Nicardipine


Thông tin kê toa tóm tắt
Chỉ định/Công dụng
Listed in Dosage.
Liều dùng/Hướng dẫn sử dụng
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.
Cách dùng
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.
Tương kỵ
Intravenous:
Incompatible w/ Na bicarbonate 5%, furosemide, ampicillin/sulbactam, ampicillin, thiopental, cefepime, micafungin, Lactated Ringer's inj.
Chống chỉ định
Patients w/ advanced aortic stenosis, unstable angina, cardiogenic shock. acute angina attack. Use w/in 1 mth of MI.
Thận trọng
Patients w/ acute cerebral infarction or haemorrhage, CHF, HTN associated w/ phaeochromocytoma, portal HTN. Hepatic and renal impairment. Pregnancy and lactation.
Phản ứng phụ
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.
Quá liều
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.
Tương tác
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.
Tác dụng
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.
Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
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