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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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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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