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PubMed1998

Pemoline hepatotoxicity in children.

Pemoline hepatotoxicity ranges from asymptomatic elevations in levels of serum aminotransferases to fulminant liver failure. We report five cases of pemoline hepatotoxicity in children (four boys, one girl), including the only reported case resulting in orthotopic liver transplantation. We conclude that pemoline causes toxic liver damage in children. The severity of the damage is highly variable, and its onset may be late in the course of treatment. Pemoline and methylphenidate may act synergistically to cause liver damage. The levels of serum aminotransferases should be monitored throughout treatment with these agents.

Adolescent↗
PubMed1997

Pemoline-associated hepatic failure: a critical analysis of the literature.

Pemoline is a central nervous system (CNS) stimulant approved for use as part of the comprehensive medical management of attention deficit hyperactivity disorder (ADHD). An increased risk of acute hepatic failure is believed to be associated with pemoline usage, raising concerns about its prescription. A descriptive meta-analysis of the existing scientific literature and drug reporting databases was undertaken to provide more accurate understanding of this possible risk. The analysis appears to indicate that current assumptions of the risk of acute hepatic failure posed by pemoline usage alone are overestimates. Several recommendations regarding hepatic monitoring in the setting of pemoline prescription are provided.

Adverse Drug Reaction Reporting Systems↗
PubMed1985

Oral pemoline kinetics in hyperactive children.

The time course of pemoline in plasma was investigated in seven prepubescent boys with attention-deficit disorders who were hyperactive. Maximum plasma concentrations of 4.3 +/- 1.0 mg/L were reached 2.8 +/- 1.8 hours after a single, 2 mg/kg oral dose of pemoline, followed by a monoexponential decline in plasma concentration over time. Mean t1/2 and total body clearance of pemoline were 8.6 hours and 0.65 ml/min/kg. The 600% interindividual variation in elimination t1/2 and the 300% variation in total body clearance of pemoline may explain the unpredictable nature of its dynamics and associated neurotoxicity in some cases.

Absorption↗
PubMed1996

Pemoline therapy in college students with attention deficit hyperactivity disorder: a retrospective study.

Pemoline, a dopamine agonist, is effective in children with attention deficit hyperactivity disorder (ADHD), but its efficacy in adults is unknown. The authors studied the efficacy and safety of pemoline, using retrospective chart review of treated students with ADHD over a 2-year period. Forty students met diagnostic and treatment criteria; pemoline was associated with much improved or very much improved Clinical Global Impression symptoms scores in 70% of the students during a treatment period of 14 or more days. Severity of illness scores dropped from 4.11 to 3.01 between baseline and subsequent evaluation. Nine evaluable patients had adverse events, most commonly headaches, insomnia, and decreased appetite. Five additional students, who failed to meet the treatment-duration criterion, terminated because of severe initial insomnia. The authors concluded that pemoline is effective and safe in students with ADHD and has a lower abuse potential than methylphenidate and dextroamphetamine, the other two widely used, structurally dissimilar compounds, but controlled studies may be necessary before any final conclusions are reached.

Adolescent↗
PubMed1986

Treatment of narcolepsy: objective studies on methylphenidate, pemoline, and protriptyline.

Methylphenidate, pemoline, and protriptyline were studied for their treatment efficacy in narcolepsy. A low, intermediate, and high dose level of each drug was studied for 1 week. For methylphenidate the doses were 10, 30, or 60 mg/day; for pemoline, 18.75, 56.25, or 112.5 mg/day; and for protriptyline 10, 30, or 60 mg/day. The order of dose levels was random from subject to subject and the daily dose was divided into thirds and taken in identically appearing capsules morning, noon, and afternoon. Subjects were 6 narcoleptic patients studied on methylphenidate (5 women and 1 man; mean age 54.5 + 11.7 years), 7 narcoleptic patients studied on pemoline (5 women and 2 men; mean age 43.0 + 7.1 years), and 4 narcoleptic patients studied on protriptyline (2 women and 2 men; mean age 42.5 + 16.9 years). Testing consisted of day-long sessions occurring at the end of each dose level and involving a clinical status questionnaire as well as maintenance of wakefulness, Wilkinson addition, and Digit-Symbol Substitution tests. Results were compared with 9 control subjects with no sleep disorder (5 women and 4 men; mean age 39.2 + 8.4 years) who were given placebo that was purported to be a "stimulant drug" and tested in a similar manner. Results demonstrated profound differences in ability to stay awake and perform between narcoleptic patients and controls. Data also suggested that methylphenidate significantly improves ability to stay awake. Pemoline seems to improve ability to perform. Protriptyline does not significantly alter ability to stay awake or to perform.

Adult↗
PubMed1995

Pemoline effects on children with ADHD: a time-response by dose-response analysis on classroom measures.

OBJECTIVE: To evaluate the dose-response by time-response characteristics of pemoline (Cylert) on dependent measures of behavior and academic performance in a laboratory classroom. METHOD: After a 2-week baseline, a double-blind crossover design was used to compare placebo, 18.75 mg, 37.5 mg, 75 mg, and 112.5 mg of pemoline, q.a.m., with each dose administered for 1 week. Medication was given at 9:00 A.M., and performance was measured beginning immediately and beginning 2, 4, and 6 hours after ingestion. The dependent measures included number of math problems completed correctly, teacher-recorded rates of on-task behavior and noncompliance, and teacher ratings on an Abbreviated Conners Teacher Rating Scale. RESULTS: There were linear effects of medication, with pemoline doses greater than 18.75 mg having an effect beginning 2 hours after ingestion and lasting through the seventh hour after ingestion. CONCLUSIONS: Results are contrasted with widespread misbeliefs regarding pemoline's time course and efficacy.

Attention Deficit Disorder with Hyperactivity↗
PubMed1995

Pretreatment with MK-801 inhibits pemoline-induced self-biting behavior in prepubertal rats.

The indirect dopamine agonist, pemoline (120-300 mg/kg s.c.), can induce self-biting behavior in the rat. The present study demonstrates that the non-competitive N-methyl-D-aspartate (NMDA) antagonist, dizocilpine (MK-801, 0.2 mg/kg s.c.), significantly attenuates pemoline-induced self-biting behavior, while simultaneously increasing locomotor activity. When animals received a fixed dose of MK-801 with increasing doses of pemoline, a competitive relationship emerged such that high-dose pemoline surmounted the antagonistic effect of MK-801. In contrast to spiperone, delayed administration of MK-801 was ineffective in blocking the subsequent expression of self-biting behavior, suggesting that dizocilpine exerts its protective effect early in the cascade of events which eventually leads to self-biting behavior in this paradigm.

Animals↗
PubMed1981

Pemoline-induced chorea.

Acute chorea in a child followed ingestion of pemoline mesylate. In guinea pigs, in an experimental model of chorea, chronic administration of pemoline induced behavioral supersensitivity to other dopaminergic agonists. Pemoline is similar to both d-amphetamine and methylphenidate in altering central dopaminergic sensitivity, and may cause chorea by similar mechanisms. Chronic pemoline therapy may offer no significant advantage over therapy with other indirect dopamine agonists.

Amphetamine↗
PubMed1980

[Preliminary results of a pilot study on the influence of pemoline on cerebral concentrations of lactate, pyruvate, creatine, creatinephosphate, ATP, AMP, and ADP (author's transl)].

Cerebral lactate, pyruvate, ATP, ADP, creatine and phosphocreatine concentrations were determined in old, 600 g, rats during daily application of 20 mg pemoline (Tradon) (n = 11) and placebo (n = 10). After application for 21 days there were observed no significant differences in ATP, ADP, AMP, creatine and phosphocreatine concentrations between pemoline and placebo treated rats. On the other hand, in pemoline-rats, there was a significant decrease in pyruvate, lactate concentrations and in lactate/pyruvate ratio. On account of an increased dopamine turnover caused by pemoline, a possible increasing aerobic glycolysis and thus a greater energy production are still being discussed.

Adenosine Diphosphate↗
PubMed1998

Pemoline toxicosis in a dog.

A 3-year-old German Short-haired Pointer was examined because of extreme agitation, hyperactivity, and vomiting that began within 24 hours after ingestion of approximately 750 mg of pemoline, a CNS stimulant. On physical examination, the dog was agitated, tachycardic, hyper-responsive, pyrectic, disoriented, and had mydriasis. These signs were consistent with excessive stimulation of the CNS and sympathomimetic effects resulting from pemoline toxicosis. Serial blood and urine samples were obtained, and toxicologic analyses were performed. Extrapolation of the plasma pemoline concentration 32 hours after ingestion provided an estimated peak plasma concentration of 368 micrograms/ml, dramatically higher than a therapeutic concentration of 1.7 to 7.0 micrograms/ml reported for children. Several sedatives were administered intravenously to alleviate clinical signs and to allow administration of activated charcoal (PO) and fluids (IV). Clinical signs resolved approximately 72 hours after ingestion of pemoline.

Animals↗
PubMed1998

Response to growth hormone in attention deficit hyperactivity disorder: effects of methylphenidate and pemoline therapy.

OBJECTIVE: To determine whether treatment of attention deficit hyperactivity disorder (ADHD) with methylphenidate hydrochloride or pemoline diminishes the response to growth hormone (GH) therapy in patients with idiopathic GH deficiency (IGHD) or idiopathic short stature (ISS). METHODS: The National Cooperative Growth Study database was used to identify patients between 3 and 20 years of age with IGHD or ISS and those within these groups who were treated with methylphenidate or pemoline for ADHD. Their growth in response to GH treatment (change in height standard deviation score [SDS]) was compared with that of patients with IGHD or ISS who were not treated for ADHD, by using a stepwise multiple regression analysis. RESULTS: In the IGHD cohort, there were 184 patients who were being treated for ADHD and 2313 who were not. In the ISS cohort there were 117 patients who were being treated for ADHD and 1283 who were not. There was a higher percentage of males being treated for ADHD in both cohorts. In the IGHD cohort, the change in height SDS was positively associated with the number of years of GH treatment, parents' heights, body mass index, and GH injection schedule, and was negatively associated with height SDS at the initiation of GH therapy, age, and maximum stimulated GH level. The use of methylphenidate or pemoline had a negative effect on the change in height SDS, but the magnitude of the effect was small. Similar effects were noted in the ISS cohort, but body mass index and the use of methylphenidate or pemoline had no effect on the change in height SDS. CONCLUSIONS: Concurrent ADHD therapy is associated with a slight decrease in the change in height SDS during GH treatment in patients with IGHD but not in those with ISS. Even in IGHD, the magnitude of the effect is small and should not deter the use of such concurrent therapy.

Attention Deficit Disorder with Hyperactivity↗
PubMed1981

Effect on growth in pemoline-treated children with attention deficit disorder.

The growth of 22 children with attention deficit disorder (ADD) was monitored longitudinally for up to four years. Each child received at least one year of continuous, successful pemoline (Cylert) therapy, after which drug "vacations" were allowed. The effective dosage of pemoline ranged from 56 to 150 mg/day during the first year of treatment. Stature and weight measurements at six-month intervals were matched to those of paired "normal" children from the Fels Longitudinal Study. Significant deficits were observed for mean weight change at six and 12 months after baseline, and for mean stature change at 12 and 18 months after baseline. However, all subsequent six-month results up to four years did not differ significantly between the two groups. These results show a temporary retardation in the rate of growth in weight and stature with later catch-up growth in children treated wih pemoline.

Adolescent↗
PubMed1980

Pemoline-induced self-biting in rats and self-mutilation in the deLange syndrome.

Self-mutilation in humans occasionally accompanies physiological disorders such as the deLange syndrome. If pemoline-induced self-biting is behaviorally similar to self-mutilation in the deLange syndrome, similar neurochemical mechanisms may be involved in both. Oral administration of 140 and 220 mg/kg pemoline reliably induced persistent self-biting in rats. This behavior was indistinguishable from stereotyped grooming and its most common target was the medial digits of the foreleg. Pemoline-induced self-biting was accompanied by hyperactivity, stereotyped behavior, abnormal social behavior, abnormal sensorimotor behavior, and unresponsiveness or avoidance of moderate levels of sensory stimuli. Several of these behaviors have also been reported in deLange patients.

Animals↗
PubMed1996

Pemoline produces ipsilateral turning behavior in unilateral 6-OHDA-lesioned rats.

1. Male Sprague-Dawley rats received either a unilateral injection of 6-hydroxy-dopamine or vehicle injection into the medial forebrain bundle. 2. Two weeks post surgery, all rats received a pemoline challenge (250 mg/kg s.c.), and rotational and stereotyped behaviors were videotaped and analyzed. 3. All rats regardless of injection expressed stereotyped behaviors and hyper-locomotion after pemoline challenge. 4. High performance liquid chromatography (HPLC) with electrochemical detection was used to evaluate changes in the levels of dopamine, serotonin and their metabolites in neostriata. 5. Rats with dopamine depleting lesions exhibited ipsilateral rotational behavior, indicating that pemoline, a central stimulant, is an indirect dopamine agonist in the rat. 6. The extent of dopamine depletion and serotonin elevation in the neostriatum in lesioned animals was related to the expression and degree of rotational behavior.

Animals↗
PubMed1986

Evidence of lack of abuse or dependence following pemoline treatment: results of a retrospective survey.

Pemoline is recognized as an efficacious and safe therapeutic agent for children suffering from Attention Deficit Disorder (ADD). A review of adverse experience reports submitted to the manufacturer suggests that Cylert (brand of pemoline) has a limited potential for abuse or dependence. Drug dependence studies in animals have demonstrated that pemoline is not self-administered in naive nor cocaine-dependent animals. Human experience indicates that, despite the fact that the drug has been available in the U.S. since 1975, use is limited and is increasing slowly. A review of the literature revealed no published case reports of euphoria, abuse, dependence or withdrawal. While there have been a few reports of tolerance, it is possible that these were a reflection of inadequate dosing rather than actual tolerance to the drug's therapeutic effects. During the 10 years that Cylert has been available in the United States, there have been only four reports of withdrawal reactions and no reported cases of dependence. Reports of intentional overdose of Cylert are minimal, with no reports involving abuse via the intravenous route.

Adolescent↗
PubMed2006

A rare case of dependence on pemoline.

This is the first case to report about a patient dependent on the dopaminergic CNS-stimulant pemoline. Throughout the treatment of adult attention-deficit hyperactivity disorder (ADHD) with pemoline mental (e.g. craving, loss of control) and physical symptoms (e.g. tolerance, withdrawal symptoms) appeared that fulfill the DSM-IV or ICD-10 criteria for dependence on psychostimulants. However, the dependence was regarded not to be induced by pemoline itself because the patient was prone to irregular and reinforced intake of amphetamines since her adolescence. Therefore, this case confirms the experience that in the treatment of ADHD the high risk to develop a dependence on psychostimulants is combined with a history of stimulant abuse.

Adult↗
PubMed1977

Gas chromatographic determination of pemoline as 5-phenyl-2,4-oxazolidinedione in human urine.

A simple gas chromatographic assay of the psychostimulant pemoline in human urine has been developed. Instead of extraction of the drug from urine, it is hydrolysed to 5-phenyl-2,4-oxazolidinedione with 1 N hydrochloric acid. After the extraction, this compound is methylated with diazomethane and determined by gas-liquid chromatography using a nitrogen-selective detector and a solid injection system. The method has been applied in preliminary human pharmacokinetic studies, by measuring the urinary excretion rate of pemoline following oral administration. At present, the screening procedures for doping control do not involve the detection of pemoline, but the method described can easily be incorporated in such procedures.

Chromatography, Gas↗
PubMed1999

Paradoxical effects of serotonin and opioids in pemoline-induced self-injurious behavior.

Self-injurious behavior (SIB) is a symptom of various psychiatric disorders with differing etiologies. Although no generally effective pharmacological treatment of SIB is available, subsets of individuals exhibiting SIB have been found to respond to opioid antagonists and selective serotonin reuptake inhibitors (SSRIs). The present study evaluated the efficacy of these two treatments in the pemoline-induced model of self-biting behavior (SBB) in rats. Using a factorial design, adult rats receiving daily pemoline at 100 mg/kg or the peanut oil vehicle were pretreated with either distilled water vehicle (1 cc/kg), naltrexone (1 mg/kg), or paroxetine (1 mg/kg). Each day, animals were rated on the severity of SBB and also periodically behavioral changes were evaluated using various other outcome measures. Paroxetine significantly increased the severity of SBB induced by pemoline, while naltrexone only marginally increased the SBB. These results were not expected and suggest that further studies into the role of serotonin agonists and antagonists are needed in evaluating this model.

Amphetamine↗