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Pharmacology > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q

Stable Angina

A

Effort/classic

Inadequate blood flow in the presence of CAD

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2
Q

Variant Angina

A

Vasospastic/prinzmetal
Transient spasm of localized portions of these vessels resulting in significant myocardial ischemia and pain
Typically in females at rest

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3
Q

Unstable Angina

A

Acute coronary syndrome
Present when episodes of angina occur at rest when there is an increase in the severity, frequency and duration of chest pain in patients with previously stable angine

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4
Q

Preload

A

Diastolic filling pressure; a function of blood volume and venous tone (controlled by sympathetic outflow)

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5
Q

Afterload

A

determined by arterial blood pressure and large artery stiffness
One of the systolic determinants of oxygen requirement

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6
Q

Classes of Angina

A

I: ordinary activity does not cause angina, only strenuous/prolonged exertion
II: Slight limitation, angina w/ climbing stairs
III: Marked limitation, angina occurs walking 1-2 blocks
IV: angina at rest

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7
Q

Drugs used in Angina

A

Nitrates, Beta-blockers (propranolol, metoprolol), CCBs (verapamil, diltiazem), Ranolazine, Ivabradine

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8
Q

Mechanism of Action of Nitrates

A

Release NO in smooth muscle, activating gunnel cyclase and increasing cGMP leading to relaxation of vascular smooth muscle (vasodilation/^venous return)

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9
Q

Adverse Effects of Nitroglycerin

A

Orthostatic hypotension, tachycardia, headache

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10
Q

Nitroglycerine (general)

A

High first-pass effect, usually given in small doses sublingually
Isosorbides denigrate lasts longer, given orally, mononitrate used for prophylaxis

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11
Q

Transdermal Nitroglycerine

A

Used for prophylaxis of angina
Slow onset, 10-12 hour effects-wear when pain commonly occurs (day vs night)
patch

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12
Q

Beta Blockers

A

Inhibits B1 receptors on heart/kidneys reducing renin release which decreases BP
Also reduced HR, contractility and wall tension
Propranolol/metoprolol used for angina prophylaxis

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13
Q

Propranolol/Metoprolol Mechanism of action

A

Blocks sympathetic effects on heart and BP>decreased myocardial oxygen demand

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14
Q

Propranolol/Metoprolol Adverse Effects

A

Asthma, AV block, acute heart failure, sedation

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15
Q

CCB Mechanism of Action

A

Nonselective block of L-type calcium channels in vessels/heart reducing vascular resistance, HR and decreased oxygen demand
Used for angina prophylaxis

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16
Q

Verapamil/Diltiazem Adverse Effects

A

(CCB)

AV block, acute heart failure, constipation, edema

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17
Q

Nifedipine/Amlodipine Mechanism of Action

A

Block vascular L-type calcium channels>cardiac channels reducing VR, HR and oxygen demand
Dihydropyridines
Prophylaxis of angina

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18
Q

Nifedipine/Amlodipine Adverse Effects

A

Excessive hypotension, baroreceptor reflex tachycardia

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19
Q

Sodium Channel Blockers (Mech of Action)

A

Ranolazine
Blocks CCB minimally, but doesn’t impact HR, BP
Reduces ischemic episodes by selective inhibition of late sodium current>influx of Ca>intracellular Ca overload/myocardial stunning
Reduces Cardiac oxygen demand
Used for STABLE angina

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20
Q

Ranolazine Adverse Effects

A

QT intervalprolongation
nausea, constipation, dizziness
Increased concentration/duration by CYP3A inhibitors

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21
Q

General Mechanisms of Antiarrhythmic Drugs

A

Alter cardiac rhythm by altering the maximum diastolic potential, rate of phase 4 depolarization, threshold potential and action potential duration

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22
Q

Class 1 Actions/Prototypes

A

Sodium channel blockers

Procainamide, lidocaine, flecanide

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23
Q

Class 2 Actions/Prototypes

A

Beta adrenergic receptor antagonist

Propranolol

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24
Q

Class 3 Actions/Prototypes

A

Potassium channel blockers

Amiodarone or Dofetilide

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25
Q

Class 4 Actions/Prototypes

A

Ca channel blockers

Verapamil

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26
Q

Class 1A

A

Proainamide (disopyramide)
Slows conduction velocity and pacemaker rate, used for atrial and ventricular arrhythmias
Oral, IV, IM

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27
Q

Class 1A MOA and Adverse Effects

A

Na (primary) and Kr (secondary) blockade

AEs: Torsades de pointes with renal failure, HTN, lupus related symptoms

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28
Q

Class 1B

A

Lidocaine (Mexiletine)
Used for ventricular arrhythmias post MI
IV or IM

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29
Q

Class 1B MOA and Adverse Effects

A

Highly selective Na block, minimal effect in normal tissue

AEs: neurologic symptoms (CNS sedation or excitation)
Reduce dose in pts with heart failure or liver disease

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30
Q

Class 1C

A

Flecanide
Dissociates from channel with slow kinetics, no change in action potential duration
Oral

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31
Q

Class 1C MOA and Adverse Effects

A

Sodium channel blockade

AEs: proarrhythmic

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32
Q

Class 2

A

Propanolol (metoprolol)
Used fo atrial arrhythmias and prevention of MI/sudden death
Oral or parenteral

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33
Q

Class 2 MOA and Adverse Effects

A

B-Adrenoceptor blockade; prolongation of action potential duration, slows SA node automaticity and AV node conduction velocity

AEs: asthma, AV blockade, acute heart failure

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34
Q

Class 3

A

Amiodarone
Used for serious ventricular/supraventricular arrhythmias
Most commonly prescribed AAD
Oral or IV, log half life (weeks-months in system)

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35
Q

Class 3 MOA and Adverse Effects

A

Blocks Na, Ca, K channels and B adrenoceptors; prolongs action potential and QT interval (slows HR/AV node conduction)

AEs: pulmonary fibrosis, hyper/hypothyroidism
Lots of interactions

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36
Q

Class 3 Subclass

A

Dofetilide

maintenance or restoration of sinus rhythm in A-fib

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37
Q

Dofetilide MOA and Adverse Effects

A

K block to prolong action potential

AE: Torsades de Pointes-VERY RARELY USED

38
Q

Class 4

A

Verapamil or Diltiazem
Used for AV nodal arrhythmias (esp prophylaxis) or rate control in A-fib
Oral or parenteral

39
Q

Class 4 MOA and Adverse Effects

A

Dependent Ca block slows conduction in AV node/Pacemaker activity-PR interval prolongation

AEs: constipation, hypotension

40
Q

Miscellaneous AADs

A

Magnesium, Potassium, Adenosine

41
Q

Magnesium MOA/AE/Application

A 
Interacts with Na/K/ATPase, K and Ca channels to normalize plasma Mg
Used in torsades de pointes
AE: muscle weakness
IV only
Counter to Calcium ion
42
Q

Potassium MOA/AE/Application

A

Increases K permeability and currents to slow pacemakers/conduction velocity
Used in arrhythmias associated with hypokalemia
AEs: reentrant arrhythmias, fibrillation or arrest
Oral or IV

43
Q

Adenosine MOA/AE/Application

A

Activates inward rectifier K and blocks Ca (complete AV blockade)
Used in paroxysmal supreventrivcular tachycardia (stops heart to repace it)
AE: flushing, chest tightness, dizziness

IV only, lasts 10-15 seconds

44
Q

Heart Failure

A

Inability of heart to pump sufficient blood to meet metabolic needs

45
Q

Systolic Heart Failure

A

Reduced mechanical pumping action (contractility) and reduced EF

46
Q

Diastolic Heart Failure

A

Stiffness and loss of adequate relaxation affecting filling and cardiac output; normal EF

47
Q

Goals of treatment in Heart Failure

A

Improve symptoms and slow or reverse deterioration in myocardial function, reduce mortality

48
Q

Medications used in Heart Failure

A

Diuretics, beta blockers, ACEs, ARBs, Angiotensin receptor-neprilysin inhibitor (ANRi), Vasodilators, digoxin, aldosterone antagonists

49
Q

Diuretics in HF

A

Furosemide (loop) or thiazides (not as powerful, better as antiHTN)
Used in both acute and chronic HF
Oral or IV

50
Q

Furosemide MOA/Doses

A

Decreases reabsorption in thick ascending limb to increase salt/water excretion (reduce preload/afterload)
20-40mg QD or BID to start, can go up to 160

51
Q

Furosemide Adverse Effects

A

Orthostatic hypotension, ototoxicity, hypovolemia, low electrolytes
Sulfa allergy

52
Q

Aldosterone Antagonists in HF (general/doses)

A

Spironolactone (or eplerenone)
Used for CHRONIC HF
Oral, 25-50mg QD but start low

53
Q

Spironolactone MOA and Adverse Effects

A

Blocks cytoplasmic aldosterone receptors in collecting tubules>increased salt/water excretion, reduced remodeling
AEs: hyperkalemia, antiandrogen actions

54
Q

ACE Inhibitors in HF

A

Lisinopril (or enalapril)
Used in chronic HF
Oral, 20-40mg QD

55
Q

Lisinopril MOA and Adverse Effects

A

Inhibits ACE leading to artery/venous dilation, reduces aldosterone secretion

AEs: cough, hyperkalemia, edema

56
Q

ARBs in HF

A

Losartan
Used when ACEs are not tolerated
Oral, 150mg QD

57
Q

Losartan MOA and Adverse Effects

A

Antagonize all effects at AT1 receptors (dilation of vessels)

AEs: hyperkalemia, angioneurotic edema

58
Q

ANRi in HF

A

Sacubitril/valsartan
49/51mg BID to start, then 97/103mg BID
Discontinue ACE 36 hours before initiating

59
Q

Beta Blockers in HF

A

Carvedilol (metoprolol)
Used to slow progression in CHRONIC HF
Oral 25mg BID with food

60
Q

Carvedilol MOA and Adverse Effects

A

Blocks B1 receptors and a1 receptors to slow HR (reduce BP)

AEs: bronchospasm, bradycardia, AV block, acute cardiac decompensation

61
Q

Vasodilators in HF

A 
Isosorbide dinitrate (hydralazine isosorbide dinitrate for blacks), Hydralazine, Nitroprusside
Acute and chronic HF and angina
62
Q

Isosorbide Dinitrate MOA and Adverse Effects

A

Releases NO for venous dilation>reduced preload and ventricular stretch

AEs: postural hypotension, tachycardia, headache

63
Q

Hydralazine

A

Increases NO synthesis reducing BP and afterload, increasing CO
reduced mortality
AEs: lupus like syndrome

64
Q

Nitroprusside

A

Rapid, powerful vasodilation reducing preload and afterload

Used for acute severe decompensated failure

IV only (wrap in foil), lasts a few minutes

AEs: Excessive hypotension, thiocyanate

65
Q

Digoxin in HF (general/doses)

A

Used for chronic symptomatic HF and rapid ventricular rate in Afib
Oral or parenteral, 0.125-0.25mg QD

66
Q

Digoxin MOA and Adverse Effects

A

Na/K/ATPase inhibition>reduced Ca expulsion/increased Ca stored in SR>increased cardiac contractility>slows HR

AEs: nausea, vomiting, diarrhea, cardiac arrhythmia

67
Q

Beta Adrenoceptor Agonists in HF

A

Dopamine and dobutamine
both IV only
Acute decompensated heart failure (shock also for dopamine)

68
Q

Dopamine MOA/AE

A

Dopamine receptor agonist, increases renal blood flow, cardiac force and BP
AE: arrhythmia

69
Q

Dobutamine

A

Beta-selective agonist (increases cAMP)>increased cardiac contractility/cardiac output
AE: arrhythmia

70
Q

Bipyridines in HF

A

Amrinone, Milrinone
Acute decompensated HF
IV only

71
Q

Amrinone MOA/AE

A

Phosphodiesterase type 3 inhibitors>vasodilators lowering PVR/cardiac contractility
AE: arrhythmia

72
Q

Natriuretic Peptides in HF

A

Nesiritide
Acute decompensated HF; does not reduce mortality
IV only

73
Q

Nesiritide MOA/AE

A

Activate BNP receptors, increases cGMP>vasodilation/diuresis

AE: renal damage, hypotension

74
Q

Ivabradine

A

Used in stable heart failure with worsening symptoms with HR at least 70 and taking BB at highest dose (to reduce risk of hospitalization)
2.5-5mg (7.5 max) BID, adjust every 2 weeks until HR 50-60
Monitor HR and rhythm

75
Q

Ivabradine MOA/AE

A

Prolongs diastolic time by inhibiting If current in HCN channel reducing HR
AE: hypotension, sick sinus, dizzy, fatigue, decompensated HF
Avoid with CYPsA4 inhibitors

76
Q

Medications for PAD

A

Aspirin, dipyridamole ER, Cilostazol, Clopidogrel, Pentoxifylline, Vorapaxar

77
Q

Aspirin for PAD

A

MOA: irreversibly inhibits prostaglandin cyclooxyrgenase in platelets
Dose: 81-325mg; Grade 1A w/ coronary/cerebrovascular
Side effects: GI upset/bleeding
Don’t use with active bleeding, hemophilia, thrombocytopenia

78
Q

Dipyridamole ER

A

MOA: inhibits activity of adenosine and PDE>accumulation of cAMP>platelet inhibition/vasodilation
Dose: 400mg (+50. aspirin)
Side Effects: angina, dyspnea, hypotension, headache, dizziness
Don’t use with active bleeding/CAD
Recommendation not specified

79
Q

Cilostazol

A

MOA: Phosphodiesterase inhibitor, suppresses platelet aggregation, artery dilator
Dose: 100mg BID
Side effects: Fever/infection, tachycardia
Don’t use with CHF
Grade 2A

80
Q

Clopidogrel

A

MOA: irreversible inhibition of platelets
Dose: 75mg
Side Effects: chest pain, purport, pain, rash
Don’t use with active bleeding
Grade 1C (only over no treatment)

81
Q

Pentoxifylline

A

MOA: Alters RBC flexibility, decreases platelet adhesion, reduces blood viscosity, decreases fibrinogen concentration
Dose: 1.2g
Side Effects: dyspnea, nausea, vomiting, headache, dizziness
Don’t use with recent retinal or cerebral hemorrhage
Not recommended with IC

82
Q

Vorapaxar

A

MOA: PAR-1 antagonist, long half life
Dose: 2.08mg QD with aspirin or clopidogrel
Side effects: >10% bleeding; depression, rash, iron deficiency, retinopathy
MONITOR signs of bleeding, H&H
BOX WARNING: history of stroke, TIA, hemorrhage, etc-last resort treatment

83
Q

Ticlopidine

A

No longer available in US due to side effects (leukopenia, thrombocytopenia, neutropenia, agranulocytosis, aplastic anemia)

84
Q

Goal of Treating Hypertension

A

Reduce associated morbidity and mortality from CV events

Goal is to be below 130/80

85
Q

Mean Arterial Pressure

A

(SBPx1/3)+(DBPx2/3)

Normal: 70-100mmHg, MUST be at least 60 for organ perfusion

86
Q

Blood Pressure Equation

A

BP=HRxSVxTPR

If you change one, the others must change to compensate

87
Q

Dyslipidemia

A

High cholesterol

88
Q

Lipoprotein components

A

VLDL carries most of triglycerides
LDL carries 60-70% of serum cholesterol
HDL

89
Q

Cholesterol Synthesis

A

Manufactured in liver, made from Acetyl CoA, occurs predominantly at night
Rate limiting step: HMG-CoA reductase

90
Q

Statin Recommendations

A

Secondary prevention, 10 year risk of 7.5-10 should receive therapy
If high-intesntiy not tolerated, used moderate intensity+ezitimibe

91
Q

Drugs for Cholesterol

A

Statins-interfere with HMG-CoA/biosynthesis of cholesterol
Ezitimibe-blocks cholesterol absorption
Bile acid resins-increase excretion of cholesterol
Niacin-decrease VLDL/LDL
Vibrates-Decrease TG

Pharmacology (7 decks)

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