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Lecture 7: Adrenergic Agonists Flashcards

1
Q

Receptor a1

A

-signals via Gq
-found on vascular, GI smooth muscle, and heart, and liver
-mediates vasoconstriction

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2
Q

a1 agonist clinical use

A

-nasal decongestion
-vascular failure in shock and supraventricular tachycardia

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3
Q

a1 ANTAgonist clinical use

A

-hypertension
-benign prostatic hyperplasia
-pheochromocytoma

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4
Q

direct a1 AGONIST drugs

A

-phenylephrine
-oxymetazoline

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5
Q

Phenylephrine (Neosynephrine)

A

-direct a1 agonist
-substrate for MAO
-high first pass metabolism

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6
Q

Phenylephrine clinical use

A

-a1 agonist
-nasal decongestant (bad tho)
-mydriasis w/o cycloplegia
-pressor
-vasoconstrictor in regional anesthesia

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7
Q

Phenylephrine administration

A

-parenteral
-oral
-local

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8
Q

2-aralkylimidazolines

A

-direct a1 receptor agonist
-basicity of imidazoline ring cause compunds to exist in ionized form at physiological pH
-partial agonists

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9
Q

2-aralkylimidazolines types

A

-naphazoline
-tetrahydrozoline
-oxymetazoline (visine)

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10
Q

2-aralkylimidazoline clinical use

A

-admin topically to promote vasoconstriction
-nasal and ophthalmic decongestants

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11
Q

Imidazoline

A

-basic ring structure
-cation is resonance stable = more basic

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12
Q

Beta receptor signaling

A

-Gs
-activate adenylyl cyclase
-increase cAMP
-cAMP dependent protein kinase
-phosphorylation of ion channels

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13
Q

B1 receptor location

A

-heart
-kidney

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14
Q

B1 receptor effect on heart

A

-increase force of contraction (inotropy)
-increase HR (chronotropy)
-increase conduction velocity in AV node

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15
Q

B1 receptor effect on kidney

A

-increase renin release

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16
Q

B1 AGONIST clinical use

A

-shock
-congestive heart failure

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17
Q

B1 ANTAgonist clinical use

A

-hypertension
-angina
-arrhythmias
-congestive heart failure

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18
Q

B2 receptor location

A

-smooth muscle

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19
Q

B2 receptor effect

A

-relax smooth muscle esp bronchial
-vasoDILATION

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20
Q

B2 AGONIST clinical use

A

-asthma
-premature labor

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21
Q

B2 ANTAgonist clinical use

A

Glaucoma

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22
Q

B3 receptor location

A

-bladder

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23
Q

B3 receptor effect

A

-relaxation
-prevention of urination

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24
Q

B3 AGONIST clinical use

A

-overactive bladder

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25
Non-selective B agonists
-isoproterenol (isuprel)
26
B1-selective B AGONISTs
-Dobutamine (Dobutrex) -Dopamine (intropin) (MOA complex)
27
B2 selective AGONISTS
-Terbutaline (brethine, bricanyl) -metaproterenol (metaprel, alupent) -albuterol (proventil, ventolin) -salmeterol (serevent) -ritodrine (yutopar)
28
B3-selective AGONISTS
-mirabegron (myrbetriq)
29
Isoproterenol (Isuprel)
-non-selective B AGONIST -bronchodilation -increase cardiac output
30
Isoproterenol (Isuprel) metabolism
-by phase II conjugation reactions -by COMT -not sensitive to MAO
31
Isoproterenol administration
-oral -parenteral -local (inhaled)
32
isoproterenol use
-asthma -COPD -cardiostimulant
33
Isoproterenol Action
-B1 and B2 AGONIST -increase Cardiac Output
34
Isoproterenol effect on peripheral vessels
-stimulate B2 -vasoDILATION -reduce peripheral resistance (may lower BP)
35
Isoproterenol clinical use
-emergency use to increase HR -patients with bradycardia or heart block -patients with SYSTOLIC dysfunction, SLOW HR, high systemic vascular resistance: after cardiac surgery in patients who previously used B-blockers -astma and COPD
36
Isoproterenol note
-not routinely used -epinephrine and dopamine more common
37
selectivity of adrenergic receptor agonists
SLide 37
38
Response to decrease in Blood pressure
-activates sympathetic fibers -activate B1 receptors = increase HR (reflex tachycardia) -activate a1 receptors = vasoCONSTRICT blood vessels -INHIBITS vagus (PSNS) -net result=increase BP
39
Response to increase in blood pressure
-INHIBITS sympathetic fibers -activates VAGUS (PSNS) = decrease HR (reflex bradycardia) -no effect on blood vessels -net result = decrease BP
40
BP= peripheral resistance x cardiac output
-resistance influenced by vasoconstriction/dilation -output influenced by HR and stroke volume
41
Norepinephrine effects
-decrease HR -increase BP -increase resistance -a1,B1
42
Epinephrine effects
-INcrease HR -maintain BP -slight DErease peripheral resistance -a1, B1, B2
43
Isoproterenol effects
-INcrease HR -slight DEcrease BP -DEcrease resistance -B1, B2
44
Selective B2 AGONists
-resorcinol derivatives -bronchoDILATION -cardiac effects only observed at high doses
45
Selective B2 AGONist metabolism
-NOT by MAO or COMT -longer duration of action than isoproterenol
46
selective B2 agonist administration
-oral -parenteral (only resorcinol derivatives) -local (inhaled)
47
selective B2 AGONist uses
-asthma -COPD -terbutaline used as tocolytic (prevent premature labor)
48
STRUCTURES
STRUCTURES
49
Resorcinol derivatives
-selective B2 AGONists -metaproterenol -terbutaline
50
Meta hydroxymethyl derivatives
-selective B2 AGONISTS -Albuterol -Salmeterol
51
Long acting B2 Agonists
-Salmeterol and Formoterol -10 min and 5 min onset respectively -longer duration -INHALED -use for long-term astma and COPD -not acute treatment
52
Problems with B2 receptor agonists
-minor cardiac stimulation
53
Dobutamine
-MIXED B1 and a1 AGONIST -dopamine derivative -racemic -racemic exerts stronger inotropic than chronotropic effect -SHORT (2min) half life
54
+ Dobutamine enatiomer
-potent B1 AGONIST
55
- Dobutamine enatiomer
-potent a1 AGONIST -reduced potency for B by 10x
56
Dobutamine metabolism
-by COMT and conjugation -NOT sensitive to MAO
57
Dobutamine administration
-IV infusion (why?)
58
Dobutamine use
-acute heart failure -shock -lab stresss test
59
Mirabegron
-B3 AGONIST -use for overactive bladder -also M3 ANTAgonist!
60
Mirabegron problems
-slow onset (8 weeks) -HTN
61
a2 receptor signaling
-Gi pathway -inhibit Ca -decrease NT release
62
a2 Agonist clinical use
-HTN -pain -glaucoma
63
a2 receptor AGONISTs
-Clonidine -Methyldopa -Guanabenz -Guanfacine -Brimodine -Apraclonidine -Tizanidine
64
Clonidine
-(phenylimino)imidazoline -a2 AGONIST -also imidazoline receptor
65
Clonidine structure
-imidazoline ring -basicity of guanidine froup decreased (pKa 13 to 8) bc attachment to dichlorophenyl ring
66
Clonidine action
-a2 AGONIST -in CNS: decrease SNS activity to heart and blood vessels -presynaptic: decrease cAMP, inhibit Ca (decrease vesicular release), activate certain Ka channels (hyperpolarize
67
Clonidine administration
-oral -parenteral -transdermal
68
Clonidine clinical use
-HTN -neuropathic pain -opiate withdrawal -ADHD
69
Clonidine problems
-hypotension -sedation -dry mouth -withdrawal sometimes after prolonged use
70
a2 AGONIST effect
-reduce SNS -inhibit NE release
71
Decreased SNS effect
-DEcrease HR -DEcrease contractility -DEcrease renin release -DEcrease vasoCONSTRICTION
72
open ring imidazolidine a2 agonists
-Guanabenz -Guanfacine
73
Guanabenz and Guanfacine admin
oral
74
Guanabenz and Guanfacine structure
-open ring imidazolidines -2 atom bridge to guanidine group decreases pKa so drug is mostly non-ionized at physiological pH
75
Guanabenz and Guanfacine clinical use
-HTN -ADHD (guanfacine)
76
Guanabenz half-life
6 hours
77
-guanfacine and clonidine half life
-12-16 hours
78
Methyldopa
-a2 AGONIST -prodrug metabolized to agonist -decrease SNS -oral
79
Methyldopate
-water soluble ester HCL salt -used for parenteral solutions
80
Methyldop(ate) uses
-HTN -esp during pregnancy
81
Methyldopa metabolism
slide 52
82
Brimodine action
-a2 AGONIST -acts on ciliary body -inhibits aq humor production (acute) -stimulate aq humor outflow (chronic)
83
Brimodine use
-Glaucoma (ophtalmic)
84
Brimonidine problems
allergic conjunctivitis
85
Meds for Glaucoma
-brimonidine -apraclonidine (para NH2 on clonidine)
86
Tizanidine
-a2 AGONIST
87
tizanidine use
-muscle spasticity
88
tizanidine adverse effects
-sedation -Na+ and water retention -dry mouth -withdrawal

Therapeutics (78 decks)

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