Serdexmethylphenidate/Dexmethylphenidate

DEA Class; Rx

Common Brand Names; Azstarys

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

Indicated for attention-deficit hyperactivity disorder (ADHD)

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

• 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
• 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

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

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

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