W3, 9 HF Treatment (pharma) Flashcards
What is Heart failure (HF) or (CHF)?
Itβs abserious condition in which the heart is not pumping enough blood around the body efficiently
A complication of HF?
When the heart is weakened by heart failure, blood and fluid can back up into the lungs, and fluid builds up in different tissues.
Cardiovascular Consequences of Heart Failure (slide)
Objectives in treatment of CHF
- To reduce congestion (oedema)
- To improve cardiac contractility
Classes of Drugs Used in Treatment of CHF (slide)
Pharmacologically active compounds extracted from foxglove plants (also called Digitalis) are ..?
Cardiac glycosides
What drug is the prototype cardiac glycoside?
Digoxin
Digoxin route of administration & excretion?
Mechanism of action of digoxin?
Adverse Reactions to Digitalis Glycosides
What drug is Beta-1 Adrenoceptor Agonists ?
Dobutamine
moa of Dobutamine
Activate cardiac beta-1 receptors β> inc cAMP β> elevated intracellular Ca2+ β> positive inotropic effect β> inc CO
What drug is Phosphodiesterase (PDE) inhibitor?
Amrinone
Moa of Amrinone
Diuretics (examples of drugs + MOA)
What drug Relaxes vascular smooth muscle by supplying nitric oxide? Name the drug class or category & drug name.
Direct Vasodilators & Venodilators (Nitrovasodilators) eg: Hydralazine
-
- Reduce preload by producing venodilation (reduce VR)
- Reduce afterload by arteriolar dilation (decrease PVR)
HF leads to (activation or inhibition) of the renin-angiotensin- aldosterone system?
Activation
Renin release due to β¦.?
increased sympathetic stimulation
and activation of beta-1 receptors in the kidneys
What is ACE enzyme
High levels of Ang II have detrimental effects on the cardiac muscle
Ψ΄ΩΩ Ψ§ΩΩ
Ψ
High levels of Ang II have detrimental effects on the cardiac muscle, causing remodeling, fibrosis and inflammatory changes.
What drug is Angiotensin-Converting Enzyme Inhibitor?
Captopril
MOA of Captopril?
ACEIs prevent the conversion of Angiotensin I to Angiotensin II.
Adverse effects to ACEIs?
Postural hypotension, hyperkalemia
persistent dry cough (Due to accumulation of bradykinin)
Effects of ACEI (slide)
Angiotensin II Receptor Blockers (ARBs)
A. 2 Drug examples?
B. MOA
A. Losartan, valsartan
B. Antagonists at Angiotensin II type 1 receptor (block effect of ang II obtained from ACE- dependent and - independent pathways
ARBs > ACEI or ACEI > ARBs and why?
- ARBs have the advantage of more complete blockade of Angiotensin II action, because ACEIs inhibit only one enzyme β
responsible for production of Angiotensin II. - ARBs do not affect bradykinin levels.
Route of administration of Losartan
- ARBs are orally active compounds
- Losartan undergoes extensive first-pass hepatic metabolism.
Beta Blockers MOA (slide)
Types of beta blockers
A.
B.
- Beta-1 selective adrenoceptor antagonists (e.g. Metoprolol, Atenolol)
- Combined Alpha-1 and Beta Blockers (e.g. Carvedilol).
What is Metoprolol?
Beta 1 antagonist that reduces the mortality of patients with heart failure
What drugs are Aldosterone Receptor Antagonists ?
Eplerenone, Spironolactone
A non- selective aldosterone receptor antagonist.
Spironolactone
Selectively binds to the mineralocorticoid receptor, blocking
the binding of aldosterone, inhibiting sodium reabsorption.
Eplerenone
MOA of Spironolactone?
- Reduces Na+ reabsorption
- Prevents salt retention, myocardial hypertrophy and hypokalemia.
Which aldosterone receptor antagonist has Less hormonal side effects?
Eplerenone
Adverse effects of Eplerenone include
hyperkalemia
How do Angiotensin Receptor-Neprilysin Inhibitors (ARNIs) act?
consists of angiotensin receptor blocker valsartan and neprilysin inhibitor (blocks both RAAS & augment natriuretic peptides)
-drug name =n LCZ696 ,, not on drug list -
What drug is Currently indicated in USA for treatment of hypertension, and
for first-line treatment of heart failure secondary to
myocardial infarction?
Eplerenone
What drugs Decrease and block the effect of some symptoms caused by release of catecholamines?
Beta blockers
Contraindicated in pregnancy.
ARBs & ACEI
Can cause hyperkalemia, gynecomastia & testicular atrophy.
Spironolactone
Long term therapy with this drug can benefit patients who had a recent myocardial infarction (protects heart)
ACEIs
toxicity of this drug can be worsened by hypokalemia
Digoxin
What drug Activate cardiac beta-1 receptors ?
Dobutamine
Mcq: What should be monitored when administering digoxin?
A. Potassium
B. Calcium
C. Sodium
D. Chloride
A. Potassium
Mcq: What drug should be carefully monitored as it has a narrow therapeutic index?
Digoxin
Mcq: What is the mechanism of action of amrinone?
Phosphodiesterase inhibitor
Mcq: Which of the following is a selective angiotensin II antagonist?
Losartan
Mcq: Which drug has less hormonal effects because itβs band specifically to aldosterone receptor?
A. Eplerenone
B. Spironolactone
A. Eplerenone
Mcq: What is the mechanism of action of digoxin?
A. increase intracellular calcium
mcq: which drug causes dry cough?
A. Captopril (ACEI)
Mcq: Which of the following inhibits Na/K ATPase and is used for the management of congestive heart failure?
A. Hydralazine
B. Digoxin
B. Digoxin
Mcq: Indicated to prevent the deterioration of the left ventricular function after myocardial infraction
A. Angiotensin converting enzyme inhibitor
B. Nitrate
C. Secondary prevention
A. Angiotensin converting enzyme inhibitor
Mcq: Selectively binds to mineralocorticoid receptors
A. Eplerenone
Mcq: which one describe the mechanism of dobutamine?
A. activation of aldosterone receptor
B. inhibition of ACE
C. activation of B1 receptor
D. release of nitric oxide
C. activation of B1 receptor
Mcq: What is the effect of co-administering digoxin and thiazide diuretics?
A. Increases the toxicity of digoxin
B. Reduces the absorption of digoxin
C. Reduce vagal activity of digoxin
A. Increases the toxicity of digoxin
Mcq: A patient has a cardiovascular disease and he is being treated for it, after a while he Develops bilateral angioedema. Which of the following drugs is likely to cause this presentation?
A. Diuretics
B. Digoxin
C. Angiotensin converting enzyme inhibitors
D. Hydralazine Answer: C
ACEI
Mcq: A patient with heart failure you gave him a drug & he comes to you with irritated throat and cough
A. ACEI
B. BB
C. Diuretic
D. Digoxin
A. ACEI
Mcq: Which of the following is true regarding RAAS in HF?
A. Using angiotensin 2 receptor blocker decreases aldosterone
B. Aldosterone causes diuresis
C. It must be blocked in HF with reduced EF
C. It must be blocked in HF with reduced EF
Mcq: Patient being treated for HF comes with enlarged swollen breast, what is the cause of this side effect?
A. Digoxin
B. ARB
C. Aldosterone blocker
D. BB
C. Aldosterone blocker
Drug List for Treatment of CHF
