Vasodilators etc Flashcards

1
Q

Long-term outpatient therapy of severe or resistant hypertension

A

Hydralazine

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2
Q

Hypertensive emergencies

A

nitroprusside

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3
Q

Hypertensive emergencies; angina

A

Nitrates

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4
Q
  1. Long-term outpatient therapy of hypertension
  2. hypertensive emergencies
  3. angina
A

Verapamil

diltiazem

nifedipine

amlodopine

Reduction of calcium influx

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5
Q
A
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6
Q

Hyperpolarization of smooth muscle membrane through opening of potassium channels

A

Minoxidil

Diazoxide

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7
Q

Long-term outpatient therapy of severe or resistant hypertension

A

Minoxidil

-Hyperpolarization of smooth muscle membrane through opening of potassium channels

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8
Q

Hypertensive emergencies (and not a NO releaser)

A

Diazoxide

-Hyperpolarization of smooth muscle membrane through opening of potassium channels

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9
Q

Hypertensive emergencies, and not a NO releaser, potassium channel opener, or a calcium influx inhibitor

A

Fenoldopam: Activation of dopamine receptors

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10
Q

excessive hypotension, dizziness, headache, peripheral edema, flushing, tachycardia, rash, and gingival hyperplasia have been reported

A

Dihydropyridines

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11
Q

Dizziness, headache, peripheral edema, AV block, bradycardia, heart failure, lupus-like rash, pulmonary edema, coughing, and wheezing are possible

A

diltiazem

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12
Q

Dizziness, headache, peripheral edema, constipation, AV block, bradycardia, heart failure, pulmonary edema, coughing, and wheezing are possible

A

verapamil, non-DHP

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13
Q

slow heart rate, can slow atrioventricular conduction, can cause heart block, and are contraindicated in patients also taking a beta-blocker

A

Non-DHPs (verapamil > diltiazem)

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14
Q

does not decrease AV conduction and therefore can be used more safely than non-DHPs in the presence of AV conduction abnormalities

A

Nifedipine

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15
Q

may increase digoxin blood levels through a pharmacokinetic interaction

A

verapamil

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16
Q

Additive with other vasodilators

A

DHPs

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17
Q

Additive with other cardiac depressants and hypotensive drugs

A

non-DHPs

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18
Q

Long-term outpatient therapy of hypertension; hypertensive emergencies; angina

A

CALCIUM CHANNEL BLOCKERS

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19
Q

prototype DHPs, MOA

A

Amlodipine and nefidipine

MOA: Blocks L-type calcium channels in vasculature > cardiac channels

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20
Q

Prototype non-DHP drugs, MOA

A

Non-Dihydropyridines

(1) Prototypes: Verapamil, Diltiazem
(2) MOA: Nonselective block of vascular and cardiac L-type calcium channels

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21
Q
  1. cause vasodilation–> decreases peripheral resistance
  2. arterioles are more sensitive than veins
  3. orthostatic hypotension is not usually a problem
  4. relaxation of arteriolar smooth muscle leads to decreased afterload and decreased O2 demand by the heart
A

Ca channel blockers (CCBs)

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22
Q

CCBs: block channels in smooth muscle at much lower concentrations

A

non-DHPs: this is significant because while they have more cardiac effects, their cardiac effects are negligible at effective therapeutic concentrations

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23
Q

(t1/2) of 35-50 hours

A

amlodipine: the other CCBs typically 2-12 hrs

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24
Q

Excessive hypotension–> stroke & MI

Hypotensive effects worse in

  1. patients with renal failure (due to reduced protein binding
  2. patients pretreated with β-blockers to prevent reflex tachycardia
A

K+ channel opener: Diazoxide

25
Q

in which patients should K channel opener diazoxide be administered in smaller doses than other patient populations?

A
  1. renal failure patients (reduced protein binding)
  2. patients pre-tx with beta blockers for reflux tachycardia
  3. hyperglycemic patients, especially if they have renal insufficiency
26
Q

in which patients should diazoxide be avoided?

A

patients with ischemic heart disease due to propensity for angina,

ischemia, and cardiac failure

27
Q

contrast dizoxide to other diuretics

A

diazoxide causes sodium and water retention; this is rarely a problem due to the typical short duration of use

28
Q

Common: headache, sweating, hypertrichosis (abnormal hair growth)

A

Minoxidil

29
Q

use is associated with

  1. reflex sympathetic stimulation
  2. sodium + fluid retention –> tachycardia, palpitations, angina, and edema
A

minoxidil

30
Q

must be used in combination with a beta blocker and loop diuretic to avoid AEs

A

minoxidil must be used in combination with a β-blocker and loop diuretic in order to avoid these effects

31
Q

Long-term outpatient therapy of severe hypertension and in topical formulations used to stimulate hair growth

A

minoxidil

32
Q

Administered by continuous IV infusion due to rapid metabolism and short half-life (10 min)

A

fendolapam

33
Q

Tachycardia, headache, and flushing

A

fendolapam

34
Q

Should be avoided in patients with glaucoma due to increases in intraocular pressure

A

D1 receptor agonist fendolapam

35
Q

Hypertensive emergencies, peri- and postoperative hypertension

A

fendolapam

36
Q

Stimulates release of nitric oxide from endothelium resulting in increased cGMP levels

A

Hydralazine

37
Q

1) dilation of arterioles, but not veins; reflex tachycardia
2) hyperpolarizes the smooth muscle membrane, reducing the probability of contraction; arteriolar dilator resulting in reduced systemic vascular resistance and mean arterial pressure
3) hyperpolarizes the smooth muscle membrane, reducing the probability of contraction. dilation of arterioles, but not veins; more efficacious than hydralazine
4) Administered by continuous IV infusion due to rapid metabolism and short half-life (10 min)
5) Metabolism occurs in part via acetylation, so bioavailability is variable among individuals dependent on rate of acetylation
6) Powerful dilation of arterial and venous vessels, reduces peripheral vascular resistance and venous return
7) Rapid metabolism results in rapid onset and short duration of effect; Should be administered by IV infusion with continuous monitoring of arterial blood pressure
8) Relaxes most types of smooth muscle (veins > arteries); virtually no direct effect on cardiac or skeletal muscle
9) Increases venous capacitance; decrease ventricular preload; pulmonary vascular pressures and heart size are reduced. In the absence of heart failure, cardiac output is reduced.
10) Decreases platelet aggregation

A
  1. pharmacodynamics of hydralazine
  2. pharmacokinetics of diazoxide
  3. pharmacokinetics of minoxidil
  4. pharmoacokinetics of fendolapam
  5. pharmacokinetics of hydralazine
  6. pharmocodynamics of nitroprusside
  7. pharmacokinetics of nitroprusside
  8. pharmacodynamics of organic nitrates
  9. pharmacodynamics of organic nitrates
  10. pharmacodynamics of organic nitrates
38
Q

headache, nausea, anorexia, palpitations, sweating, and flushing

A

hydralazine

39
Q

In patients with ischemic heart disease, reflex tachycardia and sympathetic stimulation may provoke angina or ischemic arrhythmias

A

hydralazine

40
Q

peripheral neuropathy, drug fever

A

rare outcome of hydralazine use

41
Q

Long-term outpatient therapy of hypertension. Combination with nitrates is effective in heart failure and should be considered in patients, especially African-Americans, with both hypertension and heart failure

A

hydralazine

42
Q

First-line therapy for hypertension in pregnancy, with methyldopa

A

hydralazine

43
Q

Parenteral formulation is useful in hypertensive emergencies.

A

hydralazine

44
Q

results in increased cGMP levels

A

MOA nitroprusside

45
Q
A
46
Q

Powerful dilation of arterial and venous vessels, reduces peripheral vascular resistance and venous return

A

nitroprusside

47
Q
  1. Excessive hypotension…..Cyanide and thiocyanate are released during metabolism; this is typically not problematic because it is used only briefly
  2. metabolic acidosis, arrhythmias, excessive hypotension, and death can occur if infusions are administered for several days
A

1 = nitroprusside

2 = nitroprusside (as well)

48
Q

Hypertensive emergencies; acute decompensated heart failure

A

nitroprusside

49
Q

Release of nitric oxide via enzymatic metabolism

A

organic nitrates

50
Q

Common: orthostatic hypotension, syncope, throbbing headache

A

organic nitrates

51
Q

Contraindicated if intracranial pressure is elevated

A

organic nitrates

52
Q

Synergistic hypotension with phosphodiesterase type 5 inhibitors (sildenafil, tadalafil, vardenafil)

A

organic nitrates

53
Q

Hypertensive emergencies, angina, heart failure

A

organic nitrates

54
Q

1) excessive hypotension, dizziness, headache, peripheral edema, flushing, tachycardia, rash, and gingival hyperplasia have been reported, potentially increased risk of MI, stroke, or death in patients receiving short term tx for HTN

2) Dizziness, headache, peripheral edema, constipation, AV block, bradycardia, heart failure, lupus-like rash. pulmonary edema, coughing, and wheezing are possible, can slow atrioventricular conduction, can cause heart block, and are contraindicated in patients also taking a beta-blocker

A

1 = CCB, DHPs

2 = CCB, Non-DHPs

55
Q
  1. Hypotensive effects are greater in patients with renal failure (due to reduced protein binding) and in patients pretreated with β-blockers to prevent reflex tachycardia; smaller doses should be administered to these patients
  2. associated with reflex sympathetic stimulation and sodium and fluid retention resulting in tachycardia, palpitations, angina, and edema; must be used in combination with a β-blocker and loop diuretic in order to avoid these effects
A

1 = diazoxide

2 = minoxidil

56
Q
  1. cyanide poisoning (metabolic acidosis, arrhythmias, excessive hypotension, and death) can occur if infusions are administered for several days
  2. orthostatic hypotension, syncope, throbbing headache, contraindicated if intracranial pressure is elevated, increased generation of oxygen free radicals
A
  1. nitroprusside
  2. nitroglycerin (prototype organic nitrates)
57
Q

Diminished availability of calcitonin gene-related peptide (CGRP). Compensatory responses contributing to the development of tolerance: tachycardia, increased cardiac contractility, retention of salt and water.

A

organic nitrates

58
Q
  1. sublingual route of administration is typically used to avoid first-pass
  2. Oral, transdermal, and buccal preparations are available when longer duration of action is needed
A