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Key:DUGOZIWVEXMGBE-UHFFFAOYSA-N Y Methylphenidate, sold under various trade names, Ritalin being one of the most commonly known, is a (CNS) of the and that is used in the treatment of (ADHD) and. The original patent was owned by, now.

It was first licensed by the US (FDA) in 1955 for treating what was then known as hyperactivity. Medical use began in 1960; the drug has become increasingly prescribed since the 1990s, when the of ADHD became more widely accepted. Between 2007 and 2012, methylphenidate prescriptions increased by 50% in the and in 2013 global methylphenidate consumption increased to 2.4 billion doses, a 66% increase from the year before. The continues to account for more than 80% of global consumption. ADHD and other similar conditions are believed to be linked to sub-performance of the and functions in the brain, primarily in the, responsible for (e.g.,,,,,, etc.).

Methylphenidate's involves the inhibition of, primarily as a. Methylphenidate acts by blocking the and, leading to increased of dopamine and norepinephrine within the. This effect in turn leads to increased of dopamine and norepinephrine. Methylphenidate is also a weak. Contents • • • • • • • • • • • • • • • • • • • • • • • • • • • • • • • • Uses [ ] Medical [ ] Methylphenidate is a commonly prescribed and works by increasing the activity of the. It produces such effects as increasing or maintaining alertness, combating, and improving attention. The short-term benefits and of methylphenidate are well established.

Methylphenidate, sold under various trade names, Ritalin being one of the most commonly known, is a central nervous system (CNS) stimulant of.

Methylphenidate is not approved for children under six years of age. Methylphenidate may also be prescribed for in of and. And of (MRI) studies suggest that long-term treatment with ADHD stimulants (specifically, and methylphenidate) decreases abnormalities in structure and function found in subjects with ADHD. Moreover, reviews of clinical stimulant research have established the safety and effectiveness of the long-term use of ADHD stimulants for individuals with ADHD.

In particular, the continuous treatment effectiveness and safety of both amphetamine and methylphenidate have been demonstrated in controlled with durations of several years; however, the precise magnitude of improvements in ADHD symptoms and quality of life that are produced by methylphenidate treatment remains uncertain as of November 2015. Attention deficit hyperactivity disorder [ ] Methylphenidate is approved by the US (FDA) for the treatment of. The addition of (e.g. (CBT)) can have additional benefits on treatment outcome.

The dosage used can vary quite significantly among individuals; consequently, dosage must be precisely. Current models of ADHD suggest that it is associated with functional impairments in some of the brain's, particularly those involving and. Psychostimulants like methylphenidate and amphetamine may be effective in treating ADHD because they increase neurotransmitter activity in these systems.

Approximately 70% of those who use these stimulants see improvements in ADHD symptoms. Children with ADHD who use stimulant medications generally have better relationships with peers and family members, generally perform better in school, are less distractible and impulsive, and have longer. People with ADHD have an increased risk of, and stimulant medications reduce this risk. Some studies suggest that since ADHD diagnosis is increasing significantly around the world, using the drug may cause more harm than good in some populations with ADHD. This applies to people who potentially may be experiencing a different issue and are misdiagnosed with ADHD. People in this category can then experience negative side-effects of the drug which worsen their condition, and make it harder for them to receive adequate care as providers around them may believe the drugs are sufficient and the problem lies with the user.

Narcolepsy [ ], a characterized by overwhelming daytime drowsiness and sudden need for sleep, is treated primarily with stimulants. Methylphenidate is considered effective in increasing wakefulness, vigilance, and performance. Methylphenidate improves measures of on, such as the (MSLT), but performance does not improve to levels comparable to healthy controls.

Other [ ] Methylphenidate may be used in addition to an for. It can also improve depression in several groups including,, and patients. However, the use of stimulants such as methylphenidate in cases of treatment-resistant depression is controversial. Stimulants may have fewer side-effects than in the elderly and medically ill. In individuals with, methylphenidate can be used to counteract -induced somnolence, to increase the effects of opioids, to treat depression, and to improve cognitive function. Methylphenidate and other are also used to improve in the of (OI), a / (ANS) disorder.

Enhancing performance [ ] In 2015, a and a of high quality found that therapeutic doses of and methylphenidate result in modest yet unambiguous improvements in, including,, and, in normal healthy adults; the cognition-enhancing effects of these drugs are known to occur through the of both and in the. Methylphenidate and other ADHD stimulants also improve task and increase arousal.

Stimulants such as amphetamine and methylphenidate can improve performance on difficult and boring tasks and are used by some students as a study and test-taking aid. Based upon studies of self-reported illicit stimulant use, performance-enhancing use, rather than use as a, is the primary reason that students use stimulants. Excessive doses of methylphenidate, above the therapeutic range, can interfere with working memory and. Like amphetamine and, methylphenidate increases stamina and endurance in humans primarily through of dopamine in the central nervous system. Similar to the loss of cognitive enhancement when using large amounts, large doses of methylphenidate can induce that impair athletic performance, such as and. While literature suggests it might improve cognition, most authors agree that using the drug recreationally as a study aid when ADHD diagnosis is not present does not actually improve GPA.

Moreso, it has been suggested that students who use the drug for studying may be self-medicating for potentially deeper underlying issues. Ethics of use for performance enhancement [ ] Methylphenidate is sometimes used by students to enhance their mental abilities, improving their and helping them to study., an expert in, has said that it would be unethical to stop healthy people taking the drug. He pointed out the logical which would result if people were to draw a parallel between the claims of a university that they could 'set out deliberately to improve the mental capacities of its students; suppose its stated aims were to ensure that students left the university more intelligent and learned than when they arrived.

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.' He then asked the rhetorical question of whether, 'if the claims could be sustained, should we be pleased?' He argues that it would be 'not rational' and against human enhancement to not use the drug to improve people's cognitive abilities. Has argued that the use of Ritalin in this way may give students an unfair advantage in examinations and that as a result universities may want to discuss making students give to be tested for the drug. Contraindications [ ] Methylphenidate is for individuals using (e.g., and ), or individuals with agitation,, or, or a to any ingredients contained in methylphenidate pharmaceuticals. The US FDA gives methylphenidate a of C, and women are advised to only use the drug if the benefits outweigh the potential risks.

Not enough animal and human studies have been conducted to conclusively demonstrate an effect of methylphenidate on. In 2007, literature included 63 cases of exposure to methylphenidate across three. Adverse effects [ ]. Addiction experts in psychiatry, chemistry, pharmacology,, epidemiology, and the police and legal services engaged in regarding 20 popular recreational drugs. Methylphenidate was ranked 13th in dependence, 12th in physical harm, and 18th in social harm. Methylphenidate is generally well tolerated.

The most commonly observed adverse effects with a frequency greater than include,,,, and. Adverse effects may include and.

Nervous system adverse effects may include (agitation/restlessness),, (tics), (drowsiness/fatigue), and. Adverse effects may include, changes in and (typically mild), (rapid resting heart rate), and (reduced blood flow to the hands and feet). Adverse effects may include and dry eyes, with less frequent reports of and. Other adverse effects may include,,, and.

(increased sweating) is common. Is rarely observed.

There is some evidence of mild reductions in growth rate with prolonged treatment in children, but no causal relationship has been established and reductions do not appear to persist long-term. (including,, and ) is sometimes reported. The patch has a much higher rate of reactions than oral methylphenidate. Methylphenidate can worsen in psychotic patients, and in very rare cases it has been associated with the emergence of new psychotic symptoms. It should be used with extreme caution in patients with due to the potential induction of. There have been very rare reports of, but evidence does not support a link. Is occasionally reported.

Disorders,, and are very rarely reported. Is a very rare adverse event that can be potentially serious. USFDA-commissioned studies from 2011 indicate that in children, young adults, and adults there is no association between serious adverse (,, and ) and the medical use of methylphenidate or other ADHD stimulants. Because some adverse effects may only emerge during chronic use of methylphenidate, a constant watch for adverse effects is recommended. Overdose [ ] The symptoms of a moderate acute overdose on methylphenidate primarily arise from overstimulation; these symptoms include:,,,, muscle twitching,, confusion, hallucinations,,, sweating,, headache,,,,,, and dryness of. A severe overdose may involve symptoms such as,,,, (a repetitive movement disorder),,, and. A methylphenidate overdose is rarely fatal with appropriate care.

Severe toxic reactions involving and have been reported following injection of methylphenidate tablets into an. Treatment of a methylphenidate overdose typically involves the application of, with, agonists, and serving as second-line therapies. Addiction and dependence.

Top: this depicts the initial effects of high dose exposure to an addictive drug on in the for various Fos family proteins (i.e.,,,,, and ). Bottom: this illustrates the progressive increase in ΔFosB expression in the nucleus accumbens following repeated twice daily drug binges, where these (35–37 ) ΔFosB persist in the of the nucleus accumbens for up to 2 months. Pharmacological texts describe methylphenidate as a stimulant with effects, addiction liability, and dependence liability similar to, a compound with moderate liability among; accordingly, and are possible and likely when methylphenidate is used at high doses as a recreational drug.

When used above the medical dose range, stimulants are associated with the development of. As with all addictive drugs, the overexpression of in in the is implicated in methylphenidate addiction. Methylphenidate has shown some benefits as a replacement therapy for individuals who are addicted to and dependent upon. Methylphenidate and have been investigated as a chemical replacement for the treatment of in the same way that is used as a replacement drug for upon. Its effectiveness in treatment of cocaine or psychostimulant addiction or psychological dependence has not been proven and further research is needed.

Biomolecular mechanisms. For more details on this topic, see. Methylphenidate has the potential to induce due to its effect (i.e., ) in the brain's. At therapeutic doses, ADHD stimulants do not sufficiently activate the reward system, or the in particular, to the extent necessary to cause persistent increases in in the of the; consequently, when taken as directed in doses that are commonly prescribed for the treatment of ADHD, methylphenidate use lacks the capacity to cause an. However, when methylphenidate is used at sufficiently high recreational doses through a bioavailable (e.g., or ), particularly for use of the drug as a, ΔFosB accumulates in the. Hence, like any other addictive drug, regular recreational use of methylphenidate at high doses eventually gives rise to ΔFosB overexpression in D1-type neurons which subsequently triggers a series of -mediated that induce an addiction. Interactions [ ] Methylphenidate may inhibit the metabolism of, certain, and some antidepressants ( and ).

May require dose adjustments, possibly assisted by monitoring of drug concentrations. There are several case reports of methylphenidate inducing with concomitant administration of antidepressants. When methylphenidate is coingested with, a metabolite called is formed via, not unlike the hepatic formation of from.

The reduced potency of ethylphenidate 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. Coingestion of alcohol (ethanol) also increases the blood plasma levels of d-methylphenidate by up to 40%. From methylphenidate is extremely rare, but limited evidence suggests that intake of with methylphenidate may increase the risk of liver toxicity. Pharmacology [ ] Pharmacodynamics [ ] Binding profile Measure (units) dl-MPH d-MPH l-MPH () 121 161 2250 ( nM) K i (nM) 788 206 >10000 IC 50 (nM) 51 39 980 K i (nM) >10000 >10000 >6700 IC 50 (nM) — >10000 >10000 Measure (units) dl-MPH d-MPH l-MPH () 5000 3400 >10000 ( nM) >10000 K i (nM) >>10000 IC 50 (nM) >>10000 Methylphenidate primarily acts as a (NDRI). It is a and which also shares part of its basic structure with.

Methylphenidate is most active at modulating levels of (DA) and to a lesser extent. Methylphenidate binds to and blocks (DAT) and. Variability exists between DAT blockade, and extracellular dopamine, leading to the hypothesis that methylphenidate amplifies dopamine activity, leading to nonresponse in those with low basal DA activity. On average, methylphenidate elicits a 3–4 times increase in dopamine and norepinephrine in the and. Both and methylphenidate are predominantly drugs, yet their are distinct. Methylphenidate acts as a while amphetamine is both a and of dopamine and norepinephrine.

Methylphenidate's mechanism of action in the release of dopamine and norepinephrine is fundamentally different from most other, as methylphenidate is thought to increase neuronal, whereas reduces firing rate, but causes monoamine release by reversing the flow of the through via a diverse set of mechanisms, including activation and modulation of function, among other mechanisms. The difference in mechanism of action between methylphenidate and amphetamine results in methylphenidate inhibiting amphetamine's effects on monoamine transporters when they are co-administered. Map Of India Download Pdf. Methylphenidate has both and binding affinity, with the displaying a prominent affinity for the. Both the and enantiomers displayed for the 5HT 1A and 5HT 2B subtypes, though direct binding to the was not observed. A later study confirmed the d-threo- enantiomer binding to the 5HT 1A receptor, but no significant activity on the 5HT 2B receptor was found.

Methylphenidate may protect neurons from the neurotoxic effects of and abuse. The hypothesized mechanism of neuroprotection is through inhibition of methamphetamine/DAT interactions, and through reducing cytosolic dopamine, leading to decreased production of dopamine related. The are significantly more potent than the enantiomers, and some medications therefore only contain.

Methylphenidate has been identified as a agonist in. Pharmacokinetics [ ]. Further information: Methylphenidate taken orally has a of 11–52% with a duration of peak action around 2–4 hours for instant release (i.e.

Ritalin), 3–8 hours for (i.e. Ritalin SR), and 8–12 hours for extended release (i.e.

The of methylphenidate is 2–3 hours, depending on the individual. The peak plasma time is achieved at about 2 hours. Dextromethylphenidate is much more bioavailable than levomethylphenidate when administered orally, and is primarily responsible for the psychoactivity of methylphenidate. Contrary to the expectation, taking methylphenidate with a meal speeds. Methylphenidate is into. Dextromethylphenidate is selectively metabolized at a slower rate than levomethylphenidate. Chemistry [ ].

See also: Four of methylphenidate are possible, since the molecule has two. One pair of isomers and one pair of erythro are distinguished, from which primarily exhibits the pharmacologically desired effects. The erythro are amines, a property not shared with the threo diastereomers.

When the drug was first introduced it was sold as a 4:1 mixture of erythro:threo diastereomers, but it was later reformulated to contain only the threo diastereomers. 'TMP' refers to a threo product that does not contain any erythro diastereomers, i.e. Since the threo isomers are energetically favored, it is easy to out any of the undesired erythro isomers. The drug that contains only methylphenidate is sometimes called d-TMP, although this name is only rarely used and it is much more commonly referred to as, d-MPH, or d-threo-methylphenidate. A review on the synthesis of pure (2 R,2' R)-(+)- threo-methylphenidate hydrochloride has been published. German 'Ritalin' brand methylphenidate Methylphenidate is produced in the,,,,, and.

It is also sold in,, the,,,,,,,, and several other European countries (although in much lower volumes than in the United States). Brand names for methylphenidate include Ritalin, Concerta, Aptensio, Biphentin, Daytrana, Equasym, Medikinet, Metadate, Methylin, and Quillivant. Generic forms are produced by numerous pharmaceutical companies throughout the world. In Belgium the product is sold under the name Rilatine and in Brazil, Portugal and Argentina as Ritalina.

In Thailand, it is found under the name Hynidate. In India, it is found under the names Addwize and Inspiral SR. [ ] Available forms [ ]. Clockwise from top: Concerta 18 mg, Medikinet 5 mg, Methylphenidat TAD 10 mg, Ritalin 10 mg, Medikinet XL 30 mg. Methylphenidate is available in numerous forms, a doctor will determine the appropriate formulation of the drug to prescribe based on the patient's history, the doctor's experiences treating other patients with methylphenidate products, and product pricing/availability. Currently available forms include a variety of tablets and capsules, an adhesive-based matrix transdermal system (transdermal patch), and an oral suspension (liquid syrup).

The of methylphenidate, known as, is sold as a generic and under the brand names Focalin and Attenade in both an immediate-release and an extended-release form. In some circumstances it may be prescribed instead of methylphenidate, however it has no significant advantages over methylphenidate at equipotent dosages and so it is sometimes considered to be an example of an drug. Immediate-release [ ] Methylphenidate was originally available as an immediate-release formulation under the trademark name Ritalin, although a variety of generics are now available, some under other brand names. Generic brand names include Ritalina, Rilatine, Attenta, Medikinet, Metadate, Methylin, Penid, Tranquilyn, and Rubifen.

• • • US generic manufactured by; CA generics manufactured by and. • Manufactured. • Manufactured by,, and. • Manufactured by and.

• Manufactured. • Manufactured. • US generics manufactured by County Line Pharmaceuticals and Abhai; CA generic manufactured. Concerta tablets are marked with the letters 'ALZA' and followed by: '18', '27', '36', or '54', relating to the mg dosage strength. Approximately 22% of the dose is immediate release, and the remaining 78% of the dose is released over 10–12 hours post ingestion, with an initial increase over the first 6 to 7 hours, and subsequent decline in released drug. Ritalin LA capsules are marked with the letters 'NVR' (abbrev.: Novartis) and followed by: 'R20', 'R30', or 'R40', depending on the (mg) dosage strength. Ritalin LA provides two standard doses – half the total dose being released immediately and the other half released four hours later.

In total, each capsule is effective for about eight hours. Metadate CD capsules contain two types of beads; 30% are immediate release, and the other 70% are evenly sustained release.

Quillivant XR is an extended-release oral suspension (after reconstitution with water): 25 mg per 5 mL (5 mg per mL). It was designed and is patented and made.

The medication comes in various sizes from 60ml to 180ml (after reconstitution). Each bottle is shipped with the medication in powder form containing roughly 20% instant-release and 80% extended-release methylphenidate, to which water must be added by the pharmacist in an amount corresponding with the total intended volume of the bottle. The bottle must be shaken vigorously for ten seconds prior to administration via included oral syringe to ensure proper ratio. Ritalin 10 mg tablet Generic immediate-release methylphenidate is relatively inexpensive. The average wholesale cost is about US$0.15 per ( normally charge more).

However, the most expensive brand-name extended-release tablets may retail for as much as $12.40 per defined daily dose. There are two main reasons for this price difference: • Generic formulations are less expensive than brand-name formulations. • Immediate-release tablets are less expensive than 8-hour extended-release tablets, which are much less expensive than 12-hour extended-release tablets. History, society, and culture [ ] Methylphenidate was first in 1944, and was identified as a stimulant in 1954. Methylphenidate was synthesized by Ciba (now ) chemist Leandro Panizzon. He named the drug after his wife, nicknamed Rita, who used Ritalin to compensate for low blood pressure. Originally it was marketed as a mixture of two racemates, 80% (±)-erythro and 20% (±)-threo.

Subsequent studies of the racemates showed that the central stimulant activity is associated with the threo racemate and were focused on the separation and interconversion of the erythro isomer into the more active threo isomer. Methylphenidate was first used to allay -induced coma, narcolepsy and depression. It was later used to treat memory deficits in the elderly. Beginning in the 1960s, it was used to treat children with or, known at the time as hyperactivity or minimal brain dysfunction (MBD) based on earlier work starting with the studies by American on the use of psychostimulant drugs, such as, with then called 'maladjusted children'. Production and prescription of methylphenidate rose significantly in the 1990s, especially in the, as the ADHD diagnosis came to be better understood and more generally accepted within the medical and mental health communities. In 2000 received US (FDA) approval to market 'Concerta', an extended-release form of methylphenidate.

See the section of this article, above, for more information about Concerta. Legal status [ ]. Legal warning printed on Ritalin packaging • Internationally, methylphenidate is a Schedule II drug under the.

• In the, methylphenidate is classified as a, the designation used for substances that have a recognized medical value but present a high potential for abuse. • In the, methylphenidate is a controlled 'Class B' substance. Possession without prescription carries a sentence up to 5 years or an unlimited fine, or both; supplying methylphenidate is 14 years or an unlimited fine, or both. • In, methylphenidate is listed in Schedule I of the and is illegal to possess without a prescription, with unlawful possession punishable by up to three years imprisonment, or (via ) by up to one year imprisonment and/or fines of up to two thousand dollars. Unlawful possession for the purpose of trafficking is punishable by up to ten years imprisonment, or (via summary conviction) by up to eighteen months imprisonment. • In, methylphenidate is a 'class B2 controlled substance'.

Unlawful possession is punishable by six-month prison sentence and distribution by a 14-year sentence. • In, methylphenidate is a 'Schedule 8' controlled substance. Such drugs must be kept in a lockable safe until dispensed and possession without prescription is punishable by fines and imprisonment.

• In, methylphenidate is a List II controlled substance with recognized medical value. Possession without a prescription is punishable by up to three years in prison. • In, methylphenidate is covered by the 'narcotics' schedule, prescription and distribution conditions are restricted with hospital-only prescription for the initial treatment and yearly consultations.

• In, methylphenidate is a drug and is controlled by the Drugs and Cosmetics Rule, 1945. It is dispensed only by physician's prescription.

Legally, 2 grams of methylphenidate are classified as a small quantity, and 50 grams as a large or commercial quantity. Controversy [ ]. Main article: Methylphenidate has been the subject of controversy in relation to its use in the treatment of ADHD. The prescription of medication to children to reduce ADHD symptoms has been a major point of criticism. [ ] The contention that methylphenidate acts as a has been discredited by multiple sources, according to which abuse is statistically very low and 'stimulant therapy in childhood does not increase the risk for subsequent drug and alcohol abuse disorders later in life'.

A study found that ADHD medication was not associated with increased risk of cigarette use, and in fact stimulant treatments such as Ritalin seemed to lower this risk. One of the highest use of methylphenidate medication is in Iceland [ ] where research shows that the drug was the most commonly abused substance among. The study involved 108 IV substance abusers and 88% of them had injected methylphenidate within the last 30 days and for 63% of them, methylphenidate was the most preferred substance.

Treatment of ADHD by way of methylphenidate has led to legal actions, including suits regarding, inadequate information on,, and coercive use of medications. In the US and the UK, it is approved for use in children and adolescents. In the US, the approved the use of methylphenidate in 2008 for use in treating. In the UK, while not licensed for use in adult ADHD, guidelines suggest it be prescribed off-license for the condition. Methylphenidate has been approved for adult use in the treatment of.

Fps Creator X9 Model Pack 53 Download Youtube. Research [ ] Methylphenidate may have benefit as a treatment of in patients with Alzheimer's disease. See also [ ] • • • • • • • • Notes [ ].

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