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Medical Pharmacology > Overview of Neurotransmission > Flashcards

Overview of Neurotransmission Flashcards

(102 cards)

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1
Q

what is an agonist that directly interacts with Nn receptors

A

nicotine

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2
Q

what is a partial agonist that directly interacts with Nn receptors

A

varenecline (chantix)

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3
Q

what is an antagonist that directly interacts with Nn receptors

A

mecamylamine

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4
Q

action of succinylcholine

A

a noncompetitive, depolarizing Nm blocker (cannot reach Emax)

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5
Q

action of CURare derivatives

A

nondepolarizing Nm blocker (competitive) (can still reach Emax)

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6
Q

example of CURare derivative

A

roCURonium (zemuron )

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7
Q

what are 5 targets for neurotransmitters?

A
  1. synthesis
  2. storage
  3. release
  4. termination of action
  5. receptor (direct)
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8
Q

4 indirect targets of NT

A

synthesis, storage, release, termination of action

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9
Q

direct target of NT

A

receptors

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10
Q

role of adrenal medulla in sympathetic activation

A

releases 80% epinephrine and 20% norepi in response to ACh stimulation

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11
Q

receptor type on sweat glands

A

Muscarinic receptors (M3) on erector pili and sweat glands, even though anatomically sympathetic (but postgang fibers release ACh)

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12
Q

what receptors are associated with the enteric nervous system

A

oral and aboral

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13
Q

what are oral receptors for

A

control peristalsis of GI via Gq GPCR

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14
Q

what are aboral receptors for

A

activate relaxation of GI via Gs GPCR

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15
Q

what activates oral receptors

A

ACh and other substances and Gq (peristalsis)

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16
Q

what activates aboral receptors

A

norepi and other substances and Gs (relaxation)

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17
Q

how does alteration of ACh, norepi serotonin and others with drugs impact ENS?

A

impacts oral and aboral receptors to either increase peristalsis (diarrhea!!) or cause GI slowing

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18
Q

what is NANC

A

nonadrenergic noncholinergic neurons

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19
Q

what are the NANC “players”

A

nitric oxide, vasoactive intestinal peptide, calcitonin gene related peptide, adenosine, CCK, endogenous opioids, tachykinins

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20
Q

what do NANC do

A
  1. penile erection
  2. peristalsis GI
  3. relaxation of vascular smooth muscle
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21
Q

action of sympathetic activation on blood vessels

A

a1 receptors are innervated, but B2 receptors are NOT innervated…therefore, GPCR a1 causes primary vasoconstriction then slight relaxation as the adrenal medulla releases epinephrine to activate (noninnervated) B2

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22
Q

action of sympathetic activation on lungs

A

B2 receptors (not innervated) are activated by epinephrine release by adrenal medulla, causing bronchodilation

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23
Q

what activates epi and norepi release from adrenal medulla?

A

ACh on Nn

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24
Q

sympathetic actions

A
  1. mydriasis (dilation)
  2. reduced saliva flow (a1)
  3. increased SV and HR (B1)
  4. vasoconstriction
  5. reduced peristalsis and secretion
  6. increased glucogenolysis
  7. inhibition of gladder contraction
  8. epinephrine release
  9. B2 bronchodilation
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25
parasympathetic actions
1. miosis (constriction) and accommodation 2. stimulated saliva flow 3. decreased HR (vagus) 4. bronchoconstriction (vagus) 5. peristalsis and secretion (vagus) 6. stimulate bile release (vagus) 7. bladder contraction
26
which effector organ is innervated by the sympathetic nervous system but is activated when postgang sympathetic nerve releases ACh?
adrenal medulla
27
describe somatic neuron
Ach Nm neuron (NMJ)
28
describe parasympathetic neuron
Ach releasing (long )preganglionic neuron at Nn, then Ach releasing (short) postganglionic fiber at Muscarinic receptor on target organ
29
describe sympathetic neuron
Ach releasing (short) preganglionic neuron at Nn, then norepi (mostly) releasing (long) postganglionic fiber at adrenergic receptor on target organ except adrenal medulla, has Ach releasing neuron
30
how does SNS stimulate bronchodilation
works through Nn on adrenal medulla to release epi relies on epi from adrenal medulla because B2 is not innervated
31
what is the autoreceptor
a2 -- turns off further release of sympathetic outflow from the neuron
32
what is the M1 receptor
Gq receptor in head
33
M2 receptor
Gi receptor in heart, and autoreceptor
34
M3 receptor
Gq receptor everywhere else
35
a1 receptor
Gq coupled, increases Ca which acts on smooth muscle to contract (arterial smooth muscle, mydriasis)
36
a2 receptor
Gi coupled, autoreceptor, CNS, deactivates K (If) (funny current) channels (doesn't bring back up to depolarizing) on presynaptic terminal
37
B1 receptor
Gs on the heart and juxtaglomerular cells (macula densa) to increase renin
38
B2 receptor
Gs relaxation of smooth muscle, bronchioles, gravid uterus, vascular endothelium (epi>NE) and skeletal muscle, increases glucose uptake and Na/K ATPase
39
what causes Reynaud's syndrome
excessive a1 stimulation
40
B3 receptor
Gs lipolysis, thermogenesis, detrusor relaxation (step urination)
41
what causes contraction in gravid uterus
toward the end of pregnancy, increased number of a1 receptors in the gravid uterus cause it to contract
42
how does Gs inhibit platelet activation
vasodilator activated phospholipid inside of the platelet is phosphorylated by Gs, which decreases likelihood of platelet being activated and aggregate
43
what degrades cAMP
phosphodiesterase (PDE)
44
how do some indirect agonists work
inhibit PDE so longer functioning of cAMP
45
what is the SNS autoreceptor
a2
46
what is the PSNS autoreceptor
M2 and M4
47
presynaptic mechanism of regulation
a2 autoreceptor and M2 autoreceptors
48
postsynaptic mechanism of regulation
receptor down and upregulation
49
what occurs if receptor is constantly blocked
is upregulated
50
what occurs if receptor is constantly activated
is downregulated and endocytosed via phosphorylation and activation of beta arrestin
51
how to cause tolerance
constant exposure of drug to receptor causes downregulation of receptor.
52
what causes withdrawal
a sudden stoppage of a drug that has caused downregulation of receptors, causes opposite effect of the drug bc fewer receptors and took away excess agonist
53
what causes dependence
no longer have regular or normal function without an exogenous substance due to receptor downregulation and withdrawal
54
steps of beta receptor desensitization
1. initial exposure to agonist causes cAMP response 2. continued exposure causes diminished response within a few minutes due to phosphorylation of receptor with subsequent beta arrestin binding 3. internalization of bound receptor 4. dephosphorylation by phosphatase 5. return to cell membrane OR lysosomal degradation
55
how are blood vessels controlled in PSNS
M3 receptors are NOT innervated aka no endogenous signal therefore, a drug that increases ACh won't impact this receptor because it can't travel to it
56
how are nicotinic receptors activated
2 ACh molecules
57
where are M receptors found
organs innervated by PSNS and pili erector muscle and eccrine sweat glands
58
what is the result of activation of Nn in the ganglia?
increased outflow of both SNS and PSNS
59
what is the result of inhibition of acetylcholinesterase?
accumulation of ACh and increase of SNS and PSNS
60
what controls BP
almost entirely SNS
61
describe baroreceptor reflex arc
stimulation of a1 on vascular smooth muscle causes contraction and increased peripheral resistance, increasing BP. body responds by activating M2 on the heart which decreases HR.
62
what do drugs that cause vasoconstriction usually cause?
reflex decrease in HR
63
what do drugs that cause vasodilation usually cause
reflex increase in HR
64
what is mecamylamine used for
it is a Nn antagonist used in exams to test knowledge of reflex responses of HR to BP
65
MOA mecamylamine
blocks Nn, the reflex pathway is blocked at the ganglia so no reflex change in HR can occur
66
effect of PSNS on CNS
M1 receptors, help with memory/cognition, balances with dopamine for control of movement
67
effect of PSNS on eye and ciliary muscle
M3 receptors for miosis (constriction) and lacrimation, and contract for accommodation (near vision)
68
effect of PSNS on salivation
increased salivation (M3)
69
effect of PSNS on bronchiolar smooth muscle
M3 - contraction (bronchoconstriction)
70
effect PSNS on heart
M2 causes decreased rate
71
effect of PSNS on blood vessels
M3 is not innervated on vasculature, but is stimulated by exogenous agonists' increased NO release
72
effect of PSNS on GI and sphincters
M3 receptors cause increased secretion and peristalsis
73
effect of PSNS on bladder
contract detrusor muscle (urination) (M3), trigone and sphincter relax (M2)
74
effect of PSNS on male GU
erection via NANC increased NO | M3
75
effect of SNS on CNS
beta 2 provokes fear, anxiety, mood and learning | alpha 2 increases signal to noise ratio
76
effect of SNS on the eye
alpha 1 causes mydriasis (dilation) | beta causes increased aqueous humor
77
effect of SNS on salivary
alpha 1 decreases salivary
78
effect of SNS on bronchiolar smooth muscle
beta 2 causes bronchodilation
79
effect of SNS on the heart
beta 1 increases rate, force, conduction, and automaticity
80
effect of SNS on blood vessels
alpha 1 causes contraction and increased blood pressure | beta 2 causes relaxation and decreased blood pressure via epi
81
effect of SNS on GI and sphincters
alpha 1 causes decreased secretion, and decreased peristalsis, and decreased contraction
82
effect of SNS on liver
alpha 1 and beta 2 cause glycogenolysis and gluconeogenesis
83
effect of SNS on sweat glands
M3 receptors respond to promote sweating
84
effect of SNS on kidney
beta 1 causes increased renin release from JGA
85
effect of SNS on bladder
beta 3 causes detrusor to relax | alpha 1 causes trigone and sphincter to contract
86
effect of SNS on male GU
alpha 1 causes ejaculation
87
effect of SNS on uterus
alpha 1 causes gravid contraction | beta 2 causes gravid and nongravid relaxation
88
effect of SNS on fat cells
beta 3 causes thermogenesiss, lipolysis, decreased leptin release
89
effect of SNS on skeletal muscle
beta 2 causes K and glucose uptake
90
MOA of nicotine
full agonist at nicotinic receptors, but at high doses is a depolarizing nicotinic antagonist (noncompetitive)
91
initial action of nicotine
turns on Nn receptors, but doesn't let go = depolarizing blockade (desensitization)
92
why is vascular tone predominantly sympathetic
alpha 1 receptor gets the signal from neuron that releases norepi but M3 receptors on blood vessels don't have innervation (no postganglionic fiber leads to M3) so see only sympathetic.
93
dominant tone of arterioles
sympathetic (alpha 1 is innervated, M3 is not)
94
dominant tone of veins
sympathetic
95
dominant tone of heart
parasympathetic (M2)
96
dominant tone of pupil
parasympathetic (M3)
97
dominant tone of ciliary
parasympathetic (M3)
98
dominant tone of GI
parasympathetic (M3)
99
dominant tone of bladder
parasympathetic (M3)
100
dominant tone of salivary
parasympathetic (M3)
101
dominant tone of sweat
sympathetic (but have M3)
102
what occurs with prolonged toxic levels of nicotine?
Nn receptor becomes refractory and effects will match "blockade" due to loss of dominant tone (opposite effect)

Medical Pharmacology (13 decks)

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