Lercanidipine


Concise Prescribing Info
Indications/Uses
HTN.
Dosage/Direction for Use
Adult : PO Initially, 10 mg once daily, increased up to 20 mg once daily after 2 wk according to patient’s response.
Dosage Details
Oral
Hypertension
Adult: Initially, 10 mg once daily, may be increased up to 20 mg once daily after 2 wk according to patient’s response.
Renal Impairment
 CrCl (mL/min)  Dosage
 <30  Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken on an empty stomach. Take at least 15 min before meals.
Contraindications
Unstable angina pectoris, untreated CHF, recent MI (w/in 1 mth). Severe hepatic and renal (CrCl <30 mL/min) impairment. Pregnancy and lactation. Concurrent use w/ ciclosporin and strong CYP3A4 inhibitors.
Special Precautions
Patient w/ porphyria, myasthenia-like neuromuscular disease, cardiogenic shock, systolic heart failure, aortic stenosis, sick sinus syndrome (if pacemaker is not in position), ischaemic heart disease. Mild to moderate renal and hepatic impairment.
Adverse Reactions
Significant: Precordial pain or angina pectoris, hypotension.
Nervous: Fatigue, headache, dizziness.
CV: Palpitations, peripheral oedema, tachycardia, chest pain, orthostatic hypotension, vasodilatory effect.
GI: Abdominal pain, nausea, dyspepsia, diarrhoea, constipation, gingival hyperplasia.
Resp: Tinnitus.
Hepatic: Increased liver enzyme.
Genitourinary: Polyuria, nocturia.
Musculoskeletal: Muscle weakness.
Dermatologic: Flushing, rash, itch.
Patient Counseling Information
This drug may cause fatigue or dizziness, if affected, do not drive or operate machinery.
Overdosage
Symptoms: Severe hypotension and reflex tachycardia, cardiogenic shock, severe MI, bradycardia and loss of consciousness, drowsiness, emesis, mild renal failure. Management: Symptomatic and supportive treatment. Perform gastric lavage immediately. Administer activated charcoal. May give atropine for bradycardia.
Drug Interactions
CYP3A4 inducers (e.g. carbamazepine, phenytoin) may reduce plasma concentration of lercanidipine. β-blockers (e.g. metoprolol) can reduce the bioavailability of lercanidipine.
Potentially Fatal: Ciclosporin and strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir) may greatly increase lercanidipine concentration.
Food Interaction
Alcohol may potentiate vasodilating effect of lercanidipine. Grapefruit juice inhibits metabolism of lercanidipine thus increasing its plasma concentration and hypotensive effect.
Action
Description: Lercanidipine is a dihydropyridine calcium channel blocker. It inhibits influx of Ca into cardiac and smooth muscle, causing relaxation of vascular smooth muscle thus reducing peripheral vascular resistance and BP.
Pharmacokinetics:
Absorption: Completely absorbed from the GI tract. Bioavailability: Approx 10%. Peak plasma concentration: Approx 1.5-3 hr.
Distribution: Rapidly and widely distributed in the body. Plasma protein binding: >98%.
Metabolism: Metabolised in the liver by CYP3A4 enzyme into inactive metabolites. Undergoes hepatic first-pass metabolism.
Excretion: Mainly via urine (50%, as inactive metabolites). Terminal elimination half-life: Approx 8-10 hr.
Chemical Structure

Chemical Structure Image
Lercanidipine

Source: National Center for Biotechnology Information. PubChem Database. Lercanidipine, CID=65866, https://pubchem.ncbi.nlm.nih.gov/compound/Lercanidipine (accessed on Jan. 22, 2020)

Storage
Store below 25°C. Protect form light and moisture.
MIMS Class
ATC Classification
C08CA13 - lercanidipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
References
Buckingham R (ed). Lercanidipine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2017.

Joint Formulary Committee. Lercanidipine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2017.

Preston CL (ed). Ciclosporin [Systemic] + Lercanidipine [Systemic]. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2017.

Disclaimer: This information is independently developed by MIMS based on Lercanidipine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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