Exam #2 (Pharmacology) Flashcards
1
Q
Use Dependence
A
drug binds in the open/inactive state (0/3)
-better effect at higher HR
2
Q
Reverse Use Dependence
A
drug binds better to resting state (4)
-better effect at lower HR
3
Q
Class I
Class II
Class III
Class IV
A
Class I: Na+ channel blocker
Class II: Beta blocker
Class III: K+ channel blocker
Class IV: Ca2+ channel blocker
4
Q
EKG result
Na+ blocker
K+ blocker
A
Na+ Blocker = wider QRS
K+ Blocker = inc QT interval
5
Q
Procainamide adverse effect
A
Drug induced Lupus Syndrome
6
Q
Quinidine adverse effect
A
Cinchonism (headache, tinnitus, dizziness)
7
Q
Class IA Antiarrhythmic indication
A
short term atrial and ventricular arrhythmic treatment
8
Q
Class IB Antiarrhythmic indications
A
POST-MI ventricular arrhythmia
prevention of ventricular fibrillation
(ventricular only)
9
Q
lidocaine vs mexiletile therapeutic index
A
Lidocaine: Wide therapeutic index
Mexiletine: Narrow therapeutic index
10
Q
Class IC Antiarrhythmic indication
A
supraventricular arrhythmia and atrial fibrillation
11
Q
Flecainide vs Propafenone blockage
A
Flecainide: inhibits Na+ and K+ channelsPropafenone: only inhibits Na+ channels
12
Q
Amiodarone indication
A
severe ventricular arrhythmia
13
Q
Amiodarone adverse effects
A
- hypothyroidism but also hyperthyroidism
- Bradycardia/Heart blocker
- Hepatotoxicity
- Photodermatitis (blue skin)
- Pulmonary fibrosis
14
Q
Amiodarone half life
A
58 days (stays in lipid rich tissue)
15
Q
Dronedarone indication
A
atrial fibrillation
16
Q
Sotalol blockage
A
K+ and beta blocker
17
Q
1 for persistent atrial fibrillation
A
Dofetilide
18
Q
1 for chemical conversion of atrial flutter
A
Ibutilide
19
Q
REVERSE USE DEPENDENCE
A
Sotalol
20
Q
-olol
A
Beta blockers
21
Q
beta blocker adverse effects
A
- Bronchoconstriction -> fatigue
- Vasoconstriction -> sexual disfunction, dizziness (inhibits vasodilation)
- Decrease CO -> arrhythmias up abrupt withdrawal, bradycardia
22
Q
B-adrenergic Receptor Antagonist causes
A
Prolongs heart rate, AV conduction, and contractility
23
Q
beta blocker w most B1 selectivity
A
Metoprolol
24
Q
what to give for Acute arrhythmia that occurs during surgery
A
Esmolol
25
Acebutolol is a
B1 partial agonist
26
Non-dihydropyridine Ca2+ channel blockers and action
Verapamil
Diltiazem
-reduce phase 4 spontaneous depolarization on SA and AV node
27
USE DEPENDENT drugs
Diltiazem
| Verapamil
28
Verapamil indication
-prophylaxis for Paroxysmal Supraventricular Tachycardia
29
Digoxin causes
Increases contractility
| increase vagal tone (Slows AV node conduction)
30
Adenosine indication
WPW syndrome and AVNRT
31
pharmacologic stress test drug
adenosine
32
Atropine MOA and use
Muscarinic receptor antagonist blocking the vagal nerve stimulation to reverse sinus bradycardia and AV nodal block
33
what drug do you give for bradycardia
Atropine
34
what drug do you give for torsades de pointes
magnesium sulfate
35
-pril
ACE inhibitors
36
bradykinin effect on vasodilators
potent vasodilator (stimulates release of NO and prostacyclin)
37
ACEi and Angiotensin II Receptor BlockersContraindication
- Pregnancy (teratogenic)
| - Condition that cause low renal perfusion
38
ACEi and Angiotensin II Receptor Blockers adverse effects
```
Acute renal failure
Hyperkalemia
Angioedema
Hypotension due to hypovolemia
Alteration of taste
Neutropenia
```
39
ACE inhibitors Drug Interactions
- potassium supplements or K+ sparing diuretics = hyperkalemia
- NSAIDs
40
```
ACE inhibitor half life
Captopril
Enalapril
Fosinopril
Lisinopril
```
Captopril: 2hr
Enalapril: 11 hrs
Fosinopril: 11.5 hrs
Lisinopril: 12 hrs
41
ACEi with..... increase risk for angioedema
Sacubitril and Valsartan
42
-sartan
Angiotensin II Receptor Blockers
43
Losartan can also be used for
Diabetic nephropathy
44
Neprilysin inhibitor action
inhibits degrades vasoactive and natriuretic peptides, bradykinin and adrenomedullin
45
Renin Inhibitor
Aliskiren
46
Alpha 2 Receptor Agonist drug names
Clonidine
| Methyldopa
47
Alpha 2 Receptor Agonist MOA and cause
MOA: binds to presynaptic alpha 2 receptor in the brainstem and activates it leading to dec NE release and dec sympathetic tone
- Dec TPR
- Dec renal vascular resistance
- Dec heart rate and contractility (clonidine > methyldopa)
- Inc parasympathetic tone
48
Hypertension (ADHD) treatment
Clonidine
49
Clonidine adverse effect
Rebound hypertension if sudden discontinuation
50
Methyldopa prodrug derivative
α-methylnorepinephrine
51
Methyldopa adverse effect
Hemolytic Anemia
52
Alpha Receptor Antagonist MOA
antagonist of α1 adrenergic receptors leading to relaxation of smooth muscle and vessels
53
Alpha Receptor Antagonist advers effect
orthostatic hypotension (dec baroreflex)
54
Benign Prostatic Hyperplasia treatment
Doxazosin
55
-sin and Phenoxybenzamine
Alpha Receptor Antagonist
56
Phenoxybenzamine differs from other alpha receptor antagonists how
NON-SELECTIVE
| -bind both a1 and a2 receptors as well as H-1 histamine, acetylcholine and serotonin receptors
57
Pheochromocytoma treatment
Phenoxybenzamine
58
Reflexive Tachycardia
- Binds A1 receptors resulting in dec vasoconstriction
- Binds A2 receptors but not an inhibitor (agonist) so NE can’t bind to give negative feed back resulting in inc NE release. NE circulates to the heart leading to inc HR.
- in alpha antagonist
59
Atenolol special bc
selective B1 receptor blocker
60
Labetalol special bc
selectively blocks α1 & nonselective β1 and β2 receptor
| -dose-related falls in blood pressure without reflex tachycardia and without significant reduction in heart rate
61
Preferred drug of choice for hypertension
Calcium Channel Blockers
62
Dihydropyridines drugs
Nifedipine
| Amlodipine
63
Dihydropyridines act on and action
mainly blood vessels by blocking Ca2+ channels dec cAMP leading to vasodilation
64
-statins
Competitive inhibitors of HMG-COA reductase
65
statins lead to
Dec cholesterol
Up regulation of LDL receptors
Uptake of LDL from blood
Low intracellular cholesterol -> dec VLDL production
66
statin contraindications
Pregnant, becoming pregnant, or lactating
67
statin digest facts
- Best if taken at night bc thats when cholesterol production occurs
- Absorption best when taken with food
68
statin adverse
HEPATOTOXICITY
| MYOPATHY
69
statin plus what drug increase risk for myopathy
Amiodarone or Verapamil
70
Grapefruit Juice
increase bioavailability of statins
71
Pravastatin special bc
Metabolized non-P450 pathway (can be taken w other drugs)
72
Bile Acid Binding Resins drug name
Cholestyramine
73
Cholestyramine MOA
bind bile in the lumen of the intestines and prevents reabsorption -> loss of bile leads to increase bile acid formation from cholesterol reducing hepatic cholesterol
-dec cholesterol upregulates LDL receptors
74
Cholestyramine drug interactions
- Delayed/reduced absorption of oral medications
| - Prevention of absorption of fat soluble vitamins (dec bile)
75
```
Nicotinic Acid (Niacin)
MOA
```
inhibits hormone sensitive lipase in adipose tissue preventing the breakdowns of TAGs to free fatty acids and the transport of free fatty acids to the liver
-reduction of FA transport to liver -> dec hepatic TAG synthesis -> dec secretion of VLDL by liver -> dec LDL
76
main drug that increases HDL
niacin
77
Statins indication
Protocol to administer after MI no matter lipid levels
78
niacin + statin indignation
heterozygous familial hypercholesterolemia and other forms of hypercholesterolemia
79
Fibric Acid Derivatives drugs
Gemfibrozil
| Ezetimibe
80
Fibric Acid Derivatives MOA
inhibits cholesterol absorption by enterocytes in the small intestines by inhibiting transport protein NPC1L1
81
what inc/dec Ezetimibe blood level
- Increase levels when given w fibrates
| - Decrease levels when given w cholestyramine
82
PCSK9 inhibitors drugs
Alirocumab/Evolocumab
83
PCSK9 inhibitors MOA
inhibits the enzyme PCSK9 which binds to the LDL receptor targeting it for lysosomal degradation
-enhances the removal of LDL from circulation
84
MTP Inhibitor drug
Lomitapide
85
MTP Inhibitor MOA
Binds and inhibits microsomal triglyceride transfer protein (MTP), preventing the assembly of apo B containing lipoproteins in enterocytes and hepatocytes
86
Mipomersen MOA
antisense oligonucleotide that binds to human messenger ribonucleic acid (mRNA) for apo B-100 preventing its translation -> dec VLDL and LDL
87
binds to human messenger ribonucleic acid (mRNA) for apo B-100 drug name
Mipomersen
88
Nitrate MOA
Nitrate -> NO -> inc cGMP -> activation of myosin LC phosphatase -> Dephosphorylates Myosin-LC -> inc vessel relaxation
-dilates veins more than arteries (dec preload)
89
high dose nitrate
- Dilation of arteries reduces afterload
| - Possibility of reflex tachycardia
90
Nitrate effect of platelets
Stimulates guanylyl cyclase in platelets preventing platelet aggregation
-inc cAMP dec adenosine binding
91
nitrate Contraindications
- Cant be given with Sildenafil (Viagra)
- hypotension
- Increase intracranial pressure or dec cranial blood flow
92
Isosorbide Dinitrate
longer half-life than nitroglycerin (better for chronic angina)
93
nitrates can cause (adverse effect)
headaches
94
DO NOT PRESCRIBE ...... FOR VASOSPASTIC ANGINA
BETA BLOCKERS
95
Ranolazine MOA and use
- blocks LATE Na+ channels leading to a reduction in intracellular Na+, this results in a decrease in action of Na+/Ca2+ exchanger -> dec contractility
- also blocks K+ rectifying channels
- 2nd line angina
96
Dipyridamole MOA and use
inhibits PDE preventing the degradation of cAMP (inc) leading to decrease uptake of adenosine by RBCs and endothelial cells
-antiplatelet during angina
97
what does and doesn't benefit from fibrinolytic in angina
DO NOT: Unstable Angina and NSTEMI
DO: STEMI
98
Treatment of Unstable Angina/MI (Dr. Lee pneumonic)
```
MONA
Oxygen
Aspirin
Nitroglycerin
Morphine
```
99
Systolic
(Heart Failure with Reduced Ejection Fraction)
4 main drugs
```
-ACEi (Captopril, Enalapril, Fosinopril, Lisinopril)
ARB (Losartan,
-Candesartan, Valsartan,
-Beta Blockers
-Aldosterone Antagonist (Spironolactone)
```
100
Diastolic Heart Failure (Heart Failure with Reserved Ejection Fraction) treatment
- No direct therapies
- Try to treat HTN, diabetes, or a. Fib
- Mainly diuretics
101
Beta Blockers use in heart failure and dose
- Reverse heart failure gene programing
| - Start at low dose and increase slowly
102
Spironolactone drug type and MOA
- Aldosterone Antagonist
| - acting primarily through competitive binding of mineralocorticoid receptors in the collecting tubule
103
Spironolactone contraindications
Renal Impairment
Hyperkalemia
Pregnancy
104
Spironolactone Adverse Effects
Gynecomastia
105
Spironolactone Drug Interactions
NSAIDs
Digoxin
ACEi/ARBs can lead to hyperkalemia
106
ARB (Valsartan) + Neprilysin Inhibitor used to treat
Heart Failure with Reduced Ejection Fraction
107
Dobutamine drug type and MOA
B1 agonist
| -positive inotrope that bind B1 receptor increasing Ca2+ sequestration in the SER leading to increase contractility
108
Phosphodiesterase Inhibitor 3
Milrinone
| Enoximone
109
Phosphodiesterase Inhibitor 5
Sildenafil
| Tadalafil
110
Ivabradine MOA
inhibition of the Na+ funny channels leading to prolonged diastole depolarization and dec HR
111
Ivabradine indication
HF with EF <35% with HR >70 bmp and are on max beta blockers or have contraindications to beta blockers
112
inc coumarin toxicity
gemfibrozil
113
don't give for homo
cholestyramine
114
give for hypertriglyceridemia which VLDL predominates
gemfigrozil
