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Amlodipine

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Medicinal Chemistry

Definition

Amlodipine is a calcium channel blocker used primarily to treat high blood pressure and angina. By inhibiting the influx of calcium ions through voltage-gated L-type calcium channels in vascular smooth muscle and cardiac tissue, amlodipine promotes vasodilation and reduces the workload on the heart.

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5 Must Know Facts For Your Next Test

  1. Amlodipine has a long half-life, allowing for once-daily dosing, which enhances patient compliance.
  2. It is often prescribed as a first-line treatment for hypertension and is effective in both monotherapy and combination therapy with other antihypertensive agents.
  3. Common side effects include peripheral edema, dizziness, and flushing, primarily due to its vasodilatory effects.
  4. Unlike some other calcium channel blockers, amlodipine is less likely to cause reflex tachycardia due to its gradual onset of action.
  5. Amlodipine can be particularly beneficial in patients with coronary artery disease, as it not only lowers blood pressure but also improves exercise tolerance.

Review Questions

  • How does amlodipine's mechanism of action as a calcium channel blocker contribute to its effectiveness in treating hypertension?
    • Amlodipine works by blocking L-type calcium channels in vascular smooth muscle, which decreases intracellular calcium levels. This leads to relaxation of the smooth muscle and subsequent vasodilation, which lowers systemic vascular resistance and reduces blood pressure. By inhibiting calcium entry into cardiac myocytes, it also reduces myocardial oxygen demand, making it effective for patients with both hypertension and angina.
  • Evaluate the potential side effects of amlodipine and discuss how they relate to its pharmacological action.
    • Common side effects of amlodipine include peripheral edema, dizziness, and flushing. These effects are linked to its vasodilatory action; as blood vessels expand, fluid can accumulate in tissues leading to edema. Dizziness may occur due to lowered blood pressure and reflex responses. Understanding these side effects is crucial for managing patient expectations and ensuring adherence to the treatment regimen.
  • Synthesize the clinical applications of amlodipine in managing cardiovascular diseases and analyze how its unique properties compare to other medications in its class.
    • Amlodipine is widely used not only for treating hypertension but also for managing angina and coronary artery disease due to its ability to induce vasodilation without causing significant reflex tachycardia. Compared to other calcium channel blockers like diltiazem or verapamil, amlodipine has a longer duration of action and is less likely to affect heart rate negatively. This makes it a preferred choice for many practitioners when considering long-term management strategies for cardiovascular diseases.
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