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British Medical Journal Mar 1979Review of the various drugs in current clinical use showed that over 50 of them may cause a purely sensory or mixed sensorimotor neuropathy. These include...
Review of the various drugs in current clinical use showed that over 50 of them may cause a purely sensory or mixed sensorimotor neuropathy. These include antimicrobials, such as isoniazid, ethambutol, ethionamide, nitrofurantoin, and metronidazole; antineoplastic agents, particularly vinca alkaloids; cardiovascular drugs, such as perhexiline and hydrallazine; hypnotics and psychotropics, notable methaqualone; antirheumatics, such as gold, indomethacin, and chloroquine; anticonvulsants, particularly phenytoin; and other drugs, including disulfiram, calcium carbimide, and dapsone. Patients receiving drug treatment who complain of paraesthesie, pain, muscle cramps, or other abnormal sensations and those without symptoms who are receiving drugs that are known or suspected to be neurotoxic should undergo neurological examination and studies of motor and sensory nerve conduction. This will allow the incidence of drug-induced peripheral neuropathy to be determined more precisely.
Topics: Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Anticonvulsants; Antineoplastic Agents; Cardiovascular Agents; Humans; Hypnotics and Sedatives; Peripheral Nervous System Diseases; Psychotropic Drugs
PubMed: 219931
DOI: 10.1136/bmj.1.6164.663 -
Acta Crystallographica. Section E,... Mar 2012In the title methaqua-lone analogue, C(23)H(20)N(2)O(2), the planes of the terminal aromatic rings [dihedral angle between them = 64.52 (7)°] approximately face the...
In the title methaqua-lone analogue, C(23)H(20)N(2)O(2), the planes of the terminal aromatic rings [dihedral angle between them = 64.52 (7)°] approximately face the fused-ring methyl group and both are twisted with respect to the pyrimidine plane (r.m.s. deviation = 0.028 Å), forming dihedral angles of 86.9 (3) (with the 2-tolyl ring) and 65.57 (7)°. The 2-tolyl residue is disordered over two almost coplanar but opposite orientations with the major component having a site-occupancy factor of 0.893 (3). The three-dimensional crystal packing is consolidated by C-H⋯O, C-H⋯π and π-π [2-tol-yl-2-tolyl centroid-centroid distance = 3.8099 (6) Å] inter-actions.
PubMed: 22412719
DOI: 10.1107/S1600536812007362 -
Nature Communications Jun 2024Methaqualone, a quinazolinone marketed commercially as Quaalude, is a central nervous system depressant that was used clinically as a sedative-hypnotic, then became a...
Methaqualone, a quinazolinone marketed commercially as Quaalude, is a central nervous system depressant that was used clinically as a sedative-hypnotic, then became a notorious recreational drug in the 1960s-80s. Due to its high abuse potential, medical use of methaqualone was eventually prohibited, yet it persists as a globally abused substance. Methaqualone principally targets GABA receptors, which are the major inhibitory neurotransmitter-gated ion channels in the brain. The restricted status and limited accessibility of methaqualone have contributed to its pharmacology being understudied. Here, we use cryo-EM to localize the GABA receptor binding sites of methaqualone and its more potent derivative, PPTQ, to the same intersubunit transmembrane sites targeted by the general anesthetics propofol and etomidate. Both methaqualone and PPTQ insert more deeply into subunit interfaces than the previously-characterized modulators. Binding of quinazolinones to this site results in widening of the extracellular half of the ion-conducting pore, following a trend among positive allosteric modulators in destabilizing the hydrophobic activation gate in the pore as a mechanism for receptor potentiation. These insights shed light on the underexplored pharmacology of quinazolinones and further elucidate the molecular mechanisms of allosteric GABA receptor modulation through transmembrane binding sites.
Topics: Receptors, GABA-A; Binding Sites; Cryoelectron Microscopy; Humans; Animals; Etomidate; Propofol; Quinazolinones; Allosteric Regulation; HEK293 Cells; Hypnotics and Sedatives
PubMed: 38898000
DOI: 10.1038/s41467-024-49471-y -
Evidence-based Complementary and... 2020is a medicinal herb of Leguminosae family. It is distributed in the tropical and humid regions. The plant is traditionally used in the treatment of typhoid, diabetes,... (Review)
Review
is a medicinal herb of Leguminosae family. It is distributed in the tropical and humid regions. The plant is traditionally used in the treatment of typhoid, diabetes, malaria, asthma, ringworms, tinea infections, scabies, blotch, herpes, and eczema. The review is aimed at unveiling the ethnobotanical description and pharmacological activities of Different parts of the plant are reported in folk medicine as therapeutic substances for remediation of diverse diseases and infections. The extracts and isolated compounds displayed pronounced pharmacological activities. Display of antibacterial, antioxidant, antifungal, dermatophytic, anticancer, hepatoprotective, antilipogenic, anticonvulsant, antidiabetic, antihyperlipidemic, antimalarial, anthelmintic, and antiviral activities could be due to the array of secondary metabolites such as tannins, alkaloids, flavonoids, terpenes, anthraquinone, saponins, phenolics, cannabinoid alkaloids, 1,8-cineole, caryophyllene, limonene, -selinene, -caryophyllene, germacrene D, cinnamic acid, pyrazol-5-ol, methaqualone, isoquinoline, quinones, reducing sugars, steroids, and volatile oils present in different parts of the plant. The review divulges the ethnobotanical and pharmacological activities of the plant and also justifies the ethnomedical claims. The significant medicinal value of this plant necessitates a scientific adventure into the bioactive metabolites which constitute various extracts.
PubMed: 32148534
DOI: 10.1155/2020/2580259 -
British Medical Journal Jun 1973
Topics: Amitriptyline; Dibenzazepines; Diphenhydramine; Electroconvulsive Therapy; Humans; Methaqualone; Sleep; Substance Withdrawal Syndrome; Substance-Related Disorders
PubMed: 4733259
DOI: 10.1136/bmj.2.5868.716-b -
British Medical Journal Jan 1969
Topics: Humans; Methaqualone; Sleep Initiation and Maintenance Disorders; Substance-Related Disorders
PubMed: 5761820
DOI: 10.1136/bmj.1.5636.122-d -
South African Medical Journal =... Dec 2020There is a high prevalence of substance use among youth in South Africa (SA), and adolescent girls and young women (AGYW) experience high rates of depression and... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
There is a high prevalence of substance use among youth in South Africa (SA), and adolescent girls and young women (AGYW) experience high rates of depression and anxiety. Substance use behaviours and mental health are associated with other public health problems among AGYW such as HIV and unintended pregnancy. Therefore, understanding the relationship between substance use and mental health is imperative to improve AGYW's health.
OBJECTIVES
To examine the association between heavy drinking, marijuana, methamphetamine and methaqualone (Mandrax) use and depressive and anxiety symptoms among AGYW aged 16 - 19 years who have dropped out of school in Cape Town, SA.
METHODS
Data for this report come from the baseline data of 500 participants of an ongoing cluster-randomised trial assessing the efficacy of a young woman-focused intervention to reduce substance use and HIV risk. After AGYW consented/assented to participate, they completed a urine drug screen and a baseline questionnaire.
RESULTS
Logistic and negative binomial regressions, controlling for clustering at the neighbourhood level, revealed that frequency of depressive symptoms was significantly and positively related to a positive drug screen for Mandrax (β=0.07; p=0.03). All other associations between the frequency of depressive symptoms and substance use were not statistically significant (ps>0.05). The associations between frequency of anxiety symptoms and substance use were not statistically significant (ps>0.05).
CONCLUSIONS
Our findings highlight the need to address substance use, especially Mandrax use and its associated risk, and depression in an integrated, youth-friendly setting.
Topics: Adolescent; Alcohol Drinking; Anxiety; Depression; Female; HIV Infections; Humans; Mental Health; Prevalence; South Africa; Substance Abuse Detection; Substance-Related Disorders; Surveys and Questionnaires; Young Adult
PubMed: 33404004
DOI: 10.7196/SAMJ.2020.v111i1.14520 -
Forensic Toxicology Jul 2023
Topics: Humans; Methaqualone; Substance-Related Disorders
PubMed: 37169943
DOI: 10.1007/s11419-023-00665-x -
Forensic Toxicology Jan 2023The information on analytical methods for 4-quinazolinone recreational drugs, such as methaqualone, etaqualone and 2-methoxyqualone, is almost scant. In this study,...
The next addiction-causing drug class 4-quinazolinone derivatives: analyses of methaqualone analogs including recently discovered 2-methoxyqualone by different modes of mass spectrometry.
PURPOSE
The information on analytical methods for 4-quinazolinone recreational drugs, such as methaqualone, etaqualone and 2-methoxyqualone, is almost scant. In this study, product ion spectra of gas chromatography-tandem mass spectrometry (GC-MS/MS) with different collision energies were presented for these drugs. Because 2-methoxyqualone is a new recreational drug discovered in dubious tablets very recently, much more detailed data obtained by different types of mass spectrometry instruments, and quantification data of 2-methoxyqualone in the tablet together with its validation were demonstrated.
METHODS
The methods for analyses were GC-MS/MS, high-resolution ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry and liquid chromatography-tandem mass spectrometry.
RESULTS
The GC-MS/MS product ion spectra of the three compounds with different collision energies have not been reported before. They were very useful to tentatively identify unknown compounds. If a reference standard is available, the final identification and quantification can be achieved by measurements of product ion spectra and in selected reaction monitoring mode very easily by GC-MS/MS. The final identification and quantification for the new 2-methoxyqualone were performed in this way. The content of the compound was 69.8 ± 0.5% (w/w) in the tablet. Acetaminophen and caffeine coexisted in the tablet with approximate concentrations at 10 and 5%, respectively.
CONCLUSIONS
In this article, we have presented product ion spectra of methaqualone, etaqualone and 2-methoxyqualone at different collision energies by GC-MS/MS for the first time. In addition, this is the first paper to describe the details of quantification of 2-methoxyqualone in the authentic seized product.
Topics: Tandem Mass Spectrometry; Gas Chromatography-Mass Spectrometry; Methaqualone; Tablets
PubMed: 36652055
DOI: 10.1007/s11419-022-00631-z -
British Medical Journal Aug 1970
Topics: Barbiturates; Chloral Hydrate; Diphenhydramine; Glutethimide; Humans; Hypnotics and Sedatives; Methaqualone; Motor Skills; Sleep; Sleep, REM
PubMed: 4318019
DOI: No ID Found