Angiotensin converting enzyme inhibitor

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Angiotensin-converting enzyme inhibitors, commonly referred to as ACE inhibitors, are a class of medications primarily used to treat hypertension (high blood pressure) and congestive heart failure. These drugs work by inhibiting the enzyme angiotensin-converting enzyme (ACE), which plays a crucial role in the renin-angiotensin system (RAS), a hormone system that regulates blood pressure and fluid balance.

Mechanism of Action

ACE inhibitors function by blocking the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby decreasing blood pressure. By inhibiting this conversion, ACE inhibitors reduce the production of angiotensin II and decrease the breakdown of bradykinin, a peptide that promotes vasodilation. This leads to dilation of blood vessels and a reduction in blood pressure.

Clinical Uses

ACE inhibitors are primarily used in the treatment of:

• Hypertension - They are often first-line treatments for high blood pressure.
• Heart failure - They are used to improve symptoms and decrease the progression of heart failure.
• Myocardial infarction - Post-heart attack, they are used to improve survival rates and reduce the risk of heart failure.
• Diabetic nephropathy - They help in protecting the kidneys in patients with diabetes by reducing the progression of kidney damage.

Side Effects

While generally safe, ACE inhibitors can cause several side effects, including:

• Cough - A persistent dry cough is one of the most common reasons patients discontinue use.
• Hyperkalemia - Elevated potassium levels in the blood, which can be dangerous if not monitored.
• Angioedema - Swelling of the deeper layers of the skin, potentially life-threatening especially if the swelling occurs in the throat.
• Renal impairment - Particularly in patients with pre-existing kidney issues or those taking other medications that affect kidney function.

Examples of ACE Inhibitors

Some common ACE inhibitors include:

• Enalapril
• Lisinopril
• Ramipril
• Captopril

Pharmacokinetics

ACE inhibitors are absorbed from the gastrointestinal tract, with bioavailability varying between different members of the class. They are primarily excreted by the kidneys, and dose adjustments may be necessary in patients with renal impairment.

History

The development of ACE inhibitors began with the discovery of the Brazilian pit viper's venom effects on blood pressure in the 1960s. This led to the identification of the first ACE inhibitor, captopril, in the 1970s. Since then, several more ACE inhibitors have been developed, offering varying strengths, durations of action, and side effect profiles.

Future Directions

Research continues into developing ACE inhibitors with better efficacy, fewer side effects, and broader therapeutic applications. Additionally, there is ongoing investigation into the role of ACE inhibitors in treating other medical conditions such as migraine and certain types of dementia.