Antihypertensive Agents Flashcards

1
Q

what percent of people have hypertension? by age 80 what percent will have it?

A

30%; 80%

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2
Q

complications of HTN longterm?

A

Damages kidney
heart and brain manifested as kidney failure
heart failure
coronary artery disease and stroke

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3
Q

Mean arterial pressure=

A

CO x PVR

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4
Q

CO=

A

SVxHR

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5
Q

what system coordinates BP?

A

autonomic nervous system

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6
Q

pt with HTN have a ____ set point for BP

A

higher

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7
Q

MOA of diuretics?

A

Deplete sodium and decrease blood volume

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8
Q

MOA of sympathoplegics?

A

Decrease peripheral resistance
Decrease CO by
Inhibiting cardiac function
Increasing venous pooling in capillaries

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9
Q

MOA of vasodilators?

A

Decrease pressure by relaxing/dilating vascular smooth muscle

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10
Q

MOA of angiotensin action blocker?

A

Decrease peripheral resistance and blood volume

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11
Q

groups of diuretics?

A
  • potassium sparing diuretics
  • loop diuretics
  • thiazide diuretics
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12
Q

why do we use potassium sparing diuretics?

A

Use with other diuretics (thiazides &/or loops) to prevent hypokalemia

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13
Q

why do we use loop diuretics?

A

volume overload

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14
Q

MOA of thiazide diuretics?

A
  • By depleting body stores of sodium (Na), water follows NA, decreasing blood volume.
  • Less volume, less cardiac output, eventually less PVR and lower BP
  • Initially they decrease blood volume which decrease CO
  • After weeks/months they also decrease PVR accounting for their long term effects for BP regulation
  • Decrease sodium content of arteriolar smooth muscle which leads to a decrease in muscle contraction in response to norepinephrine and Angiotensin II
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15
Q

what do thiazide diuretics work well for?

A

BP

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16
Q

prototype thiazide diuretic?

A

HCTZ hydrochlorothiazide

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17
Q

most common ADR of HCTZ?

A
  • low potassium; can be lethal (contributes to arrhythmias and/or muscle pain)
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18
Q

other ADR of HCTZ?

A
  • low magnesium
  • high BS
  • increased lipids
  • increased uric acid associated with gouty arthritis
  • low potassium
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19
Q

how much does HCTZ lower BP?

A

10-15 mm Hg

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20
Q

What is the dose of HCTZ?

A

12.5mg capsules
25mg or 50 mg tablets

most are 12.5-25 mg is what most people are on

50 mg dose = more ADRs

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21
Q

what populations respond best to HCTZ?

A

African-Americans, older patients, obese patients, smokers

22
Q

goal of sympathoplegics?

A

inhibiting function of sympathetic nervous system

23
Q

MOA of centrally acting drugs?

A
  • Reduce sympathetic outflow from the centers in the brainstem that control blood pressure.
  • Less SNS outflow, lower BP
  • These drugs work on the alpha adrenoreceptors in the brain not in the periphery.
24
Q

MOA of methyldopa?

A

Work to decrease BP by decreasing PVR

25
Q

ADRs of methyldopa?

A
  • Related to the fact that it works in the brain
  • Common side effects: sedation, decreased concentration, impotence
  • Less common: nightmares, depression, vertigo, lactation
  • Rare, but significant: Hemolytic anemia (Type II hypersensitivity)
26
Q

what centrally acting drug do we use in pregnant woman who need to decrease BP? when else is this drug used?

A

methyldopa, decreases PVR

otherwise as 2nd or 3rd line due to S/E

27
Q

how does clonidine work?

A

Lowers CO by decreasing HR and (PVR) by relaxing capillary venues

28
Q

what are the ADRs of clonidine?

A

ADRs (Works in the brain):

  • Common ADRs: Dry mouth, sedation, impotence, causes or worsens depression
  • Severe ADR: Rebound HTN. If stop clonidine suddenly can get increased SNS outflow from the brain causing sudden, severe increase in BP (higher than when started the med). It lasts for a brief period but has been associated with hypertensive hemorrhage in brain.
  • All patients should be educated: DON’T STOP SUDDENLY. The drug must be tapered (decreased slowly over several days)
29
Q

what should you educate your pt about clonidine?

A

not to stop suddenly

30
Q

drug interactions with clonidine?

A
  • Clonidine is less effective in those on tricyclic antidepressants.
  • Try not to give with other drugs that make sleepy as sleepiness adds up
31
Q

when do you use clonidine?

A

3rd-4th line agent

32
Q

what is the issue with clonidine?

A

compliance

have to use for BP have to dose 2x/d

or can use patch for non compliance (applied every 7th day)

33
Q

MOA of beta blockers?

A

Decrease BP and CO

  • Blocks beta receptors in kidneys
  • Blocks peripheral adrenergic receptors mostly in heart, so get less SNS effect (decreasing HR and contractility)
  • Beta blockade decreases renin (less angiotensin II and aldosterone, less volume)
34
Q

absorbtion of beta blockers?

A

Well absorbed orally as a group, first pass occurs with most in group so oral dose is much higher than IV dose.

35
Q

distribution of beta blockers?

A

Large volumes, go everywhere some get into CNS ( those that get into CNS increase chance of CNS side effects)

why selective and non-selective important

36
Q

ADRs of beta blockers?

A
  • In the heart causes bradycardia, cardiac conduction problems (arrhythmias), decreased pumping action making CHF worse
  • In lung can make asthma worse (non-selectives in particular)
  • In blood vessels prevents dilation effect that beta 2 gives. This is a problem only if already have a blockage in the blood vessels (peripheral vascular disease)

Other ADRs:

  • CNS: depression, sedation, sleep disturbances, rarely psychotic reactions
  • In diabetics beta blockers mask symptoms of hypoglycemia
  • Withdrawal: Occurs b/c of upregulation of beta receptors (Symptoms: Nervousness, tachycardia, increased BP)
  • Don’t stop suddenly, taper
37
Q

Nonselective beta blockers?

A

Propranolol (Inderal) - prototype
Nadolol (Corgard)
Carteolol (Cartrol) - not used

38
Q

Selective beta blockers?

A
Metoprolol (Lopressor)
Atenolol (Tenormin)
Betaxolol (Kerlone)
Esmolol (Brevibloc)
Bisoprolol (Zebeta)
Nebivolol (Bystolic)
39
Q

partial agonist beta blockers?

A

Pindolol (Visken)
Acebutolol (Sectral)
Penbutolol (Levatol)

40
Q

beta and alpha antagonists?

A

Labetalol (Normodyne)

Carvedilol (Coreg)

41
Q

two types of metoprolol salts?

A

Lopressor – immediate release 2x/d

Toprol – extended release 1x/d

42
Q

what is the beta and alpha antagonist that has 2 salt forms?

A

carvedilol

43
Q

selective vs. nonselective beta blockers?

A
  • Get greatest effect on BP through beta 1 effect. So just want to block beta 1 receptors (selective)
  • Nonselective beta blockers block beta 1 & 2 equally (ex. Propranolol)
  • Selective beta blockers block beta 1 more than beta 2 at lower doses. Once dose gets high enough loose selectivity
44
Q

classic selective B1B? when do we use them?

A

Metoprolol & Atenolol

  • Beta 1 selective beta blockers are better if have DM, asthma or peripheral vascular disease
  • These diseases made worse by beta 2 blockade
  • If patient has a contraindication & NEEDS a beta blocker better to go with selective
45
Q

newest B1B? MOA?

A

nebivolol

  • vasodilates** extra compared to others
  • So lowers BP and decreases PVR leading to fewer side effects with this beta blocker
46
Q

what is special about esmolol? what it is used for?

A
  • IV beta blocker, given as a continuous infusion (hospital drug)
  • Beta 1 selective & rapidly metabolized
  • Used for intra and post op HTN and HTN emergencies especially when tachycardic
  • B/c rapidly metabolized when turn on get a quick effect, if decrease BP too much turn it off and it is gone quickly
47
Q

What are BB good for?

A
  • add on for mild to moderate HTN

- HTN + another problem that BB will help (angina, CAD, Hx MI, CHF, migraines, anxiety)

48
Q

MOA of alpha receptor blockers?

A
  • Block alpha 1 receptors in arterioles and venules (dilation of vessels).
  • Work better in upright position than supine and so when change position can get orthostasis (orthostatic hypotension)
  • Sodium and water are retained, usually need a diuretic when use these (one of the reasons not used alone)
49
Q

ADRs of alpha receptor blockers?

A
  • Orthostatic hypotension
  • Profound first dose effect, wears off over time. Give first dose at bedtime and make it small
  • More if volume depleted (on a diuretic)
  • Dizziness, palpitations, HA, edema and fatigue
50
Q

Available alpha receptor blockers for HTN?

A

Prazosin (Minipress)
Doxazosin (Cardura)
Terazosin (Hytrin)

51
Q

pt that will benefit from alpha blockers?

A
  • Men with prostate enlargement (BPH). Alpha blockers treat BPH too.
  • Work better when use with other anti-HTN drugs than when used alone, so it must be a second or third line drug
  • Often put on a diuretic first then add a alpha blocker. Diuretics prevent the edema caused by the alpha blockers