Adrenergics Flashcards

1
Q

clonidine, in some patients

A

decreases renin and aldosterone concentrations

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2
Q

clonidine effect in different positions

A

standing: peripheral vasodilation, lying down: decreases heart rate and stroke volume

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3
Q

clonidine given IV

A

can increase blood pressure

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4
Q

phenylephrine

A

α1 agonist

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5
Q

dobutamine

A

β1 (relatively selective) agonist, two sterioisomers; increase in ionotropic (major) and chronotropic effects, autoregulatroy increase in coronary blood flow

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6
Q

isoproternol

A

non-selective β adrenergic agonist, IV administration results in increase in ionotropic and chronotropic effects, also it causes skeletal, mesenteric, and renal vasodilation (β2) which reflexly reinforces the β1 effects

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7
Q

epinephrine - low dose

A

low doses: β1 & β2 effects predominate (looks like isoproternol)

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8
Q

epinephrine - high dose

A

α1, β1 effects predominate, blood pressure increase, increases systolic bp and also diastolic if the dose is high enough

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9
Q

norepinephrine

A

α1, α2, & β1 agonist; predominant effects are on blood pressure (increases systolic and diastolic), risk of arhythmias, CO stays relatively stable (reflex to vasoconstriction opposes β1 increase in ionotropic and chronotropic effects)

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10
Q

dopamine

A

norepinephrine metabolic precursor; low doses: activates D1 (Gs) in mesenteric and vascular beds,vasodilation, important in circulatory shock,

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11
Q

dopamine - high doses

A

β1 adrenergic agonist – stimulates myocardial contraction and rate - increase in CO and systolic BP without change in peripheral vascular resistance. even higher α1

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12
Q

β2 adrenergic agonists

A

powerful bronchodilators, suppress release of mast cell inflammatory mediators, do not reduce bronchial hyperresponsiveness

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13
Q

selective β2 agonists

A

albuterol, terbutaline

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14
Q

long acting β2 agonist

A

salmeterol (12+ hours), treatment of asthma

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15
Q

β2 effects on uterine smooth muscle

A

relaxation – treatment for premature labor

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16
Q

premature labor treatment

A

β2 agonist: ritodrine, terbutalin

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17
Q

catecholamine mediated hyperglycemia

A

α1/β2 effects on hepatic glycogenolysis and increase in lactate concentrations via muscle glycogenolysis, stimulation of lypolysis

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18
Q

insulin secretion

A

increased by β2,decreased by α2

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19
Q

nasal decongestants

A

α1 agonist

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20
Q

paroxysmla atrial tachycardia

A

raise bp with α1 agonist and reflexly slow down the heart

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21
Q

hypotensive states

A

spinal anesthesia, chronic orthostatic hypotension, shock

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22
Q

types of shock

A

hypovolemic shock, cardiogenic shock, hyperdynamic shock, anaphylactic shock, septic shock

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23
Q

hypovolemic shock

A

inadequate venous return (low volume or obstruction)

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24
Q

cardiogenic shock

A

due to impaired contractile function: MI, heart failute, cardiomyopathy

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25
Q

treatment for cardiogenic shock

A

relieve ventricular after load with vasodilators, use positive iontropic agents (dobutamine, dopamine)

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26
Q

hyperdynamic shock

A

fall in peripheral resistance cause by sepsis, anaphylaxis, adrenal insufficiency, or neurological disorders

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27
Q

anaphylactic shock

A

immediate hypersensitivity response with bronchospasm, mucous membrane edema, cardiovascular collapse

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28
Q

treatment of anaphylactic shock

A

epinephrine

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29
Q

treatment of septic shock

A

antibiotics, activated protein C

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30
Q

hyperdynamic shock, high cardiac output

A

vasopressor

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31
Q

hyperdynamic shock PAWP

A

low: volume; high: ionotropic agent

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32
Q

clonidine half life

A

12 hours

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33
Q

dobutamine

A

sort of selective β1 adrenergic agonist, half life 2 minutes, useful in short term treatment of cardiac decompensation, excessive doses have α1 effect

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34
Q

the ideal aerosolized drug should be

A

absorbed poorly from the GI tract or extensively metabolized during first pass

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35
Q

salmeterol has a

A

delayed onset of action

36
Q

ritodrine

A

prevention of premature labor, β2 agonist, side effects: reduced peripheral vascular resistance, tachycardia, increased renin secretion, salt and water retention, hyperglycemia, apprehension, anxiety

37
Q

topical hemostasis

A

epinephrine

38
Q

increases renal blood flow, sodium excretion, and glomerular filtration rate

A

dopamine (short half life, given via IV infusion)

39
Q

indirectly acting sympathomimetic amines

A

indirectly cause NE release, less effective on repeated use (tachyphylaxis), slower than endogenous NE in onset and longer in duration, transported via NE uptake system

40
Q

“mixed acting” sympathomimetic amines

A

act directly on receptors and indirectly via NE release

41
Q

purely indirectly acting sympathomimetic amine

A

tyramine (cheese, etc)

42
Q

mixed acting, orally effective, sympathomimetic amine

A

ephedrine

43
Q

amphetamine

A

lipid soluble, metabolically blocked, orally active, relatively long acting, prominent CV and CNS effects, used for ADHD and narcolepsy

44
Q

ephedrine

A

orally active, CNS stimulant, used for asthma, banned for athletes (α/β agonist, also indirect)

45
Q

amphetamine CV effects

A

bp elevation, reflex decrease in heart rate, arrhythmias

46
Q

amphetamine CNS effects

A

NE and dopamine release - wakefulness, euphoria, confusion, delirium, panic states, etc. fatal OD: convulsions, coma, cerebral hemorrhage

47
Q

amphetamine side effects

A

appetite suppressant

48
Q

methylphenidate

A

ritalin: CNS stimulant, used for ADHD, attention at level of cerebral cortex, drug holidays when possible, watch for insomnia and anorexia

49
Q

paradoxical improvement of ADHD via

A

dextroamphetamine and methylphenidate

50
Q

fen-phen

A

20mil prescriptions in 1996, caused heart valve disease

51
Q

two centrally acting agents that interfere with adrenergic neuronal function

A

clonidine and methyl-dopa

52
Q

methyl-dopa

A

false neurotransmitter, α2 agonist, accumulates in secretory vesicles, converted to methylNE via same drug that converts dopamine into NE

53
Q

methyl-dopa is

A

orally active, decrease peripheral vascular resistance, adverse effects are sedation, dry mouth, hepatic toxicity

54
Q

what is special about methyl-dopa

A

false neurotransmitter and a prodrug

55
Q

reserpine

A

complex alkaloid from indian snake root plant, binds to and inactivates neuronal storage vesicles (NE, E, dopamine, serotonin)

56
Q

eventual effect of high dose reserpine

A

depletion of central and peripheral stores of catecholamines and serotonin

57
Q

good things about reserpine

A

lowers blood pressure, is cheap

58
Q

effects of α adrenergic antagonists are

A

less obvious when lying down, more obvious in hypovolemic states

59
Q

compensatory responses to α adrenergic agonists are

A

tachycardia (fast - more with general α antagonists) and fluid retention (slow)

60
Q

when α receptors are blocked, epinephrine

A

vasodilates (β2 vasodilation effects of epinephrine)

61
Q

α1 antagonists also block

A

contraction of urinary sphincter, contraction for ejaculation, (causes nasal stuffiness)

62
Q

effects of α2 adrenergic antagonists

A

enhanced sympathetic outflow, vasoconstriction, cardiac stimulation

63
Q

phenoxybenzamine

A

nonselective α adrenergic blocker, alkylating agent, related to nitrogen mustards, irreversible

64
Q

preop for pheochromocytoma surgery

A

phenoxybenzamine

65
Q

prazoin

A

selective α1 blocker, 3 hour half life, for primary systemic hypertension

66
Q

tamulosin

A

selective α1 blocker, treats benign prostatic hypertrophy (α1A>α1B), 9-15 hour half life

67
Q

β1 effect

A

block catecholamine stimulated renin secretion

68
Q

β blockers are counter-indicated in patients with

A

asthma, COPD, diabetes (mask tachycardia during hypoglycemic events)

69
Q

β blockers cause modest

A

increases in triglycerides and decreases in HDL

70
Q

selective β1 antagonist

A

metoprolol (3-4 hrs), atenolol (5-8hrs)

71
Q

nonselective β antagonists

A

propranolol (3-5 hrs), carvediolol (7-10 hrs)

72
Q

propranolol

A

lipophilic, one a day dosing despite short half life

73
Q

carevediolol

A

racemic, antioxidant, CHF treatment

74
Q

metoprolol

A

β1, genetic differences in rate of metabolism

75
Q

atenolol

A

β1, limited brain penetration

76
Q

β antagonist and exercise

A

decreased ability in patients without angina

77
Q

β antagonist major problem

A

discontinuation rebound, worsen peripheral vascular disease

78
Q

β blockers and vasodilators/diuretics

A

good combinations due to decrease in reflex tachycardia

79
Q

supraventricular and ventricular arrhythmias

A

β blockers

80
Q

early administration after MI

A

β blocker without intrinsic sympathomimetic activity

81
Q

β and α1 antagonist

A

carvediolol (CHF, hypotension?)

82
Q

in CHF take

A

carvediolol or metoprolol

83
Q

acute dissecting aortic aneurysm

A

β blocker, short term, pending surgery

84
Q

β blocker also used for

A

hyperthyroidism, migraine prophylaxis, acute panic syndrome, open angle glaucoma (reduce aqueous humor creation), pheochromocytoma (control catecholamine effects on the heart)

85
Q

shortest and longest half lives

A

dobutamine, clonidine

86
Q

tachyphylaxis

A

depletion of neurotransmitter from nerve endings