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KG - Pharmacology 2 > KG - Pharm 2 Exam 2, Antihypertensive Agents > Flashcards

KG - Pharm 2 Exam 2, Antihypertensive Agents Flashcards

1
Q

why use a combo of drugs?

A

increases efficacy and may decrease toxicity (synergism)

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2
Q

DOC HTN?

A

thiazides

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3
Q

when to use thiazides for HTN?

A
  • mild to moderate HTN

- lowers BP by 10-15 mmHg

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4
Q

which thiazide diuretic is a DIRECT vasodilator?

A

indapamide (acts as a CCB)

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5
Q

side effects diuretics?

A
  • impotence
  • gout (hyperurecemia)
  • increased renin secretion
  • K+ depletion (cramps, vent arrythm., ischemia vent fib)
  • REDUCED GLUCOSE INTOLERANCE
  • INCREASED LIPIDS
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6
Q

how can diuretic side effects be avoided?

A

use lower dose than those needed for diuresis

except impotence in elderly not always solved…

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7
Q

in combo therapy how do thiazides work?

A

counteract Na+ and H2O retention in combo therapy (w/ vasodilators, ACEI, Beta blockers)

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8
Q

when should thiazides NOT be used?

A
  • sulfa allergy

- liver metabolism (indapamide)

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9
Q

in which pt populations are thiazides most effective?

A
  • African American > whites

- elderly > younger

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10
Q

when should loop diuretics be used instead of thiazides?

A
  • severe cases HTN (renal insufficiency, CHF)
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11
Q

when should K+ sparing diuretics be used in HTN?

A
  • use w/ loops or thiazides to minimize loss K+

- avoid in combo with other K+ sparing drugs

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12
Q

when to use sympatholytics?

A

combined w/ a diuretic

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13
Q

action of sympatholytics?

A
  • activate baroreflexes & cause Na+/H2O retention

- lower BP by reducing sympathetic vasomotor tone

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14
Q

clonidine/methyldopa MOA?

A
  • stimulate medullary alpha 2 adrenergic receptors, which decreases periph symp nerve activity
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15
Q

clonidine/methyldopa therapeutic effects?

A
  • decreased sympathetic flow

- decreased renin secretion

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16
Q

HTN DOC in pregnancy?

A

methyldopa

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17
Q

which drug lowers HR and CO more - clonidine or methyldopa?

A

clonidine

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18
Q

clonidine/methyldopa adverse effects?

A
  • SEDATION, CNS effects

- xerostomia

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19
Q

methyldopa-specific adverse effects?

A
  • HEMOLYTIC ANEMIA w/ POSITIVE COOMBS TEST
  • hepatotoxic
  • incr prolactin secretion
  • gynecomastia, lactation
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20
Q

clonidine/methyldopa contraindications/precautions?

A
  • not rec for mono therapy
  • SUDDEN WITHDRAWL CLONIDINE = HTN CRISIS
  • antidepressants can inhibit clonidine’s actions
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21
Q

list alpha 1 adrenergic antagonists

A

prazosin, terazosin, doxazosin

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22
Q

prazosin, terazosin, doxazosin - MOA?

A

block alpha 1 without affecting alpha 2 receptors

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23
Q

prazosin, terazosin, doxazosin - indications/therapeutic effects?

A
  • reduce NE vasoconstriction, dilate arteries and veins
  • BP down
  • DO NOT AFFECT LIPIDS!
  • BENEFICIAL IN BPH (relaxes smooth muscle)
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24
Q

prazosin, terazosin, doxazosin - adverse effects?

A
  • postural hypotension w/ first dose = FIRST DOSE PHENOMENON
  • Na+/H2O retention
  • reflex tachy
  • drowsiness, dizziness, palpitations, HA, fatigue sometimes
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25
Q

list non-selective B-blockers

A

propranolol
nadolol
timolol

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26
Q

list selective B1 blockers

A

metoprolol
atenolol
nebivolol
acebutolol

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27
Q

list B-blockers w/ ISA

A

acebutolol

pindolol

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28
Q

how to B-blockers lower BP?

A

block adrenergic receptors in:

  • heart to reduce CO
  • kidneys to reduce renin secretion
  • CNS to reduce SNS vasomotor tone
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29
Q

populations that work best w/ b-blockers?

A

white > black
young > old
mono therapy ONLY in young, white males

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30
Q

when are B-blockers combined with other drugs?

A
  • to counteract tachycardia

- increase renin secretion

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31
Q

when are B-blockers the preferred drug for HTN?

A

for pts with:

  • angina
  • post MI
  • migraine
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32
Q

when are b-blockers the least preferred drug for HTN?

A
  • high phys activity
  • African American
  • asthma
  • DM
  • hypercholesterolemia
  • peripheral vascular dz
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33
Q

which drugs are contraindicated in pregnancy?

A

thiazides, beta blockers

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34
Q

list combined alpha 1 and b-blocker?

A

carvedilol

labetalol

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35
Q

labetalol - indications?

A
  • lower BP in HTN emergencies
  • pregnancy (emergencies, maintenance stronger than methyldopa)
  • lipid neutral
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36
Q

carvedilol - indications?

A
  • HTN, CHF, after MI

- lipid neutral

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37
Q

carvediolol/labetolol - adverse effects?

A
  • orthostatic HTN
  • bronchospasm
  • hepatotoxicity (labetalol = emer only!)
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38
Q

reason to use vasodilators for HTN?

A

ALL VASODILATORS relax smooth muscle

39
Q

which vasodilator also relaxes VEINS?

A

sodium nitroprusside

40
Q

why do the effects of vasodilators diminish with time?

A
  • reflex tachycardia

- increased renin secretion

41
Q

why should you use vasodilators in combo w/ other drugs?

A

to oppose compensatory responses (ie: reflex tachycardia)

42
Q

which vasodilators (and other drugs) are used for CHRONIC ORAL treatment?

A
  • hydralazine
  • minoxidil
  • CCBs
43
Q

which vasodilators (and other drugs) are used as IVs IN EMERGENCIES?

A
  • nitroprusside
  • fenoldopam
  • some CCBs
44
Q

hypotension from vasodilators can also have ___.

A
  • reflex tachycardia
  • increased myocardial contraction
  • increased renin secretion
  • fluid retention
  • HA, flushing
  • palpitations, dizziness
45
Q

when should you prescribe Hydralazine?

A
  • used in CHRONIC THERAPY of SEVERE HTN
  • only used when other treatments failed
  • combined w/ other agents only
  • used in severe hypertension or htn emergencies in pregnancy
46
Q

which drug should be given in HYPERTENSIVE EMERGENCIES in PREGNANCY?

A

hydralazine

47
Q

which vasodilator used for SEVERE HTN?

A

hydralazine

48
Q

hydralazine - adverse effects?

A
  • HA, nausea, anorexia, palpitations, sweating, flushing
  • angina, ischemic arrhythmias
  • SLE IN SLOW ACETYLATORS!
49
Q

which drugs can cause SLE?

A

hydralazine
isoniazid
procainamide

50
Q

which drug is used in HTN emergency situations?

A

sodium nitroprusside

51
Q

sodium nitroprusside - indications/therapeutic effects?

A
  • rapidly lowers BP (minutes) and effect disappears quickly, too
  • HTN emergencies
52
Q

sodium nitroprusside - pharmacokinetics

A
  • IV ONLY
  • metabolized to thiocyanate rapidly
  • excreted by kidney
53
Q

sodium nitroprusside - adverse effects?

A
  • cyanide accumulation
  • met. acidosis
  • arrhythmias
  • excessive hypotension
  • death (in its w/ def in cyanide metabolism)
54
Q

minoxidil - MOA

A
  • opens K+ channels and stabilizes membranes

- DILATES ARTERIOLES BUT NOT VEINS

55
Q

minoxidil - pharmacokinetics

A
  • oral
  • liver metabolism
  • active metabolite
  • 1/2 life 4 hrs, effects last 24 hrs
56
Q

minoxidil - adverse effects?

A
  • tachycardia, palpitations, angina, edema
  • HA, sweating
  • HYPERTRICHOSIS
57
Q

what is topical minoxidil known as?

A

ROGAINE!

58
Q

fenoldopam - MOA?

A
  • SPECIFIC AGONIST ON D1 RECEPTORS

- post synaptic D1 receptor stim relaxes arteriolar smooth muscle

59
Q

fenoldopam - indications/therapeutic effects?

A

HTN emergencies

60
Q

fenoldopam - pharmacokinetics?

A
  • IV
  • liver metabolism
  • 1/2 life = 5 min
61
Q

fenoldopam - adverse effects?

A

reflex tachycardia, HA, flushing

62
Q

list calcium channel blockers (dihydropiridines)

A

nifedipine
nimodipine
other -dipines

63
Q

list calcium channel blockers (others)

A

verapamil

diltiazem

64
Q

CCBs - MOA

A
  • bind to L type channels in myocardium and vasc. smooth muscle
  • closes calcium channels
  • cause decrease in Ca2+ current, long lasting relaxation of vasc smooth muscle, decr cardiac contractility/conduction
65
Q

which types of muscles do CCBs relax?

A

all smooth muscles that depends on calcium for resting tone/contraction

66
Q

which type of muscle is most sensitive to CCBs?

A

VASC SMOOTH MUSCLE but bronchiolar, GI, uterine also relaxed

67
Q

which are more sensitive to CCBs: arterioles or veins?

A

ARTERIOLES are more sensitive than veins

68
Q

major cardiac effects of CCBs?

A
  • neg inotropic effects (less contractility)
  • reduced impulse generation in SA node
  • slowed AV node conduction
69
Q

which is the strongest vasodilator of the CCBs?

A

NIFEDIPINE

70
Q

which has the strongest cardiac effects of the CCBs?

A

VERAPAMIL

71
Q

which drug is the most moderate CCB?

A

DILTIAZEM

72
Q

What are the differences in TISSUE SELECTIVITY between CCBs?

A

Nifedipine: increased HR
Verapamil: decreased HR

73
Q

CCBs pharmacokinetics?

A
  • oral
  • first pass effect
  • (could be IV if needed)
  • renal excretion mostly
  • 1/2 life 3-5 hrs
74
Q

which CCB is most likely to produce reflex tachycardia?

A

NIFEDIPINE:

highest vasodilation –> marked hypotension –> reflex tachycardia

75
Q

what are verapamil and diltiazem less likely to elicit reflex tachycardia?

A
  • have direct inhibition on heart
  • weak dilation
  • directly depress SA/AN node function
76
Q

“-dipines” adverse effect?

A

gingival hyperplasia

77
Q

dihydropyridines adverse effects?

A
  • VASCULAR side effects (ie: HA, flushing, dizziness, peripheral edema)
78
Q

most common side effect of VERAPAMIL?

A

CONSTIPATION

79
Q

which CCBs may cause bradycardia in pts w/ SA node dysfunction?

A

verapamil

diltiazem

80
Q

CCBs contraindications/precautions?

A
  • not for pts w/ LVH
  • contraindicated w/ SA or AV node abnormalities
  • CHF
81
Q

if a pt has high renin, to which two classes of drugs will he/she probably respond?

A

beta blockers and/or inhibitors of RAS (ACEI, ARBs)

82
Q

ACE inhibitors MOA?

A
  • inhibit ACE
  • lower ATII
  • lower BP by reducing vasoconstriction by ATII & release of Aldo
83
Q

how do ACE inhibitors lower BP? (pros?)

A
  • without compromising heart/brain/kidneys
  • no lipid changes
  • no reflex sympathetic activation/tachycardia bc baroreceptor resetting
84
Q

in what group of ppl are ACE inhibitors most effective as MONOTHERAPY?

A

young/middle age > old

less effective in elderly african americans

85
Q

ACE inhibitors are the DOC treatment for HTN for ___

A
  • diabetes
  • chronic renal dz
  • LVH
86
Q

benefits of ACE inhibitors?

A
  • ENHANCE ANTIHYPERTENSIVE EFFECTS OF DIURETIC DRUGS

- BALANCE ADVERSE EFFECTS OF DIURETICS

87
Q

which group of diuretics do you NOT use ACE inhibitors w/?

A

potassium sparing diuretics

88
Q

ACE inhibitors pharmacokinetics?

A
  • oral, parenteral
  • liver metabolism
  • urinary/fecal excretion
89
Q

ACE inhibitors adverse effects?

A
  • hypotension in HYPOVOLEMIC pts
  • dry hacking COUGH
  • ANGIONEUROTIC EDEMA (incr bradykinin)
  • hyperkalemia
  • ACUTE RENAL FAILURE in its w/ bilateral renal artery stenosis
90
Q

ACE inhibitors contraindications/precautions?

A
  • TERATOGENIC! not in 2nd/3rd sem pregnancy!
  • do not use w/ K+ sparing diuretics
  • do not use w/ NSAID COMBO (CAUSES DECREASED VASODILATION)
91
Q

ARBs MOA

A
  • block AT1 receptors selectively w/out affecting AT2 receptors
92
Q

what do ACE inhibitors cause that ARBs do not cause?

A
  • cough, angioedema
93
Q

when is the only time you don’t reach for a thiazide first for HTN?

A

diabetes

KG - Pharmacology 2 (10 decks)

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