IntravenousShort-term treatment of hypertensionAdult: 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.
OralHypertensionAdult: 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.
OralAngina pectorisAdult: 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.
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Oral:
Reduced doses or prolonged dose intervals may be required.
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Oral:
Reduced doses or prolonged dose intervals may be required.
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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.
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Intravenous:
Incompatible w/ Na bicarbonate 5%, furosemide, ampicillin/sulbactam, ampicillin, thiopental, cefepime, micafungin, Lactated Ringer's inj.
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Patients w/ advanced aortic stenosis, unstable angina, cardiogenic shock. acute angina attack. Use w/in 1 mth of MI.
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Patients w/ acute cerebral infarction or haemorrhage, CHF, HTN associated w/ phaeochromocytoma, portal HTN. Hepatic and renal impairment. Pregnancy and lactation.
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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.
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BP and heart rate should be monitored carefully esp during initiation of therapy and titration or upward adjustment of dosage.
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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.
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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.
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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.
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Description:
Mechanism of Action: 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.
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Store between 20-25°C. Protect from light.
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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/.
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