Adult: For the short-term treatment of acute severe hypertension: Initially, 3-5 mg/hour via continuous IV infusion over 15 minutes, may be increased in increments of 2.5 mg/hour every 5 minutes (rapid titration) or 0.5-2.5 mg/hour every 15 minutes (gradual titration) according to patient's response up to a Max of 15 mg/hour. Once the desired blood pressure is achieved, dose may be reduced to the maintenance infusion rate of 2-4 mg/hour. Dosage and treatment recommendations may vary among individual products or between countries (refer to detailed product or local institution treatment guidelines). Elderly: For short-term treatment of acute severe hypertension: Initially, 1-5 mg/hour via continuous IV infusion based on patient's blood pressure and clinical condition. Following 30 minutes, dose may be adjusted in increments of 0.5 mg/hour according to patient's response up to a Max of 15 mg/hour. Dosage recommendations may vary among individual products or between countries (refer to detailed product or local institution treatment guidelines). Child: For the treatment of acute severe hypertension in ICU or postoperative settings: Initially, 0.5-5 mcg/kg/min via continuous IV infusion; adjust dose based on patient's response. Maintenance dose: 1-4 mcg/kg/min. Dosage and treatment recommendations may vary among individual products or between countries (refer to detailed product or local institution treatment guidelines).
Oral Hypertension
Adult: Monotherapy or in combination with other antihypertensive agents (e.g. β-blockers, diuretics): As conventional cap: Initially, 20 mg tid, may be increased at intervals of at least 3 days according to individual response until the required effect is obtained. Usual maintenance dose: 20-40 mg tid. Elderly: Initiate at the lower end of the dosing range.
Oral Chronic stable angina
Adult: Monotherapy or in combination with other antihypertensive agents (e.g. nitrates, β-blockers): As conventional cap: Initially, 20 mg tid, may be increased at intervals of at least 3 days according to individual response until the required effect is obtained. Usual maintenance dose: 20-40 mg tid. Elderly: Initiate at the lower end of the dosing range.
Renal Impairment
Oral:
Dose reduction or extended dosing intervals may be required.
Intravenous:
Initially, 1-5 mg/hour via continuous IV infusion based on patient's blood pressure and clinical condition. Following 30 minutes, dose may be adjusted in steps of 0.5 mg/hour according to patient's response up to a Max of 15 mg/hour. Dosage recommendations may vary among individual products or between countries (refer to detailed product or local institution treatment guidelines).
Hepatic Impairment
Oral:
Dose reduction or extended dosing intervals may be required.
Intravenous:
Initially, 1-5 mg/hour via continuous IV infusion based on patient's blood pressure and clinical condition. Following 30 minutes, dose may be adjusted in steps of 0.5 mg/hour according to patient's response up to a Max of 15 mg/hour. Dosage recommendations may vary among individual products or between countries (refer to detailed product or local institution treatment guidelines).
Administration
regular-release: May be taken with or without food. Avoid grapefruit juice 1 hr before or 2 hr after a dose. extended-release: Should be taken with food. Avoid grapefruit juice 1 hr before or 2 hr after a dose. Avoid taking w/ high fat meals. Swallow whole, do not crush/chew.
Reconstitution
IV: Dilute with NaCl 0.9% or dextrose 5% in water to a concentration of 0.1-0.2 mg/mL. Recommendations for dilution, concentration, and compatible fluids may vary among individual products and between countries (refer to local detailed product guidelines).
Incompatibility
IV: Incompatible with Na bicarbonate and Lactated Ringer's inj.
Contraindications
Clinically significant, advanced or severe aortic stenosis; unstable angina, acute angina attack, cardiogenic shock, acute porphyria; use for secondary prevention of MI, administration during or within 1 month of MI (oral); compensatory hypertension, administration within 8 days after MI (IV).
Special Precautions
Patient with mild to moderate aortic stenosis, CHF, severe left ventricular dysfunction, hypertrophic cardiomyopathy with left ventricular outflow obstruction, stroke (infarction or haemorrhage), reduced hepatic blood flow; pulmonary oedema, portal hypertension, pre-existing elevated intracranial hypertension (IV). Avoid extravasation (IV). Avoid abrupt withdrawal. Renal and hepatic impairment. Neonates, children, and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Increased severity, frequency or duration of angina; tachycardia, MI, increased risk of ischaemic CV events; peripheral oedema, symptomatic hypotension (with or without syncope); worsening of portal vein hypertension and portal-systemic collateral blood flow index (particularly for high IV doses in cirrhotic patients). Blood and lymphatic system disorders: Thrombocytopenia (IV). Cardiac disorders: Palpitation. Ear and labyrinth disorders: Tinnitus. Gastrointestinal disorders: Nausea, vomiting, dyspepsia, dry mouth, abdominal pain. General disorders and administration site conditions: Asthenia; inj site reactions (e.g. pain, phlebitis). Investigations: Abnormal hepatic function. Metabolism and nutrition disorders: Hypokalaemia. Musculoskeletal and connective tissue disorders: Myalgia, arthralgia. Nervous system disorders: Headache, dizziness, drowsiness, paraesthesia. Psychiatric disorders: Insomnia, confusion, depression. Renal and urinary disorders: Abnormal renal function, increased urinary frequency. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Diaphoresis, rash, erythema. Vascular disorders: Flushing, orthostatic hypotension.
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor CV status, including blood pressure, heart rate and rhythm, and ECG changes. Assess for signs and symptoms of heart failure.
Overdosage
Symptoms: Marked hypotension, bradycardia, flushing, palpitations, drowsiness, slurred speech, and confusion. Management: Supportive treatment. Perform gastric lavage and elevate extremities. Administer vasopressors to treat profound hypotension. Consider giving IV Ca gluconate to reverse the effects of Ca entry blockade. Monitor blood pressure frequently, including cardiac and respiratory functions. Position the patient properly to avoid cerebral anoxia.
Drug Interactions
Additive effect leading to postural hypotension with other antihypertensive agents. May result in excessively decreased blood pressure, reduced cardiac function, and exacerbation of heart failure with β-blockers (particularly in patients with CHF). May increase the serum concentrations of ciclosporin, tacrolimus, sirolimus, and digoxin. May increase the plasma levels with CYP3A4 inhibitors (e.g. cimetidine, clarithromycin, erythromycin, ketoconazole, itraconazole, nelfinavir, ritonavir). May decrease the plasma concentrations with CYP3A4 inducers (e.g. carbamazepine, phenobarbital, phenytoin, rifampicin). May enhance the adverse effects with Mg sulfate.
Food Interaction
May increase the serum levels and toxicity with grapefruit juice.
Lab Interference
May result in false-negative aldosterone/renin ratio (ARR).
Action
Description: Mechanism of Action: Nicardipine is a dihydropyridine Ca channel blocker. It inhibits the transmembrane influx of Ca ions from entering the slow channels or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarisation, thereby producing coronary vascular smooth muscle relaxation and coronary vasodilation. In patients with vasospastic angina, it increases oxygen delivery in the myocardium. Onset: Oral: 0.5-2 hours. IV: Within minutes (constant infusion). Duration: ≤8 hours. Pharmacokinetics: Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 35%. Time to peak plasma concentration: 30-120 minutes (conventional cap). Distribution: Enters breast milk. Volume of distribution: 8.3 L/kg. Plasma protein binding: >95%. Metabolism: Extensively metabolised in the liver by CYP3A4, CYP2C8, and CYP2D6; undergoes extensive first-pass metabolism (saturable). Excretion: Via urine (60% as metabolites [oral], 49% as metabolites [IV]; <1% as unchanged drug); faeces (35% [oral], 43% [IV]). Elimination half-life: Oral: 2-4 hours (half-life over the 1st 8 hours); 8.6 hours (terminal half-life). IV: 3 minutes (α-half-life); 45 minutes (β-half-life); 14 hours (γ-half-life).
Chemical Structure
Nicardipine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4474, Nicardipine. https://pubchem.ncbi.nlm.nih.gov/compound/Nicardipine. Accessed June 25, 2024.
Storage
Store between 20-25°C. Protect from light. Protect premixed IV bags from excessive heat and do not freeze.
C08CA04 - nicardipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
References
Anon. Nicardipine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/04/2024.Buckingham R (ed). Nicardipine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2024.Cardene IV Injection, Solution (Baxter Healthcare Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/04/2024.Joint Formulary Committee. Nicardipine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2024.Kenzipine 10 mg/10mL Solution for Injection (Bell-Kenz Pharma, Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 01/04/2024.Nicardiin 1 mg/mL Solution for Infusion (Nano Medic Care Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 01/04/2024.Nicardipine 10 mg/10 mL Solution for Injection (Laboratoire Aguettant). MHRA. https://products.mhra.gov.uk. Accessed 01/04/2024.Nicardipine Hydrochloride 20 mg Capsules (Tillomed Laboratories Ltd). MHRA. https://products.mhra.gov.uk. Accessed 01/04/2024.Nicardipine Hydrochloride Capsule (Epic Pharma, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/04/2024.Nicardipine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 01/04/2024.Nicardipine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/04/2024.Nicardipine. UpToDate Lexidrug, Pediatric and Neonatal Lexi-Drugs Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/04/2024.Paediatric Formulary Committee. Nicardipine Hydrochloride. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 01/04/2024.
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