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Methylphenidate

More commonly known as Ritalin, Methylphenidate is a mild form of amphetamine used in treating ADHD in children, teens and adults. In correct doses, it calms the physical energy and focuses the mind. The exact mode of action is unknown but is assumed to be that the drug reduces visible symptoms by inhibiting the neurotransmitter activity in the brain.

This drug is used for conditions that require intervention for normal function:

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  • Attention-deficit disorder
  • Attention-deficit hyperactivity disorder
  • Narcolepsy
  • Treatment-resistant depression
  • Appetite suppressant
  • Antidepressant augmentation

Methylphenidate is contraindicated when antidepressants are used since it will increase the plasma concentrations of these medications. Toxic reactions have resulted in cardiovascular effects in some patients. MAO Inhibitors, such as Phenelzine or Tranylcypromine will interact with it. Patients with arrhythmia, hypertension or liver damage should never take this drug.

Side Effects from Methylphenidate

Patients have reported experiencing side effects that differ widely. Any experience of these side effects should be reported to the attending physician immediately:

  • Heart arrhythmia
  • Increased blood pressure
  • Appetite loss
  • Blurred vision
  • Nausea/vomiting
  • Abdominal pain
  • Muscle twitches
  • Insomnia
  • Drowsiness
  • Dizziness
  • Headache
  • Abnormal thoughts
  • Hallucinations
  • Nervousness
  • Euphoria
  • Increased respiration rate
  • Fever

Methylphenidate Availability

As a prescription-strength stimulant, Methylphenidate is a controlled substance that is to be administered under the specific direction of a qualified physician. Children dealing with ADD, or ADHD, have performed better in school when appropriate doses were administered at the right time of day for each child. Physicians have discovered that symptoms from narcolepsy and chronic fatigue syndrome are diminished when the drug is taken during the day. Cancer patients have experienced less fatigue when including Methylphenidate in the drug regimen during chemotherapy. Close monitoring allows the physician to determine if dosage changes would provide relief for the patient without side effects.

History of Methylphenidate

In 1954, CIBA pharmaceutical company, or Novartis, patented Methylphenidate as the potential cure for Mohr’s disease. Starting in the 1960s, doctors found it effective in treating ADHD, which was called hyperactivity or minimal brain dysfunction, or MBD. Today, it is the most widely prescribed treatment for ADHD around the globe. In the 1990s, production of the medication increased significantly in the United States are more children were helped through the prescription and administration of the drug.

Ritalin is the brand-name under which Methylphenidate is produced in the U.S., Mexico, Pakistan, Argentina and European countries. In the European Union, it is used much less frequently.

In 2000, an extended-release form was created, which is called Concerta, was released. Research demonstrated that the long-acting versions were helpful for some patients since effects were sustained throughout more hours of the day.

In 2006, a transdermal patch form, called Daytrana, was approved for the treatment of ADHD. Sustained presence of the drug allows the patient to focus on important tasks that require concentration.

Methylphenidate Benefits

At the proper dosage, this medicine acts as a central nervous system stimulant. Patients report a reduction in impulsive behavior and the ability to concentrate on work and other tasks. Adults feel that use of Methylphenidate allows them to organize their busy lives.

In comparison to dextroamphetamine, it has fewer side effects. Most patients tolerate this drug well at the doses that provide enough control without feeling over-medicated.

Methylphenidate Mode of Action

Researchers have yet to discover the exact means through which Methylphenidate affects patients who are diagnosed with ADHD. Many theories have surfaced about the causes of ADHD. The most common theory is that a dopamine imbalance in the brain causes the condition. As a dopamine reuptake inhibitor, it is a norephinephrine, which increases the dopamine neurotransmitter level in the brain:

  • The properties of the drug partially block the dopamine transporter that would remove dopamine from the synapses.
  • In addition, it stimulates the release of norepinephrine and dopamine into the synapse.
  • Thirdly, it increases the magnitude of the dopamine release after the stimulus, which increases the salience of the stimulus.
  • These stimulants will not work paradoxically but stimulate the underactive portions of the brain.
  • Dopamine and norepinephrine production in the striatum and prefrontal cortex increase when the drug is present.

Another theory states that the medicine affects the actions and effects of serotonin in the brain.

Criticism for Methylphenidate

Many professional educators and medical experts have expressed concerns over the frequency with which Methylphenidate is prescribed for the treatment of ADHD. Side effects cause concern for parents who were unaware that the young body will react to doses of the drug that are too high. In some circles of influence, concerns about illicit drug use have been discussed. People have questioned if use of Methylphenidate will lead to substance abuse later in life. No decisions have been made about the connection.

Methylphenidate Abuse Potential

In comparison to other stimulants, Methylphenidate is abused at much lower rates. Higher doses of Methylphenidate can have similar effectives as D-amphetamine or cocaine. These drugs act as a reinforcer and substitute fully in the drug discrimination experiments. Defining the abuse rates is challenging since researchers were challenged with defining abuse and misuse, validity of abuse liability assays and pharmacokinetic factors.

Methylphenidate and Liver Toxicity

Early clinical trials did not reveal elevations of serum aminotransferase or hepatic injury. After Methylphenidate was marketed, reports of enzyme elevations were noted and reported to the drug manufacturer. Mild to moderate elevations were not associated with jaundice or other symptoms. Given intravenously, Methylphenidate causes marked serum enzyme elevations and acute liver injury. Illicit use of Methylphenidate taken intravenously in patients with chronic hepatitis C has resulted in liver damage was hepatocellular. Acute hepatic necrosis occurred with rapid onset and rapid recovery.

Response to Liver Injury

Oral use of Methylphenidate does not result in chronic liver injury or vanishing bile duct syndrome. Drug interactions with amphetamine-related chemicals has not been demonstrated. Liver damage, which is measured through enzyme elevations, can occur but will disappear when the drug is no longer taken. Enzyme elevations recur if the patient begins to take Methylphenidate again.

In cases where Methylphenidate does not help the patient, new pharmacological agents have been introduced. Adderall and Dexedrine are used widely in place of Methylphenidate. Older psychostimulants, such as Cylert and Nitan, were used until concerns were raised about hepatotoxicity.

A new non-stimulant drug, Strattera, was developed as a selective noradrenaline reuptake inhibitor that shows promise as a therapeutic option for youngsters with ADHD.

Does Methylphenidate Increase Risk of Drug Abuse?

Brain-imaging studies on animals are being conducted to look for trends that would link ADHD treatment and drug abuse in teens. Parents have raised concerns with the family physician about the use of Methylphenidate to treat a child from an early age. Other studies have shown that the age in which medications were started could affect the frequency of drug abuse.

Studies performed on rates revealed elevated dopamine D2 receptor levels after eight months of treatments with Methylphenidate. More dopamine D2 receptors in the brain have been associated with not abusing drugs later. Lower levels of these receptors leave the patient open to drug abuse later in the teen years. Age plays an important role in the ways in which ADHD treatments affect the brain’s development.

Summary of Findings

Methylphenidate is a helpful drug in the treatment of ADHD, chronic fatigue syndrome, narcolepsy and other conditions. Patients must seek assistance from an experienced physician to find the proper dose for desired results. Over medication can cause side effects to be pronounced and dangerous. Drug interactions can be avoided when the prescribing doctor is aware of all medications the patient takes. Adults and children must be willing to talk with the physician while adjustments are being made in the dosage. Noticing the best time of day to take the drug allows the doctor to make helpful adjustments.

Like all medications, Methylphenidate is not to be used by anyone without a prescription. Misuse of the drug has caused extreme liver damage and even death. If you or someone you know is misusing Methylphenidate, call now to learn more about the dangers and how we can help you.

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