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At least 19 recordsLinked to original sources
PubMed1987

Determination of chlormezanone in human plasma after administration of chlormezanone formulations.

In the course of a bioavailability study some 800 plasma samples were analysed by means of HPLC after administration of 5 different chlormezanone formulations to 10 healthy male volunteers. A metabolic product of chlormezanone (I) could not be detected in any of the samples. The results were further verified through mass spectrometric measurements of chlormezanone, extracted from the plasma sample and separated through HPLC, in off-line mode. Chlormezanone is found as an intact molecule in human plasma samples.

Adult↗
PubMedDate not supplied

Chlormezanone plasma and blood levels in patients after single and repeated oral doses and after suicidal drug overdose.

Chlormezanone plasma concentrations were determined in 5 volunteers (group 1) after a single oral dose of 200 mg of chlormezanone with high performance liquid chromatography. A plasma elimination half-life of 23 +/- 2.3 h was calculated. The mean peak chlormezanone plasma level was 1.86 +/- 0.2 micrograms/ml, 1 h after ingestion. Additionally, chlormezanone plasma levels were determined after repeated oral doses of chlormezanone recommended for treatment of muscular spasms due to degenerative skeletal disease. After 5 days of repeated daily doses of 3 x 200 mg (group 2; 12 patients) or 3 x 400 mg (group 3; 10 patients) of chlormezanone, mean predose chlormezanone plasma levels were 12.0 +/- 2.0 micrograms/ml (group 2) and 22.7 +/- 4.0 micrograms/ml (group 3), respectively. Comparable plasma concentrations were determined after 10 days of repeated doses of 3 x 200 mg or 3 x 400 mg of chlormezanone in 3 patients from each of these 2 groups. In 7 patients of group 3, chlormezanone had to be discontinued on the 5th day due to increasing muscular weakness, ataxia and exercise-inducible tachycardia. After a loading dose of 800 mg and repeated doses of 3 x 200 mg chlormezanone to 5 patients (group 4), plasma levels of 6.5 +/- 2.1 micrograms/ml, 8.9 +/- 2.2 micrograms/ml, 12.7 +/- 2.0 micrograms/ml, and 10.4 +/- 2.4 micrograms/ml were determined after 2, 8, 16, and 36 h, respectively. Trace amounts of a degradation product of the acid-labile chlormezanone could be detected in plasma besides the unchanged drug after administration of repeated oral doses.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗
PubMed1983

Treatment of sleep disturbance in arthritis with chlormezanone.

A double-blind, crossover study was carried out in 31 patients with rheumatoid arthritis or osteoarthritis who suffered from insomnia which was considered to be caused primarily by their disease. Patients received 7-day courses of 400 mg chlormezanone, 200 mg chlormezanone and placebo in a pre-determined random order. Patients rated chlormezanone significantly (p less than 0.025) more effective than placebo in overcoming sleep disturbance and preferred the 400 mg dose. There was also a trend towards better quality of sleep with chlormezanone, although this did not attain statistical significance in this relatively small study. Daytime alertness was similar for both active and placebo treatment periods. Chlormezanone, therefore, would seem to be a useful addition to antirheumatic therapy when there is related insomnia.

Arthritis, Rheumatoid↗
PubMed1983

Chlormezanone: its effects on subjective aspects of sleep and on skilled performance related to car driving.

A double-blind, crossover study compared chlormezanone 200 mg t.d.s., chlormezanone 400 mg nocte and placebo in twelve female volunteers. There was no obvious evidence of chlormezanone causing an impairment in early morning psychomotor performance, car driving ability or subjective ratings of early morning behaviour. Subjectively reported mood changes were consistent with those expected of a tranquillising drug and the sleep-inducing and improving properties of chlormezanone were confirmed. This volunteer study suggests that chlormezanone may well be a nocturnal sedative which does not have a morning hangover effect.

Adult↗
PubMedDate not supplied

Interaction of chlormezanone with rat liver microsomes and its degradation.

Chlormezanone binds to oxidized cytochrome P450 in rat liver microsomes with a binding curve according to type I like hexobarbital but less pronounced and with a general shift to the left. Ethylmorphine N-demethylation, ethoxycoumarin and ethoxyresorufin O-deethylation are inhibited by chlormezanone in mM concentrations only whereas pentoxyresorufin O-depentylation is inhibited by about 50% in microM concentrations. Luminol and lucigenin amplified chemiluminescence indicating the formation of reactive oxygen species was not influenced in concentration ranges between mM and microM, whereas NADPH/Fe stimulated lipid peroxidation showed a tendency of inhibition. But scavenger activity could not be demonstrated: the zymosan stimulated chemiluminescence of whole blood was not influenced significantly. The degradation process of chlormezanone was elucidated. The first step involves ring opening by chemical hydrolysis with subsequent formation of an unstable acylhalfaminal which is the source of 4-chlorobenzaldehyde. This aldehyde undergoes enzymatically controlled oxidation to 4-chlorobenzoic acid which is the parent compound of following phase II reactions. The second degradation product is 2-carboxyethane-sulfinic-acid-N-methylamide, which is hydrolyzed very quickly. Neither oxidation of the sulfinic acid or its N-methylamide derivative could be observed nor N-demethylation of chlormezanone.

Animals↗
PubMed1980

Sensitive and selective method for the determination of chlormezanone in plasma by electron-capture gas chromatography.

A sensitive and selective determination method of chlormezanone in plasma has been divised. Chlormezanone in plasma was extracted with toluene at pH 4.5, and converted into p-chlorobenzaldehyde in 0.1 N NaOH. Using p-bromobenzaldehyde as an internal standard, the hydrolysis product and the internal standard were extracted with n-hexane, and the extract was concentrated in vacuo in the presence of isoamyl alcohol to prepare the sample solution. The sample solution was submitted to electron-capture gas chromatography. Chlormezanone was determined by use of the peak height ratio of p-chlorobenzaldehyde against the internal standard. The method was utilized successfully for pharmacokinetic studies of chlormezanone in plasma.

Benzaldehydes↗
PubMed1982

Chlormezanone in the treatment of migraine attacks: a double blind comparison with diazepam and placebo.

One hundred and fifty patients treated for an acute migraine attack all received a standard regimen consisting of metoclopramide 10 mg i.m. and--20 min later--paracetamol 1 g orally. Simultaneous trial medication was given. This consisted of placebo, diazepam 5 mg as tablets, or chlormezanone 400 mg as capsules given in a double dummy fashion. A successful treatment result was defined as a decrease of two or three steps on a four-point verbal pain report scale, and no need for further treatment. Patients with severe pain (all three treatment groups together) showed significantly better treatment results (p less than 0.001) than patients with pain of medium severity. In the group with severe pain there was no significant difference between diazepam, chlormezanone or placebo. In the group with pain of medium severity there was a significant (p less than 0.01) effect of chlormezanone, but no significant effect of diazepam. Chlormezanone may possibly be a valuable addition to antiemetic and analgesic therapy of migraine attacks.

Acetaminophen↗
PubMed1981

A double-blind study of benorylate and chlormezanone in musculoskeletal disease.

In a double-blind, cross-over study of 90 patients with degenerative disease of the hip, knee, cervical or lumbar spine, and capsulitis of the shoulder the analgesic drug benorylate (either alone or in combination with chlormezanone, a muscle relaxant anxiolytic drug) favourably modified pain, stiffness, quality of sleep and ability to work. Chlormezanone significantly reduced the number of breaks in sleep. There was no significant difference in the number of patients reporting side-effects on each of the four treatments, but drowsiness occurred significantly more in the chlormezanone weeks. There appeared to be no advantage in adding chlormezanone in patients suffering from osteoarthritis of the hip or knee, lumbar spondylosis or capsulitis of the shoulder, but there was significant improvement in both pain relief and quality of sleep in those patients with neck pain.

Chlormezanone↗
PubMed1982

A comparison of the effects of chlormezanone and nitrazepam on sleep.

1 Twelve volunteers, of mean age 60 years, took part in a double-blind, balanced cross-over study, to compare effects of chlormezanone 400 mg and nitrazepam 5 mg on electrophysiologically-recorded and subjectively-rated sleep. 2 In the first week of administration nitrazepam caused a significant shortening of the time to fall asleep, but following withdrawal subjects took longer to fall asleep than during the baseline period. 3 Both chlormezanone and nitrazepam initially caused increase of sleep duration and less interruption of sleep by wakefulness. By the third week, for chlormezanone this effect was no longer significant, and for nitrazepam there was a significant decline in the effect. There was no statistically significant difference between the two drugs for these measures. 4 The drugs differed little in their effects on the amount of the various sleep stages, except that nitrazepam significantly reduced the duration of slow wave sleep, whereas chlormezanone had no significant effect on slow wave sleep. Both drugs reduced the amount of REM sleep in the first 6 h of sleep but only nitrazepam reduced the percentage of the time spent in REM sleep of the whole night. 5 Subjects' own ratings of sleep quality showed that both of the drugs improved sleep, but following withdrawal it was only after nitrazepam that there was impairment of the quality of sleep. Neither drug affected subjective alertness in the morning.

Adult↗
PubMed1990

Central anticholinergic syndrome after ofloxacin overdose and therapeutic doses of diphenhydramine and chlormezanone.

A 14-year-old female with no history of psychiatric disease ingested an unknown amount of ofloxacin, diphenhydramine and chlormezanone after an argument with her patients. Approximately 12 hours after ingestion, the patient was admitted to the hospital in a delirious state with extreme mydriasis and warm and dry skin. Analytical data on admission were consistent with ofloxacin overdose and ingestion of therapeutic doses of diphenhydramine and chlormezanone. The patient received activated charcoal and forced diuresis was instituted. Psychosis and anticholinergic symptoms lasted in the next 2 days. On day 3, the psychotic and anticholinergic symptoms were nearly completely reversed by 2 mg physostigmine salicylate, given IV x 2. Since anticholinergic symptoms have not been observed after ofloxacin overdose or after therapeutic doses of diphenhydramine or chlormezanone, this case suggests a potentiation of the anticholinergic effects of diphenhydramine and chlormezanone by ofloxacin overdose.

Adolescent↗
PubMed1982

Hypnotics and hangovers: a pilot study of chlormezanone in general practice.

Ten patients were included in this pilot study of chlormezanone, assessing its effects on duration and quantity of sleep and daytime performance using a pursuit rotor and a digit symbol test. Comparisons of the sleep assessments favoured chlormezanone, although the differences were not statistically significant. There was no evidence of any reduction in daytime performance after chlormezanone. The comparison of chlormezanone and placebo on the pursuit rotor test and the visual analogue assessment of hangover both slightly favoured the drug, but there were no significant differences. The study has demonstrated that it is feasible to evaluate hypnotic drugs more exactly in general practice.

Adult↗
PubMed1996

[Flupirtine in comparison with chlormezanone in chronic musculoskeletal back pain. Results of a multicenter randomized double-blind study].

METHOD: The analgesic and muscle-relaxing properties of flupirtine maleate, chlormezanone and placebo were compared in a total of 184 patients. Of these patients, 164 met the criteria of the treatment plan (intention to treat), and the data of 140 patients were finally evaluated in accordance with the test protocol. A positive response was defined as a reduction in pain intensity and muscle tension by 2 categories on the 5-category verbal scale "very severe/severe/moderate/mild/ none" on the seventh day of treatment. RESULTS: In the per-protocol-analysis the responder rate was 60.9% for flupirtine, 47.8% for chlormezanone, and 43.8% for placebo, the difference between drugs and placebo not being significant. The overall assessment of the physicians involved was very good/ good in 47.8% and satisfactory in 37.0% of the flupirtine group, very good/good in 45.6% and satisfactory in 17.4% of the chlormezanone group, the corresponding figures for the placebo group being 33.4% and 20.6%, respectively. Flupirtine was thus superior to placebo (p = 0.007). The incidence of adverse drug reactions was 14.8% (8/54) for flupirtine, 19.3% (11/57) for chlormezanone, and 7.3% (4/55) for placebo.

Adult↗
PubMed1993

Chlormezanone in primary fibromyalgia syndrome: a double blind placebo controlled study.

Primary fibromyalgia syndrome (PFS) is a common condition that often proves resistant to health interventions. Chlormezanone combines corrective effects on disturbed sleep with muscle-relaxant properties, and therefore could be of potential benefit in PFS. Forty-two female patients with PFS (mean age 49, range 24-72 years) were randomly and blindly allocated either chlormezanone 400 mg nocte or placebo. Patients were assessed by single observer at 0, 3 and 6 weeks of treatment; assessments included sleep quality, inactivity and morning stiffness, morning alertness, tender point score, mood change and global opinion (patient and observer). No beneficial therapeutic effect could be attributed to chlormezanone. Although there are problems in assessing severity of a predominantly subjective condition, this essentially negative finding is of interest in respect to the pathogenesis of PFS.

Adult↗
PubMedDate not supplied

Investigations of interactions of chlormezanone racemate and its enantiomers on human keratinocytes and human leucoytes in vitro.

Chlormezanone is a centrally acting muscle relaxant introduced in human therapy as a racemic substance. The following investigation was performed in order to investigate whether the racemate and both enantiomers differ in their potential cytotoxicty in vitro. We investigated antiproliferative effects and cytotoxicity (PicoGreen and ATP assay) for human HaCaT keratinocytes, production of oxygen radicals (ROS) by human interleukin-3-stimulated leukocytes (Lucigenin assay) and production of sulfoleukotrienes (Cellular Antigen Stimulation Test - CAST) by human leukocytes. In the dosage range of 0.001 to 0.1 mg/ ml chlormezanone, no antiproliferative effects were measured with the racemate and both enantiomers. At 1.0 mg/ml, a decrease of proliferative activity was seen after 48 h incubation time of about 50% for the enantiomers and of about 80% for the racemate (PicoGreen) and 50% (enantiomers) or 21% (racemate) in the ATP assay, respectively. ROS production was significantly inhibited at concentrations < or =0.01 mg/ ml by the racemate and the (+)-enantiomer, whereas the (-)-enantiomer was less effective. There was no stimulation of sulfidoleukotrienes in human leukocytes by chlormezanone. Present data argue for absence of significant cytotoxicity against human HaCaT keratinocytes and a dose-dependent suppression of ROS production by human leukocytes that is not uniform among the racemate and its enantiomers.

Adenosine Triphosphate↗
PubMed1982

Four-week tolerance study of chlormezanone for the treatment of insomnia in the elderly.

A 4-week study of chlormezanone was carried out in thirty-two patients admitted to a geriatric ward and requiring regular night sedation. Two patients required 400 mg nightly, the remainder only 200 mg nightly. The duration and quality of sleep, and frequency of awaking refreshed, all improved during chlormezanone therapy. There was no deterioration in mental agility test performance. There were no serious side-effects, no significant changes in blood urea or liver function tests, and no evidence of drug accumulation. It is concluded that chlormezanone appears to be a well tolerated drug for elderly patients with sleep disturbance meriting further controlled evaluation.

Aged↗
PubMed1991

Provocation tests in a chlormezanone-induced fixed drug eruption.

Although as few as seven cases of fixed drug eruption (FDE) due to chlormezanone have been reported, it should not be overlooked as a cause of FDE. To identify the causative agent in FDEs, topical provocation tests are much safer and more convenient than systemic provocation tests. If results of topical provocation tests are reliable, they could become useful diagnostic as well as screening tests. Patch tests were performed in a suspected case of FDE due to chlormezanone on the patient's normal and prelesional skin with all ingested drugs whose concentrations were one and ten percent. The base was petrolatum. A positive reaction occurred only at the previously lesional site tested with chlormezanone, and was confirmed with oral provocation tests.

Adult↗