Introduction
Methylphenidate, a central nervous system stimulant (CNS), has emerged as the top medication for treating attention deficit hyperactivity disorder (ADHD) in children. It has also been used to treat patients with human immunodeficiency virus (HIV) infection and with depression, brain injury, cancer, pain, and cognitive impairments. The most notable result, though, has been a decrease in the symptoms of ADHD, a disorder that affects between three to five percent of school-age children overall and is more common in males. The therapeutic properties of Methylphenidate can help many children, adolescents, and adults with ADHD while having few side effects. The most frequent adverse effects are anorexia (loss of appetite), sleeplessness, and headache. When these side effects arise throughout therapy, they are typically manageable or gradually become less severe than tolerable levels. When taken as directed, this stimulant drug is generally safe; when taken orally in therapeutic amounts, it rarely causes significant side reactions. However, when it is misused, the therapeutic profile shifts.
The amount of Methylphenidate prescribed and dispensed will continue to rise as ADHD is more precisely identified and treated effectively with stimulant medicine. As a result, there is a higher chance that this medication will be abused, given the rising number of patients receiving Methylphenidate and the greater accessibility of this drug. Large doses, administered intravenously or intranasally, are frequently used abusively. The pharmacology of Methylphenidate will be discussed in this article, along with its psychiatric adverse effects when misused. To make the primary care physician better aware of potential issues while monitoring and supervising Methylphenidate, patterns of abuse, particularly intranasal use, will also be covered.
What Are the Pharmacological Effects of Methylphenidate?
Methylphenidate acts by facilitating the release of dopamine in the brain. This release is incidental to how it affects the dopamine transport system, which causes a rise in postsynaptic dopamine levels. This increase gives the orbital-frontal-limbic axis the necessary stimulus and is thought to activate the inhibitory motor system. Increased inhibition of impulsiveness is the effect of this stimulation. Therefore, by assisting them to focus their attention when it's needed, this medicine benefits kids with ADHD.
Although Methylphenidate's precise mechanism of action differs from cocaine and amphetamines, the overall result is an increase in synaptic dopamine. According to radiographic investigations using (11C)-labeled cocaine and Methylphenidate, both drugs bind to the striatum in the same part of the brain. The pleasure and frequent usage of Methylphenidate are believed to be related to the stimulation of D1 dopamine receptors in the frontal cortex and striatum-orbitofrontal cortex.
How Is the Dosage Division of Methylphenidate Done?
While there are several dosage considerations for children, adults typically take 20 to 30 mg of Methylphenidate daily. Most texts advise against exceeding 60 mg daily, while certain people could need more. This 60 mg/day cap seems arbitrary and is not supported by clinical evidence. According to studies, the recommended dose for individuals with ADHD is 1 mg/kg/day, with lesser quantities having a lessening effect. The therapeutic oral dose is what is meant by these amounts.
The effects of abusing Methylphenidate intranasally typically resemble those of abusing amphetamines and crack cocaine intranasally. Abuse of intranasal Methylphenidate has been associated with doses as high as 200 mg. Abuse-related reports of intravenous dosages vary from 40 mg to 1000 mg.
What Is the Abuse Potential of Methylphenidate Toxicity?
Research emphasizes the possibility of abuse, which should serve as a warning to doctors. However, this caution is sometimes overlooked by many patients who use oral Methylphenidate for medicinal purposes and do not abuse it. Methylphenidate exerts cocaine-like actions on receptors when administered intranasally. A sudden release of synaptic dopamine results in subjective feelings of immediate "high" and extreme gratification. As a result, the clinical picture of abuse and cocaine are frequently reasonably similar. It has been discovered that the location of Methylphenidate binding with dopaminergic pathways was "same" as that of cocaine, and patients receiving both medicines intravenously described feeling similarly "high."
As one of the most rewarding and reinforcing drugs, cocaine, claims like "subjective effects similar to cocaine are produced by Amphetamine, Dextroamphetamine, Methamphetamine, Phenmetrazine, Methylphenidate, and Diethylpropion" can help healthcare professionals assess the abuse potential of Methylphenidate. When taken in excess and administered intravenously or intranasally, Methylphenidate can change from a medicinal agent to a drug that is misused and addictive.
The likelihood that a drug will be abused is frequently directly correlated with its accessibility, and Methylphenidate is becoming more accessible than ever. The Drug Enforcement Agency (DEA) reports that from 1985 to 1995, there was a six-fold increase in the manufacture of Methylphenidate in one of the northern countries, from 1361 kilograms to 10,410 kilograms. Additionally, throughout this period, the number of kids with ADHD has grown by 2.5. Methylphenidate is currently under the DEA's regulation because it has been given schedule II status, indicating a high risk of abuse and a severe risk of physical and psychological dependence.
What Are the Adverse Health Effects of Methylphenidate?
The following are the adverse health effects:
Acute Toxicity:
Symptoms of acute Methylphenidate toxicity are similar to acute amphetamine intoxication. There have been reports of euphoria, delirium, disorientation, toxic psychosis, and hallucinations, among other mental symptoms. As Methylphenidate's pharmacologic actions are "essentially the same as those of amphetamines," such symptoms shouldn't be anticipated. Methylphenidate misuse has been linked to cases of psychosis when the substance is used in "runs," much like amphetamine abuse.
Not much information is available about the adverse psychological effects of Methylphenidate abuse. Most of the data is obtained in case reports and is frequently described as comparable to the psychological side effects of cocaine or amphetamine use. The clinical picture of Methylphenidate's side effects is similar to amphetamine intoxication and psychosis. When Methylphenidate is abused, psychiatric signs of intense rage and threats of aggressive conduct may develop. High doses have been linked to psychosis, aggression, panic attacks, and hallucinations.
Stimulant Toxicity:
Methylphenidate usage leads to toxicity comparable to other CNS stimulant overdoses. Numerous symptoms, including schizophrenia symptoms, manic-like states, psychoses, depressions (particularly during withdrawal), and multiple anxiety conditions, including panic states, are part of the clinical picture of stimulant intoxication. In addition, bruxism, repetitive touching or stereotypical bewilderment, disorientation, punding, obsessive-compulsive tendencies, aggression, and repetitive actions are examples of motor and behavioral overdose symptoms.
Hallucinations, delusions, psychosis, confusion, disorientation, and lose of associations of ideas are some psychiatric signs of stimulant overdose. Methylphenidate's psychiatric side effects are highly comparable to those of cocaine and amphetamines, adding credence to the notion that nearly all CNS stimulants will result in a similar clinical picture.
Conclusion
The practitioner, the patient's parents, and the patient must all take responsibility for preventing Methylphenidate abuse. In addition, the abuse potential of Methylphenidate must be clear to all treated patients.
