A thienodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring. The thienodiazepine ring structure forms the central core of several pharmaceutical drugs. Since thienodiazepines interact with the benzodiazepine receptor site, they typically have similar effects as benzodiazepines and can be considered as essentially identical.
Similar to benzodiazepines, the sudden discontinuation of thienodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. It is highly recommended to taper one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.
- 1 Chemistry
- 2 Pharmacology
- 3 Examples
- 4 Subjective effects
- 5 Preparation methods
- 6 Toxicity and harm potential
- 7 See also
- 8 External links
- 9 References
A thienodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring.
Thienodiazepines are often positive allosteric modulators of GABAA receptors.
Disclaimer: The effects listed below are cited from the Subjective Effect Index (SEI), which relies on assorted anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be taken with a healthy amount of skepticism. It is worth noting that these effects will not necessarily occur in a consistent or reliable manner, although higher doses (common+) are more likely to induce the full spectrum of reported effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Motor control loss - Lack of coordination may result in falls and injuries, in particular, in the elderly. Another result of motor control loss is the impairment of driving skills and the increased likelihood of road traffic accidents.
- Muscle relaxation
- Physical euphoria
- Seizure suppression
- Paradoxical reactions to thienodiazepines, as well as benzodiazepines, such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).
- Anxiety suppression
- Compulsive redosing
- Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages.
- Analysis suppression
- Thought deceleration
- Volumetric liquid dosing - If one's thienodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the thienodiazepine volumetrically into a solution so as to dose it accurately based upon the instructions described in this tutorial.
Toxicity and harm potential
Benzodiazepines and thienodiazepines are essentially identical in their pharmacological action, subjective effects, toxicity and harm potential. They can therefore be treated similarly in the appropriate efforts necessary to maximize harm reduction.
The median lethal dosage varies widely between specific substances within the thienzodiazepine class. For this reason, one should always fully research the substance before administering it to themselves or others.
It is strongly recommended that one use harm reduction practices when using these substances.
Tolerance and addiction potential
Tolerance will develop to the sedative-hypnotic effects within a couple of days. Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction. 
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. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as anxiety, insomnia and restlessness.
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 this guide. Small amounts of alcohol can also help to reduce the symptoms.
The duration and severity of withdrawal symptoms depend 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.
- Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- Canadian Guideline for Safe and Effective Use of Opioids for Chronic Non-Cancer Pain - Appendix B-6: Benzodiazepine Tapering | http://nationalpaincentre.mcmaster.ca/opioid/cgop_b_app_b06.html
- http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
- Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
- Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
- Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
- Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
- Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535
- 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
- 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
- A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812