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Pharm Block 1 > Adrenergics: Catecholamines > Flashcards

Adrenergics: Catecholamines Flashcards

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1
Q

Causes peripheral excitatory action on certain types of smooth muscle (blood vessels, radial
muscle) and on glands (salivary and sweat)

A

Catecholamines

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2
Q

Drug with peripheral inhibitor action on certain types of smooth muscle (wall of gut, bronchial
tree, blood vessels supplying skeletal muscle)

A

Catecholamines

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3
Q

Causes cardiac excitatory action that increases heart rate and force of contraction

A

Catecholamines

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4
Q

Catecholamine has metabolic actions: ______ glycogenolysis (liver and muscle) and liberation of ________

A

Increase

FFAs

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5
Q

Catecholamine’s action: endocrine actions: modulate the secretion of ______ and ______

A

insulin DECREASE

renin INCREASE

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6
Q

Catecholamine actions in the CNS: respiratory ______, _______ in wakefulness and
psychomotor activity, _______ in appetite

A

stimulation
increase
reduction

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7
Q

Catecholamines have prejunctional actions that either inhibit or facilitate the release of neurotransmitters, the _____ action being most important

A

inhibitor

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8
Q

Catecholamines and adrenergic agonists are

A

sympathomimetics

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9
Q

drugs mimic the effects of transmitter substances of the sympathetic nervous system

A

Sympathomimetic

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10
Q

How do sympathomimetic drugs work?

A

These drugs act at the postganglionic sympathetic terminal,[1] either directly activating postsynaptic receptors, blocking breakdown and reuptake, or stimulating production and release of catecholamines.

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11
Q

Adrenergic antagonists are an example of

A

(sympatholytics)

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12
Q

Adrenergic antagonists: most are _______ antagonists (exception is phenoxybenzamine)

A

competitive

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13
Q

How is it possible for adrenergic anatagonists to interfere selectively with responses that result from sympathetic stimulation

A

compounds have been developed with different affinities for the various receptors

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14
Q

Adrenergic receptor subtype:

α1 located in the Eye does

A

Contraction of the radial muscle of the iris (mydriasis)

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15
Q

Adrenergic receptor subtype:

α1 located in the arteries and veins does

A

constriction

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16
Q

Adrenergic receptor subtype:

α1 located in the GU smooth muscle for male does

A

constriction

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17
Q

Adrenergic receptor subtype:

α2 located in Pre-synaptic nerve

A

causes Inhibition of transmitter release terminals

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18
Q

Adrenergic receptor subtype:

α2 located in CNS causes

A

Inhibition of sympathetic outflow

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19
Q

Adrenergic receptor subtype:

β1 located in Heart causes

A

Increased rate and force of contraction &

Increased A-V conduction velocity

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20
Q

Adrenergic receptor subtype:

β1 located in Kidney causes

A

Renin release

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21
Q

Adrenergic receptor subtype:

β2 located in Arteries (skeletal muscle)

A

Dialation

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22
Q

Adrenergic receptor subtype:

β2 located in Bronchi

A

Dialation

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23
Q

Adrenergic receptor subtype:

β2 located in skeletal muscle

A

Glycogenolysis

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24
Q

Adrenergic receptor subtype:

β2 located in liver

A

Glycogenolysis, gluconeogenesis

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25
Adrenergic receptor subtype: Dopamine1 | located in the Kidney causes
Dilation of kidney vasculature
26
Adrenergic Agonists: | Substitution of OH groups at the __ and __ position of aromatic ring is necessary for maximal α and β activity
3 and 4
27
Adrenergic Agonists: | Presence of 2 carbon atoms between ______ and ______the affords the greatest sympathomimetic activity.
aromatic ring and amino group
28
Adrenergic Agonists: | Substitution of alkyl groups on the amino group tend to ↑ ______ (i.e., isoproterenol).
β activity
29
Adrenergic Agonists: | phenylephrine is an
α1 agonist
30
Adrenergic Agonists: What increases the oral effectiveness and duration of action of many compounds especially those with an α-CH3 group (i.e. amphetamine)
Absence of one or both OH groups (especially the 3-OH)
31
Adrenergic Agonists: | What makes the compound more resistant to MAO (i.e., amphetamine).
Substitution on the α carbon
32
``` Adrenergic Agonist Substitution of OH on β-carbon will cause what changes: lipid solubility CNS action peripheral alph and beta activity ```
↓ lipid solubility ↓ CNS action but ↑ peripheral α and β activity.
33
Norepinephrine (Levophed®) is what type of NT
- sympathetic neurotransmitter
34
Norepinephrine Receptor selectivity for
α1, α2, β1
35
Nepi has CV effect through which receptor?
Cardiovascular effects - α1 mainly
36
Nepi causes peripheral _______ which results in ______ peripheral vascular resistance
vasoconstiction | increased
37
Nepi will ______ BP and cause reflex ______
increase BP | reflex bradycardia
38
In IC situations, you could use Nepi as:
used as a vasoconstrictor under certain intensive care situations (i.e., shock)
39
If you have reduced sympathetic tone d/t neurological injury or during use of spinal anesthesia, Nepi could be used to...
elevate BP
40
Epinephrine is naturally occurring, synthesized in ?
adrenal medulla
41
What receptors is epinephrine selective for?
Receptor selectivity - α1, α2, β1, β2
42
Epinephrine CV effects: _____heart rate, contractile force, cardiac output
increase
43
Epinephrine CV effects: | ________ systolic, _______ diastolic blood pressure
increase/decrease
44
CV effects of Epi:(dose-dependent) | Causes ______of most vascular beds and ______of skeletal muscle blood vessels (dose-dependent
constriction | dialation
45
Nepi has a net effect to ______ peripheral vascular resistance
decrease
46
In the Respiratory system Epi causes
Bronchodilation
47
Epi causes Hyperglycemia by:
stimulating gluconeogenesis and glycogenolysis; inhibits insulin release
48
Epi causes Lipolysis in order to:
increase free fatty acids
49
Therapeutic use of ______ for | Rapid relief of hypersensitivity reactions to drugs and other allergens
Therapeutic uses of Epi
50
This drug is Co-administered with local anesthetics to increase duration of action
Epinephrine
51
In pts w/ Bradyarrhythmias, Epi can be used to
– restore rhythm in patients with cardiac arrest
52
What are some ophthalmic uses for Epi
mydriatic, decrease hemorrhage, conjunctival decongestion
53
Isoproterenol (Isuprel®) | Receptor selectivity
β1, β2
54
Cardiovascular effects of Isoproterenol | _______ peripheral resistance
Decrease
55
Cardiovascular effects of Isoproterenol | ________heart rate, contractile force, CO
increase
56
Cardiovascular effects of Isoproterenol | _____ mean blood pressure
Decrease
57
Respiratory effects of Isoproterenol
Bronchodialation
58
In emergencies use this drug to stimulate heart rate during bradycardia or heart block
Isoproterenol
59
Dopamine (Intropin®) synthesis is:
- naturally occurring NT
60
Receptor selectivity of dopamine
- DA1, β1, α1
61
Cardiovascular effects of Dopamine | Low dose causes______ of renal and mesenteric arteries
vasodilation
62
Cardiovascular effects of Dopamine | Low dose causes ________ peripheral resistance through this receptor
decrease via DA1 receptor
63
CV effects of Dopamine: medium dose | _______ heart rate, contractile force, cardiac output via ______
Increase | β1
64
CV effects of dopamine: high dose | vasoconstriction/vasodialation and ______ peripheral resistance (α1)
vasoconcstriction increase (α1)
65
When you have severe decompensated heart failure, shock (cardiogenic; septic) what drug would you use?
Dopamine
66
Dobutamine (Dobutrex®) is a
- synthetic catecholamine
67
Receptor selectivity for dobutamine | - (-) dobutamine
– α1 agonist & β agonist
68
Receptor selectivity for dobutamine | - (+) dobutamine
– α1 antagonist & β agonist
69
What is the overal effect of a racemic mixture of dobutamine?
β1 agonist
70
Cardiovascular effects of Dobutamine | _____ cardiac rate, contractility and output
Increased
71
CV effects of Dobutamine: | Minimal change in
peripheral resist & blood pressure
72
What drug would you prescribe for short-term treatment of cardiac decompensation (surgery, CHF, MI)
Dobutamine
73
What drug is used for cardiac stress testing
Dobutamine
74
Methyldopa (Aldomet®) is metabolized in
adrenergic nerve terminals in CNS
75
What is Methyldopa broken down into?
α-methyldopamine and α-methylnorepinephrine, which are stored in nerve terminals and released with stimulation
76
What is the significance of α-methyldopamine and α-methylnorepinephrine in regards to α2 receptor and central α2 receptors
potent α2 receptor agonists; stimulate central α2 receptors to reduce sympathetic outflow
77
CV action of methyldopa: | _____ peripheral resistance, heart rate, and cardiac output
Decrease
78
Major therapeutic use of Methyldopa?
anti-hypertensive
79
What side effects would one experience with sudden discontinuance of Methyldopa?
sedation, dry mouth, edema, rebound hypertension

Pharm Block 1 (23 decks)

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