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IPC CARDIOLOGY 2 JEN > Heart Failure Medications Pharmacology and PKPD > Flashcards

Heart Failure Medications Pharmacology and PKPD Flashcards

(78 cards)

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1
Q

What are the Morbidity and Mortality Reducing Drugs?

A

RAAS Inhibition, MRAs, SGLT, BBs, Veno/Vasodilators

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2
Q

What are the RAAS Inhibitors?

A

ACEI/ARB, ARNI

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3
Q

Effects of RAAS Inhibitors on HF?

A

Arteriolar and venous dilation
Decreases aldosterone secretion
Reduces cardiac remodeling

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4
Q

Sacubitril increases…

A

BP and natriuresis

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5
Q

What is the indication for Entresto?

A

HFrEF, HFpEF, HFmrEF

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6
Q

MOA Sacubitril?

A

Neprilysin inhibitor that blocks the breakdown of BNP –> naturesis and vasodilation

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7
Q

MOA Valsartan?

A

Blocks AG II receptor (decreases RAAS cascade)

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8
Q

Most common ADR for Entresto?

A

Hyperkalemia

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9
Q

What happens if the 36 hour wash out period is NOT given with an ACEI?

A

Increase in bradykinin and angioedema

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10
Q

The ARNI has ______ BP lowering effects than an ACEI or ARB alone

A

More

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11
Q

Almost all _____ are renally eliminated?

A

ACEI

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12
Q

ACEI and ARBs are used for which type of HFEF?

A

HFrEF

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13
Q

MRAs Effect on HF?

A

Increases salt and water excretion
Reduces cardiac remodeling

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14
Q

Major Contraindication MRA?

A

Severe kidney impairment
eGFR <30mL/min/1.73m^2 or creatinine >2.5 mg/dL in men or creatinine >2 mg/dL in women
Potassium >5.0 mEq/L

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15
Q

Which MRA is a strong CYP3A4 inhibitor?

A

Eplerenone

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16
Q

ADR Spironolactone?

A

Gynecomastia, breast tenderness, impotence

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17
Q

ADR Eplerenone?

A

Increased TGs

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18
Q

ADRs MRAs

A

Dehydration, hyperkalemia, hyperatremia, dizziness

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19
Q

What are the SGLT inhibitors?

A

Empagliflozin, Dapagliflozin, Sotagliflozin

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20
Q

Which is the SGLT2 inhibitors?

A

Empagliflozin, Dapagliflozin

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21
Q

Which is the SGLT1/2 Inhibitor?

A

Sotagliflozin

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22
Q

SGLT Effects in HF

A

-Increased sodium and water excretion
-Decreased cardiac preload and afterload
-Reduces pulmonary and peripheral edema
-Improves metabolism and efficiency of cardiac muscle

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23
Q

MOA SGLT

A

Increases urine output by osmotic diuresis (glucose excretion)
Increased fibrosis
SGLTI Inhibition: decrease absorption of sodium/glucose

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24
Q

Major Contraindications for Dapagliflozin and Sotagliflozin?

A

eGFR > 25 mL/min/1.73m^2 for initiation
DO NOT need to discontinue if eGFR falls below this while on treatment

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25
Major Contraindication for Empagliflozin?
No renal adjustments necessary
26
ADRs for SGLT?
Dehydration, genital mycotic infections/UTI Hypoglycemia, euglycemic acidosis (stop surrounding surgeries)
27
How many days prior to surgery should you stop SGLT inhibitors due to euglycemic ketoacidosis?
3 days prior to surgery
28
Which dose may require an adjustment due to SGLT?
Loop Diuretic
29
What are the Beta-Blockers used that have mortality benefit in patients with HF?
Carvedilol, Metoprolol Succinate, Bisoprolol
30
Beta-Blockers effect in HF?
Reduces HR Decreases sympathetic input to cardiac and vascular tissue Decreases arrhythmias and sudden cardiac death in patients w/ HFrEF mainly due to decrease in sympathetic drive
31
Major contraindication for Beta-Blocker?
Severe bradycardia
32
DDI of Beta-Blockers?
Additive AV nodal blockade with Non-DHP CCB
33
Which are the Vaso/Venodilators associated w HF?
Hydralazine and Isosorbide Dinitrate
34
Effects in HF: Hydralazine
Reduces afterload --> increased cardiac output
35
Major Contraindication Hydralazine?
CAD (causes reflex tachycardia and can cause angina/MI)
36
Effects in HF: Isosorbide Dinitrate
Reduces preload --> decreases ventricular stretch
37
ADR Hydralazine?
Dizziness, REFLEX TACHYCARDIA, DILE
38
Hydralazine half life?
1.5-3 hours
39
Pearls for Hydralazine and combo tablet BiDil?
Need to take 3 times daily, not great for adherence!
40
Major Contraindication for Isosorbide Dinitrate
PDE5
41
ADR Isosorbide Dinitrate
Headaches, dizziness, syncope
42
MOA Isosorbide Dinitrate
Forms the free radical nitric oxide which in smooth muscle activates guanylate cyclase which increases guanosine 3’5’ monophosphate (cGMP) leading to smooth muscle relaxation. Produces a vasodilator effect on the peripheral veins and arteries with more prominent effects on the veins.
43
Key PKPD Isosorbide Dinitrate
Dependent in formulation, oral bioavailability is low bc of first pass hepatic metabolism (10-20%)
44
Loop Diuretics Effect in HF
Increased excretion of salt and water Reduces cardiac preload and afterload Reduces pulmonary and peripheral edema
45
Loop Diuretics key note**
Improves symptoms of HF, fluid overload, SOB, that is when loop diuretics are use completely for symptom control, they do not reduce mortality in patients with HF
46
Major Contraindications Loop Diuretics
Anuria (no urine)
47
DDI Loop Diuretics
Increased risk of ototoxicity if used with aminoglycosides
48
BBW Loop Diuretics (Furosemide)
Potent diuretic at high doses can lead to profound fluid and electrolyte loss
49
Bioavailability of Loop Diuretics
Furosemide is 40-70% The rest are 90 and above
50
Diuretic Resistance: What do you do if there is increased distal sodium reabsorption (chronic loop diuretic use)?
ADD Thiazide to the loop
51
Diuretic Resistance: Poor delivery to site of effect: reduced GFR, HF, gut enema
INCREASED dose of loop diuretic
52
When do you increase the threshold of diuretics?
Chronic use, AKI/CKD, HF (gut edema)
53
What is the ceiling dose for a loop diuretic?
Once you hit a good dose, an increase in dose 80 vs 120 won't do anything different to the patient, so no need to go up.
54
Which two medications require food to ensure adequate absorption?
Ivabradine (Corlanor) Vericiguat (Verquvo) These drugs are also BOTH indicated for HFrEF only
55
MOA of Ivabradine?
Impacts the 'funny' channel in the SA node
56
DDI Ivabradine
Major substrate of CYP3A4
57
Major Contraindications Ivabradine
Severe hepatic impairment, acute decompensated HF, clinically significant hypotension, sick sinus syndrome, sinoatrial block, third degree AV block
58
ADR Ivabradine
Bradycardia, afib
59
MOA Vericiguat
Enhances production of cGMP by directly stimulating sGC independent of NO and enhances sGC sensitivity to endogenous NO, thereby increasing cGMP production. Increased levels of cGMP lead to smooth muscle relaxation and vasodilation
60
Major Contraindication Vericiguat?
Pregnancy
61
ADR Vericiguat?
Hypotension, anemia
62
DDI Vericiguat?
Category X: use in combination with PDE5 inhibitors
63
Pearls Vericiguat?
Formulation may include lactose Must have a negative pregnancy test prior to initiation
64
Which drug is the Cardiac Glycoside?
Digoxin
65
Digoxin effects in HF?
Increases cardiac contractility Increases parasympathetic tone of heart (decreases sinus rate, AV conduction)
66
Digoxin indication?
HFrEF, rate control for afib
67
MOA Digoxin
Inhibition of the sodium/potassium ATPase pump in myocardial cells results in a transient increase of intracellular sodium, which in turn promotes calcium influx via the sodium- calcium exchange pump leading to increased contractility. May improve baroreflex sensitivity.
68
ADR Digoxin?
Arrhythmia, heart block, GI and neurological side effects
69
DDI Digoxin
Major substrate of PgP, minor substrate of CYP3A4
70
Monitoring for Digoxin?
Heart rate and rhythm
71
Monitoring for Digoxin...what is the serum concentration trough goal?
Ideally 0.5-0.9 ng/mL
72
ADR Digoxin?
Tachycardia, bradycardia, anorexia, nausea, vomiting
73
Distribution of Digoxin?
HIGH volume of distribution: once absorbed, it is widely distributed into the tissues, takes 6-8 hours for that
73
Pearls Digoxin?
Almost exclusively used for patients with HFrEF and afib BEERS criteria (not ideal for older patients)
74
Heart:Serum Concentration Digoxin?
70:1
75
Excretion of Digoxin?
2/3 excreted unchanged by the kidneys , renal clearance is proportional to creatinine clearance, half life is 36-40 hours in normal renal function (worse in patients w bad renal function)
76
Digoxin Levels
Toxic effects may occur BEFORE therapeutic effects are detected Levels must be drawn after distribution period, ideally at least 10-12 hours, levels should be drawn at steady state: 5-7 days after initiation
77
What are the morbidity drugs?
Diuretics, If Channel Inhibitor, Soluble Cyclase Stimulator, Cardiac Glycoside

IPC CARDIOLOGY 2 JEN (6 decks)

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