Olradipine

Olradipine is a calcium channel blocker that is primarily used in the management of hypertension and angina pectoris. It belongs to the class of dihydropyridine calcium channel blockers, which are known for their potent vasodilatory effects.

Pharmacology

Olradipine works by inhibiting the influx of calcium ions through L-type calcium channels in the smooth muscle cells of the vascular system. This action leads to a decrease in intracellular calcium, resulting in relaxation of the vascular smooth muscle and subsequent vasodilation. The vasodilatory effect reduces peripheral vascular resistance, thereby lowering blood pressure.

Mechanism of Action

Olradipine selectively targets the L-type calcium channels, which are predominantly found in the vascular smooth muscle and cardiac muscle. By blocking these channels, olradipine reduces the contractility of the heart and dilates the arteries, which decreases the workload on the heart and lowers blood pressure.

Pharmacokinetics

Olradipine is well absorbed from the gastrointestinal tract, but it undergoes significant first-pass metabolism in the liver, which affects its bioavailability. It is highly protein-bound and is metabolized primarily by the liver enzyme CYP3A4. The elimination half-life of olradipine is approximately 8 to 12 hours, allowing for once-daily dosing in most patients.

Clinical Use

Olradipine is indicated for the treatment of hypertension and chronic stable angina. It may be used as monotherapy or in combination with other antihypertensive agents such as ACE inhibitors, beta-blockers, or diuretics.

Dosage and Administration

The typical starting dose of olradipine for adults is 5 mg once daily, which may be increased to 10 mg once daily based on the patient's response and tolerability. Dose adjustments may be necessary for patients with hepatic impairment.

Adverse Effects

Common side effects of olradipine include headache, dizziness, flushing, and peripheral edema. These effects are generally mild and tend to diminish with continued use. Rare but serious adverse effects include hypotension, bradycardia, and heart block.

Contraindications and Precautions

Olradipine is contraindicated in patients with known hypersensitivity to dihydropyridine calcium channel blockers. Caution is advised in patients with severe aortic stenosis, heart failure, or hepatic impairment.

Drug Interactions

Olradipine may interact with other medications metabolized by CYP3A4, such as simvastatin and cyclosporine. It may also potentiate the effects of other antihypertensive agents, leading to an increased risk of hypotension.

Also see

• Calcium channel blocker
• Hypertension
• Angina pectoris
• Dihydropyridine