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Drugs, Supplies and Delivery
Nisoldipine
Nisoldipine is a second-generation dihydropyridine calcium channel blocker (CCB) used primarily for the management of hypertension. It is known for its potent vasodilatory effects and selectivity for vascular smooth muscle, making it particularly effective in reducing blood pressure with minimal cardiac effects. 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 nisoldipine, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Nisoldipine selectively blocks L-type voltage-gated calcium channels in vascular smooth muscle, inhibiting calcium influx. This results in:
- Vasodilation of peripheral arteries, reducing systemic vascular resistance and blood pressure.
- Minimal effects on cardiac muscle, making it less likely to cause negative inotropic or chronotropic effects compared to non-dihydropyridine CCBs (Lippincott, Lange).
Nisoldipine’s high vascular selectivity makes it particularly useful for patients with hypertension and comorbid conditions like angina or peripheral vascular disease (BNF).
- Hypertension: Nisoldipine is indicated for the treatment of essential hypertension, either as monotherapy or in combination with other antihypertensive agents (BNF).
- Off-Label Uses:
- Chronic stable angina (due to its vasodilatory effects on coronary arteries).
- Raynaud’s phenomenon (to relieve vasospasm in peripheral arteries) (Lippincott).
- Standard Dose:
- Initial dose: 17 mg once daily (extended-release formulation).
- Maintenance dose: 17–34 mg once daily (max 34 mg/day) (BNF).
- Administration:
- Should be taken on an empty stomach (1 hour before or 2 hours after meals) to avoid reduced absorption.
- Extended-release tablets must be swallowed whole and not crushed or chewed (Lippincott).
- Common: Peripheral edema (due to arteriolar dilation), headache, flushing, dizziness, and palpitations (Lange).
- Serious: Hypotension, reflex tachycardia, and gingival hyperplasia (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 nisoldipine levels, raising the risk of toxicity (Lippincott).
- Grapefruit Juice: Inhibits CYP3A4, increasing nisoldipine bioavailability and risk of side effects (BNF).
- Rifampin: Reduces nisoldipine levels, decreasing efficacy (Lange).
Nisoldipine is the generic name for this medication. It is marketed under the brand name Sular® (extended-release formulation). Generic versions are also available, making it an affordable option for patients.
