Methylphenidate, Serum or Plasma

Methylphenidate is an oral central nervous system stimulant used to treat attention deficit hyperactivity disorders (ADHD) in children and ADD in adults. Methylphenidate is a derivative of phenethylamine, and its CNS actions are similar to the amphetamines. The exact mechanism of action is not fully understood. The drug is rapidly and well absorbed from the GI tract, achieving peak blood levels in 60 to 120 minutes. Some preparations of methylphenidate will exhibit a bimodal plasma concentration-time profile with half-lives varying from 2.5 to 8.4 hours¹ and about 80% of a dose is excreted in the urine in 24 hours. The major metabolite, ritalinic acid (pharmacologically inactive), is formed by hydrolysis of the methyl ester linkage. This takes place enzymatically and nonenzymatically in alkaline conditions during storage of serum or plasma. The use of EDTA as an anticoagulant reduces hydrolytic loss. After a 0.3 mg/kg oral dose of methylphenidate, peak plasma concentrations typically do not go much above 20 ng/mL, but they can reach as high as 70 ng/mL on a higher dose of 0.6 mg/kg. The common side effects of methylphenidate are due mainly to its adrenergic activity, including insomnia, anorexia, headache, and tachycardia.