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'''Diclazepam''' (also known as '''chlorodiazepam''') is a lesser-known novel [[psychoactive class::depressant]] substance of the [[chemical class::benzodiazepine]] class. It is a structural analog of [[diazepam]] (Valium) and is reported to produce similar effects.<ref>Yakubovs'ka et al. - Dopovidi Akademii Nauk Ukrains'koi RSR, Seriya B: Geologichni, Khimichni ta Biologichni Nauki,1977,page 819</ref>
'''Diclazepam''' (also known as '''chlorodiazepam''') is a lesser-known novel [[psychoactive class::depressant]] substance of the [[chemical class::benzodiazepine]] class. It is a structural analog of [[diazepam]] (Valium) and is reported to produce similar effects.<ref>{{cite book | veditors=((Akademii͡a nauk Ukraïnsʹkoï RSR)) | date= 1977 | title=Dopovidi Akademiï nauk Ukraïns’koï RSR. Serii͡a B: Heolohii͡a, heofizyka, khimii͡a ta biolohii͡a | publisher=Naukova dumka}}</ref>
Diclazepam was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960.<ref>US Patent 3136815 - Amino substituted benzophenone oximes and derivatives thereof</ref> Diclazepam is not currently marketed as a medication, but rather sold online as a [[research chemical]].
Diclazepam was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960.<ref>{{Citation | vauthors=((Earl, R.)), ((Henryk, S. L.)) | title=Amino substituted benzophenone oximes and derivatives thereof | url=https://patents.google.com/patent/US3136815A/en}}</ref> Diclazepam is not currently marketed as a medication, but rather sold online as a [[research chemical]].
[[Subjective effects]] are similar to diazepam and include [[anxiety suppression]], [[disinhibition]], [[anticonvulsant]], [[hypnotic]], [[muscle relaxant|muscle relaxing]], and [[amnesia]]. In animal studies, it has a potency of approximately ten times that of [[diazepam]].{{citation needed}} Its potency has not been systematically tested in humans, but its closest relatives and two main metabolites are lormetazepam<ref>http://www.benzo.org.uk/manual/bzcha01.htm#4</ref> with a potency value of x10-12 of delorazepam<ref>http://www.drugbank.ca/drugs/DB01511</ref> which is roughly x10 the potency of [[diazepam]].<ref>http://drugable.com/drug/Delorazepam</ref>
[[Subjective effects]] are similar to diazepam and include [[anxiety suppression]], [[disinhibition]], [[anticonvulsant]], [[hypnotic]], [[muscle relaxant|muscle relaxing]], and [[amnesia]]. In animal studies, it has a potency of approximately ten times that of [[diazepam]].{{citation needed}} Its potency has not been systematically tested in humans, but its closest relatives and two main metabolites are lormetazepam<ref>{{Citation | title=benzo.org.uk : Benzodiazepines: How They Work & How to Withdraw, Prof C H Ashton DM, FRCP, 2002 | url=https://www.benzo.org.uk/manual/bzcha01.htm#4}}</ref> with a potency value of x10-12 of delorazepam<ref>{{Citation | title=Delorazepam | url=https://go.drugbank.com/drugs/DB01511}}</ref> which is roughly x10 the potency of [[diazepam]].
It should be noted that [[Benzodiazepine#Discontinuation|the sudden discontinuation of benzodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> It is highly recommended to [[taper]] one's dose by gradually lowering the amount taken each day over a prolonged period of time rather than stopping use abruptly, as this can lead to severe, potentially life-threatening withdrawal symptoms.<ref>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</ref>
It should be noted that [[Benzodiazepine#Discontinuation|the sudden discontinuation of benzodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.<ref name="Lann2009">{{cite journal | vauthors=((Lann, M. A.)), ((Molina, D. K.)) | journal=The American Journal of Forensic Medicine and Pathology | title=A fatal case of benzodiazepine withdrawal | volume=30 | issue=2 | pages=177–179 | date= June 2009 | issn=1533-404X | doi=10.1097/PAF.0b013e3181875aa0}}</ref> It is highly recommended to [[taper]] one's dose by gradually lowering the amount taken each day over a prolonged period of time rather than stopping use abruptly, as this can lead to severe, potentially life-threatening withdrawal symptoms.<ref>{{cite journal | vauthors=((Kahan, M.)), ((Wilson, L.)), ((Mailis-Gagnon, A.)), ((Srivastava, A.)) | journal=Canadian Family Physician | title=Canadian guideline for safe and effective use of opioids for chronic noncancer pain. Appendix B-6: Benzodiazepine Tapering | volume=57 | issue=11 | pages=1269–1276 | date= November 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3215603/ | issn=0008-350X}}</ref>
==Chemistry==
==Chemistry==
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==Pharmacology==
==Pharmacology==
Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter [[GABA|gamma aminobutyric acid (GABA)]] by acting on its [[receptor]]s.<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of diclazepam on the nervous system.
Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter [[GABA|gamma aminobutyric acid (GABA)]] by acting on its [[receptor]]s.<ref>{{cite journal | vauthors=((Haefely, W.)) | journal=Neuroscience Letters | title=Benzodiazepine interactions with GABA receptors | volume=47 | issue=3 | pages=201–206 | date=29 June 1984 | issn=0304-3940 | doi=10.1016/0304-3940(84)90514-7}}</ref> As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of diclazepam on the nervous system.
The [[anticonvulsant]] properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.<ref>Benzodiazepines, but not beta-carbolines, limit high-frequency repetitive firing of action potentials of spinal cord neurons in cell culture. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2450203</ref>
Diclazepam has an approximate elimination half-life of 42 hours and undergoes ''N''-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound.<ref>{{cite journal | vauthors=((Bareggi, S. R.)), ((Truci, G.)), ((Leva, S.)), ((Zecca, L.)), ((Pirola, R.)), ((Smirne, S.)) | journal=European Journal of Clinical Pharmacology | title=Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans | volume=34 | issue=1 | pages=109–112 | date= 1988 | issn=0031-6970 | doi=10.1007/BF01061430}}</ref> Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzymes occurring concurrently with ''N''-demethylation.
The [[anticonvulsant]] properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.<ref>{{cite journal | vauthors=((McLean, M. J.)), ((Macdonald, R. L.)) | journal=The Journal of Pharmacology and Experimental Therapeutics | title=Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture | volume=244 | issue=2 | pages=789–795 | date= February 1988 | issn=0022-3565}}</ref>
==Subjective effects==
==Subjective effects==
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{{effects/paradoxical|
{{effects/paradoxical|
Paradoxical reactions to [[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%).<ref>http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review</ref><ref>Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf</ref><p>
Paradoxical reactions to [[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%).<ref>{{cite journal | vauthors=((Saïas, T.)), ((Gallarda, T.)) | journal=L’Encephale | title=[Paradoxical aggressive reactions to benzodiazepine use: a review] | volume=34 | issue=4 | pages=330–336 | date= September 2008 | issn=0013-7006 | doi=10.1016/j.encep.2007.05.005}}</ref><ref>{{cite journal | vauthors=((Paton, C.)) | journal=Psychiatric Bulletin | title=Benzodiazepines and disinhibition: a review | volume=26 | issue=12 | pages=460–462 | date= December 2002 | url=https://www.cambridge.org/core/journals/psychiatric-bulletin/article/benzodiazepines-and-disinhibition-a-review/421AF197362B55EDF004700452BF3BC6 | issn=0955-6036 | doi=10.1192/pb.26.12.460}}</ref><p>
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.<ref>Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs</ref><ref>Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev</ref></p>
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.<ref>{{cite journal | vauthors=((Bond, A. J.)) | journal=CNS Drugs | title=Drug- Induced Behavioural Disinhibition | volume=9 | issue=1 | pages=41–57 | date=1 January 1998 | url=https://doi.org/10.2165/00023210-199809010-00005 | issn=1179-1934 | doi=10.2165/00023210-199809010-00005}}</ref><ref>{{cite journal | vauthors=((Drummer, O. H.)) | journal=Forensic Science Review | title=Benzodiazepines - Effects on Human Performance and Behavior | volume=14 | issue=1–2 | pages=1–14 | date= February 2002 | issn=1042-7201}}</ref></p>
}}
}}
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*'''[[Effect::Anxiety|Rebound anxiety]]''' - Rebound anxiety is a commonly observed effect with [[anxiety suppression|anxiety relieving]] substances like [[benzodiazepines]]. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
*'''[[Effect::Anxiety|Rebound anxiety]]''' - Rebound anxiety is a commonly observed effect with [[anxiety suppression|anxiety relieving]] substances like [[benzodiazepines]]. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
*'''[[Effect::Dream potentiation]]'''<ref>Goyal, Sarita. "Drugs and Dreams." Indian Journal of Clinical Practice (n.d.): n. pag. Web. | http://medind.nic.in/iaa/t13/i3/iaat13i3p624.pdf</ref> or '''[[Effect::Dream suppression]]'''
*'''[[Effect::Dream potentiation]]'''<ref>{{cite journal | vauthors=((Goyal, S.)) | journal=Canadian Medical Association Journal | title=Drugs and dreams | volume=102 | issue=5 | pages=524 | date=14 March 1970 | issn=0008-4409}}</ref> or '''[[Effect::Dream suppression]]'''
*'''[[Effect::Sleepiness|Residual sleepiness]]''' - While benzodiazepines can be used as an effective [[hypnotic|sleep-inducing]] aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
*'''[[Effect::Sleepiness|Residual sleepiness]]''' - While benzodiazepines can be used as an effective [[hypnotic|sleep-inducing]] aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
*'''[[Volumetric liquid dosing]]''' - If one's benzodiazepines 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 benzodiazepine volumetrically into a non-polar solution such as propylene glycol and dose it accurately based upon the methodological instructions linked within this [[Volumetric liquid dosing|tutorial]].
*'''[[Volumetric liquid dosing]]''' - If one's benzodiazepines 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 benzodiazepine volumetrically into a non-polar solution such as propylene glycol and dose it accurately based upon the methodological instructions linked within this [[Volumetric liquid dosing|tutorial]].
==Toxicity and harm potential==
==Toxicity and harm potential==
[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</ref>]]
[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>{{cite journal | vauthors=((Nutt, D.)), ((King, L. A.)), ((Saulsbury, W.)), ((Blakemore, C.)) | journal=The Lancet | title=Development of a rational scale to assess the harm of drugs of potential misuse | volume=369 | issue=9566 | pages=1047–1053 | date=24 March 2007 | url=https://www.sciencedirect.com/science/article/pii/S0140673607604644 | issn=0140-6736 | doi=10.1016/S0140-6736(07)60464-4}}</ref>]]
{{Further|Research chemicals#Toxicity and harm potential}}
{{Further|Research chemicals#Toxicity and harm potential}}
Diclazepam likely has a [[Toxicity::low toxicity]] relative to dose.<ref>Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614</ref> However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]].
Diclazepam likely has a [[Toxicity::low toxicity]] relative to dose.<ref>{{cite journal | vauthors=((Mandrioli, R.)), ((Mercolini, L.)), ((Raggi, M. A.)) | journal=Current Drug Metabolism | title=Benzodiazepine metabolism: an analytical perspective | volume=9 | issue=8 | pages=827–844 | date= October 2008 | issn=1389-2002 | doi=10.2174/138920008786049258}}</ref> However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]].
It is strongly recommended that one use [[harm reduction practices]], such as [[volumetric dosing]], when using this substance to ensure the accurate administration of the intended dose.
It is strongly recommended that one use [[harm reduction practices]], such as [[volumetric dosing]], when using this substance to ensure the accurate administration of the intended dose.
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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. For more information on tapering from benzodiazepines in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide].
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. For more information on tapering from benzodiazepines in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide].
[[Benzodiazepine#Discontinuation|Benzodiazepine 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 [[hypertension]], [[seizures]], and death.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal.
[[Benzodiazepine#Discontinuation|Benzodiazepine 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 [[hypertension]], [[seizures]], and death.<ref name="Lann2009" /> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal.
Diclazepam presents cross-tolerance with [[Cross-tolerance::all [[GABAergic]]s]], meaning that after its consumption all benzodiazepines will have a reduced effect.
Diclazepam presents cross-tolerance with [[Cross-tolerance::all [[GABAergic]]s]], meaning that after its consumption all benzodiazepines will have a reduced effect.
===Overdose===
===Overdose===
Benzodiazepine overdose may occur when a [[benzodiazepine]] is taken in extremely heavy quantities or concurrently with other [[depressants]]. This is particularly dangerous with other GABAergic depressants such as [[barbiturate|barbiturates]] and [[alcohol]] since they work in a similar fashion, but bind to distinct allosteric sites on the GABA<sub>A</sub> receptor. Thus, their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA<sub>A</sub> receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer<ref>Twyman, R. E., Rogers, C. J., & Macdonald, R. L. (1989). Differential regulation of γ‐aminobutyric acid receptor channels by diazepam and phenobarbital. ''Annals of Neurology'', 25(3), 213-220. https://doi.org/10.1002/ana.410250302</ref>. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.
Benzodiazepine overdose may occur when a [[benzodiazepine]] is taken in extremely heavy quantities or concurrently with other [[depressants]]. This is particularly dangerous with other GABAergic depressants such as [[barbiturate|barbiturates]] and [[alcohol]] since they work in a similar fashion, but bind to distinct allosteric sites on the GABA<sub>A</sub> receptor. Thus, their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA<sub>A</sub> receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer<ref>{{cite journal | vauthors=((Twyman, R. E.)), ((Rogers, C. J.)), ((Macdonald, R. L.)) | journal=Annals of Neurology | title=Differential regulation of ?-aminobutyric acid receptor channels by diazepam and phenobarbital | volume=25 | issue=3 | pages=213–220 | date= March 1989 | url=https://onlinelibrary.wiley.com/doi/10.1002/ana.410250302 | issn=0364-5134 | doi=10.1002/ana.410250302}}</ref>. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.
Symptoms of a benzodiazepine overdose may include severe [[thought deceleration]], [[language suppression|slurred speech]], [[confusion]], [[delusions]], [[respiratory depression]], coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with [[flumazenil]], a GABA<sub>A</sub> antagonist,<ref>Amrein, R., Leishman, B., Bentzinger, C., & Roncari, G. (1987). Flumazenil in benzodiazepine antagonism. ''Medical Toxicology and Adverse Drug Experience'', 2(6), 411-429. PMID: 8306565</ref> however care is primarily supportive in nature.
Symptoms of a benzodiazepine overdose may include severe [[thought deceleration]], [[language suppression|slurred speech]], [[confusion]], [[delusions]], [[respiratory depression]], coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with [[flumazenil]], a GABA<sub>A</sub> antagonist,<ref>{{cite journal | vauthors=((Hoffman, E. J.)), ((Warren, E. W.)) | journal=Clinical Pharmacy | title=Flumazenil: a benzodiazepine antagonist | volume=12 | issue=9 | pages=641–656; quiz 699–701 | date= September 1993 | issn=0278-2677}}</ref> however care is primarily supportive in nature.
===Dangerous interactions===
===Dangerous interactions===
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.
*'''[[Depressants]]''' (''[[1,4-Butanediol]], [[2-methyl-2-butanol]], [[alcohol]], [[barbiturates]], [[GHB]]/[[GBL]], [[methaqualone]], [[opioids]]'') - This combination can result in dangerous or even fatal levels of [[respiratory depression]]. These substances potentiate the [[muscle relaxation]], [[sedation]] and [[amnesia]] caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.
*'''[[Depressants]]''' (''[[1,4-Butanediol]], [[2-methyl-2-butanol]], [[alcohol]], [[barbiturates]], [[GHB]]/[[GBL]], [[methaqualone]], [[opioids]]'') - This combination can result in dangerous or even fatal levels of [[respiratory depression]]. These substances potentiate the [[muscle relaxation]], [[sedation]] and [[amnesia]] caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.
*'''[[Dissociatives]]''' - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.
*'''[[Dissociatives]]''' - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.
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==Legal status==
==Legal status==
{{legalStub}}
{{legalStub}}
*'''Canada''': All benzodiazepines are listed in Schedule IV.<ref>http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-15.html#h-34</ref>
*'''Canada''': All benzodiazepines are listed in Schedule IV.<ref>{{Citation | vauthors=((Branch, L. S.)) | year=2022 | title=Consolidated federal laws of Canada, Controlled Drugs and Substances Act | url=https://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-15.html}}</ref>
*'''Germany''': Diclazepam is controlled under Anlage II BtMG (''Narcotics Act, Schedule II'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html|title=Anlage II BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> as of November 21, 2015.<ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl115s1992.pdf|title=Dreißigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|work=Bundesgesetzblatt Jahrgang 2015 Teil I. Nr. 45|publication-date=November 20, 2015|access-date=December 29, 2019|language=de}}</ref> It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/__29.html|title=§ 29 BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref>
*'''Germany''': Diclazepam is controlled under Anlage II BtMG (''Narcotics Act, Schedule II'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html|title=Anlage II BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> as of November 21, 2015.<ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl115s1992.pdf|title=Dreißigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|work=Bundesgesetzblatt Jahrgang 2015 Teil I. Nr. 45|publication-date=November 20, 2015|access-date=December 29, 2019|language=de}}</ref> It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/__29.html|title=§ 29 BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref>
*'''Russia''': Diclazepam is a Schedule III controlled substance since 2017.<ref>Постановление Правительства РФ от 12.07.2017 N 827 | https://www.consultant.ru/cons/cgi/online.cgi?req=doc&base=LAW&n=220067&dst=1000000001&date=02.12.2019</ref>
*'''Poland''': Diclazepam is under the IV-P group as of January 27, 2022.<ref>{{cite web |url=https://dziennikustaw.gov.pl/DU/rok/2022/pozycja/274 |title=Rozporządzenie Ministra Zdrowia z dnia 27 stycznia 2022 r. zmieniające rozporządzenie w sprawie wykazu substancji psychotropowych, środków odurzających oraz nowych substancji psychoaktywnych |language=Polish |work=DZIENNIK USTAW 2022 R. POZ. 274274 |date=2022-02-04 |deadurl=no |archiveurl=https://web.archive.org/web/20220507135441/https://dziennikustaw.gov.pl/DU/rok/2022/pozycja/274 |archivedate=2022-05-07 }}</ref> It is illegal to own, possess, and sell in Poland.<ref>{{cite web |url=https://dziennikustaw.gov.pl/DU/2022/274/D2022000027401.pdf |format=PDF |title=Rozporządzenie Ministra Zdrowia z dnia 27 stycznia 2022 r. zmieniające rozporządzenie w sprawie wykazu substancji psychotropowych, środków odurzających oraz nowych substancji psychoaktywnych |language=Polish |work=DZIENNIK USTAW 2022 R. POZ. 274274 |date=2022-02-04 }}</ref>
*'''Russia''': Diclazepam is a Schedule III controlled substance since 2017.<ref>{{Citation | title=Постановление Правительства РФ от 12.07.2017 N 827 “О внесении изменений в некоторые акты Правительства Российской Федерации в связи с совершенствованием контроля за оборотом наркотических средств и психотропных веществ” - КонсультантПлюс | url=https://www.consultant.ru/cons/cgi/online.cgi?req=doc&base=LAW&n=220067&dst=1000000001&date=02.12.2019}}</ref>
*'''Switzerland''': Diclazepam is a controlled substance specifically named under Verzeichnis E.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref>
*'''Switzerland''': Diclazepam is a controlled substance specifically named under Verzeichnis E.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref>
*'''United Kingdom''': Diclazepam is a Class C controlled substance as of May 31, 2017. It is illegal to possess, produce or supply it.<ref>The Misuse of Drugs Act 1971 (Amendment) Order 2017 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2017/634/made</ref>
*'''Turkey:''' Diclazepam is a classed as drug and is illegal to possess, produce, supply, or import.<ref name="Bakanlar Kurulu Kararı - Karar Sayısı : 2016/9712">https://resmigazete.gov.tr/eskiler/2017/01/20170112-8.pdf</ref>
*'''United States''': Diclazepam is unregulated in the United States.{{citation needed}}
*'''United Kingdom''': Diclazepam is a Class C controlled substance as of May 31, 2017. It is illegal to possess, produce or supply it.<ref>{{Citation | title=The Misuse of Drugs Act 1971 (Amendment) Order 2017 | url=https://www.legislation.gov.uk/uksi/2017/634/made}}</ref>
*'''United States''': Diclazepam is a Schedule I controlled substance as of January 23, 2023.<ref>Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I | https://www.federalregister.gov/documents/2022/12/23/2022-27278/schedules-of-controlled-substances-temporary-placement-of-etizolam-flualprazolam-clonazolam</ref>
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Diclazepam (also known as chlorodiazepam) is a lesser-known novel depressant substance of the benzodiazepine class. It is a structural analog of diazepam (Valium) and is reported to produce similar effects.[2]
Diclazepam was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960.[3] Diclazepam is not currently marketed as a medication, but rather sold online as a research chemical.
It should be noted that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.[6] It is highly recommended to taper one's dose by gradually lowering the amount taken each day over a prolonged period of time rather than stopping use abruptly, as this can lead to severe, potentially life-threatening withdrawal symptoms.[7]
Diclazepam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven-membered ring with the two nitrogen constituents located at R1 and R4. At R1, diclazepam is substituted with methyl group. Further, the benzodiazepine ring is bonded at R5 to a 2-chlorinated phenyl ring. R7 of the benzyl ring is also substituted with a chlorine group. Diclazepam also contains an oxygen group double bonded to R2 of its diazepine ring to form a ketone. This oxygen substitution at R2 is shared with other benzodiazepine drugs with the suffix -azepam.
Pharmacology
Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors.[8] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of diclazepam on the nervous system.
Diclazepam has an approximate elimination half-life of 42 hours and undergoes N-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound.[9] Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzymes occurring concurrently with N-demethylation.
The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.[10]
Subjective effects
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
Paradoxical reactions to 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%).[11][12]
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[13][14]
Cognitive effects
The cognitive effects of diclazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of diclazepam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressants cognitive effects.
The most prominent of these cognitive effects generally include:
Emotion suppression - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of antipsychotics.
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.
Rebound anxiety - Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
Residual sleepiness - While benzodiazepines can be used as an effective sleep-inducing aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
Volumetric liquid dosing - If one's benzodiazepines 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 benzodiazepine volumetrically into a non-polar solution such as propylene glycol and dose it accurately based upon the methodological instructions linked within this tutorial.
Toxicity and harm potential
Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[16]
Diclazepam likely has a low toxicity relative to dose.[17] However, it is [[Toxicity::potentially lethal when mixed with depressants like alcohol or opioids]].
It is strongly recommended that one use harm reduction practices, such as volumetric dosing, when using this substance to ensure the accurate administration of the intended dose.
Tolerance and addiction potential
Diclazepam is extremely physically and psychologically addictive.
Tolerance will develop to the sedative-hypnotic effects within 3-4 days of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. However, in certain cases, this may take significantly longer in a manner which is proportional to the duration and intensity of one's long-term usage.
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. For more information on tapering from benzodiazepines in a controlled manner, please see this guide.
Benzodiazepine 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 hypertension, seizures, and death.[6] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.
Diclazepam presents cross-tolerance with [[Cross-tolerance::all GABAergics]], meaning that after its consumption all benzodiazepines will have a reduced effect.
Overdose
Benzodiazepine overdose may occur when a benzodiazepine is taken in extremely heavy quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work in a similar fashion, but bind to distinct allosteric sites on the GABAA receptor. Thus, their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABAA receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer[18]. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.
Symptoms of a benzodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABAA antagonist,[19] however care is primarily supportive in nature.
Dangerous interactions
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.
Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.
As such, it may contain incomplete or wrong information. You can help by expanding it.
Canada: All benzodiazepines are listed in Schedule IV.[20]
Germany: Diclazepam is controlled under Anlage II BtMG (Narcotics Act, Schedule II)[21] as of November 21, 2015.[22] It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.[23]
Poland: Diclazepam is under the IV-P group as of January 27, 2022.[24] It is illegal to own, possess, and sell in Poland.[25]
Russia: Diclazepam is a Schedule III controlled substance since 2017.[26]
Switzerland: Diclazepam is a controlled substance specifically named under Verzeichnis E.[27]
Turkey: Diclazepam is a classed as drug and is illegal to possess, produce, supply, or import.[28]
United Kingdom: Diclazepam is a Class C controlled substance as of May 31, 2017. It is illegal to possess, produce or supply it.[29]
United States: Diclazepam is a Schedule I controlled substance as of January 23, 2023.[30]
↑ 6.06.1Lann, M. A., Molina, D. K. (June 2009). "A fatal case of benzodiazepine withdrawal". The American Journal of Forensic Medicine and Pathology. 30 (2): 177–179. doi:10.1097/PAF.0b013e3181875aa0. ISSN1533-404X.
↑Bareggi, S. R., Truci, G., Leva, S., Zecca, L., Pirola, R., Smirne, S. (1988). "Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans". European Journal of Clinical Pharmacology. 34 (1): 109–112. doi:10.1007/BF01061430. ISSN0031-6970.
↑McLean, M. J., Macdonald, R. L. (February 1988). "Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture". The Journal of Pharmacology and Experimental Therapeutics. 244 (2): 789–795. ISSN0022-3565.
↑Saïas, T., Gallarda, T. (September 2008). "[Paradoxical aggressive reactions to benzodiazepine use: a review]". L’Encephale. 34 (4): 330–336. doi:10.1016/j.encep.2007.05.005. ISSN0013-7006.
↑Drummer, O. H. (February 2002). "Benzodiazepines - Effects on Human Performance and Behavior". Forensic Science Review. 14 (1–2): 1–14. ISSN1042-7201.
↑Goyal, S. (14 March 1970). "Drugs and dreams". Canadian Medical Association Journal. 102 (5): 524. ISSN0008-4409.
↑Mandrioli, R., Mercolini, L., Raggi, M. A. (October 2008). "Benzodiazepine metabolism: an analytical perspective". Current Drug Metabolism. 9 (8): 827–844. doi:10.2174/138920008786049258. ISSN1389-2002.
↑Hoffman, E. J., Warren, E. W. (September 1993). "Flumazenil: a benzodiazepine antagonist". Clinical Pharmacy. 12 (9): 641–656; quiz 699–701. ISSN0278-2677.
