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At least 73 records · Page 4Linked to original sources
PubMed2002

Chiral separation of pemoline enantiomers by cyclodextrin-modified micellar capillary chromatography.

Micellar electrokinetic chromatography (MEKC) was successfully applied to the chiral separation with the addition of cyclodextrins (CDs) as chiral selector to running buffer. Chiral separation depended on the type of CDs. Mono-3-O-phenylcarbamoyl-beta-CD was effective for the chiral separation of pemoline. We investigated the type and concentration of CD and other parameters such as buffer pH, the concentration of SDS and the effect of organic modifier. The conditions for enantiomeric separation of pemoline were as follows: 40 mmol/l borate buffer at pH 9.0 with 40 mmol/l SDS, 20 mmol/l mono-3-O-phenylcarbamoyl-beta-CD and 10% 2-propanol. Baseline separation (Rs=2.21) of pemoline can be achieved.

Chromatography, Micellar Electrokinetic Capillary↗
PubMedDate not supplied

Pemoline for the treatment of cocaine dependence in methadone-maintained patients.

The authors conducted an open-label trial of pemoline, a dopaminergic CNS stimulant, for the treatment of cocaine addiction in methadone-maintained patients. Ten patients who met DSM-III-R criteria for cocaine dependence participated in an eight-week study. Findings showed that 50% of patients were discontinued from the study due to complaints of side-effects. Patients who completed treatment submitted 79% positive urine toxicology screens over the course of the study. Patients who dropped out tended to submit fewer cocaine-positive urine screens than treatment completers. In view of suggestions that dopaminergic agents in the treatment of addictions may be enhanced when combined with serotonergic agents, a single-case study of pemoline plus fenfluramine is also reported. Except for one urine sample, all of this patient's urine screens were positive for cocaine. Although findings from these studies do not support the effectiveness of pemoline for the treatment of cocaine abuse in methadone-maintained patients, conclusions must be qualified by the lack of a control group.

Adult↗
PubMed1997

Pemoline in adult attention deficit hyperactivity disorder: predictors of nonresponse.

The psychostimulants are the most widely used treatment modality for attention deficit/hyperactivity disorder (ADHD). Although positive responses to psychostimulants have been demonstrated, 46% of adults with ADHD, on average, are nonresponsive or cannot tolerate the medications because of adverse effects. We reviewed the charts of 43 students treated with pemoline and studied parameters of nonresponse. Sixteen (37%) met the study definition of nonresponse. Of these 5 (12%) were symptom nonresponders and 11 (25%) were nonresponders because of adverse effects. We found a significant relationship between age and nonresponse resulting from adverse effects, yet no other factors predicted nonresponse to pemoline. Clinicians should consider using smaller starting doses of pemoline in adults to minimize adverse effects.

Adolescent↗
PubMed1980

Analysis of pemoline in serum by high performance liquid chromatography: clinical application to optimize treatment of hyperactive children.

The analysis of pemoline (2-imino-5-phenyl-4-oxazolidine) by a rapid, sensitive, and specific high performance liquid chromatographic assay using ultraviolet detection is described. Only 100 microliters of plasma or serum is required. Analytical recoveries of 88% for pemoline and 93% for the internal standard (4-methylprimidone) are obtained by this procedure. Between-day precision studies of serum controls containing 10.2, 2.0, and 0.5 mg pemoline/liter produce coefficients of variation of 6.2, 9.4, and 16.2%, respectively. A clinical study of 28 children treated with pemoline demonstrated a linear relationship between drug dose and serum concentrations with an apparent therapeutic range falling between 1.7 and 7.0 mg/liter. These serum concentrations were achieved at drug dosages between 37.5 and 112.5 mg/day.

Adolescent↗
PubMed1980

Wakefullness and reduced rapid eye movement sleep: studies with prolintane and pemoline.

1 Effects of prolintane (15 and 30 mg) and pemoline (60 and 100 mg) on sleep were studied in six healthy adult males. Sleep was assessed by electroencephalography and by analogue scales. 2 Prolintane (15 and 30 mg) reduced rapid eye movement (REM) sleep both by delaying the first period (P < 0.05 and < 0.001 respectively) and by reducing total REM sleep (P < 0.05 and < 0.001 respectively). In some subjects there were increased awakenings during the early part of the night, and in two subjects long periods of wakefulness occurred. 3 With pemoline (60 and 100 mg) sleep duration was marked reduced (P < 0.001). There was evidence in some subjects of delay to the first REM period, and reduced percentage REM sleep (P < 0.01). Shortened and fragmented sleep with 60 and 100 mg were associated with reduced sleep efficiency indices (P < 0.001), and shorter sleep period times led to reduced REM/NREM ratios. Absence of an effect on REM latency for the subjects as a group may be related to relatively slow absorption. 4 The heterocyclic amphetamine derivatives have variable effects on sleep. The differences may be dose related, and wakefulness and reduced REM sleep may be seen together or separately. Alterations in sleep occur with doses of pemoline and prolintane which also modify performance.

Adult↗
PubMed1998

Effects of pemoline on spontaneous and event-related electrical activity of the brain.

The effect of pemoline on the electrical activity of the brain (electroencephalogram, EEG) was studied in relation to time since sleep and time of day in 6 healthy subjects carrying out periods of work lasting 18 h. Power of the spontaneous EEG increased with time since sleep and amplitude of the P3 event-related response decreased. The changes may be interpreted as the reduction in alertness with time awake. In contrast, pemoline decreased power of the spontaneous EEG and increased the amplitude the P3 response, effects that are consistent with improved alertness. The changes in brain activity were paralleled by effects on performance, in terms of percentage of correct responses and reaction time. Performance decreased with time awake, and was improved by pemoline compared with placebo. The drug counteracted the adverse effects of time since sleep, with the beneficial effect of the drug persisting over the 18-hour period of work. The findings emphasise that spontaneous and event-related activity of the EEG may be used both to complement measures of performance in the laboratory and to assess behaviour in occupational situations where performance testing is impractical.

Adolescent↗
PubMed1973

Hepatotoxicity due to pemoline. Report of two cases.

Pemoline, a central nervous system stimulant, has been used extensively in Great Britain and Europe for a variety of conditions including memory failure and depression. In the 10 years that the drug has been used no report of hepatotoxicity has appeared. A prospective study of efficacy and safety of pemoline was started in the United States approximately 3 years ago. This report describes two patients who developed reversible liver abnormalities while receiving pemoline during the study and following rechallenge with the drug.

Aged↗
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↗
PubMed1985

Pemoline abuse.

Addictive use of the stimulant drug pemoline caused a delusional disorder in a middle-aged man. Discontinuance of use of the drug promptly reversed the psychosis, which subsequently recurred when pemoline was again used. Pemoline seems to be an addictive drug and has an additional property that heretofore has been attributed mainly to amphetamines--precipitation of a paranoid psychosis.

Adult↗
PubMed1980

Pemoline, methylphenidate, and placebo in children with minimal brain dysfunction.

An eight-week double-blind comparison between pemoline (Cylert), methylphenidate (Ritalin) hydrochloride, and placebo was carried out on 60 hyperactive children. Measurements of home, school, achievement, cognitive function, and global clinical status were made at baseline, midtreatment, end of treatment, and posttreatment. Both drugs produced improvement in all areas except the achievement measures. One major difference between drugs was the apparently longer action of pemoline, since its effects at home and school tended to persist when the drug was withdrawn, whereas the patients receiving methylphenidate tended to regress to their baseline levels.

Attention Deficit Disorder with Hyperactivity↗
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↗
PubMed1985

Treatment of chronic cocaine abuse and attention deficit disorder, residual type, with magnesium pemoline.

Research suggests that attention deficit disorder (ADD) may persist into adulthood, perhaps predisposing certain individuals to stimulant abuse. The authors describe two adults with chronic cocaine abuse and apparent residual ADD. After failing to respond to conventional treatment modalities, these patients were administered magnesium pemoline. Both displayed a sustained reduction in their cocaine use, without abusing pemoline. This finding suggests that the diagnostic assessment of cocaine abusers should include a search for a history of ADD. A carefully selected subgroup of this population may benefit from treatment with other stimulant medications.

Adult↗
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↗