Adult: As monotherapy or in combination with other antihypertensive agents: Initially, 2 mg once daily; may increase in increments of 2 mg every 3-4 weeks according to response. Max: 6 mg once daily.
Patient with congenital or acquired QT prolongation, pre-existing abnormalities in the activity of the SA and AV nodes; poor cardiac reserve; heart failure, hypertrophic cardiomyopathy, outflow tract obstruction. Avoid abrupt withdrawal. Hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Increased angina and/or MI; QT prolongation, symptomatic hypotension, syncope. Cardiac disorders: Palpitations (transient), tachycardia. Gastrointestinal disorders: Nausea, abdominal discomfort, gingival hyperplasia. General disorders and admin site conditions: Asthenia, transient oedema. Investigations: Increased serum alkaline phosphatase. Nervous system disorders: Headache, dizziness (transient). Renal and urinary disorders: Polyuria. Skin and subcutaneous tissue disorders: Rash, pruritus, erythema. Vascular disorders: Transient flushing (especially of face).
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure and heart rate.
Overdosage
Symptoms: Prolonged peripheral vasodilation associated with hypotension and tachycardia, bradycardia, or prolonged atrioventricular conduction. Management: Supportive treatment and cardiac function monitoring.
Drug Interactions
Enhanced hypotensive effect with other antihypertensive agents (e.g. diuretics [e.g. furosemide], β-blockers [e.g. propranolol], ACE inhibitors [e.g. captopril]). Increased serum concentration with cimetidine, and strong CYP3A4 inhibitors (e.g. itraconazole). May reverse the decrease in renal plasma flow and glomerular filtration rate induced by ciclosporin in patient with renal transplant. Decreased serum concentration with strong CYP3A4 inducers (e.g. rifampicin).
Food Interaction
Increased serum concentration with grapefruit juice.
Lab Interference
May lead to false-negative ARR (aldosterone/renin ratio).
Action
Description: Lacidipine is a dihydropyridine Ca-channel blocker. It inhibits Ca ions from entering the slow channels or select voltage-sensitive areas of the vascular smooth muscle and myocardium during depolarisation, thus producing coronary vascular smooth muscle relaxation resulting in coronary and peripheral vasodilation. Pharmacokinetics: Absorption: Rapidly but poorly absorbed from the gastrointestinal tract. Bioavailability: Approx 10%. Time to peak plasma concentration: 30-150 minutes. Distribution: Plasma protein binding: >95% to albumin and α-1 glycoprotein. Metabolism: Metabolised in the liver by CYP3A4 isoenzymes; undergoes extensive first-pass metabolism. Excretion: Mainly via faeces (70% as metabolites); urine (remainder as metabolites). Elimination half-life: 13-19 hours.
Chemical Structure
Lacidipine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5311217, Lacidipine. https://pubchem.ncbi.nlm.nih.gov/compound/Lacidipine. Accessed Mar. 29, 2022.
C08CA09 - lacidipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
References
Anon. Lacidipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/02/2022.Buckingham R (ed). Lacidipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/02/2022.Joint Formulary Committee. Lacidipine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/02/2022.Lacidipine 2 mg Film-coated Tablets (Zentiva Pharma UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 15/02/2022.Lacipil Tablet 2 mg, 4 mg (Glaxo Wellcome S.A.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 15/02/2022.
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