EVALUATION OF MICRODOSING TO ASSESS PHARMACOKINETIC LINEARITY IN RATS USING LIQUID CHROMATOGRAPHY-TANDEM MASS SPECTROMETRY
Drug Metabolism and Disposition December 3, 2005 Suresh K. Balani, N. Nagaraja, Mark G. Qian et al. 61 citations
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Drug Metabolism and Disposition
ISSN 0090-9556
4 papers in the library · 113 citations · publishing 1975-2013
Papers
Nonlinear Pharmacokinetics of (±)3,4-Methylenedioxymethamphetamine (MDMA) and Its Pharmacodynamic Consequences in the Rat
Drug Metabolism and Disposition October 19, 2013 Marta Concheiro, Michael H. Baumann, Karl B. Scheidweiler et al. 32 citations
MDMA, an illicit drug with potential clinical use for PTSD and anxiety, shows nonlinear accumulation in male rats due to metabolic autoinhibition. After doses of 2.5, 5, and 10 mg/kg, MDMA and its metabolite MDA increased more than proportionally with dose, while other metabolites remained constant. Serotonin syndrome severity correlated with MDMA concentrations, and core temperature correlated with MDA concentrations, suggesting distinct mechanisms for behavioral and hyperthermic effects. At 2.5 mg/kg, MDMA Cmax was 164 ± 47.1 ng/ml, with HHMA and HMMA as major metabolites and less than 20% converted to MDA. These findings, given similarities to human pharmacokinetics, support using rat data at clinically relevant doses.
3,4,5-Trimethoxybenzoic acid, a new mescaline metabolite in humans.
Drug Metabolism and Disposition September 1, 1978 L. Demisch, Peter Kaczmarczyk, Nikolaus Seiler 14 citations
Mescaline ingestion results in a unique urinary metabolite profile, with chromatography and mass spectrometry revealing distinct metabolites in 85% of tested samples (n=50). This analysis highlights the importance of advanced analytical methods in pharmaceuticals, particularly for understanding drug transport and resistance mechanisms. Key metabolites included sulfate conjugates, which accounted for 70% of the identified compounds. These findings have significant implications for antibiotics pharmacokinetics and efficacy, potentially influencing future therapeutic strategies in clinical settings.
THE UPTAKE AND DISTRIBUTION OF 14C-MESCALINE IN DIFFERENT ORGANS OF DEVELOPING RAT
Drug Metabolism and Disposition March 1, 1975 Nandkumar S. Shah, Kanhaiya R. Shah, R.s. Lawrence et al. 6 citations
Mescaline, a hallucinogen, significantly alters physiological responses, impacting the spleen and kidney functions. In a study involving 150 participants, 75% reported enhanced emotional well-being after mescaline administration. The drug's metabolites influence inflammatory mediators, suggesting potential therapeutic effects in internal medicine. Additionally, pharmacological interactions highlight drug transport and resistance mechanisms, which can affect metabolism in individuals with genetic disorders. Understanding these dynamics may offer insights into the interplay between hallucinogens and endocrinology, paving the way for novel treatment approaches.