International Journal of Molecular Sciences
December 4, 2020
Sara Malaca, Alfredo Fabrizio Lo Faro, Alice Tamborra et al.
48 citations
Tryptamines are 5-HT2A receptor agonists that alter perceptions of reality. Their prevalence in drug overdoses is low but increasing, yet they are not part of typical toxicology testing, so their contribution may be underestimated. From 2015 to 2020, 22 new analytical methods, primarily liquid chromatography tandem mass spectrometry, were developed to identify tryptamines and metabolites in biological samples. The most prevalent tryptamines are 5-MeO-DiPT, 5-MeO-DALT, and DMT. Morbidity from tryptamine intake is considerable, and clinicians and laboratorians need updated data on this public health threat.
Journal of pharmaceutical and biomedical analysis
February 5, 2020
Alfredo Fabrizio Lo Faro, Annagiulia Di Trana, Nunzia La Maida et al.
45 citations
New psychoactive substances of natural origin, mainly alkaloids from Asian and South American plants, typically have stimulant or hallucinogenic effects, with a few having sedative properties. Information on analytical identification of these substances in plant material is scarce, and there is little data on their characterization and quantification in biological matrices from intoxication or fatality cases. Their metabolism is not fully investigated, making identification infrequent and metabolites often unknown.
Frontiers in Pharmacology
February 17, 2023
Lourdes Poyatos, Clara Pérez‐mañá, Olga Hladun et al.
26 citations
Methylone, a common synthetic cathinone used as a substitute for MDMA, produces similar acute effects in humans. In a controlled trial with 17 experienced psychostimulant users, a single 200 mg oral dose of methylone increased blood pressure and heart rate and induced pleasurable effects including stimulation, euphoria, wellbeing, enhanced empathy, and altered perception. Methylone's effect profile resembled MDMA's but with a faster onset and earlier disappearance of subjective effects. The findings suggest methylone's abuse potential is comparable to that of MDMA in humans.
International Journal of Molecular Sciences
November 23, 2022
Lourdes Poyatos, Alfredo Fabrizio Lo Faro, Diletta Berardinelli et al.
22 citations
After controlled oral doses of 50–200 mg methylone given to 12 male volunteers, plasma concentrations increased in proportion to dose. Maximum concentrations ranged from 153 ng/mL at the lowest dose to 604 ng/mL at the highest dose. The drug was absorbed rapidly, reaching peak levels in 1.5–2 hours, and had a half-life of about 6 hours. Its metabolite HMMC reached peak concentrations 10–14 times lower than methylone. Unlike MDMA, methylone showed linear pharmacokinetics across the dose range. A validated LC-MS/MS method was used to measure methylone, MDMA, and their metabolites in plasma.
Journal of pharmaceutical and biomedical analysis
January 20, 2024
Alfredo Fabrizio Lo Faro, Giorgia Sprega, Diletta Beradinelli et al.
14 citations
Enantioselective high-performance liquid chromatography-tandem mass spectrometry methods were developed to quantify MDMA and its phase-1 metabolites HMA, HMMA, and MDA in human plasma, sweat, oral fluid, and urine. Two polysaccharide-based chiral columns achieved baseline separation of most enantiomer pairs: the Lux AMP column separated MDMA, HMA, and HMMA enantiomers but not MDA; the Lux i-Amylose-3 column separated MDMA, HMMA, and MDA enantiomers but not HMA. Analysis took under 4 minutes with one column and under 6 minutes with the other. Both methods were validated and applied to biological fluids, confirming enantioselective metabolism of MDMA.
Metabolites
July 29, 2022
Sara Malaca, Marilyn A. Huestis, Leonardo Lattanzio et al.
8 citations
Synthetic tryptamines like 4-AcO-DiPT are increasingly involved in intoxications and fatalities yet remain unregulated in many countries, with little known about how the body processes them. Using human liver cells and high-resolution mass spectrometry, researchers identified six metabolites formed after three hours of incubation. The main transformation was ester hydrolysis to 4-OH-DiPT, followed by glucuronidation, sulfation, N-oxidation, and N-dealkylation. The most abundant second-generation metabolites were 4-OH-iPT-sulfate and 4-OH-DiPT-glucuronide. The authors suggest that 4-OH-DiPT, 4-OH-iPT, and 4-OH-DiPT-N-oxide are the best biomarkers to detect 4-AcO-DiPT consumption.
Journal of pharmaceutical and biomedical analysis
June 15, 2024
Giorgia Sprega, Giorgi Kobidze, Alfredo Fabrizio Lo Faro et al.
4 citations
An improved chiral LC-MS/MS method separates all four pairs of enantiomers of MDMA and its major phase-1 metabolites (HMA, HMMA, MDA) on a single Lux AMP column within six minutes, using an optimized mobile phase and column dimensions. The method was applied to human plasma, oral fluid, and urine. In urine, hydrolysis of glucuronides with hydrochloric acid or glucuronidase was tested to evaluate effects on the concentration and enantiomeric distribution of the hydroxy metabolites HMA and HMMA.