Absorption: Highly variable. Protein binding: ~62%. Metabolism: Extensive; Hepatic via CYP3A (major) and 2D6 (minor); intestines. Bioavailability: 76% (compared to solution). Half-life elimination: Ranolazine: Terminal: 7 hours; Metabolites (active and inactive [Yao 2009]): 6 to 22 hours. Time to peak, plasma: 2 to 5 hours. Excretion: Primarily urine (75% mostly as active and inactive metabolites; <5% as unchanged drug); feces (25% mostly as active and inactive metabolites; <5% as unchanged drug).
禁忌症
Hepatic cirrhosis; concurrent use of strong CYP3A inhibitors; concurrent use of CYP3A inducers.
懷孕分類
Adverse events have been observed in animal reproduction studies in doses that also caused maternal toxicity.
哺乳分類
It is not known if ranolazine is present in breast milk. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of exposure to the infant and the benefits of treatment to the mother.
Angina, chronic stable:Initial: 500 mg twice daily; if necessary, may increase to 1,000 mg twice daily based on symptoms; maximum dose: 1,000 mg twice daily.
小兒調整劑量
Nil
腎功能調整劑量
CrCl >30 to 80 mL/minute: No dosage adjustment necessary CrCl ?30 mL/minute:Initial: 500 mg once daily; maximum: 500 mg twice daily
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer’s labeling. Use is contraindicated with hepatic cirrhosis.