CYLERT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CYLERT (CYLERT).
CNS stimulant; increases extracellular dopamine and norepinephrine levels by blocking their reuptake and enhancing release.
| Metabolism | Hepatic, primarily via CYP3A4 |
| Excretion | Primarily renal (80-90% as unchanged drug and metabolites, with 50-60% as unchanged pemoline), minor biliary/fecal elimination (<10%) |
| Half-life | Terminal elimination half-life is 12-30 hours in children (mean 19 hours) and 8-14 hours in adults; the long half-life supports once-daily dosing, but accumulation can occur with repeated dosing |
| Protein binding | Approximately 50% bound to plasma proteins, primarily albumin |
| Volume of Distribution | Approximately 1.6 L/kg (range 1.2-2.0 L/kg), indicating extensive distribution into tissues; the large Vd suggests significant extravascular binding |
| Bioavailability | Oral bioavailability is 80-95% (well absorbed); no parenteral formulation is available |
| Onset of Action | Oral: Therapeutic effects typically appear within 1-2 weeks of daily dosing, but some behavioral improvements may be noted within 3-4 hours after the first dose |
| Duration of Action | Once-daily dosing provides sustained clinical effects for up to 24 hours; duration of action is extended due to the long half-life, and sleep disturbances may occur if taken late in the day |
37.5 mg orally once daily in the morning; may increase by 18.75 mg weekly to a maximum of 112.5 mg/day.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with GFR < 50 mL/min; no specific adjustment for GFR 50-80 mL/min, but caution advised. |
| Liver impairment | Contraindicated in Child-Pugh class B and C; dose reduction by 50% for Child-Pugh class A (maximum 56.25 mg/day). |
| Pediatric use | Children 6-12 years: initial 18.75 mg once daily; increase by 18.75 mg weekly; maximum 56.25 mg/day. Adolescents 13-17 years: initial 37.5 mg once daily; maximum 112.5 mg/day. |
| Geriatric use | Start at 18.75 mg once daily; increase slowly due to increased risk of hypertension and agitation; maximum 56.25 mg/day. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CYLERT (CYLERT).
| Breastfeeding | Not recommended during breastfeeding. Pemoline is excreted in human milk; the M/P ratio is unknown. Potential for adverse effects in the nursing infant, including agitation, insomnia, and decreased weight gain. |
| Teratogenic Risk | Pregnancy Category B. Animal studies have not shown fetal harm, but there are no adequate and well-controlled studies in pregnant women. First trimester: limited data suggest no increased risk of major malformations. Second and third trimesters: potential for decreased maternal weight gain and neonatal effects (e.g., irritability, dysphoria) if used near term. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to pemoline or any component","Hepatic impairment","Glaucoma","Use within 14 days of MAOIs","Tourette's syndrome or tics"]
| Precautions | ["Cardiovascular events including sudden death, stroke, and myocardial infarction","Psychiatric adverse reactions such as exacerbation of pre-existing psychosis or mania","Seizures","Growth suppression","Potential for abuse and dependence"] |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and weight gain during pregnancy. Assess fetal growth via ultrasound if prolonged use. Newborns exposed near term should be monitored for irritability and feeding difficulties. |
| Fertility Effects | In animal studies, pemoline reduced fertility indices at high doses. Human data are insufficient; potential for reversible suppression of spermatogenesis in males and menstrual irregularities in females. |