Dr. Laila M. Matalqah Ph.D. Pharmacology PHARMACOLOGY OF CNS part 1 General Pharmacology M212.
PHARMACOLOGY OF HEART FAILURE By Rutendo Ganyani and Sarah Folkerts.
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Transcript of PHARMACOLOGY OF HEART FAILURE By Rutendo Ganyani and Sarah Folkerts.
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PHARMACOLOGY OF HEART FAILURE
By Rutendo Ganyani and Sarah Folkerts
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What are the signs & symptoms of heart failure?
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Signs and Symptoms of heart failureSymptoms:
- Dyspnoea- Orthopnoea- Paroxysmal nocturnal
dyspnoea- Fatigue- Cough (pink, frothy
sputum)- Nocturia
Signs:
- Resting tachycardia- JVP elevation- Lung crackles- Wheezing- 3rd heart sound- Peripheral oedema- Ascites
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What are the NICE guidelines for treatment of LV heart failure?
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NICE Guidelines
Diuretic for symptom relief…..thenACEi + Beta blockers
Consider adding an Aldosterone antagonist or an ARB or hydralazine + nitrate
Consider ARB if patient can’t tolerate ACEi
Consider hydralazine + nitrate if patient can’t tolerate ACEi and ARBs
Digoxin
Implantable devices
TransplantationWhen other heart pathologies or risk factors are present, consider treatment for these. e.g. aspirin, Ca-channel blockers
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◦Describe the mechanism of action of ACE inhibitors!
◦ Side effects?
◦ Example?
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ACEi pharmacology
◦ stop the conversion of angiotensin I to angiotensin II thus stopping all the downstream effects. (vasodilation)
◦ Side effects:◦ Dry cough ◦ Hyperkalaemia◦ Other side effects include:
◦ Teratogenic
◦ Hypotension
◦ Renal impairment (do not use w/ renal artery stenosis!)
◦ Examples: • Ramipril
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◦Describe the mechanism of action of ARBs!
◦ Side effects?
◦ Example?
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Angiotensin receptor blocker (ARB) pharmacology
◦ Inhibit action of Angiotensin II
• Reduce vascular resistance
• Restore tissue perfusion
• Reduce afterload
• Reduce aldosterone production
→Reduced sodium reabsorption
→Water loss
Side effects:
Hypotension
Renal impairment
Hyperkalaemia
Examples: Losartan
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Control of renin release and formation and action of angiotensin II (RAAS system)
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◦Describe the mechanism of action of beta blockers!
◦ Side effects?
◦ Example?
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Beta blocker pharmacology◦ block beta-1 adrenergic receptors (Gs coupled receptors which cause
an increase in cAMP -> increase in PK-A -> increase of intracellular Ca in cardiac myocytes) in the heart.
◦ Reduced heart rate
◦ Decrease cardiac contractility
◦ Reduce arterial pressure
◦ Attenuate ventricular remodelling: fibrosis, apoptosis and arrythmogenesis
Side effects:
- Bronchoconstriction
- Cardiac depression
- Bradycardia
- Hypoglycaemia
- Fatigue
- Cold extremities
- Examples: Bisoprolol, metoprolol
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◦Describe the mechanism of action of Aldosterone antagonists!
◦ Side effects?
◦ Example?
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Aldosterone receptor blocker pharmacology
◦ Blocks action of aldosterone at DCT (block mineralocorticoid receptors)
→ Reduced expression of ENac
→ Reduced Na+ reabsorption
→ Increased water excretion
• K+-sparing
◦ Side effects:
◦ Hyperkalaemia, ◦ Hypotension
Mainly w/ spironolactone◦ Gynaecomastia, ◦ Impotence
◦ Examples: Eplerenone, spironolactone
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◦Describe the mechanism of action of Nitrates!
◦ Side effects?
◦ Example?
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Pharmacology of nitrates
• Metabolised to NO activate guanylate cyclase increase in cGMP activates protein kinase G vascular relaxation
• Side effect– Headache (due to dilatation of intracranial
arteries)– Postural hypotension– Dizziness
• Also problem with quickly developing tolerance that can lead to abnormal constriction of coronary arteries following withdrawal
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………….and the others◦Digoxin (in particular for heart failure w/
established atrial fibrillation or if symptomatic despite diuretics and ACEi) -> increases inotropy (=pos. inotrope)
◦Hydralazine - Unknown mechanism of action, however it dilates arteries & arterioles -> reducing the afterload. (= vasodilator)• Side effects:
• Tachycardia
• Headache
◦We will not be looking at transplantation or implantable devices….. Don’t worry about this at this stage. Just know the options exist.
Digoxin
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Summary of site of action of different drugs used to treat heart failure
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Any Questions?