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Methylphenidate

Attention-deficit/hyperactivity disorder (ADHD), is associatedwith functional, and structural brain changes.

Trade name Ritalin.

Compared to healthy controls, adolescents with ADHD have lower gray matter volume in the caudate nucleus and poorer working memory function, and thinner medial temporal cortex bilaterally.

Methylphenidate is a benzylpiperidine derivative that improves working memory, episodic memory, and inhibitory control, aspects of attention, and planning latency in healthy people.

Cortex thickness is associated with hyperactivity symptoms.

Therapeutic doses of stimulants diminish the differences in brain structure between patients with ADHD and healthy persons.

The authors speculate that this normalization of brain structure is a possible basis for the clinical effects of ADHD medications.

The effects of methylphenidate in ADHD are not always positive as an increase of dopamine transporter availability in the brain of such patients may decrease treatment efficacy and exacerbate symptoms when the medication is not used.

Methylphenidate may improve task saliency and performance of tedious tasks.

At above optimal doses, methylphenidate effects decreases learning.

A psychostimulant with a structure similar to amphetamine, differing in that it has a piperidine ring attached, making it lipid soluble.

Methylphenidate may affect brain restructuring and be altered by the age of the patient indicating methylphenidate affects adult and adolescent brains differently.

Works by inhibiting uptake of dopamine and norepinephrine, and to a lesser extent serotonin.

Inhibition of dopamine reuptake increases the level of dopamine in many areas of the brain, resulting in increased alertness.

May be associated with sudden deaths (Gould MS).

May improve symptoms of Parkinson’s disease.

Most methylphenidate prescriptions are written for children and adolescents, and adults with ADHD.

A psychostimulant with a structure similar to that of amphetamine.

It differs from amphetamine in that it is lipid-soluble.

The d isomer of methylphenidate is the primary isomer that interferes with the uptake of these neurotransmitters.

This inhibition of dopamine reuptake increases the level of dopamine in many areas of the brain, resulting in increased alertness.

Therapeutic effects are due in part to its ability to enhance the magnitude of dopamine induced by stimuli that by themselves would generate weak responses.

Methylphenidate-induced increases in dopamine improves attention and decreases distractibility.

Dopamine modulates motivation, and increases in dopamine result in increased cognitive performance by enhancing the salience of the task.

Methylphenidate may improve task saliency and performance on tedious tasks.

In older medically ill patients and terminally ill patients it has a quick onset of action, good tolerance among the elderly, and their value in enhancing opioid analgesia while countering opioid fatigue and serving as an appetite stimulant.

Used in the setting of poststroke depression and recovery, as it is safe and effective in this setting, with improvements in mood, ability to conduct activities of daily living, and motor functioning with no increase in adverse effects.

Improves gait function in older adults, especially in complex dual tasks that required higher executive control.

In PD gait speed, stride time variability, and measures of fall risk are significantly improved.

Improves gait hypokinesia and freezing patients with advanced PD who were receiving subthalamic nucleus stimulation.

In both in medically ill and poststroke patients with depression and for older patients with PD and/or gait disorders, improves mobility.

In terminal ill cancer patients it diminishes depression and/or fatigue, palliating common symptoms.

FDA warnings for psychostimulant medications regarding reports of serious cardiovascular events―including sudden death, stroke, and myocardial infarction.

However, a retrospective population-based cohort study of 150,359 stimulant users aged 25 through 64 years, was not associated with an increased risk of cardiovascular events.

In another study that also employed matched controls, found a 1.8-fold increase in the risk of sudden death or ventricular arrhythmia among 43,999 new users of methylphenidate, but it did not indicate a causal relationship because of a lack of dose-response relationship.

At low doses (1.25-5 mg), methylphenidate can be used safely in medically ill, depressed patients, including those of very advanced age.

Evidence exists that its use among individuals in their 70s and older for ADHD, depression, and the prevention of falls.

The relative safety of methylphenidate, particularly at low doses, has been demonstrated in elderly patients.

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