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PHM 521 > Antihypertension Drugs > Flashcards

Antihypertension Drugs Flashcards

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1
Q

First line antihypertensives

A

thiazide diuretics, ACEI, ARB, Calcium Channel Blockers

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2
Q

diuretics

A

thiazide diuretics, loop diuretics, mineralocorticoid (aldosterone) receptor antagonists, potassium sparing diuretics

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3
Q

RAAS blockers

A

ACEI, ARB, direct renin inhibitors

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4
Q

direct vasodilators

A

calcium channel blockers, hydralazine, minoxidil

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5
Q

sympatholytic agents

A

beta blockers, clonidine

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6
Q

thiazide diuretics can lower BP up tp ___ mmHg and can be used as _____

A

thiazide diuretics can lower BP up to 10-15 mmHg and can be used as a monotherapy for mild htn, but is often used in combination

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7
Q

chlorthalidone

A

hygroton/thalitone is a first line thiazide diuretic

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8
Q

hydrochlorothiazide;indapamide

A

lozol is a first line thiazide diuretic

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9
Q

metolazone

A

zaroxolyn is a first line thiazide diuretic

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10
Q

thiazide diuretic MOA

A

increases na, water and cl excretion by blocking reabsorption in distal convoluted tubule

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11
Q

thiazide diuretic contraindications

A

hypersensitivity to sulfonamides (low risk of cross reactivity), anuria

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12
Q

thiazide diuretic adr

A

dizziness, hyperuricemia, hyponatremia, hypokalemia, hypomagnesemia, hypercalcemia, pancreatitis

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13
Q

thiazide diuretic key PK/PD parameters

A

secreted by organic acid secretory system in the proximal tubule which completes with secretion of uric acid –> elevates levels of uric acid

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14
Q

thiazide diuretic notes

A

not as effective if CrCl < 30ml/min (chlorthalidone preferred), avoid NSAIDs, avoid in gout, less effective w/ low GFR, take in morning

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15
Q

furosemide

A

lasix is a loop diuretic

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16
Q

loop diuretic moa

A

actively secreted via nonspecific organ acid transport system into the lumen of the thick ascending loop of Henle, decreasing Na absorption

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17
Q

loop diuretic contraindication

A

anuria

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18
Q

loop diuretic adr

A

hyperuricemia, hypokalemia, hypomagnesemia, dizziness, AKI, ototoxicity

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19
Q

loop diuretic DDI

A

increased risk of ototoxicity with aminoglycosides

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20
Q

loop diuretic notes

A

results in most fluid loss, black boxed for profound fluid and electrolyte loss, more potent than thiazides, preferred in patients with HF, consider ethacrynic acid with true sulfa allergy

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21
Q

PK/PD of furosemide

A

loop diuretic, 40-70% bioavailability, lasts 4-8 hrs, 1-2 hr half life, mainly renal elimination

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22
Q

PK/PD of torsemide

A

loop diuretic, 90% bioavailability, lasts 8-12 hrs, 3.5 hr half life, mainly hepatic elimination

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23
Q

PK/PD of bumetanide

A

loop diuretic, 90% oral bioavailability, 3-6 hr duration, ~1 hr half life, half renal and half hepatic elimination

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24
Q

PK/PD of ethacrynic acid

A

loop diuretic with 100% oral bioavailability, 2-4 hr IV, 12 hr duration orally, 2-4 hr half life, renal elimination

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25
spironolactone
aldactone/carospir is a mineralocorticoid receptor antagonist (MRA)
26
eplerenone
inspra is a mineralocorticoid receptor antagonist (MRA)
27
mineralocorticoid receptor antagonist (MRA) moa
competes with aldosterone for receptor sites in the distal renal tubules increasing na, cl and water excretion whole conserving k and h ions, may block effect of aldosterone on smooth muscle
28
mineralocorticoid receptor antagonist (MRA) contraindications
anuria, hyperkalemia
29
mineralocorticoid receptor antagonist (MRA) adr
dehydration, hyponatremia, dizziness, cardiac arrhythmias due to electrolyte abnormalities spironolactone: gynecomastia, breast tenderness, impotence eplerenone: increased TG
30
mineralocorticoid receptor antagonist (MRA) key PK/PD
spironolactone: binds with high affinity to androgen receptor which causes gynecomastia and decreased libido eplerenone: much greater selectivity
31
mineralocorticoid receptor antagonist (MRA) DDi
eplerenone: strong CYP3A4 inhibitors will increase concentrations
32
mineralocorticoid receptor antagonist (MRA) notes
minimally efficacious blood pressure control when used as a monotherapy, preferred in aldosteronism and resistant htn, use with thiazide or loop diuretic to combat K loss
33
triamterene
maxzide is a potassium sparing diuretic
34
amiloride
potassium sparing diuretic
35
potassium sparing diuretic moa
competitive inhibition of epithelial na channel in collecting duct of nephron to decrease na reabsorption and increase k reabsorption
36
potassium sparing diuretic contraindications
hypersensitivity to sulfonamides
37
potassium sparing diuretic adr
hyperkalemia, hypotension, dizziness, ha, gout, sjs
38
potassium sparing diuretic PK/PD
amiloride has a longer duration of action that triamterene (24 > 8)
39
potassium sparing diuretic notes
almost always in combination tablet to decrease rates of hyperkalemia with thiazide diuretics, avoid if CrCl <45ml/min, can be used with thiazide or loop diuretic to combat K loss
40
lisinopril
prinivil/zestril is an ACEI
41
ACEI moa
competitive angiotensin converting enzyme inhibitor that prevents stimulation of angiotensin II receptor which is responsible for vasoconstriction
42
ACEI contraindications
history of acei induced, hereditary, or idiopathic angioedema, pregnancy
43
ACEI adr
hyperkalemia, aki, dizziness, dry cough, angioedema, liver failure
44
ACEI key PK/PD
renally eliminated, inhibits breakdown of bradykinin causing dry cough and angioedema
45
ACEI DDI
increased risk of hyperkalemia and/or angioedema in combination with other RAAS inhibitors
46
ACEI notes
if side effects- try ARB, combinations available (hydrochlorothiazide, ccb), target organ protection, do not use if K about 5mmol/L, do not use other RAAS
47
valsartan
Diovan is an ARB
48
ARB moa
selective reversible angiotensin II receptor
49
ARB contraindications
pregnancy
50
ARB adr
hyperkalemia, AKI, dizziness, angioedema, rhabdomyolysis
51
ARB DDI
increased risk of hyperkalemia and/or angioedema in combination with other RAASi
52
ARB notes
may use first if trying to prevent side effects like dry cough, combinations available (hydrochlorothiazide, CCB), target organ protection, do not use if K >5mmol/L, no washout period when transitioning, less dry cough /angioedema
53
amlodipine
norvasc is a DHP CCB
54
nifedipine
procardia is a DHP CCB
55
DHP CCB moa
inhibits calcium ions from entering slow channels of vascular smooth muscle- leading to vasodilation
56
DHP CCB adr
peripheral and pulmonary edema, hepatotoxicity, thrombocytopenia
57
DHP CCB key PK/PD
may cause reflex sympathetic activation --> slight tachycardia and increase in cardiac output amlodipine may take at least 3 days to 1 week to see full lowering effects
58
DHP CCB ddi
major substrate of CYP3A4
59
DHP CCB notes
immediate release nifedipine should not be used as it has increased risk for MI and mortality, can take up to one week to see full effect
60
diltiazem
cardizem is a NONDHP CCB
61
verapamil
calan is a NONDHP CCB
62
NONDHP CCB moa
inhibits ca ions from entering smooth muscle and myocardium, causing vasodilation and slowing of AV node
63
NONDHP CCB contraindications
2nd or 3rd degree heart block
64
NONDHP CCB adr
peripheral edema, pulmonary edema, ha, heart failure, heart block, hepatotoxicity
65
NONDHP CCB key PK/PD
verapamil has the greatest depressive effects on SNS
66
NONDHP CCB ddi
major substrates of CYP3A4, moderate inhibitors of CYP3A4 - ddi worse with verapamil
67
hydralazine
apresoline is a vasodilator
68
hydralazine moa
direct vasodilation
69
hydralazine contraindications
CAD- causes reflex tachycardia and angina
70
hydralazine adr
dizziness, reflex tachycardia, DILE at high doses
71
hydralazine PK/PD
variable duration and effect, short half-life that requires frequent dosing
72
hydralazine notes
dosing for htn is 4x daily, less reflex tachycardia risk than minoxidil
73
minoxidil moa
direct vasodilation
74
minoxidil contraindications
CAD- causes reflex tachycardia and angina
75
minoxidil adr
dizziness, reflex tachycardia, hypertrichosis, pericarditis
76
minoxidil notes
causes fluid and water retention- should be given with a diuretic, should be given with a beta blocker to prevent tachycardia, extremely potent vasodilator, increased risk of reflex tachycardia
77
metoprolol
lopressor/toprol is a beta blocker
78
beta blocker moa
inhibits beta 1/2 receptors decreasing HR and myocardial contractility- varies based on selectivity
79
beta blocker contraindications
severe bradycardia
80
beta blocker adr
dizziness, fatigue, reduced exercise tolerance, bronchospasm, insomnia, impotence
81
beta blocker notes
avoid abrupt withdrawal, patients may feel fatigued at start- this will abate with time, can mask feelings of low glucose, use with caution in patients with severe bronchospastic disease, can enhance hypoglycemic effects
82
beta blocker ddi
additive av nodal blockade with NONDHP CCB
83
beta 1 selective blockers
atenolol, betaxolol, bisoprolol, esmolol, metoprolol, nebivolol, acebutolol
84
blockers with beta 1 and 2 activity
carvedilol, labetalol, nadolol, pindolol, propranolol, sotalol, timolol
85
beta blockers with alpha 1 blockagte
carvedilol, labetalol
86
beta blockers with NO stimulation
nebivolol
87
beta blockers with SNS activity
acebutolol, pindolol
88
clonidine
catapres/kapvay is an alpha 2 agonist
89
alpha 2 agonist moa
stimulates alpha 2 receptors resulting in reduced sympathetic outflow from CNS
90
alpha 2 agonist adr
dry mouth, somnolence/fatigue/sedation, constipation, clonidine patch may have local irritation as well
91
alpha 2 agonist PK/PD
lipid soluble, short half-life- dosed at least 2x daily
92
alpha 2 agonist notes
avoid abrupt discontinuation, use patch for 7 days- takes 2-3 days onset- oral dosing needed at that time
93
NON DHP CCB notes
cyp3a4 major substrate inhibitor (dose adjustments for lovastatin/simvastatin), avoid in patients w HFrEF, avoid routine use with beta blockers, multiple brands exist, diltiazem is the only brand w capsules that can be sprinkled over food
94
aliskiren
tekturna is a direct renin inhibitor should not be used with other RAAS, long half life, lack of data, expensive
95
doxazosin
cardura is an alpha 1 agonist can treat htn and bph in men, increase risk of hf and orthostatic hypotension

PHM 521 (11 decks)

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