Methaqualone: Metabolie, kinetie, and dinical pharmaeologie observations

Brown, S. S.; Goenechea, S.

doi:10.1002/cpt1973143314

Cited by 44 publications

(17 citation statements)

References 13 publications

(14 reference statements)

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“…The inhibition of the conversion of the pharmacologically active methaqualone to an inactive metabolite (14,15) could explain an enhanced effect when such a combination is ingested.…”

Section: Resultsmentioning

confidence: 99%

Anin VitroDrug Interaction Study: Chlorpheniramine-Methaqualone

Hindmarsh

Wallace

LeGatt

et al. 1979

Canadian Society of Forensic Science Journal

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The antihistamine, chlorpheniramine inhibited the in vitro metabolism of methaqualone by the 10,000 x g supernatant fraction of rat liver homogenate. The formation of the major metabolite, 2-methyl-3-(2-hydroxymethylphenyl)-4(3H)-quinazolinone was monitored by GLC. Metabolite concentrations after incubation in the presence of chlorpheniramine were significantly lower than control incubations. RESUME Apres centrifugation a 10,000 9 d'un homoglmat de foie de rat, I'antihistaminique chlorpheniramine a inhibe le metabolisme in vitro du methaqualone surnageant. La formation du metabolite principal, 2 methyl-3-(2-hydroxymethylphenyl)-4(3H)-quinazolinone, a ete contrOlee par chromatographie en phase gazeuse et Iiquide. Les concentrations de metabolite, apres incubation en presence de chlorpheniramine, ont ete sensiblement plus faibles que les incubations contrOlees.

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“…The inhibition of the conversion of the pharmacologically active methaqualone to an inactive metabolite (14,15) could explain an enhanced effect when such a combination is ingested.…”

Section: Resultsmentioning

confidence: 99%

Anin VitroDrug Interaction Study: Chlorpheniramine-Methaqualone

Hindmarsh

Wallace

LeGatt

et al. 1979

Canadian Society of Forensic Science Journal

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“…12 Actually, MMQ is the methylated analogue, but not a metabolite, 13 of methaqualone, which is a quinazoline compound related functionally and structurally to glutethimide and the barbiturates. 14 The numerous cases of abuse of methaqualone reported soon after its introduction to the market, indicated a marked addictive potential of this substance which was also causing a severe withdrawal syndrome similar to delirium tremens characteristic of the sedative-hypnotic type of dependence. 15 Methaqualone was therefore withdrawn from the market in many Methaqualone overdose usually causes ataxia, lethargy, and CNS depression, although limb hyperreflexia, myoclonia, seizures, coma and other non-neurological symptoms such as respiratory and cardiac failure have been described after severe poisoning.…”

Section: Discussionmentioning

confidence: 99%

“…15 Methaqualone was therefore withdrawn from the market in many Methaqualone overdose usually causes ataxia, lethargy, and CNS depression, although limb hyperreflexia, myoclonia, seizures, coma and other non-neurological symptoms such as respiratory and cardiac failure have been described after severe poisoning. 14,16 Psychomotor agitation was observed in a life-threatening intoxication, 17 and, at lower doses, recreational users have reported a euphoriant effect.…”

Section: Discussionmentioning

confidence: 99%

Acute neurotoxicity associated with recreational use of methylmethaqualone confirmed by liquid chromatography tandem mass spectrometry

Ceschi

Giardelli

Müller

et al. 2013

Clinical Toxicology

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Methylmethaqualone is a sedative designer drug created by adding a methyl group to the 3-phenyl ring of methaqualone, and is at present not subject to restrictive regulation in many countries. To our knowledge, no case of methylmethaqualone abuse has been published to date in the scientific literature, and the only sources of information are users' reports on Web discussion forums and data from preclinical animal studies. We report a case of oral methylmethaqualone abuse confirmed by liquid chromatography tandem mass spectrometry in a 24-year-old previously healthy Caucasian male. Observed symptoms and signs such as central nervous system depression alternating with excitation, psychomotor agitation, muscle hyperactivity, and tachycardia were compatible with methaqualone-induced adverse effects. Except for the mild tachycardia (115 beats/min), other vital signs were normal: blood pressure 134/89 mmHg, body temperature 36.2°C (97.16°F), and peripheral oxygen saturation 99% while breathing room air. The ECG showed no prolongation of the QT interval and the QRS duration was normal. Laboratory analysis revealed a slight increase in creatine kinase (368 U/L) and alanine aminotransferase (90 U/L) serum concentrations. Blood alcohol concentration was 0.32 g/L. Methylmethaqualone was identified in a serum sample collected on admission which was analyzed by a liquid chromatography tandem mass spectrometry toxicological screening method using turbulent flow online extraction. After a few days the patient ingested the same amount of substance with identical symptoms. Based on the chemical structure and animal data, and according to this case report and users' Web reports, methylmethaqualone appears to have a similar acute toxicity profile to methaqualone, with marked psychomotor stimulation. Symptoms of acute toxicity can be expected to resolve with supportive care. The paper is written in US EnglishRunning head: Acute neurotoxicity after methylmethaqualone abuse. Keywords:drug of abuse, designer drug, methaqualone, acute toxicity. Number of references: 20 Figures: 2 AbstractMethylmethaqualone is a sedative designer drug created by adding a methyl group to the 3-phenyl ring of methaqualone, and is at present not subject to restrictive regulation in many countries. To our knowledge, no case of methylmethaqualone abuse has been published to date in the scientific literature, and the only sources of information are users' reports on Web discussion forums and data from preclinical animal studies. We report a case of oral methylmethaqualone abuse confirmed by liquid chromatography tandem mass spectrometry in a 24-year-old previously healthy Caucasian male. Observed symptoms and signs such as central nervous system depression alternating with excitation, psychomotor agitation, muscle hyperactivity, and tachycardia were compatible with methaqualone-induced adverse effects. Except for the mild tachycardia (115 beats/min), other vital signs were normal: blood pressure 134/89 mmHg, body temperature 36.2°C (97.16°F), perip...

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“…The drug also produces a state of tolerance to other drugs as well as to its own response (Prabhu et all967;Ballinger et a1 1972;Brown & Goenechea 1973) and a combination (250:25 mg) with diphenhydramine (Mandrax) has been shown to be a better sedative than either of its constituents or a placebo alone (Norris & Telfer 1969;Brown & Goenechea 1973).…”

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confidence: 97%