NIFEdipine, a slow-calcium channel antagonist, selectively inhibits the transmembrane influx of calcium ions into cardiac muscle and vascular smooth muscle that is dependent upon for the contractile process. The mechanism by which it relieves angina remains undetermined but it is thought to be related to the relaxation and prevention of coronary artery spasm and reduction of myocardial oxygen demand. As an antihypertensive agent, NIFEdipine is a peripheral vasodilator causing arterial vasodilation, producing a reduction in peripheral vascular resistance.
藥動學
Absorption:
Bioavailability, Oral, extended-release tablets: complete
Metabolism:
Liver, primary site, substrate of CYP3A4
Excretion:
Renal: approximately 80% changed; less than 0.1% unchanged,Feces: 20%
Dialyzable: No (hemodialysis); No (peritoneal dialysis)
Elimination Half Life: approximately 2 hours
禁忌症
cardiogenic shock
concomitant use of strong CYP450 inducers, including rifampin
hypersensitivity to NIFEdipine or any component of the tablet
懷孕分類
C(FDA) (AUS)
哺乳分類
Maternal medication usually compatible with breastfeeding(AAP).
Compatible with breastfeeding(WHO).
Infant risk is minimal(MDX).
副作用
Common:
Cardiovascular: Hypotension (up to 5% ), Palpitations (up to 7% ), Peripheral edema (7% to 29% )
Dermatologic: Flushing (4% to 25%)
Gastrointestinal: Nausea (up to 10% )
Neurologic: Dizziness (4% to 10% ), Headache (19% to 23%)
Psychiatric: Feeling nervous
Respiratory: Cough, Dyspnea
Serious:
Cardiovascular: Myocardial infarction (up to 4% ), Ventricular arrhythmia (less than 0.5% )
Gastrointestinal: Gastrointestinal obstruction, Gastrointestinal ulcer
Hematologic: Aplastic anemia
劑量和給藥方法
30 or 60 mg orally once daily,generally titrate over 7 to 14 days; MAX 120 mg/day
小兒調整劑量
Hypertension:Initial 0.25 to 0.5 mg/kg orally per day in single or 2 divided doses; MAX 3 mg/kg/day or 120 mg/day, whichever is less (guideline dosage)
Hypertrophic cardiomyopathy:0.6-0.9 mg/kg/24hr ORALLY divided into 3-4 doses