Antihypertensives I Flashcards

1
Q

What are the qualitative ways of measuring blood pressure goals?

A
  1. ) Reduced incidence of heart failure
  2. ) Reduced stroke incidence
  3. ) Reduced overall cardiovascular mortality
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2
Q

What are the six types of antihypertensive drug types?

A
  1. ) Centrally acting agents
  2. ) Peripheral anti-adrenergics
  3. ) Beta-adrenergic receptor antagonists
  4. ) Peripheral vasodilators
  5. ) RAS altering drugs
  6. ) Diuretics
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3
Q

What receptors can centrally acting agents stimulate?

A
  1. ) Stimulate imidazoline-1 receptors

2. ) Stimulate alpha-2 receptors

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4
Q

Where are imidazoline-1 receptors found?

A

Rostral ventral lateral medulla

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5
Q

Where are alpha-2 receptors found?

A

Nucleus tractus solitaris (NTS)

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6
Q

What does stimulation of imidazoline-1 receptors cause?

A

Decreased sympathetic tone

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7
Q

What does stimulation of alpha-2 receptors cause?

A

Increased parasympathetic tone

Decreased sympathetic tone

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8
Q

What centrally acting drugs cause sedation?

A

Drugs that stimulate the alpha-2 receptors

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9
Q

What are the selective alpha-2 receptor stimulants?

A

Guanabenz
Alpha-methyldopa
Guanfacine

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10
Q

What is a combined imidazoline-alpha-2 receptor stimulant?

A

Clonidine

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11
Q

What is the most used centrally acting agent and why?

A

Clonidine because it has much less sedation than selective alpha-2 stimulants and imidazoline-1 is a stronger antihypertensive

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12
Q

What is the net effect of centrally acting drugs?

A

Decreased sympathetic outflow to heart
Decreased sympathetic outflow to peripheral vasculature
Increased parasympathetic outflow to heart

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13
Q

What innervates peripheral vasculature?

A

Sympathetic but not parasympathetic

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14
Q

Why do centrally acting drugs typically need a diuretic used with them?

A

Because in essential hypertension when you decrease PVR the baroreceptors think you are hypotensive (even though you are normotensive) and increase the RAS (also CO/HR)

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15
Q

What is alpha-methyldopa?

A

A prodrug converted to alpha-methylnorepinephrine (false transmitter) in the brain (alpha-2 selective)

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16
Q

What blocks alpha-methyldopa action?

A

Neuronal uptake inhibitors

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17
Q

Side effects of centrally acting agents?

A

Sedation

Dry mouth

18
Q

What occurs if you quit cold turkey antihypertensives? Why?

A

Rebound hypertension; increased adrenergic receptors and increased affinity

19
Q

What are the peripheral adrenergic neuronal inhibitors?

A

Guanethidine

20
Q

How is guanethidine uptaken?

A

Transported into adrenergic nerves by neuronal amine transport (NAT)

21
Q

How does guanethidine work?

A

It is uptaken by vesicular monoamine transport (MAO) releasing NE from vesicles and depleting NE stores

22
Q

What does guanethidine ultimately cause?

A

Prevention of NE release with nerve stimulation

23
Q

What happens after administration of guanethidine?

A

Hypertension from NE release then hypotension from NE depletion

24
Q

Net effect of guanethidine?

A

Decreased CO
Decreased PVR
Severe salt/water retention

25
Q

What are three beta-adrenergic receptor prototype blocking agents?

A

Propranolol
Timolol
Nadolol

26
Q

What two beta-1 selective blockers lose their selectivity at large doses?

A

Atenolol

Metoprolol

27
Q

Why do beta-adrenergic receptors have no salt and water retention?

A

Because they block beta-1 responsible for renin release

28
Q

What adrenergic receptors are responsible for renin release?

A

Beta-1

29
Q

What is a short term beta-1 blocker?

A

Esmolol

30
Q

What is Esmolol used for and why?

A

A bridge to surgery during aortic dissection because it is a short term drug

31
Q

What are mixed alpha-beta adrenergic receptor blockers?

A

Labetalol

Carvedilol

32
Q

What are the four classes of vasodilators?

A
  1. ) Organic nitrates
  2. ) Alpha-adrenergic receptor antagonists
  3. ) Calcium entry blockers
  4. ) Direct vasodilators
33
Q

What are the organic nitrates?

A

Nitroprusside

Nitroglycerine

34
Q

What are the alpha-adrenergic receptor antagonists?

A

Prazosin
Terazosin
Doxazosin

35
Q

What are the dihydropyridines?

A

Dihydropyridines:
Nifedipine
Amlodipine
Felodipine

36
Q

What are the direct vasodilators?

A

Hydralazine

Minoxidil

37
Q

What are the calcium entry blockers?

A

Dihydropyridines
Verapamil
Diltiazem

38
Q

How are organic nitrates administered?

A

Sublingual

Topical

39
Q

How do organic nitrates work?

A

They are venodilators as opposed to arterial vasodilators

40
Q

What is Nitroprusside metabolized by and into what?

A

Oxyhemoglobin to NO + methemoglobin + cyanide

41
Q

What can Nitroprusside cause?

A

Methemoglobinemia

Cyanide poisoning