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1.
Acta Neuropsychiatr ; 31(4): 213-219, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31106729

RESUMO

OBJECTIVE: Psilocybin is a serotonin receptor agonist with a therapeutic potential for treatment-resistant depression and other psychiatric illnesses. We investigated whether the administration of psilocybin had an antidepressant-like effect in a rat model of depression. METHODS: Using the Flinders Sensitive Line (FSL) rat model of depression, we assessed the antidepressant-like effect of psilocin and psilocybin, measured as a reduction in immobility time in the forced swim test (FST). We measured locomotor activity in an open field test (OFT) to control for stimulant properties of the drugs. We performed a set of experiments to test different doses, treatment paradigms, and timing of the tests in relation to the drug administration. RESULTS: Psilocin and psilocybin showed no effect on immobility, struggling, or swimming behaviour in the FST and no effect on locomotor activity in the OFT. FSL rats did show significantly more immobility than their control strain, the Flinders Resistant Line, as expected. CONCLUSION: Psilocin and psilocybin showed no antidepressant-like effect in the FSL rats, despite a positive effect in humans. This suggests that other animal models of depression and other behavioural tests may be more appropriate for translational studies in the effects of psilocybin.


Assuntos
Antidepressivos/administração & dosagem , Comportamento Animal/efeitos dos fármacos , Depressão/tratamento farmacológico , Modelos Animais de Doenças , Psilocibina/administração & dosagem , Animais , Masculino , Atividade Motora/efeitos dos fármacos , Psilocibina/análogos & derivados , Ratos
2.
Sci Justice ; 59(1): 102-108, 2019 01.
Artigo em Inglês | MEDLINE | ID: mdl-30654963

RESUMO

In nature, there are >200 species of fungi with hallucinogenic properties. These fungi are classified as Psilocybe, Gymnopilus, and Panaeolus which contain active principles with hallucinogenic properties such as ibotenic acid, psilocybin, psilocin, or baeocystin. In Chile, fungi seizures are mainly of mature specimens or spores. However, clandestine laboratories have been found that process fungus samples at the mycelium stage. In this transient stage of growth (mycelium), traditional taxonomic identification is not feasible, making it necessary to develop a new method of study. Currently, DNA analysis is the only reliable method that can be used as an identification tool for the purposes of supporting evidence, due to the high variability of DNA between species. One way to identify the species of a distinctive DNA fragment is to study PCR products analyzed by real time PCR and sequencing. One of the most popular sequencing methods of forensic interest at the generic and intra-generic levels in plants is internal transcribed spacer (ITS). With real time PCR it is possible to distinguish PCR products by differential analysis of their melting temperature (Tm) curves. This paper describes morphological, chemical, and genetic analysis of mycelia of psychedelic fungi collected from a clandestine laboratory. The fungus species were identified using scanning electron microscopy (SEM), mass spectrometry, HRM analysis, and ITS sequencing. The sporological studies showed a generally smooth surface and oval shape, with maximum length 10.1 µm and width 6.4 µm. The alkaloid Psilocyn was identified by mass spectrometry, while HRM analysis and ITS sequencing identified the species as Psilocybe cubensis. A genetic match was confirmed between the HRM curves obtained from the mycelia (evidence) and biological tissue extracted from the fruiting bodies. Mycelia recovered from the evidence and fruiting bodies (control) were genetically indistinguishable.


Assuntos
Alucinógenos/análise , Micélio/genética , Psilocybe/classificação , Psilocibina/análogos & derivados , Chile , DNA Fúngico/análise , Tráfico de Drogas , Genética Forense , Cromatografia Gasosa-Espectrometria de Massas , Microscopia Eletrônica de Varredura , Psilocibina/análise , Reação em Cadeia da Polimerase em Tempo Real , Análise de Sequência de DNA , Análise de Sequência de RNA , Esporos/genética
3.
J Forensic Sci ; 64(4): 1266-1270, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30548541

RESUMO

Fatalities implicating psychedelic mushrooms are not a common clinical situation in everyday forensic medicine. Despite classification as an illegal drug in many countries, psilocybin mushrooms have the reputation of being safe. We report the case of a young man who jumped from a second story balcony under the influence of psilocybin mushrooms. The psilocin assay was performed by gas chromatography coupled to an electron-impact ionization time-of-flight detector (GC-EI-TOF) after solid-phase extraction. Total psilocin was quantified in peripheral and cardiac blood as 60 and 67 ng/mL, respectively, and in urine (2230 ng/mL), bile (3102 ng/mL), and vitreous humor (57 ng/mL). This case report and review of literature highlights the danger of psilocybin mushrooms. Isolated use of psilocybin mushrooms by a regular consumer without psychiatric history, even under "safe" circumstances, can lead to a fatal outcome.


Assuntos
Agaricales , Alucinógenos/efeitos adversos , Psilocibina/efeitos adversos , Transtornos Relacionados ao Uso de Substâncias/psicologia , Suicídio , Adolescente , Bile/química , Cromatografia Gasosa , Humanos , Masculino , Psilocibina/análogos & derivados , Psilocibina/análise , Transtornos Relacionados ao Uso de Substâncias/complicações , Corpo Vítreo/química
4.
Behav Pharmacol ; 29(6): 530-536, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29537989

RESUMO

Short-term moderate doses of serotonergic and dissociative hallucinogens can be useful in the treatment of anxiety. Recently, a trend has developed for long-term intermittent 'microdosing' (usually one-tenth of a 'full' active dose), with reports of long-lasting relief from anxiety and related disorders; however, there is no scientific evidence for the efficacy of therapeutic microdosing nor to show its lasting effects. The objective of this study was to test for lasting effects on anxiety in rats after microdosing with ketamine or psilocin. Over 6 days, Wistar rats (N=40) were administered ketamine (0.5 or 3 mg/kg), psilocin (0.05 or 0.075 mg/kg), or saline on three occasions. A 5-min elevated plus-maze test was conducted 48 h after the final drug treatment (n=8). Dependent variables were entries (frequency), spent time (%), and distance traveled (cm) in each zone, as well as total frequency of rears, stretch-attend postures, and head dips. Statistical analyses of drug effects used separate independent one-way analysis of variance and pair-wise comparisons using independent t-tests. Statistical effects were modest or borderline and were most consistent with a mildly anxiogenic profile, which was significant at lower doses; however, this conclusion remains tentative. The lower doses of ketamine and psilocin produced comparable effects (to one another) across each variable, as did the higher doses. This pattern of effects may suggest a common (e.g. neurotransmitter/receptor) mechanism. We conclude that microdosing with hallucinogens for therapeutic purposes might be counter-productive; however, more research is needed to confirm our findings and to establish their translational relevance to clinical 'psychedelic' therapy.


Assuntos
Antagonistas de Aminoácidos Excitatórios/farmacologia , Alucinógenos/farmacologia , Ketamina/farmacologia , Aprendizagem em Labirinto/efeitos dos fármacos , Psilocibina/análogos & derivados , Animais , Relação Dose-Resposta a Droga , Locomoção/efeitos dos fármacos , Masculino , Psilocibina/farmacologia , Ratos , Ratos Wistar , Fatores de Tempo
5.
Clin Pharmacokinet ; 56(12): 1543-1554, 2017 12.
Artigo em Inglês | MEDLINE | ID: mdl-28353056

RESUMO

INTRODUCTION: Psilocybin is a psychedelic tryptamine that has shown promise in recent clinical trials for the treatment of depression and substance use disorders. This open-label study of the pharmacokinetics of psilocybin was performed to describe the pharmacokinetics and safety profile of psilocybin in sequential, escalating oral doses of 0.3, 0.45, and 0.6 mg/kg in 12 healthy adults. METHODS: Eligible healthy adults received 6-8 h of preparatory counseling in anticipation of the first dose of psilocybin. The escalating oral psilocybin doses were administered at approximately monthly intervals in a controlled setting and subjects were monitored for 24 h. Blood and urine samples were collected over 24 h and assayed by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay for psilocybin and psilocin, the active metabolite. The pharmacokinetics of psilocin were determined using both compartmental (NONMEM) and noncompartmental (WinNonlin) methods. RESULTS: No psilocybin was found in plasma or urine, and renal clearance of intact psilocin accounted for less than 2% of the total clearance. The pharmacokinetics of psilocin were linear within the twofold range of doses, and the elimination half-life of psilocin was 3 h (standard deviation 1.1). An extended elimination phase in some subjects suggests hydrolysis of the psilocin glucuronide metabolite. Variation in psilocin clearance was not predicted by body weight, and no serious adverse events occurred in the subjects studied. CONCLUSIONS: The small amount of psilocin renally excreted suggests that no dose reduction is needed for subjects with mild-moderate renal impairment. Simulation of fixed doses using the pharmacokinetic parameters suggest that an oral dose of 25 mg should approximate the drug exposure of a 0.3 mg/kg oral dose of psilocybin. Although doses of 0.6 mg/kg are in excess of likely therapeutic doses, no serious physical or psychological events occurred during or within 30 days of any dose. CLINICAL TRIALS IDENTIFIER: NCT02163707.


Assuntos
Glucuronídeos/farmacocinética , Alucinógenos/farmacocinética , Psilocibina/análogos & derivados , Psilocibina/farmacocinética , Adulto , Cromatografia Líquida/métodos , Relação Dose-Resposta a Droga , Feminino , Meia-Vida , Alucinógenos/administração & dosagem , Alucinógenos/efeitos adversos , Humanos , Masculino , Pessoa de Meia-Idade , Dinâmica não Linear , Psilocibina/administração & dosagem , Psilocibina/efeitos adversos , Espectrometria de Massas em Tandem/métodos , Adulto Jovem
6.
Drug Metab Rev ; 49(1): 84-91, 2017 02.
Artigo em Inglês | MEDLINE | ID: mdl-28074670

RESUMO

Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic relevance but considerable physiological variability between individuals that can influence dose-response and toxicological profile has been reported. This review aims to discuss metabolism of psilocybin and psilocin, by presenting all major and minor psychoactive metabolites. Psilocybin is primarily a pro-drug that is dephosphorylated by alkaline phosphatase to active metabolite psilocin. This last is then further metabolized, psilocin-O-glucuronide being the main urinary metabolite with clinical and forensic relevance in diagnosis.


Assuntos
Alucinógenos/farmacocinética , Pró-Fármacos/farmacocinética , Psilocibina/análogos & derivados , Psilocibina/farmacocinética , Humanos , Metabolômica
7.
Forensic Sci Int ; 270: 111-120, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27936426

RESUMO

A method for the statistical comparison of mass spectral data is demonstrated for applications in controlled substance analysis. The method uses an unequal variance t-test at each mass-to-charge ratio in the scan range to determine if two spectra are statistically associated or discriminated. If the two spectra are associated, a random-match probability is calculated to estimate the likelihood that the mass spectral fragmentation pattern in question occurs by random chance alone. If the two spectra are discriminated, the fragment ions responsible for the discrimination are determined. In this work, mass spectral data from case samples containing amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxymethamphetamine (MDMA), phentermine, and psilocin were investigated. All spectra were collected in an accredited forensic laboratory using routine methods for controlled substance analysis. Using the statistical method, spectra of case samples were statistically associated to the corresponding reference standard at the 99.9% confidence level. In these instances, random-match probabilities ranged from 10-39 to 10-29, indicating the probability that the characteristic fragmentation pattern occurred by random chance is extremely small. Further, spectra of case samples were discriminated from other reference standards at the 99.9% or 99.0% confidence level, with 1-26 ions responsible for discrimination in each comparison.


Assuntos
Anfetaminas/química , Estimulantes do Sistema Nervoso Central/química , Espectrometria de Massas , Estatística como Assunto , Humanos , Fentermina/química , Psilocibina/análogos & derivados , Psilocibina/química
8.
J Pharm Biomed Anal ; 125: 427-32, 2016 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-27021629

RESUMO

The taxonomic identification of the biological material contained in the hallucinogenic mushrooms culture media, was carried out using a DNA-based approach, thus highlighting the usefulness of this approach in the forensic identification of illegal samples also when they are present as basidiospores mixed in culture media and spore-bearing fruiting body are not present. This approach is very useful as it allows the unequivocal identification of potentially illicit material before the cultivation and it enables to stop the material to the Customs and to destroy it due to its dangerousness without cultivating the "grow-kits" and without instructing a criminal case. In fact, even if psilocin and psilocybin and the whole mushrooms are illegal in many countries, there is no specific indication in the law about the so called "grow-kits", containing the spores. To confirm the data obtained by the taxonomic identification, a simple, reliable, efficient LC-UV method, using tryptamine as internal standard, suitable for the forensic quali-quantitative determination of psilocin and psilocybin in hallucinogenic mushroom was optimized, validated and applied to the mushrooms grown after the cultivation of the grow-kits seized by the judicial authority, with the authorization of the Ministry of Health. A cation exchange column was used in a gradient elution mode (Phase A: 50mMK2HPO4; 100mM NaCl pH=3 Phase B: methanol). The developed method was linear over the calibration range with a R(2)>0.9992 for both the analytes. The detection and quantification limits were respectively 0.01 and 0.1µg/mL for psilocybin and 0.05µg/mL and 0.1µg/mL for psilocin and the intra- and inter-day precision was satisfactory (coefficients of variation <2.0% for both the analytes). The content of psilocybin in the mushrooms grown from the seized "grow-kits" ranged from 1.02 to 7.60mg/g of dry vegetable material, while the content of psilocin from 0.415 to 8.36mg/g.


Assuntos
Basidiomycota/química , DNA/química , Alucinógenos/química , Psilocibina/análogos & derivados , Psilocibina/análise , Cromatografia Líquida , Espectrofotometria Ultravioleta
9.
Behav Pharmacol ; 27(4): 309-20, 2016 06.
Artigo em Inglês | MEDLINE | ID: mdl-26461483

RESUMO

Psilocybin has recently attracted a great deal of attention as a clinical research and therapeutic tool. The aim of this paper is to bridge two major knowledge gaps regarding its behavioural pharmacology - sex differences and the underlying receptor mechanisms. We used psilocin (0.25, 1 and 4 mg/kg), an active metabolite of psilocybin, in two behavioural paradigms - the open-field test and prepulse inhibition (PPI) of the acoustic startle reaction. Sex differences were evaluated with respect to the phase of the female cycle. The contribution of serotonin receptors in the behavioural action was tested in male rats with selective serotonin receptor antagonists: 5-HT1A receptor antagonist (WAY100635 1 mg/kg), 5-HT2A receptor antagonist (MDL100907 0.5 mg/kg), 5-HT2B receptor antagonist (SB215505 1 mg/kg) and 5-HT2C receptor antagonist (SB242084 1 mg/kg). Psilocin induced dose-dependent inhibition of locomotion and suppression of normal behaviour in rats (behavioural serotonin syndrome, impaired PPI). The effects were more pronounced in male rats than in females. The inhibition of locomotion was normalized by 5-HT1A and 5-HT2B/C antagonists; however, PPI was not affected significantly by these antagonists. Our findings highlight an important issue of sex-specific reactions to psilocin and that apart from 5-HT2A-mediated effects 5-HT1A and 5-HT2C/B receptors also play an important role. These findings have implications for recent clinical trials.


Assuntos
Alucinógenos/farmacologia , Psilocibina/análogos & derivados , Receptores de Serotonina/efeitos dos fármacos , Serotonina/metabolismo , Animais , Relação Dose-Resposta a Droga , Ciclo Estral/fisiologia , Feminino , Alucinógenos/administração & dosagem , Locomoção/efeitos dos fármacos , Masculino , Psilocibina/administração & dosagem , Psilocibina/farmacologia , Ratos , Ratos Wistar , Receptores de Serotonina/metabolismo , Reflexo de Sobressalto/efeitos dos fármacos , Antagonistas da Serotonina/farmacologia , Fatores Sexuais
10.
Neuropharmacology ; 99: 210-20, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26192543

RESUMO

The development of pharmacological magnetic resonance imaging (phMRI) has presented the opportunity for investigation of the neurophysiological effects of drugs in vivo. Psilocin, a hallucinogen metabolised from psilocybin, was recently reported to evoke brain region-specific, phMRI signal changes in humans. The present study investigated the effects of psilocin in a rat model using phMRI and then probed the relationship between neuronal and haemodynamic responses using a multimodal measurement preparation. Psilocin (2 mg/kg or 0.03 mg/kg i.v.) or vehicle was administered to rats (N=6/group) during either phMRI scanning or concurrent imaging of cortical blood flow and recording of local field potentials. Compared to vehicle controls psilocin (2 mg/kg) evoked phMRI signal increases in a number of regions including olfactory and limbic areas and elements of the visual system. PhMRI signal decreases were seen in other regions including somatosensory and motor cortices. Investigation of neurovascular coupling revealed that whilst neuronal responses (local field potentials) to sensory stimuli were decreased in amplitude by psilocin administration, concurrently measured haemodynamic responses (cerebral blood flow) were enhanced. The present findings show that psilocin evoked region-specific changes in phMRI signals in the rat, confirming recent human data. However, the results also suggest that the haemodynamic signal changes underlying phMRI responses reflect changes in both neuronal activity and neurovascular coupling. This highlights the importance of understanding the neurovascular effects of pharmacological manipulations for interpreting haemodynamic neuroimaging data.


Assuntos
Encéfalo/efeitos dos fármacos , Circulação Cerebrovascular/efeitos dos fármacos , Alucinógenos/farmacologia , Psilocibina/análogos & derivados , Animais , Encéfalo/irrigação sanguínea , Encéfalo/fisiologia , Mapeamento Encefálico , Circulação Cerebrovascular/fisiologia , Relação Dose-Resposta a Droga , Eletrodos Implantados , Hemodinâmica/efeitos dos fármacos , Hemodinâmica/fisiologia , Imagem por Ressonância Magnética , Masculino , Oxigênio/sangue , Psilocibina/farmacologia , Ratos Sprague-Dawley , Percepção do Tato/efeitos dos fármacos , Percepção do Tato/fisiologia , Vibrissas/fisiologia
11.
Toxins (Basel) ; 7(4): 1018-29, 2015 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-25826052

RESUMO

The pharmacological activities and acute toxicity of the psilocin (PC) and dried residues of the crude extracts of psychotropic mushrooms were investigated in mice. The hallucinogenic substances were effectively isolated, by using methanol, from the species of Psilocybe semilanceata and Pholiotina cyanopus, that were collected in the north-east region of Poland. The chemical analysis of these extracts, which was performed by liquid chromatography with mass spectrometry detection (LC-MS), indicated the presence of psilocin and other hallucinogenic substances, including indolealkylamines and their phosphorylated analogues. When the pure psilocin or fungal extracts were used, slight differences in determined LD50 values were observed. However, the application of PC evoked the highest level of toxicity (293.07 mg/kg) compared to the activity of extracts from Ph. cyanopus and P. semilanceata, where the level of LD50 was 316.87 mg/kg and 324.37 mg/kg, respectively. Furthermore, the behavioral test, which considered the head-twitching response (HTR), was used to assess the effects of the studied psychotropic factors on the serotonergic system. Both, the fungal extracts and psilocin evoked characteristic serotoninergic effects depending on the dose administered to mice, acting as an agonist/partial agonist on the serotonergic system. A dose of 200 mg/kg 5-hydroxytryptophan (5-HTP) induced spontaneous head-twitching in mice (100% effect), as a result of the formation of 5-hydroxytryptamine (5-HT) in the brain. Compared to the activity of 5-HTP, the intraperitoneal administration of 1mg/kg of psilocin or hallucinogenic extracts of studied mushrooms (Ph. cyanopus and P. semilanceata) reduced the number of head-twitch responses of about 46% and 30%, respectively. In contrast, the administration of PC exhibited a reduction of about 60% in HTR numbers.


Assuntos
Agaricales/química , Misturas Complexas/toxicidade , Alucinógenos/toxicidade , Psilocibina/análogos & derivados , Animais , Animais não Endogâmicos , Comportamento Animal/efeitos dos fármacos , Feminino , Dose Letal Mediana , Metanol/química , Camundongos , Psilocibina/toxicidade , Solventes/química
13.
Biol Pharm Bull ; 38(1): 134-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25342005

RESUMO

Psilocin (3-[2-(dimethylamino)ethyl]-1H-indol-4-ol) is a hallucinogenic component of the Mexican mushroom Psilocybe mexicana and a skeletal serotonin (5-HT) analogue. Psilocin is the active metabolite of psilocybin (3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate). In the present study, we examined the effects of systemically administered psilocin on extracellular dopamine and 5-HT concentrations in the ventral tegmental area (VTA), nucleus accumbens, and medial prefrontal cortex of the dopaminergic pathway in awake rats using in vivo microdialysis. Intraperitoneal administration of psilocin (5, 10 mg/kg) significantly increased extracellular dopamine levels in the nucleus accumbens. Psilocin did not affect the extracellular 5-HT level in the nucleus accumbens. Conversely, systemic administration of psilocin (10 mg/kg) significantly increased extracellular 5-HT levels in the medial prefrontal cortex of rats, but dopamine was decreased in this region. However, neither extracellular dopamine nor 5-HT levels in the VTA were altered by administration of psilocin. Behaviorally, psilocin significantly increased the number of head twitches. Thus, psilocin affects the dopaminergic system in the nucleus accumbens. In the serotonergic system, psilocin contribute to a crucial effect in the medial prefrontal cortex. The present data suggest that psilocin increased both the extracellular dopamine and 5-HT concentrations in the mesoaccumbens and/or mesocortical pathway.


Assuntos
Dopamina/metabolismo , Alucinógenos/farmacologia , Núcleo Accumbens/efeitos dos fármacos , Córtex Pré-Frontal/efeitos dos fármacos , Psilocibina/análogos & derivados , Serotonina/metabolismo , Animais , Masculino , Núcleo Accumbens/metabolismo , Córtex Pré-Frontal/metabolismo , Psilocibina/farmacologia , Ratos Wistar , Área Tegmentar Ventral/efeitos dos fármacos , Área Tegmentar Ventral/metabolismo
14.
J Anal Toxicol ; 39(2): 126-9, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25540060

RESUMO

A method for the simultaneous extraction of the hallucinogens psilocin, bufotenine, lysergic acid diethylamide (LSD) as well as iso-LSD, nor-LSD and O-H-LSD from hair with hydrochloride acid and methanol is presented. Clean-up of the hair extracts is performed with solid phase extraction using a mixed-mode cation exchanger. Extracts are measured with liquid chromatography coupled with electrospray tandem mass spectrometry. The method was successfully validated according to the guidelines of the 'Society of Toxicological and Forensic Chemistry' (GTFCh). To obtain reference material hair was soaked in a solution of the analytes in dimethyl sulfoxide/methanol to allow incorporation into the hair. These fortified hair samples were used for method development and can be employed as quality controls.


Assuntos
Bufotenina/análise , Cabelo/química , Dietilamida do Ácido Lisérgico/análise , Psilocibina/análogos & derivados , Cromatografia Líquida , Humanos , Limite de Detecção , Dietilamida do Ácido Lisérgico/metabolismo , Psilocibina/análise , Extração em Fase Sólida , Espectrometria de Massas em Tandem
15.
Forensic Sci Int ; 237: 1-6, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24513688

RESUMO

A two-step synthesis of psilocin glucuronide (PCG), the main metabolite of psilocin, with methyl 2,3,4-tri-O-isobutyryl-1-O-trichloroacetimidoyl-α-d-glucopyranuronate is reported. With the synthesized PCG, hydrolysis conditions in serum and urine were optimized. Escherichia coli proved to be a better enzyme source for ß-glucuronidase than Helix pomatia. It was essential to add ascorbic acid to serum samples to protect psilocin during incubation. Furthermore the stability of PCG and psilocin was compared as stability data are the basis for forensic interpretation of measurements. PCG showed a greater long-term stability after six months in deep frozen serum and urine samples than psilocin. The short-term stability of PCG for one week in whole blood at room temperature and in deep frozen samples was also better than that of psilocin. Therefore, PCG can be considered to be more stable than the labile psilocin and should always be included if psilocin is analyzed in samples.


Assuntos
Estabilidade de Medicamentos , Glucuronídeos/química , Alucinógenos/química , Psilocibina/análogos & derivados , Manejo de Espécimes , Congelamento , Glucuronidase/química , Humanos , Hidrólise , Estrutura Molecular , Psilocibina/química
17.
Ther Drug Monit ; 35(4): 420-42, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23851905

RESUMO

Psychoactive drugs of fungal origin, psilocin, ibotenic acid, and muscimol among them have been proposed for recreational use and popularized since the 1960s, XX century. Despite their well-documented neurotoxicity, they reached reputation of being safe and nonaddictive. Scientific efforts to find any medical application for these hallucinogens in psychiatry, psychotherapy, and even for religious rituals support are highly controversial. Even if they show any healing potential, their usage in psychotherapy is in some cases inadequate and may additionally harm seriously suffering patients. Hallucinogens are thought to reduce cognitive functions. However, in case of indolealkylamines, such as psilocin, some recent findings suggest their ability to improve perception and mental skills, what would motivate the consumption of "magic mushrooms." The present article offers an opportunity to find out what are the main symptoms of intoxication with mushrooms containing psilocybin/psilocin, muscimol, and ibotenic acid. The progress in analytical methods for detection of them in fungal material, food, and body fluids is reviewed. Findings on the mechanisms of their biologic activity are summarized. Additionally, therapeutic potential of these fungal psychoactive compounds and health risk associated with their abuse are discussed.


Assuntos
Agaricales/química , Alucinógenos/farmacologia , Ácido Ibotênico/farmacologia , Muscimol/farmacologia , Psilocibina/análogos & derivados , Animais , Líquidos Corporais/metabolismo , Alucinógenos/efeitos adversos , Humanos , Ácido Ibotênico/efeitos adversos , Muscimol/efeitos adversos , Psilocibina/efeitos adversos , Psilocibina/farmacologia
18.
Scand J Clin Lab Invest ; 73(5): 400-6, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23692208

RESUMO

AIM: The study aimed to collect information concerning the increasing use of new psychoactive substances, commonly sold through online shops as 'Internet drugs' or 'legal highs', or in terms of masked products such as 'bath salts' and 'plant food'. METHODS: The Karolinska Institutet and Karolinska University Laboratory and the Swedish Poisons Information Centre have initiated a project called 'STRIDA' aiming to monitor the occurrence and trends of new psychoactive substances in Sweden, and collect information about their clinical symptoms, toxicity and associated health risks. A liquid chromatographic-tandem mass spectrometric (LC-MS/MS) multi-component method has been developed, currently allowing for the determination of > 80 novel psychoactive compounds or metabolites thereof. This study focused mainly on the particular drug substances identified and the population demographics of the initial STRIDA cases. RESULTS: In urine and/or blood samples obtained from 103 consecutive cases of admitted or suspected recreational drug intoxications in mostly young subjects (78% were ≤ 25 years, and 81% were males) presenting at emergency departments all over the country, psychoactive substances were detected in 82%. The substances comprised synthetic cannabinoids ('Spice'; JWH analogues), substituted cathinones ('bath salts'; e.g. butylone, MDPV and methylone) and tryptamines (4-HO-MET), plant-based substances (mitragynine and psilocin), as well as conventional drugs-of-abuse. In 44% of the cases, more than one new psychoactive substance, or a mixture of new and/or conventional drugs were detected. CONCLUSION: The initial results of the STRIDA project have documented use of a broad variety of new psychoactive substances among mainly young people all over Sweden.


Assuntos
Drogas Ilícitas/sangue , Psicotrópicos/sangue , Transtornos Relacionados ao Uso de Substâncias/epidemiologia , Adolescente , Adulto , Anfetaminas/sangue , Benzodiazepinas/sangue , Agonistas de Receptores de Canabinoides/sangue , Feminino , Humanos , Indóis/sangue , Masculino , Metanfetamina/análogos & derivados , Metanfetamina/sangue , Pessoa de Meia-Idade , Psilocibina/análogos & derivados , Psilocibina/sangue , Alcaloides de Triptamina e Secologanina/sangue , Transtornos Relacionados ao Uso de Substâncias/sangue , Suécia/epidemiologia , Triptaminas/sangue , Adulto Jovem
19.
Drug Test Anal ; 5(3): 182-5, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22887928

RESUMO

"Magic mushrooms" is the most common name given to hallucinogenic fungi containing the psychoactive alkaloids psilocybin and psilocin. In recent years, fungis' sclerotia, commonly called "magic truffles" have become a form of supply of psychoactive Psilocybe alkaloids since Psilocybe sclerotia are not specifically included in the laws banning the sale, the purchase and the use of such substances and mushrooms containing them. A liquid chromatography -tandem mass spectrometry (LC-MS/MS) method was developed for the rapid determination of psilocybin and psilocin in Psilocybe sclerotia. Following a simple step extraction with methanol, the alkaloids were separated on a reversed-phase column using a gradient of 0.1% formic acid - acetonitrile s a mobile phase at a flow rate of 0.2 mL/min.. Separated analytes were detected by electrospray ionization tandem mass spectrometry in the positive ion mode using multiple reaction monitoring. The developed method was linear over the calibration range for all two substances under investigation, with a r(2) > 0.99. The detection and quantification limits were 0.3 µg and 1 µg per 100 mg truffles, for both psilocin and psilocybin and the intra- and inter-day coefficients of variation were always better than 15%. Using this method, the presence of only psilocybin was demonstrated in examined Psilocybe sclerotia. The content of psilocybin was found to vary over a concentration range of 59.3 to 167.8 µg per 100 mg of fresh sclerotia.


Assuntos
Alucinógenos/análise , Psilocybe/química , Psilocibina/análogos & derivados , Psilocibina/análise , Espectrometria de Massas em Tandem/métodos , Cromatografia Líquida de Alta Pressão/economia , Cromatografia Líquida de Alta Pressão/métodos , Limite de Detecção , Espectrometria de Massas em Tandem/economia , Fatores de Tempo
20.
Int J Legal Med ; 127(3): 593-601, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23183899

RESUMO

A validated method for the simultaneous determination of psilocin, bufotenine, lysergic acid diethylamide and its metabolites in serum, plasma and urine using liquid chromatography-electrospray ionization/tandem mass spectrometry was developed. During the solid-phase extraction procedure with polymeric mixed-mode cation exchange columns, the unstable analytes were protected by ascorbic acid, drying with nitrogen and exclusion of light. The limits of detection and quantitation for all analytes were low. Recovery was ≥86 % for all analytes and no significant matrix effects were observed. Interday and intraday imprecisions at different concentrations ranged from 1.1 to 8.2 % relative standard deviation, bias was within ±5.3 %. Processed samples were stable in the autosampler for at least 2 days. Furthermore, freeze/thaw and long-term stability were investigated. The method was successfully applied to authentic serum and urine samples.


Assuntos
Bufotenina/análise , Cromatografia Líquida/métodos , Alucinógenos/análise , Dietilamida do Ácido Lisérgico/análise , Psilocibina/análogos & derivados , Extração em Fase Sólida/métodos , Espectrometria de Massas por Ionização por Electrospray/métodos , Adulto , Bufotenina/sangue , Bufotenina/urina , Estudos de Casos e Controles , Feminino , Toxicologia Forense , Alucinógenos/sangue , Alucinógenos/urina , Humanos , Dietilamida do Ácido Lisérgico/sangue , Dietilamida do Ácido Lisérgico/urina , Masculino , Pessoa de Meia-Idade , Psilocibina/análise , Psilocibina/sangue , Psilocibina/urina , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Método Simples-Cego , Manejo de Espécimes
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