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QuickView for Methylphenidate (compound)


PubChem
Name: Methylphenidate
PubChem Compound ID: 10199290
Description: A central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE.
Molecular formula: C14H20ClNO2
Molecular weight: 269.767 g/mol
DrugBank
Identification
Name: Methylphenidate
Name (isomeric): DB00422
Drug Type: small molecule
Description: A central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE.
Synonyms:
Methylphenidate HCl; Methylphenidylacetate hydrochloride; d-methylphenidate HCl; Metilfenidato [INN-Spanish]; Methylphenidatum [INN-Latin]; Metilfenidato [Italian]; Methylphenidate hydrochloride; Methyl phenidyl acetate; Phenidylate; Metilfenidat hydrochloride
Brand: Centredin, PMS-Methylphenidate, Ritalin-SR, Ritcher Works, Methylin, Calocain, Methylin ER, Methylofenidan, Centedrin, 4311/B Ciba, Methylphenidan, Focalin XR, Ritaline, Focalin, Plimasine, Metadate, Methypatch, Ritalin hydrochloride, Metadate CD, Riphenidate, Centedrine, Ritalin, Metadate ER, Methylphen, Meridil, Ritalin LA, Ritalin SR, Concerta, Daytrana, Centedein
Category: Dopamine Uptake Inhibitors, Adrenergic Agents, Sympathomimetics, Adrenergic Uptake Inhibitors, Central Nervous System Stimulants
CAS number: 113-45-1
Pharmacology
Indication: For use as an integral part of a total treatment program which typically includes other remedial measures (psychological, educational, social) for a stabilizing effect in children with a behavioral syndrome characterized by the following group of developmentally inappropriate symptoms: moderate-to-severe distractibility, short attention span, hyperactivity, emotional lability, and impulsivity.
Pharmacology: Methylphenidate is a central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of dextroamphetamine.
Mechanism of Action:
Methylphenidate blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins. Methylphenidate acts at the brain stem arousal system and the cerebral cortex and causes increased sympathomimetic activity in the central nervous system. Alteration of serotonergic pathways via changes in dopamine transport may ...
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Absorption: Readily absorbed in a biphasic manner. It reaches peak absorption at approximately two hours for the first phase and five hours for the second phase. Bioavailability is low (approximately 30%)
Protein binding: Low (approximately 15%)
Biotransformation: Hepatic, methylphenidate is metabolized primarily by de-esterification to ritalinic acid (α-phenyl-2-piperidine acetic acid, PPAA), which has little to no pharmacologic activity.
Half Life: 2.4 hours in children and 2.1 hours in adults
Toxicity: Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes. LD50=190mg/kg (orally in mice)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Take on empty stomach: 1 hour before or 2 hours after meals.
Avoid excessive quantities of coffee or tea (Caffeine).
Drug interaction:
GuanethidineMethylphenidate may decrease the effect of guanethidine.
CyclosporineMethylphenidate increases the effect and toxicity of cyclosporine
TrandolaprilMethylphenidate may antagonize the antihypertensive effect of Trandolapril. Monitor for changes in blood pressure if Methylphenidate is initiated, discontinued or dose changed.
RasagilinePossible hypertensive crisis with this combination.
CarbamazepineCarbamazepine may decrease the effect of methylphendiate.
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Enzymes