METHYLPHENIDATE

OFFICIAL NAMES: Methylphenidate, Ritalin, Methylin, Metadate, Concerta

STREET NAMES: Vitamin R, West Coast

DRUG CLASSIFICATIONS: Schedule II, stimulant

OVERVIEW

Methylphenidate (MPH), one of the most commonly prescribed psychoactive drugs in the United States, is the drug of choice for the treatment of attention deficit hyperactivity disorder (ADHD) in children, adolescents, and adults. It is also a drug of choice for thieves: MPH is on the U.S. Department of Justice's Drug Enforcement Administration's (DEA) list of the top 10 prescription drugs most often stolen.

According to The Christian Science Monitor, legal use of MPH in the 1990s increased by about 700% between 1990 and 2000. However, as the legal usage of MPH increased, so did its abuse. That abuse is well documented among high school and college students who use it to overcome fatigue and to enhance memory, without realizing the drug's dangers.

Children with ADHD are inattentive, impulsive, and hyperactive. The areas of their brains that control attention and restraint do not function properly. Stimulant drugs, specifically amphetamines, have been used in the United States to treat children with inattention and hyperactivity disorders since the 1930s. MPH was also discovered to have a calming effect on hyperactive children and a "focusing" effect on those with attention deficit disorder (ADD). However, it was not until the 1960s that the U.S. Food and Drug Administration (FDA) approved methylphenidate for the treatment of ADHD. At the turn of the twenty-first century, approximately 90% of all methylphenidate was prescribed for ADHD children. Most of the rest was prescribed to treat adults with a sleeping sickness known as narcolepsy.

Estimates suggest that 6–7% of all American school-age children were being prescribed MPH for behavior problems in 2002. Although the exact amount of MPH abuse is unknown, experts agree its prevalence is low compared to cocaine abuse, but warn that the number of new cases of methylphenidate abuse is growing. In 2001, Terrace Woodworth, DEA deputy director, told the U.S. Congress that the problem of MPH abuse is primarily a U.S. problem. The United States is the primary consumer of methylphenidate, producing and consuming about 85% of the entire world's supply.

Unlike other amphetamine stimulants, MPH has not been clandestinely manufactured in homemade laboratories. According to the DEA, legally manufactured MPH has been diverted for illegal, non-prescription use. Police authorities report rising rates of illegal sales, prescription forgery, scams involving doctor shopping, and outright thefts of the drug. In a one-year period from 1996 to 1997, the DEA reports that 700,000 pills were stolen.

CHEMICAL/ORGANIC COMPOSITION

Methylphenidate, a derivative of piperidine, a synthetic chemical that is used in the manufacture of rubber, is structurally similar to amphetamine and cocaine. These three drugs are all central nervous system stimulants that act on a chemical within the human body known as dopamine, one of the substances within the human body that controls feelings of pleasure.

Unlike cocaine and amphetamine, however, MPH does not cause feelings of pleasure in the brains of individuals with ADHD. However, when healthy people unaffected by ADHD take methylphenidate illicitly, they get, at least initially, a sharp signal reception that the brain interprets as pleasure. Unfortunately, people without ADHD soon develop a tolerance to the drug and need increasing amounts of the drug to achieve the same effect, often leading to methylphenidate abuse.

INGESTION METHODS

MPH is most often taken in pill form. It is available in prescribed quantities of 5-, 10-, and 20-mg tablets. A sustained or delayed release 20-mg tablet is also available. In 2001, the FDA approved Concerta, a longer acting MPH tablet that is taken once a day. Besides its long lasting action, Concerta has another benefit: Abusers sometimes grind MPH tablets into a powder and snort it up their noses, but Concerta is formulated so that it cannot be ground into a powder. According to the DEA, methylphenidate abusers also dissolve the immediate-release MPH tablets in water and then inject the mixture.

THERAPEUTIC USE

Besides attention deficit hyperactivity disorder (ADHD), methylphenidate is used to treat narcolepsy, a sleeping disorder. Occasionally, MPH has also been used to treat behavioral symptoms that result from traumatic brain injury (TBI), stroke, depression, and the pain experienced by people with cancer. Combined with pain relievers, MPH tends to produce significant reductions in pain intensity and sedation in cancer patients.

Individuals with narcolepsy suffer sudden onsets of deep sleep. Regular use of MPH on a twice-a-day dosage schedule (or a once-a-day schedule if the newer sustained release forms of MPH are used) allows those individuals to live relatively normal lives.

Individuals with TBI, which usually is caused by a blow to the head, a fall, or a car accident, often exhibit ADHD-like symptoms. MPH is sometimes used to treat those symptoms. Before the development of modern antidepressants, MPH was sometimes used for the treatment of depression. Any benefits seen in TBI treatment appear to be related to an improvement in symptoms of depression.

However, by far the largest group of users of methylphenidate are people who have ADHD. Children with ADHD often exhibit symptoms such as inattention, distractibility, impulsiveness, and hyperactivity. These symptoms interfere with the patient's ability to learn. MPH is used to modify brain chemistry and allows the individuals to better focus on tasks such as homework.

One unpredictable benefit of MPH treatment, according to a 1999 research paper, is that children with ADHD who receive MPH treatment may be less likely to develop substance abuse disorders.

USAGE TRENDS

While the prevalence of MPH abuse is low, at least compared to other forms of drug abuse, officials worry that the rate of MPH abuse is increasing, especially among high school and college students.

Scope and severity

In 1999, methylphenidate was the most widely dispensed stimulant medication used for treating ADHD. More of it was used than amphetamine, the next most frequently used stimulant that is used to treat ADHD.

Yearly, an estimated four to six million children in the United States take MPH on a daily basis as a treatment for ADHD. In comparison, only about 25,000 school-age youths were on the medication in England and Wales during 2000. Definitive statistics are not available for the drug's illegal use, and so the exact extent to which it is being abused in any country is unknown. However, it is known that abuse rates increase along with the number of legal prescriptions written. In a study of MPH abusers over a four-year period of 1992–1996, researchers found a significant increase in methylphenidate misuse, especially in white adolescents.

According to a 2001 published survey of cases reported to poison control centers, there was a sevenfold increase in the number of cases in which MPH was involved during the five-year period that ended in 1999. However, the total number of cases making up the sevenfold increase totaled only 530.

In 1990, there were 271 emergency room mentions for MPH in reports to the Drug Abuse Warning Network (DAWN). In 1999, that figure had grown to 1,478 mentions, but the good news is that the 1999 figure represented a slight decrease from 1998's all-time high of 1,728 mentions. To put those figures into context, in 1998 there were 168,763 cocaine-related visits to hospital emergency rooms.

Age, ethnic, and gender trends

According to the Woodworth congressional testimony, "Boys are four times more likely to receive a diagnosis of ADHD and be prescribed stimulant medication." Critics are also disturbed about a trend of prescribing the drug to ever-younger children. For instance, in 1998 a national auditing firm estimated that 4,000 MPH prescriptions were written for children two years of age or less. Some experts, disturbed by this disquieting statistic, point out that MPH has not been approved for use in children under six years of age because safety and effectiveness in that age range has not been established.

MENTAL EFFECTS

Methylphenidate is considered a mild central nervous system stimulant that affects the brain and nerves, relieving fatigue, and inducing clearer thoughts for relatively short periods. According to the DEA, possible effects experienced by those who do not have ADHD or narcolepsy include increased alertness, excitation, and euphoria. Increased energy and increased mental clarity may be experienced for a short period.

PHYSIOLOGICAL EFFECTS

Physiological effects include increased pulse rate and blood pressure, which contribute to the feelings of increased energy and stamina.

Harmful side effects

Common harmful side effects include insomnia, nervousness, and loss of appetite. Other adverse reactions include skin rash, fever, anorexia, nausea, dizziness, headache, abdominal pain, irregular heartbeat and breathing, and generalized anxiety. The irregular breathing may come from an allergic reaction to the drug. The allergic reaction can also cause swelling of the lips, tongue, face, or throat.

Individuals who ingest methylphenidate by dissolving the tablets in water and injecting the mixture risk complications due to the insoluble fillers used in the tablets. When injected, these materials block small blood vessels and can cause serious damage to the lungs and retina of the eye.

Snorting the drug can also be dangerous. The delicate tissues that line the nasal cavities and air passages can be damaged by direct contact with MPH because the tablets contain hydrocholoride salt of methylphenidate, which yields dilute hydrochloric acid when it comes into contact with moisture within the nose. While this is not a problem in the stomach (because hydrochloric acid is one of the stomach acids used to digest foods), the acid can burn the delicate epithelial nasal tissues. This can result in open sores, nose bleeds, and with chronic use can lead to deterioration of the nasal cartilage.

"Shooting up," street parlance for dissolving the drug in water and using a syringe to inject it, can cause harmful side effects. Not only can dust, dirt, and other contaminants fall into the liquid mixture, but bacteria, talc, lint, and other particles are also injected with the drug. The inert ingredients that manufacturers include to increase the bulk of the tablets can create serious health problems when injected directly into veins or body tissues. Complications from injections include overdose, blood clots, infections such as blood poisoning, abscesses, hepatitis, AIDS from sharing needles, scars, and circulatory and pulmonary problems. The effects of overdose include agitation, increased body temperature, hallucinations, paranoia, convulsions, and possibly even death.

The FDA classifies methylphenidate as being in pregnancy category C, which means it is not known whether it would harm an unborn baby. Medical authorities advise pregnant women not to take MPH without consulting a doctor.

Other side effects of MPH include allergic reactions, extensive bruising, and abnormally low red and white blood cells counts. Individuals who abuse the drug suffer from loss of appetite so severe that they develop anorexia. They can also suffer abdominal pain, extreme weight loss, and skin rashes.

Long-term health effects

Chronic abuse of MPH can lead to marked tolerance and psychological dependence. According to the DEA, chronic MPH intoxication is identical to the paranoid psychosis of amphetamine intoxication. Studies indicate that 5–15% of the amphetamine users who become psychotic fail to make a complete recovery.

REACTIONS WITH OTHER DRUGS OR SUBSTANCES

Because of the dangerous adverse reactions (including the risk of death), individuals should not take methylphenidate if they have taken a class of drugs known as monamine oxidase (MAO) inhibitors within 14 days. Most MAO inhibitors are antidepressants, but some anti-tuberculosis drugs such as Ethambutol also have MAO effects. Since drug users are prone to many infectious diseases, it is not unheard of for drug abusers to come down with tuberculosis (TB).

TREATMENT AND REHABILITATION

Withdrawal from methylphenidate abuse can be both difficult and dangerous. Medical reference books warn that MPH withdrawal should be undertaken with careful supervision by slowly reducing dosages over time.

Individuals who go through MPH withdrawal experience intense cravings for the drug. Other expected unpleasant withdrawal side effects include agitation, anxiety, decreased energy, fatigue, increased appetite, lethargy, increased need for sleep, and vivid or unpleasant dreams. During withdrawal, individuals may also experience abdominal pain, fever, infection, loss of appetite, diarrhea, shortness of breath, nausea, vomiting, dizziness, emotional upset, insomnia, nervousness, and weight loss. MPH withdrawal can also cause depression and suicidal feelings. Psychosis and paranoia, though rare, can also be precipitated.

A review of the medical literature reveals no specific treatments or rehabilitation regimes for MPH withdrawal. However, drug rehabilitation organizations can help individuals go through MPH withdrawal.

PERSONAL AND SOCIAL CONSEQUENCES

Like its chemical cousins cocaine and amphetamine, MPH abuse can lead to tolerance and psychic dependence. Tolerance develops when the drug is used chronically and higher and higher dosages are needed to get the same effects. Frequent episodes of binge use can be followed by severe depression and an overpowering desire to continue using the drug despite the onset of serious negative medical and social consequences, including psychotic episodes, paranoid delusions, hallucinations, hospitalization, or incarceration.

LEGAL CONSEQUENCES

In the United States, the legal consequence of possession, illegal sale, or even giving away of MPH drugs can be severe under terms of the Controlled Substance Act (CSA), which is part of the Comprehensive Drug Abuse Prevention and Control Act of 1970, the legal foundation of the federal government's fight against the abuse of drugs and other substances. Because of the abuse potential of MPH, the DEA has placed stringent Schedule II controls and licensing requirements on the manufacture, distribution, and prescription of the sub-stance. Breaking those rules can result in fines and imprisonment.

Under Section 844 of the CSA, simple possession of a controlled substance (including methylphenidate) without a doctor's prescription can result in imprisonment for one year for a first offense and a fine of $1,000 or both. A second offense can result in imprisonment for up to two years and a fine of $2,500. A third offense can result in up to three years of prison time and a fine of $5,000.

Distribution, which includes selling or even giving any mixture or substance containing a detectable amount of methylphenidate is illegal under CSA Section841. For a first offense, it is punishable by a prison term of not more than 20 years and fines up to $1 million for an individual or $5 million if not an individual. If death or serious bodily injury results, imprisonment terms not less than 20 years or more than life. A second offense is punishable by a prison term of not more than 30 years, and a fine of up to $2 million for an individual or up to $10 million if not an individual. If death or serious injury results, life imprisonment is the punishment. A person convicted of selling MPH to someone younger than 21 years of age is subject to "twice the maximum punishment authorized."

Legal history

The FDA approved Ritalin, the original brand name of methylphenidate, in 1961 as a Schedule II drug. When the U.S. Congress passed the CSA in 1970, MPH, as a controlled Schedule II substance, came under the regulation of that law.

In 2001, plaintiffs representing children treated with Ritalin filed a federal lawsuit against Novartis Pharmaceuticals Corp. (the manufacturers of Ritalin), the American Psychiatric Association (APA), and the Children and Adults with Attention Deficit Hyperactivity Disorder organization (CHADD). The lawsuit charged that the trio of organizations had conspired to increase the sales of MPH by broadening the definition of ADHD in the APA's Diagnostic and Statistical Manual of Mental Disorders (DSM). The plaintiffs also criticized CHADD for accepting grant money from Novartis.

However, senior U.S. District Judge Rudi Brewster ruled that the plaintiffs did not have enough evidence to support their claims. He gave them additional time to produce new evidence, but when they failed to do so he ultimately dismissed the case with prejudice, meaning the plaintiffs cannot re-file it.

In 2002, several states, including Connecticut and Minnesota, passed laws that ban teachers from recommending psychotropic drugs, especially Ritalin, to parents. The legislators were concerned that educators were pressuring parents to put their children on MPH so that it would be easier for teachers to deal with ADHD kids in classrooms. Legislators believe it should be up to parents and their doctors to decide whether their children should be put on the drug.

Federal guidelines, regulations, and penalties

Since methylphenidate is a Schedule II controlled substance, it is tightly regulated from manufacture to delivery to the doctor or pharmacy. Schedule II drugs require strict manufacturing quotas, careful inventory controls that require special order forms, and separate record-keeping requirements. Prescriptions may not be refilled—a new prescription is required for every new supply. Unlike less stringently regulated drugs, the methylphenidate prescriptions cannot be phoned in to the pharmacy; the prescriptions must be written. Some states such as California and Indiana require special numbered and triplicate prescription forms for tracking purposes. Breaking those regulations can result in jail time of up to one year and a fine of $25,000, according to CSA Section 842: Prohibited Acts B.

See also Amphetamines

RESOURCES

Books

Breggin, P. R. Talking Back to Ritalin: What Doctors Aren't Telling You About Stimulants for Children. Monroe, ME: Common Courage Press, 1998.

DeGrandpre, R. Ritalin Nation: Rapid Fire Culture and the Transformation of Human Consciousness. New York: W.W. Norton & Company, 1999.

Diller, L. H. Running on Ritalin: A Physician Reflects on Children, Society and Performance in a Pill. New York: Bantam Books, 1998.

Hallowell, E. M., and Ratey, J. J. Driven to Distraction: Recognizing and Coping with Attention Deficit Disorder from Childhood to Adulthood. New York: Pantheon Books, 1994.

Periodicals

"Abusing Ritalin: Dangers of Prescription Drug Abuse." Scholastic Choices v. 17 (September 2001).

"Frequently Asked Question About Ritalin." Ritalin on College Campuses.<http://pubweb.acns.nwu.edu/~cam717/faq.html>.

Marks, A. "Schoolyard Hustlers' New Drug: Ritalin." The Christian Science Monitor's Electronic Edition (October 31, 2000): pp. 4.

"Ritalin (Methylphenidate)." Alberta Alcohol and Drug Abuse Commission (AADAC).<http://corp.aadac.com/drugs/factsheets/Ritalin.asp>.

Other

Ciampa, L. Ritalin Abuse Scoring High on College Illegal Drug Circuit. CNN.Com (January 8, 2001). <http://www.cnn.com/2001HEALTH/children/01/08/college.ritalin/>.

Organizations

Attention Deficit Information Network, 475 Hillside Ave., Needham, MA, USA, 02194, (617) 455-9895.

Children and Adults with Attention Deficit Disorders, 499 N.W. 70th Ave., Suite 101, Planation, FL, USA, 33317, (800) 233-4050, <http://www.chadd.org>.

Health Services Administration (SAMHSA), U.S. Dept. of Health and Human Services, 5600 Fishers Lane, Rockville, MD, USA, 20857, (301) 443-0001, (301) 443-1563, 1-800-622-Help, [email protected], <http://www.samhsa.gov/centers/cmhs/cmhs.html>.

National Attention Deficit Disorder Association, 1788 Second Street, Suite 200, Highland Park, IL, USA, 60035, (847) 432-3223, (847) 432-5874, [email protected], <http://www.add.org>.

University of Kentucky Center for Prevention Research, 1151 Red Mile Rd. Ste. 1-A, Lexington, KY, USA, 40507, (606) 257-5588, <http://www.uky.edu/RGS/PreventionResearch/welcome.html>.

Maury M. Breecher, PhD, MPH