Antihypertensives Flashcards Preview

Pharmacology > Antihypertensives > Flashcards

Flashcards in Antihypertensives Deck (135):
0

ACE inhibitor drugs

Captopril
Enalapril
Lisinopril

1

ACE inhibitors mechanism

No reflex tachycardia, etc.
Decreased sodium and H2O retention
Increased renin
Increased bradykinin (potent vasodilator)

2

ACE inhibitors Description

Decrease PVR therefore decrease BP
**Decrease diabetic nephropathy**
**Decrease albuminuria**

3

ACE inhibitors indications

HTN-must effective in young white patients (black and elderly have low renin ... add a diuretic)

CHF

DOC patients s/p MI

4

ACE inhibitors Adverse

**Hyperkalemia**
**Dry cough**
Rash, fever, altered taste, hypotension
**Angioedema (supervise first dose)***
Acute renal failure in patients with **BILATERAL RENAL ARTERIAL STENOSIS**
Decreased vasoconstriction on efferent therefore decreased GFR, **elevated creatinine**

5

ACE inhibitor contraindications

Pregnancy--fetal hypotension leading to renal agenesis and anuria
Hyperkalemia
Bilateral renal a. stenosis

6

Angiotensin receptor blockers (ARB) Drugs

Losartan
Valsartan

7

Angiotensin receptor blockers description

Alternative to ACE - I
Blocks the ATII receptor

8

Angiotensin receptor blockers mechanism

Very similar to ACE-I
Decreased PVR decreased BP
Decreased nephrotoxicity
***No effect on bradykinin***

9

Angiotensin receptor blockers Indication

HTN (white people)
CHF
s/p MI

10

Angiotensin receptor blockers adverse effects

Similar to ACE-I
Angio edema risk is much lower (related to bradykinin)

11

Angiotensin receptor blocker contraindications

Pregnancy - fetal hypotension, renal failure, anuria
Hyperkalemia
Bilateral renal a. stenosis

12

Renin inhibitor drugs

Aliskiren

13

Renin inhibitor mechanism

Inhibits production of both ATII and aldosterone

14

Aliskiren contraindications

Pregnancy
Bilateral renal a. stenosis
Hyperkalemia

15

Calcium channel blocker drugs

Verapamil
Diltiazem
Nifedipine
Amlodipine

16

Verapamil Description

Calcium channel blocker
Non dihydropyridine
**Least selective**
Cardiac and vascular smooth muscle effects

17

Verapamil mechanism

Bind to L type calcium channels in the heart and muscle of the peripheral vasculature ->decreased calcium entry -> relaxation of muscle -> -ve inotropism and/or vasodilation

18

Verapamil indication

Used in patients with angina, migraine or SVT
Used when first line agents are ineffective or contraindicated (patients with diabetes, asthma and PVD)
Effective in blacks and whites
Intrinsic natriuretic effect -> no need to add a diuretic

19

Verapamil adverse

High dose of short acting -> increased risk for MI
**Reflex tachycardia**
******Constipation******

20

Verapamil contraindication

***CHF due to -ve inotropic effects ***

21

Diltiazem description

Calcium channel blocker
Non dihydropyridine
A little more selective for vasculature than verapamil but still affects heart
Good side effect profile

22

Diltiazem mechanism

Bind to L type calcium channels in the heart and muscle of the peripheral vasculature -> decreased calcium entry -> relaxation of muscle -> -ve inotropic effects and/or vasodilation

23

Diltiazem indication

Pts with angina, migraine or SVT
Used when first line agents are ineffective or contraindicated (diabetes, asthma and PVD)
Effective in blacks and whites
Intrinsic natriuretic effect -> no need to add a diuretic

24

Diltiazem Adverse

High dose short acting increases risk of MI
Reflex tachycardia

25

Nifedipine and Amlodipine description

Dihydropyridines
Act only on smooth vascular muscle
Second gen amlodipine has little interaction with digoxin and warfarin

26

Nifedipine and amlodipine mechanism

Calcium channel blockers
Greater affinity for vasculature so they don't cause a decrease in CO
**Very useful for HTN but not arrhythmias**

27

Nifedipine and amlodipine indication

Used when first line agents are ineffective or contraindicated (diabetes, asthma, PVD)
Effective in blacks and whites
Intrinsic natriuretic effect -> no need to add a diuretic

28

Nifedipine and Amlodipine Adverse

Hypotension -> dizziness, HA, fatigue, peripheral edema
Bradycardia
Heart block

29

Thiazides drugs

Chlorthalidone
Hydrochlorothiazide
Metolazone

30

Thiazide indications

DOC for black and elderly (with normal renal and cardiac function)

31

Thiazide Mechanism

Increased sodium and H2O excretion therefore decreased ECF -> decreased CO and renal blood flow (in the long term, there is normal plasma volume but decreased PVR)

32

Thiazide adverse

**Hypokalemia**
Hyperuricemia
Hyperglycemia
Hypomagnesium
Hyperlipidemia

33

Thiazide contraindications

Diabetes

34

Loop Diuretics

Ethacrynic acid
Furosemide
Torsemide

35

Loop diuretics description

Prompt action in pts with poor renal function or heart failure

36

Loop diuretic mechanism

decreased renal vascular resistance
increased renal blood flow

37

Loop diuretics indication

DOC for pts with poor renal function or unresponsive to other diuretics *ex. thiazide*

38

Amiloride and Triamterene

ENaC
Decrease the potassium lost in urine caused by thiazide or loop diuretics

40

Disopyramide description
Antiarrhythmic

Class 1A
Stronger -ve inotrope than quinidine and procainamide
Strong antimuscarinic properties
Causes peripheral vasoconstriction
Blocks K channels

41

Disopyramide indication
Antiarrhythmic

Supraventricular and ventricular arrhythmia

42

Disopyramide adverse
Antiarrhythmic

Pronounced -ve inotropic effects
Cardiac failure without preexisting myocardial dysfunction
Severe antitmuscarinic effects (dry mouth, urine retention, blurred vision, constipation, etc)

43

Class 1 A general
Antiarrhythmic

Sodium channel blockers
Never drug of choice
Ventricular and Supraventricular

44

Class 1A effect
Antiarrhythmic

Slow phase 0 depolarization (sodium channels)
Also prolongs phase 3 (potassium channels)

Slowing of conduction, prolonging AP & increase ventricular effective refractory period

Intermediate speed of association with activated and inactivated Na channels -> affects normal healthy tissue too

Procainamide, Disopyramide, and Quinidine

45

Class 1 B general
Antiarrhythmic

Sodium channel blocker
Ventricular only

46

Class 1 B effect
Antiarrhythmic

Slows phase 0 and decreases slope of phase 4
Minimally shortens phase 3 repolarization (no clinical effect)
Little effect of depolarization in normal cells
Rapid association/dissociation with sodium channels

Used primarily in ventricular arrhythmia (atria is too fast)

47

Tocainide adverse
Antiarrhythmic

Severe hematological and pulmonary toxicity

48

Mexiletine adverse
Antiarrhythmic

Mainly CNS and GI

49

Lidocaine is drug of choice when?
Antiarrhythmic

DOC for V tach and V fib after cardioversion in acute ischemia

50

Lidocaine toxic dose produces
Antiarrhythmic

Convulsions and coma

51

Class 1 C general
Antiarrhythmic

Sodium channel blocker
Ventricular and supraventricular

52

Class 1C effect
Antiarrhythmic

Markedly depress phase 0 of AP, no change in repolarization (K)
Slowing of conduction of AP, but little effect on duration or ventricular effective refractory period

Associate and re-associates slowly with sodium channels -> prominent effects even in normal cells
***Most likely of class 1s to cause arrhythmia***

53

Propafenone description
Antiarrhythmic

Class 1C
Decreases slope of phase 0 without affecting duration of AP

Prolongs conduction and refractoriness in all areas of the myocardium

Reduces spontaneous automaticity

54

Propafenone indication
Antiarrhythmic

Life threatening ventricular arrhythmia and maintenance of normal sinus rhythm in patients with symptomatic a fib

55

Class II mechanism
Antiarrhythmic

Beta blockers
Supraventricular only

56

Class II effect
Antiarrhythmic

Reduce HR and myocardial contractility (beta 1)

Prolongs repolarization at AV node and decreased slope of phase 4 (blocking adrenergic release) -> slows conduction of impulses through the myocardial conduction

Reduce rate of spontaneous depolarization in cells with pacemaker activity
Little effect on AP in most myocardial cells

57

Class III mechanism
Antiarrhythmic

K channel blockers
Ventricular and supraventricular

58

Class III effect
Antiarrhythmic

Blocks repolarizing K channels
Prolongs AP (and QT interval) without altering phase 0 or resting membrane potential
Prolongs effective refractory period

**ALL have potential to induce arrhythmia**

59

Amiodarone adverse main
Antiarrhythmic

Interstitial pulmonary fibrosis
Blue / gray skin discoloration due to iodine accumulation

60

Amiodarone contraindications
Antiarrhythmic

Patients taking digoxin, theophylline, warfarin, quinidine or have bradycardia, SA or AV block, severe hypotension, or respiratory failure

61

Dofetilide
Antiarrhythmic

Potent and pure K channel blocker
Class III

62

Dofetilide indication
Antiarrhythmic

Maintaining or conversion to norma sinus rhythm in chronic a fib / flutter

63

Dofetilide Adverse
Antiarrhythmic

HA, chest pain, dizziness, v tach, Torsades (prolongs QT interval)

64

Class IV mechanism
Antiarrhythmic

Calcium channel blockers
Supraventricular only

65

Class IV effect
Antiarrhythmic

Blocks L type calcium channels
Decrease inward calcium current -> decrease rate of phase 4 spontaneous depolarization
Slows conduction in SA and AV nodes
Major effects on vascular smooth muscles and heart

Use primarily for supraventricular arrhythmia

66

Digoxin description
Antiarrhythmic

Shorten refractory period in atrial and ventricular myocardial cells

Prolongs effective refractory period and diminishes conduction velocity in AV node

67

Digoxin Indication
Antiarrhythmic

Control ventricular response rate in A fib and flutter with impaired left ventricular function or heart failure

Mechanism of action
Heart failure- +ve inotrope -> increases intracellular calcium
Arrhythmia - **Direct AV node blocking** effects (inhibits calcium currents) and vagomimetic properties (activates ACh mediated K currents in the atrium)

Major indirect actions
Hyperpolarization, shorten atrial APs, increase AV node refractoriness -> decrease fraction of impulses that are conducted through the node

68

Digoxin adverse
Antiarrhythmic

Toxic dose -> ectopic ventricular beats (v tach and V fib)

69

Adenosine description
Antiarrhythmic

Naturally occurring nucleoside (P1r agonist)

High dose: Decrease conduction velocity and prolongs refractory period as well as decreases automaticity in **AV node**

70

Adenosine indication
Antiarrhythmic

***DOC for abolishing acute SVT (emergency situations)***
Lidocaine is used in acute V tach emergencies

Mechanism of action
Enhanced K conductance; decrease cAMP mediated Calcium influx -> hyperpolarization, especially in the AV node

71

Adenosine PK
Antiarrhythmic

half life 15 sec

72

Adenosine adverse
Antiarrhythmic

Low toxicity - Flushing, burning, chest pain (similar to MI, hypotension)

Bronchoconstriction in asthmatics (may last up to 30 mins)

73

Magnesium description
Antiarrhythmic

Functional calcium antagonist

74

Magnesium indication
Antiarrhythmic

Torsades de pointes (prolonged QT interval)
Digitalis induced arrhythmia (lidocaine also used)
Prophylaxis of arrhythmia in acute MI

75

Atropine indication
Antiarrhythmic

**Used in bradyarrhythmia** to decrease vagal tone -> increased HR

76

Rhythm control
Antiarrhythmic

Restore and maintain sinus rhythm -> generally involves drugs acting on the AV node to slow conduction
Class IC (flecainide and propfenone) and Class III (amiodarone and dofetilide)

77

Rate Control
Antiarrhythmic

Control ventricular rate while allowing atrial fibrillation to continue
-ve dromotropic agents to slow conduction in the AV node

Calcium channel blockers, Beta blockers, digoxin

78

In the treatment of hypertension, a reduction in cardiac output is most likely to result in the development of which of the following?
Chronic cough
Periorbital edema
Peripheral edema
Peripheral neuropathy
Type 2 Diabetes

Peripheral edema

79

A reduction in body fluid volume is most likely to result in the development of what?

Reflex tachycardia

80

One of the potential consequences of reducing blood pressure is increasing renin activity. Which of the following agents affects the renin-angiotensin process in the body?
Atenolol
Captopril
Minoxidil
Nifedipine
Verapamil

Captopril

81

Spironolactone
Eplerenone

Aldosterone antagonist -> inhibition of Na+ and H2O retention -> inhibition of vasoconstriction
Decreased cardiac remodeling
**1st line in patients with HTN and severe LV dysfunction**
-reduced K+ excretion-> risk of hyperkalemia

82

Atenolol & Metoprolol mechanism

Beta 1 selective
Decreased CO, contractility and HR
Decreased CNS sympathetic output (especially with exercise)
Decreased NE and renin (Beta1) -> decreased ATII and aldosterone

83

Atenolol & Metoprolol, Propanolol, Pindolol indication

More effective in young/white patient

DOC only for patients with CAD or left ventricular dysfunction and HTN

84

Atenolol & Metoprolol, Propranolol, Pindolol PK

May take weeks to develop full effects

85

Atenolol, Metoprolol, Propranolol, Pindolol Adverse

Bradycardia, CNS effects, hypotension, impotence, lipid disturbance (decreased HDL, increased TAG), hypoglycemia
Abrupt withdrawal -> angina and MI in patients with heart disease

86

Propranolol contraindication

Asthma and COPD, sinus bradycardia

87

Pindolol, Propranolol, Atenolol, Metoprolol Contraindication

Sinus bradycardia, mask symptoms of hypoglycemia (diabetics)

88

Pindolol indication

B partial agonist
Preferred beta blocker in pregnancy

89

Doxazosin, Prazosin, Terazosin Class

alpha blockers

90

Alpha blocker drugs for HTN

Doxazosin, Prazosin, Terazosin

91

Doxazosin, Prazosin, Terazosin Mechanism

Alpha blockers
Decreased PVR and MAP by relaxation of arterial and venous smooth muscle

**Minimal change in CO, renal blood flow and GFR -> no long term tachycardia**

92

Doxazosin, Prazosin, Terazosin Description

Competitive inhibition of alpha one receptors

Sodium and Water retention-> usually give with a diuretic

93

Doxazosin, Prazosin, Terazosin Indication

Alpha blocker
Mild to moderate HTN in combination with propranolol or a diuretic (less common now due to adverse effects)

***BPH***

94

Doxazosin, Prazosin, Terazosin Adverse

**Reflex tachycardia and orthostatic hypotension may be seen with first dose, but not long term (alpha 2 blocks response by inhibiting NE) -> ameliorate with beta blocker

Dizziness, drowsiness, HA, fatigue, nausea, palpitations

95

Doxazosin contraindications

Has been shown to increase rate of CHF

96

Labetalol class

mixed alpha beta blocker

97

Labetalol description

NO reflex tachycardia or increased CO (beta 1 effect is greater)
**Safe in PREGNANCY**

98

Labetalol indication

long term treatment of HTN

HTN emergencies: IV admin-> rapid drop in BP

99

Labetalol Adverse effects

Orthostatic hypotension

100

Labetalol contraindication

Pheochromocytoma

101

Clonidine & methyldopa class

central acting alpha 2 agonist

102

Central acting alpha 2 agonist description
Clonidine & Methyldopa

Does not decrease renal blood flow or GFR

103

Clonidine mechanism

Decreases sympathetic outflow (NE) by acting on presynaptic auto receptors -> decreases PVR and CO -> decreases BP

104

Clonidine PK

Oral; well absorbed. Administer with diuretic (sodium and water retention)

105

Clonidine adverse

Sedation, dry mouth, dizziness, HA, sexual dysfunction are common
Rebound HTN after abrupt withdrawal

106

Methyldopa mechanism

Decreased sympathetic outflow -> decreased PVR and BP
CO not affected

107

Methyldopa indication

**DOC Pregnancy induced HTN**
Renal insufficiency

108

Methyldopa PK

Oral; well absorbed
Administer with diuretic

109

Methyldopa adverse

Sedation, dry mouth, dizziness, HA, sexual dysfunction are common
Rebound HTN after abrupt withdrawal

110

Methyldopa contraindication

Can cause positive Coombs test, hemolytic anemia, hepatitis

111

Hydralazine class

Direct vasodilator

112

Hydralazine description

Never 1st line treatment
Direct acting smooth muscle relaxant
Reflex tachycardia, increased plasma renin ->Sodium and water retention
(coadmin with a diuretic and betablocker)

113

Hydralazine Mechanism

Opening of Potassium channels in smooth muscle -> arteriolar dilation (NOT venous)

114

Hydralazine Indication

DOC pregnancy induced hypertensive emergencies related to eclampsia

115

Hydralazine PK

Oral or IV

116

Hydralazine Adverse

HA, tachycardia, nausea, sweating, flushing
**Lupus like syndrome**
Reflex tachycardia and fluid retention
Volume overload -> edema and CHF

117

Minoxidil (Rogaine) class

direct vasodilator

118

Minoxidil (Rogaine) description

Never 1st line treatment
Direct acting smooth muscle relaxant
Reflex tachycardia, increased plasma renin ->Sodium and water retention
(coadmin with a diuretic and betablocker)

119

Minoxidil (Rogaine) mechanism

Opening of Potassium channels in smooth muscle -> arteriolar dilation (NOT venous)

120

Minoxidil (Rogaine) Indication

Severe malignant HTN

Male pattern baldness (hypertrichosis)

121

Minoxidil (Rogaine) Adverse

HA, tachycardia, nausea, sweating, flushing
Reflex tachycardia and fluid retention
Volume overload -> edema and CHF

122

Bosentan class

Non selective endothelin receptor blocker

123

Bosentan description

Blocks the endothelin mediated (ETa and ETb) vasoconstriction

124

Bosentan contraindications

PREGNANCY CATEGORY X

125

Epoprostenol description

synthetic PGI2

126

Epoprostenol mechanism

Lowers peripheral, *pulmonary* and coronary resistance

127

Bosentan indication

Pulmonary HTN

128

Epoprostenol indication

Pulmonary HTN

129

Epoprostenol PK

continuous IV infusion

130

Epoprostenol Adverse

Flushing, HA, ****JAW PAIN****, diarrhea, arthralgia

131

Typical 1st line treatment

ACE-I's ARB's

132

1st line in patients with acute or chronic CAD

ACE-I's, or ARB's and add Beta blocker

133

Patients with LV dysfunction first line treatment

Thiazide or loop diuretic and beta blocker along with ACE-I or ARB (plus hydralazine and isosorbide dinitrate if black)

134

HTN treatment for MI patients

Begin on beta blocker before adding ACE-I or ARB

135

HTN treatment for patients who have a history of ischemic stroke

Get an ACE-I or ARB and a thiazide diuretic