Calcium Channel Blockers (CCBs): Types and Classification
Calcium channel blockers are divided into two main structural and functional categories: dihydropyridines and non-dihydropyridines, each with distinct pharmacological properties and clinical applications. The main calcium channel blockers include dihydropyridines (amlodipine, felodipine, nifedipine, and nisoldipine) and non-dihydropyridines (diltiazem and verapamil). 1, 2
Dihydropyridine CCBs
Dihydropyridines have high selectivity for L-type calcium channels in the vasculature and produce potent peripheral vasodilation:
- Amlodipine: Used for hypertension and angina 3
- Felodipine: Dihydropyridine derivative used for hypertension 4
- Nifedipine: Potent vasodilator
- Nisoldipine: Primarily used for hypertension
- Isradipine: Binds to calcium channels with high affinity and specificity 5
Key Characteristics of Dihydropyridines:
- Potent peripheral vasodilation
- Minimal direct effects on cardiac conduction
- May cause reflex tachycardia (especially short-acting formulations)
- Higher incidence of peripheral edema (12.3%) 2
- Primary use in hypertension and angina
Non-Dihydropyridine CCBs
Non-dihydropyridines have less vascular selectivity but more pronounced effects on cardiac tissues:
- Diltiazem: Moderate to weak inhibitor of CYP3A4 1
- Verapamil: Has significant negative chronotropic and inotropic effects 1, 2
Key Characteristics of Non-Dihydropyridines:
- Significant slowing of sinoatrial and atrioventricular node conduction
- Negative chronotropic and inotropic effects
- Lower incidence of peripheral edema (3.1%) 2
- Used for hypertension, angina, and rate control in atrial fibrillation/flutter
- Should not be used in heart failure with reduced ejection fraction 2
Mechanism of Action
CCBs work by inhibiting the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle cells by blocking voltage-dependent L-type calcium channels 2, 6. This results in:
- Relaxation of arterial smooth muscle
- Decreased peripheral vascular resistance
- Reduced blood pressure
- Increased coronary blood flow
- Prevention of coronary artery spasm 2
Clinical Considerations
Drug Interactions:
Contraindications:
Side Effects:
Overdose Management:
- Calcium administration (first-line)
- Vasopressors for hypotension
- Atropine for significant bradycardia
- High-dose insulin for refractory hypotension 9
The selection of a specific calcium channel blocker should be based on the patient's comorbidities, potential drug interactions, and the specific cardiovascular condition being treated 10.