Drug Guide

Ritalin and Other Methylphenidates

By Anthony McDaniel, M.D.

Methylphenidate (MPH; Ritalin, Concerta, Metadate, or Methylin) is a psychostimulant drug approved for treatment of attention-deficit hyperactivity disorder, postural orthostatic tachycardia syndrome, and narcolepsy. It may also be prescribed for off-label use in treatment-resistant cases of lethargy, depression, neural insult, obesity, and rarely other psychiatric disorders such as obsessive-compulsive disorder. Methylphenidate belongs to the piperidine class of compounds and increases the levels of dopamine and norepinephrine in the brain through reuptake inhibition of the monoamine transporters. It also increases the release of dopamine and norepinephrine. MPH possesses structural similarities to amphetamine, and, though it is less potent, its pharmacological effects are even more closely related to those of cocaine. MPH is most commonly known by the Novartis trademark name Ritalin, which is an instant-release racemic mixture, although a variety of formulations and generic brand names exist. Other brand names include Ritalina, Rilatine, Attenta, Methylin, Penid, and Rubifen; and the sustained release tablets Concerta, Metadate CD, Methylin ER, Ritalin LA, and Ritalin-SR. Focalin is a preparation containing only dextro-methylphenidate, rather than the usual racemic dextro- and levo-methylphenidate mixture of other formulations. A newer way of taking methylphenidate is by using a transdermal patch (under the brand name Daytrana), similar to those used for nicotine replacement therapy.

Methylphenidate has shown some benefits as a replacement therapy for individuals dependent on methamphetamine. Cocaine and methamphetamine interfere with the protein DAT, over time causing DAT upregulation and lower cytoplasmic dopamine levels in their absence. Methylphenidate and amphetamine have been investigated as a chemical replacement for the treatment of cocaine dependence in the same way that methadone is used as a replacement for heroin. Its effectiveness in treatment of cocaine or other psychostimulant dependence has not been proven and further research is needed. Early research began in 2007–2008in some countrieson the effectiveness of methylphenidate as a substitute agent in refractory cases of cocaine dependence, owing to methylphenidate's longer half life, and reduced vasoconstricive effects. This replacement therapy is used in other classes of drugs such as opiates for maintenance and gradual withdrawal such as methadone, suboxone, etc.

Methylphenidate has high potential for abuse and addiction due to its pharmacological similarity to cocaine and amphetamines. Methylphenidate, like other stimulants, increases dopamine levels in the brain, but at therapeutic doses this increase is slow, and thus euphoria does not typically occur except in rare instances. The abuse potential is increased when methylphenidate is crushed and insufflated (snorted), or when it is injected, producing effects almost identical to cocaine. Cocaine-like effects can also occur with very large doses taken orally. The dose, however, that produces euphoric effects varies between individuals. Methylphenidate is actually more potent than cocaine in its effect on dopamine transporters. Methylphenidate should not be viewed as a weak stimulant as has previously been hypothesized.

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