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Pronunciation |
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(PEM
oh
leen) |
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U.S. Brand
Names |
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Cylert® |
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Generic
Available |
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No |
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Synonyms |
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Phenylisohydantoin; PIO |
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Pharmacological Index |
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Stimulant |
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Use |
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Treatment of attention deficit hyperactivity disorder (ADHD) (not first-line)
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Restrictions |
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C-IV |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Known hypersensitivity to pemoline or any component; hepatic impairment
(including abnormalities on baseline liver function tests); children <6 years
of age; Tourette's syndrome |
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Warnings/Precautions |
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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. |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
|
Pemoline in combination with antiepileptic medications may decrease seizure
threshold
Use caution when pemoline is used with other CNS acting medications
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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 |
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Pharmacodynamics/Kinetics |
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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
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Usual Dosage |
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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 |
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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Monitoring
Parameters |
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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 |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Pemoline has minimal sympathomimetic effects; there are no precautions in
using vasoconstrictors |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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Administer medication in the morning |
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Dosage Forms |
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Tablet: 18.75 mg, 37.5 mg, 75 mg
Tablet, chewable: 37.5 mg |
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