Antihypertensives Flashcards
0
Q
ACE inhibitors mechanism
A
No reflex tachycardia, etc.
Decreased sodium and H2O retention
Increased renin
Increased bradykinin (potent vasodilator)
1
Q
ACE inhibitor drugs
A
Captopril
Enalapril
Lisinopril
2
Q
ACE inhibitors Description
A
Decrease PVR therefore decrease BP
- *Decrease diabetic nephropathy**
- *Decrease albuminuria**
3
Q
ACE inhibitors indications
A
HTN-must effective in young white patients (black and elderly have low renin … add a diuretic)
CHF
DOC patients s/p MI
4
Q
ACE inhibitors Adverse
A
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
Q
ACE inhibitor contraindications
A
Pregnancy–fetal hypotension leading to renal agenesis and anuria
Hyperkalemia
Bilateral renal a. stenosis
6
Q
Angiotensin receptor blockers (ARB) Drugs
A
Losartan
Valsartan
7
Q
Angiotensin receptor blockers description
A
Alternative to ACE - I
Blocks the ATII receptor
8
Q
Angiotensin receptor blockers mechanism
A
Very similar to ACE-I
Decreased PVR decreased BP
Decreased nephrotoxicity
No effect on bradykinin
9
Q
Angiotensin receptor blockers Indication
A
HTN (white people)
CHF
s/p MI
10
Q
Angiotensin receptor blockers adverse effects
A
Similar to ACE-I
Angio edema risk is much lower (related to bradykinin)
11
Q
Angiotensin receptor blocker contraindications
A
Pregnancy - fetal hypotension, renal failure, anuria
Hyperkalemia
Bilateral renal a. stenosis
12
Q
Renin inhibitor drugs
A
Aliskiren
13
Q
Renin inhibitor mechanism
A
Inhibits production of both ATII and aldosterone
14
Q
Aliskiren contraindications
A
Pregnancy
Bilateral renal a. stenosis
Hyperkalemia
15
Q
Calcium channel blocker drugs
A
Verapamil
Diltiazem
Nifedipine
Amlodipine
16
Q
Verapamil Description
A
Calcium channel blocker
Non dihydropyridine
Least selective
Cardiac and vascular smooth muscle effects
17
Q
Verapamil mechanism
A
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
Q
Verapamil indication
A
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
Q
Verapamil adverse
A
High dose of short acting -> increased risk for MI
- *Reflex tachycardia**
- Constipation*
20
Q
Verapamil contraindication
A
**CHF due to -ve inotropic effects **
21
Q
Diltiazem description
A
Calcium channel blocker
Non dihydropyridine
A little more selective for vasculature than verapamil but still affects heart
Good side effect profile
22
Q
Diltiazem mechanism
A
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
Q
Diltiazem indication
A
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
