Cylert, also called pemoline, is a central nervous system (CNS) stimulant. Pemoline is structurally different from amphetaminesand methylphenidate. It is a white, tasteless, odorless powder, relatively insoluble in water, chloroform, ether, acetone, and benzene.
Cylert is normally supplied in tablet form or oral administration. It is also available as chewable tablets. It is primarily indicated for treatment of attention-deficit hyperactivity disorder (ADHD); however, due to its association with life threatening hepatic failure, it should not ordinarily be considered as first line drug therapy for ADHD. Presently, Cylert is classified as a Schedule IV drug.
Pemoline has a pharmacological activity similar to other CNS stimulants; however, it has minimal sympathomimetic effects. Though studies indicate that pemoline may act in animals through dopaminergic mechanisms, the precise method of action in humans is unknown.
There is neither sufficient evidence that clearly establishes the mechanism whereby Cylert produces its mental and behavioral effects in children, nor conclusive evidence of how these effects relate to the condition of the central nervous system (CNS).
Indications and Dosage:
Cylert is indicated for treatment of attention deficit hyperactivity disorder (ADHD). However, due to the danger and association of severe hepatic failure, it should not be employed as a first-line treatment for the condition.
It is recommended that in the event pemoline is prescribed and administered, it should be part of a larger total treatment program that typically includes other remedial measures (social, psychological, educational) for a stabilizing effect.
Cylert is administered in a single dose orally each morning. The recommended starting dose is 37.5mg/day. This daily dose should be gradually increased by 18.75mg at one week intervals until the desired clinical response is obtained. The effective daily dose for most patients will range from 56.25 to 75mg. The maximum recommended dose is 112.5mg/day.
Clinical improvement with pemoline has shown to be gradual. When taking the recommended dose, significant benefits may not be apparent until three to four weeks of continual therapy. When possible, drug administration should be occasionally interrupted to determine if there is any recurrence of behavioral symptoms sufficient to require continued therapy.
A number of adverse reactions have been associated with Cylert. There have been reports of hepatic dysfunction or failure, ranging from asymptomatic reversible increases in liver enzymes to hepatitis, jaundice.
Isolated reports of aplastic anemia have also been reported. In addition, central nervous system (CNS) effects that have been reported include convulsive seizures, hallucinations, dyskinetic movements of the tongue, lips, face and extremities, abnormal oculomotor function, mild depression, dizziness, increased irritability, headache, and drowsiness.
The most commonly reported side effect of Cylert is insomnia. In the majority of cases it is transient in nature or responds to a reduction in dosage.
Cylert is a DEA-Schedule IV controlled substance. The drug failed to demonstrate a potential for self-administration in primates. However, the similarity of Cylert to other psychostimulants with known risk of dependence suggests that psychological and/or physical dependence may occur. There have been isolated reports of transient psychotic symptoms in adults following the long-term misuse of excessive oral doses of pemoline. It should be given with caution to emotionally unstable patients who may increase the dosage of their own initiative.
Anorexia and weight loss may occur during the initial few weeks of treatment. In most cases it is transient in nature; weight gain normally resumes within three to six months. Nausea and stomach ache have also been reported.
Pemoline interaction with other drugs has not been studied in humans. Those taking Cylert concurrently with other drugs, especially substances that affect the CNS, should be closely monitored.
Information for Parents and Kids:
Safety and efficacy in children under age 6 have not been established. Long-term effects of Cylert in children have not been established.
Animal studies have shown no impairment by Cylert on fertility or adverse effects on pregnancy. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, the drug should not be used by pregnant women unless clearly necessary.
It is unknown if Cylert is excreted in human breast milk. Due to the fact that many drugs are, caution should be exercised when Cylert is taken by nursing women.
Warnings and Precautions:
Research suggests that in psychotic children administration of Cylert may exacerbate symptoms of behavioral disturbance and thought disorder. Cylert should be administered with caution to patients with significantly impaired renal function.
Since the market introduction of Cylert, there have been reports of elevated liver enzymes associated with its use. Many of these patients had this increase detected several months after beginning Cylert treatment. Most were asymptomatic; with the enzyme increase returning to normal after the drug was discontinued. Treatment with Cylert should be initiated only in people without liver disease and with normal baseline liver function.
CNS stimulants such as pemoline have been reported to precipitate motor and phonic tics and Tourette’s syndrome. Therefore, clinical evaluation for tics and Tourette’s in children and their families should precede the use of stimulants.
Cylert is not indicated in all cases of ADHD and should be considered only in relation to the child’s complete history and evaluation. The decision to prescribe pemoline should depend on the clinician’s assessment of the severity and chronicity of the symptoms and their appropriateness for the child’s age.
Withdrawal symptoms from pemoline have been reported in long-term therapy after abrupt cessation of the drug. Abruptly stopping Cylert may cause extreme fatigue and mental depression. The dosage should be reduced gradually to prevent withdrawal symptoms.
Over-dosage & Contraindications:
Signs and symptoms of acute overdose, resulting primarily from overstimulation of the CNS and excessive sympathomimetic effects, may include vomiting, tremors, hyperreflexia, delirium, agitation, muscle twitches, convulsions, headache, hyperpyrexia, tachycardia, hypertension and mydriasis.
The patient must be protected against self-injury and against external stimuli that would aggravate overstimulation already present. Gastric contents may be evacuated by gastric lavage. Other measures to detoxify the gut include administration of activated charcoal and a cathartic.
Cylert is contraindicated in patients with known hypersensitivity or idiosyncrasy to the drug.
Generic Name: pemoline
Chemical Formula: C9H8N2O2
Routes of Administration: oral
Elimination Half Life: approximately 12 hours
Legal Status: by prescription only