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At least 19 recordsLinked to original sources
PubMed1992

Pharmacodynamics of pemoline in attention deficit disorder with hyperactivity.

The onset, duration, and offset of pemoline action to improve cognitive performance is examined intensively in 25 prepubescent males suffering from attention-deficit disorder with hyperactivity (ADDH). The purpose was to characterize the pharmacodynamics of pemoline in ADDH patients through correlation of plasma pemoline concentration with psychometric measures of memory search efficiency and paired-associates learning, with the physiological effect of pemoline on dopaminergic transmission concurrently measured by analysis of plasma prolactin response. The effect of pemoline on neuroprocessing is apparent within the first 2 hours after administration with an inverse relationship between plasma pemoline and prolactin concentration present at hour one only (r = 0.84; p = 0.005). Pemoline therapy for 3 weeks does not significantly affect area under the curve for pemoline or prolactin nor did the effect on memory search efficiency decrease, suggesting no apparent tolerance.

Attention↗
PubMed1990

Hepatotoxicity due to pemoline (Cylert): a report of two cases.

Pemoline (Cylert) is an agent used to treat attention deficit disorders and other behavioral syndromes. There have, however, been three published reports of mild hepatic dysfunction in five patients coincident with pemoline therapy. We report two further cases of probable pemoline hepatotoxicity. One case involved a mild aminotransferase elevation in a 6-year-old who was on pemoline for 5 months. The second case, in an 11-year-old, developed hepatic failure with marked prolongation in prothrombin time nonresponsive to parenteral vitamin K, deep jaundice, and submassive hepatic necrosis. This patient had a long history of pemoline usage. Pharmacokinetics are briefly discussed. A spectrum of hepatic disease due to pemoline is considered and the importance of obtaining aminotransferase values before, during initiation, and throughout treatment is stressed.

Attention Deficit Disorder with Hyperactivity↗
PubMed1977

Gas chromatographic determination of pemoline in biological fluids using electron capture detection.

A simple and sensitive gas chromatographic (GC) method for the determination of pemoline in biological fluids, utilizing electron capture detection is described. Plasma samples with a pemoline analog added as internal standard were deproteinized with sulfosalicylic acid, and the supernatants were heated at 80 degrees. The pemoline-dione formed was extracted with benzene, and the extract was analyzed on a gas chromatograph equipped with a tritium foil electron capture detector. Poly A-103 (3%) on Gas-Chrom Q (100-120 mesh) packed in a 3-ft. silanized glass column was used as the stationary phase, with nitrogen serving as carrier gass. Under the same GC conditions, benzene extracts of pemoline-dione from acid-hydrolyzed urine samples were analyzed. Us-ng 1 ml of plasma or urine, the lower limit for the assay was about 0.1 microgram/ml. The method is accurate and reproducible, with a relative standard deviation with +/-4%. Mandelic acid (a metabolite of pemoline) does not interfere with the assay.

Animals↗
PubMed1978

The effects of pemoline on nuclear fusion, karyokinesis, and cytokinesis in caffeine treated cells.

The effect of 0.2% caffeine combined with 5-phenyl-2-imino-4 oxazolidone (pemoline, Tradon), in different ways, on mitosis in lateral roots of Vicia faba L. has been studied by means of aerated hydrocultivation. The results show that prolonged treatment with 10(-6) g/ml or 3 x 10(-4) g/ml (=saturated solution) pemoline to a certain degree compensates the negative influences of caffeine on mitotic index during and after the caffeine treatment. Depending on the duration of treatment 10(-6) g/ml pemoline are able to increase rates of nuclear fusions, bimitoses and 4n-mitoses, while 3 x 10(-4) g/ml have the opposite effects. The number of irregular cytokineses is increased by 10(-6) g/ml, whereas no abnormal cell walls are formed during treatment with 3 x 10(-4) g/ml pemoline. The conclusion is that pemoline has the same sites of action as caffeine, partly antagonistically, partly synergistically.

Caffeine↗
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↗
PubMed1979

The clinical and psychological effects of pemoline in depressed patients--a controlled study.

The clinical and psychological effects of pemoline were compared with placebo in a double-blind study of 20 depressed patients. Target symptoms were disturbances of concentration and memory, tension, depression, fatigue, decreased libido, anorexia and insomnia. The two groups were matched for their clinical picture, age, sex, and duration of illness. During the three-week study period the pemoline group received 50 mg daily. Significant differences in some clinical symptoms were found between the groups, but not in the performance of psychological tests, administered before and after the three-week study period. These differences proved the effectiveness of pemoline in combating symptoms of disturbances in concentration, memory, tension, depression and fatigue.

Adult↗
PubMed1992

A double-blind, randomized, crossover trial of pemoline in fatigue associated with multiple sclerosis.

Fatigue occurs in a majority of patients with MS and is generally independent of measurable neurologic disability. Few options for treatment are available. We conducted a double-blind, placebo-controlled, crossover trial for each of two 4-week treatment periods. Forty-six eligible patients entered and five dropped out due to concurrent exacerbations. Nineteen patients (46.3%) experienced excellent or good relief of fatigue with pemoline, and eight patients (19.5%) with placebo (p = 0.06, Fisher's exact test). One-fourth of patients did not tolerate the drug well, and 7% had to discontinue pemoline during the study due to side effects. The most common side effects were anorexia, irritability, and insomnia. Pemoline may be an effective short-term treatment for fatigue associated with MS, but its adverse effects are not well tolerated by many patients.

Adult↗
PubMed1978

GLC determination of pemoline in biological fluids.

A specific GLC method for the determination of microgram quantities of the central stimulant pemoline in biological fluids is described. Extraction problems due to the low solubility of pemoline are avoided by acid hydrolysis of the drug to 5-phenyl-2,4-oxazolidinedione, which then can be easily isolated by two-phase extraction with dichloromethane, ether, or chloroform. Amide-imide tautomerism enables a cleanup of the extract. Quantitative determination at the microgram level is done on a methylated fraction of the dichloromethane extract by GLC using a suitable internal standard. For supporting evidence of the GLC method's specificity, the compound is also identified by examining an aliquot of the final dichloromethane extract by TLC.

Chromatography, Gas↗
PubMed1979

Sensitive GLC assay for pemoline in biological fluids using nitrogen-specific detection.

Extractive alkylation was used to determine intact pemoline in serum and urine. Pemoline was extracted into methylene chloride as an ion-pair with tetrapentylammonium hydroxide under alkaline conditions. Evaporation of the solvent at 70 degrees in the presence of methyl iodide yielded the N,N-dimethylpemoline derivative. GLC analysis was performed on a 5% FFAP column with nitrogen-specific detection. Sensitivity was 0.05 microgram/ml with 1 ml of urine of serum. Calibration curves were linear to at least 4 microgram/ml with serum and 15 microgram/ml with urine. Precision was excellent with a pooled relative standard deviation of +/- 7.5% for serum samples in a 0.1-4 microgram/ml range.

Chromatography, Gas↗
PubMed1975

Antagonistic effects of pemoline to colchicine and caffeine.

Pemoline, the constituent of Tradon, is able to slow down the decrease of the mitotic index caused by 0.1% caffeine in roots of Vicia faba, and mitotic aberrations are reduced. With 0.005% colchicine and 3 x 10(-4) g/ml pemoline, no metaphase-accumulation can be observed, and anaphase-disorder is delayed.

Caffeine↗
PubMed1978

Assay of pemoline in human plasma, saliva and urine by capillary gas chromatography with nitrogen-selective detection.

A simple gas chromatographic assay of the psycho-stimulant pemoline in human urine, plasma and saliva has been developed. Instead of direct extraction of the drug from urine, plasma and saliva, it is hydrolyzed to 5-phenyl-2,4-oxazolidine-dione with 1 N hydrochloric acid. After extraction this compound is methylated with diazomethane and determined by gas-liquid chromatography using a capillary SCOT column with a mixed stationary phase, a solid injection system and a nitrogen-selective detector. 5-Phenyl-2,4-oxazolidinedione, which was also found to be a metabolite of pemoline, could be determined quantitatively in human urine.

Chromatography, Gas↗
PubMed1979

Impaired growth in hyperkinetic children receiving pemoline.

Decreased longitudinal growth was observed in 24 hyperkinetic children receiving pemoline therapy. Mean height velocity was 3.67 +/- 0.25 cm/year during therapy but 5.35 +/- 0.42 cm/year after treatment had been discontinued (P less than 0.01). There appeared to be an inverse relationship between growth velocity and drug dosage. All patients receiving less than the median dose of 3.72 mg/kg grew 4 cm/year or more, while seven of 12 patients receiving more than this dose grew at a slower rate. Body weight, basal and stimulated growth hormone values, and plasma somatomedin concentrations were not significantly altered by pemoline treatment, suggesting that this drug may have a direct effect on cartilage metabolism.

Body Height↗
PubMed1990

Relative efficacy of long-acting stimulants on children with attention deficit-hyperactivity disorder: a comparison of standard methylphenidate, sustained-release methylphenidate, sustained-release dextroamphetamine, and pemoline.

Twenty-two children with attention deficit-hyperactivity disorder underwent a double-blind, placebo-controlled, crossover evaluation of the efficacy of standard methylphenidate twice a day and comparable doses every morning of a sustained-release preparation of methylphenidate (SR-20 Ritalin), a sustained-release form of dextroamphetamine (Dexedrine Spansule), and pemoline. The children were participating in a summer treatment program in which they engaged in recreational and classroom activities. Dependent measures include evaluations of social behavior during group recreational activities, classroom performance, and performance on a continuous performance task. Results revealed generally equivalent and beneficial effects of all four medications. Dexedrine Spansule and pemoline tended to produce the most consistent effects and were recommended for 10 of the 15 children who were responders to medication. The continuous performance task results showed that all four medications had an effect within 2 hours of ingestion, and the effects lasted for 9 hours. The implications of these results for the use of long-acting stimulant medication in children with attention deficit-hyperactivity disorder are discussed.

Adolescent↗
PubMed1976

[The effect of pemolin on the mitotic activity of Vicia faba L (author's transl)].

The effect of diverse concentrations of 5-phenyl-2-imino-4-oxazolidone (PIO, pemolin, Tradon) on the mitotic activity in lateral roots of Vicia faba L. was studied by aerated and non-aerated hydrocultivation with and without mineral nutrition, respectively. With optimal conditions (aerated nutrient solution) weak PIO-concentrations, most significantly 10(-6) g/ml, effected a marked increase of the mitotic index. Contrarily, strong PIO-concentrations (10(-4) and 3 X 10(-4) g/ml = saturated solution) significantly decreased the mitotic index though simultaneously preserving the mitotic activity in long-term experiments, when on account of nutrient deficiency it had already collapsed in weak PIO-concentrations and the controls. The activating effect of weak PIO-concentrations compared with the controls is more significant in stress situations (nutrient deficiency, O2-deficiency) than under optimal conditions. Furthermore a slight acceleration of mid-mitotic phases (metaphase--anaphase) recognized by a marked decrease in percentage of these phases, can be stated with weak PIO-concentrations, again particularly so with 10(-6) g/ml. In total, dependent on concentration, pemolin presumably may either activate or suppress cell metabolism and particularly the mitotic cycle. The exact site of action of the substance is still unknown.

Air↗
PubMed1990

Pemoline-associated hepatic injury.

Among 100 cases of hepatic injury attributed to the administration of pemoline, 43 had sufficient accompanying information to permit analysis. All but two patients were less than 20 years old, and 80% were less than 12 years old. Males predominated the study. Injury appeared as early as 1 week or as late as greater than 1 year of taking the drug. The injury was uniformly hepatocellular as judged by the high values for aminotransferases and by death in massive necrosis in one patient. Mechanism was judged to be idiosyncratic, and the idiosyncrasy was probably metabolic rather than immunologic.

Adolescent↗
PubMed1976

Clinical trial with amantadine and pemoline in elderly patients.

In a controlled clinical trial, amantadine 400 mg daily, 200 mg daily and 200 mg daily given with 20 mg of pemoline daily were compared with placebo in the treatment of elderly patients suffering from involutional cerebropathy characterized by psychomotor slowing down. The results showed that amantadine 400 mg daily was superior to placebo but was associated with a high incidence of side-effects (37 per cent), amantadine 200 mg daily was not superior to placebo but when pemolint 20 mg daily was added the combination was superior to placebo and few side-effects were reported.

Aged↗