Hej Psy! Der er langsomt ved at dukke nogle videnskabelige papirer op, som så småt kortlægger metaboliseringen af Mephedrone. Jeg ville lige dele dem med jer, hvis i skulle være interesserede.
OBS: Det kræver forholdsvist øvede engelske, biologiske og evt. kemiske kundskaber at læse og forstå ALLE papirer.
Hold venligst diskussion på et højt niveau, da subjektive 'trip-rapporter' og ligegyldige udmeldinger som "Jamen jeg var altså mere blæst, end hvis jeg var på efedrin" er ligegyldige og unødvendige.
Analytical data:
Kode:
Olivier Roussel, Martine Perrin, Philippe Herard, Marc Chevance, Patrick Arpino
Abstract – A capsule, presumed to contain ecstasy, was seized in 2007 and transmitted to the laboratory of the IRCGN
for confirmation purpose. However, after chemical analysis using ion mobility spectrometry, gas chromatographyelectron
ionisation mass spectrometry (GC-EI/MS), nuclear magnetic resonance spectroscopy (NMR), and liquid
chromatography, electrospray ionisation mass spectrometry (LC-ESI/MS), the substance was identified as 4-
methylephedrone and not as ecstasy. This case was an example of the development of new addictive drugs, specifically
designed to by-pass current legislation, and generally called ‘designer drugs’.
Key words: 4-methylephedrone, NMR, GC-MS, LC-ESI/MS
http://www.ata-journal.org/articles/...t/ata09028.pdfOg en mere gennemgående analyse af bk-PEA's metabolisering
in vivoKode:
Metabolism of the new designer drug mephedrone
and toxicological detection of the beta keto designer drugs
mephedrone, butylone and methylone in urine
M.R. Meyer, F.T. Peters, H.H. Maurer
Department of Experimental and Clinical Toxicology, Saarland University,
D-66421 Homburg (Saar), Germany
Introduction: Beta keto (bk) designer drugs are a new class of drugs of
abuse. In contrast to mephedrone (2-methylamino-1-p-tolylpropane-1-one),
the metabolism of butylone (2-methylamino-1-(3,4-methylenedioxyphenyl)
butan-1-one, bk-MBDB) and methylone (3,4-methylenedioxymethcathinone,
bk-MDMA) has already been investigated. So far, these designer drugs have
not yet been included in our systematic toxicological analysis (STA).
Aim: The first aim of the presented work was to study the metabolism of
mephedrone and to incorporate all of the above-mentioned bk-designer drugs
into our STA. The second aim was to check for suitability of our rat model
by comparing incurred rat urine samples with human urine samples from
mephedrone and butylone users.
Methods: For the metabolism study, urine samples from male Wistar rats
(20 mg/kg BW) were extracted (liquid-liquid or Isolute Confirm HCX
cartridges) after enzymatic cleavage of conjugates. After extraction and
acetylation, the metabolites were separated and identified by GC–MS in
the electron ionisation and in the positive chemical ionisation mode. For
toxicological detection, a common users dose corresponding to 1 mg/kg
BW were administered to rats and urine was collected over a 24 h period.
Human urine submitted to our laboratory for toxicological analysis was
collected approximately 6 hours after intake of an unknown amount of
butylone and mephedrone. The rat and human urine samples were analyzed
using our STA based on an acid hydrolysis followed by liquid-liquid
extraction, acetylation and analysis via full-scan GC-MS. Finally, the
results from the metabolism and screening studies in rats were compared
to those obtained from the patients’ urine to verify the suitability of the
used rat model.
Results: Analysis of the rat and human samples revealed the following
main metabolic steps for mephedrone: N-demethylation to the primary
amine, reduction of the keto moiety to the respective alcohol and oxidation
of the tolyl moiety to the corresponding alcohols and carboxylic acids. The
metabolites of butylone and mephedrone detected in rat urine could also be
found in human urine samples. Using our STA, the parent compounds and
N-demethyl metabolites could be detected in rat urine after a common user’s
dose as well as in the patients’ urine samples in the case of mephedrone and
butylone.
Conclusion: Besides the elucidation of the metabolism of the new designer
drug mephedrone, we were able to show, that our STA was suitable to proof
S1-23
Ann Toxicol Anal. 2009; 21(S1) Abstracts
an intake of at least butylone and/or mephedrone in human urine. These
examples showed again that the used rat model was suitable to predict the
qualitative metabolism and detectability of drugs in human urine.
Keywords: designer drugs, butylone, mephedrone, methylone, metabolism
http://www.ata-journal.org/articles/...ta2009s102.pdf---
Hvis vi går ud fra at ephedrin og 4-MMC har en nogenlunde ens risikoprofil (omend rapporterne hentyder, at 4-MMC er værre), kan vi begynde at se på hvordan skaderne af ephedrin kommer til overfladen, så at sige.
Citat:
working on the basis that ephedrine and 4-methylephedrine have a similar toxicological profile we can use ephedrine data to get an idea of the problems long term mephedrone use is going to have. There is a strong possibility that mephedrone also causes neurological damage as well as the ephedrine-like peripheral effects.
Kode:
CMAJ • March 5, 2002; 166 (5)
Ephedrine is a sympathomimetic
drug prescribed as a nasal decongestant,
with properties similar to epinephrine;
its effects on both α- and β-adrenergic
receptors and its central effects resemble
those of amphetamines (see figure).7
The adverse effects of ephedrine are hypothesized
to be related to coronary
artery constriction, vasospasm, shortening
of cardiac refractory periods allowing
re-entrant cardiac arrhythmias,
hypertension-induced subarachnoid hemorrhage,
cerebral artery vasoconstriction
and sympathomimetic-induced
platelet activation.
full article free access
http://www.cmaj.ca/cgi/reprint/166/5/633Kode:
Norpseudoephedrine aka phenylpropanolamine adverse reactions also includes discussion of ephedrine toxicity
Adverse Drug Reaction Bulletin:
August 1984 - Volume 107 - Issue 1 - ppg 396-399
Phenylpropanolamine resembles ephedrine in
activity but is said to cause less CNS stimulation. As
well as being a constituent in cold remedies, it has also
been used as an appetite suppressant. There are many
reports of hypertension following its use as an appetite
suppressant, but even single doses of 50mg
phenylpropanolamine contained in a cold remedy were
sufficient to increase the diastolic blood pressure in
12% of subjects to over 100 mm Hg . Stroke
following the ingestion of large doses of
phenylpropanolamine is a well recognized
complication12. Myocardial injury has been reported
in three previously healthy young patients following
phenylpropanolamine ingestion13. In one of these
cases ischaemic chest pain occurred following ingestion
of a single capsule containing phenylpropanolamine
50mg, chlorpheniramine 4mg, and belladonna
alkaloids 0.2mg. In the other two cases, myocardial
damage was associated with very large doses of
phenylpropanolamine ingested as a deliberate drug
overdose.
http://journals.lww.com/adversedrugr...in_Cold.1.aspxFlere rapporter om efedrin og lignende strukturers toksiske egenskaber:
Kode:
The RAND report, commissioned by the National Institutes of Health (NIH), was able to identify sentinel events related to ephedra and ephedrine consumption. For ephedra containing products, the following were identified as sentinel events: two deaths, three myocardial infarctions, nine cerebrovascular accidents, three seizures, and five psychiatric cases. For ephedrine consumption, sentinel events included: three deaths, two myocardial infarctions, two cerebrovascular accidents, one seizure, and three psychiatric cases. The symptoms described in the psychiatric cases included psychosis, hallucinations, delusions, homicidal intent, insomnia and paranoia. Between ephedra and ephedrine, 50 additional cases were identified as possible sentinel events. Another study, funded by the National Center for Complementary and Alternative Medicine (NCCAM), released preliminary results on the relative safety of ephedra compared with other herbal products. The study found that the relative risk for an adverse reaction from ephedra was more than 100 times greater compared with other herbs.
https://www.clevelandclinicmeded.com...03/ephedra.htmEfedrin (og de fleste analoger) er altså et farligt stof, ikke så meget pga. neurotoksitet, men fordi det i langtidsbrug og overdosis skader hjerte og kredsløb voldsomt.Kode:
Major safety concerns have been associated with ephedra or ephedrine use, including hypertension, tachycardia, CNS excitation, arrhythmia, myocardial infarction, and stroke. In 1997, due to over 800 U.S. reports of serious toxicity (and many more worldwide) including at least 22 deaths in adolescents and young adults, the U.S. Food and Drug Administration (FDA) adopted a policy that ephedra-containing products must: (1) be labeled with all possible adverse effects, including death; (2) contain no more than 8mg of ephedrine per serving; and (3) be used for no more than seven days. The FDA also proposed a maximum daily dose of 24mg, and a ban on ephedra-caffeine combination products (these proposed limits were subsequently withdrawn).
In 2002, Samenuk et al. identified 926 cases of possible ephedra toxicity reported to the Adverse Reaction Monitoring System of the FDA between 1995-1997. In 37 patients, use of ephedra was temporally related to stroke (16 patients), myocardial infarction (10), or sudden death (11). Autopsies performed in patients who experienced sudden death showed a normal heart in one, coronary atherosclerosis in three, and cardiomyopathies in three. In 36 of the 37 patients, use of ephedra was reported to be within the manufacturers' dosing guidelines.
In 2003, a report was prepared by Shekelle et al. on behalf of the RAND Southern California Evidence-based Practice Center for the Agency for Healthcare Research and Quality, U.S. Department of Health and Human Services. This study reviewed available clinical trials, as well as more than 1,500 adverse event reports to the FDA and adverse event reports to the manufacturer Metabolife. Although most prospective trials were not sufficiently large and most adverse event reports were not sufficiently detailed, the authors identified three deaths, two myocardial infarctions, two cerebrovascular accidents, one seizure, and three psychiatric cases that were considered to be "sentinel events" (i.e., strongly tied to ephedra use within 24 hours without other plausible explanations). In addition, 50 other possible sentinel events were identified.
A 2003 analysis by Bent et al. in Annals of Internal Medicine found that products containing ephedra account for 64% of all adverse reactions to herbs in the United States, but only represent 0.82% of herbal product sales. The relative risk for an adverse reaction in a person using ephedra compared with other herbs was extremely high, ranging from 100 (95% CI, 83 to 140) for kava to 720 (95% CI, 520 to 1100) for Ginkgo biloba . It was concluded that ephedra use poses a greatly increased risk of adverse reactions compared with other herbs. A 2003 analysis published in Neurology also found increased risk of stroke associated with ephedra-containing products.
Håber det kunne bruges til noget.
Det hele er tyvstjålet fra bluelight, men jeg ved at bestemt ikke alle herinde, læser der.
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