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Nicardipine is an antihypertension from calcium channel blocker (Dihydropyridine

calcium channel blocker)


Mechanism of Action
Calcium-channel blocker (dihydropyridine), inhibits transmembrane
influx of extracellular calcium ions across membranes of myocardial
cells and vascular smooth muscle cells without changing serum
calcium concentrations; this inhibits cardiac and vascular smooth
muscle contraction, thereby dilating main coronary and systemic
arteries
Produces vasodilation and decreases peripheral resistance
Absorption
Bioavailability: 35%
Onset: PO, 0.5-2 hr; IV, 10-20 min
Duration: Immediate release and IV, 8 hr; extended release, 8-12 hr
Peak plasma time: Immediate release, 0.5-2 hr; extended release, 2-4 hr
Metabolism
Metabolized in liver by CYP3A4 (first pass)
Metabolites: Pyridine analogue (inactive)
Elimination
Half-life: 2-4 hr
Dialyzable: HD, no
Total plasma clearance: IV, 0.3-0.9 L/hr/kg; PO, 1.62-7.86 L/hr/kg
Excretion: Urine (60%), feces (35%)
Adverse Effects

>10% Headache (IV; 15%)


1-10% Flushing (6-10%), Peripheral edema (PO; 6-8%), Pedal edema (PO;
6.8%), Headache (PO; 6.3%), Hypotension (IV; 6%), Exacerbation of angina
(6%), Asthenia (PO; 3%), Nausea (PO; 1.6%), Ventricular extrasystoles (IV;

1%), Dizziness (1%), Rash (PO; 1%), Polyuria (IV; 1%)


<1% (selected) Asthenia (IV), Facial edema, Hypotension (PO), Myalgia
(PO), Syncope (IV), Tachycardia

Contraindications

Hypersensitivity to nicardipine or other calcium-channel blockers


Advanced aortic stenosis

Cautions

May cause symptomatic hypotension or tachycardia, titrate slowly to avoid


systemic hypotension and possible negative inotropic effects with congestive
heart failure (CHF), angina, and left ventricular dysfunction (particularly
during treatment initiation, after dose increase, or after withdrawal of beta

blocker)
Peripheral edema may occur
Exacerbation of angina or MI reported with dosage titration of

dihydropyridine calcium-channel blockers


With acute cerebral infarction or hemorrhage, titrate slowly to avoid systemic

hypotension
Use with caution in patients with hypertrophic cardiomyopathy and mild-to-

moderate aortic stenosis


Use with caution in hepatic or renal impairment, lower doses may be required
IV: Use with caution in hypertension associated with pheochromocytoma and

portal hypertension
Change infusion site every 12 hours
BP starts to fall within minutes of infusion
Extended-release form not recommended for angina

Nicardipine Formula
Dose 5- 15 mg/h IV
Contoh: sediaan 10 mg/amp
kandungan dala5m 1 amp = 5 cc = 10 mg
Cara pemberian: Sediaan nicardipine 1 ampul (10 mg) dilarutkan dalam 50 ml
dextrose/ NaCl sehingga 50 ml= 10 mg (setelah dilarutkan)

Jika dosis yang diinginkan


5mg/ jam : 50 ml x 5 mg/jam = 25 mg/jam = 0,4 ml/menit
10 mg

10mg/ jam : 50 ml x 10 mg/jam = 50 mg/jam = 0,8 ml/menit


10 mg
15mg/ jam : 50 ml x 15 mg/jam = 75 mg/jam = 1,2 ml/menit
10 mg
Theraputic Guidline ASA 2010

Pada pasien stroke perdarahan intraserebral akut (AHA/ ASA,Class Iib, Level
of eevidence C), apabila TDS>200 mmHg atau Mean Arterial Pressure (MAP)
>150 mmHg, tekanan darah diturunkan dengan menggunakan obat
antihipertensi intravena secara kontinu dengan pemantauan tekanan darah

setiap 5 menit.
Pada pasien stroke perdarahan intraserebral dengan TDS 150- 220 mmHg,
penurunan tekanan darah dengan cepat hingga TDS 140 mm cukup aman
(AHA/ASA, Class Iia, Level of evidence B).

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