Methaqualone is a potent quinazoline, a class of sedative-hypnotics, that has a high potential for abuse. While the oral use of methaqualone (Quaalude, Mandrax) has waned in western countries since the mid-late 1980's, the practice of smoking methaqualone is a serious public health problem in South Africa, other parts of Africa and India. In the context of diminishing resources devoted to substance abuse treatment in regions affected by methaqualone abuse, it would be desirable to base treatment on the best evidence available. This review aimed to provide health care workers, policy-makers and consumers with the necessary information to make decisions regarding effective treatment of this highly dependence-producing drug.
To compare the effectiveness of any type of pharmacological or behavioural treatment administered in either an in-patient or out-patient setting compared with either a placebo or no treatment or a waiting list, or with another form of treatment administered in either an in- or out-patient setting.
The authors searched the following databases: Cochrane Drugs and Alcohol Group'Register of Trials (February 2004); Cochrane Central Register of Controlled Trials (CENTRAL-The Cochrane Library, Issue 2, 2004); MEDLINE (OVID - January 1966 to february 2004), PsycInfo (OVID - January 1967 to february 2004). Relevant conference proceedings and reference lists of relevant articles were hand-searched. Broad internet searches were conducted and contact made with experts in the field.
All randomised controlled trials and quasi-randomised trials of the effectiveness of treatment programmes (in- or out-patient) for methaqualone dependence and abuse were considered for inclusion in this review.
The authors independently assessed study eligibility and quality.
No studies were found that met the inclusion criteria.
To date, no randomized controlled trials appear to have been conducted. Consequently, the effectiveness of inpatient versus outpatient treatment, psychosocial treatment versus no treatment, and pharmacological treatments versus placebo for methaqualone abuse or dependence has yet to be established.
"These problems led to the implementation of tighter regulation of the drug, and by the mid- 1980s, it had been withdrawn from most markets (Carroll and Gallo, 1985; Gass, 2008). Nevertheless, recreational use of illegally produced methaqualone still constitutes a substantial health problem in some parts of the world (Parry et al., 2004; McCarthy et al., 2005). "
[Show abstract][Hide abstract] ABSTRACT: In the present study we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude®), an infamous sedative-hypnotic and recreational drug from the 1960-70s. Methaqualone was demonstrated to be a positive allosteric modulator (PAM) at human α1,2,3,5β2,3γ2S GABAA receptors (GABAARs) expressed in Xenopus oocytes, whereas it displayed highly diverse functionalities at the α4,6β1,2,3δ GABAAR subtypes, ranging from inactivity (α4β1δ), through negative (α6β1δ) or positive allosteric modulation (α4β2δ, α6β2,3δ), to superagonism (α4β3δ). Methaqualone did not interact with the benzodiazepine, barbiturate or neurosteroid binding sites in the GABAAR. Instead, the compound is proposed to act through the transmembrane β((+))/α((-)) subunit interface of the receptor, possibly targeting a site overlapping with that of the general anesthetic etomidate. The negligible activities displayed by methaqualone at numerous neurotransmitter receptors and transporters in an elaborate screening for additional putative CNS targets suggest that it is a selective GABAAR modulator. The mode of action of methaqualone was further investigated in multichannel recordings from primary frontal cortex networks, where the overall activity changes induced by the compound at 1-100 μM concentrations were very similar to those mediated by other CNS depressants. Finally, the free methaqualone concentrations in mouse brain arising from doses producing significant in vivo effects in assays for locomotion and anticonvulsant activity were found to correlate fairly well with its potencies as a modulator at the recombinant GABAARs. Hence, we propose that the multifaceted functional properties exhibited by methaqualone at GABAARs give rise to its effects as a therapeutic and recreational drug.
The American Society for Pharmacology and Experimental Therapeutics.
[Show abstract][Hide abstract] ABSTRACT: The study was conducted in response to the lack of epidemiological data in recent time on the use of psychoactive substances by adolescents in metropolitan Lagos-a city unique for its socio-economic profile. We considered some methodological issues omitted in several previous studies. A total of 4,286 school pupils (mean age 15.2) were anonymously administered a Self-Report Questionnaire to ascertain a range of key drug use factors in lifetime and 1-year periods. The rate of use of most of the 14 substances investigated was much higher than reported in any other study on comparable population sample. We found that 61.8 and 32.1% of respondents have used one or more substances in their lifetime and in the past 1 year, respectively. High lifetime rates of use were found for common stimulants: coffee, kolanut, and prescription drugs (barbiturates and minor tranquilisers). The rate of use of proscribed addictive substances, cannabis, heroin, and cocaine, ranged between 4.0 and 4.8%. Missing data and non-response rates were few; however, social acquiescence, under and over reporting, could be mitigant to estimation of rates and patterns of use. We advocate properly articulated school-based educative programmes that can facilitate drug demand reduction.
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