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Pharmacology > Adrenergic Drugs (Exam 1) > Flashcards

Adrenergic Drugs (Exam 1) Flashcards

1
Q

Adrenergic Neurotransmitters

A

Norepinephrine and Epinephrine

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2
Q

Adrenergic postganlionic neurons primarily release…

A

norepinephrine

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3
Q

Adrenal medulla primarily releases…

A

epinephrine
80% E and 20% NE

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4
Q

Tyrosine

A

Synthesizes norepinephrine and epinephrine

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5
Q

How does tyrosine synthesize NE and E?

A

Tyrosine –> L-DOPA –> dopamine –> norepinephrine –> epinephrine

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6
Q

Tyrosine hydroxylase (TH)

A

Rate-limiting enzyme that converts tyrosine into DOPA

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7
Q

Which neurotransmitter has overlapping affinity for same receptors, transporters, and metabolizing enzymes as NE/E?

A

Dopamine

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8
Q

MAO and COMT enzymes

A

Breakdown NE and E

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9
Q

Vanillylmandelic Acid (VMA)

A

Major metabolite for NE and E

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10
Q

MAO

A

Monoamine Oxidase

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11
Q

COMT

A

Catechol-O-Methytransferase

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12
Q

Vesicular monoamine transporter (VMAT)

A

Responsible for uptake in storage vesicles

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13
Q

Norepinephrine Transporter (NET)

A

Responsible for reuptake into presynaptic terminal

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14
Q

Alpha 2 Receptors

A

Located presynaptically function as autoreceptors

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15
Q

Antagonist at VG Na+ channels

A

Decrease signaling

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16
Q

Antagonist at presynaptic VG Ca2+ channels

A

Decrease signaling

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17
Q

Tyrosine hydroxylase inhibitor

A

Decreases signaling

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18
Q

COMT inhibitor

A

Increases signaling

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19
Q

MAO inhibitor

A

Increases signaling

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20
Q

Antagonist at presynaptic alpha2 receptors

A

Increase signaling

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21
Q

Alpha1 Receptors (A, B, D)

A

Gq

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22
Q

Alpha2 Receptors (A, B, C)

A

Gi

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23
Q

Beta1-3 Receptors

A

Gs

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24
Q

NE and E are responsible for…

A

Fight or flight functions

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25
Norepinephrine fight or flight response
Increase HR and BP Peripheral Vasoconstriction
26
Epinephrine fight or flight response
Increase HR and BP Peripheral Vasoconstriction Increase Lipid Breakdown Coronary/Bronchial Dilation Glycogen --> Glucose
27
Adrenergic signaling in the EYE
Alpha1 - contraction of iris radial muscle causing mydriasis Beta - increase aqueous humor production
28
Adrenergic signaling in the HEART
Beta1 - increased heart rate and contractility
29
Adrenergic signaling in the BLOOD VESSELS
Alpha1 - vasoconstriction Beta2- vasodilation Overall effect is vasoconstriction
30
Adrenergic signaling in the LUNGS
Beta2- relaxation of bronchial smooth muscle leading to bronchodilation
31
Adrenergic signaling in the GI
Decrease digestion and secretions
32
Adrenergic signaling in the BLADDER
Beta2.3 - detrusor muscle relaxation Alpha1 - urinary sphincter and prostate contraction Overall effect is inhibition of urination
33
Adrenergic signaling in the APOCRINE SWEAT GLAND
Increased secretion (sweating)
34
Adrenergic signaling in the MISC. METABOLIC FUNCTIONS
Gluconeogenesis, glycogenolysis Lipolysis Renin release
35
Adrenergic signaling effects
Increase alertness/promotes wakefulness Reduce pain perception Focus attention
36
Beta Blockers
Reduce adrenergic signaling in brain and cause fatigue and decreased alertness
37
Locus Coeruleus
Produces much of norepinephrine Important in formation of emotional memories
38
Alpha1 Affinity for Catecholamine
NE > E
39
Alpha2 Affinity for Catecholamine
E > NE
40
Beta1 Affinity for Catecholamine
E = NE
41
Beta2 Affinity for Catecholamine
E >> NE
42
Alpha1 Binding Effects
Vasoconstriction Increased blood flow Increased blood pressure Mydriasis Increased closed bladder sphincters
43
Alpha2 Binding Effects
Inhibits NE, acetylcholine, and insulin release
44
Beta1 Binding Effects
Increased HR, lipolysis, myocardial contractility, and renin
45
Beta2 Binding Effects
Vasodilation Decreased blood flow Bronchodilation Increased Gylcogenolysis and glucagon release Relaxes uterine smooth muscle
46
Blood Pressure
BP = cardiac output x peripheral vascular resistance
47
Activation of SNS
Increases blood pressure
48
Activation of Alpha1 Receptors
Vasoconstriction
49
Activation of Beta2 Receptors
Vasodilation
50
Activation of Beta1 Receptors on Heart
Increased heart rate and heart contractility
51
Activation of Beta1 Receptors on Kidneys
Increase renin release
52
Beta3 Agonists
Reduce urination Used in treatment of overactive bladder
53
Alpha1 Antagonists
Vasodilation - treats hypertension Prostate muscle relaxation - treats benign prostatic hyperplasia
54
Beta2 Agonists
Bronchodilation - treats asthma and COPD
55
Beta Blocker Treatment
Treats heart failure, hypertension, tachycardias, arrythmias, glaucoma
56
Sympathomimetics
Enhance adrenergic signaling
57
Direct Acting
Act as agonist at alpha/beta receptors
58
Indirect Acting
Increase adrenergic signaling without directly activating receptors
59
Indirect Acting Mechanisms
Inhibition of NET VMAT inhibition leading to reverse transport of NET Inhibition of metabolizing enzymes
60
Catecholamine Structure
Catechol ring and amine-containing side chain
61
Receptor Affinity
Affinity for adrenergic receptors is reduced when lacking aromatic ring and beta -OH groups
62
Phenylephrine
Alpha receptor agonist Low affinity for receptors
63
Amphetamine
Indirect sympathomimetic Lacks aromatic and beta OH groups Does not bind to alpha or beta
64
Dopamine
Actives adrenergic receptors Low affinity Lack of beta OH group
65
Alpha Receptor Selectivity
Absence of 4-OH group decreases binding to beta receptors
66
Beta Receptor Selectivity
Larger alkyl chains on amine group increases selectivity
67
SARs COMT
Adds methyl group to 3-OH
68
SARs MAO
Oxidizes alpha-carbon leading to removal of amine group
69
Isoproterenol
Beta receptor selective agonist based on presence of isopropyl group
70
Drugs Lacking 3-OH Group
Not susceptible to COMT metabolism Increases oral bioavailability and drug half life
71
Alpha Carbon Functional Groups
Provide steric hinderance against monoamine oxidase Increases oral bioavailability and drug half life
72
Hydrophilicity
Lacking hydroxyl group = more lipophilic Cross membranes easier and improved oral bioavailability
73
Antiadrenergic
Decrease adrenergic signaling Most are direct acting
74
Metyrosine
Blocks tyrosine hydroxylase Reduces synthesis of dopamine, norepinephrine, epinephrine Used in treatment pf pheochromocytoma (adrenal tumor)
75
Beta Blocker Structure
One aromatic ring and one amine group
76
Alpha Blocker Structure
One aromatic ring and one amine group

Pharmacology (18 decks)

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