What are ACEIs ?
What are ACEIs ?
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ACE inhibitors (short for Angiotensin-Converting Enzyme Inhibitors) are a class of medications primarily used to:
_Lower high blood pressure (hypertension)
_Treat heart failure
_Prevent strokes and heart attacks
_Protect the kidneys (especially in patients with diabetes)
History
History
1.Discovery of ACE
1.Discovery of ACE
In 1956, Leonard T. Skeggs and colleagues identified the angiotensin-converting enzyme (ACE) in human plasma.
ACE plays a key role in converting angiotensin I to angiotensin II, a powerful vasoconstrictor that raises blood pressure.
In 1956, Leonard T. Skeggs and colleagues identified the angiotensin-converting enzyme (ACE) in human plasma.
ACE plays a key role in converting angiotensin I to angiotensin II, a powerful vasoconstrictor that raises blood pressure.
2. Snake Venom ConnectionIn the 1960s, Brazilian scientist Sérgio Ferreira discovered a bradykinin-potentiating factor (BPF) in the venom of the Bothrops jararaca snake.
This peptide inhibited ACE, which led to vasodilation and lowered blood pressure.
3. Development of CaptoprilIn the 1970s, Miguel Ondetti and David Cushman at the Squibb Institute synthesized captopril, the first orally active ACE inhibitor.
Captopril was approved by the FDA in 1981.
It was highly effective, but some patients experienced side effects due to its sulfhydryl group.
4. Next-Generation ACE Inhibitors Other ACE inhibitors like enalapril and lisinopril were developed to reduce side effects while maintaining efficacy.
These drugs do not have a sulfhydryl group and are better tolerated.
Mechanism of action
Mechanism of action
Angiotensin-converting enzyme (ACE) inhibitors are medications that help relax blood vessels and lower blood pressure. They achieve this by interfering with the body's renin-angiotensin-aldosterone system (RAAS), which plays a crucial role in regulating blood pressure.
1. Inhibition of Angiotensin II Formation
1. Inhibition of Angiotensin II Formation
_Normal Function: ACE converts angiotensin I (an inactive peptide) into angiotensin II, a potent vasoconstrictor that narrows blood vessels, increasing blood pressure.
_ACE Inhibitors' Role: By blocking ACE, these drugs reduce the production of angiotensin II, leading to vasodilation (widening of blood vessels) and, consequently, lower blood pressure.
2. Reduction of Aldosterone Secretion
2. Reduction of Aldosterone Secretion
_Angiotensin II stimulates the release of aldosterone, a hormone that promotes sodium and water retention, increasing blood volume and pressure.
_With decreased angiotensin II levels, aldosterone secretion diminishes, leading to increased excretion of sodium and water, further reducing blood pressure.
3. Increase in Bradykinin Levels
_ACE also breaks down bradykinin, a peptide that promotes vasodilation.
_Inhibiting ACE leads to higher bradykinin levels, enhancing vasodilation and contributing to the blood pressure-lowering effect.
_However, elevated bradykinin can also cause side effects like a persistent dry cough and, rarely, angioedema.
Example of medication
Example of medication
Enaladex 5mg
Enaladex 5mg
Enalapril maleate
Adwipril
Adwipril
Perindopril
Gopten 0.5mg
Gopten 0.5mg
Trandolapril
Amlodipine/
Amlodipine/
Benazepril
Benazepril
Amlodipine Besylate and Benazepril Hydrochloride 10mg/20mg
Monopril
Monopril
fosinopril sodyum
Minotensol
Minotensol
Meoxipril hydrochloride 7.5mg
Tritace 2.5mg
Tritace 2.5mg
Ramipril
Quinapril
Quinapril
Accupril
lisinoprl 20mg
lisinoprl 20mg
Angiotensin 20
Angiopress Comp
Angiopress Comp
captopril 50mg + hydrochlorothiazide 25mg
Indications
Indications
1. Hypertension (High Blood Pressure)
1. Hypertension (High Blood Pressure)
ACE inhibitors relax blood vessels, making it easier for the heart to pump and reducing blood pressure.
Often used as first-line treatment, especially in younger patients or those with diabetes.
2. Heart Failure
2. Heart Failure
Helps reduce strain on the heart by lowering afterload and preload.
Improves symptoms, reduces hospitalizations, and prolongs survival.
3. Post-Myocardial Infarction (Heart Attack)
3. Post-Myocardial Infarction (Heart Attack)
ACE inhibitors reduce mortality after a heart attack, especially in patients with left ventricular dysfunction or heart failure.
4. Chronic Kidney Disease (CKD)
4. Chronic Kidney Disease (CKD)
Particularly useful in diabetic nephropathy.
Slows the progression of kidney disease by reducing intraglomerular pressure and proteinuria.
5. Diabetes (With or Without Hypertension)
Used to protect the kidneys even in normotensive diabetic patients with microalbuminuria.
6. Left Ventricular Dysfunction (Asymptomatic)
Prescribed even if patients don’t have symptoms yet, to prevent progression to heart failure.
Side effect
Side effect
"While ACE inhibitors are highly effective in managing hypertension and protecting renal function, their use may be limited by notable side effects — the most characteristic being a persistent dry cough and the most dangerous being life-threatening angioedema."
"While ACE inhibitors are highly effective in managing hypertension and protecting renal function, their use may be limited by notable side effects — the most characteristic being a persistent dry cough and the most dangerous being life-threatening angioedema."
Common Side
Common Side
Dry, Persistent Cough
_Occurs in approximately 10% of patients.
_Caused by increased levels of bradykinin.
_May resolve upon discontinuation of the medication.Dizziness or Lightheadedness
_Especially noticeable when standing up quickly.
_Due to lowered blood pressure.Elevated Blood Potassium Levels (Hyperkalemia)
_Can lead to muscle weakness or heart rhythm disturbances.
_Regular monitoring is essential.Fatigue and Headache
General feelings of tiredness or headaches may occur.
Serious Side Effects
Serious Side Effects
Angioedema
-Swelling of the face, lips, tongue, or throat.
_Can be life-threatening; requires immediate medical attention.Kidney Function Impairment
_May cause a decline in kidney function.
_Monitoring of kidney parameters is recommended.Skin Rashes
_Includes various types of rashes, such as urticaria or photosensitivity reactions.
_More common with certain ACE inhibitors like captopril.
Precautions & Contraindications
Precautions & Contraindications
“While ACE inhibitors are widely prescribed and highly effective, they require careful consideration of specific precautions and contraindications"
“While ACE inhibitors are widely prescribed and highly effective, they require careful consideration of specific precautions and contraindications"
⚠️ Precautions When Using ACE Inhibitors
⚠️ Precautions When Using ACE Inhibitors
These are important warnings or conditions where extra monitoring is needed:
1. Monitor Renal Function
1. Monitor Renal Function
🧪 Check creatinine and GFR before and during therapy.
Especially in:Chronic kidney disease (CKD)
Elderly patients
Patients on diuretics or NSAIDs
2. Monitor Serum Potassium
2. Monitor Serum Potassium
Risk of hyperkalemia increases in:
Diabetic patients
Patients taking potassium supplements or potassium-sparing diuretics (e.g., spironolactone)
3. Risk of Hypotension
3. Risk of Hypotension
Especially after the first dose in:
Volume-depleted patients (e.g., on diuretics)
Heart failure patients
4. Cough
4. Cough
Persistent dry cough is common; not harmful but may require switching to an ARB.
🚫 Contraindications of ACE Inhibitors
🚫 Contraindications of ACE Inhibitors
These are conditions where ACE inhibitors must be avoided:
1. Pregnancy
1. Pregnancy
❌ Contraindicated in all trimesters
Causes fetal toxicity, renal failure, oligohydramnios, and death
Women of childbearing age should use contraception.
2. History of Angioedema
2. History of Angioedema
Especially ACE inhibitor–induced angioedema or hereditary angioedema
Risk of recurrence and airway obstruction.
3. Bilateral Renal Artery Stenosis
3. Bilateral Renal Artery Stenosis
ACE inhibitors can cause acute renal failure in these patients.
4. Concomitant Use with Aliskiren (a renin inhibitor)
4. Concomitant Use with Aliskiren (a renin inhibitor)
❌ Contraindicated in diabetic patients due to high risk of:
Hypotension
Hyperkalemia
Renal dysfunction
Monographs
Monographs
captopril.pdfCaptopril
Benazepril pharma.pdfBenazepril
ramipril.pdfRamipril
perindopril haneen elsayed.pdfPerindopril
Moexipril (2).pdfMeoxipril
lisinopril.pdfLisinopril
fosinopril.pdfFosinopril
enalapril.pdfEnalapril
trandolapril.pdfTrandolapril
quinapril.pdfQuinapril
Refrences
Refrences
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