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Pharm Exam 3 > 5 - Adrenergic Agonists > Flashcards

5 - Adrenergic Agonists Flashcards

1
Q

Direct acting adrenergic receptor agonists

A

DA

NE

Epi

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2
Q

Dopamine to NE

A

DOPA B hydroxylase

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3
Q

Structural differene between Epi and NE

A

Terminal NH2 on epi contains a methyl group

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4
Q

NE vs Epi selectivity

A

Epi = non-selective

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5
Q

______ drugs have not yet been marketed

A

receptor-subtype-specific

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6
Q

Direct acting α1 recepor agonists

A

Phenylephrine

Methoxamine

Oxymetazoline

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7
Q

Oxymetazoline

A

(visine)

Direct α1 agonist

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8
Q

Direct α1 agonists act via what MOA

A

Gq –> PLC –> PIP2

>> Ca++ increase / PK-C activation

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9
Q

α1 agonists promote _____

A

mydriasis

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10
Q

β1 receptors are important in what two functions

A

Cardio (ino/chrono)

Renin

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11
Q

Direct acting α2 receptor agonists

A

Clonidine

Methyldopa

Guanabenz

Guanfacine

Tizanidine

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12
Q

α2 agonists act via what MOA

A

Gi -> ↓ Adenylate cyclase -> ↓cAMP

↓ cAMP-dependent kinase activity

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13
Q

Clonidine does not _____

Uses?

A

decrease renal blood flow

Hypertensive urgency, ADHD, tourette

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14
Q

Direct acting non-selective B recepor agonists

A

Isoproterenol

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15
Q

B1 selective agonists

A

Dobutamine

Dopamine

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16
Q

B2 selective agonists

A

Terbutaline

Metaproterenol

Albuterol

Salmeterol

Ritodrine

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17
Q

Direct acting B receptor agonists MOA

A

Gs –> ↑Adenylate Cyclase –> ↑cAMP –>

↑ cAMP-dependent protein kinase

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18
Q

Explain EC50

A

The concentration needed in order to give 50% response response

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19
Q

Receptor activation comparison for a1 receptors

A

PENI

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20
Q

Receptor activation comparison for B1 and B2 receptor (agonists)

A

I, E, N, P

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21
Q

NE displays less activation of which of the B receptors

A

B2

(activation/concentraiton curve shifted to RIGHT)

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22
Q

Cardiovascular effects of sympathomimetics (Pulse rate)

A

NE = decrease

Epi and Iso = increase

(Isoproterenol > Epi)

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23
Q

Cardiovascular (BP) effects of sympathomimetics

A

NE = Increase

Epi = Basically no change

Iso = reduce

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24
Q

Cardiovascular (peripheral resistance) effects of sympathomimetics

A

NE = Large increase

Epi = Slight decrease

Iso = Large decrease

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25
Q

Isoproterenol has effects on both ____

A

B1 and B2

= Direct stimulation of the heart

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26
Q

Phenylephrine cardiovascular effects

A

Increased BP (vasoconstriction)

Reduced HR (↑ vagal tone -> ↑ baroreceptor)

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27
Q

Phenylephrine CV effects are similar to…

A

NE

Increase BP by vasoconstriction

decrease heart rate via baroreceptor stimulation of vagal tone

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28
Q

Epinephrine CV effects

A

a1 vasoconstriction & B2 vasodilation cancel each other out

= NO change in BP

B1 = ↑HR

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29
Q

Isoproterenol CV effects

A

Reduced BP – Vasodilation (B2)

Increased HR – B1 (also baroreceptor)

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30
Q

L norepinephrine:

  • receptor
  • Metabolism
  • Use?
A

Potent α and β1 receptor agonist

Substrate for MAO and COMT

Used as pressor

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31
Q

Epi:

  • Metabolism
  • Use
A

Substrate for COMT and MAO

Anaphylaxis and Glaucoma

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32
Q

_________ is used in preparations to prevent oxidation of _____ and _________

A

Sodium bisulfite

L-Norepi and Epi

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33
Q

Phenylephrine receptor

A

a1

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34
Q

Phenylephrine metabolism

A

Substrate for MAO

(not for COMT because missing the OH group)

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35
Q

2 aralkylimidazolines compounds

A

Naphazoline

Tetrahydrozoline

Oxymetazoline

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36
Q

2-aralkylimidazolines receptor

A

a1 - PARTIAL agonists

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37
Q

2-aralkylimidazolines use

A

local/topical vasoconstriction (nasal/ophth. decongestants)

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38
Q

2-aralkylimidazolines chemistry

A

basic imidazoline ring causes them to exist in ionized form at physiologic pH

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39
Q

a2 receptor locations

A

CV control center (solitary tract in medulla)

40
Q

Clonidine receptor

A

Selective a2 agonist

41
Q

Function of dichlorophenyl group in clonidine

A

decreases the basicity of the guanidine group

42
Q

Clincal use for clonidine

A

HTN

Opiate withdrawal

*especially for refractory patients

43
Q

a2 agonist general MOA

general effects?

A

reduce Sy output from brain –> reduce BP

REDUCE: HR, inotropy, Renin, vasoconstriction

44
Q

“Open ring” imidazolidines (compounds)

receptor?

A

Guanabenz

Guanafacine

a2 receptor agonists

45
Q

Guanabenz/Guanfacine : Function of two-atom bridge to guanine group

A

dereases pKa

(drug is mostly non-ionized at physiological pH)

46
Q

Shortest half life imidazolidine

A

Guanabenz (6h)

47
Q

Use for Guanabenz / Guanfacine

A

HTN and ADHD

48
Q

Guanfacine may affect…

A

a2 receptors outside the CV control center in medulla

49
Q

Methyldopa receptor

A

a2 agonist

50
Q

Methyldopa is a…

A

prodrug

metabolized to active agonist =

(1R, 2S) -a-MethylNorepinephrine

51
Q

Methyldopa acts at…

A

central a2 receptors to decrease sympathetic outflow

52
Q

Parenteral solution of methyldopa

A

Methyldopate (water soluble ester)

53
Q

Methyldopa clinical use

54
Q

Enzymes involved in Methyldopa metabolism to 1R,2S MethylNE

A
  1. L-aromatic amino acid-Decarboxylase
  2. Dopamine B-hydroxylase
55
Q

Other uses for a2 agonists

A

Apraclonidine = glaucoma

Tizanidine = muscle spasticity

56
Q

Adverse effects of a2 agonists

A

Sedation

Na/Water retention

Dry mouth

Withdrawal Symptoms

57
Q

Co-treatment for a2 agonists

A

diuretics, to reduce water retention

58
Q

a2 receptors are also present in…

A

the spinal cord (reflexes)

Dampening the a2R will reduce muscle spasiticty

59
Q

Nonselective B agonists

A

Isoproterenol

60
Q

Isoproterenol effects

A

Bronchodilation

Increased CO

(nonsel. activation of B receptors)

61
Q

Isoproterenol metabolism

A

metabolized by conjugation reactions (Phase 2)

and by COMT

(not sensitive to MAO)

62
Q

What causes B selectivity for isoproterenol?

A

Putting a larger group on the terminal amine

63
Q

Isoproterenol use

A

Asthma + COPD

Cardiostimulant

64
Q

Selective B2 agonists

A

Metaproterenol, Terbutaline

Albuteral/Levalbuterol, Salmeterol

Salmeterol, Formoterol

65
Q

Metaproterenol and Terbutaline are derivatives of

A

Resorcinol

66
Q

Albuterol and Salmeterol are derivatives of

A

Meta hydroxymethyl

67
Q

____ are only obsserved at higher doses of Resorcinol and meta hydroxymethyl derivatives

A

Cardiac effects

68
Q

Metaproterenol and Terbutaline metabolism

A

not metabolized by MAO or COMT

= longer duration of action than isoproterenol

69
Q

Metaproterenol and Terbutaline use

A

Asthma/COPD

Terbutaline = tocolytic (prevent premature labor)

70
Q

Albuterol and salmeterol metabolism and use

A

neither MAO nor COMT

Asthma / COPD

71
Q

Racemic mixtures

A

Albuterol + Salmeterol

Dobutamine

72
Q

More potent isomer for second gen B2 receptor agonists

A

Levalbuterol

R group = C(CH3)3

73
Q

3rd gen B2 agonists are all _______

A

Very long acting

(No metabolism by COMT/MAO….12-24 hour duration)

74
Q

What is the main issue with 3rd gen B2 agonists

A

Long onset of action

Salmeterol = 10-20 Minutes

Formoterol = Less than 5 minutes

75
Q

3rd gen B2 agents

A

Salmeterol and Formoterol

76
Q

Salmeterol and Formoterol use

A

Long term Asthma

COPD

*NOT acute/rescue inhaler

77
Q

Direct acting beta agonist with mixed properties

A

Dobutamine

78
Q

Dobutamine is a derivative of

79
Q

Dobutamine racemic mixture and receptor

A

(+) = potent B1 agonist, a1 antagonist

(-) = a1 agonist, B1 potency reduced 10x

80
Q

Net effect of dobutamine enantiomers

A

Positive inotropy

Little/no chronotropic

81
Q

Dobutamine metbolism

A

COMT and conjugation

Not sensitive to MAO

82
Q

Dobutamine PK

A

Short half life!

(2 minutes)

83
Q

Dobutamine use

A

Acute HF

Shock

84
Q

Indirect acting sympathomimetics

A
  • Amphetamine
  • Pseudoephedrine
  • Ephedrine
  • Phenylpropanolamine
  • Tyramine
85
Q

Amphetamine mechanism of action

A
  • Competitive blocking of NET-mediated uptake (also includes DAT for dopamine) ** reverse action of plasma membran transporter**
  • Release of NT via VMAT

*both increase the amount of NE in synapse

86
Q

Clincal use for amphetamines

A

ADHD, narcolepsy, anorexiant

87
Q

Other uses for amphetamines

A

nasal decongestants

88
Q

Derivatives of ephedra

A

D-(-)-ephedrine

L-(-)-pseudoephedrine

89
Q

D-(-)-ephedrine has desired…

A

R-configuration at the beta OH

S-configuration ata the alpha carbon

= DIrect agonist activity of adrenergics!

90
Q

L-(-)-pseudoephedrine configuration

A

S,S distereoisomer

the S configuration of B-OH reduces its agonist activity

91
Q

Major mechanism of L-(-)-pseudoephedrine

A

Reversal of the transporter

92
Q

Structural difference between the ephedrine and pseudoephedrine

A

The configuration of the OH group on the beta carbon

93
Q

L-(-)-pseudoephedrine doesn’t have…

A

CNS penetration

d/t OH group S configuration

94
Q

Synthesis of methamphetamine

A

ephedrine — (lithium + NH4+) –>methamphetamine

95
Q

ephedrine and pseudo cause ____ via the ___ receptor

A

vascular constriction

a1 receptor

Pharm Exam 3 (11 decks)

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