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Flashcards in Antihypertensives I Deck (41)
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1

What are the qualitative ways of measuring blood pressure goals?

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

2

What are the six types of antihypertensive drug types?

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

3

What receptors can centrally acting agents stimulate?

1.) Stimulate imidazoline-1 receptors
2.) Stimulate alpha-2 receptors

4

Where are imidazoline-1 receptors found?

Rostral ventral lateral medulla

5

Where are alpha-2 receptors found?

Nucleus tractus solitaris (NTS)

6

What does stimulation of imidazoline-1 receptors cause?

Decreased sympathetic tone

7

What does stimulation of alpha-2 receptors cause?

Increased parasympathetic tone
Decreased sympathetic tone

8

What centrally acting drugs cause sedation?

Drugs that stimulate the alpha-2 receptors

9

What are the selective alpha-2 receptor stimulants?

Guanabenz
Alpha-methyldopa
Guanfacine

10

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

Clonidine

11

What is the most used centrally acting agent and why?

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

12

What is the net effect of centrally acting drugs?

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

13

What innervates peripheral vasculature?

Sympathetic but not parasympathetic

14

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

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)

15

What is alpha-methyldopa?

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

16

What blocks alpha-methyldopa action?

Neuronal uptake inhibitors

17

Side effects of centrally acting agents?

Sedation
Dry mouth

18

What occurs if you quit cold turkey antihypertensives? Why?

Rebound hypertension; increased adrenergic receptors and increased affinity

19

What are the peripheral adrenergic neuronal inhibitors?

Guanethidine

20

How is guanethidine uptaken?

Transported into adrenergic nerves by neuronal amine transport (NAT)

21

How does guanethidine work?

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

22

What does guanethidine ultimately cause?

Prevention of NE release with nerve stimulation

23

What happens after administration of guanethidine?

Hypertension from NE release then hypotension from NE depletion

24

Net effect of guanethidine?

Decreased CO
Decreased PVR
Severe salt/water retention

25

What are three beta-adrenergic receptor prototype blocking agents?

Propranolol
Timolol
Nadolol

26

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

Atenolol
Metoprolol

27

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

Because they block beta-1 responsible for renin release

28

What adrenergic receptors are responsible for renin release?

Beta-1

29

What is a short term beta-1 blocker?

Esmolol

30

What is Esmolol used for and why?

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