No

Stimulant

Treatment of attention deficit hyperactivity disorder (ADHD) (not first-line)

C-IV

B

Known hypersensitivity to pemoline or any component; hepatic impairment (including abnormalities on baseline liver function tests); children <6 years of age; Tourette's syndrome

Not considered first-line therapy for ADHD due to association with hepatic failure. Signed informed consent following a discussion of risks and benefits must be obtained prior to the initiation of therapy. Therapy should be discontinued if a response is not evident after 3 weeks of therapy. Pemoline should not be started in patients with abnormalities in baseline liver function tests, and should be discontinued if clinically significant liver function test abnormalities are revealed at any time during therapy. Use with caution in patients with renal dysfunction or psychosis. In general, stimulant medications should be used with caution in patients with bipolar disorder, diabetes mellitus, cardiovascular disease, seizure disorders, insomnia, porphyria, or hypertension (although pemoline has been demonstrated to have a low potential to elevate blood pressure relative to other stimulants). May exacerbate symptoms of behavior and thought disorder in psychotic patients. Potential for drug dependency exists - avoid abrupt discontinuation in patients who have received for prolonged periods. Stimulant use has been associated with growth suppression, and careful monitoring is recommended.

Central nervous system: Insomnia, dizziness, drowsiness, mental depression, increased irritability, seizures, precipitation of Tourette's syndrome, hallucinations, headache, movement disorders

Dermatologic: Rash

Endocrine & metabolic: Suppression of growth in children

Gastrointestinal: Anorexia, weight loss, stomach pain, nausea

Hematologic: Aplastic anemia

Hepatic: Increased liver enzyme (usually reversible upon discontinuation), hepatitis, jaundice, hepatic failure

Symptoms of overdose include tachycardia, hallucinations, agitation

There is no specific antidote for intoxication and the bulk of the treatment is supportive. Hyperactivity and agitation usually respond to reduced sensory input or benzodiazepines, however, with extreme agitation haloperidol (2-5 mg I.M. for adults) may be required. Hyperthermia is best treated with external cooling measures, or when severe or unresponsive, muscle paralysis with pancuronium may be needed.

Pemoline in combination with antiepileptic medications may decrease seizure threshold

Use caution when pemoline is used with other CNS acting medications

Blocks the reuptake mechanism of dopaminergic neurons, appears to act at the cerebral cortex and subcortical structures; CNS and respiratory stimulant with weak sympathomimetic effects; actions may be mediated via increase in CNS dopamine

Peak effect: 4 hours

Duration: 8 hours

Protein binding: 50%

Metabolism: Partially by the liver

Half-life: Children: 7-8.6 hours; Adults: 12 hours

Time to peak serum concentration: Oral: Within 2-4 hours

Elimination: In urine; only negligible amounts can be detected in feces

Children greater than or equal to 6 years: Oral: Initial: 37.5 mg given once daily in the morning, increase by 18.75 mg/day at weekly intervals; usual effective dose range: 56.25-75 mg/day; maximum: 112.5 mg/day; dosage range: 0.5-3 mg/kg/24 hours; significant benefit may not be evident until third or fourth week of administration

Alcohol: Additive CNS effect, avoid use

Baseline liver enzymes and every 2 weeks thereafter; the labeling for Cylert® has been revised to provide updated recommendations for liver function monitoring and a Patient Information Consent Form

Pemoline has minimal sympathomimetic effects; there are no precautions in using vasoconstrictors

No effects or complications reported

Take exactly as directed; do not change dosage or discontinue without consulting prescriber. Response may some time. Avoid alcohol, caffeine, or other stimulants. Maintain adequate fluid intake (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience nausea, decreased appetite, or altered taste sensation (small frequent meals may help maintain adequate nutrition); drowsiness, dizziness, or mental depression, especially during early therapy (use caution when driving or engaging in tasks requiring alertness until response to drug is known). Report unresolved rapid heartbeat; excessive agitation, nervousness, insomnia, tremors, dizziness, or seizures; skin rash or irritation; altered gait or movement; unusual mouth movements or vocalizations (Tourette's syndrome); or yellowing of skin or eyes, dark urine, or pale stools. Breast-feeding precautions: Breast-feeding is not recommended.

Administer medication in the morning

Tablet: 18.75 mg, 37.5 mg, 75 mg

Tablet, chewable: 37.5 mg