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Pharmacology > Anti-Hypertensive Drugs > Flashcards

Anti-Hypertensive Drugs Flashcards

1
Q

Etiology of Hypertension

A

> 90% of patients have essential hypertension

Risk Factors: Family history, obesity, diet, age, physical inactivity, smoking, African Americans (4x more likely), middle age men > females

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2
Q

Hypertension guidelines

A

sustained systolic BP > 130 mmHg
or
sustained diastolic BP > 80 mmHg
** results from: increased peripheral vascular smooth muscle tone –> increased arteriolar resistance and reduced capacitance on the venous system

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3
Q

Hypertension Categories (4)

A 
Normal: < 120 and < 80
Elevated 120-129 and < 80
Stage 1: 130-139 or 80-89
Stage 2: > 140 or > 90
** current guideline goals is to reduce BP to < 130/80 mmHg
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4
Q

BP control

A

Arterial BP: directly proportional to CO and PVR
CO and PVR: controlled by baroreflexes (SNS and RAAS)
** Antihypertensive drugs reduce either or both

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5
Q

Anatomical Sites of BP control (4)

A

1) Resistance of arterioles
2) Capacitance of Venules
3 Pump output of the Heart
4) Volume (kidneys)

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6
Q

Compensatory Response to Decrease BP

A

Decreased blood pressure will compensate via two reflex mechanism:

1) Increased sympathetic outflow = tachycardia
2) Increased Renin release = Salt and water retention (increase plasma volume)

Both will lead to Increase BP
** not all hypertensive drugs result in a reflex.. generally drugs that work on the vessels cause reflexes

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7
Q

Stage 1 vs Stage 2 control of Hypertension

how many drugs prescribed

A

Stage 1: Often controlled with a single drug
Stage 2: Often requires multiple drugs
** life-style changes are the first recommendation to all patients with pre-hypertension and Stage 1 hypertension

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8
Q

Current Recommendations for Treatment

A

Initiation of pharmacotherapy
- most patients can be started on a single drug (should consider giving 2 drugs of different classes to patients with Stage 2 hypertension)

Stage 2 Hypertension:
- 2 first line drugs of different classes (patients with stage 2 hypertension and average BP of 20/10 mmHg above the BP target)

If BP is still not controlled: vasodilator given

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9
Q

First-Line agents, Second-Line agents, and Other agents

A

First Line: ACE inhibitors, ARBs, Calcium Channel blockers, and Thiazide diuretics

Second Line: Beta-blockers, aldosterone antagonist

Other: Loop diuretics, alpha-blockers, direct vasodilators, central alpha 2-agonist, renin inhibitors

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10
Q

ACE Inhibitor Drugs

A

Captopril
Enalapril
Lisinopril

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11
Q

ACE Inhibitor MOA

A

First Line agent (particularly for diabetics and patients with CKD)

  • Decrease BP by decreasing PVR
  • inhibits ACE - converts angiotensin I –> Angiotensin II (vasoconstrictor)
  • *** blockage of ACE leads to Increased Renin and Angiotensin I due to lack of feedback inhibition
  • Decreases Na+ and H2O retention
  • Increases bradykinin levels (ACE metabolizes bradykinin) - which leads to decrease BP and mild vasodilation
  • DO NOT reflexively increase CO or HR
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12
Q

ACE Inhibitors- Clinical Applications

A

Hypertension (most effective in white or young patients or can be given with a diuretic to = same effectiveness in black patients

Preserves renal function in patients with nephropathy (diabetic or non-diabetic) – angiotensin II constricts renal efferent arterioles - thus blocking allows arterioles to dilate and decrease GFR (dec. hyper-filtration) ** UNILATERAL

Effective for treating Chronic HF

Standard of care for patients following MI (started 24 hrs after end of infarction)

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13
Q

ACE inhibitors AE

A

Dry hacking cough (due to increase Bradykinin)
Hyperkalemia - effects due to blocking of aldosterone
Hypotension
Angioedema (rare but life-threatening) < 1%
Acute Renal Failure (patients with bilateral renal artery stenosis) - in bilateral vasoconstriction the efferent arteriole is maintaining GFR and ACE inhibitor will cause a plummet in GFR = Death
Rash, fever, altered taste

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14
Q

ACE Inhibitors Contraindications

A

Pregnancy

  • 1st trimester - Inc. risk of malformations
  • 2nd and 3rd trimester - risk of fetal hypotension, anuria, and renal failure

Patients with bilateral renal stenosis

Patients with a history of angioedema related to previous ACEI treatments or hereditary idiopathic angioedema

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15
Q

ARB Drugs

A

Losartan

Valsartan

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16
Q

ARB MOA

A

Angiotensin II receptor Blocker (blocks AT1 Receptor)
*** Increased levels of angiotensin II, angiotensin I, renin do to lack of feedback mechanism
First line agent
Alternatives to ACEI (does not produce dry cough)
Dec. in BP causing arteriolar and venous dilation
blocks aldosterone secretion: Dec Na+ and H2O retention
Dec. Diabetic Nephrotoxicity
Does Not Increase Bradykinin Levels

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17
Q

ARB AE

A

Similar to those of ACE inhibitors

Dry cough does not occur
Angioedema risk is significantly lower than with ACEI
** Losartan reduces plasma uric acid levels by inhibiting URAT1 transporter- useful in patients that also have gout

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18
Q

ARB Contraindications

A

Pregnancy

Patients with bilateral renal stenosis

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19
Q

Renin Inhibitor
MOA
End Result

A

Aliskiren
Alternative agent in the treatment of hypertension
** Not clinically as effective than ARB or ACEI

MOA: Inhibits the enzyme activity of Renin and prevents the conversion of angioteninogen to angiotensin I

End Result: Inhibits theA production of angiotensin II and aldosterone

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20
Q

Renin Inhibitor AE

A

Similar to those of an ACEI
No dry cough
Decreased risk of angioedema than with ACEI

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21
Q

Calcium channel blockers

A

Verapamil (non-dihydropyridines)
Diltiazem (non-dihydropyridines)
Nifedipine (dihydropyridine)
Amlodipine (dihydropyridine)

First line agent (particularly black and/or the elderly)

Separated into two classes: (non-dihydropyridines or dihydropyridines)

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22
Q

Verapamil and Diltiazem

A

Verapamil:
Least selective Ca2+ channel blocker
significant effects in cardiac and vascular smooth muscle - relaxation and decrease contractility and HR
Uses:
- treat angina, supra ventricular tachyarrhythmias, hypertension, migraine, and cerebral vasospasm

Diltiazem:
Effects cardiac and vascular smooth muscle (less effective on cardiac then verapamil)
Good side-effect profile
Uses:
- treat angina, hypertension, supra ventricular tachyarrhythmias, and cerebral vasospasm

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23
Q

Dihydropyridines

A

Nifedipine
Amlodipine

Greater affinity for vascular Ca2+ channels than for cardiac channels
Reduces calcium entry into the smooth muscle to causes coronary and peripheral vasodilation and lower BP
Primary use is to treat hypertension, can also be used for angina
** Not used for cardiac arrhythmias

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24
Q

Calcium channel blockers - Clinical App.

A

Hypertension (Black of elderly patients)
Have intrinsic natriuretic effects (diuretic not needed)
Useful in patients with asthma, diabetes, peripheral vascular disease

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25
Q

Calcium channel blockers- PK

A

High-doses of short-acting dihydropyridine blockers can increase risk of MI (due to reflex stimulation)
Sustained release preparations are preferred

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26
Q

Calcium channel blockers- AE

A

Verapamil
- Constipation, negative inotropic signals, gingival hyperplasia

Dihydropyridines
- hypotension, peripheral edema (feet/ankles), dizziness, headache, fatigue, gingival hyperplasia, flushing, REFLEX TACHYCARDIA (short-acting preparations)

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27
Q

Calcium channel blockers Contraindications

A

Non-dyhyrdopyridines
- contraindicated in patients taking b-blockers or who have a 2nd or 3rd degree AV block, or severe left ventricular systolic dysfunction

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28
Q

Diuretic Drugs and MOA

A

Thiazide (Hydrochlorothiazide, Metolazone, Chlorthalidone)
First line agent (particularly black and/or elderly patients)

MOA

  • Lower BP by increasing Na+ and H2O excretion- decreasing blood volume
  • Long term treatment = normal plasma volume but sustained decrease in PVR
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29
Q

Thiazides- Clinical Apps.

A

Counteract Na+ and H2O retention caused by other anti-hypertensive drugs
Particularly useful in the black and elderly (with normal renal and cardiac function)

30
Q

Thiazides AE

A 
Hypokalemia
Hyperuricemia
Hyperglycemia
Hypomagnesium
Hyperchlosterolemia
Sex dysfunction
31
Q

Loop Diuretics (furosemide)

A

Act promptly in patients with poor renal function or heart failure
more potent in inducing diuresis and can cause more side effects
used primarily in patients who do not respond to thiazides therapy adequately
causes dec. renal vascular resistance and inc. renal blood flow

32
Q

K+ sparing Diuretics MOA and uses

A

Dec. loss of K+ in the urine due to thiazide or loop diuretics
used in combination therapy

33
Q

Aldosterone Antagonist clinical application

A

Spironolactone and Eplerenone

  • Inhibits Na+ and H2O retention via aldosterone receptor
  • reduced K+ excretion - risk for hyperkalemia
  • Used in treatment of hypertension and HF
  • Can be used as a part of first line therapy in patients with hypertension and severe left ventricular dysfunction
34
Q

Beta Blocker Drugs and clinical applications

A

Propranolol (Non-selective)
Metoprolol (B1-selective)
Atenolol (B1-selective)
Pindolol (partial Non-selective agonist) - preferred blocker in pregnancy

Used only as add on therapy to first line agents in primary prevention patients

First line therapy ONLY for patients with CAD, HF, or post MI- plus hypertension

35
Q

Beta-blockers: MOA and PK

A

MOA:
Reduce BP by dec. Cardiac Output, contractility, and Heart Rate
Blunt sympathetic reflex with exercise
inhibits both release of NE and Renin (B1 receptors)

PK: May take several weeks to develop full effects

36
Q

Beta-blockers AE

A

Bradycardia, CNS effects (fatigue, lethargy, insomnia, hallucinations), hypotension, decrease libido, and impotence

Disturb lipid metabolism (Dec. HDL and Inc. TAGs)

Hypoglycemia (b2)

drug withdrawal effects (quick withdrawal may induce angina, MI or sudden death) –> must be tapered off

Propranolol - contraindicated in patients with COPD or Asthma

37
Q

Alpha 1 blockers Drugs MOA and effects

A

Prazosin
Doxazosin

Competitive inhibitor of alpha 1 adrenoreceptors

Dec. PVR and Dec. Arterial BP by relaxing both arterial and venous smooth muscle

Causes minimal changes in CO, renal blood flow, and GFR (no long term tachycardia)

Na+ and H2O retention does occur

Effective in lowering BP but more side effects than any other antihypertensive

38
Q

Alpha 1-blockers - Clinical Applications

A

Hypertension (due to side-effect profile and advent of safer antihypertensives, are seldom used in treatment in hypertension.

Generally used for alternative reasons : BPH - DOC to relieve symptoms

Have been used in HF but not commonly

39
Q

Alpha 1 blockers AE

A

Orthostatic hypotension (syncope) upon first does or increase in dose

concomitant use of a beta-blocker to blunt initial reflex tachycardia

CNS effects: dizziness, headache, lack of energy, nausea, and palpitations

** Doxazosin shown to increase rate of congestive HF

40
Q

Mixed Alpha and Beta blocker: PK, advantages, AE

A

Labetalol (more potent on beta than alpha)
PK:
- oral or parenteral admin.
- used in hypertension management (safe in pregnancy)
- IV = rapid reduction in BP- useful in hypertensive emergencies
Advantages:
- Dec. BP with associated alpha-1 blockade and is not associated with a reflex tachycardia
AE:
Orthostatic Hypotension

41
Q

Central alpha 2- agonist

A

Clonidine

Methyldopa

42
Q

Clonidine: MOA, Uses, AE

A

MOA:
- Reduces sympathetic outflow (a2 receptor)
- Decreases PVR and CO –> dec. BP
- Does not affect renal blood flow or GFR
Uses:
- Used in hypertension management including hypertension crisis
AE:
- Drowsiness, dry mouth, dizziness, headache, and sexual dysfunction
- Rebound hypertension may occur follow quick withdrawal
** avoid concomitant use with beta blockers

43
Q

Methyldopa: MOA, Uses, AE

A

MOA:

  • Alpha-2 agonist converted to alpha methyl dopamine and alpha methylnorepinephrine centrally to diminish sympathetic outflow
  • Dec. PVR and Dec. BP
  • Does not dec. Renal Blood flow or GFR

Uses:

  • DOC of pregnancy induced hypertension
  • Used in management of hypertension

AE:

  • sedation, drowsiness, dizziness, nausea, headache fatigue, and sexual dysfunction
  • nightmares, mental depression, and vertigo
  • Development of Positive Coombs test (can result in hemolytic anemia, hepatitis, and Drug fever)
44
Q

Direct Vasodilators

A

Hydralazine
Minoxidil

Not first line treatment
Direct acting smooth muscle relaxants (arterioles)
produces reflex tachycardia, renin release
Major side effects can be blocked if combined with beta blocker and diuretics

45
Q

Hydralazine: PK, Uses, AE

A

PK:

  • IV or oral
  • acts mainly on the arterioles

Uses:

  • to treat pregnancy induced hypertension/pre-eclampsia
  • used to manage hypertension as a last line therapy

AE:

  • Fluid retention and reflex tachycardia
  • reversible lupus like syndrome (metabolized by acetylation)
  • Headaches, nausea, sweating, and flushing

** usually admins. with beta blocker and thaizide

46
Q

Minoxidil: Uses, AE

A

Causes direct peripheral vasodilation of the arterioles
Uses:
- oral treatment for severe malignant hypertension

AE:

  • reflex tachycardia, and fluid retention
  • hypertrichosis (baldness treatment)
47
Q

Pulmonary Hypertension

A

An increase in BP in the pulmonary artery, vein, or capillaries

Tx:
Prostaglandins
Inhibitors of endothelin synthesis
vasodilators

48
Q

Epoprostenol

A

Synthetic PGI2
lowers peripheral, pulmonary, and coronary resistance
Given via continuous IV infusion
AE: flushing, headache, jaw pain, diarrhea, and arthralgias

49
Q

Bosentan

A

Non-selective endothelin receptor blocker
Blocks both the initial transient depressor (ETA) and the prolonged pressor (ETB) responses to endothelin
Category X for pregnancy

50
Q

Sildenafil

A

Inhibitor of PDE5 (phosphodiesterase 5)
Inc. cGMP = smooth muscle relaxation

AE: headache, flushing, dyspepsia, cyanopsia
Contraindicated with Nitrates

51
Q

Comorbid condition: None Treatment

A

First Line: ACEI or ARB, CCB, or thaizide

Second Line: beta blockers, aldosterone antagonist

52
Q

Comorbid condition: Acute or Chronic CAD Treatment

A

First Line: beta-blockers + ACEI or ARB

Second Line: Thaizide, CCB

53
Q

Comorbid condition: Chronic Kidney Disease Treatment

A

First Line: ACEI or ARB

Second Line: CCB or Thiazide

54
Q

Comorbid condition: Diabetes treatment

A

First Line: ACEI or ARB

Second Line: CCB or Thiazide

55
Q

Comorbid condition: HF treatment

A

First Line: ACE or ARB + thiazide (or Loop) + beta blocker

Second Line: Aldosterone antagonist, hydrazine/isosorbide dinatrate (black)

56
Q

Comorbid condition: MI Treatment

A

First Line: beta blocker the ACEI/ARB

Second Line: Aldosterone Antagonist

57
Q

Comorbid condition: Prior Ischemic Stroke Treamtne

A

First Line: ACEI or ARB

Second Line: CCB or Thiazide

58
Q

Hypertensive Crisis

A

Clinical syndrome - generally diastolic > 120 mmHg leading to vascular and organ damage

Divided into Two Types:

  • Emergencies (target organ damage)
  • Urgencies
59
Q

Hypertensive EMERGENCY

A

DBP > 150 mmHg in otherwise healthy person
or
DBP > 120 mmHg in individuals with pre-existing complications

Damage of target organs (brain, kidney, heart)

Immediate BP reduction is required (IV drugs)

60
Q

Hypertensive URGENCY

A

No target organ damage

Patients should be started of 2 oral drugs and close evaluation continued on an outpatient basis

61
Q

Hypertensive Emergency Causes

A
  • Essential hypertension
  • renal parenchymal disease
  • renovascular disease
  • pregnancy (eclampsia)
  • endocrine dysfunction
  • Drugs (cocaine, crack, etc)
  • Drug withdrawal
  • CNS disorder
  • Autonomic hypereactivity
62
Q

Hypertensive Emergency- Management

A

Admission into ICE- IV drugs
Arterial line to measure BP
BP should be progressively reduced using short acting titratable drugs
** abrupt dec. in BP can lead to MI, Stroke, and visual changes

Lowe BP no more than 25% with 1 hr. (goal is 100-110 mmHg DBP)
If stable further reduction to (160/100 mmHg SBP/DBP) within 2-6 hrs

63
Q

Hypertensive Emergency - Treatments

A 
Sodium Nitroprusside
Labetalol 
Fenoldopam 
Nicardipine
Nitroglycerin 
Diazoxide
Phentolamine
Esmolol
Hydralazine
64
Q

Sodium Nitroprusside

A

Always give IV (poisonous oral)
short half life (t1/2= 1-2 min)
requires continuous infusion
Prompt vasodilation and reflex tachycardia
causes peripheral vasodilation by direct effects on arterial and venous smooth muscle

AE:

  • hypotension, goose bumps, abdominal cramps, nausea, vomiting, headache
  • cyanide toxicity (rare) -metabolite (treat with sodium thiosulfate infusion)
65
Q

Labetalol

A

Combined beta and alpha blocker
IV bolus or infusion for hypertensive emergencies
t 1/2 = 3-6 hrs.
DOES NOT cause reflex tachycardia
Contraindications: Asthma, COPD, 2nd or 3rd degree AV blocks, or bradycardia

66
Q

Fenoldopam

A

Peripheral Dopamine (D1) receptor agonist
evokes arteriolar dilation
infusion for hypertensive emergencies
t 1/2 = 30 min
Maintains or increases renal perfusion as lowering BP
Promotes natures
safe in all hypertensive emergency (especially in patients with renal insufficiency)

67
Q

Nicardipine

A

Calcium channel blocker
IV infusion for hypertensive emergency
t 1/2 = 30 min
evokes reflex tachycardia

68
Q

Nitroglycerin

A

Vasodilator (more effect on veins than arteries)
DOC for hypertensive emergencies in patients with cardiac ischemia or angina or after bypass surgery
t 1/2 = 2-5 min
Hypotension = most serious side effect

69
Q

Diazoxide

A

Arteriolar dilation
Prevents vascular smooth muscle contraction by opening K+ channels and stabilizing the membrane potential
t 1/2 = 24 hrs
AE:
- Hypotension, reflex tachycardia, Na+ and H2O retention
- inhibits insulin release and can be used to treat hypoglycemia secondary to insulinoma

70
Q

Other options

A

Phentolamine:
DOC for patients with catecholamine released emergencies

Esmolol:
Often used for aortic dissection or post-operative hypertension

Hydralazine:
DOC in treating hypertensive emergencies in pregnancy related to eclampsia

Pharmacology (20 decks)

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