Last reviewed 2026-04-20 · How we verify

Caduet (Amlodipine Besylate)

Calcium channel antagonist inhibiting transmembrane calcium influx into vascular and cardiac muscle.

Amlodipine besylate is a dihydropyridine calcium channel blocker indicated for hypertension and coronary artery disease including chronic stable angina and vasospastic angina. The drug demonstrates good tolerability with edema as the most common dose-related adverse reaction, occurring in 1.8-10.8% of patients depending on dose. Major drug interactions include simvastatin (limit to 20 mg daily) and CYP3A inhibitors requiring dose monitoring and adjustment. The medication has been evaluated in over 11,000 patients with discontinuation rates due to adverse reactions of only 1.5%, comparable to placebo.

At a glance

Mechanism of action

Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle cells. The drug binds to both dihydropyridine and nondihydropyridine binding sites on calcium channels, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. The contractile processes of cardiac and vascular smooth muscle depend on extracellular calcium ion movement through specific ion channels, which amlodipine selectively inhibits. Amlodipine acts as a peripheral arterial vasodilator that directly reduces peripheral vascular resistance and blood pressure. Within the physiologic pH range, amlodipine is an ionized compound (pKa=8.6) with a gradual rate of association and dissociation with the calcium channel receptor, resulting in a gradual onset of effect. Negative inotropic effects can be detected in vitro but have not been observed in intact animals at therapeutic doses, and serum calcium concentration is not affected by the drug. In exertional angina, amlodipine reduces total peripheral resistance and the rate pressure product, thereby decreasing myocardial oxygen demand. In vasospastic angina, amlodipine blocks constriction and restores blood flow in coronary arteries and arterioles in response to various vasoconstrictors including calcium, potassium, epinephrine, serotonin, and thromboxane A2 analogs.

Approved indications

• Hypertension
• Coronary Artery Disease (CAD)
• Chronic Stable Angina
• Vasospastic Angina (Prinzmetal’s or Variant Angina)
• Angiographically Documented CAD
• Primary Hyperlipidemia
• Heterozygous Familial Hypercholesterolemia (HeFH)
• Homozygous Familial Hypercholesterolemia
• Primary Dysbetalipoproteinemia
• Hypertriglyceridemia
• Type 2 Diabetes Mellitus with multiple risk factors for CHD
• Multiple risk factors for coronary heart disease (CHD) but without clinically evident CHD

Common side effects

• Low blood pressure
• Worsening heart failure
• Fatigue at rest
• Arrhythmia
• Cramping or pain
• Bradycardia
• High blood pressure
• Worsening kidney function
• Loose stools
• Leg swelling
• Abnormal serum calcium
• Rising liver enzymes

Drug interactions

• CYP3A inhibitors (moderate and strong)
• CYP3A inducers
• Sildenafil
• Simvastatin
• Cyclosporine
• Tacrolimus

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Caduet CI brief — competitive landscape report
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• Pfizer Inc. portfolio CI