Table 2.
Pharmacokinetic properties of atypical antipsychotics in children versus adults
| Medication | FDA approval for ASD | Pharmacokinetics in adults | Pharmacokinetics in pediatrics | Monitoring information |
|---|---|---|---|---|
| Risperidone | Yes | Half-life: extensive metabolizers, 3 hours; poor metabolizers, 20 hours 9-hydroxyrisperidone – extensive metabolizers, 21 hours; poor metabolizers, 30 hours Intramuscular route 3–6 days Time to peak concentration: Oral route 1 hour 9-hydroxyrisperidone – extensive metabolizers, 3 hours; poor metabolizers, 17 hours Elimination: urine (70%), feces (14%) |
Similar to adults after appropriate adjustments of dose for weight | Blood pressure, heart rate (especially during dosing titration), mental status, AIMS, extrapyramidal symptoms, growth, body mass index, CBC with differential (monitor WBC and ANC especially for clozapine), liver enzymes (especially in obese children who are rapidly gaining weight), lipid profile, fasting blood glucose, and HbA1c |
| Aripiprazole | Yes | Half-life ~75 hours Time to peak concentration: Oral route 3–5 hours Intramuscular route 1–3 hours Elimination: feces (55%), urine (25%) |
Similar to adults for patients 10–17 years of age | |
| Olanzapine | No | Half-life: oral and intramuscular routes (short-acting) ~30 hours Time to peak concentration Oral route ~6 hours Elimination: urine Oral route 25 L/hour |
Half-life: oral and intramuscular routes (short-acting) ~37.2 hours Time to peak concentration Oral route ~4.7 hours Elimination: urine Oral route ~9.6 L/hour |
|
| Quetiapine | No | Half-life ~6 hours Time to peak concentration 1.5 hours Elimination: urine (73%) |
Half-life ~5.3 hours Time to peak concentration Oral route 0.5–3 hours |
|
| Ziprasidone | No | Half-life: Oral route 7 hours Time to peak concentration Oral route 6–8 hours Elimination: feces (66%) 7.5 mL/min/kg |
Half-life Oral route 3.3–4.1 hours Time to peak concentration Oral route 5–5.5 hours Elimination: feces (major) Oral route 11.5–13.1 mL/min/kg |
|
| Clozapine | No | Half-life ~12 hours Time to peak concentration Oral route 2.5 hours Elimination: urine (50%), feces (30%) |
Similar to adults. May see higher concentrations of desmethyl metabolite in comparison with clozapine (especially in females) when compared with adult data. | |
| Paliperidone | No | Half-life: Oral route 23 hours Intramuscular route 25–49 days Time to peak concentration Oral route ~24 hours Intramuscular route 13 days Elimination: urine (80%) |
Adolescents weighing >51 kg are similar to adults Adolescents weighing <51 kg had an observed increase of exposure by 23% (not considered clinically significant) |
Notes:
Adapted from Lexicomp Online. © 2015 Wolters Kluwer Clinical Drug Information, Inc. and its affiliates and/or licensors. All rights reserved.29
Abbreviations: AIMS, abnormal involuntary movement scale; ANC, absolute neutrophil count; ASD, autism spectrum disorder; CBC, complete blood count; FDA, US Food and Drug Administration; WBC, white blood cells.