serdexmethylphenidate/dexmethylphenidate (Rx)

Brand and Other Names:Azstarys
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

serdexmethylphenidate/dexmethylphenidate

capsule: Schedule II

  • 26.1mg/5.2mg
  • 39.2mg/7.8mg
  • 52.3mg/10.4mg
  • Dexmethylphenidate is a Schedule II controlled substance; controlled substance schedule pending for serdexmethylphenidate

Attention Deficit Hyperactivity Disorder

Indicated for attention-deficit hyperactivity disorder (ADHD)

Initial: 39.2 mg/7.8 mg PO qAM

After 1 week: Increase to 52.3 mg/10.4 mg PO qAM

Not to exceed 52.3 mg/10.4 mg PO qAM

Dosage Modifications

Renal impairment

  • No experience with use in renal impairment
  • Since renal clearance is not an important route of serdexmethylphenidate or methylphenidate elimination, renal impairment is expected to have little effect on the pharmacokinetics

Hepatic impairment

  • No experience with use in hepatic impairment

Dosing Considerations

Pretreatment screening

  • Assess for presence of cardiac disease by performing careful history, family history of sudden death or ventricular arrhythmia, and physical examination
  • Assess risk for abuse and dependence before prescribing and while on therapy; maintain careful prescription records, educate patients about abuse, monitor for signs of abuse and overdose, and periodically reevaluate need for long-term use
  • Screen for preexisting psychosis (eg, behavior disturbance, thought disorder, manic or mixed mood disorder)

Dosage Forms & Strengths

serdexmethylphenidate/dexmethylphenidate

capsule: Schedule II

  • 26.1mg/5.2mg
  • 39.2mg/7.8mg
  • 52.3mg/10.4mg
  • Dexmethylphenidate is a Schedule II controlled substance; controlled substance schedule pending for serdexmethylphenidate

Attention Deficit Hyperactivity Disorder

Indicated for attention-deficit hyperactivity disorder (ADHD) in patients aged ≥6 years

<6 years: Safety and efficacy not established

6-12 years

  • Initial: 39.2 mg/7.8 mg PO qAM
  • After 1 week: May increase to 52.3 mg/10.4 mg PO qAM OR decrease to 26.1 mg/5.2 PO qAM, depending on response and tolerability
  • Not to exceed 52.3 mg/10.4 mg PO qAM

13-17 years

  • Initial: 39.2 mg/7.8 mg PO qAM
  • After 1 week: Increase to 52.3 mg/10.4 mg PO qAM
  • Not to exceed 52.3 mg/10.4 mg PO qAM

Dosage Modifications

Renal impairment

  • No experience with use in renal impairment
  • Since renal clearance is not an important route of serdexmethylphenidate or methylphenidate elimination, renal impairment is expected to have little effect on the pharmacokinetics

Hepatic impairment

  • No experience with use in hepatic impairment

Dosing Considerations

Pretreatment screening

  • Assess for presence of cardiac disease by performing careful history, family history of sudden death or ventricular arrhythmia, and physical examination
  • Assess risk for abuse and dependence before prescribing and while on therapy; maintain careful prescription records, educate patients about abuse, monitor for signs of abuse and overdose, and periodically reevaluate need for long-term use
  • Screen for preexisting psychosis (eg, behavior disturbance, thought disorder, manic or mixed mood disorder)
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Interactions

Interaction Checker

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                    Adverse Effects

                    ≥5%

                    Clinical trials with other methylphenidate products in pediatric and adult patients with ADHD commonly reported (≥5% and at least twice the rate of placebo) the following:

                    Decreased appetite

                    Decreased weight

                    Nausea

                    Abdominal pain

                    Dyspepsia

                    Vomiting

                    Insomnia

                    Anxiety

                    Affect lability

                    Irritability

                    Dizziness

                    Increased blood pressure

                    Tachycardia

                    Postmarketing Reports

                    Blood and lymphatic system disorders: Pancytopenia, thrombocytopenia, thrombocytopenic purpura

                    Cardiac disorders: Angina pectoris, bradycardia, extrasystole, supraventricular tachycardia, ventricular extrasystole, palpitations, increased heart rate

                    Eye disorders: Diplopia, mydriasis, visual impairment, blurred vision

                    General disorders: Chest pain, chest discomfort, hyperpyrexia

                    Gastrointestinal disorders: Dry mouth

                    Hepatobiliary disorders: Hepatocellular injury, acute hepatic failure

                    Immune system disorders: Hypersensitivity reactions such as angioedema, anaphylactic reactions, auricular swelling, bullous conditions, exfoliative conditions, urticaria, pruritus, rashes, eruptions, and exanthemas

                    Investigations: Alkaline phosphatase increased, bilirubin increased, hepatic enzyme increased, platelet count decreased, white blood cell count abnormal

                    Musculoskeletal, connective-tissue and bone disorders: Arthralgia, myalgia, muscle twitching, rhabdomyolysis, muscle cramps

                    Nervous system: Convulsion, grand mal convulsion, dyskinesia, serotonin syndrome in combination with serotonergic drugs, nervousness, headache, tremor, drowsiness, vertigo

                    Psychiatric disorders: Disorientation, libido changes, hallucination, hallucination auditory, hallucination visual, logorrhea, mania, restlessness, agitation

                    Skin and subcutaneous tissue disorders: Alopecia, erythema, hyperhidrosis

                    Urogenital system: Priapism

                    Vascular disorders: Raynaud phenomenon

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                    Warnings

                    Black Box Warnings

                    CNS stimulants, including serdexmethylphenidate/methylphenidate, other methylphenidate-containing products, and amphetamines, have a high potential for abuse and dependence

                    Assess risk of abuse before prescribing and monitor for signs of abuse and dependence while on therapy

                    Contraindications

                    Known hypersensitivity to serdexmethylphenidate, methylphenidate, or other components; bronchospasm, rash, and pruritus reported with serdexmethylphenidate/methylphenidate; hypersensitivity reactions (eg, angioedema) and anaphylactic reactions reported in patients treated with other methylphenidate products

                    Concomitant use with MAOIs or within 14 days following discontinuation with an MAOI

                    Cautions

                    CNS stimulants have a high potential for abuse and dependence; assess risks before prescribing and carefully monitor while on therapy

                    Priapism, sometimes requiring surgical intervention, reported with methylphenidate in both pediatric and adults patients; not reported upon initiating, but may develop after some time on the drug (often subsequent to increased dose or during drug withdrawal); seek immediate medical attention for abnormally sustained or frequent and painful erections

                    Peripheral vasculopathy, including Raynaud phenomenon, reported with CNS stimulants; signs and symptoms generally improve after dose reduction or discontinuation; observe for digital changes during treatment; further clinical evaluation (eg, rheumatology referral) may be necessary

                    Monitor growth in pediatric patients during treatment with stimulants; patients who are not growing or gaining weight as expected may need to have their treatment interrupted

                    Periodically reevaluate long-term use and adjust dose; periodically discontinue to assess patient's condition

                    Serious cardiovascular reactions

                    • CNS stimulants cause an increased blood pressure (mean increase ~2-4 mmHg) and heart rate (mean increase ~3-6 bpm); individuals may have larger increases; monitor all patients for hypertension and tachycardia; consider benefits and risks in patients for whom an increase in blood pressure would be problematic
                    • Adults: Sudden death, stroke, and myocardial infarction reported with CNS stimulant treatment at recommended doses
                    • Pediatric patients: Sudden death reported with structural cardiac abnormalities and other serious heart problems taking CNS stimulants at recommended doses for ADHD
                    • Avoid use in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, coronary artery disease, and other serious heart problems
                    • Promptly evaluate patients who develop exertional chest pain, unexplained syncope, or arrhythmias during treatment

                    Psychiatric adverse reactions

                    • May exacerbate symptoms of behavior disturbance and thought disorder in patients with preexisting psychotic disorders
                    • May induce manic or mixed mood episode; before prescribing, screen patients for risk factors for developing a manic episode (eg, comorbid or history of depressive symptoms, family history of suicide, bipolar disorder, or depression)
                    • At recommended doses, CNS stimulants may cause psychotic or manic symptoms (eg, hallucinations, delusional thinking, mania) in patients without a prior history; if such symptoms occur, consider discontinuing drug

                    Drug interaction overview

                    • MAOIs
                      • Contraindicated
                      • Do not coadminister serdexmethylphenidate/methylphenidate with MAOIs or within 14 days after discontinuing MAOI treatment, owing to potential for hypertensive crisis
                    • Antihypertensives
                      • Monitor blood pressure and adjust antihypertensive dose as needed
                      • Serdexmethylphenidate/methylphenidate may decrease effectiveness of antihypertensives
                    • Halogenated anesthetics
                      • Avoid serdexmethylphenidate/methylphenidate on day of surgery
                      • Concomitant use of serdexmethylphenidate/methylphenidate with halogenated anesthetics (eg, halothane, isoflurane, enflurane, desflurane, sevoflurane) may increase risk of sudden blood pressure and heart rate increase during surgery
                    • Risperidone
                      • Monitor for extrapyramidal symptoms (EPSs)
                      • Coadministration of methylphenidate with risperidone may increase risk of EPSs when there is dosage change (increased or decreased) of either or both medications
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                    Pregnancy & Lactation

                    Pregnancy

                    Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Psychostimulants at 1-866-961-2388

                    No data are available on use in pregnant females; dexmethylphenidate is the d-threo enantiomer of racemic methylphenidate; published studies and postmarketing reports on methylphenidate use during pregnancy have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

                    However, there may be risks to the fetus associated with the use of CNS stimulants use during pregnancy

                    Clinical considerations

                    • CNS stimulants can cause vasoconstriction and thereby decrease placental perfusion
                    • No fetal and/or neonatal adverse reactions reported with therapeutic doses of methylphenidate during pregnancy; however, premature delivery and low-birth-weight infants reported in amphetamine-dependent mothers

                    Lactation

                    Serdexmethylphenidate: Data are unavailable on presence in human milk, effects on breastfed infants, or effects on milk production

                    Dexmethylphenidate

                    • Limited published literature, based on milk sampling from 7 mothers, reports methylphenidate is present in human milk, which resulted in infant doses of 0.16-0.7% of the maternal weight–adjusted dosage and a milk/plasma ratio ranging between 1.1 and 2.
                    • There are no reports of adverse effects on breastfed infants and no effects on milk production

                    Clinical considerations: Monitor breastfeeding infants for adverse reactions (eg, agitation, anorexia, reduced weight gain)

                    Pregnancy Categories

                    A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                    B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                    C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                    D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                    X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                    NA: Information not available.

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                    Pharmacology

                    Mechanism of Action

                    Dexmethylphenidate (d-MPH): CNS stimulant; blocks reuptake of norepinephrine and dopamine, causing an increase of their release into the extraneuronal space; mode of therapeutic action for ADHD is unknown

                    Serdexmethylphenidate: Prodrug of d-MPH formulated with immediate-release d-MPH

                    Absorption

                    Peak plasma time: 2 hr (serdexmethylphenidate/d-MPH); 8 hr (serdexmethylphenidate alone)

                    Peak plasma concentration: 14 ng/mL

                    AUC: 186 hrng/mL

                    Effect of food

                    • No clinically meaningful differences in dexmethylphenidate exposure observed when administered after an overnight fast, with a high-fat, high-caloric meal, or sprinkled onto applesauce or water
                    • Peak plasma time lengthened from 2 to 4-4.5 hr

                    Distribution

                    Protein bound

                    • Serdexmethylphenidate: 56%
                    • Dexmethylphenidate: 47%

                    Vd

                    • Serdexmethylphenidate: 29.3 L/kg
                    • Dexmethylphenidate: 2.65 L/kg

                    Metabolism

                    Serdexmethylphenidate: Prodrug of dexmethylphenidate; likely converted to dexmethylphenidate mainly in lower GI tract; enzymes involved in conversion not identified

                    Dexmethylphenidate: Metabolized primarily via de-esterification to dextro-alpha-phenyl-piperidine acetic acid (ie, dextro-ritalinic acid); ritalinic acid has little or no pharmacological activity

                    Elimination

                    Half-life

                    • Serdexmethylphenidate: 5.7 hr
                    • Dexmethylphenidate: 11.7 hr

                    Clearance

                    • Serdexmethylphenidate: 3.6 L/hr/kg (PO)
                    • Dexmethylphenidate: 0.4 L/hr/kg (IV)

                    Excretion

                    • Serdexmethylphenidate: Urine 62% (0.4% unchanged); feces 37% (11% unchanged)
                    • Ritalinic acid: ~63% of total recovered dose in urine and feces
                    • Methylphenidate: Urine ~90%
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                    Administration

                    Oral Administration

                    Administer in morning with or without food

                    Unable to swallow capsule whole

                    • Open and sprinkle entire contents into 50 mL of water or over 2 tablespoons of applesauce
                    • Consume all drug/food mixture immediately or within 10 minutes of mixing
                    • Do not store mixture for future use

                    Switching from other methylphenidate products

                    • If switching from other methylphenidate products, discontinue that treatment, and titrate serdexmethylphenidate/methylphenidate using titration schedule described
                    • Do not substitute products on a milligram-per-milligram basis, owing to different pharmacokinetic profiles and composition

                    Dose reduction and discontinuation

                    • Reduce dose, or if necessary, discontinue drug, if paradoxical aggravation of symptoms or other adverse reactions occur
                    • Periodically discontinue drug to assess pediatric patients’ conditions
                    • Discontinue if improvement not observed after appropriate dosage adjustment over a 1-month period

                    Storage

                    • Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
                    • Protect from moisture
                    • Dispense in tight container

                    Disposal

                    • Comply with local laws and regulations on drug disposal of CNS stimulants
                    • Dispose of remaining, unused, or expired drug by a medicine take-back program or by an authorized collector registered with the Drug Enforcement Administration
                    • If take-back program or authorized collector unavailable, mix drug with undesirable, nontoxic substance to make it less appealing to children and pets, then place in container (eg, sealed plastic bag) and discard in household trash
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                    Images

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                    Patient Handout

                    A Patient Handout is not currently available for this monograph.
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                    Formulary

                    FormularyPatient Discounts

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                    The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                    Tier Description
                    1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                    2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                    3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                    4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    NC NOT COVERED – Drugs that are not covered by the plan.
                    Code Definition
                    PA Prior Authorization
                    Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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                    Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.