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Cardio Week 2 > Antihypertensive Drugs and their use in Management of Essential HTN > Flashcards

Antihypertensive Drugs and their use in Management of Essential HTN Flashcards

1
Q

What are the ACE inhibitors?

A
  • Captopril
  • Lisinopril
  • Enalapril (pro-drug)
  • Ramipril (pro-drug)
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2
Q

What are some AT1-receptor blockers?

A
  • Losartan (pro-drug)
  • Valsartan
  • Iresartan
  • Telmisaratan
  • Candesartan
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3
Q

What is a renin inhibitor?

A

Aliskerin

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4
Q

What are some dihydropyridine Ca2+ channel blockers?

A
  • Amoldipine
  • Nifedipine
  • Nicardipine
  • Nimodipine
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5
Q

What are some direct vasodilators?

A
  • Minoxidil
  • Na-Nitroprusside
  • Hydralazine
  • Fenaldopam
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6
Q

What is hypertensive treatment indicated in a patient 60y/o+? JNC 8

A

SBP over 150 or
DBP over 90

goal is less than these numbers

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7
Q

What is hypertensive treatment indicated in a patient less than 60y/o?

A

DBP over 90 or SBP over 140. Grade A (age 30-59)

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8
Q

What are the main effects of Prazosin?

A

decrease TPR and reduce BP by blocking a1 receptors on arteries and veins

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9
Q

What are the main effects of Doxazosin and Terazosin?

A

relieve symptoms of BPH by relaxing the muscles of the bladder and prostate

not great anti-HTN agents

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10
Q

Side effects of a-blockers?

A

first dose hypotension (give at bedtime)

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11
Q

Are a-blockers first-line for HTN?

A

No, mostly due to results of the ALLHAT study which showed that they increased CHF risk in patients with HTN.

mostly used for BPH now

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12
Q

What are some 3rd generation B-blockers with a and B activities?

A
  • Labetalol
  • Carvedilol
  • Nebivolol
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13
Q

What receptors does Labetalol inhibit?

A

non-selective B (B1/B2) and a1

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14
Q

What is Labetalol given for?

A

IV for HTN emergency (pheochromocytoma and preeclampsia)

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15
Q

What are some functions of Carvedilol?

A

mixed a1-B antagonist with:

  • antioxidant (binds and scavenges ROS)
  • protects membranes from lipid peroxidation (prevents LDL oxidation and uptake into arteries)
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16
Q

What are some functions of Nebivolol?

A

B1 selective antagonist with NO-mediated vasodilation and Antioxidant activity

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17
Q

What is the MOA of BB without ISA?

A

they block myocardial B1 receptors leading to decreased HR and contractility and

block juxtaglomerular B1 receptors, inhibiting renin release

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18
Q

Do BB cause retention of salt and water?

A

No, can be administered without a diuretic. (however, more effective with one)

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19
Q

Are BB designed for first line use for HTN?

A

No, if necessary it is preferable to use 3rd generation (causes increase stroke risk) as per JNC 8

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20
Q

Indications for BB?

A
  • Hypertensive patients with conditions such as MI, IHD, or CHF (carvedilol and metoprolol XL are cardio protective in these patients and tend to increase SV)
  • Hypertensive patients with hyperthyroidism and migraines
  • prevent subsequent MI
  • HTN with high renin
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21
Q

What BB is used in open angle glaucoma treatment?

A

Timolol (reduces production of aqueous humor)

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22
Q

What else can BB be used for?

A
  • stage fright
  • altering memory
  • sinus and AV arrhythmias
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23
Q

What are some side effects of 1st/2nd generation BBs?

A

-poor perfusion to extremities (due to a1 mediated vasoconstriction when the sympathetic system is activated following decreased BP)

  • bradycardia
  • bronchospasm
  • bad dreams, depression
  • metabolic effects
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24
Q

T or F. ALL BB should be avoided in asthma

A

T. (B1/3rd generation are okay in patients with COPD)

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25
Q

What are some of the metabolic effects of BB?

A
  • block glycogeneolysis
  • delay recovery from hypoglycemia in type I diabetes (mask tachycardia)
  • block HSL in adipocytes - increase LDL and TAG
  • reduce HDL
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26
Q

How can the delay recovery from hypoglycemia in type I diabetes seen in BB be avoided?

A

not seen in 3rd ben or with selective B1-blockers

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27
Q

Is it safe to withdraw BB use suddenly?

A

no, prolonged use up-regulates B-receptors in the heart. Abrupt withdrawal causes tachycardia

taper 10-14 days prior

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28
Q

What do ACEIs do?

A
  • inhibit conversion of angio I to II
  • inhibit bradykinin breakdown, a vasodilator
  • slightly decrease aldosterone levels

increase renal BF (dilate renal artery) without an increase in GFR and increase synthesis of prostaglandins

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29
Q

What does the increase in Prostaglandins via ACEIs do?

A

delay progression of renal disease in diabetics (renoprotective)

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30
Q

What are the effects of Angiotensin II?

A
  • cardiac and vascular hypertrophy (via PKC activation)
  • systemic vasoconstriction
  • increased thirst
  • stimulates aldosterone release from the adrenal cortex
  • stimulates ADH release from the pituitary leading to renal sodium and fluid retention
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31
Q

Side effects of ACEIs?

NOTE: ACEIs are the go-to for CHF because they dilate both arteries and veins, leading to decreased after load and preload, respectively.

A
  • Hyperkalemia (especially in renal insufficiency)
  • Can precipitate acute renal failure (monitor creatinine)
  • Dry cough (most common)
  • Angioedema
  • Fetotoxicity
32
Q

How do ACEIs induce dry cough?

A

bradykinin activates stretch receptors in the trachea, which might cause dry cough in 10-15% of patients

33
Q

Can you give ACEIs any time during pregnancy?

A

only 1st trimester

34
Q

What do ARBs do?

A

selectively block AT II type 1 receptors causing vasodilation and increased Na+ and water excretion leading to decreased TPR, plasma volume, CO, and BP.

35
Q

When are ARBS most commonly used?

A

when ACEIs produce cough or angioedema

36
Q

What does Losartan do?

A

competitive inhibitor of TxA2 receptors, attenuates platelet aggregation and increases uric acid urinary excretion (uricosuric)- ONLY ONE

37
Q

What is the main contraindication for all ARBs?

38
Q

L-type Ca2+ channels exist in both cardiac and vasculature. What is Verapamil specific for?

A

myocardium mostly (thus, not great for HTN)

39
Q

L-type Ca2+ channels exist in both cardiac and vasculature. What is Diltiazem specific for?

A

intermediate between Verapamil and Dihydropyridines in specificity for vasculature

again-better use in heart problems.

40
Q

Effect of CCBs?

A

reduce BP by relaxing arteriolar smooth muscles and decreasing peripheral vascular resistance

do not cause a large baroreceptor-mediated sympathetic discharge and mild to no changes in HR

41
Q

Clinical uses of CCBs?

A
  • most effective in lowering BP in patients with low renin HTN such as elderly patients and AAs
  • preferred in older patients with systolic hypertension
42
Q

What are some a2 agonists?

A
  • Clonidine

- Methyldopa

43
Q

What does clonidine do?

A

agonist of postsynaptic 2a receptors in the rostral ventrolateral medusa (RVLM) which causes decreased sympathetic impulses from RVLM to the heart and blood vessels and a decrease in PVR and decrease in HR

44
Q

Uses of clonidine?

A
  • releases endogenous opiates
  • used as analgesic in neuropathic pain
  • ADHD
  • tertiary use in HTN
45
Q

Side effects of clonidine?

A

sedation,
erectile dysfunction,
fatigue,
HTN upon quick withdrawal

46
Q

What does hydralazine do?

A

causes arteriolar smooth muscle relaxation.

47
Q

What follows the smooth muscle relaxation with hydralazine?

A

strong reflex sympathetic stimulation leading to catechlamine/renin secretion

need to add BB and diuretic to counteract these effects if long-term use

48
Q

Side effects of hydralazine?

A
  • pronounced tachycardia

- lupus like syndrome

49
Q

What is Fenoldopam?

A

selective D1 partial agonist used in hypertensive emergency

50
Q

What does Minoxidil do?

A

opens K+ ATP K channels and relaxes smooth muscles

only used for severe HTN

51
Q

What part of the vasculature is Minoxidil active on?

A

dilates arterioles but not veins

52
Q

What happens following the smooth muscle relaxation caused by Minoxidil?

A

strong reflex sympathetic stimulation leading to catechlamine/renin secretion

53
Q

Side effects of Minodixil?

A

hirsutism (male pattern hair growth in women)

54
Q

What is the compensatory reaction to vasodilators?

A

vasodilators decrease vascular resistance leading to decreased AP, which causes increased sympathetic activity, decreased renal sodium excretion, and increased renin secretion

Increased renin secretion also prevents renal sodium excretion.

55
Q

How does Nitroprusside cause vasodilation?

A

a pro-drug that forms NO which stimulates smooth muscle guanylate cyclase which increases cGMP in vascular smooth muscle and causes relaxation

56
Q

What are the effects of Nitroprusside in the body?

A
  • dilates both arteries and veins
  • reduces TPR and induces venous pooling

short half-life

57
Q

How does Nitroprusside affect CO?

A

decreases CO in normal subjects, but increases CO in patients with left
ventricular failure because TPR (i.e. afterload) is reduced.

58
Q

What is Nitroprusside used for?

A

Has a very short half-life and is given IV for hypertensive

emergencies in patients with ventricular failure

59
Q

Side effects of Nitroprusside?

A

potential accumulation of cyanide in patients with renal failure

60
Q

How are diuretics given for HTN?

A

as mono therapy or adjunctive with ANY other antihypertensive (augments them all)

Patients with edematous conditions, such as heart failure and renal insufficiency, frequently require a diuretic for optimal control of BP.

61
Q

T or F. Treatment with thiazide-type diuretics was more effective than CCB or ACEI

62
Q

Side effects of Diuretics?

A

associated with hypokalemia,

hypomagenesemia and potential hyponatremia after long-term use

63
Q

What are the best drugs for mono therapy of HTN?

A

Diuretics (particularly in low doses) and ACEIs

64
Q

What patients show the best response to diuretics?

A

Patients with “volume dependent” hypertension (with low renin levels) show better responses. A poor response to thiazides may reflect either an overwhelming load of dietary sodium or an impaired renal capacity to excrete the sodium.

65
Q

What is a major advantage of BBs?

A

secondary protection in CAD, a characteristic not well established for other drugs.

Very useful in hypertensives with hyperthyroidism,
migraine, glaucoma (eye drops).

66
Q

Indications for ACEIs and ARBs?

A
  • all HTN but mostly high renin HTN

- should be first line antihypertensive in diabetic patients with HTN and in patients prone to CHF

67
Q

T or F. ACEI are less effective than CCB in reducing BP in Blacks

68
Q

Contraindications of ACEIs and ARBs?

A
  • avoid in any condition that may cause hyperkalemia

- pregnancy

69
Q

Can short-acting Dihydropyridine CCBs (such as clonidine) be used for HTN?

A

No, just long acting (Amoldipine, Nicardipine, Nimodipine)

70
Q

In the General black population, including those with diabetes, their initial treatment should include what?

A

a thiazide and/or a CCB. (safe with diabetes)

71
Q

Use of antihypertensives in management of essential HTN

A
  • Initiate therapy with a thiazide diuretic, CCB, or ACEI/ARB in most non-black patients.
  • Initiate therapy with a thiazide diuretic and/or CCB in black patients.
72
Q

First line antihypertensive in diabetes mellitus?

73
Q

First line antihypertensive in CHF with HTN?

A

ACEIs, diuretics, cardioselective CV and/or Aldosterone antagonists

74
Q

First line antihypertensive in MI?

A

BB and ACEIs/ARBs

75
Q

First line antihypertensive in chronic kidney disease, particularly with proteinurea?

Cardio Week 2 (11 decks)

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