Flordipine

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Flordipine is a calcium channel blocker of the dihydropyridine class, primarily used in the management of hypertension and angina pectoris. It functions by inhibiting the influx of calcium ions through L-type calcium channels, which are predominantly found in the vascular smooth muscle and cardiac muscle. This action results in vasodilation and a subsequent decrease in blood pressure.

Pharmacology

Flordipine selectively targets the L-type calcium channels, which are responsible for the contraction of vascular smooth muscle. By blocking these channels, Flordipine causes relaxation of the smooth muscle, leading to vasodilation and reduced peripheral resistance. This mechanism is beneficial in lowering blood pressure and reducing the workload on the heart.

Pharmacokinetics

Flordipine is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 1 to 2 hours after oral administration. It undergoes extensive first-pass metabolism in the liver, resulting in a bioavailability of about 20-30%. The drug is highly protein-bound and is metabolized primarily by the cytochrome P450 enzyme CYP3A4. The elimination half-life of Flordipine is approximately 8 to 10 hours, allowing for once-daily dosing.

Clinical Uses

Flordipine is indicated for the treatment of:

• Hypertension: As a first-line agent or in combination with other antihypertensive drugs.
• Angina pectoris: Particularly in patients with stable angina, to reduce the frequency and severity of anginal attacks.

Adverse Effects

Common side effects of Flordipine include:

• Headache
• Dizziness
• Flushing
• Peripheral edema
• Palpitations

Less common but serious adverse effects may include:

• Hypotension
• Bradycardia
• Heart failure

Contraindications

Flordipine is contraindicated in patients with:

• Severe aortic stenosis
• Cardiogenic shock
• Unstable angina

Drug Interactions

Flordipine may interact with other medications, including:

• Beta-blockers: May enhance the hypotensive effect.
• CYP3A4 inhibitors: Such as ketoconazole and erythromycin, which can increase Flordipine plasma levels.
• Grapefruit juice: Can increase the bioavailability of Flordipine by inhibiting CYP3A4.

Research and Development

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

Also see

• Calcium channel blocker
• Hypertension
• Angina pectoris
• Dihydropyridine