Kruse Part 2 Flashcards

1
Q

Vasodilators include

A
  • calcium channel blockers
  • potassium channel openers
  • dopamine agonist
  • NO donors
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2
Q

Calcium channel blockers (CCBs) include

A

Dihydropyridines

non-dihydropyridines

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3
Q

Dihydropyridines include

A
amlodipine
clevidipine
felodipine
isradipine
nicardipine
nifedipine
nisoldipine
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4
Q

Non-dihydropyridines

A

diltiazem

verapamil

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5
Q

Potassium channel openers include

A

diazoxide

minoxidil

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6
Q

Dopamine agonists include

A

fenoldopam

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7
Q

NO donors include

A

hydralazine
nitroprusside
organic nitrates

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8
Q

Calcium channel blockers

A

-all CCBs bind to L-type Ca2+ channels

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9
Q

Non-dihydropyridine effects

A

-prominent cardiac effects, but also act at vascular tissues

verapamil>diltiazem

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10
Q

Dihydropyridines (DHPs) effects

A
  • predominantly arteriolar vasodilation effects

- amlodipine, etc.

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11
Q

CCBs Adverse Effects and Toxicity

A
  • generally very well tolerated
  • excessive vasodilation–dizziness, hypotension, headache, flushing, nausea; diminished by long-acting formulations and long half-life agents
  • constipation (especially verapamil), peripheral edema, coughing, wheezing, pulmonary edema
  • use of verapamil/diltiazem with a beta blocker is contraindicated because of the potential for AV block
  • verapamil/diltiazem should not be used in patients with ventricular dysfunction, SA or AV nodal conduction defects and systolic BP
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12
Q

CCBs clinical uses

A
  • hypertension–most useful when combined with another agent to counteract the reflex cardiovascular responses
  • hypertensive emergencies: parenteral formulations
  • angina: reduction of O2 demand makes particularly useful
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13
Q

Potassium Channel Openers MOA

A

-increased potassium permeability stabilizes the smooth muscle cell membrane at resting potential, reducing the probability of contraction

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14
Q

K+ Channel Opener: Diazoxide

A
  • arteriolar vasodilation
  • diminishing use in hypertensive emergencies due to adverse effects: excessive hypotension can cause stroke and MI; hyperglycemia
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15
Q

K+ Channel Opener: Minoxidil

A
  • arteriolar vasodilation
  • clinical uses include severe hypertension and baldness
  • adverse effects: headache, sweating, hypertrichosis, reflex tachycardia and edema–must be used with Beta blocker and diuretic to avoid these effects
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16
Q

Fenoldopam

A
  • D1 receptor agonist
  • renal afferent arteries contain dopamine receptors–activation increases blood flow to the kidneys
  • for HTN emergencies and postoperative HTN
  • adverse effects include tachycardia, headache, and flushing
  • should be avoided inpatients with glaucoma due to increases in intraocular pressure
17
Q

Hydralazine MOA

A

-release NO from endothelium–dilates arterioles, but not veins

18
Q

Hydralazine Clinical Uses

A

Hydralazine Clinical Uses -first line oral therapy for hypertension in pregnancy, with methyldopa

  • combination with nitrates is effective in patients with heart failure
  • parenteral formulation useful in hypertensive emergencies
19
Q

Hydralazine adverse effects

A
  • can induce fluid and sodium retention
  • headache, nausea, anorexia, sweating, flushing, palpitations
  • reflex tachycardia can provoke angina in patients with ischemic heart disease
  • lupus-like syndrome
20
Q

Nitroprusside and organic nitrates uses

A

-used to treat hypertensive emergencies, heart failure, and angina (nitrates)

21
Q

Nitroprusside and organic nitrate effects

A
  • dilates both arterial and venous vessels–decreases TPR and venous return
  • decreases both preload and afterload
  • mainly relaxation of large veins–>decreased venous return–>decreased preload–>decreased O2 demand (major effect), smaller decrease in after load
22
Q

Nitroprusside adverse effects

A

-excessive hyptension, cyanide poisoning

23
Q

Nitrates adverse effects

A

-orthostatic hypotension, syncope, throbbing headache

24
Q

Beta blocker use in hypertension

A
  • no longer 1st line treatment for hypertension, except when concomitant with a compelling indication: heart failure, recent MI, reduced left ventricular function
  • predispose ot diabetes, particularly when combined with thiazide
  • relative contraindication in asthma
  • less stroke protection than other antihypertensives
25
Q

Beta blockers with alpha blocking activity

A

labetalol

carvedilol

26
Q

Labetalol

A
  • selective alpha1 blocker
  • nonselective beta blocker
  • partial agonist at B2
  • IV for severe hypertension
  • Acceptable option for hypertension during pregnancy
27
Q

Carvedilol

A
  • nonselective B-blocker + alpha1-blocker

- also has antioxidant properties

28
Q

B-blockers with vasodilating activity

A
  • non-selective vasodilating beta blockers–carteolol, carvedilol, labetalol
  • b1-selective vasodilating beta blockers: betaxolol, nebivolol
  • these drugs produce peripheral vasodilation through a variety of mechanisms: increased NO, activate B2 receptors; block of alpha1 receptors; block Ca2+ entry; open K+ channels; antioxidant activity;a ntiproliferative effects
29
Q

Esmolol

A
  • very rapid onset and short DOA
  • B1-selective
  • used as IV infusion for peri-operative tachycardia and hypertension, hypertensive emergencies, arrhythmias
  • used in electroconvulsive therapy
30
Q

alpha1-selective receptor blockers uses

A

-3rd or 4th line treatment of essential hypertension; added to other agents from different classes in refractory cases; also used in men with concurrent HTN and BPH

31
Q

Alpha-1 blocker effects

A
  • prevent vasoconstriction of both arteries and veins
  • decrease TPR, decrease venous return, decrease preload
  • usually do not increase heart rate or cardiac output
  • do not increase NE release (no a2-block)
  • favorable effects on lipids (decrease LDL and triglycerides; increase HDL)
  • relaxes SM in the prostate
32
Q

Alpha1 blocker adverse effects

A
  • postural hypotension and syncope, especially with initial doses
  • usually given at bedtime to minimize hypotensive effects
33
Q

Clonidine Effects

A
  • alpha2-receptor agonist
  • IV-increase BP (peripheral alpha 2b) followed by decreased BP (central alpha 2a)
  • oral-decrased BP
  • patch
34
Q

Clonidine uses

A
  • essential hypertension (rarely used)

- adjunct for narcotic, alcohol and tobacco withdrawal

35
Q

Clonidine side effects

A
  • dry mouth, sedation, impotence, depression

- sudden withdrawal causes hypertensive crisis

36
Q

Methyldopa

A

Methyldopa -false NT concept

  • converted to methyl-NE
  • stored in vesicles instead of NE
  • released and acts as a centrally acting alpha2-agonist
  • decreases central sympathetic outflow and decreases bp
  • now only used to treat hypertension in pregnancy because of safety
37
Q

Methyldopa side effects-

A

sedation, dry mouth, sexual dysfunction, postural hypotension, anemia