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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
Q

Norepinephrine fight or flight response

A

Increase HR and BP
Peripheral Vasoconstriction

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26
Q

Epinephrine fight or flight response

A

Increase HR and BP
Peripheral Vasoconstriction
Increase Lipid Breakdown
Coronary/Bronchial Dilation
Glycogen –> Glucose

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27
Q

Adrenergic signaling in the EYE

A

Alpha1 - contraction of iris radial muscle causing mydriasis
Beta - increase aqueous humor production

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28
Q

Adrenergic signaling in the HEART

A

Beta1 - increased heart rate and contractility

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29
Q

Adrenergic signaling in the BLOOD VESSELS

A

Alpha1 - vasoconstriction
Beta2- vasodilation
Overall effect is vasoconstriction

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30
Q

Adrenergic signaling in the LUNGS

A

Beta2- relaxation of bronchial smooth muscle leading to bronchodilation

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31
Q

Adrenergic signaling in the GI

A

Decrease digestion and secretions

32
Q

Adrenergic signaling in the BLADDER

A

Beta2.3 - detrusor muscle relaxation
Alpha1 - urinary sphincter and prostate contraction
Overall effect is inhibition of urination

33
Q

Adrenergic signaling in the APOCRINE SWEAT GLAND

A

Increased secretion (sweating)

34
Q

Adrenergic signaling in the MISC. METABOLIC FUNCTIONS

A

Gluconeogenesis, glycogenolysis
Lipolysis
Renin release

35
Q

Adrenergic signaling effects

A

Increase alertness/promotes wakefulness
Reduce pain perception
Focus attention

36
Q

Beta Blockers

A

Reduce adrenergic signaling in brain and cause fatigue and decreased alertness

37
Q

Locus Coeruleus

A

Produces much of norepinephrine
Important in formation of emotional memories

38
Q

Alpha1 Affinity for Catecholamine

39
Q

Alpha2 Affinity for Catecholamine

40
Q

Beta1 Affinity for Catecholamine

41
Q

Beta2 Affinity for Catecholamine

A

E&raquo_space; NE

42
Q

Alpha1 Binding Effects

A

Vasoconstriction
Increased blood flow
Increased blood pressure
Mydriasis
Increased closed bladder sphincters

43
Q

Alpha2 Binding Effects

A

Inhibits NE, acetylcholine, and insulin release

44
Q

Beta1 Binding Effects

A

Increased HR, lipolysis, myocardial contractility, and renin

45
Q

Beta2 Binding Effects

A

Vasodilation
Decreased blood flow
Bronchodilation
Increased Gylcogenolysis and glucagon release
Relaxes uterine smooth muscle

46
Q

Blood Pressure

A

BP = cardiac output x peripheral vascular resistance

47
Q

Activation of SNS

A

Increases blood pressure

48
Q

Activation of Alpha1 Receptors

A

Vasoconstriction

49
Q

Activation of Beta2 Receptors

A

Vasodilation

50
Q

Activation of Beta1 Receptors on Heart

A

Increased heart rate and heart contractility

51
Q

Activation of Beta1 Receptors on Kidneys

A

Increase renin release

52
Q

Beta3 Agonists

A

Reduce urination
Used in treatment of overactive bladder

53
Q

Alpha1 Antagonists

A

Vasodilation - treats hypertension
Prostate muscle relaxation - treats benign prostatic hyperplasia

54
Q

Beta2 Agonists

A

Bronchodilation - treats asthma and COPD

55
Q

Beta Blocker Treatment

A

Treats heart failure, hypertension, tachycardias, arrythmias, glaucoma

56
Q

Sympathomimetics

A

Enhance adrenergic signaling

57
Q

Direct Acting

A

Act as agonist at alpha/beta receptors

58
Q

Indirect Acting

A

Increase adrenergic signaling without directly activating receptors

59
Q

Indirect Acting Mechanisms

A

Inhibition of NET
VMAT inhibition leading to reverse transport of NET
Inhibition of metabolizing enzymes

60
Q

Catecholamine Structure

A

Catechol ring and amine-containing side chain

61
Q

Receptor Affinity

A

Affinity for adrenergic receptors is reduced when lacking aromatic ring and beta -OH groups

62
Q

Phenylephrine

A

Alpha receptor agonist
Low affinity for receptors

63
Q

Amphetamine

A

Indirect sympathomimetic
Lacks aromatic and beta OH groups
Does not bind to alpha or beta

64
Q

Dopamine

A

Actives adrenergic receptors
Low affinity
Lack of beta OH group

65
Q

Alpha Receptor Selectivity

A

Absence of 4-OH group decreases binding to beta receptors

66
Q

Beta Receptor Selectivity

A

Larger alkyl chains on amine group increases selectivity

67
Q

SARs COMT

A

Adds methyl group to 3-OH

68
Q

SARs MAO

A

Oxidizes alpha-carbon leading to removal of amine group

69
Q

Isoproterenol

A

Beta receptor selective agonist based on presence of isopropyl group

70
Q

Drugs Lacking 3-OH Group

A

Not susceptible to COMT metabolism
Increases oral bioavailability and drug half life

71
Q

Alpha Carbon Functional Groups

A

Provide steric hinderance against monoamine oxidase
Increases oral bioavailability and drug half life

72
Q

Hydrophilicity

A

Lacking hydroxyl group = more lipophilic
Cross membranes easier and improved oral bioavailability

73
Q

Antiadrenergic

A

Decrease adrenergic signaling
Most are direct acting

74
Q

Metyrosine

A

Blocks tyrosine hydroxylase
Reduces synthesis of dopamine, norepinephrine, epinephrine
Used in treatment pf pheochromocytoma (adrenal tumor)

75
Q

Beta Blocker Structure

A

One aromatic ring and one amine group

76
Q

Alpha Blocker Structure

A

One aromatic ring and one amine group

Pharmacology (18 decks)

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