Calcium channel blockers (CCBs) inhibit L-type voltage-gated calcium channels in cardiac and smooth muscle cells.
Classification
| Classification | Effect | Examples | Adverse effects |
|---|---|---|---|
| Dihydropyridine CCBs | Primarily act on vascular smooth muscles to cause vasodilation | Amlodipine, nifedipine, felodipine, nicardipine, clevidipine, and nimodipine | Reflex tachycardia, headache, flushing, dizziness, and peripheral edema |
| Non-dihydropyridine CCBs | Primarily act on the heart | Verapamil and diltiazem | Bradycardia, atrioventricular block, worsening heart failure, and constipation |
- Kinetics
- Undergo 1st pass metabolism (Poor oral bioavailability)
- Hepatic enzyme inhibitors
- Mechanism of action
- Vasodilation → reduced peripheral resistance
- Reduced sinoatrial node automaticity → negative chronotropy
- Reduced conduction through the atrioventricular node → negative dromotropy
- Reduced myocardial contractility → negative ionotropy
- Indications
- Hypertension
- Hypertension in pregnancy
- Stable angina
- Prinzmetal angina
- Arrhythmias (non-dihydropyridines only)
- To prevent vasospasms in subarachnoid haemorrhage (nimodipine)
- Hypertensive emergency
- Contraindications
- Non-dihydropyridine CCBs are contraindicated in patients with:
- Heart block
- Sick sinus syndrome
- Heart failure with reduced ejection fraction
- Severe bradycardia
- Non-dihydropyridine CCBs are contraindicated in patients with:
- Notable drug interactions
- Beta blockers + non-dihydropyridine CCBs → severe bradycardia or heart block