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Lercanidipine – Effects, Dosage and Side Effects

Lercanidipine is a calcium channel blocker used to treat high blood pressure. It relaxes blood vessels and effectively lowers blood pressure.

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Things worth knowing about "Lercanidipine"

Lercanidipine is a calcium channel blocker used to treat high blood pressure. It relaxes blood vessels and effectively lowers blood pressure.

What is Lercanidipine?

Lercanidipine is a prescription medication belonging to the class of calcium channel blockers (calcium antagonists), specifically a third-generation dihydropyridine. It is primarily used to treat arterial hypertension (high blood pressure). Lercanidipine is recognized for its high vascular selectivity and favorable tolerability profile.

Mechanism of Action

Lercanidipine blocks voltage-gated L-type calcium channels in the smooth muscle cells of blood vessel walls. By inhibiting calcium influx, the vessel walls relax, causing vasodilation (widening of blood vessels) and a reduction in peripheral vascular resistance. This results in a lowering of blood pressure.

Compared to older calcium channel blockers (such as nifedipine), lercanidipine has a slower onset of action and a longer duration of effect, leading to a more gradual blood pressure reduction and a lower risk of reflex tachycardia (rapid heart rate).

Indications

Arterial hypertension – as monotherapy or in combination with other antihypertensive agents
Use in patients who do not tolerate other calcium antagonists due to side effects such as ankle swelling

Dosage

The usual starting dose is 10 mg once daily, taken at least 15 minutes before a meal. If blood pressure control is insufficient, the dose may be increased to 20 mg daily after 2 weeks. The exact dosage is always determined by the treating physician.

Important Notes on Administration

Lercanidipine should not be taken with grapefruit juice, as it inhibits the enzyme responsible for breaking down the drug, potentially raising blood levels.
The medication should be taken at the same time each day for consistent effect.
Discontinuation should not be abrupt but gradual and only under medical supervision.

Side Effects

Lercanidipine is generally well tolerated. Possible side effects include:

Common: Headache, flushing (facial redness), ankle edema (fluid retention in legs), palpitations, dizziness
Occasional: Nausea, abdominal discomfort, fatigue, tachycardia (fast heart rate)
Rare: Gingival hyperplasia (gum overgrowth), allergic reactions, muscle pain

Edema occurs less frequently with lercanidipine than with other dihydropyridines, owing to its high membrane affinity and gradual onset of vasodilation.

Contraindications and Interactions

Contraindications

Severe heart failure or unstable angina
Severe renal or hepatic impairment
Pregnancy and breastfeeding
Concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole, ciclosporin)

Drug Interactions

CYP3A4 inhibitors (e.g., certain antibiotics, antifungals, ciclosporin) can increase plasma levels of lercanidipine.
CYP3A4 inducers (e.g., rifampicin, antiepileptics) may reduce the effectiveness of lercanidipine.
Beta-blockers and other antihypertensives may enhance the blood pressure-lowering effect.
Alcohol can potentiate the vasodilatory effect and lead to circulatory problems.

References

European Medicines Agency (EMA): Product information for Lercanidipine. Available at: https://www.ema.europa.eu
Mancia G et al. – 2023 ESH Guidelines for the Management of Arterial Hypertension. Journal of Hypertension, 2023. Available at: https://www.ncbi.nlm.nih.gov/pubmed
Burnier M, Brunner HR – Lercanidipine: A New Generation Calcium Antagonist. Expert Opinion on Pharmacotherapy, 2000. Available at: https://www.ncbi.nlm.nih.gov/pubmed

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