Adrenergics Flashcards

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
Q

What adrenergic agonist should be used to treat hypotensive emergencies?

A

Ne, phenylephrine, methoxamine

26
Q

What adrenergive agonist should be used to treat chronic HTN

A

ephedrine

27
Q

What adrenergic agonist should be used to treat cardiogenic shock (massive acute MI)

A

dopamine, dobutamine

28
Q

What adrenergic agonist should be used to treat CHF

A

dopamine

29
Q

What adrenergic agonist should be used to manage HTN

A

any a2 agonist

30
Q

What adrenergic agonist should be used to treat HTN emergencies

A

fenoldopam

31
Q

What adrenergic agonist should be used to treat complete AV block and cardiac arrest

A

Epinephrine, isoproterenol

32
Q

What adrenergic agonist should be used to treat decongestion

A

Phenylephrine, ephedrine, pseudoephedrine

33
Q

What adrenergic agonists should be used to treat bronchial asthma

A

albuterol, terbutaline

34
Q

What adrenergic agonist should be used to treat anaphylaxis

A

epinephrine

35
Q

What adrenergic agonist should be used to induce mydriasis

A

phenylephrine

36
Q

What adrenergic agonist should be used to treat glaucoma

A

apraclonidine, brimonidine

37
Q

What adrenergic agonist should be used to suppress premature labor

A

terbutaline

38
Q

What adrenergic agonist should be sued to treat stress incontinence

A

Ephedrine

39
Q

What adrenergic agonist should be used to Tx priapism

A

phenylephrine

40
Q

What adrenergic agonist should be used to tx narcolepsy

A

amphetamines, methylphenidate

41
Q

What adrenergic agonist should be used to treat ADHD

A

methylphenidate

42
Q

What adrenergic agonist should be used to tx obesity

A

Phentermine, ephedrine, amphetamines

43
Q

What are the CV adverse effects of adrenergic agonists

A

Inc BP, Inc cardiac work, sinus tachycardia

44
Q

What are the CNS adverse effects of adrenergic agonists

A

Amphetamines - insomnia, dec appetite, anxiety, psychoses

cocaine - convulsions, arrhythmias, hemorrhagic stroke

45
Q

What indirect antiandrenergics deplete NE

A

reserpine, guanethidine

46
Q

What indirect antiadrenergics inhibit NE synthesis

A

metyrosine

47
Q

What indirect antiadrenergics activate inhibitory a2 Receptors

A

Clonidine

48
Q

What indirect antiadrenergics are used to treat chronic HTN

A

guanethidine, clonidine

49
Q

What indirect antiadrenergic is used to treat a pheochromocytoma

A

metyrosine

50
Q

What are the nonselective alpha R antagonists

A

Phentolamine (competitive), phenoxybenzamine (noncompetitive)

51
Q

What are the alpha 1 receptor specific antagonists

A

-osin’s

52
Q

what are the mixed alpha receptor antagonists

A

labetalol, carvedilol

53
Q

What are the non selective B antagonists

A

propanolol (A), pindolol (pa), nadolol (a), penbutolol (pa)

54
Q

What are the B1 selective antagonists

A

metoprolol (ia), betaxolol (a), acebutolol (pa), atenolol (a)

55
Q

What is the difference when using phentolamine and prazosin to cause cardiac stimulation

A

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
Q

What alpha antagonists are used to treat pheochromocytoma

A

phentolamine, phenoxybenzamine

57
Q

What alpha antagonists are used to treat chronic HTN

A

-osin

58
Q

What alpha antagonists are used to treat ED

A

phentolamine, papverine

59
Q

What alpha antagonists are used to treat BPH

A

tamsulin, silodosin

these specifically target a1a R

60
Q

What are the adverse effects of alpha R antagonists

A

postural Hypotension, increase HR, salt/water retention, impaired ejaculation, nasal stuffiness

61
Q

What are the effects of B blockers

A

inhibit renin release, inc respiratory secretion, decrease intraocular pressure, tx hyperthyroidism, tx HTN, tx angina pectoris, MI, arrhythmias, HF

62
Q

What are the adverse effects of B blockers

A

CNS - sedation, depression, sleep disturbances
Resp - inc resistance, can trigger bronchospasm
dec HDL/LDL ration
May delay recovery from insulin induced hypoglycemia