Elgodipine

Elgodipine is a pharmaceutical compound classified as a calcium channel blocker (CCB). It is primarily used in the management of hypertension and certain types of angina pectoris. Elgodipine functions by inhibiting the influx of calcium ions through L-type calcium channels, which are predominantly found in the smooth muscle cells of the vascular system and the myocardium.

Pharmacology

Elgodipine belongs to the dihydropyridine class of calcium channel blockers, which are known for their potent vasodilatory effects. By blocking calcium entry into cells, Elgodipine causes relaxation of vascular smooth muscle, leading to a decrease in peripheral vascular resistance and a subsequent reduction in blood pressure.

Mechanism of Action

Elgodipine selectively inhibits L-type calcium channels, which are responsible for the contraction of cardiac and smooth muscle. This inhibition results in decreased intracellular calcium concentrations, leading to muscle relaxation. In the heart, this effect can reduce myocardial oxygen demand and improve coronary blood flow, making it useful in the treatment of angina.

Pharmacokinetics

Elgodipine is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 1-2 hours after oral administration. It is extensively metabolized in the liver, primarily via the cytochrome P450 enzyme system, and is excreted mainly in the urine. The elimination half-life of Elgodipine is approximately 8-12 hours, allowing for once or twice daily dosing.

Clinical Uses

Elgodipine is indicated for the treatment of:

• Hypertension: As a first-line or adjunctive therapy to lower blood pressure and reduce the risk of cardiovascular events.
• Angina pectoris: To relieve chest pain and improve exercise tolerance in patients with chronic stable angina.

Adverse Effects

Common side effects of Elgodipine include:

• Headache
• Dizziness
• Flushing
• Peripheral edema

Less common but serious adverse effects may include:

• Hypotension
• Bradycardia
• Heart failure

Contraindications

Elgodipine is contraindicated in patients with:

• Severe aortic stenosis
• Cardiogenic shock
• Known hypersensitivity to dihydropyridines

Drug Interactions

Elgodipine may interact with other medications, including:

• Beta-blockers: May enhance the hypotensive effect.
• CYP3A4 inhibitors: Such as ketoconazole or itraconazole, which may increase Elgodipine plasma levels.

Also see

• Calcium channel blocker
• Hypertension
• Angina pectoris
• Dihydropyridine