Antihypertensive drugs and their use of Essential Hypertension Flashcards

1
Q

What is essential hypertension

A

Hypertension for a reason we cant explain.

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2
Q

Normal BP

A

systolic below 120, diastolic below 80.

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3
Q

Prehypertension

A

Systolic 120-139, diastolic 80-89

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4
Q

Stage 1 HTN

A

Systolic 140-159, diastolic 90-99

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5
Q

Stage 2 HTN

A

Over 160, and over 100

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6
Q

The tone of resistance and capacitnce of blood vessels is regulated by three things:

A

1) Sympathetic NS (barometric reflex, Vasoconstriction and HR increase)
2. ) RAAS- vasoconstriction and volume adjustement
3) Local release of hormones (endothelin, nitric oxide, kinins, etc…)

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7
Q

Antihypertensive agents

A

Agents that interfere with the activity of the Peripheral sympathetic nervous system

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8
Q

When you think about adrenergic receptors in vessels, think

A

Alpha. Alpha 1 receptors, along with angiotensin receptors, are called GP coupled receptors as they activate phospholipase C, then PIP2, then IP3, IP3 causes calcium release and contraction/ constriction of vessels.

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9
Q

When you think heart, think what receptors

A

Beta…specifically beta 1. these are responsible for leading to the opening of L-type calcium channels via cyclicAMP, this brings more calcium into the heart, when more ca is in the heart you get greater force of contraction.

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10
Q

Beta 2

A

lungs.

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11
Q

Reserpine Mechanism

A
Depletes Norep (NE) and 5-HT from neurons, and epinephrine from adrenal gland.
Leads to decreased sympathetic tone and thus, reduced TPR, CO, renin release, and BP.
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12
Q

Use or Reserpine

A

Mild to moderate HTN

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13
Q

Side effects

A

sedation and mental depression, increased incidence of gastric ulcers, don’t use in pts with depression history

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14
Q

Alpha 1 adrenergic blockers mechanism

A

block peripheral alpha 1 receptors in arterioles and venules

The pharmacological effects are that these drugs decrease TPR and lower BP, relieve BPH, increase HDL and lower LDL

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15
Q

Prazosin

A

alpha one blocker, antihypertensive

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16
Q

What alpha one blockers can you use to treat BPH?

A

Terazosin and Doxazosin

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17
Q

What side effect must you watch for with Prazosin

A

First use hypotension. Give the drug at bedtime

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18
Q

Mechanism of action for beta blockers

A

Block Beta one receptors which leads to lower heart rate, lower contractility, and lower cardiac output.

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19
Q

Also block beta one at the juxtaglomerulus and do what

A

inhibit renin release

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20
Q

Work well in what type of htn patients

A

Basically all of them, but may work especially well in these with high renin. Also, highly preferred in patients with conditions such as MI, ischemic heart disease, or CHF

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21
Q

Additional use of Beta blockers

A

3rd generation beta blockers used to lower mortality in patients with heart fialure
Useful in preventing second MI in patients with ischemic heart disease
Sinus AV and arrhythmias
Open angle glaucoma. Stage firght and horror

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22
Q

Propanolol uses?

A

Produces resting bracycardia and lower heart rate during exercise.
Membrane stabilizing activity
Dont use with asthmatics

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23
Q

Beta blckers side effects

A

Cold extremities, Bradycardia, bronchospasm, CNS side effects, metabolic problems *can delay recovery from hypoglyc in diabets, can cause rise in LDL and triglycerides with a decrease in HDL, drug withdrawls syndrome (prolonged use causes the upregulation of beta receptors in the heart, abrupt withdrawl creates tacchcardia

24
Q

ACEi mechanism of action

A

INhibit conversion of ANG I to ANG II and degradation of bradykinin (vasodialtor)
Leads to less aldosterone
Production of renin and AI goes up
ACEi raise renal blood flow via vasodilation of the afferent and efferent arterioles

25
Q

By inhibiting ANG II, what do ACEi do?

A

Lower aldosterone production, Lower ADH production, decrease vascular vasoconstriction, lower the effects of the thirst center

26
Q

Sideeffects of ACEi

A

Hypotension, Hyperkalemia, Dry cough, ANgioedema, Fetotoxicity

27
Q

ARBs

A

Angiotensin II Receptor Blockers

28
Q

What do ARBs do? Mech?

A

Block angiotensin 2 receptors
Cause vasodilation, high Na and water excretion, lower TPR, plasma volume, CO, and BP
They have no effect on bradykinin, therefore they are the substitute when ACEi cause cough.

29
Q

What is unique about the ARB Losartan

A

It increases uric acid excretion and inhibits some CYP activity

30
Q

Side effects of ARBS

A

Hypotension, Hyperkalemia, Hepatic dysfunction reported with Losartan and Valsartan, Fetotoxic

31
Q

Whats teh name of the Renin inhibitor

A

Aliskiren

32
Q

What are the effects of the Renin inhibitor

A

Used as an anti-HTN agent, not used alone but used with ACEi or ARBs

33
Q

The Three classes of Calcium channel blockers

A

Phenylalkylamines, Benzothiazepines, Dihydropyridines

34
Q

What do the three classes differ in

A

basic chemistrya nd selectivity for cardiac vs vascular calcium channels.

35
Q

Phenyalkylamines hace specificy for what?

A

myocardium. Its not as efficient as a systemic vasodilator

36
Q

Benzothiazepines specific for

A

Vascular Calcium channels

37
Q

Hihydropyridines specific for

A

Vascular calcium channels in vessels

38
Q

Effects of Dihyropyridines

A

Contraction of vascular smooth muscle is dependent on intracellular calcium concentration, inhibiting this movement of calcium lowers contraction. This decreases arterial resistnace

39
Q

Dihydropyridines are more effective in waht population?

A

Elderly subjects and African Americans…subjects with low renin HTN

40
Q

General side effects associated with all DHPs

A

ankle edema, hypotension, constipation, reflex sympathetic response

41
Q

Hydralazine mech

A

Arteriolar smooth muscle relaxer, triggers reflex sympathetic response and renin release.
Heart rate also goes up. Na and water conserved.
Fluid retention

42
Q

Hydralazine use

A

Hypertensive emergency due to eclampsia

43
Q

Side effects of Hydralazine

A

Palpitations, Autoimmune (hemolytic anemia, glomerulonephritis, lupus like syndrome)

44
Q

Minoxidil Mech

A

Relaxes arteriolar smooth muscle by opening K channels. Dilates arterioles but not veins. Powerful activator of renin secretion

45
Q

Side effects of Minoxidil

A

Renin goes way up, Hirsutism

46
Q

Topical minoxidil is?

A

Rogaine

47
Q

Fenoldopam

A

Agonist of dopamine receptors.

48
Q

How are diuretics used in treatment of hypertension

A

As monotherapy or adjunctive with other anti-htn meds

49
Q

Diuretics with Beta blockers

A

decreases mortality in all HTN pts

50
Q

Diuretics and ACEi

A

best tolerated drugs for monotherapy of HTN

51
Q

ALpha one blockers summary

A

useful in young patients who wish to remain physically active.
Some studies show alpha blocker treatment increases risk for heart failure.
Relieve BPH

52
Q

Beta blockers summary

A

Major advantage: protection to Coronary Artery DIsease, many other drugs do not show this.
Particularly useful in pts with tacchycardia, high CO, and/or low renin (Not african americans or elderly)
Useful in hypertensives with hyperthyroidism, migraine, glaucoma

53
Q

Beta blockers cont

A

3rd generation preferred over first b/c they offer smoother effect with less side effects

54
Q

ACEi summary

A

useful in management of all degrees of HTN but especially those with high renin levels.
Most always the initial anti-HTN drug prescribed.
In AA and the elderly, thiazide and ACEi are necessary
AVOID IN conditions that may cause hyperkalemia

55
Q

Dihydropyridine

A

Widely used is treatment of HTN and other cardio diseases

Particularly useful in groups with low renin

56
Q

Treatment of HTN in pts with CHF?

A

ACEi