CARDIOVASCULAR- Pharmacology Flashcards
1
Q
Drugs used for Primary (essential) hypertension
A
Diuretics, ACE inhibitors, angiotensin II recetor blockers (ARBs), calcium channel blockers
2
Q
For Hypertension with Cardiac Heart failure, which drugs are recommended?
A
Diuretics, ACE inhibitors/ ARBs, β blockers (compensated CHF), aldosterone antagonists
3
Q
Which drugs must be used cautiously in decompensated CHF?
A
β blockers
4
Q
When are β blockers contraindicated?
A
Cardiogenic shock
5
Q
For patients with hypertension with Diabetes, which antihypertensive drugs are recommended?
A
ACE inhibitors/ ARBs. Calcium channel blockers, diuretics, β blockers, α blockers
6
Q
Which antihypertensive drugs work as protective against diabetic nephropathy?
A
ACE inhibitors/ ARBs
7
Q
Dihydropyridine Calcium channel blockers
A
Amlodipine, nimodipine, nifedipine
8
Q
Non Dihydropyridine Calcium channel blockers
A
Diltiazem, Verapamil
9
Q
Mechanism of action of Calcium channel blockers
A
Block voltage dependent L type calcium channels of cardiac and smooth muscle, thereby reduce muscle contractility
10
Q
Which Calcium channel blockers have more effect in vascular smooth muscle?
A
Amlodipine= nifedipine> diltiazem> verapamil
11
Q
Which Calcium channel blockers have more effect in heart?
A
Verapamil> diltiazem> amlodipine= nifedipine
12
Q
Clinical use for Dihydropyridine Calcium channel blockers
A
(Except nimodipine)
Hypertension, angina (including prinzmetal), Raynaud phenomenom
13
Q
Clinical use for Non Dihydropyridine Calcium channel blockers
A
Hypertension, angina, atrial fibrilation/ flutter
14
Q
Clinical use for Nimodipine
A
Subarachnoid hemorrhage (prevents cerebral vasospasm)
15
Q
These are Toxic effects of Calcium channel blockers
A
Cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, and constipation
16
Q
Mechanism of Action of Hydralazine
A
↑ cGMP→ smooth muscle relaxation
Vasodilates arterioles> vein
17
Q
Which effect does Hydralazine has?
A
Afterload reduction
18
Q
Clinical use for Hydralazine
A
Severe hypertension, CHF
First line therapy for hypertension in pregnancy
19
Q
First line therapy for hypertension in pregnancy
A
Metildopa
Hydralazine
20
Q
Which drug is coadministered with hydralazine to prevent reflex tachycardia?
A
β blockers
21
Q
Why are β blockers coadministered with hydralazine?
A
To prevent reflex tachycardia
22
Q
Toxic effects of Hydralazine?
A
Compensatory tachycardia, fluid retention, nausea, headache, angina
Lupus like syndrome
23
Q
When is Hydralazine contraindicated?
A
In angina/ Coronary artery disease
24
Q
In hypertensive emergency which are the common used drugs?
A
Nitroprusside, nicardipine, clevidipine, labetalol, fenoldopam
25
How long does it takes for Nitroprusside to act?
Short acting
26
Which is the mechanism of action of Nitroprusside
↑ cGMP via direct release NO
27
Possible secondary effect of Nitroprusside
Can cause cyanide toxicity (releases cyanide)
28
Mechanism of Action of Fenoldopam
Dopamine D1 receptor agonist
29
Effect of Fenoldopam
Coronary, peripheral, renal, and splanchic vasodilation
30
Clinical effect of Fenoldopam
↓ BP
| ↑ natriuresis
31
Which is the mechanism of action of Nitroglycerin, isosorbide dinitrate?
Vasodilate by ↑ NO in vascular smooth muscle→ ↑ in cGMP and smooth muscle relaxation.
32
Which vessels are more dilated with Nitroglycerin, isosorbide dinitrate?
Dilates veins >> arteries
33
What is the effect of Nitroglycerin, isosorbide dinitrate?
↓ preload
34
Clinical use for Nitroglycerin, isosorbide dinitrate
Angina, acute coronary syndrome, pulmonary edema
35
Toxic effect of Nitroglycerin, isosorbide dinitrate
Reflex tachycardia, hypotension, flushing, headache, "Monday disease" in industrial exposure
36
Which drug helps with the reflex tachycardia caused by Nitroglycerin, isosorbide dinitrate?
β blockers
37
What is the "Monday disease" ?
Development of tolerance for the vasodilating action during the work week and loss of tolerance over the weekend results in tachycardia, dizziness, and headache upon reexposure
38
Which is the goal in antianginal therapy?
Reduction of myocardial O2 consumption (MVO2) by ↓ 1 or more of the determinants of MVO2
39
Which are determinants of myocardial O2 consumption?
End diastolic volume
Blood pressure
Heart rate
Contractility
40
Which are the main medications in Antianginal therapy?
Nitrates
β Blockers
Nitrates + β blockers
41
What is affected with nitrates?
Preload
42
Which effects do Nitrates have as Antianginal therapy?
```
↓ End diastolic volume
↓ Blood pressure
↑ Contractility (reflex response)
↑ Heart rate (reflex response)
↓ Ejection time
↓ MVO2
```
43
Effects of β Blockers as Antianginal Therapy
```
↑ End diastolic volume
↓ Blood pressure
↓ Contractility
↓ Heart rate
↑ Ejection time
↓ MVO2
```
44
What effect do Nitrates + β blockers have as Antianginal Therapy?
```
No effect or ↓ End diastolic volume
↓ Blood pressure
Little/ no effect in Contractility
↓ Heart rate
Little/ no effect on Ejection time
↓↓ MVO2
```
45
Which calcium channel blocker has similar effects to nitrates in Antianginal therapy?
Nifedipine
46
Which drugs are contraindicated in Angina?
partial β agonists
47
Which partial β agonists are contraindicated in Angina?
Pindolol and Acetabutol
48
Lipid lowering agents
```
HMG- CoA reductase inhibitors
Niacin (vitamin B3)
Bile acid resins
Cholestherol absorption blockers
Fibrates
```
49
HMG-CoA reductase inhibitors
```
Lovastatin
Pravastatin
Simvastatin
Atorvastatin
Rosuvastatin
```
50
Which effects do HMG-CoA reductase inhibitors have?
↓↓↓ LDL
↑ HDL
↓ Tiglycerides
51
What is the mechanism of action of Pravastatin?
Inhibit conversion of HMG- CoA to mevalonate, a cholesterol precursor
52
Side effect of HMG-CoA reductase inhibitors
Hepatotoxicity (↑ LFTs), rhabdomyolisis
53
When do HMG-CoA reductase inhibitors have increased risk for rhabdomyolisis?
When used with fibrates and niacin
54
Effect of Niacin
↓↓ LDL
↑↑ HDL
↓ Tiglycerides
55
What vitamin is Niacin?
Vitamin B3
56
Which mechanism of action does Niacin has?
Inhibits lipolysis in adipose tissue, reduces hepatic VLDL synthesis
57
Possible side effects of Niacin
Red, flushed face
Hyperglycemia
Hyperuricemia
58
How do you decreased the probability of flushed face as a side effect of Niacin?
With aspirin or long term use
59
How is hyperglycemia manifested in Niacin administration?
Acanthosis nigricans
60
Which vitamin can exacerbate Gout?
Vitamin B3 (Niacin) because increases Hyperuricemia
61
Bile Acid Resins
Cholestyramine
Colestipol
Colesevelam
62
Effect of Bile Acid Resins
↓↓ LDL
Slightly ↑ HDL
Slightly ↑ Tiglycerides
63
Which is the mechanism of action of Bile acid resins?
Prevent intestinal reabsorption of bile acids; liver mistuse cholesterol to make more
64
What needs to be in mind before administering Bile acid resins?
Patients hate it- tastes bad and causes GI discomfort, ↓ absorption of fat soluble vitamins
65
Another side effect of Bile acid resins
Cholesterol gallstones
66
Cholesterol absorption blockers
Ezetimibe
67
What is the effect of Ezetimibe?
↓↓ LDL
68
Mechanism of action of Ezetimibe
Prevent cholesterol absorption at small intestine brush border
69
Side effect of Cholesterol absorption blockers
Rare ↑ LFTs, diarrhea
70
Name Fibrates
Gemfibrozil
Clofibrate
Bezafibrate
Fenofibrate
71
Effect of Fibrates
↓ LDL
↑ HDL
↓↓↓ Tiglycerides
72
Mechanism of action of Fibrates
Upregulate LPL → ↑ TG clearance
| Activates PPAR α to induce HDL synthesis
73
Side effects of Fibrates
Myositis (↑ risk with concurretn statins)
Hepatotoxicity (↑ LFTs)
Cholesterol gallstones
74
When is increased the risk for Cholesterol gallstones when using fibrates?
With concurrent bile acid resins
75
Cardiac glycoside
Digoxin
76
How are the pharmacologic properties of Digoxin
75% bioaviailability
20-40 % protein bound
t1/2= 40 hours, urinary excretion
77
Mechanism of action of digoxin
Direct inhibition of Na+/ K+ ATPase leads to indirects inhibition of Na+/ Ca2+ exchanger/ antiport.
↑ Ca2+ intracellular →positive inotropy. Stimulates vagus nerve → ↓ Heart rate
78
Clinical use for Digoxin
CHF (↑ contractility)
| Atrial Fibrilation
79
What effect does Digoxin has in Atrial Fibrilation?
↓ conduction at AV node and depression of SA node
80
Cholinergic side effects of Cardiac glycosides
Nausea, vomiting, diarhea, blurry yellow vision
81
ECG changes due to use of Digoxin
↑ PR, ↓ QT, ST scooping, T wave inversion, arrhytmia, AV block
82
Which electrolyte changes can Digoxin produce?
Hyperkalemia
83
What does Hyperkalemia caused by Cardiac glycosides indicate?
Poor prognosis
84
Which factros predispose to Digoxin toxicity?
Renal failure, hypokalemia, verapamil, amiodarone, quinidine
85
Why verapamil, amiodarone, quinidine increase the possibility of Digoxin toxicity?
↓ Digoxin clearance; displaces digoxin from tissue binding sites
86
Why does hypokalemia can increase the risk of toxic effects of Digoxin?
Permissive for digoxin binding at K+ binding site on Na+/ K+ ATPase
87
Antidote for Digoxin toxicity
Slowly normalize K+, cardiac pacer, anti digoxin Fab fragments, Mg2+
88
Class I Antiarrhytmics mechanism of Action
Na+ channel blockers
89
What effect do Class I Antiarrhytmics have?
Slow or Block (↓) conduction (especially in depolarized cells)
↓ slope of phase 0 depolarization and ↑ threshold for firing in abnormal pacemaker cells
90
Which is the dependant to use Class I Antiarrhytmics?
Are state dependent (selectively depress tissue that is frequently depolarized (eg. tachycardia))
91
Which state ↑ toxicity for all class I drug?
Hyperkalemia
92
How many classes of Antiarrythmics class I exist?
Class IA
Class IB
Class IC
93
Class IA Antiarrythmics
Quinidine
Procainamide
Disopyramide
94
Mechanism of Action of Class IA Antiarrythmics
↑ Action Potential duration, ↑ effective refractory period (ERP), ↑ QT interval
95
Clinical use for Class IA Antiarrythmics
Both atrial and ventricular arrythmias, especially re-entrant and ectopic Supraventricular tachycardia and VT
96
Toxic effect of Class IA Antiarrythmics
Thrombocytopenia
| Torsades de pointes
97
What is cinchonism?
Headache
| Tinnitus
98
Which Class IA Antiarrythmic causes cinchonism?
Quinidine
99
Class IA Antiarrythmics that can cause reversible SLE like syndrome
Procainamide
100
Class IA Antiarrythmic related to cause heart failure
Disopyramide
101
How Class IA Antiarrythmics can cause torsades de pointes?
Due to ↑ QT interval
102
Class IB Antiarrythmics
Lidocaine, Mexiletine
103
Class IB Antiarrythmics mechanism of Action
↓ Action Potential
104
Which tissue is preferentially affected with Class IB Antiarrythmics?
Ischemic or depolarized Purkinje and ventricular tissue
105
Another drug that can also fall into the Class IB Antiarrythmics
Phenytoin
106
Clinical use for Class IB Antiarrythmics
Acute ventricular arrhytmias (especially post MI)
| Digitalis induced arrhytmias
107
Which Antiarrythmics are better for post MI?
Class IB Antiarrythmics
108
Toxic effects of Class IB Antiarrythmics
CNS stimulation/depression
| Cardiovascular depression
109
Class IC Antiarrythmics
Flecainide
| Propafenone
110
Which is the mechanism of action of Class IC Antiarrythmics?
Significantly prolongs refractory period in AV node
| Minimal effect in Action potential duration
111
Clinical use for Class IC Antiarrythmics
Supraventricular Tachycardia, including atrial fibrilation
112
Antiarrythmics used as last resort in refractory Ventricular Tachycardia
Class IC Antiarrythmics
113
When are Class IC Antiarrythmics contraindicated?
post MI
| Structural and ischemic heart disease
114
Toxic effect of Class IC Antiarrythmics
Proarrhytmic
115
Who are Antiarrhytmics class II?
β blockers
| Metoprolol, propanolol, esmolol, atenolol, timolol, carvedilol
116
Mechanism of action Antiarrhytmics class II
Decrease SA and AV nodal activity by ↓ cAMP, ↓ Ca2+ currents
| Suppress abnormal pacemakers by ↓ slope of phase 4
117
What effet do Antiarrhytmics class II have in AV node?
AV node particularly sensitive- ↑ PR interval
118
Which characteristic does Esmolol has as Antiarrhytmic?
Very short acting
119
Clinical use for Antiarrhytmics class II
Supraventricular Tachycardia
| lowing ventricular rate during atrial fibrillation and atrial flutter
120
Toxic effects of β blockers
Incompetence, exacerbation of COPD and asthma
Cardiovascular effects (bradycardia, aV block, CHF)
CNS effects (sedation, sleep alterations)
May mask the signs of hipoglycemia
121
Which Antiarrhytmic class II can cause dyslipidemia?
Metoprolol
122
Side effect of Propanolol
Can excacerbate vasospasm in Prinzmetal angina
123
When are Antiarrhytmics class II contraindicated?
In cocaine users
124
Why are β blockers contraindicated for cocaine users?
Risk of unopposed α adrenergic receptor agonist activity
125
How is β blocker overdose treated?
With Glucagon
126
Antiarrhytmics class III
```
AIDS:
Amiodarone
Ibutilide
Dofelitide
Sotalol
```
127
How do Antiarrhytmics class III work
K+ channel blockers
128
Mechanism of action of Antiarrhytmics class III
↑ Action Potential duration, ↑ Effective refractory Potential
129
When are Antiarrhytmics class III used?
When other antiarrhytmics fail
130
Which ECG change do Antiarrhytmics class III cause?
↑ QT interval
131
Clinical use of Antiarrhytmics class III
Atrial fibrillation, atrial flutter
132
Antiarrhytmics class III used for Ventricular Tachycardia
Amiodarone
| Sotalol
133
Toxic effects caused by Sotalol
Torsades de pointes
| Excessive β blockade
134
Side effect of Ibutilide
Torsades de pointes
135
You need to be careful when using amiodarone because it can cause...
```
Pulmonary fibrosis
Hepatotoxicity
Hypothyroidism/Hyperthyroidism
Corneal deposits
Skin deposits (gray/blue) resulting in photodermatitis
Neurologic effects
Constipation
Cardivascular effects
```
136
Which is the reason amiodarone can cause Hypothyroidism/Hyperthyroidism?
Is 40% iodine by weight
137
Cardiac side effect of Amiodarone
Bradycardia
Heart block
CHF
138
When using amiodarone what do you need to check?
PFTs (pulmonary function tests)
LFTs (liver function tests)
TFTs (Tyroid function tests)
139
Which antiarrhytmic effects does amiodarone has?
Class I, II, III, IV effects and altered the lipid membrane
140
Class IV Antiarrhytmics
Verapamil
| Diltiazem
141
Effect of Class IV Antiarrhytmics
Ca2+ channel blockers
142
Mechanism of Action of Class IV Antiarrhytmics
↓ Conduction velocity
| ↑ Effective refractory period
143
ECG changes with Ca2+ channel blockers
↑ PR interval
144
Clinical use for Class IV Antiarrhytmics
Prevention of nodal arrhytmias (eg. SPT)
| Rate control on Atrial Fibrilation
145
Toxic effect of Class IV Antiarrhytmics
Constipation, flushing, edema, Cardiovascular effects
146
Which cardiovascular side effects do Class IV Antiarrhytmics have?
CHF
AV block
Sinus node depression
147
Which are other antiarrhythmics that aren't classified with other families?
Adenosine
| Mg2+
148
Mechanism of action of Adenosine
↑ K+ out of cells → hyperpolarizing the cell and ↓ Ica
149
Drug of choice in diagnosing/ abolishing supraventricular tachycardia
Adenosine
150
How long does it takes for Adenosine to act?
Very short acting (15 seg)
151
Adverse effects of Adenosine
Flushing
Hypotension
Chest pain
152
Who block the effects of Adenosine?
Effects blocked by Theophylline and caffeine
153
When is Mg2+ used as Antiarrhythmic?
Effective in torsades de pointes and digoxin toxicity
