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Pharm Block 1 > Adrenergics: Catecholamines > Flashcards

Adrenergics: Catecholamines Flashcards

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
Q

Adrenergic receptor subtype: Dopamine1

located in the Kidney causes

A

Dilation of kidney vasculature

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26
Q

Adrenergic Agonists:

Substitution of OH groups at the __ and __ position of aromatic ring is necessary for maximal α and β activity

A

3 and 4

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27
Q

Adrenergic Agonists:

Presence of 2 carbon atoms between ______ and ______the affords the greatest sympathomimetic activity.

A

aromatic ring and amino group

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28
Q

Adrenergic Agonists:

Substitution of alkyl groups on the amino group tend to ↑ ______ (i.e., isoproterenol).

A

β activity

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29
Q

Adrenergic Agonists:

phenylephrine is an

A

α1 agonist

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30
Q

Adrenergic Agonists:
What increases the oral effectiveness and duration of action of many compounds especially those with an α-CH3 group (i.e. amphetamine)

A

Absence of one or both OH groups (especially the 3-OH)

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31
Q

Adrenergic Agonists:

What makes the compound more resistant to MAO (i.e., amphetamine).

A

Substitution on the α carbon

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32
Q 
Adrenergic Agonist
Substitution of OH on β-carbon will cause what changes:
lipid solubility
CNS action
peripheral alph and beta activity
A

↓ lipid solubility
↓ CNS action but
↑ peripheral α and β activity.

33
Q

Norepinephrine (Levophed®) is what type of NT

A
  • sympathetic neurotransmitter
34
Q

Norepinephrine Receptor selectivity for

A

α1, α2, β1

35
Q

Nepi has CV effect through which receptor?

A

Cardiovascular effects - α1 mainly

36
Q

Nepi causes peripheral _______ which results in ______ peripheral vascular resistance

A

vasoconstiction

increased

37
Q

Nepi will ______ BP and cause reflex ______

A

increase BP

reflex bradycardia

38
Q

In IC situations, you could use Nepi as:

A

used as a vasoconstrictor under certain intensive care situations (i.e., shock)

39
Q

If you have reduced sympathetic tone d/t neurological injury or during use of spinal anesthesia, Nepi could be used to…

A

elevate BP

40
Q

Epinephrine is naturally occurring, synthesized in ?

A

adrenal medulla

41
Q

What receptors is epinephrine selective for?

A

Receptor selectivity - α1, α2, β1, β2

42
Q

Epinephrine CV effects:

_____heart rate, contractile force, cardiac output

A

increase

43
Q

Epinephrine CV effects:

________ systolic, _______ diastolic blood pressure

A

increase/decrease

44
Q

CV effects of Epi:(dose-dependent)

Causes ______of most vascular beds and ______of skeletal muscle blood vessels (dose-dependent

A

constriction

dialation

45
Q

Nepi has a net effect to ______ peripheral vascular resistance

A

decrease

46
Q

In the Respiratory system Epi causes

A

Bronchodilation

47
Q

Epi causes Hyperglycemia by:

A

stimulating gluconeogenesis and glycogenolysis; inhibits insulin release

48
Q

Epi causes Lipolysis in order to:

A

increase free fatty acids

49
Q

Therapeutic use of ______ for

Rapid relief of hypersensitivity reactions to drugs and other allergens

A

Therapeutic uses of Epi

50
Q

This drug is Co-administered with local anesthetics to increase duration of action

A

Epinephrine

51
Q

In pts w/ Bradyarrhythmias, Epi can be used to

A

– restore rhythm in patients with cardiac arrest

52
Q

What are some ophthalmic uses for Epi

A

mydriatic, decrease hemorrhage, conjunctival decongestion

53
Q

Isoproterenol (Isuprel®)

Receptor selectivity

A

β1, β2

54
Q

Cardiovascular effects of Isoproterenol

_______ peripheral resistance

A

Decrease

55
Q

Cardiovascular effects of Isoproterenol

________heart rate, contractile force, CO

A

increase

56
Q

Cardiovascular effects of Isoproterenol

_____ mean blood pressure

A

Decrease

57
Q

Respiratory effects of Isoproterenol

A

Bronchodialation

58
Q

In emergencies use this drug to stimulate heart rate during bradycardia or heart block

A

Isoproterenol

59
Q

Dopamine (Intropin®) synthesis is:

A
  • naturally occurring NT
60
Q

Receptor selectivity of dopamine

A
  • DA1, β1, α1
61
Q

Cardiovascular effects of Dopamine

Low dose causes______ of renal and mesenteric arteries

A

vasodilation

62
Q

Cardiovascular effects of Dopamine

Low dose causes ________ peripheral resistance through this receptor

A

decrease via DA1 receptor

63
Q

CV effects of Dopamine: medium dose

_______ heart rate, contractile force, cardiac output via ______

A

Increase

β1

64
Q

CV effects of dopamine: high dose

vasoconstriction/vasodialation and ______ peripheral resistance (α1)

A

vasoconcstriction
increase
(α1)

65
Q

When you have severe decompensated heart failure, shock (cardiogenic; septic) what drug would you use?

A

Dopamine

66
Q

Dobutamine (Dobutrex®) is a

A
  • synthetic catecholamine
67
Q

Receptor selectivity for dobutamine

- (-) dobutamine

A

– α1 agonist & β agonist

68
Q

Receptor selectivity for dobutamine

- (+) dobutamine

A

– α1 antagonist & β agonist

69
Q

What is the overal effect of a racemic mixture of dobutamine?

A

β1 agonist

70
Q

Cardiovascular effects of Dobutamine

_____ cardiac rate, contractility and output

A

Increased

71
Q

CV effects of Dobutamine:

Minimal change in

A

peripheral resist & blood pressure

72
Q

What drug would you prescribe for short-term treatment of cardiac decompensation (surgery, CHF, MI)

A

Dobutamine

73
Q

What drug is used for cardiac stress testing

A

Dobutamine

74
Q

Methyldopa (Aldomet®) is metabolized in

A

adrenergic nerve terminals in CNS

75
Q

What is Methyldopa broken down into?

A

α-methyldopamine and α-methylnorepinephrine, which are stored in nerve terminals and released with stimulation

76
Q

What is the significance of α-methyldopamine and α-methylnorepinephrine in regards to α2 receptor and central α2 receptors

A

potent α2 receptor agonists; stimulate central α2 receptors to reduce sympathetic outflow

77
Q

CV action of methyldopa:

_____ peripheral resistance, heart rate, and cardiac output

A

Decrease

78
Q

Major therapeutic use of Methyldopa?

A

anti-hypertensive

79
Q

What side effects would one experience with sudden discontinuance of Methyldopa?

A

sedation, dry mouth, edema, rebound hypertension

Pharm Block 1 (23 decks)

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