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Ritalin Pharmacology, Pharmacokinetics, Studies, Metabolism - Methylphenidate Hcl

Ritalin Pharmacology, Pharmacokinetics, Studies, Metabolism - Methylphenidate Hcl

CLINICAL PHARMACOLOGY

Ritalin is a mild central nervous system stimulant.

The mode of action in man is not completely understood, but Ritalin presumably activates the brain stem arousal system and cortex to produce its stimulant effect.

There is neither specific evidence which clearly establishes the mechanism whereby Ritalin produces its mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system.

Ritalin in the SR tablets is more slowly but as extensively absorbed as in the regular tablets. Relative bioavailability of the SR tablet compared to the Ritalin tablet, measured by the urinary excretion of Ritalin major metabolite (a-phenyl-2-piperidine acetic acid) was 105% (49%-168%) in children and 101% (85%-152%) in adults. The time to peak rate in children was 4.7 hours (1.3-8.2 hours) for the SR tablets and 1.9 hours (0.3-4.4 hours) for the tablets. An average of 67% of SR tablet dose was excreted in children as compared to 86% in adults.

In a clinical study involving adult subjects who received SR tablets, plasma concentrations of Ritalin’s major metabolite appeared to be greater in females than in males. No gender differences were observed for Ritalin plasma concentration in the same subjects.

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