Ecstasy substitute poses major health risks

By Terrapinzflyer · May 9, 2011 · ·
  1. Terrapinzflyer
    Scientists at Anglia Ruskin University haves shown that one of the most common 'legal high' designer drugs, benzylpiperazine, is not only dangerous when it's taken - repeated consumption poses major health risks.

    According to study leader Mike Cole, BZP users claim it has similar effects to ecstasy, but without some of the more unpleasant side-effects. 'It was reclassified as a controlled drug in the UK in December 2009,' he says.

    'Before this, it was made by people who did it for a living, and it was relatively pure. The legislation drove the synthesis underground, as it's a fairly straightforward one-pot reaction, but once the drug is made it starts to react with the starting materials, and badly made BZP also contains other substances such as dibenzylpiperazine.'

    Cole's group, in conjunction with his colleague Lata Gautam, made a number of batches of BZP under different conditions to manipulate the proportions of the impurities. They then tested them against several human cell lines - fibroblasts, liver and kidney cells - both singly and as mixtures. They found that BZP is toxic to the kidney, while the precursor piperazine is toxic to the liver. The impurities are even more harmful and have synergistic effects with BZP itself. 'The damage you see is greater than the sum of the parts,' he says. 'If people suspected to have taken these drugs end up in hospital, medics should do liver and kidney function tests, as it's not always immediately apparent that damage has occurred,' he says.

    The research was presented at the annual meeting of the American Academy of Forensic Sciences.

    According to Ric Treble, scientific advisor at LGC, the number of these 'legal high' drugs is increasing rapidly. 'I believe 41 new compounds were identified last year,' he says. 'They are often sold as "research chemicals" and there is very little information about their short or long term effects.

    Rogue chemists study the chemical literature in search of the next big 'high', Treble says, and make a lot of money out of them. 'They are mostly small chemicals that are relatively easy to make. The belief is they were initially being made in custom labs in China, where they have access to the chemicals and expertise to make them very quickly. The BZPs were, perhaps, the first examples of these, and governments are now rushing to try and control new ones as they appear.'

    According to David Nichols, professor of pharmacology at Purdue University, people make and try new ones, and then post information about them on blogs.

    'Benzylpiperazines are not that difficult to make, and you could make thousands of them with different substitutions,' he says. 'I doubt we've yet touched the surface of what's likely to be active, and what will appear on the market next. No doubt people are going to start making some of these to see if they can hit on one that's really marketable.'

    The next step for Cole's group is to understand better how the cells deal with the drugs. 'We want to understand which metabolic processes are switched on and off to cause the damage, and how this can be used to help patients,' he says. 'We also want to raise awareness of just how dangerous these drugs are.'

    Sarah Houlton
    09 May 2011

    http://www.rsc.org/chemistryworld/News/2011/May/09051102.asp

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  1. Terrapinzflyer
    Scientists are first to study toxic effects of BZP

    Scientists at Anglia Ruskin University have revealed for the first time the serious long-term health risks associated with Benzylpiperazine (BZP), dubbed the "new ecstasy".

    BZP was a popular legal high before it was reclassified as a controlled substance in December 2009.

    According to Dean Ames, the Forensic Science Service's drugs intelligence adviser, the designer drug has replaced MDMA as the main ingredient in ecstasy tablets.

    Dean Ames said:
    "It's a rare drug now, MDMA. There are hundreds of thousands of tablets in circulation in the UK that look like ecstasy tablets, but which actually contain piperazines (a class of compounds that includes BZP).

    The tablets are still being sold as ecstasy and because they have an effect, young people may think they are taking ecstasy."


    Anglia Ruskin's research, led by Professor Mike Cole and Dr Beverley Vaughan, is the first of its kind to examine the health implications of taking piperazines and will help to educate medical staff as to the most serious symptoms associated with their ingestion, namely liver and kidney damage.

    "The market for and abuse of clandestinely synthesised designer drugs has increased significantly over the last decade and this has been accompanied by an increase in the number of reports of death and serious illnesses related to the ingestion of these substances," said Professor Cole, whose preliminary findings were presented at the American Academy of Forensic Sciences' annual conference.

    "Before our research there had been no systematic study of the toxicity of these drugs and this is needed if we are to treat drug users effectively and inform people of the potential hazards associated with taking them."

    The data produced by Professor Cole and Dr Vaughan provides clear evidence of the cellular cytotoxicity of BZP and its synthetic by-products at levels likely to occur following their ingestion. It also indicates that in general the liver, the site of detoxification for the body, is most sensitive to the actions of these drugs.

    "Cells derived from the liver and kidney were exposed to BZP - its starting materials and its impurities - at concentrations which reflected a dose for a user of these drugs. The cells were examined to determine whether significant changes had occurred, including apoptosis (cell suicide) and necrosis (cell murder)," explained Professor Cole.

    "It was found that BZP itself is toxic to the kidney whilst the starting material, piperazine hexahydrate, showed toxicity in only the liver. In general the study showed that water soluble drugs, impurities and mixtures were toxic to liver cells, whilst compounds and mixtures which are fat soluble are toxic to the kidney.

    "Mixtures of drugs and impurities, synthesised to reflect street samples, produced a variety of toxic effects depending upon the composition of the mixture - but all were significantly toxic.

    "The work is important because it begins to provide an explanation of why people who have taken these drugs exhibit the symptoms that they do in A&E rooms.

    "It also shows that different batches of drugs will have different effects because of the different proportions of drug and impurity in the material, and that users are exposed to toxic mixtures of drugs for which both the short and longer-term effects will not be known and cannot easily be predicted."

    Addictions expert Sarah Graham, who is a spokesperson for the Government drugs helpline FRANK, said: "BZP is not safe - it is an entirely synthetic party drug which mimics the effects of ecstasy and speed. It is a stimulant which can raise your blood pressure and may lead to a fit or heart attack.

    "You never know what you are getting because the chemical make up continually changes and mixing the drug with alcohol can increase the risks."

    http://www.anglia.ac.uk/ruskin/en/home/news/bzp.html
  2. Terrapinzflyer
    ARU scientists reveal true risks of 'new Ecstasy' drug

    Scientists Anglia Ruskin University have revealed for the first time the serious long-term health risks associated with a drug dubbed the “new Ecstasy”.
    Benzylpiperazine (BZP) was a popular legal high before it was reclassified as a controlled substance in December 2009.

    According to Dean Ames, the Forensic Science Service’s drugs intelligence adviser, the designer drug has replaced MDMA as the main ingredient in Ecstasy tablets.

    Anglia Ruskin’s research, led by Professor Mike Cole and Dr Beverley Vaughan, is the first of its kind to examine the health implications of taking piperazines – a class of compounds that includes BZP.

    It will help to educate medical staff as to the most serious symptoms associated with their ingestion, namely liver and kidney damage.

    Prof Cole, whose preliminary findings were presented at the American Academy of Forensic Sciences’ annual conference, said: “The market for and abuse of clandestinely synthesised designer drugs has increased significantly over the last decade and this has been accompanied by an increase in the number of reports of death and serious illnesses related to the ingestion of these substances.

    “Before our research there had been no systematic study of the toxicity of these drugs and this is needed if we are to treat drug users effectively and inform people of the potential hazards associated with taking them.”

    The data produced by Professor Cole and Dr Vaughan provides clear evidence of the cellular cytotoxicity of BZP and its synthetic by-products at levels likely to occur following their ingestion.

    It also indicates that in general the liver, the site of detoxification for the body, is most sensitive to the actions of these drugs.

    Prof Cole said: “Cells derived from the liver and kidney were exposed to BZP – its starting materials and its impurities – at concentrations which reflected a dose for a user of these drugs.

    “It was found that BZP itself is toxic to the kidney whilst the starting material, piperazine hexahydrate, showed toxicity in only the liver.

    “In general the study showed that water soluble drugs, impurities and mixtures were toxic to liver cells, whilst compounds and mixtures which are fat soluble are toxic to the kidney.”

    Suzan Uzel
    05/05/201
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