Lercanidipine

Lercanidipine is a third-generation calcium channel blocker of the dihydropyridine type. It is characterized by high lipophilicity (fat solubility), which leads to slow, steady accumulation in the blood vessel walls.

A key advantage over amlodipine: lercanidipine causes ankle edema considerably less often. This makes it particularly suitable for patients who suffer from this typical side effect of calcium channel blockers.

Lercanidipine is available as a single-ingredient product and in combination with enalapril (Enalapril/Lercanidipin-ratiopharm). It is taken once daily.

Lercanidipine blocks voltage-dependent L-type calcium channels in the vascular muscle:

Mechanism of action:

• Blocks the influx of calcium into vascular smooth muscle cells
• Arteries and arterioles dilate
• Peripheral vascular resistance decreases
• Blood pressure falls

Special features (3rd generation):

• Extremely high lipophilicity
• Slow accumulation in the cell membranes of the vessel wall
• Steady, slow onset of action
• No reflex increase in heart rate
• Less edema due to even dilation of the blood vessels

Advantages over amlodipine:

• Considerably less ankle edema
• Less facial redness (flushing)
• Lower reflex activation of the sympathetic nervous system
• Renal vasodilation (kidney protection)

Onset of action: Peak plasma levels after 1.5-3 hours. Due to storage in the membranes, the effect lasts 24 hours.

Lercanidipine is suitable for:

• Adults with mild to moderate high blood pressure

Particularly recommended for:

• Patients with ankle edema while taking amlodipine
• Patients who develop flushing while taking nifedipine
• In combination with ACE inhibitors (enalapril)
• Older patients

Not suitable:

• Severe heart failure (NYHA III-IV)
• Unstable angina pectoris
• Severe aortic stenosis
• Within 4 weeks after a heart attack
• Severe liver or kidney impairment
• Pregnancy and breastfeeding

High blood pressure:

• Usual dose: 10 mg once daily
• If needed, increase to 20 mg once daily
• Maximum dose: 20 mg daily

In older patients:

• Starting dose: 10 mg once daily
• No dose adjustment needed if organ function is normal

Available strengths:

• 10 mg, 20 mg tablets

Combination product:

• Lercanidipine + enalapril (Enalapril/Lercanidipin-ratiopharm)

How to take:

• Once daily, preferably in the morning
• Take at least 15 minutes before a meal
• Swallow with sufficient water
• NO grapefruit juice (inhibits breakdown)

Important – take on an empty stomach: Lercanidipine should be taken before eating, because a high-fat meal can increase absorption fourfold. This can lead to an undesirably strong drop in blood pressure.

Notes:

• No alcohol close to the time of taking it (increased vasodilation)
• Regular blood pressure checks
• No abrupt discontinuation needed (but consult your doctor)

Lercanidipine must not be taken in cases of:

• Hypersensitivity to lercanidipine or other dihydropyridines
• Severe heart failure (NYHA III-IV)
• Unstable angina pectoris
• Severe aortic stenosis
• Within 4 weeks after a heart attack
• Severe liver or kidney impairment (GFR below 30 ml/min)
• Pregnancy and breastfeeding
• At the same time as strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir)
• At the same time as cyclosporine

Caution in cases of:

• Sick sinus syndrome (without a pacemaker)
• Left ventricular dysfunction
• Mild to moderate kidney or liver impairment

Pregnancy: Contraindicated. There are insufficient data on safety during pregnancy.

Common (1-10%):

• Headache
• Facial redness (flushing) – less frequent than with amlodipine
• Palpitations
• Ankle edema – considerably less frequent than with amlodipine (approx. 1-2% vs. 10-15%)

Uncommon (0.1-1%):

• Dizziness

Rare:

• Gastrointestinal complaints
• Fatigue
• Skin rash
• Muscle pain
• Chest pain

Very rare:

• Angina pectoris
• Syncope (fainting)
• Gingival hyperplasia (overgrowth of the gums)
• Elevated liver enzymes
• Increased urge to urinate

Advantage: The rate of ankle edema is significantly lower with lercanidipine than with amlodipine or nifedipine. This is the main reason for choosing lercanidipine.

Contraindicated with:

• Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir)
• Cyclosporine (mutual increase in blood levels)

Caution with:

• Moderate CYP3A4 inhibitors (erythromycin, fluconazole)
• CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) → reduced effect
• Digoxin → slight increase in blood levels
• Simvastatin → close monitoring
• Beta blockers → stronger lowering of blood pressure (usually desired)
• Cimetidine → increased lercanidipine levels

Grapefruit: Grapefruit juice inhibits CYP3A4 and can considerably increase lercanidipine levels. Avoid grapefruit juice!

Alcohol: Alcohol enhances the vasodilating effect. Avoiding it close to the time of taking the medication is recommended.