Amlodipine Uses and Indications
Amlodipine is primarily indicated for the treatment of hypertension and coronary artery disease, including chronic stable angina, vasospastic angina, and angiographically documented CAD. 1
Hypertension
- Amlodipine is FDA-approved for the treatment of hypertension, to lower blood pressure and reduce the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions 1
- It can be used alone or in combination with other antihypertensive agents for effective blood pressure control 1
- In the ALLHAT study, amlodipine was equally effective as chlorthalidone (a thiazide diuretic) and lisinopril (an ACE inhibitor) in preventing coronary heart disease mortality and morbidity 2
- Amlodipine works by inhibiting calcium influx through "slow" channels in peripheral vascular smooth muscle cells, producing vasodilation in peripheral vascular beds 3
Coronary Artery Disease
Chronic Stable Angina
- Amlodipine is indicated for the symptomatic treatment of chronic stable angina, either as monotherapy or in combination with other antianginal agents 1
- It is considered an alternative to beta-blockers in patients who cannot tolerate them 2
- The European Society of Cardiology recommends amlodipine as a second-line agent when angina persists despite treatment with a beta-blocker 2
- Clinical trials have shown that amlodipine provides good anti-anginal and anti-ischemic efficacy for a full 24 hours with once-daily dosing 4
Vasospastic Angina (Prinzmetal's or Variant Angina)
- Amlodipine is indicated for the treatment of confirmed or suspected vasospastic angina 1
- It has been shown to be consistently effective in patients with vasospastic angina 4
- It can be used as monotherapy or in combination with other antianginal agents 1
Angiographically Documented CAD
- In patients with recently documented CAD by angiography and without heart failure or ejection fraction <40%, amlodipine is indicated to reduce the risk of hospitalization for angina and to reduce the risk of coronary revascularization procedures 1
Heart Failure Considerations
- Amlodipine is one of the few calcium channel blockers that can be safely used in patients with compensated heart failure when other therapies are insufficient 2
- Unlike non-dihydropyridine calcium channel blockers (diltiazem and verapamil), amlodipine does not have significant negative inotropic effects 5
- In the ALLHAT study, amlodipine was associated with a higher risk of heart failure compared to chlorthalidone, but this did not translate to increased mortality 2
Pharmacological Properties
- Amlodipine belongs to the dihydropyridine subclass of calcium channel blockers 5
- It has a long elimination half-life of 36-45 hours, allowing for once-daily dosing 5, 6
- Absorption after oral administration is slow with peak plasma concentration occurring 6-8 hours after dosing, which contributes to its gradual onset of action 6
- This gradual onset reduces the incidence of side effects such as reflex tachycardia and headache, which can be troublesome with other calcium antagonists 4
- Amlodipine has high selectivity for vascular smooth muscle with minimal effect on myocardial contractility or cardiac conduction 5
Common Side Effects and Precautions
- The most common adverse effects are related to vasodilation: peripheral edema, headaches, and flushing 7
- Unlike some other calcium channel blockers, amlodipine does not cause significant postural hypotension, reflex tachycardia, or cardiac conduction disturbances 7
- Amlodipine has not shown unfavorable effects on serum glucose or lipid levels 5
- When combined with statins, amlodipine has minimal drug interactions compared to other calcium channel blockers like diltiazem and verapamil 2
Dosing Considerations
- The usual starting dose is 5 mg once daily, which can be increased to 10 mg daily if required to control symptoms 4
- Amlodipine can be taken with or without food 1
- For patients with angina, clinical studies have confirmed that once-daily dosing provides anti-anginal efficacy for a full 24 hours 4
Amlodipine's unique pharmacokinetic profile, efficacy in both hypertension and various forms of coronary artery disease, and favorable side effect profile make it a versatile and valuable medication in cardiovascular disease management.