Saturday, April 17, 2010

Research into Valium and the risk of dependence continues

Even though there have been a wide range of drugs on the market for many years derived from the benzodiazepines, the research into their character and performance continues apace. This does not mean the drugs are any less safe than when they were first introduced more than fifty years ago. It simply reflects the genuine desire to improve their performance. The key problem remains the need to limit time. No matter how effective the drug may be, there is a real risk of psychological or physical dependence if people take the drug at too high a dosage or over too long a period of time. Why is this? The reason is that, in the same way as cannabis and the more powerful heroin affect the chemistry of the brain, so the benzodiazepines offer chemical rewards to the pleasure centers of the brain. Researchers in the US and Switzerland have recently released the results of study into the precise mechanism at work. We have long known that the benzodiazepines affect the level of the neurotransmitter called Gamma-Aminobutyric Acid (GABA). As the amount of GABA increases, this triggers the release of dopamine, which is a so-called gratification hormone. It makes us feel good. It rewards us for taking the pill and encourages us to repeat the activity. In this, the benzodiazepines are working in exactly the same way as the addictive street drugs. However, the latest research pinpoints a specific receptor in the GABA's chemical structure. For the technically minded, this is called the Alpha1 Sub-Unit of the GABA Type A Receptor.

You are now all saying, "So what?" In fact, this is a very big "what". For the last fifty and more years, we have had to limit our uses of some very valuable drugs. Suppose we can tweak the benzodiazepines so they bind to Alpha2, Alpha3, or to the Type B Receptor. This linkage may produce the result we want without triggering the release of the dopamine. If no dopamine is released, we have a non-addictive version of the benzodiazepines. That is not just for the anti-anxiety and antidepressive drugs. It also includes useful drugs used for appetite suppression, and so on.

Over the last ten years, there has been new research into producing the next generation of valium. Early results in manipulating Alpha2 and Alpha3 have not yet proved a success, but Merck and the other pharmaceutical companies are investing increasing amounts of money in the push to modify the chemistry of the current anti-anxiety and panic disorder drugs to produce the same effect but without the problem of dependence. Until this work delivers clinical trial results sufficient to satisfy the FDA, we will continue to rely on valium - a drug that has consistently proved itself effective to control anxiety and worry, and eliminate the threat of panic attacks. But, of course, with the condition that we do not exceed the dosage instructions given to us by doctors and pharmacists. The risk of dependence is manageable but real. If we do abuse this drug, we end up in much the same position as if we had become addicted to heroin or one of its derivatives. Once the brain's reward system has been activated, it produces increasingly unpleasant withdrawal symptoms if we stop taking the drug. Many people find they lack the willpower to fight through the symptoms and stay free. Let us hope the researchers can tweak valium so we can have the benefits without this risk.


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