Talk:Cinolazepam: Difference between revisions

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{{headerpanel|{{Approval}}{{DepressantOD|benzodiazepines}}}}

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| {{DepressantOD|benzodiazepines}}

| {{~~Approval~~}}

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[[File:Opugn4T.jpg|150px|thumbnail|Gerodorm (Cinolazepam) 40 mg tablets]]

{|

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~~| ''[[Cinolazepam/Summary|Summary sheet: Cinolazepam]]''~~

|}

'''Cinolazepam''' ('''Gerodorm''') is a a short-acting [[psychoactive]] drug of the [[Chemical class::benzodiazepine]] class which produces hypnotic, anxiolytic, sedative, muscle relaxant, [[anticonvulsant]], and amnesic effects. Due to its strong sedative properties, it is primarily used as an hypnotic.

'''Cinolazepam''' ('''Gerodorm''') is a short-acting [[psychoactive]] drug of the [[Chemical class::benzodiazepine]] class which produces hypnotic, anxiolytic, sedative, muscle relaxant, [[anticonvulsant]], and amnesic effects.<ref>A clinical and neurophysiological evaluation of clotiazepam, a new thienodiazepine derivative. | http://www.ncbi.nlm.nih.gov/pubmed/2885366</ref> Due to its strong sedative properties, it is primarily used as an hypnotic.<ref>Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. | http://www.ncbi.nlm.nih.gov/pubmed/2889679</ref>

Cinolazepam has an elimination half-life of approximately 9 hours, and is considered to be a short-acting benzodiazepine. It has a fast onset of action, with a peak blood level occurring 0.5 to 2 hours after oral administration.

Cinolazepam has an elimination half-life of approximately 9 hours, and is considered to be a short-acting benzodiazepine. It has a fast onset of action, with a peak blood level occurring 0.5 to 2 hours after oral administration.<ref>Drug bank | http://www.drugbank.ca/drugs/DB01594</ref>`

At heavy doses, Cinolazepam has been anecdotally reported<ref>https://drugs-forum.com/forum/showpost.php?p=1287037&postcount=2</ref> to produce atypical hallucinatory effects, like those of [[Zolpidem]] and [[Zopiclone]], although to a lighter extent.

=Legal ~~issues~~=

Cinolazepam is not approved for sale in the United States ~~or Canada~~.

==Chemistry==

[[Category:~~Approval~~]][[Category:Proofread]]

Cinolazepam 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.

==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 clonazelam 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>

==Subjective effects==

{{effects/base|

{{effects/physical|

*'''[[Effect::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.

*'''[[Effect::Respiratory depression]]'''

*'''[[Effect::Dizziness]]'''

*'''[[Effect::Muscle relaxation]]'''

*'''[[Effect::Motor control loss]]'''

}}

|{{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>

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>

}}

|{{effects/cognitive|

*'''[[Amnesia]]'''

*'''[[Disinhibition]]'''

*'''[[Dizziness]]'''

*'''[[Effect::Delusions|Delusions of sobriety]]'''

*'''[[Information processing suppression|Information processing suppression]]'''

*'''[[Motor control loss]]'''

*'''[[Muscle relaxation]]'''

*'''[[Physical euphoria]]'''

*'''[[Thought deceleration]]'''

*'''[[Seizure suppression]]'''

*'''[[Effect::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.

}}

===Experience reports===

There are currently {{#ask:[[Category:Cinolazepam]][[Category:Experience]] | format=count}} experience reports which describe the effects of this substance in our [[experience index]].

{{#ask: [[Category:Cinolazepam]][[Category:Experience]]|format=ul|Columns=1}}

==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>]]

Cinolazepam 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]]]].

It is strongly recommended that one use [[responsible use|harm reduction practices]] when using this substance.

===Tolerance and addiction potential===

Cinolazepam is [[Addiction potential::extremely physically and psychologically addictive]].

Tolerance will develop to the sedative-hypnotic effects [[Time to full tolerance::within a couple of days of continuous use]]. After cessation, the tolerance returns to baseline in [[Time to zero tolerance::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 [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.

Cinolazepam presents cross-tolerance with [[Cross-tolerance::all [[benzodiazepines]]]], meaning that after its consumption all benzodiazepines will have a reduced effect.

===Dangerous interactions===

==Legal status==

*'''Canada''' - Cinolazepam is not approved for sale{{citation needed|date=November 2020}}

*'''United Kingdom''' - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.<ref>Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted</ref>

*'''United States''' - Cinolazepam is not approved for sale{{citation needed|date=November 2020}}

==See also==

*[[Responsible use]]

*[[Psychoactive substance index]]

*[[Entactogens]]

*[[Alcohol]]

*[[Benzodiazepines]]

*[[Depressants]]

Preparation methods for this compound within our [[tutorial index]] include:

* [[Volumetric liquid dosing]]

==External links==

*[[wikipedia:Cinolazepam|Cinolazepam (Wikipedia)]]

*[https://isomerdesign.com/PiHKAL/explore.php?id=3060 Cinolazepam (TiHKAL / Isomer Design)]

==References==

[[Category:Psychoactive substance]]

[[Category:Proofread]]

@@ Line 1: / Line 1: @@
+{{headerpanel|{{Approval}}{{DepressantOD|benzodiazepines}}}}
+{{SummarySheet}}
-{|
-|-
-|-
-| {{DepressantOD|benzodiazepines}}
-| {{Approval}}
-|}
 {{SubstanceBox/Cinolazepam}}
 [[File:Opugn4T.jpg|150px|thumbnail|Gerodorm (Cinolazepam) 40 mg tablets]]
-{|
-|-
-|-
-| ''[[Cinolazepam/Summary|Summary sheet: Cinolazepam]]''
-|}
-'''Cinolazepam''' ('''Gerodorm''') is a a short-acting [[psychoactive]] drug of the [[Chemical class::benzodiazepine]] class which produces hypnotic, anxiolytic, sedative, muscle relaxant, [[anticonvulsant]], and amnesic effects. Due to its strong sedative properties, it is primarily used as an hypnotic.
+'''Cinolazepam''' ('''Gerodorm''') is a short-acting [[psychoactive]] drug of the [[Chemical class::benzodiazepine]] class which produces hypnotic, anxiolytic, sedative, muscle relaxant, [[anticonvulsant]], and amnesic effects.<ref>A clinical and neurophysiological evaluation of clotiazepam, a new thienodiazepine derivative. | http://www.ncbi.nlm.nih.gov/pubmed/2885366</ref> Due to its strong sedative properties, it is primarily used as an hypnotic.<ref>Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. | http://www.ncbi.nlm.nih.gov/pubmed/2889679</ref>
-Cinolazepam has an elimination half-life of approximately 9 hours, and is considered to be a short-acting benzodiazepine. It has a fast onset of action, with a peak blood level occurring 0.5 to 2 hours after oral administration.
+Cinolazepam has an elimination half-life of approximately 9 hours, and is considered to be a short-acting benzodiazepine. It has a fast onset of action, with a peak blood level occurring 0.5 to 2 hours after oral administration.<ref>Drug bank | http://www.drugbank.ca/drugs/DB01594</ref>`
 At heavy doses, Cinolazepam has been anecdotally reported<ref>https://drugs-forum.com/forum/showpost.php?p=1287037&postcount=2</ref> to produce atypical hallucinatory effects, like those of [[Zolpidem]] and [[Zopiclone]], although to a lighter extent.
-=Legal issues=
-Cinolazepam is not approved for sale in the United States or Canada.
+==Chemistry==
-[[Category:Approval]][[Category:Proofread]]
+{{chemistry}}
+Cinolazepam 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 R<sub>1</sub> and R<sub>4</sub>.
+==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 clonazelam 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>
+==Subjective effects==
+{{EffectStub}}
+{{Preamble/SubjectiveEffects}}
+{{effects/base|
+{{effects/physical|
+*'''[[Effect::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.
+*'''[[Effect::Respiratory depression]]'''
+*'''[[Effect::Dizziness]]'''
+*'''[[Effect::Muscle relaxation]]'''
+*'''[[Effect::Motor control loss]]'''
+}}
+|{{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>
+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>
+}}
+|{{effects/cognitive|
+*'''[[Amnesia]]'''
+*'''[[Disinhibition]]'''
+*'''[[Dizziness]]'''
+*'''[[Effect::Delusions|Delusions of sobriety]]'''
+*'''[[Information processing suppression|Information processing suppression]]'''
+*'''[[Motor control loss]]'''
+*'''[[Muscle relaxation]]'''
+*'''[[Physical euphoria]]'''
+*'''[[Thought deceleration]]'''
+*'''[[Seizure suppression]]'''
+*'''[[Effect::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.
+}}
+}}
+===Experience reports===
+There are currently {{#ask:[[Category:Cinolazepam]][[Category:Experience]] | format=count}} experience reports which describe the effects of this substance in our [[experience index]].
+{{#ask: [[Category:Cinolazepam]][[Category:Experience]]|format=ul|Columns=1}}
+==Toxicity and harm potential==
+{{toxicity}}
+[[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>]]
+{{Further|Research chemicals#Toxicity and harm potential}}
+Cinolazepam 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]]]].
+It is strongly recommended that one use [[responsible use|harm reduction practices]] when using this substance.
+===Tolerance and addiction potential===
+Cinolazepam is [[Addiction potential::extremely physically and psychologically addictive]].
+Tolerance will develop to the sedative-hypnotic effects [[Time to full tolerance::within a couple of days of continuous use]]. After cessation, the tolerance returns to baseline in [[Time to zero tolerance::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 [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.
+Cinolazepam presents cross-tolerance with [[Cross-tolerance::all [[benzodiazepines]]]], meaning that after its consumption all benzodiazepines will have a reduced effect.
+===Dangerous interactions===
+{{DangerousInteractions}}
+{{DangerousInteractions/Intro}}
+{{DangerousInteractions/Depressants}}
+==Legal status==
+{{legalStub}}
+*'''Canada''' - Cinolazepam is not approved for sale{{citation needed|date=November 2020}}
+*'''United Kingdom''' - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.<ref>Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted</ref>
+*'''United States''' - Cinolazepam is not approved for sale{{citation needed|date=November 2020}}
+==See also==
+*[[Responsible use]]
+*[[Psychoactive substance index]]
+*[[Entactogens]]
+*[[Alcohol]]
+*[[Benzodiazepines]]
+*[[Depressants]]
+Preparation methods for this compound within our [[tutorial index]] include:
+* [[Volumetric liquid dosing]]
+==External links==
+*[[wikipedia:Cinolazepam|Cinolazepam (Wikipedia)]]
+*[https://isomerdesign.com/PiHKAL/explore.php?id=3060 Cinolazepam (TiHKAL / Isomer Design)]
+==References==
+<references />
+[[Category:Psychoactive substance]]
+[[Category:Proofread]]