Riluzole is a glutamate antagonist. Riluzole has been reported to confer a survival benefit to the subgroup of patients with bulbar-onset amyotrophic lateral sclerosis.
藥理
Glutamate Inhibitor. The efficacy of riluzole in amyotrophic lateral sclerosis remains unclear.
藥動學
Absorption: High-fat meal decreases AUC by 20% and peak blood levels by 45%. Protein binding, plasma: 96%, primarily to albumin and lipoproteins Distribution: Vd ~3.4 L/kg Metabolism: Hepatic via CYP1A2 and UGT-HP4 Bioavailability: Oral ~60% Half-life elimination: 12 hours Excretion: Urine (90%; 2% as unchanged drug) and feces (5%)
禁忌症
Hypersensitivity to riluzole
懷孕分類
C
哺乳分類
No human data available to assess risk of infant harm or effects on milk production; caution advised while breastfeeding.
副作用
asthenia, elevation of serum transaminases, worsening of spasticity, gastrointestinal symptoms, and blood pressure elevations.
劑量和給藥方法
Amyotrophic lateral sclerosis: 50 mg PO BID
小兒調整劑量
腎功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.