Wolff Heart Failure Drugs Flashcards
What class does Captopril fall under, what does it do, and what are its clinical applications?
- ACEI (“pril”)
- prevents angiotensin I converting to angiotensin II therefore:
- lowers AT II levels
- increases renin plasma levels
- Decreases aldosterone secretion
- Lowers BP overall
- Used for Htn, HFrEF, and diabetic neuropathy
What are the toxicities of Captopril?
- Cough is #1 reason people stop taking ACEI’s
- Angioedema (fatal stop immediately)
- Fetal toxicity (black box warning)
What class does Losartan fall under, what does it do, and what are it’s applications?
- ARB (“sartan”)
- its a non peptide angiotensin II receptor antagonist
- Leads to more complete inhibition of the RAS than ACEI’s
- doesn’t potentiate bradykinin
- Used in:
- Diabetic nephropathy
- Htn
- HF
Losartan has a higher selectivity for ___ than ___ receptor.
Losartan has a higher selectivity for AT1** than **AT2 receptor.
Toxicities of Losartan?
- Fetal toxicity
- Angioedema (?)
- AE’s are more common in those with diabetic nephropathy
What is “noteworthy” about Valsartan?
It is not a prodrug meaning that it doesn’t required activation by the liver and it is excreted in feces relatively un changed
ACEI and ARB should be administered to who? (ACEI are slightly preferred to ARB’s)
- all patients with LV systolic failure o LV dysfunction without HF unless:
- not tolerated (try ARB)
- Pregnant
- Hypotensive
- Serum creatinine >3
- Hyperkalemia
What are the renal/adrenal effects of ANP?
- Increased GFR
- Decreased renin and aldosterone secretion
- decrease Na and water reabsorption in collecting duct
- Decrease ADH secretion and it’s effects in collecting duct
What is the MOA of Valsartan/Sacubitril?
- Sacubitril is prodrug that inhibits Neprilysin
- Valsartan is ARB that is not a prodrug
What are the effects and indications for Valsartan/Sacubitril?
- Neutral endopeptidase blockage leads to increasesd levels of ANP & BNP
- Valsartan antagonizes AT1 receptors
- Used for Heart failure
Common AE’s of Valsartan/Sacubitril?
- Hypotension
- Hyperkalemia
- Increased serum creatine
Angioedema is not common, but is serious
What classes of drugs/drugs are used to prevent deterioration of cardiac function?
- ACEI/ARB
- Beta adrenergic blockers
- Spironolactone/Eplenerone
Heart failure ___ sympathetic activity which will result in, ____ HR, ____ contractility, and__vascular resistance.
Heart failure increases** sympathetic activity which will result in, **increased HR, increased** contractility, and_increased_** vascular resistance.
What are the three Beta Blockers that are used for heart failure?
- Metoprolol
- Bisoprolol
- Carvedilol
How is Carvedilol different than Metoprolol and bisoprolol for patients with HF?
- Inverse agonist at B2 receptors which are present in the heart
- “biased” ligand that causes phosphorylation of cytoplasmic tail of receptor or interaction with B-arrestin and downstream signaling occurs
What is Carvedilol’s MOA?
- nonselective beta and alpha adrenergic blocker
- blocks Beta more than alpha
Carvedilol clinical uses?
- Given if stable to prevent symptomatic HF
- Given if there is a recent or remote hx of MI or ACS and reduced ejection fraction
What is Labetalol used for?
Severe htn or treatment of hypertensive emergencies
What two types of drugs should be given to all patients (unless contraindicated) with left ventricular systolic dysfunction caused by MI to reduce their mortality?
- Carvedilol/Metoprolol/Bisoprolol (1 of these beta blockers)
- ACEI
Beta blockers should be given to all patients with symptomatic CHRF and LVEF <40% except in the case of…?
- Bronchospastic disease
- Symptomatic bradycardia or heart block
What are the contraindications to Beta blockers?
- Hypersensitivity to Carvedilol
- decompensated cardiac failure
- Bronchospastic disorders/asthma
- Cardiogenic shock
- Hepatic impairment
What are patients cautioned against abrupt withdrawal of Beta blockers?
- If the drug is abruptly stopped rather than gradually, patients with CAD run the risk of acute tachycardia, htn, or ischemia
What other diseases are exacerbated by Beta blockers?
- Vasospastic angina
- Bronchospastic disease
- DM
- HF
- Hepatic impairment
- Myasthenia gravis
- PAD
- Pheochromocytoma
- Psoriasis
- Thyorid disease
What is the MOA and effects of Ivabradine?
- Specific inhibition of hyperpolarization activated cyclic nucleotide gated channels within SA node
- Its effects are disrupting the funny Na current to prolong diastole and slow HR down
What is Ivabradine used for?
- Treatment of resting HR over 70 bpm in patients who are stable but have symptomatic LVHF <35% and cannot tolerate more beta blockers
What are the Contraindications of Ivabradine?
- Acute decompensated HF
- Hypotension
- Sick sinus syndrome/AV block
- Pacemaker
- Severe hepatic issues
- Strong CYP3A4 inhibitor use
what is the MOA of Spironolactone?
- Competitive antagonist of aldosterone receptors
Effects and uses of Spironolactone?
- K sparing diuretic
- Antagonizes profibrotic effect of aldosterone
- Used to:
- Counteract K loss induced by other Diuretics
- Reduce fibrosis in HFrEF and post MI heart failure