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Pharmacology > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

What agonist drug inhibits reuptake of Dopamine and NE

A

cocaine (indirect)

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2
Q

What agonist drugs inhibits MAO so more NE is available

A

Selegiline (eldepryl)

Phenelzine (Nardil)

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3
Q

What agonist drugs reverse uptake to increase NE and dopamine release?

A

Amphetamines

Methylphenidate (Ritalin)

Tyramine (diagnostic, not a drug)

ALL highly addictive

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4
Q

What is ephedrine

A

direct agonist and indirect releasing drug of NE and dopamine

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5
Q

What drugs are beta agonists?

A

Dobutamine (Dobutrex)

Isoproterenol (Isuprel)

Albuterol (Ventolin)

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6
Q

What drugs are alpha agonists

A

Phenylephrine (Neo-Synephrine)

Clonidine (Catapres)

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7
Q

What drugs are mixed alpha and beta agonists

A

norepinephrine (Levophed)

epinephrine (Adrenalin)

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8
Q

Difference between direct and indirect agonists

A

indirect affects amount of NT at target site

direct interacts with receptors

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9
Q

What GPCR is alpha 1

A

Gq

phospholipase C–> IP3 and DAG

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10
Q

What GPCR is alpha 2

A

Gi

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11
Q

What GPCR is beta 1

A

Gs

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12
Q

What GPCR is beta 2

A

Gs

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13
Q

What GPCR is beta 3

A

Gs

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14
Q

What GPCR is D1

A

Gs

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15
Q

What GPCR is D2

A

Gi

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16
Q

Where are alpha 1 receptors

A

vascular smooth muscle–> contraction

pupillary dilator M–> contracts so pupil DILATES

prostate–> contraction

heart–> increase force (inotropy)

skeletal muscle (some)

skin vessels and mucous membranes (contract/decrease)

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17
Q

Where are alpha 2 receptors

A

neurons–> modulate NT release

platelets–> aggregation

ad. and chol. nerve terminals–> inhibit NT release

some vascular smooth muscle–> contraction

fat cells–> inhibit lipolysis

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18
Q

Where are beta 1 receptors

A

heart–> increase force (inotropy) and rate (chronotropy) of contraction

juxtaglomerular cells–> INCREASE renin release

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19
Q

What is the overall effect of activating beta 1 receptors in the heart

A

increase BP and TPR

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20
Q

Where are beta 2 receptors

A

respiratory, uterine, vascular smooth muscle–> RELAX

skeletal muscle–> K+ uptake

liver–> + glycogenolysis and gluconeogenesis

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21
Q

Where are beta 3 receptors

A

bladder–> relax detrusor M

fat cells–> + lipolysis

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22
Q

Where are D1 receptors

A

kidney and brain smooth muscle–> dilates renal BV

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23
Q

Where are D2 receptors

A

nerve endings–> modulate NT release

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24
Q

Where does epinephrine act

A

a1=a2, b1=b2

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25
Q

What is the function of epinephrine

A

increase inotropy, heart rate, conduction velocity at AV node (b1)

increase systolic BP (no change in MAP) (a1)

can decrease diastolic BP and TPR (b2)

skin vessels and mucous membranes (a1)

relaxes bronchial M (b2)

decrease bronchial secretion and congestion within mucosa (a1)

increase renin release (b1)

increase FFA in blood (b3)

increase blood glucose levels (b2)

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26
Q

How can epinephrine cause muscle tremors and hypokalemia?

A

activates B2 receptors that enhance K+ uptake in skeletal muscle

–> hyperpolarizes muscles so can’t get another AP, tremor and depletes blood potassium concentration

less K+ excreted

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27
Q

What receptors does norephinephrine act on

A

a1=a2, B1

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28
Q

What does norephinephrine do

A

potent cardiac stimulant (b1)
—> DECREASES HR d/t vagal response

potent vasoconstrictor (a1)

no bronchodilaton or vasodilation (no b2)

increase TPR and BP (a1 and b1)

role in baroreflex

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29
Q

TPR in epi vs NE

A

increase in NE d/t a1 and b1

decrease in epi d/t b2

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30
Q

What receptors does phenylephrine act on

A

a1

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31
Q

What does phenylephrine do

A

role of baroreflex

mydriatic (dilates pupil) and decongestant (a1)

severe vasoconstriction (a1)

increase BP (a1)

severe bradycardia (d/t vagal response)

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32
Q

What receptor does clonidine act on

A

selective a2 agonist

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33
Q

What does clonidine do

A

presynaptic a2 in lower brainstem:

decrease sympathetic output

decrease BP

bradycardia

peripheral a2:
vasoconstriction (when given IV before reaching CNS)

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34
Q

What is clonidine used to treat

A

HTN

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35
Q

What receptors do isoproterenol act on

A

non-selective beta agonist (b1 and b2)

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36
Q

What does isoproterenol do

A

+ inotropy and chronotropy (b1)

increase cardiac output (b1)

bronchodilation (b2)

vasodilator–> decrease arterial pressure (b2)

37
Q

What receptors does dobutamine act on

A

mostly B1, some a1 (rare)

38
Q

What does dobutamine do

A

a1: - isomer agonist, + isomer antagonist

potent inotropy (b1)

less potent chronotropy c/t isoproterenol

39
Q

What receptor does albuterol act on

A

b2

40
Q

What does albuterol do

A

bronchodilation

41
Q

What drugs are highly addictive

A

indirect agonist d/t increase in NE and DO in CNS

–> lipophilic, easily cross BBB

42
Q

What is the function of tyramine

A

should increase systolic BP when given IV

metabolized by MAO in liver, tests peripheral adrenergic fxn

43
Q

What drugs to give in hypotensive emergency (overdose, shock)

A

norepinephrine, phenylephrine

44
Q

What drug to give for chronic HTN

A

ephedrine

45
Q

What drug to give for cardiogenic shock

A

dobutamine

46
Q

What drug to give for short-term heart failure

A

dobutamine

47
Q

What drug to give for long-term HTN

A

alpha 2 agonist

48
Q

What drugs to give for emergent AV block and cardiac arrest

A

epinephrine, isoproterenol

treat heart and dilates lungs

49
Q

What drugs to treat depression

A

phenelzine, selegiline (MAO-)

50
Q

What drugs to treat narcolepsy

A

amphetamines, methylphenidate (reverse uptake)

51
Q

What drug to treat ADHD

A

methylphenidate

52
Q

What drugs to treat obesity

A

ephedrine, amphetamines

53
Q

What drug to treat asthma

A

albuterol

54
Q

What drugs for decongestion

A

phenylephrine, ephedrine

55
Q

What drug for anaphylaxis

A

epinephrine (acts on heart and lungs)

56
Q

What drug to evaluate retina

A

phenylephrine (mydriasis)

57
Q

What drug for glaucoma

A

selective a2 agonist

58
Q

What drug for stress urinary incontinence

A

ephedrine

59
Q

What drugs primarily work on CNS?

A

indirect agonists

60
Q

Adverse effects of adrenergic agonists

A

increased BP and work of heart–> MI or HF

tachycardia and v-arrhythmias–> sudden death

insomnia, decreased appetite, anxiety, psychoses (via indirect agonists @ CNS)

convulsions and hemorrhagic stroke (cocaine)

61
Q

What adverse effects can cocaine cause

A

convulsions and hemorrhagic stroke

62
Q

What drug inhibits NE release and prevents storage

A

guanethidine (ismelin)

indirect antagonist

63
Q

What drug inhibits tyrosine hydroxylase (no NE synthesis)

A

Metyrosine (Demser)

indirect antagonist

64
Q

What drugs are nonselective alpha antagonists

A

Phentolamine (OraVerse)

Phenoxybenzamine (Dibenzyline)

65
Q

What drugs are selective alpha 1 antagonists

A

Prazosin (Minipress)

Tamsulosin (Flomax)

Doxazosin (Cardura)

66
Q

What drugs are mixed antagonists

A

Labetalol (Trandate)

Carvedilol (Coreg)

mainly B and alpha 1

67
Q

What drugs are nonselective beta antagonists

A

Propranolol (Inderal)

Pindolol (Visken)

Nadolol (Corgard)

68
Q

What drugs are selective B1 antagonists

A

Metoprolol (Toprol)

Betaxolol (Kerlone)

Acebutolol (Sectral)

Atenolol (Tenormin)

69
Q

What is the difference between phentolamine and phenoxybenzamine

A

BOTH nonselective alpha antagonists

phentolamine reversible, short acting

phenozybenzamine irreversible non-competitive, longer acting

70
Q

Alpha antagonist effects

A

decrease TPR and BP

postural hypotension

reflex tachycardia

prostate SM relaxation, decrease resistance to urine flow

relax pupillary dilator M–> miosis (constrict pupil)

71
Q

What drugs to treat pheochromocytoma (tumor adrenal medulla)

A

phentolamine
phenozybenzamine
metyrosine

(antagonists)

72
Q

What drugs to treat chronic HTN

A

prazosin
doxazosin

(no non-selective antagonists)

73
Q

What drugs to treat erectile dysfunction

A

phentolamine plus nonspecific vasodilator (papaverine)

74
Q

Drug to treat BPH

A

tamsulosin (a1 ant with little effect on BP)

prazosin and doxazosin used but severely decrease BP

75
Q

Adverse effects of alpha antagonists

A

seen less with a1 ant

postural hypotension (inhibit a1 in venous SM)

nasal stuffiness

tachycardia

retention of fluid and salt

impaired ejaculation

76
Q

Beta blocker effects

A

decrease inotropy and chronotropy

slow conduction at AV node

initial rise in TPR but decrease with chronic use

inhibits renin release

increased airway resistance

reduce intraocular pressure by decreasing production of aqueous humor

inhibit lipolysis

increase VLDL, decrease HDL

inhibit glycogenolysis and gluconeogenesis

77
Q

What type of agonists are beta blockers with intrinsic sympathomimetic activity

A

partial agonists

–> block sympathetic effects but have submaximal agonist effects–> blunted sympathetic response

78
Q

Why give partial agonist vs antagonist

A

less risk for bradycardia, increased VLDL/HDL ration

–>desired effect without causing too much “damage”

79
Q

What beta blockers are antagonists

A

atenolol

nadolol

propranolol

80
Q

What beta blockers are partial agonists

A

acebutolol

labetalol

pindolol

81
Q

What beta blockers are inverse agonists

A

betaxolol

metoprolol

82
Q

What antagonists treat HTN

A

both mixed and beta blockers

83
Q

What drugs to give to reduce frequency of angina and improve exercise intolerance

A

beta blockers

–>decrease work and oxygen consumption

84
Q

What drugs to give to prolong survival after MI

A

propranolol

metoprolol

85
Q

What drugs to give to eliminate a-flutter, a-fib, ventricular ectopic beats

A

beta blockers

86
Q

What drugs to give or chronic HF

A

metoprolol

carvedilol

DO NOT use in acute or severe congestive HF

87
Q

What drug to give for glaucoma

A

betaxolol

NO propranolol

88
Q

What drug to give for hyperthyroidism

A

propranolol

89
Q

Adverse effects of beta blockers

A

sedation, sleep disturbances, depression
switch to hydrophilic drug

increased airway resistance, trigger bronchospasm and asthma attack in those at risk
switch to b1 selective

decrease HR, contractility and excitability
switch to partial agonist

increase VLDL, decrease HDL with chronic use
switch to partial agonist

hypoglycemia (although safer in Type 2 DM)
swithc to b1 selective

toxicity and hyperresponsiveness to ABRUPT discontinuation

Pharmacology (6 decks)

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