Methylphenidate (APTENSIO XR, CONCERTA, COTEMPLA XR-ODT, DAYTRANA [transdermal], METADATE CD, METADATE ER, METHYLIN, METHYLIN ER, QUILLIVANT XR, RITALIN, RITALIN LA, RITALIN-SR) is approved by the Food and Drug Administration (FDA) for the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Methylphenidate increases the neurotransmitters dopamine and...
These drugs are listed as Limited Use (offers limited benefit or benefits only certain people or conditions).
Methylphenidate (APTENSIO XR, CONCERTA, COTEMPLA XR-ODT, DAYTRANA [transdermal], METADATE CD, METADATE ER, METHYLIN, METHYLIN ER, QUILLIVANT XR, RITALIN, RITALIN LA, RITALIN-SR) is approved by the Food and Drug Administration (FDA) for the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Methylphenidate increases the neurotransmitters dopamine and norepinephrine. This drug is not a cure for either ADHD or narcolepsy.
The chemical structure of methylphenidate resembles that of amphetamine ("speed"-like drugs). Federal law classifies methylphenidate as a Schedule II controlled substance that requires a new, handwritten prescription for each new and refill prescription.
Narcolepsy is uncontrolled sleepiness, especially during the day. It is a rare condition. There is a lack of well-documented evidence that the benefits of using most stimulants to treat narcolepsy outweigh the risks.
Tics, a neurological condition that waxes and wanes, occur mostly in children ages 7 to 13. There are reports of methylphenidate both decreasing vocal tics and worsening tics.
Little information on the long-term safety and effectiveness of methylphenidate is available. The safety and efficacy of using methylphenidate for children under age 6 have not been established.
Common adverse effects of methylphenidate are headache, stomachache and loss of appetite. Short-acting forms are more apt to cause dizziness, and long-acting forms are more likely to cause insomnia. The shell of the extended-release tablets may be observed in the stool. This does not mean the methylphenidate was not absorbed.
A 2013 article published in Prescrire International, a respected and independent source of drug information, reported cases of dystonia (in which muscles contract involuntarily) and trismus (commonly known as lockjaw) with methylphenidate use.
Suppression of growth
Suppression of growth (weight or height) has been reported with the long-term use of stimulants in children. Prescrire International published an article in October 2011 examining the effects of methylphenidate on suppression of growth in children. According to the article, the data examined in the studies showed that growth was affected in children, and this effect occurred especially during the first year of treatment.
Methylphenidate may induce psychosis with mood changes and hallucinations, especially when used for a long time and in high doses.4 Symptoms may include seeing or hearing things, believing things that are not real or becoming suspicious. Other psychiatric problems — such as new or worsened behavior and problems with clear thinking, bipolar illness and aggressive behavior or hostility — have been reported in patients taking methylphenidate and other stimulant medications.
Methylphenidate should not be used in patients with marked anxiety, tension or agitation because it can aggravate these symptoms. It also should never be used in patents who have glaucoma, tics (involuntary repetitive movements) or Tourette’s syndrome (a neurological disorder that occurs in childhood or adolescence and is characterized by tics and involuntary vocalizations).
In 2015, Health Canada, an agency similar to the FDA, updated the warning section of the labels of drugs used to treat ADHD on the risk of suicidal thoughts and behaviors. The advisory stated that Health Canada had received reports that included thoughts of suicide, suicide attempts and, in a very small number of cases, suicide.
There also have been reports of several heart-related problems in individuals taking usual doses of ADHD medications, including sudden death in patients who have an underlying serious heart problem or defect, stroke and heart attack in adults, and increased blood pressure and heart rate.
In 2015, Prescrire International published an article on reports of pulmonary hypertension (high blood pressure in the lung that can later weaken the heart) and heart valve disorders associated with methylphenidate use in both children and adults.
Prolonged and painful erections, sometimes requiring surgery, have been reported in both pediatric and adult patients using methylphenidate. This typically occurs after some time on the drug, often after a dose increase or during a period when the drug is stopped (a drug holiday). Patients who develop abnormally long or frequent and painful erections should seek immediate medical attention.
In 2004, Prescrire International examined the benefits of sustained-release methylphenidate tablets compared with short-acting forms for the drug. The article stated that the effects of sustained-release forms taken once daily were not significantly different from those of short-acting methylphenidate tablets taken three times a day. The sustained-release formulation cannot be cut, crushed or chewed.
Nearly one-half of almost 13,000 poisoning exposures to methylphenidate involved children under age 6 who usually swallowed prescriptions belonging to others. One-third of the cases in children from ages 6 to 12 involved the child’s own medication. About one-third of cases of those over age 12 involved their own prescription, and some poisonings were suicide attempts. Many incidents involved unintentionally administering an incorrect dose.
In 2012, the Danish Medicines Agency published a report on new data on the safety of methylphenidate when used in the treatment of ADHD. Since the first report was published in 2010, the agency continues to receive reports of adverse reactions associated with the use of methylphenidate. According to the information in the 2012 report, the most common adverse effects were of the nervous system and psychiatric symptoms, and the majority of the new cases were reported in children.
In 2020, Lancet published results of research showing that use of methylphenidate was associated with an increased risk of seizure during the first 30 days after starting the drug. The increased risk was not found beyond 30 days of continued treatment with the drug.
Regulatory actions surrounding methylphenidate
2007: The FDA directed manufacturers of ADHD drugs to develop Medication Guides. When a prescription for any ADHD drug is filled, pharmacists must distribute an FDA-approved Medication Guide that both alerts patients to the possible cardiovascular and psychiatric risks associated with the medicines and describes precautions that can be taken to help patients use the medication more safely.
2013: The FDA issued an advisory that methylphenidate therapy has been associated in postmarketing reports with peripheral vasculopathy (damage to blood vessels outside of the heart), including Raynaud’s phenomenon. These disorders typically affect fingers and toes. Raynaud’s phenomenon is characterized by a pale to blue to red sequence of color changes in the fingers or toes, most commonly after exposure to cold. Fingers or toes also may feel numb or painful.
The FDA also issued a safety alert warning that methylphenidate products may be associated with rare cases of priapism (prolonged and sometimes painful erections). The drug product label and Medication Guide for these products were revised.
2015: The FDA issued a safety warning that permanent, disfiguring loss of skin color is associated with methylphenidate transdermal system (DAYTRANA; known as the methylphenidate patch).