Thienodiazepines: Difference between revisions

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Tolerance will develop to the sedative-hypnotic effects within a couple of days.<ref>Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535</ref> Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.<ref>Clinical Pharmacology, Clinical Efficacy, and Behavioral Toxicity of Alprazolam: A Review of the Literature | http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00003.x/pdf</ref> <ref>The American Psychiatric Publishing Textbook of Substance Abuse Treatment | http://books.google.com/books?id=6wdJgejlQzYC&pg=PA222&hl=en#v=onepage&q&f=false</ref>

====Discontinuation====

It is notoriously difficult ~~to discontinue use of thienodiazepines and~~ potentially life-threatening for ~~tolerant~~ individuals using regularly to ~~do so~~ without tapering their dose over a period of weeks. ~~Thienodiazepines are positive allosteric modulators~~ of [[~~GABA~~]] [[~~receptors~~]] so, as ~~the brain is calibrated to operate with higher than usual inhibition, the number of GABA receptors expressed is reduced via downregulation~~. Abrupt discontinuation ~~following chronic use of benzodiazepines~~ causes rebound stimulation which presents as [[anxiety]], [[wakefulness|insomnia]] and restlessness ~~while the body attempts to return to homeostasis~~.

Similar to benzodiazepines, thienodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of [[high blood pressure]], [[seizures]], and death.<ref>A fatal case of benzodiazepine withdrawal. | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as [[anxiety]], [[wakefulness|insomnia]] and restlessness.

~~There is an increased risk of seizure following the discontinuation of thienodiazepines. Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal.~~ It is safest to reduce the dose each day by a very small amount for a couple of weeks until close to abstinence. Small amounts of [[~~ethanol~~]] can also help to reduce the symptoms.

It is safest to reduce the dose each day by a very small amount, for a couple of weeks until close to abstinence. If using a short half-life thienodiazepine, a longer acting drug can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from thienodiazepine in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide]. Small amounts of [[alcohol]] can also help to reduce the symptoms.

The duration and severity of symptoms depends on a number of factors including the half-life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting thienodiazepines. Thienodiazepines with longer half-lives will exhibit ~~discontinuation~~ symptoms with a slow onset and extended duration.

The duration and severity of withdrawal symptoms depends on a number of factors including the half-life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting thienodiazepines. Thienodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.

==See also==

@@ Line 73: / Line 73: @@
 Tolerance will develop to the sedative-hypnotic effects within a couple of days.<ref>Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535</ref> Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.<ref>Clinical Pharmacology, Clinical Efficacy, and Behavioral Toxicity of Alprazolam: A Review of the Literature | http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00003.x/pdf</ref> <ref>The American Psychiatric Publishing Textbook of Substance Abuse Treatment | http://books.google.com/books?id=6wdJgejlQzYC&pg=PA222&hl=en#v=onepage&q&f=false</ref>
 ====Discontinuation====
-It is notoriously difficult to discontinue use of thienodiazepines and potentially life-threatening for tolerant individuals using regularly to do so without tapering their dose over a period of weeks. Thienodiazepines are positive allosteric modulators of [[GABA]] [[receptors]] so, as the brain is calibrated to operate with higher than usual inhibition, the number of GABA receptors expressed is reduced via downregulation. Abrupt discontinuation following chronic use of benzodiazepines causes rebound stimulation which presents as [[anxiety]], [[wakefulness|insomnia]] and restlessness while the body attempts to return to homeostasis.
+Similar to benzodiazepines, thienodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of [[high blood pressure]], [[seizures]], and death.<ref>A fatal case of benzodiazepine withdrawal. | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as [[anxiety]], [[wakefulness|insomnia]] and restlessness.
-There is an increased risk of seizure following the discontinuation of thienodiazepines. Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal. It is safest to reduce the dose each day by a very small amount for a couple of weeks until close to abstinence. Small amounts of [[ethanol]] can also help to reduce the symptoms.
+It is safest to reduce the dose each day by a very small amount, for a couple of weeks until close to abstinence. If using a short half-life thienodiazepine, a longer acting drug can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from thienodiazepine in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide]. Small amounts of [[alcohol]] can also help to reduce the symptoms.
-The duration and severity of symptoms depends on a number of factors including the half-life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting thienodiazepines. Thienodiazepines with longer half-lives will exhibit discontinuation symptoms with a slow onset and extended duration.
+The duration and severity of withdrawal symptoms depends on a number of factors including the half-life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting thienodiazepines. Thienodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.
 ==See also==