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 |
| Molecular Weight | 296.36 |
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 | Contraindicated: Increased risk of fetal cardiovascular malformations and cleft palate. |
| 2nd trimester | Contraindicated: Risk of fetal growth restriction and preterm birth. |
| 3rd trimester | Contraindicated: May cause neonatal irritability and feeding difficulties. |
Clinical note
Comprehensive clinical and safety monograph for CYLERT (CYLERT).
| Placental transfer | Extensive; crosses placenta readily. |
| Breastfeeding | Contraindicated due to potential for serious adverse effects in the infant, including agitation and insomnia. |
| Lactation Rating | L5 |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to pemoline or any componentHistory of hepatic dysfunction or hepatitisTourette's disorder or ticsConcomitant use with MAOIs or within 14 days of discontinuationGlaucomaAgitation or severe anxietyPregnancy
| 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 |
| Food/Dietary | Avoid alcohol and caffeine-containing beverages or foods as they may increase CNS stimulation and risk of adverse effects. No other significant food interactions. |
Loading safety data…
| 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. |
| 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. |
| Clinical Pearls |
| CYLERT (pemoline) is a CNS stimulant used for ADHD. Due to risk of hepatic failure, baseline and periodic LFTs are mandatory. Monitor for tics, insomnia, and growth suppression in children. Avoid use in patients with hepatic impairment or pre-existing psychosis. Taper to discontinue to avoid withdrawal. |
| Patient Advice | Take exactly as prescribed; do not increase dose without consulting doctor. · Avoid use if you have liver disease; report jaundice, dark urine, or abdominal pain immediately. · May cause insomnia; take last dose early in the day. · Monitor weight and height in children; report slowed growth. · Do not stop abruptly; taper under medical supervision to avoid withdrawal symptoms. · May cause dizziness or blurred vision; avoid driving until effects known. |