Nicardipine

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: Reduced doses or prolonged dose intervals may be required.
Hepatic impairment: Reduced doses or prolonged dose intervals may be required.

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.
Renal impairment: Reduced doses or prolonged dose intervals may be required.
Hepatic impairment: Reduced doses or prolonged dose intervals may be required.

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.
Incompatibility: Incompatible w/ Na bicarbonate 5%, furosemide, ampicillin/sulbactam, ampicillin, thiopental, cefepime, micafungin, Lactated Ringer's inj.

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.

Patients w/ advanced aortic stenosis, unstable angina, cardiogenic shock. acute angina attack. Use w/in 1 mth of MI.

Patients w/ acute cerebral infarction or haemorrhage, CHF, HTN associated w/ phaeochromocytoma, portal HTN. Hepatic and renal impairment. Pregnancy and lactation. Monitoring Parameters BP and heart rate should be monitored carefully esp during initiation of therapy and titration or upward adjustment of dosage.

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.

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.

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.

Avoid concomitant admin w/ grapefruit juice as it may increase the serum levels and toxicity of nicardipine.

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.
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.

Intravenous: Store between 20-25°C. Protect from light. Oral: Store between 20-25°C. Protect from light.

Anti-Anginal Drugs / Calcium Antagonists

C08CA04 - nicardipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.