Nicardipine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO HTN Immediate-release: Initial: 20 mg tid, increase at intervals of at least 3 days. Maintenance: 20-40 mg tid. Sustained-release: Initial: 30 mg bid. Max: 60 mg bid. Angina pectoris Immediate-release: Initial: 20 mg tid, increase at intervals of at least 3 days. Maintenance: 60-120 mg/day. IV Short-term treatment of HTN Initial: 3-5 mg/hr via slow infusion. Max: 15 mg/hr. Reduce to 3 mg/hr after response is achieved.
Dosage Details
Intravenous
Short-term treatment of hypertension
Adult: Initially, 3-5 mg/hour via continuous infusion over 15 minutes, may be adjusted according to blood pressure in increments of 0.5-2.5 mg/hour every 15 minutes; once desired blood pressure is achieved may reduce to maintenance rate: 2-4 mg/hour. Max: 15 mg/hour.

Oral
Hypertension
Adult: Immediate-release: Initially, 20 mg tid, may be increased at intervals of at least 3 days until required effect is achieved. Maintenance: 20-40 mg tid. Sustained-release: Initially, 30 mg bid, increased up to 60 mg bid.

Oral
Angina pectoris
Adult: Immediate-release: Initially, 20 mg tid, may be increased at intervals of at least 3 days until required effect is achieved. Maintenance: 60-120 mg/day.
Renal Impairment
Oral:
Reduced doses or prolonged dose intervals may be required.
Hepatic Impairment
Oral:
Reduced doses or prolonged dose intervals may be required.
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.
Incompatibility
Intravenous:
Incompatible w/ Na bicarbonate 5%, furosemide, ampicillin/sulbactam, ampicillin, thiopental, cefepime, micafungin, Lactated Ringer's inj.
Contraindications
Patients w/ advanced aortic stenosis, unstable angina, cardiogenic shock. acute angina attack. Use w/in 1 mth of MI.
Special Precautions
Patients w/ acute cerebral infarction or haemorrhage, CHF, HTN associated w/ phaeochromocytoma, portal HTN. Hepatic and renal impairment. Pregnancy and lactation.
Adverse Reactions
Pedal oedema, tachycardia, hypotension, abnormal ECG, palpitations, flushing, headache, asthenia, dizziness, paraesthesia, somnolence, myalgia, nausea, vomiting, constipation, dyspepsia, dry mouth, rash, polyuria, dyspnoea, hypokalaemia, increased urinary frequency, haematuria, nocturia.
IV/Parenteral/PO: C
MonitoringParameters
BP and heart rate should be monitored carefully esp during initiation of therapy and titration or upward adjustment of dosage.
Overdosage
Symptoms: Hypotension, bradycardia, palpitations, flushing, drowsiness, confusion, slurred speech. Management: Symptomatic and supportive treatment. For profound hypotension, vasopressors may be used. IV Ca gluconate may reverse the effects of Ca entry blockade.
Drug Interactions
Concomitant use w/ β-blockers may precipitate or worsen heart failure. May alter serum levels w/ CYP3A4 inducers (e.g. carbamazepine, rifampicin) or inhibitors (e.g. cimetidine). May increase serum levels of ciclosporin, tacrolimus, sirolimus and digoxin.
Food Interaction
Avoid concomitant admin w/ grapefruit juice as it may increase the serum levels and toxicity of nicardipine. Reduced levels w/ St John's wort. Alcohol may increase CNS depression.
Action
Description: Nicardipine is a dihydropyridine Ca channel blocker. It inhibits Ca ion from entering the slow channels or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarisation, producing a relaxation of coronary vascular smooth muscle and coronary vasodilatation. It also increases myocardial oxygen delivery in patients w/ vasospastic angina.
Onset: Oral: 0.5-2 hr. IV: 10 min.
Duration: Immediate-release cap: ≤8 hr. Sustained-release cap: 8-12 hr. IV: ≤8 hr.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the GI tract. Bioavailability: Approx 35%. Time to peak plasma concentration: Immediate-release cap: 30-120 min; sustained-release cap: 60-240 min.
Distribution: Plasma protein binding: >95%.
Metabolism: Undergoes hepatic metabolism via CYP3A4 isoenzyme. Saturable extensive first-pass effect.
Excretion: Via urine and faeces mainly as inactive metabolites. Terminal half-life: Approx 8.6 hr.
Storage
Store between 20-25°C. Protect from light.
MIMS Class
References
Anon. Nicardipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/01/2014.

Buckingham R (ed). Nicardipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/01/2014.

Cardene Premixed Injection (Astellas Pharma Ltd.). U.S. FDA. https://www.fda.gov/.

McEvoy GK, Snow EK, Miller J et al (eds). Nicardipine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 08/01/2014.

Nicardipine Hydrochloride Injection (Sandoz Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/.

Disclaimer: This information is independently developed by MIMS based on Nicardipine 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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