Abuse Liability

In most people, methylphenidate increases general activity, decreases food intake, produces positive subjective effects (an elevated mood), and can interfere with sleep. With continued use, tolerance can develop to these effects and users will often escalate their doses to achieve the desired effects of their initial doses of methylphenidate. Continued high-dose methylphenidate use can result in toxic consequences similar to those seen after amphetamine use—with ANXIETY, sleeplessness, and even tually a toxic paranoid psychosis. High-dose users often begin with oral methylphenidate use but switch to injecting the drug in order to maximize the effect and achieve the initial "rush" that is typical of intravenous drug abuse. Commercially manufactured methylphenidate pills (the only form available) contain talcum, an insoluble substance, which can cause toxic effects (such as abcesses) when the pills are dissolved in water and injected intravenously or under the skin.

Laboratory animals tested with methylpheni-date show increases in locomotor activity after single doses, increased sensitivity to this effect after repeated doses, and the development of stereotyped repetitive behavior patterns after chronic dosing. In addition, these animals remain more responsive to methylphenidate even after the drug treatment has been discontinued. It has been suggested that the continuous repetition of behavior that characterizes the response to chronic methylphenidate treatment is a good model for the human stimulant psychosis and, as in animals, humans who use high doses become increasingly sensitive to stimulants such as methylphenidate, with psychosis increasingly likely at lower doses after its initial appearance. There are, however, no data to support this hypothesis.

In addition to its action as an appetite suppressant, methlyphenidate has been found to have other therapeutic utility. Like ¿-amphetamine, it has been used successfully in the treatment of ATTENtion-deficit Hyperactivity Disorder (ADHD), a syndrome that first becomes evident during childhood and is characterized by excessive activity and difficulty in maintaining attention. Because of its relatively short half-life, two or three doses of methylphenidate are required each day, although recently a slow-release form of the medication has become available, promising more stable blood levels with only a single daily dosing. Methylphenidate has been shown to alleviate or moderate many of the symptoms of this disorder, although it is not effective in all cases and its long-term efficacy is not well understood.

Side effects of treatment can include insomnia, loss of appetite, and weight loss, all effects of stimulant drugs in general. In addition, concern about the longer lasting effects on learning and cognition in youngsters maintained on this drug for many years has made practitioners cautious and often unwilling to prescribe it. Recent research and prac tice, however, has supported methylphenidate as the stimulant of choice for treating this disorder. As with the amphetamines, methylphenidate is also effective in the treatment of narcolepsy, in which sudden attacks of sleep can occur unexpectedly.


GRILLY, D. M. (1989). Drugs and human behavior.

Needham, MA Allyn & Bacon. KALANT, O.J. (1973). The amphetamines: Toxicity and addiction, 2nd ed. Springfield, IL: Charles C. Thomas.

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