Elnadipine

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

Pharmacology

Elnadipine 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 relaxation of the vascular smooth muscle, resulting in vasodilation and a subsequent decrease in blood pressure. The reduction in peripheral vascular resistance is the primary mechanism by which elnadipine lowers blood pressure.

Mechanism of Action

Elnadipine selectively blocks calcium channels in the vascular smooth muscle, which prevents calcium from entering these cells. Calcium is essential for muscle contraction, so its inhibition leads to muscle relaxation. This relaxation of the smooth muscle in the arterial walls causes the arteries to dilate, reducing systemic vascular resistance and lowering blood pressure.

Pharmacokinetics

Elnadipine 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 in the plasma and is metabolized primarily by the liver. The metabolites are excreted mainly in the urine.

Clinical Uses

Elnadipine is primarily used in the treatment of:

• Hypertension: By reducing peripheral vascular resistance, elnadipine effectively lowers blood pressure in patients with hypertension.
• Angina pectoris: The vasodilatory effects of elnadipine improve blood flow to the heart muscle, which can help alleviate the symptoms of angina.

Side Effects

Common side effects of elnadipine include:

• Headache
• Dizziness
• Flushing
• Peripheral edema

These side effects are generally mild and often resolve with continued use. However, patients should be monitored for any adverse reactions, especially if they have pre-existing conditions that may be exacerbated by vasodilation.

Contraindications

Elnadipine should be used with caution in patients with:

• Severe aortic stenosis
• Unstable angina
• Severe hypotension

Drug Interactions

Elnadipine may interact with other medications, such as:

• Other antihypertensive agents, which may potentiate the blood pressure-lowering effects.
• CYP3A4 inhibitors, which can increase the plasma concentration of elnadipine.

Research and Development

Ongoing research is exploring the potential benefits of elnadipine in other cardiovascular conditions and its long-term effects on cardiovascular health.

Also see

• Calcium channel blocker
• Hypertension
• Angina pectoris
• Dihydropyridine