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Methylphenidate - Wikipedia, the free encyclopedia. Methylphenidate. Systematic (IUPAC) name. Methyl phenyl(piperidin- 2- yl)acetate. Clinical data. Trade names.
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Ritalin, Concerta, Aptensio, Biphentin, Daytrana, Equasym, Medikinet, Metadate, Methylin, Quillivant. AHFS/Drugs. com. Monograph. Medline. Plusa. 68. License data. Pregnancycategory. AU: B3. US: C (Risk not ruled out)Dependenceliability. Physical: None. Psychological: Moderate. Addictionliability.
Moderate. Routes ofadministration. Oral, insufflation, intravenous, transdermal. Legal status. Legal status. Pharmacokinetic data. Bioavailability~3. The original patent was owned by CIBA, now Novartis Corporation. It was first licensed by the U.
S. Food and Drug Administration (FDA) in 1. Medical use began in 1.
ADHD became more widely accepted. The United States continues to account for more than 8. Methylphenidate acts by blocking the dopamine transporter and norepinephrine transporter, leading to increased concentrations of dopamine and norepinephrine within the synaptic cleft. This effect in turn leads to increased neurotransmission of dopamine and norepinephrine.
Food and Drug Administration (FDA) for the treatment of attention deficit hyperactivity disorder. Methylphenidate is considered effective in increasing wakefulness, vigilance, and performance. It can also improve depression in several groups including stroke, cancer, and HIV- positive patients. He pointed out the logical non sequitur which would result if people were to draw a parallel between the claims of a university that they could . Suppose they further claimed that not only could they achieve this but that their students would be more intelligent and mentally alert than any students in history.
FDA gives methylphenidate a pregnancy category of C, and women are advised to only use the drug if the benefits outweigh the potential risks. In 2. 00. 7, empirical literature included 6. Methylphenidate was ranked 1.
Gastrointestinal adverse effects may include abdominal pain and weight loss. Nervous system adverse effects may include akathisia (agitation/restlessness), irritability, dyskinesia (tics), lethargy (drowsiness/fatigue), and dizziness. Cardiac adverse effects may include palpitations, changes in blood pressure and heart rate (typically mild), and tachycardia (rapid resting heart rate). Ophthalmologic adverse effects may include blurred vision and dry eyes, with less frequent reports of diplopia and mydriasis. Hyperhidrosis (increased sweating) is common. Chest pain is rarely observed.
The Daytrana patch has a much higher rate of dermal reactions than oral methylphenidate. Libido disorders, disorientation, and hallucinations are very rarely reported. Priapism is a very rare adverse event that can be potentially serious. Its effectiveness in treatment of cocaine or psychostimulant addiction or psychological dependence has not been proven and further research is needed. Concomitant administration may require dose adjustments, possibly assisted by monitoring of plasma drug concentrations. The reduced potency of ethylyphenidate and its minor formation means it does not contribute to the pharmacological profile at therapeutic doses and even in overdose cases ethylphenidate concentrations remain negligible.
It is a benzylpiperidine and phenethylaminederivative which also shares part of its basic structure with catecholamines. Methylphenidate is most active at modulating levels of dopamine and to a lesser extent norepinephrine. Specifically, methylphenidate is a dopamine reuptake inhibitor while amphetamine is both a releasing agent and reuptake inhibitor of dopamine and norepinephrine. Each of these drugs has a corresponding effect on norepinephrine which is weaker than its effect on dopamine. Methylphenidate's mechanism of action in the release of dopamine and norepinephrine is fundamentally different from most other phenethylamine derivatives, as methylphenidate is thought to increase general firing rate.
Both the dextrorotary and levorotary enantiomers displayed receptor affinity for the serotonergic 5. HT1. A and 5. HT2.
B subtypes, though direct binding to the serotonin transporter was not observed. The half- life of methylphenidate is 2. The peak plasma time is achieved at about 2 hours. Dextromethylphenidate is selectively metabolized at a slower rate than levomethylphenidate. One pair of threo isomers and one pair of erythro are distinguished, from which only d- threo- methylphenidate exhibits the pharmacologically usually desired effects.
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