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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
Calcium channel blockers- PK
High-doses of short-acting dihydropyridine blockers can increase risk of MI (due to reflex stimulation) Sustained release preparations are preferred
26
Calcium channel blockers- AE
Verapamil - Constipation, negative inotropic signals, gingival hyperplasia Dihydropyridines - hypotension, peripheral edema (feet/ankles), dizziness, headache, fatigue, gingival hyperplasia, flushing, REFLEX TACHYCARDIA (short-acting preparations)
27
Calcium channel blockers Contraindications
Non-dyhyrdopyridines - contraindicated in patients taking b-blockers or who have a 2nd or 3rd degree AV block, or severe left ventricular systolic dysfunction
28
Diuretic Drugs and MOA
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
29
Thiazides- Clinical Apps.
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
Thiazides AE
``` Hypokalemia Hyperuricemia Hyperglycemia Hypomagnesium Hyperchlosterolemia Sex dysfunction ```
31
Loop Diuretics (furosemide)
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
K+ sparing Diuretics MOA and uses
Dec. loss of K+ in the urine due to thiazide or loop diuretics used in combination therapy
33
Aldosterone Antagonist clinical application
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
Beta Blocker Drugs and clinical applications
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
Beta-blockers: MOA and PK
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
Beta-blockers AE
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
Alpha 1 blockers Drugs MOA and effects
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
Alpha 1-blockers - Clinical Applications
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
Alpha 1 blockers AE
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
Mixed Alpha and Beta blocker: PK, advantages, AE
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
Central alpha 2- agonist
Clonidine | Methyldopa
42
Clonidine: MOA, Uses, AE
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
Methyldopa: MOA, Uses, AE
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
Direct Vasodilators
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
Hydralazine: PK, Uses, AE
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
Minoxidil: Uses, AE
Causes direct peripheral vasodilation of the arterioles Uses: - oral treatment for severe malignant hypertension AE: - reflex tachycardia, and fluid retention - hypertrichosis (baldness treatment)
47
Pulmonary Hypertension
An increase in BP in the pulmonary artery, vein, or capillaries Tx: Prostaglandins Inhibitors of endothelin synthesis vasodilators
48
Epoprostenol
Synthetic PGI2 lowers peripheral, pulmonary, and coronary resistance Given via continuous IV infusion AE: flushing, headache, jaw pain, diarrhea, and arthralgias
49
Bosentan
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
Sildenafil
Inhibitor of PDE5 (phosphodiesterase 5) Inc. cGMP = smooth muscle relaxation AE: headache, flushing, dyspepsia, cyanopsia Contraindicated with Nitrates
51
Comorbid condition: None Treatment
First Line: ACEI or ARB, CCB, or thaizide Second Line: beta blockers, aldosterone antagonist
52
Comorbid condition: Acute or Chronic CAD Treatment
First Line: beta-blockers + ACEI or ARB Second Line: Thaizide, CCB
53
Comorbid condition: Chronic Kidney Disease Treatment
First Line: ACEI or ARB Second Line: CCB or Thiazide
54
Comorbid condition: Diabetes treatment
First Line: ACEI or ARB Second Line: CCB or Thiazide
55
Comorbid condition: HF treatment
First Line: ACE or ARB + thiazide (or Loop) + beta blocker Second Line: Aldosterone antagonist, hydrazine/isosorbide dinatrate (black)
56
Comorbid condition: MI Treatment
First Line: beta blocker the ACEI/ARB Second Line: Aldosterone Antagonist
57
Comorbid condition: Prior Ischemic Stroke Treamtne
First Line: ACEI or ARB Second Line: CCB or Thiazide
58
Hypertensive Crisis
Clinical syndrome - generally diastolic > 120 mmHg leading to vascular and organ damage Divided into Two Types: - Emergencies (target organ damage) - Urgencies
59
Hypertensive EMERGENCY
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
Hypertensive URGENCY
No target organ damage Patients should be started of 2 oral drugs and close evaluation continued on an outpatient basis
61
Hypertensive Emergency Causes
- Essential hypertension - renal parenchymal disease - renovascular disease - pregnancy (eclampsia) - endocrine dysfunction - Drugs (cocaine, crack, etc) - Drug withdrawal - CNS disorder - Autonomic hypereactivity
62
Hypertensive Emergency- Management
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
Hypertensive Emergency - Treatments
``` Sodium Nitroprusside Labetalol Fenoldopam Nicardipine Nitroglycerin Diazoxide Phentolamine Esmolol Hydralazine ```
64
Sodium Nitroprusside
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
Labetalol
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
Fenoldopam
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
Nicardipine
Calcium channel blocker IV infusion for hypertensive emergency t 1/2 = 30 min evokes reflex tachycardia
68
Nitroglycerin
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
Diazoxide
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
Other options
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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