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. |
| Molecular Weight | 329.82 |
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 | Data limited; methylphenidate associated with increased risk of cardiac malformations in some studies. Use only if benefit outweighs risk. |
| 2nd trimester | Limited data; potential for adverse effects on fetal growth and development. Use with caution and only if clearly needed. |
| 3rd trimester | Use near term may increase risk of neonatal withdrawal syndrome, including irritability, feeding difficulties, and respiratory distress. Avoid use in late pregnancy. |
Clinical note
Comprehensive clinical and safety monograph for XELSTRYM (XELSTRYM).
| Placental transfer | Methylphenidate crosses the placenta; fetal plasma concentrations are approximately 30-70% of maternal levels. |
| Breastfeeding | Methylphenidate is excreted into breast milk in low concentrations. Monitor infant for agitation, insomnia, and poor weight gain. American Academy of Pediatrics considers methylphenidate as 'usually compatible' with breastfeeding, but use caution, especially with high maternal doses. |
■ 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 |
Hypersensitivity to methylphenidate or any componentConcurrent treatment with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuationGlaucomaTics or family history of Tourette's syndromeSevere hypertension, angina pectoris, cardiac arrhythmias, or other serious cardiac conditions
| 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) |
| Food/Dietary | XELSTRYM should be taken with food to reduce the risk of gastrointestinal side effects. Avoid high-fat meals immediately before or after application as they may increase drug absorption. Limit caffeine intake as it may potentiate stimulant effects. Avoid consumption of acidic foods or beverages (e.g., citrus fruits, colas) within one hour of patch removal, as urine acidification can decrease drug elimination and increase side effects. |
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| Lactation Rating | L3 (Moderately Safe) |
| 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). |
| 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. |
| Clinical Pearls | XELSTRYM (dextroamphetamine) transdermal system is a CNS stimulant indicated for ADHD. Apply to clean, dry, intact skin on the hip, upper arm, chest, or back. Rotate application sites to minimize skin irritation. Do not apply to oily, damaged, or irritated skin. Remove the patch after 9 hours; onset of action occurs within 2 hours of application. Monitor for signs of abuse, hypertension, tachycardia, and psychiatric adverse reactions. Use with caution in patients with pre-existing cardiovascular abnormalities or bipolar disorder. May reduce seizure threshold in patients with epilepsy. |
| Patient Advice | Apply the patch once daily in the morning to clean, dry, hairless skin on the hip, upper arm, chest, or back. · Remove the patch after 9 hours; do not wear for longer than recommended. · Wash hands after applying or removing the patch; avoid touching eyes. · Do not cut or trim the patch; use as supplied. · Rotate application sites to prevent skin irritation; do not use the same site two days in a row. · Avoid exposing the patch area to direct heat sources (e.g., heating pads, electric blankets, hot tubs) as it may increase drug absorption. · Store patches at room temperature; keep out of reach of children. · Dispose of used patches by folding adhesive sides together and discarding in the trash; flush unused patches down the toilet. · Common side effects include decreased appetite, trouble sleeping, headache, and application site reactions. · Contact your doctor if you experience chest pain, shortness of breath, fainting, or signs of allergic reaction (rash, hives, itching). · Avoid alcohol while using this medication. · Do not stop taking this medication abruptly without consulting your doctor. |