Anti cardiac failure agents

Question 1

Pharmacological effect

Answer 1

A. Stimulation of cardiac performance
A1 reduction in end systolic volume: increasing myocardial contractility
A2 increase in diastolic end volume (increase in preload):
1) prolongation of ventricular filling -
«-» chronotropy (diastole extension)
2) increasing (restoring) the volume (volume) of circulating fluid

B. Reduction of heart load if necessary:
B1 «-» chronotropy
B2 afterload reduction: arteriodilatation
B3 reducing preload
1) venodilation
2) reducing the amount (volume) of circulating fluid

C. Delaying of remodeling and fibrosis

Question 2

RAAS activity reducing agents

Answer 2

ACE-I &ARB

Principles of action- B2, B3.1, C
Antifibrotic, remodelation inhibitory activity
 CHF

Question 3

Diuretic agents

Answer 3

Principles of action- B3.2
Decrease of diastolic end pressure ,decreases heart load,enhancement of cardiac systolic activity

Loop, thiazide and thiazide like diuretics are potassium excreting.

=>AHF,CHF

Question 4

MRA

Answer 4

Principles of action- B3.2 & C
The underlying effect is not due to an increase in diuresis, but rather with the beneficial effects of aldosterone blockade on * myocardial fibrosis
inhibition and improved vasodilatory function in b/v

Potassium sparing.

**Spironolactone nonselective MRA
Eplerenone selective MRA

1. Mild diuretic effect
2. Antifibrotic effect
3. Antiandrogen effect (S only)

=> CHF

SE: hyperkalaemia, **gynecomastia (antiandrogenous activity)

Question 5

BAB

Answer 5

2. BABgeneration

Metoprolol, Bisoprolol
Principles of actionA2.1, B1, C

3. BAB generation

Nebivolol, Carvedilol
Principles of actionA2.1, B1, B2, B3.1, C

Short- and medium-term remodeling inhibitory effects

Question 6

Ivabradine- Sinus node inhibitor

Answer 6

Principles of action - A2.1, B1

Due to Frank-Stalling’s law cardiac performance will be increased
with condition that the patient is not hypervolemic
There is no characteristic «-» inotropic effec

Question 7

Neprilysin inhibitor

Answer 7

Neprilysin inhibits NP and AT 2, Bradykinin which is responsible for (vasodilation, diuresis, sodium excretion, antifibrosis)

Pre-drug / active form
Sacubitril / Sacubitrilate
Neprilysin inhibition
Principles of action–
B2, B3.1, B3.2., C

=>CHF with reduced ejection
fraction

Muat be combined with ARB to prevent increase in concentration of AT2

Question 8

Cardiac glycosides

Answer 8

Digoxin

Operating principles - A1, A2.1, B1
Na and K channel inhibition->increase in intracellular Ca concentration-> cardiotonic activity

„+” inotropic effect, because myocardial cells have increased Ca2 +
concentration – cardiotonic activity
«- » chronotropic effect - n.vagus parasympathomimetic effect

 AHF
 CHF

SE: cardiac - overdose ~70% cases rhythm disorders !!!,
extrasystoles, atrial tachycardia, bradycardia, AV block
Extracardiac SE - nausea, diarrhea, visual disturbances
Caution in use!
Risk of material cumulation

Question 9

Dobutamine

Answer 9

Beta 1 adrenoreceptor agonist. Priniciple of action A1

„+” inotropic effect with increased Ca2 + concentration in myocardial cells –cardiotonic activity
Mild „+” chronotropic effect

Has mild beta 2 and alpha 1 adrenomimetic effects - reduces peripheral vascular resistance (after load), but
systolic pressure remains unchanged or increases (increases CO)

Question 10

Dopamine

Answer 10

Dopamine 1 receptor, beta 1, alpha 1 adrenoceptor agonist. Priniciple of action A1.
The effect is dose-dependent: at low doses - improves renal microcirculation (GFR), at medium doses - induces a “+” inotropic effect - cardiotonic effect,
in high doses - predominantly vasopressor effect

Question 11

Calcium channel sensitizers

Answer 11

Levosimendan
Principles of action- A1, B2, B3.1
Binding to troponin C in cardiomyocytesincreases myofibrillar sensitivity against Ca 2+

Triple action:

1. «+» inotropy (without oxygen) Consumption increase
2. Vasodilation
3. Cardioprotection

Question 12

NO Donors

Answer 12

Principle of action- B3.1

GTN
Sodium nitroprusside

Vasodilatory activity

Question 13

Morphine

Answer 13

Opioid receptor agonists
Reduces tachypnoea
Use in AHF with pulmonary edema