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Psychotropic Use during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Methaqualone (Quaalude, Sopor, Parest) is an effective hypnotic and sedative agent and is not presently commercially available. No clear medicinal advantage of methaqualone over the other available hypnotics can be shown and the drug is commonly abused by drug-dependent people. Tolerance to the drug develops in abusers. No published reports are available that analyze the possible association of the use of methaqualone during pregnancy with congenital malformations. However, its use during gestation is not recommended because of its abuse potential. The frequency of congenital anomalies was not increased among rats or rabbits whose mothers were administered 200 mg/kg methaqualone orally (rabbits) from days 1 to 29 or 100 mg/kg (rats) from days 1 to 20 (Bough et al., 1963).
Alcohol and Sedatives
Published in Frank Lynn Iber, Alcohol and Drug Abuse as Encountered in Office Practice, 2020
No longer available as a prescription drug due to its demonstrated cardiovascular and respiratory depression effects, methaqualone is favored as a street drug because of its very rapid absorption from the GI tract and its very prompt high.
Saliva Drug Analysis
Published in Steven H. Y. Wong, Iraving Sunshine, Handbook of Analytical Therapeutic Drug Monitoring and Toxicology, 2017
Edward J. Cone, Amanda J. Jenkins
Other nonbarbiturate-sedative hypnotics have been detected in saliva. Sharp et al43 detected methaqualone in saliva samples of healthy subjects after a single oral dose of 250 mg. The mean experimental S/P (total) ratio ± SD was 0.11 ± 0.02. Peat et al.44 reported detection of methaqualone and its major hydroxy metabolite in saliva after oral administration. Initially, the metabolite was present in much lower concentrations (0 to 4 hr), but matched or exceeded concentrations of the parent compound at later times (4 to 24 hr). Saliva concentrations of methaqualone and metabolite were approximately 10% of those observed in plasma. Another sedative, meprobamate, was reported to be present in saliva in nearly equal concentrations as found plasma after oral administration.45 Chloral hydrate and metabolites have been detected in horse saliva after chloral hydrate doping.46 In this study, the concentration of chloral hydrate and the metabolite, trichloroethanol, in saliva were approximately equal to plasma concentrations, whereas saliva trichloroacetic acid concentrations were much lower.
Return of the Quaaludes? Prolonged agitated delirium after intentional ingestion of the methaqualone analog SL-164 – a case report
Published in Substance Abuse, 2021
Katrin Romanek, Helena Fels, Torsten Dame, Gisela Skopp, Frank Musshoff, Hans Eiglmeier, Florian Eyer
Methaqualone (2-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone) is a sedative-hypnotic, anxiolytic and muscle relaxant drug of the quinazolinone class. It acts as a GABAA receptor modulator similar to benzodiazepines and barbiturates, but with strong affinity to a different GABAA receptor subtype (α4β3δ) compared to the other mentioned sedatives.1 It was widely distributed under the brand names “Quaalude” in the USA and “Mandrax” in the UK and South Africa from the 1960s to the early 80 s. In the 1970s, ‘Quaaludes’ were one of the most frequently prescribed sedatives in the United States, originally marketed as a safe and non-habit-forming sedative-hypnotic alternative to barbiturates. This soon turned out to be incorrect as methaqualone became increasingly popular as a recreational drug due to its calming but also euphoric effects.2 The widespread abuse of methaqualone and its misuse as a date rape drug finally led to a halt in commercial production in almost all countries.
Synthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Mostafa M. Ghorab, Maged S. Abdel-Kader, Ali S. Alqahtani, Aiten M. Soliman
Quinazolines are fused heterocyclic ring systems known for their variable biological activity12–15. They are well known for their inhibitory activity towards various protein kinase enzymes and their anticancer activity16. For example, lapatinib, a dual reversible EGFR and HER2 inhibitor. Also, gefitinib and erlotinib are reversible EGFR inhibitors; they are examples of FDA approved small molecules TK inhibitors17. Methaqualone, a potent hypnotic, was considered as an important landmark in synthetic anticonvulsants18. The 3-[β-keto-gamma-(3-hydroxy-2-piperidyl)-propyl]-4-quinazolone (A) was the first isolated natural quinazolinone alkaloid known by its antimalarial activity19. The quinazolinone derivatives (B) and benzo[g]quinazolinone (C) were reported to possess potent EGFR and HER2 inhibitory activity20,21 (Figure 1). On the other hand, the Ephedra alkaloid, Norephedrine (NE) is a stereoisomer of phenylpropanolamine that is naturally occurring sympathomimetic22. Investigation revealed that long-term use of NE caused severe side effects, including fatality23. In addition to medicinal use, the properties of this alkaloid have attracted considerable attention in natural product chemistry field that leads to its use as a starting material in the preparation of chiral ligands for asymmetric catalytic synthesis24,25.
Adolescent female school dropouts who use drugs and engage in risky sex: effects of a brief pilot intervention in Cape Town, South Africa
Published in AIDS Care, 2019
Tara Carney, Felicia A. Browne, Bronwyn Myers, Tracy L. Kline, Brittni Howard, Wendee M. Wechsberg
Despite the FGD findings indicating acceptability of the intervention, few statistically significant differences were observed by study arm at 1-month follow-up. However, certain within-group changes were observed among participants assigned to the intervention group; specifically, reductions in cannabis use, impaired sex with any partner and impaired sex with a main partner, compared with participants in the control group which only reduced cannabis use. The reduction in cannabis use within both groups could indicate that the questionnaire or biological testing served as an intervention in itself. Receiving their drug test results may have motivated some participants to stop using drugs (Browne, Carney, Myers, & Wechsberg, 2016). The increase in methaqualone use among participants in the intervention arm was surprising and warrants further study, especially because methaqualone is commonly used with cannabis.