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| Methylphenidate Hydrochloride
| | #REDIRECT [[Methylphenidate]] |
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| Methylphenidate hydrochloride is a central nervous system (CNS) stimulant primarily used in the treatment of attention deficit hyperactivity disorder ([[Attention Deficit Hyperactivity Disorder|ADHD]]) and narcolepsy. It is a prescription medication that affects chemicals in the brain and nerves that contribute to hyperactivity and impulse control.
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| ==Pharmacology==
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| Methylphenidate hydrochloride works by inhibiting the reuptake of dopamine and norepinephrine, two neurotransmitters in the brain. This action increases the concentration of these neurotransmitters in the synaptic cleft, thereby enhancing neurotransmission and improving attention and focus.
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| ===Mechanism of Action===
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| Methylphenidate binds to the dopamine transporter (DAT) and norepinephrine transporter (NET), blocking the reuptake of these neurotransmitters into the presynaptic neuron. This blockade results in increased levels of dopamine and norepinephrine in the synaptic cleft, which enhances neurotransmission and improves symptoms of ADHD.
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| ===Pharmacokinetics===
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| Methylphenidate is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 1 to 2 hours after oral administration. It is metabolized primarily by de-esterification to ritalinic acid, which has little to no pharmacologic activity. The half-life of methylphenidate is approximately 2 to 3 hours, necessitating multiple doses throughout the day for sustained therapeutic effect.
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| ==Clinical Uses==
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| Methylphenidate hydrochloride is primarily indicated for the treatment of ADHD in children and adults. It is also used to treat narcolepsy, a sleep disorder characterized by excessive daytime sleepiness and sudden sleep attacks.
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| ===ADHD===
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| In patients with ADHD, methylphenidate improves attention, concentration, and impulse control. It is often part of a comprehensive treatment plan that includes psychological, educational, and social measures.
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| ===Narcolepsy===
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| For narcolepsy, methylphenidate helps to reduce excessive daytime sleepiness and improve wakefulness.
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| ==Side Effects==
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| Common side effects of methylphenidate hydrochloride include insomnia, decreased appetite, weight loss, and increased heart rate. More serious side effects can include hypertension, psychiatric symptoms such as hallucinations, and potential for abuse and dependence.
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| ==Contraindications==
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| Methylphenidate is contraindicated in patients with marked anxiety, tension, and agitation, as well as those with glaucoma, tics, or a family history of Tourette syndrome. It should not be used in patients currently taking monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping such treatment.
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| ==Regulation and Abuse Potential==
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| Methylphenidate is classified as a Schedule II controlled substance in the United States due to its potential for abuse and dependence. It is important for prescribers to monitor patients for signs of misuse, abuse, and addiction. | |
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| ==Also see==
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| * [[Attention Deficit Hyperactivity Disorder]]
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| * [[Narcolepsy]]
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| * [[Central Nervous System Stimulant]]
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| * [[Dopamine]]
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| * [[Norepinephrine]]
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| {{Drugbox
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| | Verifiedfields = changed
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| | verifiedrevid = 477002146
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| | IUPAC_name = Methyl 2-phenyl-2-(piperidin-2-yl)acetate hydrochloride
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| | image = Methylphenidate.svg
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| | width = 200
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| | image2 = Methylphenidate-3D-balls.png
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| | width2 = 200
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| | tradename = Ritalin, Concerta, others
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| | Drugs.com =
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| | MedlinePlus = a682188
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| | pregnancy_AU = B3
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| | pregnancy_US = C
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| | legal_AU = S8
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| | legal_CA = Schedule III
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| | legal_UK = Class B
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| | legal_US = Schedule II
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| | legal_UN =
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| | routes_of_administration = Oral, transdermal
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| | bioavailability = 11–52%
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| | protein_bound = 10–33%
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| | metabolism = Liver (de-esterification)
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| | elimination_half-life = 2–3 hours
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| | excretion = Urine (90%)
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| | CAS_number = 298-59-9
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| | ATC_prefix = N06
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| | ATC_suffix = BA04
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| | PubChem = 4158
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| | DrugBank = DB00422
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| | ChemSpiderID = 4015
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| | UNII = 207ZZ9QZ49
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| | KEGG = D08143
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| | ChEBI = 6887
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| | ChEMBL = 731
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| | C = 14
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| | H = 19
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| | Cl = 1
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| | N = 1
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| | O = 2
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| | smiles = CN1CCCC1C(C(=O)OC)c2ccccc2
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| | StdInChI = 1S/C14H19NO2/c1-17-14(16)13(11-7-4-2-5-8-11)12-9-6-10-15-12/h2,4-5,7-8,12-13H,6,9-10H2,1H3
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| | StdInChIKey = DUGOZIWVEXMGBE-UHFFFAOYSA-N
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| }}
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| [[Category:Stimulants]]
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| [[Category:ADHD medications]]
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| [[Category:Narcolepsy treatments]]
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| [[Category:Controlled substances]]
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