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Pharmacology Capstone Flashcards

0
Q

parasympathetic nervous system is aka

A

craniosacral

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1
Q

sympathetic nervous system is aka

A

thoracolumbar

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2
Q

Parasympathetic NT and R

A

NT=Ach

R=NAchR, MAchR

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3
Q

Sympathetic NT and R

A 
NT= NE>epi>Da; Ach
R= alpha, Beta, D, nAchR, mAchR
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4
Q

Cholinergic - think?

A

acetyl choline

muscarinic and nicotinic receptors

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5
Q

adrenergic think?

A

norepinephrine
epinephrine
dopamine

alpha, beta, D receptors
from tyrosine

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6
Q

major NT of the parasymp system

A

Ach

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7
Q

found at ALL PREganglionic autonomic fibers

A

Ach

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8
Q

found at ALL POST ganglionic parasympathetic fibers

A

Ach

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9
Q

found at a few POSTgaglionic sympathetic fibers (WHERE?)

A

Ach

sweat glands

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10
Q

major NT of the sympathetic nervous system

A

NE

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11
Q

found at a vast majority of postganglionic sympathetic fibers

A

NE

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12
Q

synthesis occurs in adrenal medulla and a few neuronal pathways in brainstem

A

EPI

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13
Q

Synthesized in the cytoplasm of neurons

A

Dopamine

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14
Q

Dopamine has actions where?

A

in the CNS and renal vascular smooth muscle

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15
Q

Neurons that release Ach are called

A

cholinergic neurons

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16
Q

Order of steps in cholinergic neurotransmission

A 
Synthesis 
storage
release 
binding 
termination
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17
Q

Synthesis of Ach

A

CHOLINE TRANSPORTER transports choline into neurons
dependant on cotransport with NA

CHOLINE ACETYLTRANSFERASE (ChAT) conbines acetyl coenxyme A with choline to make Ach

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18
Q

Storage of Ach

A

ATPase dependent Ach vesicular transporter transports Ach into neuronal vesicles.

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19
Q

Release of Ach

A

AP reaches axon terminal, causes opening of VgCa2+channels
Ca2+enters the neuron
Ca2+ influx promotes fusion of vesicular membrane with cell membrane
Ach is released

the SNARE protein complex is responsible for fusion of the vesicle membrane and synaptic membrane through VAMP and SNAP proteins

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20
Q

Binding of Ach to cholinergic receptors

A

Ach diffuses across the synaptic cleft
binds nachrs which facilitates Na entry into post-gang fiber or release of epi/NE from adrenal medulla
post-synaptic machrs are also activated by ach causing smooth muscle contraction, decrease in HR, glandular secretin etc

Ach can bind to and activate both nachr (+) and machr (-) to modify its own release.

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21
Q

activation of prejunctional nAchRs _________ Ach release

A

stimulates/potentiates

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22
Q

activation of prejunctional machrs ________further release

A

inhibits

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23
Q

Termination of Ach signaling

A

Acetylcholinesterase cleaves Ach into acetate and choline
acetate diffuses out of the synapse
choline is recycled into the nerve

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24
What two types of receptors does Ach bind to?
nAchR | mAchR
25
Where are NnAchrs found
all ganglia (sym and parasymp) and adrenal medulla (symp)
26
where are mAChrs found
smooth and cardiac muscle gland cells nerve terminals
27
nAchR is what type of a channel
ionotropic (ligand gated ion channel)
28
nAchR allows what to pass through the channel
Na
29
mAchR is what type of receptor
metabotrpoic, GPCR
30
how many subtypes of muscarinic receptors are there
5
31
what are the predominant smooth muscle muscarinic receptors
M2 and M3
32
what is the predominant muscarinic receptor in cardiac muscle
M2
33
adrenergic transmission, think
catecholamines | NE, E, Da
34
principle NT of most of sympathetic post ganglionic fibers and ov certain tracts in CNS
NE
35
major hormone/NT released by adrenal medulla
epi
36
predominant NT of mammalian extrapyramidal system and several mesocortical and mesolimbic neuronal pathways
Dopamine
37
Steps of catecholamine signalling
``` synthesis storage release binding termination ```
38
Synthesis of catecholamines
tyrosine transported into nerve terminal by a Na dependent transporter trosine--> DOPA->Dopamine->NE->Epi final step occurs only in the adrenal medulla and in a few epi containing neuonal pathways in the brainstem
39
Storage of catecholamines
vesicular monoamine transporter (VMAT-2) transports Da into the vesicle promiscuous, can also transport NE, epi, and seratonin across the vesicle membrane
40
reserpine
inhibits VMAT-2, leads to depletion of catecholamines from sympathetic nerve endings.
41
Release of catecholamines
similar to release of Ach after depolarization and influx of Ca2+. in adrenal medulla, triggering event is release of Ach and its interaction with nAchRs on chromaffin cells to produce localized deppol
42
Binding of catecholamines to adrenergic receptors
diffuse across synaptic cleft and bind to adrenergic alpha and beta receptors effector organ responses include: contraction, glycogenolysis, gluconeogenesis, relaxation and increased force and rate of cardiac muscle contraction
43
Termination of catecholamine signaling (3 ways)
reuptake into nerve terminals dilution by diffusion metabolic transformation
44
major mechanism that terminates the actions of catecholamines
reuptake
45
reuptake of catecholamines
by two neuronal membrane transporters NET and DAT (NE transporter and DA transporter)
46
Dilution by diffusion of catecholamines
diffuseion out of the junctional cleft and uptake ate extraneuronal sites by transporters ENT/ OCT1 and OCT2)
47
Metabolic transformation of catecholamines occurs through what enzymes?
MAO | COMT
48
examples of common sympathetic cotransmitters
ATP, | NPY
49
feedback on prejunctional receptors to inhibit release of each other
NE, NPY, ATP | sympathetics
50
examples of receptors on sympathetic nerve varicosities that also inhibit the release of sympathetic NTs include
M2 and M4, serotonin, PGE2, histamine, enkephalin, DA, and alpha 2
51
examples of receptors on sympathetic nerve varicosities that enhance sympathetic NT release
Beta 2, ang II, nAchR
52
How many subtypes of alpha adrenergic receptors are there?
2 - alpha1 and alpha2
53
THE END RESULT OF ALPHA-1 RECEPTOR ACTIVATION IS
muscle contraction
54
smooth muscle contraction results in ______ cardiac muscle contraction leads to ________ (alpha-1)
vasoconstriction | increase in contractile force on the heart
55
exception to alpha-1 rule
gut activation of alpha 1 receptors and subsequent increas in Ca2+ causes hyperpolarization and muscle relaxation by activation of Ca2+ dependent K+channels
56
ACTIVATION OF ALPHA-2 RESULTS IN
vascular smooth muscle contraction, decreased insulin secretion adna a decreased release of NE (presynaptic alpha-2 receptors)
57
how many subtypes of Beta adrenergic receptors are there
three | B1, B2, B3
58
All B receptors are _____coupled receptors
Gs coupled
59
B1 receptors are found mainly
myocardium
60
ACTIVATION OF BETA-1 RECEPTORS RESULTS IN
increased force and rate of heart contraction and AV nodal conduction velocity
61
B2 receptors are mainly found
smooth muscle and most other sites
62
BETA 2 RECEPTOR ACTIVATION CAUSES
RELAXATION of | vascular, broncial, GU and GI smooth muscle
63
Beta 3 receptors are found
adipose tissue
64
ACTIVATION OF BETA 3 RECEPTORS RESULTS IN
lipolysis
65
triad of symptoms for pheochromocytoma
headache, perspiration, palpitations
66
alpha 1 receptors are found primarily
on sm m surrounding the vasculature
67
alpha 2 receptor primary location is
presynaptic in brain, leading to a decrease in sympathetic outflow
68
alpha 1 receptors are _____coupled
Gq
69
alpha 2 receptors are _____ coupled
Gi, Go
70
``` Primary tissue locations of adrenergic receptor subtypes a1 a2 b1 b2 b3 ```
a1 - postjunctional smooth muscle (contraction a2 - presynaptic neurons, postynaptic tissues and blood platelets - (ocular, adipose, intestinal, hepatic, renal, endocrine) b1 - heart (stimulation) b2 - bronchial, uterine, and vascular smooth muscle (relaxation) b3 - adipose tissue (lipolysis)
71
centrally acting a2 think....
decrease in sympathetic outflow | decrease in sympathetic tone
72
muscarinic think....
increase body fluids
73
how do B2 and mAchR act on sm m surrounding organs
B2=relax | mAchR= contract
74
What type of receptor is the Dopamine receptor
GPCR
75
how many types of DA receptors are there
five
76
DA activates the D1 receptors in _______ whcich increases_____ and causes _____
renal sm. m CAMP dilation
77
stimulation of the D1 receptor will result in
vasodilation, natriuresis and diuresis (via renal vascular smooth muscle)
78
At higher concentrations DA can activate _____ and ____ receptors to cause ______ and _______
alpha 1 beta 1 general vascular vasoconstriction increase in HR
79
decreased sweating cause
increased temperature
80
Smooth muscle of blood vessels is innervated by
sympathetic neurons | NOT parasympathetic neruons
81
how does vascular relaxation happen
need an intact epithelium stumuli - Ach, physical stimuli, and vasoactive products of inflammation and platelet aggregation (bradykinin, histamine, serotonin, purines, thrombin) endothelial cells release nitric oxide, which acts on sm m cells causes vasodilation Ach activates a mAchr in this scenario
82
three exceptions of mAchRs causing contraction
intestines urinary bladder vasculature
83
Baroreceptor reflex
need to add slides for this section but i dont GAFRN
84
Rule of thumb - Alpha 1
stimulate contraction of all smooth muscle | vascular sm m= vasoconstriction; glandular sm m= secretion
85
Rule of thumb - Beta2
relax smooth muscle | vascular sm m - vasodilation
86
Rule of thumb - muscarinic receptors
contract smooth muscle
87
Increase BP causes ______ baroreceptor firing leading to ______
increased decrease in sympathetic output increase in parasympathetic output
88
decreased BP leads to_______baroreceptor firing, resulting in _______
decreased increase sympathetic discharge decrease parasympathetic discharge
89
ordinary pressor doses of NE in a normal subject produce
increase in peripheral vascular resistance, increase in MAP and slowing of the heart rate (compensatory response from reflexes)

Neuro I (30 decks)

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