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Therapeutics 2 - Exam 5 > yang > Flashcards

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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
what is methyldopate?
ester hydrochloride salt that is water soluble and used parenterally
26
what is the clinical use of methyldopa?
HTN especially in pregnancy
27
what drugs are central acting alpha-2 agonists?
clonidine methyldopa guanabenz guanfacine
28
what is the action of methyldopa?
false transmitter that displaced NE from vesicle
29
what are the effects of alpha-2 agonists?
decrease TPR, HR, and renin activity
30
what are the SE of methylopa?
sedation sodium/water retention (combine with diuretic)
31
what is the impact of beta blockers on angina?
reduce myocardial oxygen demand via reduced HR and contractility
32
what is the impact of beta-blockers on cardiac arrhythmia?
slows AV nodal conduction
33
what is the impact of beta blockers in post-MI?
reduce myocardial oxygen demand and slows AV nodal conduction
34
what is the impact of beta-blockers in HTN?
decrease CO and inhibit renin secretion
35
what is the role of beta blockers in congestive HF?
decrease chronic overstimualtion/toxicity of compensatory catecholamines
36
what drugs are non-selective beta blockers?
propranolol timolol nadolol pindolol carteolol
37
what are the indications for propranolol?
HTN (no effect on BP in normotensive individuals) angina cardiac arrhythmias ischemic heart disease prophylaxis for migraines
38
what are the indications of timolol?
open-angle glaucoma HTN angina migraine
39
what are the problems with beta-blockers?
use caution asthmatic due to beta-2 receptor blockade rebound HTN if abrupt d/c so taper dose
40
what are the pharmacologic effects of propranolol?
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
what is the metabolism of propranolol?
extensive first-pass hepatic metabolism lipophilic
42
what is the half life of propranolol?
3-4 hours
43
what is nadolol?
non selective beta blocker that is less lipophilic and mostly excreted unchanged in the urine
44
what is the half life of nadolol?
20 hours
45
what are the clinical uses of nadolol?
HTN angina migraine
46
what is pindolol?
non selective beta blocker with intrinsic sympathomimetic activity that is less likely to cause bradycardia or lipid abnormalities
47
what is the indication of pindolol?
HTN angina migraine best for patients who have severe bradycardia (under 40 BPM) or little cardiac reserve
48
what drugs are non selective beta blockers with intrinsic sympathomimetic activity?
carteolol pindolol
49
what is carteolol
non selective beta blocker with ISA that is less likely to cause bradycardia or lipid abnormalities
50
what is the indication of carteolol?
HTN glaucoma
51
what drugs are beta-1 selective antagonists?
metoprolol bisoprolol atenolol esmolol
52
what are the indications of metoprolol?
HTN angina cardiac arrhythmias ischemic heart disease congestive HF
53
what are the problems associated with metoprolol?
rebound HTN if d/c abruptly so taper dose
54
what is metoprolol?
para-substituted phenyl derivative and selective beta-1 antagonist that is cardioselective and has moderate lipophilicity
55
what is the half life of metoprolol?
3 to 4 hours
56
what is the indication of bisoprolol?
reduces mortality in systolic HF
57
what is atenolol?
cardioselective beta-1 antagonist that has low lipophilicity (water-soluble metoprolol)
58
what is the half life of atenolol?
6 to 9 horus
59
what is the indication of atenolol?
HTN angina
60
what is esmolol?
very short acting (9 minute half life) selective beta-1 antagonist that is administered parenterally and exhibits rapid hydrolysis via esterases
61
what is the indication of esmolol?
supra ventricular tachycardia atrial flutter/fibrillation perioperative HTN
62
what is the CI of esmolol?
sodium bicarbonate
63
what is nebivolol?
3rd generation beta-1 antagonist that possesses vasodilation due to nitric oxide production
64
what is the indication for nebivolol?
HTN
64
what is the effect of beta blockers?
decrease HR, contractility, renin release no effect on BP in normotensive patients
64
what is the indication of beta blockers?
HTN angina cardiac arrhythmias MI HF migraine prophylaxis (propranolol) glaucoma (timolol) intraoperative HTN (esmolol)
64
what is beta blocker withdrawal syndrome?
abrupt d/c can result in exacerbations of HTN or angina and MI
64
what drugs are mixed beta antagonists?
carvediolol labetolol
64
what are the problems of beta blockers?
bradycardia AV block negative inotrophy decrease CO extremity vasoconstriction particualry cold extremities CNS symptoms ED mask of hypoglycemia beta blocker withdrawal syndrome bronchoconstriction
64
what are the CI of beta blockers?
asthma COPD congestive HF (type 4)
65
what is the action of labetolol?
alpha-1 antagonism and non selective beta-1 and beta-2 antagonism with beta-2 partial agonism (3:1 beta-alpha)
65
what is action of carvediolol?
alpha-1 antagonism and non selective beta-1 and beta 2 antagonism (10:1 beta alpha)
65
what are the effects of mixed beta antagonists?
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
what is the indication of labetolol?
HTN emergencies pheochromoctyoma
66
what is the indication of carvediolol?
HF HTN
67
what are the problems of mixed beta antagonists?
similar to beta blockers taper dose when d/c
68
what is fenoldopam?
dopamine-1 receptor agonist that does not activate alpha 1 or beta receptors for severe HTN
69
what are the effects of fenoldopam?
maintains or increases renal perfusion while lowering BP useful for patients with renal impairment
70
what is the CI of fenoldopam?
glaucoma increases IOP

Therapeutics 2 - Exam 5 (14 decks)

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