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Valium

Where did it get that REPUTATION?

We wanted to take a closer look at the pill

that's always popping up

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Well, it was back in 1955 at the Hoffman-LaRoche Drug Company, a chemist called Dr Leo Sternbach synthesized a drug he thought was in the chemical family quinazoline Noxides. The drug was initially ignored because the company was interested in other projects but a few years later, during a laboratory clean up would you believe, the drug was rediscovered. As the lab proceeded to test the new compound, they found that it had an impressive ability to calm laboratory and even wild animals, producing muscle relaxation as well as preventing convulsions. When the chemistry of the drug was further evaluated, it was found not to have the structure Sternbach originally thought it had, being in fact a benzodiazepine (a minor tranquilizer) and was given the name chlordiazepoxide. This would actually become marketed as Librium and you can't tell the Valium story without including Librium. In an attempt to determine what aspects of Librium's chemical structure were related to which aspects of its effects, the researchers synthesized several other drugs in the benzodiazepine family. Most of them produced very similar effects to Librium - except one, which was found to be much more potent. This drug was given the generic name of diazepam and the trade name Valium. Since the development of Librium and Valium, drug companies have synthesized hundreds of other benzodiazepines and there are currently over 25 benzodiazepines available by prescription in Western countries. It is however, still possible to buy Valium and other benzodiazepines over the counter in many countries like India

How does a benzodiazepine actually work in my brain?

The complex actions of the benzodiazepines are still beyond our understanding and scientists will be the first to admit that there is still a lot more to learn. Rather ironic considering the amount of pills that have been prescribed to millions of people over the years. The knowledge according to researchers, is that anxiety is a state created by an anatomical and biochemical circuit in the brain called the limbic system. It is a very old and difficult to define, area of the brain that is present in evolutionary simple animals as well as in the more recently developed 'higher' animals, such as humans. Researchers have found that damage to certain parts of the limbic system can result in changes in emotional behaviour. Monkeys that normally display fear and aggression towards humans have been shown to become quite tame when specific areas of their limbic systems are destroyed. Similarly in rats, stimulation in this area with a mild electrical current produces reactions of defensiveness and fear. To explain how drugs work in the brain, you need to understand how the brain sends its messages. Electrical messages move around the brain from cell to cell. When a message reaches a gap (or synapse,) between cells, it needs to be 'ferried' across by a neurotransmitter chemical released by the cell. Once the job is done, the neurotransmitter is reabsorbed by the next nerve cell, to await the next message. On the receiving end of each nerve are receptors which are sensitive to the message carried by the neurotransmitters. Researchers have found that benzodiazepines will actually attach (bind) themselves to particular receptors and in fact, they have even called them benzodiazepine receptors . The more effective a benzo is in relieving anxiety, the more strongly it has been known to bind to these benzodiazepine receptors. Other drugs that reduce anxiety like alcohol and barbiturates, will not bind to those same receptors. The second part of this story is about another neurotransmitter called GABA (gamma- aminobutric acid) which is found in the brain and spinal cord. Its particular job is to slow down the activity of the nerves that it contacts. It also seems to help the benzodiazepine drugs bind even more those particular receptors, therefore increasing the effect. The scientists theorize that benzos like Valium work by increasing GABA's ability to do its own job - ie. to decrease the activity of many groups of nerves in the brain and spinal column. This slowing or reducing of messages to nerves in the limbic system will then reduce the reaction time to anxiety producing events. So, we have a reduction of the nerve activity in the spinal cord and limbic system which will produce muscle relaxation and, via the limbic system, relief from certain fears and anxieties. At the same time, the benzo's may reduce the ability of other neurotransmitters to stimulate a fear reaction

Why has Valium had such very good - then seriously bad, press?

In the 1960's and early 70's, Valium and Librium seemed to meet all the criteria for a good treatment for anxiety. They produced little actual sedation at effective doses, were quite safe even when taken in large amounts and 'appeared' to produce little risk of dependence or abuse. Valium was riding on the wave of the barbiturate backlash and Valium and Librium were seen as the perfect answer as overdoses on Valium alone were practically unheard of. In 1975 in the US, Valium seemed to really hit the heights, with 61.3 million prescriptions being written that year alone and it remained a best-seller for two and a half decades. In Britain, benzo's are still the most commonly prescribed medication. It is interesting to note that studies have concluded Valium to be effective for fairly severe long lasting disorders. However tranquillisers, particularly Valium, are used frequently by people with less severe, relatively temporary anxiety (i.e. stress brought about by a specific stressful event). However, medical studies have actually told us very little about the ability of tranquillisers to relieve this type of anxiety.
Today, massive medical documentation clearly shows that dependence is a common and almost anticipated complication in the use of benzos such as Valium. Debate continues however, with some doctors and scientists still maintaining that the only adverse effect of chronic benzo use is dependence and possible withdrawal symptoms when the drugs are discontinued. Others have found a clear correlation between poor mental health of long term users whose adverse effects include chronic depression, OCD (Obsessive Compulsive Disorder), personality changes and phobias. M. Lader at the institute of psychiatry in London estimates the incidences of these adverse reactions at about 5%, even in short term use of the drugs.

 

The problems with dependence

Dependence is not related to self control or to physical or psychological weakness. Dependence can easily be reproduced in experimental animals or even tissues taken from experimental animals

There is reason to be concerned about the dangers of long term use of Valium. Many opiate users have come to know Valium and associated benzos intimately, either as a booster for their gear, or as part of a home detox or something when you're hanging out. Many users have also got their benzo habits kicked off by the black market trade in these drugs, eventually turning up at their Gp's with a benzo dependence. The experiences described as Valium withdrawals are reactions to the absence of Valium in the body, usually following high dosages or long term use of the drug. These reactions, most frequently jitteriness, tremors, anxiety, insomnia, strange tastes and smells, tinnitus, panic, sweating, cramps, and, under extreme conditions, convulsions (seizures), can all indicate physical dependence on the drug. Post withdrawal symptoms can last from several weeks, months, even longer and continued support may be required to prevent relapse. Dependence is not related to self control or to physical or psychological weakness . Dependence can easily be reproduced in experimental animals or even tissues taken from experimental animals. Physical or psychological dependence can develop very quickly with these drugs and it seems that some people are more susceptible to dependence than others. Psychologist W. O'Mara talks of the paradoxical effects of Valium. "When the drug is prescribed irresponsibly, without a clear explanation of the withdrawals and adverse effects, the withdrawal symptoms can become very frightening and if not understood as being part of the withdrawal syndrome, can sometimes be misunderstood as mental illness.

Diazepam should be used with caution in people with impaired liver or kidney function (such as hepatitis C) and sedation, or respiratory and cardiovascular (heart) depression may be enhanced by other drugs like opiods, neuroleptics (drugs for epilepsy) and alcohol. It should not be used alone to treat bereavement, depression or anxiety that's associated with depression as it maymust always be sought from a sympathetic GP when detoxing of these drugs.

(We hope all Prisons Governors take note of this fact as they repeatedly withdraw benzo users far too quickly, often precipitate suicide or aggressive behaviour. It can be used for short term severe anxiety states, when it has been clearly established that these are not depression related".

Never reduce the intake of a benzodiazepine like Valium rapidly or overnight if you have been taking them for more than one month. Help without any reducing at all - that's another article - ed).

The Drug Companies and the Millennium

Adverse reactions. In the U.S., manufacturers feel compelled to report adverse reactions and note that e.g. Depression can occur. In most European countries however, drug manufacturers do not even mention this adverse reaction, even though depression is a long-term effect that has been well-documented in medical literature. Since these reactions are often interpreted as a worsening health, many patients become ensnared by dependence merely because they respond with adverse reactions. It is high time for WHO (The World Health Organisation) and national regulatory authorities to force ROCHE and other benzodiazepine manufacturers to supply complete and accurate information on the many adverse reactions that are possible.

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(All references used are available from Black Poppy 0181 968 3311 - ed).

Black Poppy, Science on Substances - Valium