Methylphenidate (Ritalin) stimulates the central nervous system. It is used in the treatment of ADHD (Attention deficit hyperactive disorder) and Narcolepsy.

Methylphenidate (Ritalin) Uses:

• Attention-deficit/hyperactivity disorder:
  • Treatment of attention-deficit/hyperactivity disorder (ADHD)
• Narcolepsy (Methylin, Metadate ER, Ritalin, and Ritalin SR):
  • Symptomatic management of narcolepsy
• Off Label Use Of Methylphenidate in Adults:
  • As a palliative treatment in patients with depression caused by terminal illnesses
  • Cancer-related fatigue;
  • Major depressive disorder (in geriatric patients as antidepressant augmentation)

Methylphenidate (Ritalin) Dose in Adults

Methylphenidate use in the treatment of ADHD:

• Immediate-release (IR) products (tablets, chewable tablets, and solution):
  • Initial: 2 times a day, before breakfast and lunch, take 5 mg orally;
  • weekly intervals, raise the dose by 5 to 10 mg each day;
  • The maximum dose: 60 mg/day (in 2 to 3 divided doses).
• Extended-release (ER), sustained-release (SR) products (capsules, tablets, chewable tablets, orally disintegrating tablets, and oral suspension):
  • Concerta: (Adults <65 years):
    • Patients not currently taking methylphenidate:
      • Initial: 18 to 36 mg orally once every morning
    • Patients currently taking immediate-release (IR) methylphenidate or sustained-release (SR) [Canadian product]:
      • Initial: Note: Dosing based on current regimen and clinical judgment; suggested dosing listed below:
  • IR methylphenidate:
    • Patients taking IR methylphenidate 5 mg 2 to 3 times daily:
      • 18 mg orally once every morning
    • Patients taking IR methylphenidate 10 mg 2 to 3 times daily:
      • 36 mg orally once every morning
    • Patients taking IR methylphenidate 15 mg 2 to 3 times daily:
      • 54 mg orally once every morning
    • Patients taking IR methylphenidate 20 mg 2 to 3 times daily:
      • 72 mg orally once every morning
  • SR methylphenidate (Concerta Canadian product labeling 2017):
    • Patients taking methylphenidate SR 20 mg daily:
      • 18 mg orally once every morning
    • Patients taking methylphenidate SR 40 mg daily:
      • 36 mg orally once every morning
    • Patients taking methylphenidate SR 60 mg daily:
      • 54 mg orally once every morning
    • Dose adjustment:
      • At weekly intervals, the dose may be raised in 18 mg increments.
      • Dosage strength of 27 mg is available for situations in which a dosage between 18 to 36 mg is desired.
      • Maximum dose: 72 mg/day.
  • Aptensio XR:
    • Initial: 10 mg orally once daily; may be titrated in 10 mg increments at weekly intervals;
    • The maximum: 60 mg/day.
  • Biphentin [Canadian product]:
    • Patients not currently taking methylphenidate:
      • Initial: may be raised to a maximum dose of 80 mg/day by taking 10 to 20 mg orally once daily.
    • Conversion from immediate-release methylphenidate formulations to Biphentin:
      • Use a once-day dose that is comparable to the total daily dose.
  • Foquest [Canadian product]:
    • Patients not currently taking methylphenidate:
      • Initial: 25 mg orally once daily; when needed, adjust the dose at 5-day intervals to the lowest effective dose (maximum: 100 mg/day)
    • Patients currently taking methylphenidate:
      • Initiate Foquest with the next lower strength based on total methylphenidate daily dose;
      • Adjust dose at 5-day intervals as needed to the lowest effective dose (maximum: 100 mg/day).

Note:

• Do not substitute immediate release formulations or other controlled release formulations with Foquest on a milligram for milligram basis (pharmacokinetic profiles differ).
  • Jornay PM:
    • Initial: 20 mg orally once daily in the evening between 6:30 and 9:30 PM (eg, 8:00 PM);
    • may be increased in increments of 20 mg/day at weekly intervals to a maximum daily dose of 100 mg/day.

Note:

• If converting from another methylphenidate formulation, discontinue the previous formulation and titrate Jornay PM using this same schedule;
• Do not substitute on a milligram-per-milligram basis.
  • Metadate ER, Ritalin-SR:
    • Administer 2 or 3 times daily; replace immediate-release tablets when the divided dosage corresponds to sustained-/extended-release tablet strength (duration of action: ~8 hours);
    • The maximum: 60 mg/day
  • Metadate CD, Quillivant XR:
    • Initial: 20 mg orally once daily; may be adjusted in 10 to 20 mg increments at weekly intervals;
    • The maximum: 60 mg/day
    • Conversion from other methylphenidate formulations to Quillivant XR:
      • Discontinue the previous formulation and titrate using the above schedule;
      • Do not substitute on a milligram-per-milligram basis
  • QuilliChew E R:
    • Initial: 20 mg orally once daily in the morning; maybe adjusted by 10, 15 or 20 mg at weekly intervals (tablets are scored and may be broken in half to achieve the 10 mg and 15 mg doses); maximum: 60 mg/day
    • Conversion from other methylphenidate formulations to QuilliChew ER:
      • Discontinue the previous formulation and titrate using the above schedule;
      • Do not substitute on a milligram-per-milligram basis
  • Ritalin LA:
    • Initial: 20 mg orally once daily (10 mg once daily may be considered for some patients);
    • The dose may be increased by 2.5 to 5 mg every 1 to 3 days in divided doses
    • maximum: 60 mg/day
    • Conversion from immediate-release or sustained-release methylphenidate formulation to Ritalin LA:
      • Use an equivalent total daily dose administered once daily.

Methylphenidate use in the Narcolepsy:

• Immediate-release tablets and solution (Methylin, Ritalin):
  • Initial: 5 mg orally twice daily before breakfast and lunch;
  • increase by 5 to 10 mg daily at weekly intervals to a maximum dose of 60 mg/day (in 2 to 3 divided doses).
• Extended- and sustained-release tablets (Metadate ER, Ritalin-SR):
  • Administer 2 or 3 times orally daily.
  • Replace immediate-release tablets when the divided dosage corresponds to sustained-/extended-release tablet strength (duration of action: ~8 hours); maximum: 60 mg/day

Methylphenidate Off label use in the treatment of depression in patients with a terminal illness (for palliative care in medically ill):

• Immediate release:
  • 5 to 5 mg orally once daily before breakfast or twice daily before breakfast and lunch;
  • before breakfast and lunch as tolerated, up to a maximum dose of 20 to 40 mg/day, in increments of 10 mg at weekly intervals.
  • Do not use sustained release

Off label use in the treatment of cancer-related Fatigue:

• Immediate-release:
  • Initial: 5 mg orally twice daily (at 8 am and 1 pm);
  • increase the dose based on tolerability in increments of 10 mg/day every 3 days up to a maximum of 40 mg/day.

Methylphenidate (Ritalin) Dose in Childrens

Use in the treatment of Attention deficit-hyperactivity disorder (ADHD):

• Methylphenidate is recommended first-line therapy for children and adolescents;
• a discontinuation trial is also recommended after 6 months of therapy, to reassess underlying psychopathology.
• Note: Medication should be discontinued if no improvement is noted after appropriate dosage adjustment over 1 month.
• Immediate-release products (eg, Methylin, Ritalin):
  • Children 3 to 5 years, in cases of moderate to severe dysfunction:
  • Limited data is available; AAP considers this drug as the first-line agent in this patient population if pharmacological treatment deemed necessary (AAP 2011);
  • the American Academy of Child and Adolescent Psychiatry Preschool Psychopharmacology Working Group recommends a discontinuation trial after 6 months of treatment in preschoolers to reassess underlying psychopathology (Gleason 2007).
  • The response may be variable and less robust than that observed in older pediatric patients.
  • of note, response to methylphenidate was predicted by the number of comorbidities (eg, no or single comorbidity showed a large treatment response [similar to school-aged children] while ≥3 comorbidities predicted no response) (Ghuman 2008).
    • Initial: 2.5 mg orally twice a day,
    • may gradually titrate to 7.5 mg 2 or 3 times a day over 2 to 4 weeks;
    • others have used a rapid titration to 7.5 mg 3 times a day within 1 week.;
    • a small population of preschool children may benefit from 1.25 mg 3 times per day.
    • Although ADHD scores were statistically and clinically improved with methylphenidate use, the effect size was smaller with this younger patient population than that seen in school-age children (Greenhill 2006).
    • The 10-month continuation phase trial showed continued or stable clinical improvement at a mean dose of 19.98 mg/day in the 10th month.
  • Children ≥6 years and Adolescents:
    • Initial: Before breakfast and lunch, take 2.5 to 5 mg orally twice daily; increase the dose by 5 to 10 mg every other week.;
    • some patients may require 3 doses per day (eg, additional dose after school) to a usual maximum daily dose of 60 mg/day, not to exceed 2 mg/kg/day;
    • however, some patients weighing >50 kg may require and tolerate daily doses up to 100 mg per day with more frequent monitoring.
• Extended-release, sustained-release, and long-acting products:
  • Aptensio XR:
    • Children ≥6 years and Adolescents:
      • Initial: 10 mg orally once daily in the morning;
      • may titrate in 10 mg increments at weekly intervals; maximum daily dose: 60 mg/day
  • Concerta:
    • Children ≥6 years and Adolescents:
      • Methylphenidate-naive patients:
        • Initial: 18 mg orally once daily
      • Patients currently using immediate-release methylphenidate:
        • Initial dose: Dosage is according to current regimen and physician clinical judgment; suggested dosing are listed below, monitor closely with any therapy change:
    • Switching from methylphenidate immediate-release 5 mg 2 to 3 times a day:
      • Concerta 18 mg once daily
    • Switching from methylphenidate immediate-release 10 mg 2 to 3 times a day:
      • Concerta 36 mg once daily
    • Switching from methylphenidate immediate-release 15 mg 2 to 3 times a day:
      • Concerta 54 mg once daily
    • Switching from methylphenidate immediate-release 20 mg 2 to 3 times a day:
      • Concerta 72 mg once daily
    • Dosage adjustment:
      • The following maximum daily dose for age may be increased by Concerta 18 mg/day increments over intervals of 7 days to get the desired effect.
    • Note:
      • Dosage strength of 27 mg is available for situations where a dosage between 18 and 36 mg is needed.
    • The maximum daily dose of Concerta:
      • Children 6 to 12 years:
        • Usual maximum daily dose: 54 mg per day;
        • But some patients could require and be able to take doses of up to 108 mg per day.
      • Adolescents:
        • The typical daily dose cap is 72 mg, although some patients may need and tolerate daily doses as high as 108 mg. (AACA [Pliszka 2007])
  • Cotempla XR-ODT:
    • Children ≥6 years and Adolescents ≤17 years:
      • Initial: 17.3 mg orally once daily in the morning;
      • may titrate in 8.6 or 17.3 mg increments at weekly intervals;
      • The maximum daily dose: 51.8 mg/day
  • Jornay PM:
    • Children ≥6 years and Adolescents:
      • Initial: 20 mg orally once daily in the evening between 6:30 and 9:30 PM (eg, 8:00 PM);
      • may rise at weekly intervals in increments of 20 mg/day.
      • The maximum daily dose: 100 mg/day.

Note:

• while switching from another methylphenidate formulation, the previous formulation must be discontinued and titrate Jornay PM using the above schedule;
• Do not substitute on a milligram-per-milligram basis.
  • Metadate CD:
    • Children ≥6 years and Adolescents:
      • Initial: Once daily oral dose of 20 mg; possible weekly increases of 10 to 20 mg/day; typical daily maximum dose of 60 mg/day
      • however, some patients weighing >50 kg may require and tolerate daily doses up to 100 mg per day with frequent monitoring.
  • Metadate ER, Ritalin-SR:
    • Children ≥6 years and Adolescents:
      • Immediate-release tablets are replaced when the 8-hour dosage corresponds to sustained-/extended-release tablet size;
      • Ritalin SR may be administered once or twice a day.
      • The usual maximum daily dose: 60 mg/day;
      • however, some patients weighing >50 kg may require and tolerate daily doses up to 100 mg per day with frequent monitoring.
  • QuilliChew ER:
    • Children ≥6 years and Adolescents:
      • Initial: 20 mg orally once daily in the morning; maybe adjusted in 10, 15, or 20 mg increments at weekly intervals (tablets are scored and may be broken in half to achieve dose) to a maximum daily dose of 60 mg/day

Note:

• While switching from another formulation of methylphenidate, the previous formulation must be discontinued and titrate QuilliChew ER using the above schedule;
• Do not substitute on a milligram-per-milligram basis.
  • Quillivant XR:
    • Children ≥6 years and Adolescents:
      • Initial: 20 mg orally once daily in the morning;
      • may be raised to a maximum daily dose of 60 mg/day in weekly increments of 10 to 20 mg/day.
  • Ritalin LA:
    • Children ≥6 years and Adolescents:
      • Methylphenidate-naive patients:
        • Initial: 20 mg orally once daily;
        • may increase by 10 mg/day increments at weekly intervals;
        • The typical daily dose maximum is 60 mg, although certain individuals who weigh more than 50 kg may require and tolerate daily doses of up to 100 mg with frequent monitoring.

Note:

• If a lower initial dose is required, patients may begin with Ritalin LA 10 mg once every day.
• Alternatively, patients may start treatment with an immediate-release product, and switch to Ritalin LA once the immediate-release dosage is titrated to 5 mg twice a day (see below).
  • Patients currently receiving immediate-release methylphenidate:
    • The same total daily dose of Ritalin LA should be used.
  • Patients currently receiving methylphenidate sustained-release (SR):
    • The same total daily dose of Ritalin LA should be used.

Canadian labeling:

• Concerta:
  • Children ≥6 years and Adolescents:
    • Sustained-release methylphenidate [Canadian product] to Concerta: Oral:
      • Switching from methylphenidate SR 20 mg daily:
        • Concerta 18 mg orally once every morning
      • Switching from methylphenidate SR 40 mg daily:
        • Concerta 36 mg orally once every morning
      • Switching from methylphenidate SR 60 mg daily:
        • Concerta 54 mg orally once every morning

  • ---

Biphentin [Canadian product]:

• Children ≥6 years and Adolescents:
  • Methylphenidate naive patients:
    • Initial: 10 to 20 mg orally once daily; adjustments may be made in 10 mg increments per week
    • The maximum daily dose: 60 mg/day.

Note:

• In some children and adolescents, higher doses may be necessary; do not exceed 1 mg/kg/day or the adult maximum of 80 mg/day;
• monitor closely for adverse events, reduce the dose or discontinue if adverse events occur.
  • Patients currently receiving immediate-release methylphenidate:
    • Use an equivalent total daily dose administered once every day.

Topical: Transdermal patch (Daytrana):

• Children and Adolescents 6 to 17 years:
  • Initial: 10 mg (12.5 cm ) patch once daily; apply to hip 2 hours before the effect is needed and remove 9 hours after application (eg, 3 hours before bedtime);
  • titrate dose according to response and tolerability; may increase to next transdermal patch dosage size not frequently than every week.
  • The patch may be removed before 9 hours if a shorter duration of action is required or if late-day adverse effects appear or may be worn for up to 16 hours if the extended duration of effects is required.
  • Plasma concentrations usually start to decline as soon as the patch is removed but the absorption of the drug may continue for several hours after patch removal.

Note:

• The drug manufacturer's labeling recommends patients switching from another formulation of methylphenidate to the transdermal patch should be started at 10 mg regardless of their previous dose and titrated as required because of the differences in bioavailability of the transdermal formulation.
• However, some clinicians have supported higher starting patch doses for patients converting from oral methylphenidate doses of >20 mg/day;
• for example, the 15 mg (18.75 cm) patch has been investigated to have the same effect to that of 22.5 mg a day of the immediate-release preparation, 27 mg daily of the osmotic-release preparation (Concerta), or 20 mg per day of the encapsulated bead preparation (Metadate CD).

Approximate oral methylphenidate equivalents for the 20 mg and 30 mg patches, with a 9-hour patch wear time,  are (Arnold 2007):

Methylphenidate (Ritalin) Use in the Narcolepsy:

• Children ≥6 years and Adolescents:
  • Immediate-release tablets and oral solution (Methylin, Ritalin):
    • Initial: Before breakfast and lunch, take 5 mg orally twice day. From then, raise the dose by 5 to 10 mg/day at weekly intervals, taking it 2 to 3 times daily, up to a maximum of 60 mg/day (in 2 to 3 divided doses)
  • Extended-/sustained-release tablets (Metadate ER, Ritalin-SR):
    • May be given in place of immediate-release products, once the immediate-release formulation daily dose is titrated and the titrated 8-hour dosage corresponds to sustained- or extended-release tablet size to a maximum daily dose of 60 mg/day

Methylphenidate Pregnancy Risk Category: C

• The information available on the use of methylphenidate during pregnancy in women with attention deficit/ hyperactivity disorder (ADHD) or narcolepsy is sparse and conflicting.
• Methylphenidate might be an option if ADHD is being treated in pregnancy.

Methylphenidate, also known as RitalinUse during breastfeeding

• Breast milk contains methylphenidate.
• The relative infant dose of methylphenidate (RID) is 0.7%.
• This was calculated using the highest concentration of breast milk and compared with a maternal weight-adjusted dose of 52 mg/day.
• When the RID of the medication is less than 10%, breastfeeding is generally acceptable.
• Some sources mention that breastfeeding is only recommended if the RID for psychotropic drugs is less than 5%.
• The RID of Methylphenidate was calculated with a milk concentration of 19. mcg/L. This gives an absolute infant dose via breastmilk of 2.9 mg/kg/day.
• After three mothers were given methylphenidate for ADHD, the milk concentration was determined.
• The maternal dose ranged between 35 and 80 mg/day.
• Two additional case reports were also submitted by the authors. They calculated that the RID for methylphenidate was 1%.
• A case report showed that methylphenidate in breast milk was not detectable after 20-21 hours following the administration of the immediate-release tablets to the mother.
• Three cases did not report adverse events, but infants in two of the cases were older (6 and 11 months respectively) and exposed to a limited amount.
• Studies of long-term developmental effects are not available.
• One child was normal for growth and medical development up to one year old.
• According to the manufacturer of the product, when deciding whether to discontinue or continue breastfeeding during therapy, it is important to consider both the risks to the infant as well as the benefits to the mother.
• Monitor infants who are breastfeed to monitor for any adverse reactions such as agitation or anorexia.

Common Side Effects of Methylphenidate (Ritalin):

• Central Nervous System:
  • Insomnia
  • Headache
  • Irritability
• Gastrointestinal:
  • Decreased Appetite
  • Xerostomia
  • Nausea

Methylphenidate Side effect (Less Common):

• Cardiovascular:
  • Tachycardia
  • Palpitations
  • Increased Blood Pressure
  • Increased Heart Rate
• Central Nervous System:
  • Anxiety
  • Tics
  • Dizziness
  • Psychomotor Agitation
  • Depressed Mood
  • Emotional Lability
  • Nervousness
  • Restlessness
  • Aggressive Behavior
  • Increased Diastolic Blood Pressure
  • Agitation
  • Depression
  • Hypertonia
  • Lack Of Emotion
  • Vertigo
  • Confusion
  • Sedation
  • Tension
  • Tension Headache
  • Paresthesia
• Dermatologic:
  • Hyperhidrosis
  • Excoriation
  • Skin Rash
• Endocrine & Metabolic:
  • Weight Loss
  • Decreased Libido
• Gastrointestinal:
  • Vomiting
  • Abdominal Pain
  • Upper Abdominal Pain
  • Anorexia
  • Bruxism
  • Dyspepsia
  • Motion Sickness
  • Constipation
• Hematologic & Oncologic:
  • Bruise
• Neuromuscular & Skeletal:
  • Back Pain
  • Tremor
• Ophthalmic:
  • Blurred Vision
  • Eye Pain
• Respiratory:
  • Nasopharyngitis
  • Streptococcal Pharyngitis
  • Cough
  • Upper Respiratory Tract Infection
  • Oropharyngeal Pain
• Miscellaneous:
  • Fever

Uncommon Side effects of Methylphenidate (Ritalin):

• Cardiovascular:
  • Cardiac Arrhythmia
  • Decreased Blood Pressure
  • Decreased Pulse
  • Heart Murmur
  • Hypertension
  • Increased Pulse
• Central Nervous System:
  • Drug Abuse
  • Drug Dependence
  • Gilles De La Tourette Syndrome
  • Hypervigilance
  • Jitteriness
  • Mood Changes
  • Outbursts Of Anger
  • Panic Attack
  • Sleep Disorder
  • Toxic Psychosis
• Dermatologic:
  • Macular Eruption
• Endocrine & Metabolic:
  • Growth Suppression
  • Hot Flash
  • Increased Thirst
• Gastrointestinal:
  • Abdominal Distress
  • Diarrhea
• Genitourinary:
  • Erectile Dysfunction
• Hematologic & Oncologic:
  • Anemia
  • Leukopenia
• Hepatic:
  • Increased Serum Alanine Aminotransferase
• Neuromuscular & Skeletal:
  • Asthenia
  • Muscle Spasm
• Ophthalmic:
  • Dry Eye Syndrome
• Respiratory:
  • Dyspnea
  • Sinusitis

Contraindications to Methylphenidate (Ritalin):

• allergies to the medication or any of its ingredients
• When combined with MAO inhibitors or used within 14 days
• Anxiety, tension, or agitation that is characterized by anxiety and tension.
• Glaucoma
• Tourette syndrome, tics or family history
• Hypertension severe
• Heart failure
• Arrhythmia
• Hyperthyroidism and thyrotoxicosis.
• Recent MI or angina
• Use of halogenated anesthetics in conjunction
• Patients with uncommon genetic (hereditary), fructose intolerance, difficulty absorbing glucose-galactose, or sucrose-isomaltase deficiencies
• Advanced arteriosclerosis
• Pheochromocytoma
• People with a history or drug abuse.

Warnings and precautions

• Cardiovascular events
  • Patients suffering from preexisting structural heart disease may be at increased risk for sudden cardiac death, myocardial injury, or stroke.
  • Patients with structural cardiac abnormalities must avoid Methylphenidate and other stimulant drugs.
  • Patients with angina, heart failure or patients suffering from recent MI, such as moderate or severe hypertension or angina, should avoid it.
  • Patients who have a family history involving sudden death or ventricular rhythmias should inquire about a family history involving sudden death and/or ventricular arrhythmias. Patients at high risk should have a cardiac examination, an ECG, and an Echo.
  • If patients experience exertional chest pain, unexplained systolic symptoms, or other signs of cardiac disease, they should be seen immediately.
• Hypersensitivity
  • It has been associated with allergic reactions, including anaphylaxis or angioedema.
• Peripheral vasculopathy
  • Stimulant drugs can cause vasoconstriction, which may lead to peripheral vasculopathy.
  • Patients experience improvements when they are given a lower dosage or stopped altogether.
  • The effects of peripheral vasculopathy on the periphery have been documented at various times and at therapeutic doses in all ages.
  • Rarely have we seen digital ulceration or soft tissue destruction. If you notice any, refer to rheumatology for further evaluation.
• Priapism
  • According to the FDA warning and manufacturers' labels, erections that last more than four hours and are painful and sometimes require surgery have been reported in both children and adults. There are at least 22 published cases.
  • It has been reported that priapism can develop after some time using the drug.
  • This may be after an increase in dosage or during withdrawal (drug holidays, discontinuation).
  • Patients who have certain hematological disorders (eg, sickle-cell disease), malignancies or perineal trauma or concomitant alcohol use, illicit drugs or other medications that are associated with priapism could be at higher risk (Eiland, 2014).
  • If patients experience painful, prolonged, or persistent erections, discontinue therapy immediately and consult a physician.
  • In severe cases, a urologist should be consulted immediately.
  • There have been different products and dosage forms associated with priapism.
  • It is unknown if the risk of recurrence will be present if you re-challenge with a new formulation.
  • Avoidance of stimulants and atomoxetine is recommended for patients suffering from severe priapism (Eiland, 2014).
• Visual disturbance
  • Stimulants have been associated with blurred vision and difficulty in accommodation.
• Potential for abuse: [US Boxed Warning]
  • There is a high risk of dependence and abuse with CNS stimulants such as methylphenidate-containing products and amphetamines.
  • Before prescribing medication, assess the risk of abuse. Monitor for signs and symptoms of abuse or dependence during treatment.
  • A long-term abuse can result in psychological dependence and marked tolerance.
  • Parenteral abuse can lead to psychotic episodes.
  • Because severe depression can occur, it is important to supervise those who are withdrawing from abusive drug use.
  • Long-term treatment may cause drug withdrawal. This may lead to a relapse that may need follow-up.
• Cardiovascular diseases
  • CNS stimulants can increase blood pressure and heart rate; pediatric patients experienced a mean increase of 3 to 6 beats per minute and a rise in blood pressure of 2 to 4 millimeters Hg.
  • Patients with heart disease, hypertension, heart failure, recent MI and ventricular arrhythmia should be cautious.
  • Patients with severe hypertension, hyperthyroidism or angina may be allergic to certain products.
• Psychiatric disorders
  • Patients with preexisting psychosis should be cautious (may worsen symptoms of behavior and thought disorder) and bipolar disorder (may cause mixed/manic episodes).
  • Stimulant use may cause new-onset psychosis and mania.
  • Before starting treatment, patients should be tested for bipolar disorder.
  • This could be associated with aggressive behavior in children or hostility (causal relationship unknown); monitor for the development of these behaviors.
  • ADHD patients are more likely to attempt suicide and have suicidal thoughts. However, large cohort studies have not shown a causal relationship between methylphenidate and attempted murder.
  • Suicide-related behavior should be monitored.
• Seizure disorder
  • Patients with a history or seizure disorder should exercise caution. It may reduce seizure threshold and cause new-onset seizure activity.
  • In the event of seizures, discontinue use
• Tourette syndrome/tics
  • Patients with Tourette syndrome and other tic disorders should be cautious.
  • Although stimulants can cause Tourette syndrome and motor and phonic tics, there is not much evidence to support an increase in tics.
  • Before starting therapy, check for Tourette syndrome and tics. Some products are contraindicated.

Monitoring required while using Methylphenidate (Ritalin):

• Periodic differential, CBC and platelet counts
• Monitoring your heart rate and blood pressure
• Monitor for suicidal thoughts, mood instability, depression and aggression.
• Children should be monitored for height and weight
• Monitor your patient for signs of stimulation or hyperactivity;
• You should monitor the patient for any digital ischemic signs or peripheral vasculopathy.
• Use the transdermal patch to check for erythema and blistering.
• Assess the patient for any signs and symptoms of cardiovascular disease.

How to take Methylphenidate (Ritalin)?

Oral Methylphenidate:

• Controlled-release capsule (Biphentin and Foquest)
  • It should be taken in the morning, and should be swallowed whole with water.
  • Capsules should not be broken down or chewed.
  • You can open the capsules and sprinkle them on yogurt, ice cream or apple sauce, but you should not chew or crush the beads.
  • Sprinkled on food, it should not be left for more than ten minutes.
  • After taking the tablet, patients should rinse off their mouth.
  • It should not be administered if it takes more than 10 minutes.
• Instant-release (IR), tablet (Ritalin), solution (Methylin), chewable tablet (Methylin).
  • Take each dose between 30 and 45 minutes before you eat.
  • If you have difficulty sleeping, ensure that the last dose of your daily medication is taken before 6 p.m.
  • Take a chewable tablet and 8 ounces of water.
• The extended-release capsule (Aptensio XR. Jornay PM. Metadate CD. Ritalin LA).
  • Use with or without food
  • Administer Aptensio XR and Metadate CD in the morning, and Jornay PM at night between 6:30 and 9:30 pm.
  • You can also open capsules and sprinkle the contents onto small amounts (equal to 1 teaspoon) of applesauce.
  • Take the applesauce mixture and swallow it immediately, without chewing.
  • Do not crush, chew or split capsule contents.
• Extended-release, orally disintegrating tablet (CotemplaXR-ODT).
  • Take the tablet every morning with or without food. Take the tablet out of the blister pack using dry hands. Peel back the foil (but don't push it through the foil) and then administer immediately.
  • You can let the tablet dissolve on your tongue, without having to chew or crush it.
• Extended-release suspension (QuillivantXR)
  • Take the medication in the morning, with or without food. Before administering, shake the bottle for at least 10 seconds. Wash the container after each use with the oral dosing device provided.
• Extended-release chewable tablet (QuilliChew ERR):
  • Take the tablet in the morning, with or without food. You can cut the tablets in half.
• Extended-release tablet Metadate ER
  • Take the tablet 30 to 45 minutes before you eat. Take the entire tablet and swallow it with water or another fluid. Do not chew, crush or chew the tablet.
• Concerta
  • Take it in the morning. You can take it with or without food, but you should drink water or another fluid. Do not crush, chew or divide the tablets.
• Sustained-release tablet, (Ritalin SR):
  • Take the tablet whole and swallow it.

Topical Methylphenidate

• Transdermal (Daytrana).
  • Apply clean, dry, and intact skin to the hips, avoiding the waistline.
  • Pre-treatment of the patch should not include hydrocortisone, other solutions, creams or ointments.
  • To alternate hips, apply the same technique every day.
  • To ensure proper adhesion, press down for 30 seconds.
  • Avoid exposing the application site to heat sources outside, as this could increase drug absorption.
  • If the patch is hard to separate from the liner, or if medication (a sticky substance) remains, it should be discarded and a new one applied.
  • Use a patch that is damaged or torn and do not cut it.
  • You can replace the patch if it becomes loose. However, you should not apply more than nine hours.
  • Do not reapply dressings, tape or common adhesives.
  • If the effect lasts for a shorter time or side effects are severe, you can remove the patch immediately.
  • After handling, wash your hands with soapy water.
  • Avoid touching the sticky sides of the patch.
  • To make it easier to remove patches, you can apply an oil-based product to the edges (e.g. petroleum jelly, olive oils) if they are difficult to remove.
  • Never apply acetone-based products to patch. You should dispose of the used patch by folding it on its side and putting it in a container with a lid.

Mechanism of action of Methylphenidate (Ritalin):

• Methylphenidate stimulates central nervous system by blocking the reuptake norepinephrine/dopamine into presynaptic neuronal neurons.
• It appears to stimulate the cerebral cortex as well as subcortical structures, similar to amphetamines.

The start of action

• The average time for the oral chewable tablets is between 20 and 60 minutes.
• Orally, the sustained-release tablet (Ritalin SR) can delay the onset by 60 to 180 minutes.
• 60 minutes is the minimum time it takes for Daytrana to take effect.

Maximum effect:

• It is visible within two to seven hours after the oral immediate-release tablet was taken and four to seven hours after the sustained-release tablet.

The time taken to complete an action

• The duration of the oral controlled release capsule (Foquest), is 16 hours. The extended-release capsule, Metadate CD & RitalinLA, is 6-8 hours. Aptensio XR lasts less than 16 hours.

The extended-release tablet's action time:

• (Concerta), is 8-12 hours. The immediate-release chewable tablet and oral solution, as well as the immediate-release tablet (Methylin or Ritalin), are 3 - 5 Hours.

The sustained release tablet's action time:

• The time for (Ritalin-SR), is between 2 and 8 hours, while the time for transdermal (Daytrana), is 11 to 12 hours.
• When taken orally, it is easily absorbed. It is easily absorbed when taken orally.AbsorptionThe transdermal patch's effectiveness is enhanced when it is applied to an inflamed or hot area. The drug absorbs continuously for nine hours after application.
• 10% - 33% of drug isProtein-bound. It is extensively metabolized by de-esterification.
• ThebioavailabilityBoth the oral solution and immediate-release chewable tablets are equivalent.
• Between 78 and 97 percent of the medication is eliminated in the urine either unmodified or as metabolites. Feces are used for excretion of 1% to 3%.

Methylphenidate Brand Names (International):

• Aptensio XR
• Concerta
• Cotempla XR-ODT
• Daytrana
• Metadate CD
• Metadate ER
• Methylin
• QuilliChew ER
• Quillivant XR
• Relexxii
• Ritalin
• Ritalin LAACT Methylphenidate ER
• APO-Methylphenidate
• APO-Methylphenidate ER
• APO-Methylphenidate SR
• Biphentin
• Concerta
• Foquest
• PHL-Methylphenidate HCl
• PHL-Methylphenidate
• PMS-Methylphenidate
• PMS-Methylphenidate ER
• RATIO-Methylphenidate
• Ritalin
• Ritalin SR
• SANDOZ Methylphenidate SR
• TEVA-Methylphenidate ER-C
• Adaphen
• Adaphen XL
• Addwize
• Aradix Retard
• Artige
• Attenta
• Cognil
• Comcerta
• Concentra
• Concentra SR
• Concerta
• Concerta LP
• Concerta Oros
• Delmosart
• Equasym
• Equasym Depot
• Equasym
• Retard
• Equasym XL
• Inspiral
• Matoride XL
• Medikinet
• Medikinet CR
• Medikinet MR
• Medikinet Retard
• Medikinet XL
• Metadate CD SR
• Methylin
• Methylphen
• Metidate
• MFD
• Penid
• Phenida
• Prohiper
• Quasym LP
• Rilatine
• Ritalin
• Ritalin LA
• Ritalin LP
• Ritalin SR
• Ritalin-SR
• Ritalina
• Ritalina LA
• Ritaline LP
• Rubifen
• Rubifen
• SR
• Tradea
• Tradea LP
• Xenidate XL

Methylphenidate Brand Names in Pakistan: