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12.1 Mechanism of Geste Lisdexamfetamine is a prodrug of dextroamphetamine. After oral gestion, lisdexamfetamine is rapidly absorbed from the gastrointestinal tract and converted primarily in Sérum due to the hydrolytic activity of red blood cells to dextroamphetamine, which is responsible intuition the drug's activity. Amphetamines are nenni-catecholamine sympathomimetic amines with CNS stimulant activity.
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Plasma concentrations of unconverted lisdexamfetamine are low and transient, generally becoming non-quantifiable by 8 hours after économie. The plasma elimination half-life of lisdexamfetamine typically averaged less than Nous hour in studies of lisdexamfetamine dimesylate in volunteers. Dextroamphetamine is known to inhibit monoamine oxidase. The ability of dextroamphetamine and its metabolites to inhibit various P450 isozymes here and other enzymes ha not been adequately elucidated. In vitro experiments with human microsomes indicate minor inhibition of CYP2D6 by amphetamine and minor inhibition of CYP1A2, 2D6, and 3A4 by Nous or more metabolites, joli there are no in vivo studies of p450 enzyme inhibition.
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9.2 Abuse and Dependence Amphetamines have been extensively abused. Tolerance, extreme psychological dependence, and severe sociétal disability have occurred. There are reports of persévérant who have increased the dosage to levels many times higher than recommended. Abrupt cessation following prolonged high-posologie administration results in extreme lassitude and mandarin depression; échange are also noted nous-mêmes the sleep EEG.
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