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Pharmacology > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

Hydrochlorothiazide: Brand name, others in class

A

HydroDiuril

Chlorthalidone, 5 others

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2
Q

Hydrochlorothiazide: Drug class

A

Pharmacologic: thiazide diuretic
Therapeutic: diuretic, antihypertensive

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3
Q

Hydrochlorothiazide: Pharmacodynamics (5)

A

Block reuptake of CL and NA fron tubular fluid after glomerular filtration
Appears to cause decrease in SVR via unclear mechanism
Lowers BP up to 10-15mmHg in many pts
Useful as monotherapy or in combinations
Chlorthaladone may be slightly better

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4
Q

Hydrochlorothiazide: Pharmacokinetics (5)

A 
F ~70%
Excreted unchanged in urine
Short half life (hours)
Not available in IV formulation
Onset 2h, peak 5h, duration 10h
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5
Q

Hydrochlorothiazide: Toxicity (5)

A 
Allergy to sulfa Abx
Cause K and Mg depletion
Cause Na and Cl depletion, metabolic alkalosis
Volume depletion
Worsen hyperuricemia
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6
Q

Hydrochlorothiazide: Interactions

A

Additive effects with most other antihypertensives

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7
Q

Hydrochlorothiazide: Special considerations (3)

A

More side effects in geriatric patients
Pregnancy Class D
Much less effective in pts with reduced GFR

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8
Q

Hydrochlorothiazide: Indications/dose/route (2)

A

12.5mg or 25mg po every morning

Little benefit, more toxicity when given in higher doses

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9
Q

Hydrochlorothiazide: Monitor (7)

A

BP, weight, edema, K, Mg, BUN, creatinine

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10
Q

Lisinopril: Brand name (2), others in class (3)

A

Prinivil, Zestril

Captopril, enalapril, ramipril (total of 10)

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11
Q

Lisinopril: Drug class (6)

A

Pharmacologic: ACE inhibitor
Therapeutic: antihypertensive, treatment of CHF, preserving renal function, preserving LV function after MI, acute management of MI

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12
Q

Lisinopril: Pharmacodynamics (2)

A

Inhibits conversion of AT I to AT II by ACE

Diminishes both vasoconstriction and stimulation of aldosterone secretion by AT II

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13
Q

Lisinopril: Pharmacokinetics (4)

A

Well absorbed
Onset 1h, peak 6h, duration 24hr
Once a day is fine
Excreted primarily in urine as unchanged drug

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14
Q

Lisinopril: Toxicity (5)

A

Orthostatic hypotension
Use with caution in pts with impaired renal function or RAS (dilates efferent arteriole!)
Caution in pts on diuretics or with aortic stenosis
Angioedema, cough
Acute renal failure

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15
Q

Lisinopril: Interactions (3)

A

Additive effects with most other antihypertensives
NSAIDs may reduce ability to lower BP
Hyperkalemia with KCl, others

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16
Q

Lisinopril: Special considerations (2)

A

Often discontinue diuretics prior to beginning use to reduce hypotension
Category C/D in pregnancy, abnormal cartilage development

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17
Q

Lisinopril: Indications/dose/route

A

Begin 10mg/day, titrate slowly up to 40mg/day max

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18
Q

Lisinopril: Monitor (6)

A

BP, weight, edema, K, BUN, creatinine

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19
Q

Losartan: Brand name

A

CoZaar

7 others in class

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20
Q

Losartan: Drug class (4)

A

Pharmacologic: angiotensin-1 receptor blocker (ARB)
Therapeutic: Antihypertensive, preserve renal function, treatment of CHF

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21
Q

Losartan: Pharmacodynamics

A

Block stimulation of ATI receptor by ATII, thereby reducing vasoconstriction and production of aldosterone

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22
Q

Losartan: Pharmacokinetics (4)

A

F ~30%
Onset 6h
Extensive first pass effect
Active metabolite 40x more potent, much longer half-life

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23
Q

Losartan: Toxicity (3)

A

Dizziness
Orthostatic hypotension
Worsening of renal failure

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24
Q

Losartan: Interactions

A

Additive effects with most other antihypertensives

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25
Q

Losartan: Special Considerations (2)

A 
Pregnancy class C/D
Use care in pts on diuretics, with RAS, or mitral or aortic stenosis
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26
Q

Losartan: Indications/dose/route

A

For HTN, daily doses 25-100mg q day

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27
Q

Losartan: Monitor (6)

A

BP, weight, edema, electrolytes, BUN, creatinine

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28
Q

Nitroprusside: brand name (2)

A

Nipride, Nitropress

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29
Q

Nitroprusside: Drug class (5)

A

Pharmacologic: vasodilator
Therapeutic: antihypertensive, management of severe CHF, management of pulmonary HTN, produce controlled hypotension to reduce bleeding during surgery

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30
Q

Nitroprusside: Pharmacodynamics (3)

A

Acts directly on vascular SM to cause dilation of both veins and arterioles
Metabolized to release CN- and NO, which -> guanylate cyclase -> production of cGMP from GTP -> vasodilation
cGMP then hydrolyzed to GMP by PDE

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31
Q

Nitroprusside: Pharmacokinetics (4)

A

Only route is IV
Rapid onset and cessation (minutes) -> minute-to-minute titration
CN- metabolite converted to SCN in liver, then excreted in urine
Must be given by continuous infusion, no longer than 24 hours

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32
Q

Nitroprusside: Toxicity (4)

A

Excessive hypotension
Accumulation of CN- and thiocyanate
Headache
Decreased blood flow to brain

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33
Q

Nitroprusside: Interactions

A

Additive effects with most other antihypertensives

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34
Q

Nitroprusside: Special considerations (3)

A

Monitor pts VERY closely - must be in ICU with arterial line, no longer than 24 hrs
Avoid high infusion rates or prolonged infusions to prevent accumulation of CN-
Use caution in pts with increased intracranial pressure

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35
Q

Nitroprusside: Indications/dose/route

A

For treatment of hypertensive crisis, given as IV infusion at 0.3-10mcg/kg/min, NO longer than 24 hours

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36
Q

Nitroprusside: Monitor (4)

A

BP, HR, metabolic acidosis

Most often requires arterial line

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37
Q

Hydralazine: Brand name

A

Apresoline

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38
Q

Hydralazine: Drug class (4)

A

Pharmacologic: peripheral vasodilator
Therapeutic: antihypertensive, treatment of CHF, vasodilator

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39
Q

Hydralazine: Pharmacodynamics (3)

A

Direct acting vasodilator
Induces endothelium to produce NO (different from nitroprusside), which then -> to SM cells and -> production of cGMP
Minimal venodilating effect

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40
Q

Hydralazine: Pharmacokinetics (6)

A

Given po, im, iv
Metabolized extensively in GI mucosa and in liver
Eventually excreted as metabolites in urine
F ~40%
Onset 30 after po dose, 10 min after iv dose
Persist for 2-6 hours

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41
Q

Hydralazine: Toxicity (2)

A

More dangerous in pts with renal disease, prior stroke, angina
Watch for hypotension, edema, occasionally drug-induced lupus

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42
Q

Hydralazine: Interactions

A

Additive effects with most other antihypertensives

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43
Q

Hydralazine: Special considerations (2)

A

Never use as chronic oral monotherapy for treatment of HTN, will -> edema, reflex tachycardia (rarely used today except for final month of pregnancy with extreme HTN)
Concern giving to patients with CAD

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44
Q

Hydralazine: Indications/dose/route

A

Dose 10-50 mg po 4x/day

45
Q

Hydralazine: Monitor (6)

A

BP, weight, edema, BUN, creatinine, symptoms of lupus or angina

46
Q

Verapamil: Brand name (2), others in class (4)

A

Isoptin, Calan

Others: nifedipine, amlodipine, diltiazem, nicardipine (total 8)

47
Q

Verapamil: Drug class (3)

A

Pharmacologic: Ca entry blocker
Therapeutic: antihypertensive, antianginal, antiarrhythmic

48
Q

Verapamil: Pharmacodynamics (5)

A

Reduces BP by inhibiting influx of Ca through slow channels, -> dilating peripheral arterioles
Produces negative inotropic effect
**Angina: reduces afterload, decreasing oxygen consumption
Inhibits spasm of coronary arteries in vasospastic angina
Blocks reentry paths through AV nodes in paroxysmal SVT

49
Q

Verapamil: Pharmacokinetics (6)

A 
Absorbed rapidly, but F ~30%
Also available in SR tablets
Cleared by kidney and liver (produces active metabolites
Onset 2h po, 1-5 min IV
Half life 6-12h
May be given po or IV
50
Q

Verapamil: Toxicity (4)

A

Hypotension, AV block, worsening of CHF, bradycardia

51
Q

Verapamil: Interactions (2)

A

Additive effects with most other antihypertensives

Additive toxic effects on heart when given with beta-blockers

52
Q

Verapamil: Special considerations (3)

A

Use reduced dose in pts with both renal and hepatic disease
Short-acting nifedipine (and similar CEBs) can increase risk of MI
Pregnancy C

53
Q

Verapamil: Indications/dose/route

A

80 mg 3x/day, or 240mg SR once daily

54
Q

Verapamil: Monitor (3)

A

Weight, edema, BP

55
Q

Clonidine: Brand name, others in class (1)

A

Catapres

Other: Methyldopa

56
Q

Clonidine: Drug class (3)

A

Pharmacologic: central alpha-2 agonist
Therapeutic: antihypertensive, adjunct to Rx of opioid withdrawal, prophylaxis of migraine

57
Q

Clonidine: Pharmacodynamics

A

Stimulates alpha-2 adrenoceptors in brainstem -> down-regulation of sympathetic output

58
Q

Clonidine: Pharmacokinetics (3)

A

Onset 1h, duration 8h
F ~ 85%
Also available as cutaneous patch

59
Q

Clonidine: Toxicity (3)

A

Withdraw gradually because of risk of rebound HTN
Risk of bradycardia in sinus node disease
Lethargy, fatigue, depression

60
Q

Clonidine: Interactions (2)

A

Additive effects with most other antihypertensives

Additive sedation with other CNS drugs

61
Q

Clonidine: Special Considerations (2)

A 
Pregnancy class C
Avoid in pts with renal insufficiency
62
Q

Clonidine: Indications/dose/route

A

Begin with 0.1mg po bid, up to 1.2mg per day

Transdermal: begin with 0.1mg per 24 hr as a 7 day patch

63
Q

Clonidine: Monitor (3)

A

BP, HR, fatigue

64
Q

Trimethaphan: Brand name, others in class

A

Arfonad

No others in class

65
Q

Trimethaphan: Drug class

A

Pharmacologic: ganglionic transmission blocker
Therapeutic: antihypertensive (acute, by IV)

66
Q

Trimethaphan: Pharmacodynamics (2)

A

Blocks nicotinic transmission within both sympathetic and parasympathetic ganglia (Nn receptors)
Produces veno- and vasodilatation

67
Q

Trimethaphan: Pharmacokinetics (3)

A

Useful only when given IV
Produces fall in BP within minutes
Partly metabolized, partly excreted by kidneys

68
Q

Trimethaphan: Toxicity (3)

A

Watch for sudden, severe drop in BP
Fall in HR
Reduction in just about any sympathetic or parasympathetic response

69
Q

Trimethaphan: Interactions

A

Additive effects with most other antihypertensives

70
Q

Trimethaphan: Special considerations (2)

A

Pts miserable, only used during general anesthesia

Helps to tilt pt to help control BP

71
Q

Trimethaphan: Indications/dose/route

A

Give by IV infusion to treat HTN crisis, or for controlled hypotension during cardiovascular surgery

72
Q

Trimethaphan: Monitor (2)

A

Minute to minute monitoring of BP and HR

73
Q

Reserpine: Brand name, others in class

A

No brand name

74
Q

Reserpine: Drug class

A

Pharmacologic: Rauwolfia alkaloid
Therapeutic: Antihypertensive

75
Q

Reserpine: Pharmacodynamics (3)

A

Binds to vesicles that contain NE OR serotonin, preventing their uptake and depleting the neuron of NE or serotonin
Takes 2-3 weeks to deplete
Includes neurons and the adrenal medulla

76
Q

Reserpine: Pharmacokinetics

A

Good oral bioavailability, but biologic effects take 2-3 weeks (slow depletion of NE/serotonin from vesicles)

77
Q

Reserpine: Toxicity (3)

A

Dizziness
Orthostatic hypotension
Depression!!! (NOT used today!)

78
Q

Reserpine: Interactions

A

Additive effects with most other antihypertensives

79
Q

Reserpine: Special considerations (2)

A

FDA approved in 1953

First antihypertensive drug + first sympatholytic drug approved

80
Q

Reserpine: Indications/dose/route

A

For HTN, 0.1-0.2mg po qd

81
Q

Reserpine: Monitor (3)

A

BP, sympathetic tone, depression

82
Q

Atenolol: Brand name, others in class (2)

A

Tenormin

Others: Propranolol, metoprolol (Toprol XL)

83
Q

Atenolol: Drug class (4)

A

Pharmacologic: beta-adrenoceptor blocker (beta-1 specific)
Therapeutic: antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal

84
Q

Atenolol: Pharmacodynamics (2)

A

Binds directly to beta-receptors (beta-1&raquo_space; beta-2) -> lower BP via several mechanisms (lower CO, lower RAAS activation)
Less effective in preventing strokes than other drugs, so used less often as initial monotherapy

85
Q

Atenolol: Pharmacokinetics (5)

A 
Available po or IV
Variable oral F
Onset 1-2h, duration 12-24h
Can be given once per day
Renally excreted (longer half life)
86
Q

Atenolol: Toxicity (4)

A

Excessive hypotension
Bradycardia
Heart block can worsen CHF if severe (but good for mild to moderate CHF)
Worsen bronchospasm in severe asthmatics

87
Q

Atenolol: Interactions (2)

A

Additive effects with most other antihypertensives

Additive AV block with CEBs

88
Q

Atenolol: Special considerations (3)

A

May be especially useful in HTN pts with exertional angina, MI, a. fib
Watch out for abrupt withdrawal
No longer first line drug unless other indications exist

89
Q

Atenolol: Indications/dose/route

A

For treatment of HTN, 25-100 mg per day, in one or two doses

90
Q

Atenolol: Monitoring (3)

A

BP, HR, exercise tolerance

91
Q

Prazosin: Brand name, others in class (3)

A

Minipress

Terazosin, doxazosin, tamsulosin

92
Q

Prazosin: Drug class (4)

A

Pharmacologic: alpha-1 adrenoceptor blocker
Therapeutic: Antihypertensive, treatment of BPH, treatment of Raynaud’s syndrome, treatment for kidney stones

93
Q

Prazosin: Pharmacodynamics

A

Blocks alpha-1 receptors on arterioles and veins, thereby inhibiting NE-mediated vasoconstriction and venoconstriction

94
Q

Prazosin: Pharmacokinetics (4)

A

Available po or transdermal
Variable oral bioavailability (~60%)
Onset 2h, duration 12-24h
Extensively metabolized in liver

95
Q

Prazosin: Toxicity (3)

A

Excessive hypotension with passing out, especially orthostatic, especially in pts on diuretics

96
Q

Prazosin: Interactions

A

Additive effects with most other antihypertensives, especially diuretics

97
Q

Prazosin: Special considerations (2)

A

Start gradually at bedtime to avoid first-time passing out

Male pts with BPH?

98
Q

Prazosin: Indications/dose/route

A

As monotherapy, begin with 1mg tid, advance to 20mg per day divided tid

99
Q

Prazosin: Monitor (3)

A

BP, weight, edema

100
Q

Labetalol: Brand name, others in class

A

Trandate

Others (KNOW): Carvedilol/Coreg(tm)

101
Q

Labetalol: Drug class (2)

A

Pharmacologic: Alpha and beta receptor blocker
Therapeutic: Antihypertensive, treatment of CHF

102
Q

Labetalol: Pharmacodynamics (2)

A

Reduces BP by blocking access of NE to beta-receptors and alpha-1 receptors -> lowering BP by several different mechanisms
Pts differ in degree of beta- vs alpha-blockade

103
Q

Labetalol: Pharmacokinetics (3)

A

Excellent absorption but high first pass effects (F~25%)
Onset 1-2h po, 2-5min IV
Extensively metabolized in liver by IID6

104
Q

Labetalol: Toxicity (3)

A 
Avoid in pts with bradycardia, heartblock, CHF, asthma, shock
Use caution in pts with cardiomyopathy, pheochromocytoma
Pregnancy class D
105
Q

Labetalol: Interactions

A

Additive effects with most other antihypertensives

106
Q

Labetalol: Special considerations (3)

A

Use reduced doses in pts with impaired liver function
Dizziness is most troubling early side effect
Most often used for hypertensive crisis (as with nitroprusside)

107
Q

Labetalol: Indications/dose/route (2)

A

Most commonly given IV with initial small boluses of 20mg, followed by continuous infusion at 2mg/min
Not usually given po for chronic treatment (80mg tid or 240mg SR qd)

108
Q

Labetalol: Monitor (2)

A

BP, HR

Pharmacology (10 decks)

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