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Pharm Exam 3 > 5 - Adrenergic Agonists > Flashcards

5 - Adrenergic Agonists Flashcards

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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
Isoproterenol has effects on both \_\_\_\_
B1 and B2 = Direct stimulation of the heart
26
Phenylephrine cardiovascular effects
Increased BP (vasoconstriction) Reduced HR (↑ vagal tone -\> ↑ baroreceptor)
27
Phenylephrine CV effects are similar to...
NE Increase BP by vasoconstriction decrease heart rate via baroreceptor stimulation of vagal tone
28
Epinephrine CV effects
a1 vasoconstriction & B2 vasodilation cancel each other out = **NO change in BP** B1 = **↑HR**
29
Isoproterenol CV effects
Reduced BP -- Vasodilation (B2) Increased HR -- B1 (also baroreceptor)
30
L norepinephrine: * receptor * Metabolism * Use?
Potent α and β1 receptor agonist Substrate for MAO and COMT Used as **pressor**
31
Epi: * Metabolism * Use
Substrate for COMT and MAO Anaphylaxis and Glaucoma
32
\_\_\_\_\_\_\_\_\_ is used in preparations to prevent oxidation of _____ and \_\_\_\_\_\_\_\_\_
Sodium bisulfite L-Norepi and Epi
33
Phenylephrine receptor
a1
34
Phenylephrine metabolism
Substrate for MAO (*not* for COMT because missing the OH group)
35
2 aralkylimidazolines compounds
Naphazoline Tetrahydrozoline Oxymetazoline
36
2-aralkylimidazolines receptor
a1 - PARTIAL agonists
37
2-aralkylimidazolines use
local/topical vasoconstriction (nasal/ophth. decongestants)
38
2-aralkylimidazolines chemistry
basic imidazoline ring causes them to _exist in ionized form at physiologic pH_
39
a2 receptor locations
CV control center (solitary tract in medulla)
40
Clonidine receptor
Selective a2 agonist
41
Function of dichlorophenyl group in clonidine
decreases the basicity of the guanidine group
42
Clincal use for clonidine
HTN Opiate withdrawal \*especially for refractory patients
43
a2 agonist general MOA general effects?
reduce Sy output from brain --\> reduce BP REDUCE: HR, inotropy, Renin, vasoconstriction
44
"Open ring" imidazolidines (compounds) receptor?
Guanabenz Guanafacine a2 receptor agonists
45
Guanabenz/Guanfacine : Function of two-atom bridge to guanine group
dereases pKa (drug is mostly non-ionized at physiological pH)
46
Shortest half life imidazolidine
Guanabenz (6h)
47
Use for Guanabenz / Guanfacine
HTN and ADHD
48
Guanfacine may affect...
a2 receptors *outside* the CV control center in medulla
49
Methyldopa receptor
a2 agonist
50
Methyldopa is a...
prodrug metabolized to active agonist = **(1R, 2S) -a-MethylNorepinephrine**
51
Methyldopa acts at...
central a2 receptors to decrease sympathetic outflow
52
Parenteral solution of methyldopa
Methyldopate (water soluble ester)
53
Methyldopa clinical use
HTN
54
Enzymes involved in Methyldopa metabolism to 1R,2S MethylNE
1. L-aromatic amino acid-Decarboxylase 2. Dopamine B-hydroxylase
55
Other uses for a2 agonists
Apraclonidine = glaucoma Tizanidine = muscle spasticity
56
Adverse effects of a2 agonists
Sedation Na/Water retention Dry mouth Withdrawal Symptoms
57
Co-treatment for a2 agonists
diuretics, to reduce water retention
58
a2 receptors are also present in...
the spinal cord (reflexes) Dampening the a2R will reduce muscle spasiticty
59
Nonselective B agonists
Isoproterenol
60
Isoproterenol effects
Bronchodilation Increased CO (nonsel. activation of B receptors)
61
Isoproterenol metabolism
metabolized by conjugation reactions (Phase 2) and by COMT (*not sensitive to MAO*)
62
What causes B selectivity for isoproterenol?
Putting a larger group on the terminal amine
63
Isoproterenol use
Asthma + COPD Cardiostimulant
64
Selective B2 agonists
Metaproterenol, Terbutaline Albuteral/Levalbuterol, Salmeterol Salmeterol, Formoterol
65
Metaproterenol and Terbutaline are derivatives of
Resorcinol
66
Albuterol and Salmeterol are derivatives of
Meta hydroxymethyl
67
\_\_\_\_ are only obsserved at higher doses of Resorcinol and meta hydroxymethyl derivatives
Cardiac effects
68
Metaproterenol and Terbutaline metabolism
not metabolized by MAO or COMT = longer duration of action than isoproterenol
69
Metaproterenol and Terbutaline use
Asthma/COPD Terbutaline = tocolytic (prevent premature labor)
70
Albuterol and salmeterol metabolism and use
neither MAO nor COMT Asthma / COPD
71
Racemic mixtures
Albuterol + Salmeterol Dobutamine
72
More potent isomer for second gen B2 receptor agonists
Levalbuterol R group = C(CH3)3
73
3rd gen B2 agonists are all \_\_\_\_\_\_\_
Very long acting (No metabolism by COMT/MAO....12-24 hour duration)
74
What is the main issue with 3rd gen B2 agonists
_Long onset of action_ Salmeterol = 10-20 Minutes Formoterol = Less than 5 minutes
75
3rd gen B2 agents
Salmeterol and Formoterol
76
Salmeterol and Formoterol use
Long term Asthma COPD \*NOT acute/rescue inhaler
77
Direct acting beta agonist with mixed properties
Dobutamine
78
Dobutamine is a derivative of
DA
79
Dobutamine racemic mixture and receptor
**(+)** = potent **B1** agonist, **a1** antagonist **(-)** = **a1** agonist, **B1** potency *reduced 10x*
80
Net effect of dobutamine enantiomers
Positive inotropy Little/no chronotropic
81
Dobutamine metbolism
COMT and conjugation Not sensitive to MAO
82
Dobutamine PK
Short half life! | (2 minutes)
83
Dobutamine use
Acute HF Shock
84
Indirect acting sympathomimetics
* Amphetamine * Pseudoephedrine * Ephedrine * Phenylpropanolamine * Tyramine
85
Amphetamine mechanism of action
* 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
Clincal use for amphetamines
ADHD, narcolepsy, anorexiant
87
Other uses for amphetamines
nasal decongestants
88
Derivatives of ephedra
D-(-)-ephedrine L-(-)-pseudoephedrine
89
D-(-)-ephedrine has desired...
R-configuration at the beta OH S-configuration ata the alpha carbon = DIrect agonist activity of adrenergics!
90
L-(-)-pseudoephedrine configuration
S,S distereoisomer the S configuration of B-OH ***reduces*** its agonist activity
91
Major mechanism of L-(-)-pseudoephedrine
Reversal of the transporter
92
Structural difference between the ephedrine and pseudoephedrine
The configuration of the OH group on the beta carbon
93
L-(-)-pseudoephedrine doesn't have...
CNS penetration d/t OH group S configuration
94
Synthesis of methamphetamine
ephedrine --- (lithium + NH4+) --\>methamphetamine
95
ephedrine and pseudo cause ____ via the ___ receptor
vascular constriction a1 receptor

Pharm Exam 3 (11 decks)

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