Sleeping pills: How do they help you sleep?

The major classes of sleeping pills

Sleeping pills are mainly divided into 2 classes.  Though there are other classes of medications that are used as sleeping pills such as anti-histamines and anti-depressants, benzodiazepines and benzodiazepine-like non-benzodiazepines are the two major categories of sleeping pills.  Most work similarly with only one exception of Rozerem.  The common mechanism of action leads to similar side effects and issues as they help you sleep better through the same pathway.

Benzodiazepines and benzodiazepine-like non-benzodiazepines

Benzodiazepines and benzodiazepine-like non-benzodiazepines help you sleep through the enhancement of gamma-aminobutyric acid-Benzodiazepine receptor complex.   Gamma-aminobutyric aced (GABA) is a small-molecule neurotransmitter synthesized within the presynaptic terminal of GABA containing neurons.  Once synthesized, GABA is stored in vesicles and remains at the post-synaptic terminal until the arrival of an action potential results in the release of the contents of these vesicles.  Benzodiazepines and benzodiazepine-like sedatives bind to benzodiazepine receptors in the central nervous system locking the receptor into a conformation in which it has a greater affinity for the GABA neurotransmitter resulting in reduction of the activity of neurons.  The binding of GABA to the site opens the chloride channel and the admission of chloride ions into neurons increases the negative electrical charge (hyperpolarization) within the neuron making it more difficult for the neuron to fire an electrical signal and excite adjoining neurons.  Simply put, in the presence of benzodiazepines such as Estazolam, Flurazepam and Temazepam or benzodiazepine-like non-benzodiazepines like Ambien, Sonata and Lunesta, the neurons are less likely to excite neighboring cells thus resulting in better ability to sleep. 

Is there a difference between Benzodiazepines and benzodiazepine-like non-benzodiazepines then in helping me sleep?

The main difference between the benzodiazepine sleeping pills and benzodiazepine-like sleeping pills is that benzodiazepine sleeping pills bind non-selectively to Benzodiazepine receptors in the central nervous system whereas benzodiazepine-like sleeping pills have a certain degree of selectivity to Benzodiazepine receptor subtype 1.  The non-selectivity of the benzodiazepine as a class in general result in certain effects such as muscle relaxant effects as well and anxiolytic effects associated with certain benzodiazepines.  As an example, Valium many times is used for its muscle relaxant effects and anxiolytic effects rather than its sedative effects so even though it is a benzodiazepine, it is not thought of as a sedative.  Xanax will help with anxiety and will make you sleepy but it is mainly categorized as an anxiolytic, not really used as a sleeping pill, per se.  

On its own

Rozerem is a non-benzodiazepine sedative but not a benzodiazepine-like sedative.  Rozerem is a highly selective, potent melatonin receptor agonist.  Rozerem selectively targets the melatonin receptor MT1 and MT2.  Melatonin receptor subtype MT1 is believed to regulate sleepiness and MT2 is thought to help the body shift between day and night.  Rozerem has been reported to have greater affinity, selectivity, and potency than melatonin for the MT1 receptor, resulting in a better ability to induce sleep onset while the duration of action is reported to be longer.  Therefore, it is approved for the treatment of insomnia due to prolonged sleep onset not really for helping maintain sleep once one has fallen asleep. 

Since it does not exert its effects through the GABA-Benzodiazepine receptor complex, it does not share all of the side effects or issues with the Benzodiazepine (BDZ) sleeping pills or BDZ-like non-BDZ sleeping pills.  It has its own set of issues and some similar to BDZ and BDZ-like sleeping pills.  

Knowledge after all, IS power.

Understanding how the sleeping pills work can help you have a more intelligent discussion with your doctor about what might be a better choice of medication to improve your sleep quality.  A well informed person can better understand whether a sleeping pill may be the right choice for them at the right time helping reduce misuse of sleeping pills resulting in financial burden as well as consequences affecting one’s health. 

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Comments 1 comment

gorgia098 5 years ago

Hi, Nice post. I really liked the contents you have posted. It is really very useful blog about alcohol and drug treatment. I learned a lot about benzodiazapines from this blog. Thanks a lot for it.

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