Benzodiazepines (Xanax, Ativan, Valium, etc)

4 Oct 2018 2:33 PM | C.


Everyone loves benzodiazepines - they are like the chocolate bar in the prescription candy shop: a staple that almost everyone enjoys indulging in. I am no exception to that.  However, I have made a decision that the abuse potential of the benzodiazepines is too high for me, and that I must permanently restrict myself from them. 

I was prescribed Xanax when I first went to college to help with social anxiety, panic attack disorder, and mild insomnia (which later got much, much worse). I made switches to both Ativan and Valium throughout my college career due to the quick build up of tolerance these drugs are prone to and the fact that I was using them extensively, to the point of excess. In short, they work incredibly well to eliminate the symptoms, but they don't eliminate the cause. In fact, they help to mask the cause by providing an escape from the symptoms.


Class: Benzodiazepine
Prescribed for: General Anxiety, Panic Attack disorder, Insomnia
Mechanism: Allosteric GABA-A Modulator (benzodiazepine site)

The "benzos" are an entire class of drugs that all share the common backbone structure above. A benzene ring is a flat, six-membered ring with resonating double bonds (shown above as a hexagon with a smaller circle inside, the smaller circle is to notate the double bonds). A diazepine ring is a seven-membered ring with two nitrogen atoms (shown above on the right side with two teal nitrogens). So a benzodiazepine is the combination of these functional groups.

There are many different types of benzodiazepines that all have a similar function - the difference chemically has to do with the "R groups" (circled in red on the image). All of the benzodiazepines bind to the GABA-A receptors in the brain at the same spot as Ambient (Zolpidem)! It works in a similar manner - by increasing the effect of GABA in the brain. GABA is an inhibitory neurotransmitter, which means it decreases brain cell activity. When the benzodiazepines are on the GABA-A receptor and GABA binds, it is able to have a larger effect than it normally does.

One of the most interesting facets of pharmacology is how two drugs can bind to the same place on the same receptor and cause very different effects. This is because proteins are very flexible, squishy molecules and when a drug binds to it, it changes the way this squishy molecule is shaped. This is called "induced fit." So two different molecules can bind to the same place, but change the shape slightly differently which leads to different therapeutic effects. Likewise, two different molecules can bind to different places, but change the shape the same and lead to the same effect! It's crazy.


MY PERSONAL TAKE

For many out there, the benzodiazepines are successful treatment for their anxiety-related problems. Where I differ from them is my innate vulnerability to substance abuse due to my neurodiversity and a lack of self-control when it comes to reducing or eliminating my self-awareness of my own emotional and physical pain. I am always anxious. For me, the anxiety is not the disorder that needs semi-regular intervention, it is always present. So it then becomes very, very difficult when presented with a prescribed drug that takes it away to monitor and control my usage. This is one of the reasons abortive medicines have such a strong addictive potential. I had a very negative experience where I semi-accidentally took too many benzodiazepines to try to end a panic attack that resulted in my then ex-girlfriend giving me an ultimatum about them. After we broke up, I considered resuming using them under stringent conditions, but have since come to the conclusion that it's not worth the risk of falling back into substance abuse. And as annoying as it is to accept that she was right about it, it's true.

A random yet interesting fact about the benzodiazepines is that they will get rid of a "bad trip" when someone is activating their serotonin system with LSD. It is well known that benzodiazepines can eliminate the repetitive loop of a bad trip and allow the person to come out of that state. What's interesting about this to me is that it is a perfect matching of classical neuropharmacology. LSD activates the serotonin system, specifically the 5-HT2A Receptor, which is mainly excitatory. If someone takes too much LSD and is in a hyper-excited state, the benzodiazepine - which functions through GABA, an inhibitory molecule - corrects that effect. Most of the time with effects in the brain, it doesn't work like a simple addition problem, but in this one case it seems like it does!

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