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Relexxii

(methylphenidate hydrochloride extended-release, OROS)

Relexxii (methylphenidate hydrochloride extended-release, OROS); CII

Full Prescribing Information DailyMed Drug Information

Summary

Relexxii is a long-acting methylphenidate tablet using the same class of OROS osmotic delivery as Concerta, approved for ADHD from age 6 through 65. Its differentiator is the strength ladder: 45 mg, 63 mg and 72 mg exist as single tablets, so a patient needing more than 54 mg takes one tablet rather than two. It is not labeled as bioequivalent to Concerta. Schedule II; brand and authorized generic.

Forms & Strengths

  • Extended-release tablets (OROS, swallow whole): 18 mg, 27 mg, 36 mg, 45 mg, 54 mg, 63 mg, 72 mg

Dosing

  • Age: 6 to 65 y/o
  • Onset: ~ 1 hour
  • Duration: up to 12 hours
  • Release Profile: 18% IR / 82% ER via OROS osmotic delivery
  • Initial Dose:
    • 6 to 17 y/o, new to methylphenidate: 18 mg once daily in the morning
    • 18 to 65 y/o, new to methylphenidate: 18 mg or 36 mg once daily in the morning
    • From methylphenidate 2-3 times daily, per dose: 5 mg to 18 mg; 10 mg to 36 mg; 15 mg to 54 mg; 20 mg to 72 mg
  • Titration: 18 mg every 7 days; 27, 45 and 63 mg give intermediate steps
  • Max Dose:
    • 6 to 12 y/o: 54 mg/day
    • 13 to 17 y/o: 72 mg/day, not to exceed 2 mg/kg/day
    • 18 to 65 y/o: 72 mg/day
  • Considerations: Swallow whole; chewing or dividing destroys the osmotic pump. The 45, 63 and 72 mg strengths avoid two-tablet regimens above 54 mg. Do not substitute milligram-for-milligram with another methylphenidate.

Pharmacology

  • Mechanism: Blocks presynaptic dopamine and norepinephrine reuptake at DAT and NET; does not meaningfully promote catecholamine release at therapeutic doses
  • Delivery / Release: 18% IR / 82% ER via OROS osmotic delivery. The overcoat dissolves within an hour, then a push layer forces drug through a laser-drilled orifice; two core layers make release rise over 6 to 7 hours.
  • Metabolism: De-esterified to PPAA (ritalinic acid), inactive. Half-life ~3.5 hours, ~90% recovered in urine. Renal impairment has little effect.
  • Class Positioning: Same osmotic principle as Concerta, not the same product: 18% against 22% immediate fraction, Tmax 5.5 h against 6 to 10 h, no bioequivalence study. Advantage: single-tablet dosing at 45, 63 and 72 mg.

Indications

  • ADHD (ICD-10: F90.0, F90.1, F90.2, F90.8, F90.9): patients 6 to 65 y/o

Off-Label Uses

  • ADHD in children 4 to 5 years old (ICD-10: F90.x): behavioral parent training first line; if medication is needed use IR methylphenidate, not OROS. Expert consensus. (AAP 2019)
  • Narcolepsy (ICD-10: G47.419): IR methylphenidate carries this indication, Relexxii does not. Insufficient.
  • Substituting for Concerta at the same strength: common at 18 to 54 mg but unsupported by any bioequivalence study. Recheck response after a switch. Insufficient.
  • Where the evidence does not support use: treatment-resistant depression, binge eating disorder, cancer-related and chronic fatigue. Adult literature only; insufficient in children. (AHRQ 2024)
  • Cognitive enhancement in a youth without ADHD: not an indication and not supported.

Contraindications & Warnings

  • Boxed Warning: Abuse, misuse and addiction, with overdose and death. Assess abuse risk before prescribing and reassess throughout treatment.
  • Contraindicated:
    • Hypersensitivity to methylphenidate; angioedema and anaphylaxis reported
    • MAOI use, current or within 14 days: hypertensive crisis
  • Use with caution:
    • Structural cardiac abnormality, cardiomyopathy, arrhythmia or coronary disease: avoid
    • Pre-existing hypertension: monitor blood pressure and pulse
    • Psychotic or bipolar disorder: exacerbation and treatment-emergent mania
    • GI narrowing: the tablet is nondeformable
    • Significant hyperopia or angle-closure risk: refer to ophthalmology
    • Personal or family history of tics or Tourette's syndrome
    • Substance use disorder in the patient or the household
  • Screen before starting:
    • Cardiac history and exam including family sudden death; the label requires no routine ECG
    • Tics, and risk factors for a manic episode
    • Abuse and diversion risk in patient and household
    • Ability to swallow a tablet whole; any GI stricture or bowel surgery
    • Baseline height, weight, blood pressure and heart rate

Drug Interactions

  • MAOIs (phenelzine, tranylcypromine, selegiline, linezolid, methylene blue): hypertensive crisis. Contraindicated within 14 days.
  • Antihypertensives: effectiveness reduced. Increase BP monitoring and adjust the antihypertensive.
  • Halogenated anesthetics (sevoflurane, isoflurane, desflurane): intraoperative BP and HR surge. Hold on the day of surgery.
  • Risperidone: EPS may increase when either dose changes in either direction. Monitor across any titration.
  • Serotonergic agents (SSRIs, SNRIs, TCAs, triptans, tramadol): serotonin syndrome in postmarketing reports only, not in the interaction table. Counsel on symptoms.

Administration

  • Once daily in the morning, with or without food.
  • Swallow whole. Do not chew, divide or crush; there is no sprinkle option.
  • If the child cannot swallow a tablet, use a bead capsule (Ritalin LA) or a liquid (Quillivant XR).
  • The intact shell passes in the stool; warn the family before the first dose.
  • Never substitute milligram-for-milligram; use the labeled conversion table and recheck response after any switch.
  • Missed dose: skip it rather than giving it late in the day.
  • Store locked; the 63 and 72 mg strengths are high-value diversion targets.

Side Effects

  • Common, pediatric 6 to 17 y: upper abdominal pain, the only reaction above 5%; insomnia, nasopharyngitis, vomiting, pyrexia 2% to 3%.
  • Common, adults (all above 5%): decreased appetite, headache, dry mouth, nausea, insomnia, anxiety, dizziness, weight loss, irritability, hyperhidrosis.
  • Serious:
    • Sudden death with structural cardiac disease: avoid the drug in that population
    • New psychosis or mania, including with no psychiatric history: consider discontinuing
    • Priapism, sometimes surgical, typically after a dose increase and also during drug holidays
    • Peripheral vasculopathy and Raynaud's with digital ulceration: assess digits each visit
    • Long-term growth suppression; GI obstruction from the nondeformable tablet in pre-existing narrowing
    • Acute angle closure glaucoma; new or worsening tics and Tourette's
    • Postmarketing: convulsion, dyskinesia, serotonin syndrome, hypersensitivity reactions

Monitoring & Labs

  • Cardiovascular: BP and HR at baseline, at every dose change, and at least every 6 months.
  • Growth: height, weight and BMI at baseline and every 6 months; failure to gain triggers interruption.
  • Appetite and sleep: at every visit and dose change; the usual reasons titration stalls short of 72 mg.
  • Psychiatric and tics: screen for psychosis, mania, aggression, depressed mood and tics at baseline and every visit.
  • Abuse and diversion: at every refill, pill count, ask about sharing and selling, check the PDMP. A boxed-warning obligation.
  • Dose ceiling: at every titration step in a 13 to 17 year old, recalculate 2 mg/kg/day. Under 36 kg the weight cap bites before the 72 mg cap.
  • Laboratory: none is required by this label.

Discontinuation & Taper

  • No taper required; the label gives no tapering schedule.
  • Discontinue if no improvement after appropriate dose adjustment over one month.
  • Withdrawal after prolonged use: dysphoria, fatigue, vivid dreams, sleep change, increased appetite.
  • Priapism has occurred during drug holidays and on discontinuation.
  • Drug holidays are reasonable where growth or appetite limits treatment; an interrupted day is fully unmedicated.

Pregnancy & Lactation

  • Pregnancy: no drug-associated risk of major birth defects or miscarriage identified. Stimulant vasoconstriction may reduce placental perfusion. Background risk 2% to 4% and 15% to 20%. Weigh against untreated maternal ADHD.
  • Lactation: infant dose 0.16% to 0.7% of the maternal weight-adjusted dose; undetectable in infant serum in every reported case, including 72 mg daily. Not a reason to stop breastfeeding. (LactMed 2025)
  • Lactation, milk supply: prolactin falls; large doses may interfere before supply is established. Monitor the infant for agitation, anorexia and poor weight gain. (LactMed 2025)
  • Exposure Registry: National Pregnancy Registry for ADHD Medications, 1-866-961-2388.

Counseling Points

  • Counsel the family on:

    • Relexxii and Concerta not being the same tablet even where milligrams match; watch the first week after a substitution.
    • The 45, 63 and 72 mg strengths being the reason for this product: one tablet replaces two.
    • Seeing the intact shell in the stool; it is the spent pump, not a wasted dose.
    • Half a 45 mg tablet being a broken osmotic pump, not 22.5 mg.
    • Dosing at the same early hour daily; a late dose pushes the ascending peak into the evening.
    • Moving the largest meal to breakfast and the evening, when appetite returns.
    • Locked storage; the high strengths are the ones peers ask for.

  • Advise them to call for:

    • Chest pain, fainting, or a racing heart that does not settle.
    • New hallucinations, or new suspicious or fearful thinking.
    • Numbness, coldness or colour change in fingers or toes.
    • A new or markedly worse tic.
    • A painful erection lasting more than a few hours; a surgical emergency.
    • Severe abdominal pain or vomiting, especially with any history of bowel narrowing.
    • Eye pain with blurred vision or halos around lights.
    • Clothes fitting more loosely, or no weight gain across a few months.

References

  1. DailyMed. Relexxii (methylphenidate hydrochloride) extended-release tablets prescribing information. Vertical Pharmaceuticals. 2025. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=22d5fa47-b5b9-4fd9-980c-4eb88e95ae5d
  2. DailyMed. Concerta (methylphenidate hydrochloride) extended-release tablets prescribing information. Janssen Pharmaceuticals. 2026. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1a88218c-5b18-4220-8f56-526de1a276cd
  3. FDA. openFDA National Drug Code Directory, generic_name methylphenidate. 2026. https://api.fda.gov/drug/ndc.json?search=generic_name:%22methylphenidate%22&limit=1000
  4. LactMed. Methylphenidate. Drugs and Lactation Database, NICHD. 2025. https://www.ncbi.nlm.nih.gov/books/NBK501310/
  5. American Academy of Pediatrics. Clinical practice guideline for the diagnosis, evaluation, and treatment of ADHD in children and adolescents. Pediatrics. 2019. https://publications.aap.org/pediatrics/article/144/4/e20192528/81590/
  6. AHRQ. Attention deficit hyperactivity disorder: diagnosis and treatment in children and adolescents. Comparative Effectiveness Review No. 267. 2024. https://www.ncbi.nlm.nih.gov/books/NBK602989/
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