Introduction Into Autonomic Pharmacology Flashcards

(82 cards)

1
Q

Compounds associated with the parasympathetic system?

A

Acetylcholine
Muscarine
Nicotine

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2
Q

Compounds associated with the sympathetic system?

A

Norepinephrine/Noradrenaline

Epinephrine (Adrenaline)

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3
Q

Cholinergic drugs influence….

Adrenergic drugs influence…

A

Parasympathetic

Sympathetic

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4
Q

The receptors of the PANS are named after exogenous agents. What are they

A

Muscarine and Nicotine

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5
Q

Sympathetic preganglionic fibers leave the CNS through which spinal nerves?

A

Thoracic and Lumbar

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6
Q

Parasympathetic preganglionic fibers leave the CNS through which spinal nerves?

A

Cranial Nerves

Sacral

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7
Q

All preganglionic nerves release _____ into post ganglioncic nerves expressing ____ receptors

A

Acetylcholine

Nicotinic Cholinergic Receptors

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8
Q

Somatic motor neurons release _____ directly onto _______ receptors

A

Acetylcholine

Nicotinic cholinergic receptors

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9
Q

Parasympathetic postganglionic nerves release _____ onto organs with _____ receptors

A

Acetylcholine

Muscarinic

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10
Q

Sympathetic postgangionic nerves primarily release _____ that can bind to _____ receptors

A

Norepinephrine

Adrenergic

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11
Q

Sympathetic postganglionic nerves acting on skin release ____ onto _____ receptors

A

Acetylcholine

Muscarinic Receptors of Thermoregulatory Sweat Glands

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12
Q

Sympathetic postganglionic nerves acting on the kidneys release ____ to bind ______ receptors

A

Dopamine

Dopamine D1 to cause vasodilation

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13
Q

Postganglionic sympathetics acting on the adrenals cause….

A

Epi and a little bit of NE release into the bloodstream

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14
Q

Which muscarinic receptors are found postsynaptically?

Presynaptically?

A

Post – 1, 3, 4, 5

Pre – 2, 4

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15
Q

Why have muscarinic receptors presynaptically?

A

Inhibitory autoreceptors

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16
Q

ACh in the synapse is quickly metabolized by ______ and ______

A

Acetylcholinesterase

Butylcholineesterase

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17
Q

ACh metabolism generates…

A

Acetate and Choline

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18
Q

What does ChAT do?

A

Choline AcetylTransferase transfers an acetyl to choline from AcCoA to remake ACh.

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19
Q

ACh is taken back into synaptic vesicles by…

A

Acetylcholine transporter (vAchT)

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20
Q

Sympathetic receptors found post synaptically?

Pre synaptically?

A

Post – alpha1, beta1, beta2

Pre – alpha2, beta2

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21
Q

How is NE made?

A

Tyrosine turned to DOPA by tyrosine hydroxylase
DOPA to Dopamine by Aromatic Acid Decarboxylase
Dopamine to NE by dopamine beta-hydroxylase

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22
Q

After release, NE is returned by ____

A

NET (NorEpinephrine Transporter)

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23
Q

What two fates may occur for NE after its reuptake?

A

MAOs could turn it into dihydroxyphenylglycol

Taken into vesicles by VMAT (vesicular monamine transporter)

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24
Q

Postsynaptically, NE is metabolized by ______ into ______

A

COMT (catechl-0-methyltransferase

Normetanephrine

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25
How do Methylphenidate (Ritalin) and amphetamines (adderall) increase NE/DA release?
Blocking VMAT | Indirect activation of SANS
26
Classification of drugs that mimic acetylcholine? Block acetylcholine?
Parasympathomimetic | Parasympatholytic
27
Classification of drugs that mimic NE? Block NE?
Sympathetomimetic | Sympatholytic
28
Three sites you might look for Nicotinic Cholinergic receptors?
Ganglionic Skeletal Muscle Neronal
29
Nicotinic cholinergic receptors consist of ___ subunits
5
30
Nicotinic cholinergic receptors -- why should be care about their subunits?
The arrangement decides on function and affinity | ex. the pentameric alpha7 homomeric Ach receptor can bind 5 ACh molecules
31
Gq coupled Muscarinic receptors include...
M1, M3, M5
32
Gi coupled Muscarinic receptors include...
M2, M4
33
In PANS, the most important presynaptic muscarinic receptor is _____ and the most important postsynaptic receptors is _____.
M2 | M3
34
M2 is primarily located where?
Heart and Bladder | Also, Certain brain regions
35
Which muscarinic receptors are usually found in the brain?
M1, M4, M5
36
Function of M5 receptors?
Vasodilation of cerebral blood vessels
37
Describe the structure of muscarinic receptors?
GPCRS | 7 transmembrane
38
Effects of M3 activation?
Increases in calcium | Neuronal activation through a PLC mechanism
39
Effects of M2 activation?
Inhibit NT release by activating GIRK and inhibiting VGCC via AC inhibition
40
Adrenergic receptors are invited into ____ subtypes with three isoforms each
alpha1, alpha2, and beta
41
G couplings for alpha1, alpha2, and beta subtypes
Alpha1 -- Gq-coupled Alpha2 -- Gi-coupled beta -- Gs-coupled
42
Which adrenergic receptors are primarily responsible for SANS responses?
alpha1 and beta
43
Where are alpha2 receptors at?
Mostly CNS | also GI tract and pancreas
44
The radial muscles of the iris contain ____ receptors
alpha1 | aka. THE DILATOR
45
The circular muscles of the iris contain _____ receptors
M3 | Cause consriction, Miosis
46
The ciliary muscles contain ___ receptors
M3R
47
Why should we care about the M3R on ciliary muscles?
Contraction changes accommodation | Stretches trabecular meshwork, may reduce open angle glaucoma
48
Beta receptors are also present on the ciliary endothelium. Why?
They increase the secretion of aqueous humor | Blockage for glaucoma treatment
49
Blood Pressure is driven by what two factors
Flow (Q) | Resistance (R)
50
Flow is driven by what two factors
``` Stroke Volume (SV) Heart Rate (HR) ```
51
How can the autonomic nervous system control Bloodpressure?
Control R with Vasodilation/Vasoconstriction Control SV by changing force of contraction Control HR by changing frequency
52
ANS triggered vasoconstriction uses ____ receptors in vascular smooth muscles
alpha1
53
Activation of Beta2 receptors in vessels cause...
Relaxation of the smooth muscle | Vasodilation
54
What vessels are exposed to both alpha and beta stimulation, who wins?
Alpha
55
How are alpha1 and alpha2 receptors in vessel walls activated? What do they do?
Activated by Ep in the blood stream | Cause vasoconstriction
56
What is the significance of non-innervated M3 receptors in the endothelial lining?
They respond to exogenous cholinergic drugs
57
Activation of endothelial M3s causes....
Release of NO Vasodilation by relaxation of the vascular smooth muscle Trumps the vasoconstriction response of smooth muscle M3
58
ANS responses in the heart are primarily mediated by ____ and ____
M2 and beta1
59
The beta receptors in the heart cause...
Increase in HR and force of contraction
60
M2 receptors in the heart cause...
Slowed HR and decreased force of contraction
61
parasympathetic receptors in the lung are mostly ______. They are located on ______.
M3 | Smooth muscle cells and mucosal glands
62
Activation of M3 in the lungs causes...
Bronchoconstriction | Release of Mucous
63
Sympathetic receptors in the lungs are primarily.... and located on.....
beta2 | Smooth muscle cells
64
Activation of beta2 in the lungs causes
Muscle relaxation and Bronchodilation
65
Apocrine sweat glands (stress induced), Piloerection, and erector muscles use....
alpha 1 receptors
66
Where are apocrine sweat glands usually found
Armpits, Genatalia, Palms
67
What receptors are responsible for eccrine (thermoregulatory) sweating?
M3s
68
Parasympathetic and Sympathetic receptor and response. | Salivary Glands.
Both increase secretion -- alpha1, M3
69
Parasympathetic and Sympathetic receptor and response. | Smooth Muscle Sphincters.
``` S = Contraction (alpha1) P = Relaxation (M2) ```
70
Parasympathetic and Sympathetic receptor and response. | Smooth muscle walls
``` S = Relaxation (alpha2, beta2) P = Contraction (M3) ```
71
Parasympathetic and Sympathetic receptor and response. | GI secretions.
``` S = Inhibition (alpha2) P = Increased (M1,M3) ```
72
Parasympathetic and Sympathetic receptor and response. Bladder Wall.
``` S = Relaxation (beta3) P = Contraction (M3) ```
73
Sympathetic receptor and response. Ureter and sphincter.
Contraction (alpha1)
74
Sympathetic receptor and response. Uterus.
Relaxation (beta2) | Contraction (alpha1)
75
Sympathetic receptor and response. Penis
Ejaculation (alpha1)
76
Sympathetic receptor and response. Liver.
Gluconeogenesis, Glycogenolysis (alpha1, beta2)
77
Sympathetic receptor and response. Fat cells.
Lipolysis (alpha1, beta1-3)
78
Sympathetic receptor and response. Kidney.
Increased renin secretion (beta1)
79
Sympathetic receptor and response. Pancreas.
Decreased Insulin release (alpha2)
80
Activation of M3 receptor on the bladder causes...
Contraction of the bladder wall | urge to urinate
81
Beta3 activition on the detrusor wall causes...
relaxation
82
Activation of alpha1 on the urethra causes...
contraction