Adrenergics Flashcards

(62 cards)

1
Q

What is the signal transduction pathway for beta receptors

A

Accumulate cAMP and activate PKA

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2
Q

What is the signal transduction pathway for alpha 2 receptors

A

Decrease cAMP and inhibit PKA

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3
Q

What are the three mechanisms of action for indirect acting adrenergic drugs?

A

Reuptake blocker (cocaine), MAO inhibitor (selegine, phenelzine), and releasing agents (Amphetamines, methylphenidate)

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4
Q

What alpha adrenergic agonists prefer a1>a2?

A

phenylephrine, methoxamine

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5
Q

What alpha adrenergic agonists prefer a2>a1

A

Clonidine, methyNE

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6
Q

What is the receptor selectivity for NE

A

a1=a2; B1>B2

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7
Q

What is the receptor selectivity for epinephrine?

A

a1=a2; B1=B2

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8
Q

What beta adrenergic agonists prefer B1>B2

A

Dobutamine

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9
Q

What Beta adrenergic agonists select both B R equally

A

isoproterenol

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10
Q

What Beta adrenergic agonists prefer B2»B1

A

Albuterol, terbutaline, ritodrine

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11
Q

What Dopamine agonists prefer D1 & D2 equally

A

dopamine

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12
Q

What dopamine receptor agonists prefer D1»D2

A

Fenoldopam

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13
Q

What are the effects of epinephrine and the corresponding receptor?

A

Cardiac function - B1 - increase HR, contractility
Vascular tone - B2, a1 - inc systolic BP, same MAP
Respiratory - B2 - relax s. m. - a1 - dec secretion, congestion
skeletal m - B2 - tremor, inc K uptake
Elevate Blood Glucose - B2- inc liver glycogenolysis - a2/B2 - inhibit insulin release
Increase blood FFA - B
Increase renin release - B1

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14
Q

What are the effects of NE and the corresponding receptor

A

Cardiac stimulation - B1 - pump harder but dec HR

Potent vasoconstriction - a1

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15
Q

Why does NE decrease HR

A

The rise in BP is detected by the baroreceptors, which tell the hard to pump slower

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16
Q

What are the effects of dopamine and what are the corresponding receptors

A

vasodilation of the renal, cerebral, mesenteric, coronary a. - D1
Activation presynaptic D2 - suppress NE release

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17
Q

What is the signal transduction pathway for alpha 1 R

A

IP3, DAG, MAPK, PI3K,

These stimulate cell growth

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18
Q

What is the effects of phenylephrine

A

a1>a2. mydriasis (pupillary dilation), decongestion, severe vasoconstriction (inc BP)

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19
Q

What happens to phenylephrine is you block the baroreflex

A

The drug is 10x more potent on vasoconstriction

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20
Q

What are the effects of clonidine

A

a2>a1. Central effect on the a2 receptors in the brainstem, which decreases NE output –> lower BP and HR

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21
Q

What are the effects of isoproterenol

A

B1=B2. Increase cardiac output (B1), vasodilation / bronchodilation (B2). Therefore keeping BP about the same

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22
Q

What are the effects of dobutamine

A

B1>B2. Increase cardiac output

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23
Q

What are the effects of terbutaline, albuterol

A

B2>B1. Bronchodilation, relax uterus

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24
Q

Are indirect adreneric agonists polar or nonpolar

A

nonpolar

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25
What adrenergic agonist should be used to treat hypotensive emergencies?
Ne, phenylephrine, methoxamine
26
What adrenergive agonist should be used to treat chronic HTN
ephedrine
27
What adrenergic agonist should be used to treat cardiogenic shock (massive acute MI)
dopamine, dobutamine
28
What adrenergic agonist should be used to treat CHF
dopamine
29
What adrenergic agonist should be used to manage HTN
any a2 agonist
30
What adrenergic agonist should be used to treat HTN emergencies
fenoldopam
31
What adrenergic agonist should be used to treat complete AV block and cardiac arrest
Epinephrine, isoproterenol
32
What adrenergic agonist should be used to treat decongestion
Phenylephrine, ephedrine, pseudoephedrine
33
What adrenergic agonists should be used to treat bronchial asthma
albuterol, terbutaline
34
What adrenergic agonist should be used to treat anaphylaxis
epinephrine
35
What adrenergic agonist should be used to induce mydriasis
phenylephrine
36
What adrenergic agonist should be used to treat glaucoma
apraclonidine, brimonidine
37
What adrenergic agonist should be used to suppress premature labor
terbutaline
38
What adrenergic agonist should be sued to treat stress incontinence
Ephedrine
39
What adrenergic agonist should be used to Tx priapism
phenylephrine
40
What adrenergic agonist should be used to tx narcolepsy
amphetamines, methylphenidate
41
What adrenergic agonist should be used to treat ADHD
methylphenidate
42
What adrenergic agonist should be used to tx obesity
Phentermine, ephedrine, amphetamines
43
What are the CV adverse effects of adrenergic agonists
Inc BP, Inc cardiac work, sinus tachycardia
44
What are the CNS adverse effects of adrenergic agonists
Amphetamines - insomnia, dec appetite, anxiety, psychoses | cocaine - convulsions, arrhythmias, hemorrhagic stroke
45
What indirect antiandrenergics deplete NE
reserpine, guanethidine
46
What indirect antiadrenergics inhibit NE synthesis
metyrosine
47
What indirect antiadrenergics activate inhibitory a2 Receptors
Clonidine
48
What indirect antiadrenergics are used to treat chronic HTN
guanethidine, clonidine
49
What indirect antiadrenergic is used to treat a pheochromocytoma
metyrosine
50
What are the nonselective alpha R antagonists
Phentolamine (competitive), phenoxybenzamine (noncompetitive)
51
What are the alpha 1 receptor specific antagonists
-osin's
52
what are the mixed alpha receptor antagonists
labetalol, carvedilol
53
What are the non selective B antagonists
propanolol (A), pindolol (pa), nadolol (a), penbutolol (pa)
54
What are the B1 selective antagonists
metoprolol (ia), betaxolol (a), acebutolol (pa), atenolol (a)
55
What is the difference when using phentolamine and prazosin to cause cardiac stimulation
Phentolamine (nonselective a) will cause a larger increase in B1 effect because there is no negative feedback on NE release (a2 job) Prazosin has no tachycardia
56
What alpha antagonists are used to treat pheochromocytoma
phentolamine, phenoxybenzamine
57
What alpha antagonists are used to treat chronic HTN
-osin
58
What alpha antagonists are used to treat ED
phentolamine, papverine
59
What alpha antagonists are used to treat BPH
tamsulin, silodosin | these specifically target a1a R
60
What are the adverse effects of alpha R antagonists
postural Hypotension, increase HR, salt/water retention, impaired ejaculation, nasal stuffiness
61
What are the effects of B blockers
inhibit renin release, inc respiratory secretion, decrease intraocular pressure, tx hyperthyroidism, tx HTN, tx angina pectoris, MI, arrhythmias, HF
62
What are the adverse effects of B blockers
CNS - sedation, depression, sleep disturbances Resp - inc resistance, can trigger bronchospasm dec HDL/LDL ration May delay recovery from insulin induced hypoglycemia