Pemoline

Pronunciation

(PEM oh leen)

U.S. Brand Names

Cylert®; PemADD® [DSC]; PemADD® CT [DSC]

Synonyms

Phenylisohydantoin; PIO

Generic Available

Yes

Use

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

Use - Unlabeled/Investigational

Narcolepsy

Restrictions

C-IV

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown/not recommended

Contraindications

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

Warnings/Precautions

Not considered first-line therapy for ADHD due to association with hepatic failure. The manufacturer has recommended that signed informed consent following a discussion of risks and benefits must or should 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. Stimulants may unmask tics in individuals with coexisting Tourette's syndrome.

Adverse Reactions

Frequency not defined.

Central nervous system: Insomnia, dizziness, drowsiness, mental depression, increased irritability, seizure, 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

Overdosage/Toxicology

Symptoms of overdose include tachycardia, hallucinations, and agitation. There is no specific antidote for intoxication and treatment is primarily supportive.

Drug Interactions

Anticonvulsants: Pemoline may decrease seizure threshold; efficacy of anticonvulsants may be decreased

CNS depressants: Effects may be additive; use caution when pemoline is used with other CNS acting medications

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Mechanism of Action

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

Pharmacodynamics/Kinetics

Onset of action: Peak effect: 4 hours

Duration: 8 hours

Protein binding: 50%

Metabolism: Partially hepatic

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

Time to peak, serum: 2-4 hours

Excretion: Urine; feces (negligible amounts)

Dosage

Children

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

Dosing adjustment/comments in renal impairment: Clcr<50 mL/minute: Avoid use

Administration

Administer medication in the morning.

Monitoring Parameters

Liver enzymes (baseline and every 2 weeks)

Patient Education

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 hydration (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); or 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); yellowing of skin or eyes; or dark urine or pale stools. Breast-feeding precaution: Breast-feeding is not recommended.

Additional Information

Treatment of ADHD should include "Drug Holidays" or periodic discontinuation of stimulant medication in order to assess the patient's requirements and to decrease tolerance and limit suppression of linear growth and weight. The labeling for Cylert® includes recommendations for liver function monitoring and a Patient Information Consent Form.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

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

Dosage Forms

[DSC] = Discontinued product

Tablet (Cylert®, PemADD® [DSC]): 18.75 mg, 37.5 mg, 75 mg

Tablet, chewable (Cylert®, PemADD® CT [DSC]): 37.5 mg

International Brand Names

Betanamin® (JP); Ceractiv® (CL); Cylert® (CL, IL); Stimul® (LU); Tamilan® (AR); Tradon® (DE)

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