Methylphenidate is a piperidine-derivative CNS stimulant that has pharmacologic actions that are qualitatively similar to those of amphetamines.
藥動學
Methylphenidate hydrochloride appears to be well absorbed from the GI tract; however, oral bioavailability of the drug is low (about 30%; range: 10–52%), which suggests substantial first-pass metabolism. It is about 10–33% bound to plasma proteins. Methylphenidate is metabolized primarily by de-esterification by carboxylesterase 1A1 to form α-phenylpiperidine acetic acid (ritalinic acid), which has little or no pharmacologic activity. Approximately 50, 80, and 95% of the dose was recovered as metabolites in urine within 6, 24, and 90 hours, respectively. The mean terminal elimination half-life was reported to be 3.5 or 2.5 hours, respectively.
禁忌症
Marked anxiety, tension, agitation and glucoma.
懷孕分類
C
哺乳分類
Adverse effects on the breast-fed infant or on milk production have not been reported to date; however, any long-term neurodevelopmental effects are unknown.
1. Adults: 20-30mg/daily/30-45 min TID AC 2. Children (6 years and over): Start with 5mg BID (before breakfast and lunch) with gradual increments of 5-10mg weekly, up to 60mg/daily. If no improvement after 1 month, discontinue therapy.