathetic (M3) --> contraction --> urinary release sympathetic (B3) --> relaxation --> urinary retention
44
why does sympathetic innervation cause relaxation and parasympathetic innervation cause contraction in urinary muscles?
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
internal urethral sphincter muscle
surrounds the urethral orifice at junction with bladder sympathetic (a1) --> contraction --> urinary retention
46
external urethral sphincter
skeletal muscle under voluntary control
47
sympathomimetic drugs
a/b adrenergic agonists direct agonists: a1, B1, B2 direct antagonists: presynaptic a2 indirect: PDE inhibitors
48
sympatholytic
a/b adrenergic antagonists direct antagonists: a1, B1, B2 direct agonists: presynaptic a2 indirect: decrease availability of NE
49
parasympathomimetic
nicotinic and muscarinic agonists direct agonists: ACh-like compounds direct antagonists: presynaptic M2 indirect: cholinesterase inhibitors
50
parasympatholytic
nicotinic and muscarinic antagonists direct antagonists: nAChR and mAChR direct agonists: presynaptic M2 indirect: botulism toxin; decreases ACh release at NMJ
51
asthma
episodic, reversible bronchoconstriction caused by identifiable triggers
52
effects of asthmatic attacks
1. mucus hypersecretion into the lumen of the bronchi 2. airway inflammation 3. airway hyperreactivity (increased muscle tone around bronchi)
53
cause of asthma
neurologic dysfunction - the nerves innervating the muscle around airways are abnormal *the muscle itself is NORMAL*
54
parasympathetic innervation of the airways
ACh --> n-AChR on postgang --> ACh --> M2, M3 on airway results in bronchoconstriction
55
auto-inhibition mechanism of airways
M2 receptors on presynaptic side of the pre and post ganglionic fibers M2 --> Gi protein --> inhibitory to synapse
56
parasympathetic regulatory mechanisms for sympathetic pathways
M2 receptors located on airway M2 --> Gi protein --> decrease cAMP --> promotes contraction
57
is sympathetic or parasympathetic innervation dominant in the airways
parasympathetic maintains muscle tone
58
sympathetic innervation of the airways
ACh --> n-AChR on postgang --> NE --> B2 receptors on airway results in bronchodilation B2 --> Gs protein --> increase cAMP --> inhibits contraction --> relaxation
59
sympathetic regulatory mechanisms for parasympathetic pathways
collateral cross talk uses B2 receptors on parasympathetic ganglia
60
indirect B2 agonists
phosphodiesterase inhibitors inhibiting PDE --> cAMP persists --> relaxation