XELSTRYM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XELSTRYM (XELSTRYM).
XELSTRYM (dextroamphetamine transdermal system) is a sympathomimetic amine that increases synaptic concentrations of dopamine and norepinephrine by inhibiting their reuptake and promoting their release from presynaptic terminals.
| Metabolism | Primarily metabolized by CYP2D6, with minor contributions from other pathways (e.g., deamination and oxidation). |
| Excretion | Renal (90% as unchanged drug and metabolites, primarily dehydrodexmethylphenidate and inactive metabolites); minor biliary/fecal elimination (<5%) |
| Half-life | Mean terminal elimination half-life of dexmethylphenidate is approximately 2-3 hours in children and adolescents, with no significant accumulation at steady state; clinical effects correlate with plasma concentrations. |
| Protein binding | Approximately 15-20% bound to plasma proteins (primarily albumin) with no concentration-dependent binding. |
| Volume of Distribution | Apparent volume of distribution (Vd/F) is approximately 2.2-2.7 L/kg, indicating extensive tissue distribution; distribution half-life is about 1.2 hours. |
| Bioavailability | Transdermal: absolute bioavailability is approximately 55-60% compared to intravenous dosing, with dose-proportional exposure. |
| Onset of Action | Transdermal: onset of clinical effect generally observed within 2-3 hours after patch application; delayed release due to skin absorption. |
| Duration of Action | Transdermal patch: duration of clinical effect is approximately 10-12 hours after patch application, corresponding to the 9-hour wear time plus residual absorption; effects persist for the intended 12-hour period. |
Initial: one 9-mg patch applied to the hip once daily; titrate weekly in 4.5-mg increments to desired effect; maximum dose: 18 mg/day.
| Dosage form | SYSTEM |
| Renal impairment | No specific adjustment required; use caution in severe renal impairment (eGFR <30 mL/min/1.73 m²). |
| Liver impairment | No specific adjustment required; use caution in severe hepatic impairment (Child-Pugh class C). |
| Pediatric use | Weight-based dosing for patients 6-17 years: apply patch to hip once daily; start at 9 mg/day; titrate weekly by 4.5 mg; maximum 18 mg/day. |
| Geriatric use | Lower starting dose (9 mg/day) and slower titration recommended due to increased sensitivity and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XELSTRYM (XELSTRYM).
| Breastfeeding | Dexmethylphenidate is excreted into human breast milk. The milk-to-plasma (M/P) ratio is approximately 1.9 based on limited data from methylphenidate studies. The relative infant dose is estimated to be 0.2-0.7% of the maternal weight-adjusted dose. Due to potential for adverse effects (e.g., agitation, sleep disturbances, decreased weight gain) in the nursing infant, advise against breastfeeding while on XELSTRYM. If use is necessary, monitor the infant for symptoms of CNS stimulation. |
| Teratogenic Risk | XELSTRYM (dexmethylphenidate) is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal reproduction studies, dexmethylphenidate has been shown to cause fetal developmental toxicity (e.g., reduced fetal weight, increased incidences of skeletal variations) at doses equivalent to the maximum recommended human dose. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. First trimester exposure carries theoretical risk of teratogenicity; third trimester use may lead to neonatal withdrawal symptoms (e.g., irritability, feeding difficulties, respiratory depression). |
■ FDA Black Box Warning
WARNING: ABUSE AND DEPENDENCE. Central nervous system (CNS) stimulants, including XELSTRYM, 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.
| Serious Effects |
["Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing an MAOI","Hypersensitivity to amphetamine products or other components of the patch","Agitated states","Glaucoma","History of drug abuse"]
| Precautions | ["Serious cardiovascular events (sudden death, stroke, myocardial infarction) in patients with pre-existing cardiac abnormalities","Blood pressure and heart rate increase","Psychiatric adverse events (exacerbation of pre-existing psychosis, mania, aggression)","Seizures (use with caution in patients with seizure disorders)","Peripheral vasculopathy (Raynaud's phenomenon)","Long-term suppression of growth (monitor weight and height in pediatric patients)"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure and heart rate throughout pregnancy due to risk of hypertension and tachycardia. Assess fetal growth via serial ultrasound (e.g., monthly after 20 weeks) to detect intrauterine growth restriction. Consider fetal echocardiography if maternal cardiac adverse effects occur. Neonates should be monitored for withdrawal symptoms (e.g., irritability, poor feeding) for 48 hours after delivery. |
| Fertility Effects | In animal studies, dexmethylphenidate did not impair fertility in males or females at doses up to 1.6 times the maximum recommended human dose. In humans, no dedicated fertility studies are available; however, CNS stimulants may rarely affect libido or erectile function. No significant impact on female fertility is anticipated based on current data. |