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Therapeutics 2 - Exam 5 > yang > Flashcards

yang Flashcards

1
Q

what drugs are alpha-1 antagonists?

A

prazosin
terazosin
doxazosin

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2
Q

what is the pk of alpha-1 antagonists?

A

prazosin –> 3 hours
terazosin –> 12 hours
doxazosin –> 20 hours

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3
Q

what is the metabolism of alpha-1 antagonists?

A

extensive metabolism that is excreted in the bile

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4
Q

what is the MOA of prazosin?

A

Alpha-1 antagonism decreases TPR –> activates the baroreceptor reflex —-> increases NE release into the myocardium –> increase in HR via beta-1 receptors.
Negative feedback via alpha-2 receptors in the myocardium mitigates NE release

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5
Q

what are alpha-1 antagonists?

A

quinazolines that produce vasodilation via alpha-1 antagonism in arterioles and venules without causing reflex tachycardia or increased CO (presynaptic alpha-2 effect)

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6
Q

what are the effects of alpha-1 antagonists?

A

decrease TPR with less reflex tachycardia than nonselective antagonists (phentolamine)

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7
Q

what are the compensatory effects of alpha-1 antagonists?

A

reflex tachycardia
renin release
co-administer diuretic to decrease retention of salt and water

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8
Q

what are the clinical use of alpha-1 antagonists?

A

BPH
HTN (not first line)
reynaud’s disease

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9
Q

what is reynaud’s disease

A

numbness due to cold or stress producing vasconstriction in hands/feet

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10
Q

what are the problems with alpha-1 antagonists?

A

first dose phenomenon (most common with prazosin)

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11
Q

what is the first dose phenomenon?

A

orthostatic hypotension and syncope particularly with first dose

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12
Q

what are the effects of direct-acting alpha-2 agonists?

A

inhibit NE release and decrease sympathetic tone in CNS –> resulting in decreased HR, contractility, and renin release, and less vasoconstriction

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13
Q

what is clonidine?

A

alpha-2 agonist and imidazoline receptor
activates the presynaptic alpha-2 receptor in the CNS to decrease SNS activity to the heart and blood vessels

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14
Q

how is clonidine administered?

A

oral
parenteral
transdermal

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15
Q

what is the half life of clonidine?

A

8-12 hours

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16
Q

is clonidine lipophilic or hydrophilic?

A

lipophilic

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17
Q

what are the clinical uses of clonidine?

A

HTN
ADHD
neuropathic pain/opiate withdrawal
restless leg syndrome

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18
Q

what are the SE of clonidine?

A

hypotension
sedation
dry mouth
withdrawal syndrome after prolonged use –> HTN tachycardia, angina, MI so taper dose

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19
Q

what are guanabenz and guanfacine?

A

oral direct acting alpha-2 agonists and open ring imidazolidines that are mostly non-ionized at physiological pH

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20
Q

what is the half life of guanabenz?

A

6 hours

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21
Q

what is the half life of guanfacine?

A

12-16 hours

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22
Q

what is the clinical usage of guanabenz and guanfacine?

A

HTN
ADHD

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23
Q

what is methyldopa?

A

oral direct-acting alpha-2 agonist and prodrug that reduces sympathetic outflow

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24
Q

what is the metabolic pathway of methyldopate

A

methyldopate –> methylopa (via esterase) –> alpha-methyldopamine (via L-aromatic amino acid decarboxylase) –> (IR,2S)-alpha-methylnorepineprhine (via dopamine beta-hydroxylase)

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25
Q

what is methyldopate?

A

ester hydrochloride salt that is water soluble and used parenterally

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26
Q

what is the clinical use of methyldopa?

A

HTN especially in pregnancy

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27
Q

what drugs are central acting alpha-2 agonists?

A

clonidine
methyldopa
guanabenz
guanfacine

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28
Q

what is the action of methyldopa?

A

false transmitter that displaced NE from vesicle

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29
Q

what are the effects of alpha-2 agonists?

A

decrease TPR, HR, and renin activity

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30
Q

what are the SE of methylopa?

A

sedation
sodium/water retention (combine with diuretic)

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31
Q

what is the impact of beta blockers on angina?

A

reduce myocardial oxygen demand via reduced HR and contractility

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32
Q

what is the impact of beta-blockers on cardiac arrhythmia?

A

slows AV nodal conduction

33
Q

what is the impact of beta blockers in post-MI?

A

reduce myocardial oxygen demand and slows AV nodal conduction

34
Q

what is the impact of beta-blockers in HTN?

A

decrease CO and inhibit renin secretion

35
Q

what is the role of beta blockers in congestive HF?

A

decrease chronic overstimualtion/toxicity of compensatory catecholamines

36
Q

what drugs are non-selective beta blockers?

A

propranolol
timolol
nadolol
pindolol
carteolol

37
Q

what are the indications for propranolol?

A

HTN (no effect on BP in normotensive individuals)
angina
cardiac arrhythmias
ischemic heart disease
prophylaxis for migraines

38
Q

what are the indications of timolol?

A

open-angle glaucoma
HTN
angina
migraine

39
Q

what are the problems with beta-blockers?

A

use caution asthmatic due to beta-2 receptor blockade
rebound HTN if abrupt d/c so taper dose

40
Q

what are the pharmacologic effects of propranolol?

A

decreased CO, HR, renin release, and LDL
increase VLDL and bronchial airway resistance
inhibits lipolysis, compensatory glycogenolysis, and glucose release in response to hypoglycemia

41
Q

what is the metabolism of propranolol?

A

extensive first-pass hepatic metabolism
lipophilic

42
Q

what is the half life of propranolol?

43
Q

what is nadolol?

A

non selective beta blocker that is less lipophilic and mostly excreted unchanged in the urine

44
Q

what is the half life of nadolol?

45
Q

what are the clinical uses of nadolol?

A

HTN
angina
migraine

46
Q

what is pindolol?

A

non selective beta blocker with intrinsic sympathomimetic activity that is less likely to cause bradycardia or lipid abnormalities

47
Q

what is the indication of pindolol?

A

HTN
angina
migraine
best for patients who have severe bradycardia (under 40 BPM) or little cardiac reserve

48
Q

what drugs are non selective beta blockers with intrinsic sympathomimetic activity?

A

carteolol
pindolol

49
Q

what is carteolol

A

non selective beta blocker with ISA that is less likely to cause bradycardia or lipid abnormalities

50
Q

what is the indication of carteolol?

A

HTN
glaucoma

51
Q

what drugs are beta-1 selective antagonists?

A

metoprolol
bisoprolol
atenolol
esmolol

52
Q

what are the indications of metoprolol?

A

HTN
angina
cardiac arrhythmias
ischemic heart disease
congestive HF

53
Q

what are the problems associated with metoprolol?

A

rebound HTN if d/c abruptly so taper dose

54
Q

what is metoprolol?

A

para-substituted phenyl derivative and selective beta-1 antagonist that is cardioselective and has moderate lipophilicity

55
Q

what is the half life of metoprolol?

A

3 to 4 hours

56
Q

what is the indication of bisoprolol?

A

reduces mortality in systolic HF

57
Q

what is atenolol?

A

cardioselective beta-1 antagonist that has low lipophilicity (water-soluble metoprolol)

58
Q

what is the half life of atenolol?

A

6 to 9 horus

59
Q

what is the indication of atenolol?

60
Q

what is esmolol?

A

very short acting (9 minute half life) selective beta-1 antagonist that is administered parenterally and exhibits rapid hydrolysis via esterases

61
Q

what is the indication of esmolol?

A

supra ventricular tachycardia
atrial flutter/fibrillation
perioperative HTN

62
Q

what is the CI of esmolol?

A

sodium bicarbonate

63
Q

what is nebivolol?

A

3rd generation beta-1 antagonist that possesses vasodilation due to nitric oxide production

64
Q

what is the indication for nebivolol?

64
Q

what is the effect of beta blockers?

A

decrease HR, contractility, renin release
no effect on BP in normotensive patients

64
Q

what is the indication of beta blockers?

A

HTN
angina
cardiac arrhythmias
MI
HF
migraine prophylaxis (propranolol)
glaucoma (timolol)
intraoperative HTN (esmolol)

64
Q

what is beta blocker withdrawal syndrome?

A

abrupt d/c can result in exacerbations of HTN or angina and MI

64
Q

what drugs are mixed beta antagonists?

A

carvediolol
labetolol

64
Q

what are the problems of beta blockers?

A

bradycardia
AV block
negative inotrophy
decrease CO
extremity vasoconstriction particualry cold extremities
CNS symptoms
ED
mask of hypoglycemia
beta blocker withdrawal syndrome
bronchoconstriction

64
Q

what are the CI of beta blockers?

A

asthma
COPD
congestive HF (type 4)

65
Q

what is the action of labetolol?

A

alpha-1 antagonism and non selective beta-1 and beta-2 antagonism with beta-2 partial agonism (3:1 beta-alpha)

65
Q

what is action of carvediolol?

A

alpha-1 antagonism and non selective beta-1 and beta 2 antagonism (10:1 beta alpha)

65
Q

what are the effects of mixed beta antagonists?

A

decrease TPR via reduced alpha-medicated vasoconstriction resulting in lowering BP
prevents reflex tachycardia (due to beta blocking activity)
vasodilation via alpha-1 blockade helps prevent bradycardia associated with beta blockade

65
Q

what is the indication of labetolol?

A

HTN emergencies
pheochromoctyoma

66
Q

what is the indication of carvediolol?

67
Q

what are the problems of mixed beta antagonists?

A

similar to beta blockers
taper dose when d/c

68
Q

what is fenoldopam?

A

dopamine-1 receptor agonist that does not activate alpha 1 or beta receptors for severe HTN

69
Q

what are the effects of fenoldopam?

A

maintains or increases renal perfusion while lowering BP
useful for patients with renal impairment

70
Q

what is the CI of fenoldopam?

A

glaucoma increases IOP

Therapeutics 2 - Exam 5 (14 decks)

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