Metabolism of chlormezanone in man and laboratory animals

McChesney, Evan W.; Banks, W. F.; Portmann, G.A.; Crain, A.V.R.

doi:10.1016/0006-2952(67)90054-8

Cited by 20 publications

(4 citation statements)

References 7 publications

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“…However this negative result may be due to the fact that the authors did not take into account the pharmacokinetics of the compound, and evaluated its phannacodynamic activity one hour after administration while the C, , , occurs between 2 hours (McChesney et al, 1967) and 4 hours after dosing (Ohya et al, 1980). In contrast, Hindmarch and Gudgeon found that the repeated administration of 600 mg per day for 5 days caused a significant decrease in performance on the digit symbol substitution test as well as a subjective feeling of tiredness.…”

Section: Accepted I7 March 1991mentioning

confidence: 95%

“…Similarly, Hindmarch and Gudgeon (1 983) found no evidence of any sedative effect of chlormezanone after a single administration of 200 mg using a test battery of established sensitivity to the sedative effects of benzodiazepines (Wittenborn, 1979;Hindmarch, 1980;Johnson and Chernik, 1982). However this negative result may be due to the fact that the authors did not take into account the pharmacokinetics of the compound, and evaluated its phannacodynamic activity one hour after administration while the C, , , occurs between 2 hours (McChesney et al, 1967) and 4 hours after dosing (Ohya et al, 1980). In contrast, Hindmarch and Gudgeon found that the repeated administration of 600 mg per day for 5 days caused a significant decrease in performance on the digit symbol substitution test as well as a subjective feeling of tiredness.…”

Section: Introductionmentioning

confidence: 99%

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Effects of acute and repeated doses of two muscle relaxants chlormezanone and thiocolchicoside, on vigilance and psychomotor performance of healthy volunteers

Patat¹,

Klein²,

Surjus³

et al. 1991

Human Psychopharmacology

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This was a randomized double blind, placebo-controlled cross over study performed on 12 healthy female volunteers. It consisted of three treatment sessions of 7 days separated by a one week wash out period. The objectives of the study were to assess the sedative activity of 2 muscle relaxant drugs: chlormezanone (600 mg daily) and thiocolchicoside (I6 mg daily) after a single oral administration and at steady state (day 7).The drugs were administered orally, during each treatment period as 3 capsules daily for 7 days. Assessment criteria explored psychometric tests, body sway and subjective feeling rating scales. Chlormezanone induced objective disturbances of vigilance and concentration characterised by a decrease in the performance of an arithmetic calculation test and an increase in body sway area recorded in comparison with thiocolchicoside and placebo. These impairments were mainly marked on steady state. Most of the volunteers (10 over 12) complained of drowsiness throughout this treatment. Thiocolchicoside was devoided of any objective or subjective sedative side effect.

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Section: Accepted I7 March 1991mentioning

confidence: 95%

Section: Introductionmentioning

confidence: 99%

Effects of acute and repeated doses of two muscle relaxants chlormezanone and thiocolchicoside, on vigilance and psychomotor performance of healthy volunteers

Patat¹,

Klein²,

Surjus³

et al. 1991

Human Psychopharmacology

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“…Several representative and well-known pharmaceutical inhibitors containing alkyl-alkyl sulfones are shown in Scheme 1a. [5][6][7][8][9][10] Conventionally, sulfones are prepared via the oxidation of sulfides with strong oxidants after thiol-involved couplings, 11,12 resulting in low functional group compatibility. Strategies for sulfone construction via the introduction of hypervalent sulfur in the same oxidation state into organic frameworks are of great interest due to the oxidative economy and step economy of such processes.…”

Section: Introductionmentioning

confidence: 99%

Transition-Metal-Free Reductive Cross-Coupling Employing Metabisulfite as a Connector: General Construction of Alkyl–Alkyl Sulfones

2021

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“…Trancopal is an anxiolytic agent with a known sedative action (Gauz 1959) which has been used on a 200 mg three times daily basis for several years. Since the agent has a plasma half-life of 24 hours (McChesney et al 1967) the possibility of giving the drug once daily in a 400 mg dose at night was put forward. The sedative action could then be of benefit in helping the patient to sleep at night and the extended halflife might give a sufficient residual level of the drug on the following day to reduce anxiety.…”

Section: Introductionmentioning

confidence: 99%

A Controlled Study Comparing a Three Times Daily Dose of Chlordiazepoxide with a Single Night-Time Dose of Trancopal in the Control of Anxiety, Using a Double-Blind, Double-Dummy Technique

Donald¹,

Molla²

1978

J Int Med Res

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A double-blind, double-dummy between-patient study in general practice was carried out to compare the effectiveness of a single, night-time dosage of Trancopal and a three times daily dose of chlordiazepoxide in controlling neurotic anxiety. Ninety-three patients received either 400 mg of Trancopal at night and a chlordiazepoxide placebo capsule three times daily or 10 mg of chlordiazepoxide three times daily and one or two Trancopal placebo tablets at night. Each was treated for four weeks. Three assessments were made using a physicians' rating scale (modified Hamilton Scale). A visual analogue scale was completed by patients initially and at weekly intervals and physicians' and patients' global assessments were made at Weeks 2 and 4.Each treatment group improved considerably over the period of the study both for sleep and anxiety ratings. A statistically significant correlation was found between improvement in day-time fatigue and loss of energy and improvement in sleep disturbance only in the Trancopal group. Loss of concentration was analyzed separately in patients over 40 years old and there was a significant improvement in the physicians' rating in the Trancopal group.There was a very close correlation throughout between the physician's and patient's own assessment of improvement. Few side-effects not already reported at the start of the trial were reported on either treatment. It was concluded that Trancopal at a usual dosage of 400 mg at night offers an effective alternative to a divided dose of chlordiazepoxide. Not only is the beneficial effect on symptoms of anxiety similar but there is some suggestion of a greater improvement in sleep and less interference with day-time functioning.

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Metabolism of chlormezanone in man and laboratory animals

Cited by 20 publications

References 7 publications

Effects of acute and repeated doses of two muscle relaxants chlormezanone and thiocolchicoside, on vigilance and psychomotor performance of healthy volunteers

Effects of acute and repeated doses of two muscle relaxants chlormezanone and thiocolchicoside, on vigilance and psychomotor performance of healthy volunteers

Transition-Metal-Free Reductive Cross-Coupling Employing Metabisulfite as a Connector: General Construction of Alkyl–Alkyl Sulfones

A Controlled Study Comparing a Three Times Daily Dose of Chlordiazepoxide with a Single Night-Time Dose of Trancopal in the Control of Anxiety, Using a Double-Blind, Double-Dummy Technique

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