Za Pharmacy
Drugs, Supplies and Delivery
Nicardipine
Nicardipine is a dihydropyridine calcium channel blocker (CCB) widely used for the management of hypertension and angina. It is particularly valued for its potent vasodilatory effects and rapid onset of action, making it suitable for both acute and chronic settings. This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to provide a detailed overview of nicardipine, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Nicardipine selectively blocks L-type voltage-gated calcium channels in vascular smooth muscle, inhibiting calcium influx. This results in:
- Vasodilation of peripheral and coronary arteries, reducing systemic vascular resistance and blood pressure.
- Increased coronary blood flow, which helps alleviate angina symptoms (Lippincott, Lange).
Unlike non-dihydropyridine CCBs (e.g., verapamil, diltiazem), nicardipine has minimal effects on cardiac conduction and contractility, making it a safer option for patients with heart failure or conduction disorders (BNF).
- Hypertension:
- Chronic Hypertension: Used as an oral formulation for long-term management.
- Hypertensive Emergencies: Intravenous (IV) nicardipine is effective for rapid blood pressure control in acute settings (BNF).
- Chronic Stable Angina: Improves myocardial oxygen supply by dilating coronary arteries (Lippincott).
- Off-Label Uses:
- Subarachnoid hemorrhage (to prevent vasospasm).
- Preterm labor (to suppress uterine contractions) (Lange).
- Oral Formulation (Chronic Hypertension/Angina):
- Initial dose: 20 mg three times daily.
- Maintenance dose: 20–40 mg three times daily (max 120 mg/day) (BNF).
- Intravenous Formulation (Hypertensive Emergencies):
- Initial infusion rate: 5 mg/hour, titrated to effect.
- Maintenance dose: 3–5 mg/hour (max 15 mg/hour) (Lippincott).
Administration:
- Oral tablets should be taken with or without food, but consistency is key to maintaining stable plasma levels.
- IV nicardipine should be administered under close monitoring in a clinical setting (Lange).
- Common: Headache, flushing, peripheral edema, dizziness, and palpitations (Lippincott).
- Serious: Hypotension, reflex tachycardia (especially with rapid IV administration), and acute kidney injury (BNF).
- Hypotension: Use with caution in patients with severe hypotension or cardiogenic shock.
- Heart Failure: Avoid in patients with severe heart failure due to risk of worsening symptoms (Lippincott).
- Hepatic Impairment: Dose reduction may be necessary in patients with liver dysfunction (BNF).
- Pregnancy: Generally safe but should be used under medical supervision (Lange).
- Beta-Blockers: May exacerbate hypotension and heart failure; monitor closely.
- CYP3A4 Inhibitors (e.g., ketoconazole, erythromycin): Increase nicardipine levels, raising the risk of toxicity (Lippincott).
- Grapefruit Juice: Inhibits CYP3A4, increasing nicardipine bioavailability and risk of side effects (BNF).
- Rifampin: Reduces nicardipine levels, decreasing efficacy (Lange).
Nicardipine is the generic name for this medication. It is marketed under various brand names, including Cardene® (oral and IV formulations). Generic versions are also available, making it an affordable option for patients
