- Klíčová slova
- psychadeliky asistovaná psychoterapie,
- MeSH
- antidepresiva terapeutické užití MeSH
- halucinogeny farmakokinetika farmakologie terapeutické užití MeSH
- lidé MeSH
- LSD terapeutické užití MeSH
- neuroplasticita fyziologie účinky léků MeSH
- psilocybin * farmakologie fyziologie terapeutické užití MeSH
- psychoterapie metody MeSH
- uživatelé drog psychologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
- přehledy MeSH
- MeSH
- diagnostické techniky neurologické MeSH
- halucinogeny farmakokinetika škodlivé účinky terapeutické užití MeSH
- lidé MeSH
- mozek účinky léků MeSH
- nežádoucí účinky léčiv MeSH
- psilocybin * farmakokinetika škodlivé účinky terapeutické užití MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
- přehledy MeSH
Psilocybin, a psychoactive alkaloid contained in hallucinogenic mushrooms, is nowadays given a lot of attention in the scientific community as a research tool for modeling psychosis as well as due to its potential therapeutic effects. However, it is also a very popular and frequently abused natural hallucinogen. This review summarizes all the past and recent knowledge on psilocybin. It briefly deals with its history, discusses the pharmacokinetics and pharmacodynamics, and compares its action in humans and animals. It attempts to describe the mechanism of psychedelic effects and objectify its action using modern imaging and psychometric methods. Finally, it describes its therapeutic and abuse potential.
- MeSH
- chování zvířat účinky léků MeSH
- halucinogeny škodlivé účinky farmakokinetika farmakologie terapeutické užití MeSH
- lidé MeSH
- mozek účinky léků MeSH
- poruchy spojené s užíváním psychoaktivních látek MeSH
- psilocybin škodlivé účinky farmakokinetika farmakologie terapeutické užití MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
Ayahuasca is a drink made from two plants native to the Amazon, Banisteriopsis caapi and Psychotria viridis, which contain the psychoactive chemicals: harmala alkaloids and dimethyltryptamine (DMT). The drink has long been used by aboriginal populations for its putative spiritual and medicinal benefits in countries such as Brazil, Ecuador and Peru. In the 20th century, ayahuasca spread beyond its native habitat and has been incorporated into syncretistic practices that are being adopted by non-indigenous peoples in modern Western contexts. Ayahuasca‘s globalization in the past few decades has led to a number of legal cases which pit religious freedom against national drug control laws. Two principal constituents of ayahuasca are harmala alkaloids and DMT. These compounds, when ingested in combination, produce a unique biochemical synergy resulting in profound idiosyncratic psychoactive effects. Harmala alkaloids are controlled substances in some countries and DMT is prohibited by international drug control conventions. Therefore relatively little is known about therapeutic use of ayahuasca. This article provides an overview of ayahuasca and explores some of the medical and philosophical implications of contemporary ayahuasca use.
- Klíčová slova
- ayahuasca, globalizace, tradiční místní znalosti, využití v medicíně, harmalové alkaloidy,
- MeSH
- Banisteriopsis chemie MeSH
- halucinace MeSH
- halucinogeny farmakokinetika farmakologie MeSH
- kardiovaskulární systém účinky léků MeSH
- LD50 MeSH
- lidé MeSH
- modely u zvířat MeSH
- N,N-dimethyltryptamin MeSH
- rostlinné extrakty farmakokinetika farmakologie MeSH
- serotonin MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- přehledy MeSH
- MeSH
- Amanita chemie MeSH
- atropin farmakokinetika farmakologie izolace a purifikace MeSH
- halucinogeny farmakokinetika farmakologie chemie MeSH
- houby chemie MeSH
- indolové alkaloidy farmakologie izolace a purifikace MeSH
- isoxazoly farmakokinetika farmakologie izolace a purifikace MeSH
- kyselina ibotenová farmakokinetika farmakologie izolace a purifikace MeSH
- lidé MeSH
- muscimol farmakokinetika farmakologie izolace a purifikace MeSH
- N,N-dimethyltryptamin farmakokinetika farmakologie izolace a purifikace MeSH
- psilocybin farmakokinetika farmakologie izolace a purifikace MeSH
- rostlinné přípravky farmakokinetika farmakologie izolace a purifikace MeSH
- skopolamin farmakokinetika farmakologie izolace a purifikace MeSH
- Solanaceae chemie MeSH
- tropany farmakokinetika farmakologie izolace a purifikace MeSH
- Check Tag
- lidé MeSH
p-Methoxymethamphetamine (PMMA) is an illegal psychedelic drug of abuse derived from an amphetamine structure with a risk to health and reports of several cases of intoxications and fatalities caused by its ingestion. However, its pharmacokinetics based on a controlled study is unknown and only partial information on its biotransformation in animal models is available. Our experimental design aimed to study the disposition and kinetic profile of PMMA and its metabolites in rat plasma and selected tissues after the bolus subcutaneous dose of 40mg/kg, using a GC-MS method. Prior to this, we performed a qualitative verification of its metabolites appearing in excreted urine fractions. PMMA maximum plasma concentration of 4014+/-1122ng/mL was reached 30min after dosing, whereas the appearance of metabolites was rather delayed. The disposition of PMMA was characterized by its approximate half-life of 1.0h, volume of distribution of 6.4L/kg and plasma clearance of 4.4L/h. PMMA tissue concentration exceeded plasma and the highest one was found in the lungs (c(max) 42,988+/-10,223ng/g). Penetration through the blood/brain barrier was more efficient considering PMMA and its N-desmethylated metabolite PMA (para-methoxyamphetamine) than hydroxylated metabolites. The maximum brain/plasma ratio value of PMMA (15.8) and PMA (11.8) was reached after 8h of observation. The experimental results ascertained could be useful for subsequent evaluation of the psychotropic or neurotoxic effects of PMMA and for diagnostic concern of intoxication.
- MeSH
- amfetaminy farmakokinetika MeSH
- financování organizované MeSH
- halucinogeny farmakokinetika MeSH
- hematoencefalická bariéra metabolismus MeSH
- injekce subkutánní MeSH
- krysa rodu rattus MeSH
- methamfetamin analogy a deriváty farmakokinetika MeSH
- permeabilita MeSH
- plíce metabolismus MeSH
- plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
- poločas MeSH
- potkani Wistar MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
RATIONALE: Mescaline is a nonselective serotonin receptor agonist. It has relatively delayed onset of action and prolonged duration. Mescaline attenuates various behavioral parameters in rats; however, no information is available about its pharmacokinetics in rats and its relation to the behavioral changes produced by the drug.
- MeSH
- časové faktory MeSH
- financování organizované MeSH
- habituace (psychofyziologie) účinky léků MeSH
- halucinogeny farmakokinetika toxicita MeSH
- inhibice (psychologie) MeSH
- injekce subkutánní MeSH
- krysa rodu rattus MeSH
- meskalin farmakokinetika toxicita MeSH
- metabolická clearance fyziologie MeSH
- mozek metabolismus účinky léků MeSH
- orientace účinky léků MeSH
- plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
- pohybová aktivita účinky léků MeSH
- potkani Wistar MeSH
- úleková reakce účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
2,5-Dimethoxy-4-bromoamphetamine (DOB) is one of the potent hallucinogenic phenylalkylamines, whose ingestion has already caused several deaths reported all over the world. However, there is insufficient information on DOB properties based on controlled pharmacokinetic studies available. The aim of this study was to clarify the distribution profile of DOB and its phenolic metabolite 2-methoxy-5-hydroxy-4-bromoamphetamine (2M5H4BA) in blood and biological tissues of experimental rats. The rats were administered a 20 mg/kg dose of DOB.HCl by oral ingestion or subcutaneous injection. Plasma and brain, liver and lung tissues were collected at 0.5, 1, 2, 4, 8, 16, and 32 h after dosing (three animals per time point). The samples were prepared by a liquid-liquid extraction procedure and the extracts were assayed by GC-MS. After per oral application, DOB peak plasma level of 320 ng/mL was reached after one-hour post dosing as well as 2M5H4BA peak concentration of 203 ng/mL. A rapid phase of DOB absorption, 2M5H4BA formation and their tissue distribution during the first two hours after application were followed by a slow decrease rate of the elimination process until 32 h. After subcutaneous application, high plasma levels of the unchanged parent drug and relatively reduced formation of its metabolite 2M5H4BA were observed. DOB maximum plasma concentration of 1143 ng/mL was reached after one-hour post application, whereas its metabolite peak level after 8 h was 213 ng/mL. The concentration profiles of both compounds in plasma after per oral and subcutaneous administration revealed the existence of significant first pass effect after per oral administration that significantly affected DOB bioavailability. DOB tissue concentrations exceeded plasma and the highest values were found in the lungs, where drug accumulation occurred with prolonged retention till 32 h after subcutaneous dose. Although the plasma/tissue transfer was more effective for the lipophilic parent drug than for its hydroxylated metabolite 2M5H4BA, the metabolite tissue levels were significant. The hallucinogenic potential of 2M5H4BA appearing in brain remains unclear as nothing is known about its pharmacological activity at present.
- MeSH
- 2,5-dimethoxy-4-methylamfetamin aplikace a dávkování analogy a deriváty farmakokinetika krev MeSH
- aplikace orální MeSH
- financování organizované MeSH
- halucinogeny aplikace a dávkování farmakokinetika krev MeSH
- injekce subkutánní MeSH
- játra chemie MeSH
- krysa rodu rattus MeSH
- mozek - chemie MeSH
- plíce chemie MeSH
- plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
- potkani Wistar MeSH
- soudní toxikologie MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- MeSH
- alkoholismus farmakokinetika farmakologie MeSH
- amfetaminy farmakokinetika farmakologie MeSH
- finanční podpora výzkumu jako téma MeSH
- halucinogeny farmakokinetika farmakologie MeSH
- kokain farmakokinetika farmakologie MeSH
- narkotika farmakokinetika farmakologie MeSH
- nikotin farmakokinetika farmakologie MeSH
- poruchy spojené s užíváním psychoaktivních látek MeSH
- Publikační typ
- přehledy MeSH
