Ritalin

— THERAPEUTIC CATEGORIES —
  • ADHD
  • Sleep-wake disorders

Ritalin Generic Name & Formulations

General Description

Methylphenidate HCl 5mg, 10mg+, 20mg+; tabs; +scored.

Pharmacological Class

CNS stimulant.

See Also

How Supplied

Caps, tabs—100

How Supplied

Ritalin Tablets is supplied in bottles of 100 in the following strengths:

  • 5 mg: round, yellow, imprinted “CIBA 7”

  • 10 mg: round, pale green, scored, imprinted “CIBA 3”

  • 20 mg: round, pale yellow, scored, imprinted “CIBA 34”

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP controlled room temperature]. Protect from light. Dispense in tight, light-resistant container (USP).  

Generic Availability

YES

Mechanism of Action

The mechanism of action of methylphenidate is not completely understood, but it presumably activates the brain stem arousal system and cortex to produce its stimulant effect. Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.

Ritalin Indications

Indications

Attention deficit hyperactivity disorder.

Ritalin Dosage and Administration

Prior to Treatment Evaluations

Assess for the presence of cardiac disease (eg, a careful history, family history of sudden death or ventricular arrhythmia, and physical exam).

Assess the risk of abuse. After prescribing, keep prescription records, educate patients about abuse, monitor for signs of abuse and overdose, and re-evaluate the need for Ritalin use.

Adult

Give in 2–3 divided doses preferably 30–45mins before meals. Usual dose: 20–30mg/day. Max 60mg/day.

Children

<6yrs: not established. ≥6yrs: initially 5mg twice daily before breakfast and lunch. May increase by 5–10mg weekly; max 60mg/day.

Adults and Children

General Dosing Information

  • <6yrs: not established. Swallow whole or sprinkle contents onto applesauce (swallow immediately); do not crush, chew, or divide beads. 

  • ≥6yrs: initially 20mg once daily in the AM, may increase by 10mg weekly; max 60mg/day. 

  • Switching from other methylphenidate products: see full labeling.

Patients Currently Using Ritalin 

  • Previous or current Ritalin Dose of 5 mg twice daily → Recommended Ritalin LA Dose of 10 mg once daily.

  • Previous or current Ritalin Dose of 10 mg twice daily → Recommended Ritalin LA Dose of 20 mg once daily.

  • Previous or current Ritalin Dose of 15 mg twice daily → Recommended Ritalin LA Dose of 30 mg once daily.

  • Previous or current Ritalin Dose of 20 mg twice daily → Recommended Ritalin LA Dose of 40 mg once daily.

  • Previous or current Ritalin Dose of 30 mg twice daily → Recommended Ritalin LA Dose of 60 mg once daily.

Switching from other Methylphenidate Products

  • If switching from other methylphenidate products, discontinue that treatment, and titrate with Ritalin LA using the titration schedule.

  • Do not substitute on a mg-per-mg basis with other methylphenidate products.

  • Do not exceed daily dosage of 60 mg.

Ritalin Contraindications

Contraindications

During or within 14 days of MAOIs.

Ritalin Boxed Warnings

Boxed Warning

Abuse, misuse, and addiction.

Boxed Warning

Abuse and Dependence

  • High potential for abuse and dependence.

  • Assess the risk of abuse prior to prescribing and monitor during therapy.

Ritalin Warnings/Precautions

Warnings/Precautions

High potential for abuse, misuse, and addiction; assess patient’s risk before prescribing. Assess for presence of cardiac disease before initiating. Avoid in known structural cardiac abnormalities, cardiomyopathy, serious arrhythmias, coronary artery disease, or other cardiac disease. Pre-existing psychotic disorder. Bipolar disorder. Screen for risk factors of developing a manic episode prior to initiation. Consider discontinuing if new psychotic/manic symptoms occur. Risk for acute angle glaucoma. History of increased IOP or open angle glaucoma; monitor closely. Assess family history and evaluate for tics or Tourette’s syndrome before initiating; monitor for emergence or worsening, and discontinue if clinically appropriate. Peripheral vasculopathy, including Raynaud's Phenomenon; monitor for digital changes. Monitor BP, HR, growth in children. Reduce dose or discontinue if paradoxical aggravation of symptoms occur. Reevaluate periodically. Pregnancy. Nursing mothers: monitor infants.

Warnings/Precautions

Potential for Abuse and Dependence 

  • High potential for abuse and dependence.

  • Assess the risk of abuse prior to prescribing and monitor during therapy.

Serious Cardiovascular Reactions 

  • Sudden death, stroke, and myocardial infarction have been reported in adults receiving CNS stimulants. Sudden death has been reported in pediatric patients with structural cardiac abnormalities and other serious heart problems receiving CNS stimulants.

  • Avoid use in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, coronary artery disease, and other serious heart problems.

  • Evaluate further if exertional chest pain, unexplained syncope, or arrhythmias develop during treatment.

Blood Pressure and Heart Rate Increases

  • Monitor all patients for potential tachycardia and hypertension.

Psychiatric Adverse Reactions

  • Exacerbation of pre-existing psychosis: May exacerbate symptoms of behavior disturbance and thought disorders in patients with pre-existing psychotic behavior.

  • Induction of a manic episode in patients with bipolar disorder: May induce a mixed/manic episode in patients with bipolar disorder. Screen for risk factors for developing a manic episode prior to treatment (eg, comorbid or history of depressive symptoms or a family history of suicide, bipolar disorder, and depression).

  • New psychotic or manic symptoms: May cause psychotic or manic symptoms in patients without a history of psychotic illness or mania. Consider discontinuing if symptoms occur.

Priapism

  • Prolonged and painful erections, sometimes requiring surgical intervention, have been reported.

  • Priapism has not been reported during drug initiation but developed after some time on the drug.

  • Seek immediate medical attention if priapism occurs.

Peripheral Vasculopathy, including Raynaud’s Phenomenon

  • Signs and symptoms are usually intermittent and mild; very rare sequelae include digital ulceration and/or soft tissue breakdown.

  • These signs and symptoms generally improve after reduction in dose or discontinuation.

  • Observe carefully for digital changes during treatment. Evaluate further (eg, rheumatology referral) for certain patients.

Suppression of Growth 

  • In pediatric patients, closely monitor growth (weight and height).

  • May need to interrupt treatment in patients who are not growing or gaining height or weight as expected.

Pregnancy Considerations

Pregnancy Exposure Registry 

  • There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ADHD medications, including Ritalin, during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for ADHD Medications at 1-866-961-2388 or visit https://womensmentalhealth.org/adhd-medications/.

Risk Summary

  • Use in pregnant women have not identified a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes. 

  • The estimated background risk of major birth defects and miscarriage is unknown.

Clinical Considerations

  • Fetal/Neonatal Adverse Reactions: May cause vasoconstriction and may decrease placental perfusion. No fetal and/or neonatal adverse reactions have been reported, but premature delivery and low birth weight infants have been reported in amphetamine-dependent mothers. 

Nursing Mother Considerations

Risk Summary  

  • Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for Ritalin and any potential adverse effects on the breastfed infant from Ritalin or from the underlying maternal condition. 

Clinical Considerations

  • Monitor breastfeeding infants for adverse reactions, such as agitation, insomnia, anorexia, and reduced weight gain.

Pediatric Considerations

The safety and efficacy of Ritalin in pediatric patients <6 years have not been established.

The long-term efficacy of Ritalin in pediatric patients has not been established.

Long-Term Suppression of Growth: Monitor growth during treatment with stimulants, including Ritalin. May need to interrupt treatment in pediatric patients who are not growing or gaining weight as expected.

Geriatric Considerations

Ritalin has not been studied in the geriatric population.

Ritalin Pharmacokinetics

Absorption

The time to peak rate in children was 1.9 hours (0.3–4.4 hours) for the Ritalin tablets.

Distribution

Plasma protein bound: 10–33%. 

The volume of distribution was 2.65 ± 1.11 L/kg for d- methylphenidate and 1.80 ± 0.91 L/kg for l-methylphenidate.

Metabolism

Methylphenidate is metabolized primarily by de-esterification to alpha-phenyl-piperidine acetic acid (ritalinic acid), which has little or no pharmacologic activity.

Elimination

After oral administration, 78% to 97% of the dose is excreted in the urine and 1% to 3% in feces in the form of metabolites within 48–96 hours.

Most of the dose is excreted in the urine as alpha-phenyl-2-piperidine acetic acid (60% to 86%).

Ritalin Interactions

Interactions

See Contraindications. Hypertensive crisis with MAOIs. May antagonize antihypertensive drugs (eg, K+-sparing or thiazide diuretics, CCBs, ACE inhibitors, ARBs, beta blockers, centrally acting alpha-2 receptor agonists); monitor and adjust dose of antihypertensives as needed. Concomitant halogenated anesthetics may increase the risk of sudden BP and HR increase during surgery; avoid use. Concomitant risperidone may increase risk of extrapyramidal symptoms; monitor.

Ritalin Adverse Reactions

Adverse Reactions

Headache, insomnia, abdominal pain, decreased appetite, anorexia, tachycardia, palpitations, anxiety, hyperhidrosis, weight loss, dry mouth, nausea; priapism, hypertension, glaucoma, motor/verbal tics.

Ritalin Clinical Trials

Clinical Trials

Children and Adolescents

  • Approval of Ritalin LA was based on a randomized, double-blind, placebo-controlled, parallel group clinical study in 134 children ages 6 to 12 with DSM-IV diagnoses of ADHD. Patients received a single morning dose of Ritalin LA 10 to 40 mg/day or placebo for up to 2 weeks.

  • The patient’s regular schoolteacher completed the Conners ADHD/DSM-IV Scale for Teachers (CADS-T) at baseline and the end of each week. The CADS-T assesses symptoms of hyperactivity and inattention. The change from baseline of the (CADS-T) scores during the last week of treatment was analyzed as the primary efficacy parameter.

  • Ritalin LA achieved a statistically significant improvement in symptom scores from baseline (-10.7 points) compared with placebo (+2.8 points).

Ritalin Note

Not Applicable

Ritalin Patient Counseling

Patient Counseling

Controlled Substance Status/High Potential for Abuse and Dependence

  • Advise patients that Ritalin can be abused and lead to dependence. Do not give Ritalin to anyone else. Store Ritalin in a safe place, preferably locked, to prevent abuse.

Serious Cardiovascular Risks

  • Advise patients that there is a potential serious cardiovascular risk, including sudden death, myocardial infarction, stroke, and hypertension with Ritalin use. Contact healthcare provider if patients experience symptoms, such as exertional chest pain, unexplained syncope, or other symptoms suggestive of cardiac disease.

Blood Pressure and Heart Rate Increases 

  • May cause elevations to blood pressure and pulse rate.

Psychiatric Risks

  • May cause psychotic or manic symptoms, even in patients without prior history of psychotic symptoms or mania.

Priapism

  • May cause painful or prolonged penile erections. Seek immediate medical attention in the event of priapism.

Circulation Problems in Fingers and Toes [Peripheral Vasculopathy, Including Raynaud’s Phenomenon] 

  • May cause peripheral vasculopathy, including Raynaud’s phenomenon, and associated signs and symptoms: fingers or toes may feel numb, cool, painful, and/or may change color from pale, to blue, to red. Instruct patients to report to their physician any new numbness, pain, skin color change, or sensitivity to temperature in fingers or toes. 

  • Contact physician immediately if any signs of unexplained wounds appear on fingers or toes during treatment.

Suppression of Growth

  • May cause slowing of growth and weight loss.

Pregnancy Registry

  • Advise patients that there is a pregnancy exposure registry that monitors pregnancy outcomes in patients exposed to ADHD medications, including Ritalin, during pregnancy.

Ritalin Generic Name & Formulations

General Description

Methylphenidate HCl 5mg, 10mg+, 20mg+; tabs; +scored.

Pharmacological Class

CNS stimulant.

See Also

    How Supplied

    Tabs—100

    How Supplied

    Ritalin Tablets are supplied in bottles of 100 in the following strengths:

    • 5 mg: round, yellow, imprinted “CIBA 7”

    • 10 mg: round, pale green, scored (imprinted “CIBA 3”)

    • 20 mg: round, pale yellow, scored (imprinted “CIBA 34”)

    Storage

    Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP controlled room temperature]. Protect from light. Dispense in tight, light-resistant container (USP).  

    Generic Availability

    YES

    Mechanism of Action

    The mechanism of action of methylphenidate is not completely understood, but it presumably activates the brain stem arousal system and cortex to produce its stimulant effect. Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.

    Ritalin Indications

    Indications

    Narcolepsy.

    Ritalin Dosage and Administration

    Prior to Treatment Evaluations

    Assess for the presence of cardiac disease (eg, a careful history, family history of sudden death or ventricular arrhythmia, and physical exam).

    Assess the risk of abuse. After prescribing, keep prescription records, educate patients about abuse, monitor for signs of abuse and overdose, and re-evaluate the need for Ritalin use.

    Adult

    Give in 2–3 divided doses preferably 30–45mins before meals. Usual dose: 20–30mg/day. Max 60mg/day.

    Children

    <6yrs: not established. ≥6yrs: initially 5mg twice daily before breakfast and lunch. May increase by 5–10mg weekly; max 60mg/day.

    Adults and Children

    General Dosing Information

    • <6yrs: not established. Swallow whole or sprinkle contents onto applesauce (swallow immediately); do not crush, chew, or divide beads. 

    • ≥6yrs: initially 20mg once daily in the AM, may increase by 10mg weekly; max 60mg/day. 

    • Switching from other methylphenidate products: see full labeling.

    Patients Currently Using Ritalin 

    • Previous or current Ritalin Dose of 5 mg twice daily → Recommended Ritalin LA Dose of 10 mg once daily.

    • Previous or current Ritalin Dose of 10 mg twice daily → Recommended Ritalin LA Dose of 20 mg once daily.

    • Previous or current Ritalin Dose of 15 mg twice daily → Recommended Ritalin LA Dose of 30 mg once daily.

    • Previous or current Ritalin Dose of 20 mg twice daily → Recommended Ritalin LA Dose of 40 mg once daily.

    • Previous or current Ritalin Dose of 30 mg twice daily → Recommended Ritalin LA Dose of 60 mg once daily.

    Switching from other Methylphenidate Products

    • If switching from other methylphenidate products, discontinue that treatment, and titrate with Ritalin LA using the titration schedule.

    • Do not substitute on a mg-per-mg basis with other methylphenidate products.

    • Do not exceed daily dosage of 60 mg.

    Ritalin Contraindications

    Contraindications

    During or within 14 days of MAOIs.

    Ritalin Boxed Warnings

    Boxed Warning

    Abuse, misuse, and addiction.

    Boxed Warning

    Abuse and Dependence

    • High potential for abuse and dependence.

    • Assess the risk of abuse prior to prescribing and monitor during therapy.

    Ritalin Warnings/Precautions

    Warnings/Precautions

    High potential for abuse, misuse, and addiction; assess patient’s risk before prescribing. Assess for presence of cardiac disease before initiating. Avoid in known structural cardiac abnormalities, cardiomyopathy, serious arrhythmias, coronary artery disease, or other cardiac disease. Pre-existing psychotic disorder. Bipolar disorder. Screen for risk factors of developing a manic episode prior to initiation. Consider discontinuing if new psychotic/manic symptoms occur. Risk for acute angle glaucoma. History of increased IOP or open angle glaucoma; monitor closely. Assess family history and evaluate for tics or Tourette’s syndrome before initiating; monitor for emergence or worsening, and discontinue if clinically appropriate. Peripheral vasculopathy, including Raynaud's Phenomenon; monitor for digital changes. Monitor BP, HR, growth in children. Reduce dose or discontinue if paradoxical aggravation of symptoms occur. Reevaluate periodically. Pregnancy. Nursing mothers: monitor infants.

    Warnings/Precautions

    Potential for Abuse and Dependence 

    • High potential for abuse and dependence.

    • Assess the risk of abuse prior to prescribing and monitor during therapy.

    Serious Cardiovascular Reactions 

    • Sudden death, stroke, and myocardial infarction have been reported in adults receiving CNS stimulants. Sudden death has been reported in pediatric patients with structural cardiac abnormalities and other serious heart problems receiving CNS stimulants.

    • Avoid use in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, coronary artery disease, and other serious heart problems.

    • Evaluate further if exertional chest pain, unexplained syncope, or arrhythmias develop during treatment.

    Blood Pressure and Heart Rate Increases

    • Monitor all patients for potential tachycardia and hypertension.

    Psychiatric Adverse Reactions

    • Exacerbation of pre-existing psychosis: May exacerbate symptoms of behavior disturbance and thought disorders in patients with pre-existing psychotic behavior.

    • Induction of a manic episode in patients with bipolar disorder: May induce a mixed/manic episode in patients with bipolar disorder. Screen for risk factors for developing a manic episode prior to treatment (eg, comorbid or history of depressive symptoms or a family history of suicide, bipolar disorder, and depression).

    • New psychotic or manic symptoms: May cause psychotic or manic symptoms in patients without a history of psychotic illness or mania. Consider discontinuing if symptoms occur.

    Priapism

    • Prolonged and painful erections, sometimes requiring surgical intervention, have been reported.

    • Priapism has not been reported during drug initiation but developed after some time on the drug.

    • Seek immediate medical attention if priapism occurs.

    Peripheral Vasculopathy, including Raynaud’s Phenomenon

    • Signs and symptoms are usually intermittent and mild; very rare sequelae include digital ulceration and/or soft tissue breakdown.

    • These signs and symptoms generally improve after reduction in dose or discontinuation.

    • Observe carefully for digital changes during treatment. Evaluate further (eg, rheumatology referral) for certain patients.

    Suppression of Growth 

    • In pediatric patients, closely monitor growth (weight and height).

    • May need to interrupt treatment in patients who are not growing or gaining height or weight as expected.

    Pregnancy Considerations

    Pregnancy Exposure Registry 

    • There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ADHD medications, including Ritalin, during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for ADHD Medications at 1-866-961-2388 or visit https://womensmentalhealth.org/adhd-medications/.

    Risk Summary

    • Use in pregnant women have not identified a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes. 

    • The estimated background risk of major birth defects and miscarriage is unknown.

    Clinical Considerations

    • Fetal/Neonatal Adverse Reactions: May cause vasoconstriction and may decrease placental perfusion. No fetal and/or neonatal adverse reactions have been reported, but premature delivery and low birth weight infants have been reported in amphetamine-dependent mothers. 

    Nursing Mother Considerations

    Risk Summary  

    • Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for Ritalin and any potential adverse effects on the breastfed infant from Ritalin or from the underlying maternal condition. 

    Clinical Considerations

    • Monitor breastfeeding infants for adverse reactions, such as agitation, insomnia, anorexia, and reduced weight gain.

    Pediatric Considerations

    The safety and efficacy of Ritalin in pediatric patients <6 years have not been established.

    The long-term efficacy of Ritalin in pediatric patients has not been established.

    Long-Term Suppression of Growth: Monitor growth during treatment with stimulants, including Ritalin. May need to interrupt treatment in pediatric patients who are not growing or gaining weight as expected.

    Geriatric Considerations

    Ritalin has not been studied in the geriatric population.

    Ritalin Pharmacokinetics

    Absorption

    The time to peak rate in children was 1.9 hours (0.3–4.4 hours) for the Ritalin tablets.

    Distribution

    Plasma protein bound: 10–33%. 

    The volume of distribution was 2.65 ± 1.11 L/kg for d- methylphenidate and 1.80 ± 0.91 L/kg for l-methylphenidate.

    Metabolism

    Methylphenidate is metabolized primarily by de-esterification to alpha-phenyl-piperidine acetic acid (ritalinic acid), which has little or no pharmacologic activity.

    Elimination

    After oral administration, 78% to 97% of the dose is excreted in the urine and 1% to 3% in feces in the form of metabolites within 48–96 hours.

    Most of the dose is excreted in the urine as alpha-phenyl-2-piperidine acetic acid (60% to 86%).

    Ritalin Interactions

    Interactions

    See Contraindications. Hypertensive crisis with MAOIs. May antagonize antihypertensive drugs (eg, K+-sparing or thiazide diuretics, CCBs, ACE inhibitors, ARBs, beta blockers, centrally acting alpha-2 receptor agonists); monitor and adjust dose of antihypertensives as needed. Concomitant halogenated anesthetics may increase the risk of sudden BP and HR increase during surgery; avoid use. Concomitant risperidone may increase risk of extrapyramidal symptoms; monitor.

    Ritalin Adverse Reactions

    Adverse Reactions

    Headache, insomnia, abdominal pain, decreased appetite, anorexia, tachycardia, palpitations, anxiety, hyperhidrosis, weight loss, dry mouth, nausea; priapism, hypertension, glaucoma, motor/verbal tics.

    Ritalin Clinical Trials

    Clinical Trials

    Children and Adolescents

    • Approval of Ritalin LA was based on a randomized, double-blind, placebo-controlled, parallel group clinical study in 134 children ages 6 to 12 with DSM-IV diagnoses of ADHD. Patients received a single morning dose of Ritalin LA 10 to 40 mg/day or placebo for up to 2 weeks.

    • The patient’s regular schoolteacher completed the Conners ADHD/DSM-IV Scale for Teachers (CADS-T) at baseline and the end of each week. The CADS-T assesses symptoms of hyperactivity and inattention. The change from baseline of the (CADS-T) scores during the last week of treatment was analyzed as the primary efficacy parameter.

    • Ritalin LA achieved a statistically significant improvement in symptom scores from baseline (-10.7 points) compared with placebo (+2.8 points).

    Ritalin Note

    Not Applicable

    Ritalin Patient Counseling

    Patient Counseling

    Controlled Substance Status/High Potential for Abuse and Dependence

    • Advise patients that Ritalin can be abused and lead to dependence. Do not give Ritalin to anyone else. Store Ritalin in a safe place, preferably locked, to prevent abuse.

    Serious Cardiovascular Risks

    • Advise patients that there is a potential serious cardiovascular risk, including sudden death, myocardial infarction, stroke, and hypertension with Ritalin use. Contact healthcare provider if patients experience symptoms, such as exertional chest pain, unexplained syncope, or other symptoms suggestive of cardiac disease.

    Blood Pressure and Heart Rate Increases 

    • May cause elevations to blood pressure and pulse rate.

    Psychiatric Risks

    • May cause psychotic or manic symptoms, even in patients without prior history of psychotic symptoms or mania.

    Priapism

    • May cause painful or prolonged penile erections. Seek immediate medical attention in the event of priapism.

    Circulation Problems in Fingers and Toes [Peripheral Vasculopathy, Including Raynaud’s Phenomenon] 

    • May cause peripheral vasculopathy, including Raynaud’s phenomenon, and associated signs and symptoms: fingers or toes may feel numb, cool, painful, and/or may change color from pale, to blue, to red. Instruct patients to report to their physician any new numbness, pain, skin color change, or sensitivity to temperature in fingers or toes. 

    • Contact physician immediately if any signs of unexplained wounds appear on fingers or toes during treatment.

    Suppression of Growth

    • May cause slowing of growth and weight loss.

    Pregnancy Registry

    • Advise patients that there is a pregnancy exposure registry that monitors pregnancy outcomes in patients exposed to ADHD medications, including Ritalin, during pregnancy.

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