Version May 2024
The FDA is requiring updates to the Boxed Warning and other sections in the prescribing information of prescription stimulants to ensure consistency across the class of medicines and address continuing concerns of misuse, abuse, substance use disorder, and overdose. The current prescribing information for some prescription stimulants does not provide up-to-date warnings about the harms of misuse and abuse, and particularly that most individuals who misuse prescription stimulants get them from other family members or peers. The FDA is adding information that patients should never share prescription stimulants with anyone, and the Boxed Warning will describe the risks of misuse, abuse, substance use disorder, and overdose consistently across all medicines in the class, as well as advise health care professionals to monitor patients closely for signs and symptoms of misuse, abuse, and substance use disorder. Information on these risks is being required in several sections of the prescribing information, including Warnings and Precautions, Drug Abuse and Dependence, Overdosage, and Patient Counseling sections; updates to existing Medication Guides are also required to help educate patients and caregivers about these risks.
Further information can be found at https://www.fda.gov/drugs/drug-safety-and-availability/fda-updating-warnings-improve-safe-use-prescription-stimulants-used-treat-adhd-and-other-conditions.
CNS stimulants, including serdexmethylphenidate/dexmethylphenidate, other methylphenidate-containing products, and amphetamines, have a high potential for abuse and dependence. Assess the risk of abuse prior to prescribing, and monitor for signs of abuse and dependence while on therapy.
Attention-deficit/hyperactivity disorder: Oral: Initial: Serdexmethylphenidate 39.2 mg/dexmethylphenidate 7.8 mg once daily in the morning; after 1 week, may increase dose to serdexmethylphenidate 52.3 mg/ dexmethylphenidate 10.4 mg once daily; maximum dose: serdexmethylphenidate 52.3 mg/ dexmethylphenidate 10.4 mg once daily. A dose reduction or discontinuation may be needed for paradoxical aggravation of symptoms or other adverse reactions.
Converting from other methylphenidate products to serdexmethylphenidate/dexmethylphenidate: Discontinue other methylphenidate product and begin serdexmethylphenidate/dexmethylphenidate according to initial and titration dosing; do not substitute on a mg-per-mg basis.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, since little unchanged drug is eliminated in the urine, dosage adjustment in renal impairment is not required.
There are no dosage adjustments provided in the manufacturer's labeling.
(For additional information see "Serdexmethylphenidate and dexmethylphenidate: Pediatric drug information")
Attention-deficit/hyperactivity disorder (ADHD):
Note: Serdexmethylphenidate/dexmethylphenidate (Azstarys) has a different pharmacokinetic profile and base composition of methylphenidate and should not be substituted for any other methylphenidate products on a mg:mg basis. Azstarys is a fixed-dose combination product, titration increments based on available capsule strengths. Discontinue medication if no improvement is seen after appropriate dosage adjustment over a 1-month period of time.
Children ≥6 years: Azstarys: Oral: Initial: Serdexmethylphenidate 39.2 mg/dexmethylphenidate 7.8 mg capsule once daily in the morning; after 1 week, may titrate dose based on response and tolerability to a higher dose of serdexmethylphenidate 52.3 mg/dexmethylphenidate 10.4 mg capsule once daily or if necessary, decrease dose to serdexmethylphenidate 26.1 mg/dexmethylphenidate 5.2 mg capsule once daily. Discontinuation may be necessary for paradoxical aggravation of symptoms or other adverse reactions; maximum daily dose: serdexmethylphenidate 52.3 mg/dexmethylphenidate 10.4 mg per day.
Adolescents: Azstarys: Oral: Initial: Serdexmethylphenidate 39.2 mg/dexmethylphenidate 7.8 mg capsule once daily in the morning for 1 week then increase to serdexmethylphenidate 52.3 mg/dexmethylphenidate 10.4 mg capsule once daily; maximum daily dose: serdexmethylphenidate 52.3 mg/dexmethylphenidate 10.4 mg per day. A dose reduction or discontinuation may be needed for paradoxical aggravation of symptoms or other adverse reactions.
Converting from other methylphenidate products to Azstarys: Discontinue other methylphenidate product and begin Azstarys according to initial and titration dosing shown above.
Children ≥6 years and Adolescents: There are no dosage adjustments provided in manufacturer's labeling (has not been studied); however, dosage adjustment unlikely because renal elimination is not an important factor in the clearance of serdexmethylphenidate or dexmethylphenidate.
Children ≥6 years and Adolescents: There are no dosage adjustments provided in manufacturer's labeling (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. See Dexmethylphenidate monograph. Also refer to Methylphenidate for adverse effects seen with other methylphenidate products.
Frequency not defined:
Endocrine & metabolic: Weight loss
Nervous system: Drug abuse, drug dependence
Neuromuscular & skeletal: Linear skeletal growth rate below expectation
Postmarketing: Cardiovascular: Peripheral vascular disease, Raynaud's disease
Hypersensitivity (eg, bronchospasm, rash, pruritus) to serdexmethylphenidate, dexmethylphenidate, methylphenidate, or any component of the formulation; concomitant use with or within 14 days of monoamine oxidase inhibitors.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Concerns related to adverse effects:
• Cardiovascular events: CNS stimulant treatment has been associated with sudden death in pediatric patients with preexisting structural cardiac abnormalities, and sudden death, stroke, and myocardial infarction (MI) have been reported in adults. Stimulants should be avoided in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, coronary artery disease, or other serious cardia problems. Prior to initiating stimulant, assess medical history and family history of sudden death or ventricular arrhythmia. Promptly conduct cardiac evaluation in patients who develop exertional chest pain, unexplained syncope, or any other symptoms of cardiac disease during stimulant treatment.
• Hypersensitivity: Hypersensitivity reactions, including angioedema and anaphylactic reactions, have been reported in patients treated with methylphenidate-containing products.
• Peripheral vasculopathy: Stimulants are associated with peripheral vasculopathy, including Raynaud phenomenon; signs and symptoms are usually intermittent and mild, and generally improve with dose reduction and discontinuation. Peripheral vasculopathy effects have been observed at different times, at therapeutic doses, and in all age groups. Digital ulceration and/or soft tissue breakdown have been observed rarely; monitor for digital changes during therapy and seek further evaluation (eg, rheumatology) if necessary.
• Priapism: Prolonged and painful erections, sometimes requiring surgical intervention, have been reported with use of methylphenidate-containing products, in both pediatric and adult patients. Priapism has been reported to develop after some time on the drug, often subsequent to an increase in dose but also during a period of drug withdrawal (drug holidays or discontinuation). Patients with certain hematological dyscrasias (eg, sickle cell disease), malignancies, perineal trauma, or concomitant use of alcohol, illicit drugs, or other medications associated with priapism may be at increased risk (Eiland 2014). Patients who develop abnormally sustained or frequent and painful erections should discontinue therapy and seek immediate medical attention. An emergent urological consultation should be obtained in severe cases. In patients with severe cases of priapism that were slow to resolve and/or required detumescence by aspiration, avoidance of stimulants and atomoxetine may be preferred (Eiland 2014).
Disease-related concerns:
• Abuse and dependence: CNS stimulants, including serdexmethylphenidate/dexmethylphenidate, other methylphenidate-containing products, and amphetamines, have a high potential for abuse and dependence. Assess the risk of abuse prior to prescribing, and monitor for signs of abuse and dependence while on therapy.
• Cardiovascular disorders: CNS stimulants may increase BP (mean increase 2 to 4 mm Hg) and heart rate (3 to 6 bpm). Use with caution in patients with hypertension, heart failure, recent MI, ventricular arrhythmia, and other cardiovascular conditions that might be exacerbated by increases in BP or heart rate.
• Psychiatric disorders: Use with caution in patients with preexisting psychosis (may exacerbate symptoms of behavior and thought disorder) or bipolar disorder (may induce mixed/manic episode). New-onset psychosis or mania may occur with stimulant use. Patients should be screened for bipolar disorder and risk factors for developing a manic episode prior to treatment (eg, comorbid or history of depressive symptoms; family history of suicide, bipolar disorder, or depression); consider discontinuation if psychotic or manic symptoms (eg, delusional thinking, hallucinations, mania) occur.
• Seizure disorder: Limited information exists regarding stimulant use in seizure disorder. Whereas patients with attention-deficit hyperactivity disorder are at an increased risk for seizure activity compared to the general population, a retrospective study using drug claims data showed that the use of stimulant medications was associated with a lower risk (Cortese 2013; Wiggs 2018). Manufacturers of some stimulants recommend discontinuing therapy if seizures occur.
• Tourette syndrome/tics: Use with caution in patients with Tourette syndrome or other tic disorders. Stimulants may exacerbate tics (motor and phonic) and Tourette syndrome; however, evidence demonstrating increased tics is limited. Evaluate for tics and Tourette syndrome prior to therapy initiation (AACAP [Murphy 2013]; Pliszka 2007).
Special populations:
• Pediatric: Use of CNS stimulants have been associated with appetite suppression, weight loss, and slowing of growth rate; monitor growth rate, height, and weight during treatment. Treatment interruption may be necessary in patients who are not increasing in height or gaining weight as expected.
Other warnings/precautions:
• Discontinuation of therapy: Abrupt discontinuation, rapid dose reduction, or administration of an antagonist may result in withdrawal symptoms, including dysphoric mood, fatigue, vivid, unpleasant dreams, insomnia or hypersomnia, increased appetite, and psychomotor retardation or agitation.
CNS stimulant treatment has been associated with sudden death in children and adolescents with preexisting structural cardiac abnormalities; one study reported methylphenidate increased risk for arrhythmia and myocardial infarction (MI) in youth without congenital heart disease (Shin 2016) and a retrospective case-control study reported an association with stimulants and sudden unexplained death in youth (Gould 2009). However, as noted in reviews (Martinez-Raga 2013; Westover 2012) several large studies have not found an association between prescription stimulants and cardiovascular events; though most retrospective studies were large (n=55,383 to 2,131,953), some had statistical power or methodological limitations (Westover 2012). A large retrospective cohort study involving 1,200,438 children and young adults (aged 2 to 24 years) prescribed attention-deficit hyperactivity disorder (ADHD) medication (methylphenidate, dexmethylphenidate, dextroamphetamines, amphetamine salts, pemoline, or atomoxetine) found no evidence that ADHD medication was associated with an increased risk of serious cardiovascular events (ie, acute MI, sudden cardiac death, stroke) in current (adjusted hazard ratio: 0.75; 95% CI: 0.31 to 1.85) or former (adjusted hazard ratio: 1.03; 95% CI: 0.57 to 1.89) users compared with nonusers, nor in current compared with former users. Results were similar with multiple alternative analyses to assess for bias or study assumptions. While point estimates of relative risks for ADHD drugs did not demonstrate increased risk, the upper limit of the 95% CI suggested a doubling of the risk could not be ruled out, although absolute magnitude of increased risk would be low. Data on any individual medication, other than methylphenidate, were too sparse for separate regression analyses (Cooper 2011). Prior to treatment with medications for ADHD, the American Heart Association and the American Academy of Pediatrics recommend that all children and adolescents diagnosed with ADHD have a thorough cardiovascular assessment, including patient and family health histories, determination of all medications used (prescribed and over-the-counter), and a physical examination focused on cardiovascular disease risk factors. An ECG is not mandatory but is reasonable to consider prior to stimulant medication therapy. Prompt evaluation and appropriate referral and testing, if warranted, should occur if any cardiac symptoms present (Vetter 2008).
Evaluation of the effect of stimulants on growth in ADHD diagnosed children <12 years receiving treatment for at least 3 years with stimulants has shown decreased height and weight changes over time compared to age matched control; height: 4.7 to 5.5 cm/year compared to 6.3 cm/year and 2.1 to 3.3 kg/year compared to 4.4 kg/year (Poulton 2016). In 5,315 pediatric patients (age range: 8 to 17 years) actively treated with stimulants (methylphenidate, dexmethylphenidate, dextroamphetamine, atomoxetine, lisdexamfetamine), significant reductions in total femoral, femoral neck, and lumbar bone mineral density (BMD) were observed compared to matched unmedicated controls (n=1,967); also reported were significantly more subjects in the stimulant-treated group with BMD measurements in the osteopenic range compared to matched controls (38.3% to 21.6%); of note, there was no data on duration of medication treatment, dosing, or therapy changes (Howard 2017). A longitudinal cohort-controlled trial reported no difference in peak height velocity and final adult height in subjects with ADHD and/or treated with stimulants (Harstad 2014).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Azstarys: Serdexmethylphenidate 26.1 mg and dexmethylphenidate 5.2 mg [contains fd&c blue #1 (brilliant blue)]
Azstarys: Serdexmethylphenidate 39.2 mg and dexmethylphenidate 7.8 mg [contains fd&c blue #1 (brilliant blue), fd&c red #40 (allura red ac dye)]
Azstarys: Serdexmethylphenidate 52.3 mg and dexmethylphenidate 10.4 mg [contains fd&c red #40 (allura red ac dye), fd&c yellow #6 (sunset yellow)]
No
Capsules (Azstarys Oral)
26.1-5.2 mg (per each): $16.74
39.2-7.8 mg (per each): $16.74
52.3-10.4 mg (per each): $16.74
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
C-II
Oral: Administer in the morning without regard to food. Capsules may be opened, and the contents sprinkled onto 50 mL of water or 2 tablespoons of applesauce. The prepared mixture should be administered immediately after or within 10 minutes of mixing; do not store for future use.
Oral: Administer in the morning without regard to food. Capsules may be swallowed whole or opened and contents sprinkled into 50 mL of water or over 2 tablespoons of applesauce; consume within 10 minutes; do not store for future use.
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Azstarys: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/212994s000lbl.pdf#page=26
Attention-deficit hyperactivity disorder: Treatment of attention-deficit hyperactivity disorder in patients ≥6 years of age.
Serdexmethylphenidate/dexmethylphenidate may be confused with methylphenidate, dexmethylphenidate.
Azstarys may be confused with Astatin brand name for atorvastatin [multiple international markets].
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acebrophylline: May enhance the stimulatory effect of CNS Stimulants. Risk X: Avoid combination
Amifampridine: Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine. Risk C: Monitor therapy
Amisulpride (Oral): Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Amisulpride (Oral). Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Antihypertensive Agents: Dexmethylphenidate may diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Antipsychotic Agents: May enhance the adverse/toxic effect of Dexmethylphenidate-Methylphenidate. Dexmethylphenidate-Methylphenidate may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, the risk of extrapyramidal symptoms may be increased when these agents are combined. Risk C: Monitor therapy
ARIPiprazole: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of ARIPiprazole. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
ARIPiprazole Lauroxil: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of ARIPiprazole Lauroxil. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Asenapine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Asenapine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Benperidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Benperidol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Blonanserin: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Blonanserin. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Brexpiprazole: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Brexpiprazole. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Bromperidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Bromperidol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
BuPROPion: May enhance the neuroexcitatory and/or seizure-potentiating effect of Agents With Seizure Threshold Lowering Potential. Risk C: Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Cariprazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Cariprazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
ChlorproMAZINE: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of ChlorproMAZINE. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Clothiapine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Clothiapine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
CloZAPine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy
DroPERidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of DroPERidol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Esketamine: May enhance the hypertensive effect of CNS Stimulants. Risk C: Monitor therapy
Flupentixol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Flupentixol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
FluPHENAZine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of FluPHENAZine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Haloperidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Haloperidol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Iloperidone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iloperidone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Inhalational Anesthetics: Dexmethylphenidate-Methylphenidate may enhance the hypertensive effect of Inhalational Anesthetics. Risk X: Avoid combination
Iobenguane Radiopharmaceutical Products: CNS Stimulants may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. Risk X: Avoid combination
Ioflupane I 123: Dexmethylphenidate may diminish the diagnostic effect of Ioflupane I 123. Risk C: Monitor therapy
Iohexol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Iomeprol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Iopamidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination
Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy
Loxapine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Loxapine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Lumateperone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Lumateperone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Lurasidone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Lurasidone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Methotrimeprazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Methotrimeprazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Molindone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Molindone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Dexmethylphenidate. Risk X: Avoid combination
OLANZapine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of OLANZapine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Paliperidone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Paliperidone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Periciazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Periciazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Perphenazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Perphenazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
PHENobarbital: Dexmethylphenidate may increase the serum concentration of PHENobarbital. Risk C: Monitor therapy
Pimozide: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Pimozide. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Pipamperone [INT]: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Pipamperone [INT]. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Polyethylene Glycol-Electrolyte Solution: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Polyethylene Glycol-Electrolyte Solution. Specifically, the risk of seizure may be increased. Risk C: Monitor therapy
Primidone: Dexmethylphenidate may increase serum concentrations of the active metabolite(s) of Primidone. Specifically, phenobarbital concentrations could become elevated. Dexmethylphenidate may increase the serum concentration of Primidone. Risk C: Monitor therapy
Prochlorperazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Prochlorperazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Promazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Promazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
QUEtiapine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of QUEtiapine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
RisperiDONE: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of RisperiDONE. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Serotonergic Agents (High Risk): Dexmethylphenidate-Methylphenidate may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Sertindole: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Sertindole. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Sodium Phosphates: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Sodium Phosphates. Specifically, the risk of seizure or loss of consciousness may be increased in patients with significant sodium phosphate-induced fluid or electrolyte abnormalities. Risk C: Monitor therapy
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Solriamfetol: CNS Stimulants may enhance the hypertensive effect of Solriamfetol. CNS Stimulants may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Sulpiride: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Sulpiride. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Thioridazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Thioridazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Thiothixene: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Thiothixene. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Trifluoperazine: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Trifluoperazine. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Ziprasidone: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Ziprasidone. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Zuclopenthixol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Zuclopenthixol. Specifically, the risk of seizures may be increased. Risk C: Monitor therapy
Food may delay time to peak drug levels. Management: Administer without regard to meals.
Serdexmethylphenidate is a prodrug of dexmethylphenidate; dexmethylphenidate is the d-threo enantiomer of racemic methylphenidate; refer to the methylphenidate monograph for additional information.
Data collection to monitor pregnancy and infant outcomes following exposure to attention-deficit hyperactivity disorder medications is ongoing. Health care providers are encouraged to enroll patients exposed to serdexmethylphenidate/dexmethylphenidate during pregnancy in the National Pregnancy Registry for Psychostimulants (1-866-961-2388).
It is not known if serdexmethylphenidate is present in breast milk. Serdexmethylphenidate is a prodrug of dexmethylphenidate; dexmethylphenidate is the d-threo enantiomer of racemic methylphenidate, which is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Infants exposed to serdexmethylphenidate/dexmethylphenidate via breast milk should be monitored for agitation, anorexia, and reduced weight gain.
Refer to the Methylphenidate monograph for additional information.
Cardiac evaluation should be completed at baseline and on any patient who develops exertional chest pain, unexplained syncope, and any symptom of cardiac disease during treatment with stimulants; BP and heart rate (baseline, following dose increases and periodically during treatment); growth rate (height and weight) and appetite in children; weight in adults; signs of peripheral vasculopathy (eg, digital changes); sleep and behavioral changes. Assess for risk of abuse prior to prescribing and signs of misuse, abuse, or substance use disorder throughout treatment (NICE 2018).
The exact mechanism of action of serdexmethylphenidate/dexmethylphenidate in attention-deficit hyperactivity disorder is unknown. Serdexmethylphenidate is a prodrug of dexmethylphenidate. Dexmethylphenidate is the more active, d-threo-enantiomer, of racemic methylphenidate. It is a CNS stimulant that blocks the reuptake of norepinephrine and dopamine, and increases their release into the extraneuronal space. Studies (in vitro) with serdexmethylphenidate demonstrated little or no affinity to monoaminergic reuptake transporters.
Distribution: Vd: Serdexmethylphenidate: 29.3 L/kg.
Protein binding: Serdexmethylphenidate: ~56%; dexmethylphenidate ~47%.
Metabolism: Serdexmethylphenidate is likely converted to dexmethylphenidate mainly in the lower GI tract; dexmethylphenidate is metabolized via de-esterification to inactive metabolite d-α-phenyl-piperidine acetate (d-ritalinic acid).
Bioavailability: Serdexmethylphenidate: <3%.
Half-life elimination: Serdexmethylphenidate: 5.7 hours; dexmethylphenidate: 11.7 hours.
Time to peak: Dexmethylphenidate: ~2 hours; may be delayed to 4 to 4.5 hours with food.
Excretion: Serdexmethylphenidate: Urine: ~62% (~0.4% as unchanged drug); feces: ~37% (~11% as unchanged drug).
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