|Summary sheet: Clonazolam|
|Common names||Clonazolam, Clonitrazolam|
|Systematic name||6-(2-chlorophenyl)-1-methyl-8-nitro-4H-s-triazolo- (4,3-a)-(1,4)-benzodiazepine|
|Routes of Administration|
Clonazolam (also known as Clonitrazolam) is a novel depressant substance of the benzodiazepine chemical class which produces anxiolytic, sedative, muscle relaxant, and amnesic effects when administered. This compound is a novel research chemical derivative of the FDA-approved drugs clonazepam (Klonopin, Rivitrol) and alprazolam (Xanax). Clonazolam is reported to be roughly 2.5x as potent as alprazolam.
The synthesis of clonazolam was first reported in 1971. It was described as the most active compound in the series tested. Clonazolam is reputed to be highly potent, and concerns have been raised that it and flubromazolam may pose comparatively higher risks than other designer benzodiazepines due to their ability to produce strong sedation and amnesia at oral doses as low as 0.5 mg, or 500 micrograms (ug). It is reported to have a medium-length onset of action (20 - 60 minutes).
Very little is known about this substance, but it has recently become easily accessible through online research chemical vendors where it is being sold as a designer drug. Due to its extremely high potency, it is often found on blotter paper or in volumetrically dosed solutions. Ingestion of raw clonazolam powder is unsafe due to its microgram-range potency and the ease in which it can lead to multi-day blackouts.
The sudden discontinuation of benzodiazepines can lead to life-threatening seizures or death for individuals who have been using them regularly, in heavy doses, or for extended periods of time. For this reason, it is recommended to discontinue use by tapering one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping one's usage abruptly.
Due to the high dependence-forming and addiction potential that this substance shares with other members of the benzodiazepine class, as well as its alcohol-like ability to induce dangerously disinhibited black-out states, it is strongly advised to use proper harm reduction practices if choosing to use this substance.
- 1 Chemistry
- 2 Pharmacology
- 3 Subjective effects
- 4 Common usage
- 5 Toxicity and harm potential
- 6 Legal status
- 7 See also
- 8 External links
- 9 References
Clonazolam 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. The benzyl ring of clonazolam is substituted at R8 with a nitro group, NO2-. Further, the diazepine ring is bonded at R6 to a 2-chlorinated phenyl ring.
Clonazolam also contains a 1-methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Clonazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam." Clonazolam is also a nitrobenzodiazepine, a subclass of benzodiazepines which contain a nitro (NO2-) group. Other nitrobenzodiazepines include clonazepam and flunitrazepam.
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. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of clonazelam on the nervous system.
Clonazolam is reported to be similar to alprazolam and other benzodiazepines that suppress emotions and produce moderate-strong feelings of relaxation, pleasure and comfort in the body. This seems to present itself more often in those with pre-existing anxiety. Many anecdotal reports from users of this compound have stated it as being one of the most euphoric benzodiazepines.
The cognitive effects of clonazolam are thought to be mainly amnesic, but also include most other typical effects seen with benzodiazepines. Clonazolam is reported to cause "blackouts" at a higher rate than other benzodiazepines.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Sedation - Clonazolam 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.
- Muscle relaxation - This effect is particularly strong when compared to other benzodiazepines such as alprazolam.
- Motor control loss
- Increased libido
- Respiratory depression
- 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%).
- Anxiety suppression
- Amnesia - Clonazolam is reported to cause "blackouts" at a higher rate than other benzodiazepines.
- Euphoria - A distinct portion of users report feeling a marked sense of emotional well-being and comfort while under the influence of this substance. Because this does not occur regularly or consistently for most users, it is speculated that this effect only manifests among those who have unusually high baseline levels of anxiety. However, people without anxiety issues also report clonazolam as being euphoric.
- Compulsive redosing
- 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.
- Memory suppression - Clonazolam primarily suppresses short-term memory, resulting in forgetfulness, and/or disorganized behaviors.
- Analysis suppression
- Motivation suppression - Due to clonazolam's heavy sedation and lethargy, doing any type of activity that requires moving, or high amounts of effort may be difficult to do on this compound, especially at higher doses.
- Thought deceleration
- Language suppression - Clonazolam & most benzodiazepines are known to cause slurred speech and difficulty communicating words in a clear fashion.
- Rebound anxiety - Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines and etizolam. 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.
- Dream potentiation or Dream suppression
- Residual sleepiness - While clonazolam can be used as an effective sleep-inducing aid, its effects may persist into the morning afterwards, which may lead users to feeling "groggy" or "dull" for up to a few hours.
- Thought deceleration
- Thought disorganization
- Motivation suppression
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
- 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. Clonazolam is especially important to weigh out and volumetrically dose properly due to it being active in the microgram range. To avoid adverse effects, one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the methodological instructions linked within this tutorial here.
Toxicity and harm potential
Tolerance and addiction potential
Clonazolam is generally considered to be extremely physically and psychologically addictive.
Tolerance will develop to the sedative-hypnotic effects within a couple of 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.
Clonazolam presents cross-tolerance with all benzodiazepines, meaning that after its consumption all benzodiazepines will have a reduced effect.
Discontinuation and withdrawal
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 high blood pressure, seizures, and death. Substances 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.
If one wishes to discontinue after a period of regular use, 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 benzodiazepine such as alprazolam or etizolam, a longer acting variety such as diazepam or clonazepam can be substituted. Symptoms may still be present, but their severity will be reduced significantly.
For more information on tapering from benzodiazepines in a controlled manner, please see this guide. Small quantities of alcohol can also help to reduce the symptoms, but otherwise cannot be used as an effective tapering agent.
The duration and severity of withdrawal symptoms depend on a number of factors including the half-life of the substance 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 benzodiazepines. Benzodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.
Benzodiazepine overdose may occur when a benzodiazepine is taken in extremely heavy quantities or concurrently with practically all 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, cross-potentiating each other.
For example, 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. This can result in dangerously disinhibited, total blackout states along with potential lethal respiratory depression.
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. A person might seem like they are sleepwalking, usually expressing vague emotions such as depression or aggressiveness. A person is also more susceptible to consume more of the same or other substance due to their impaired judgement, which is typically not seen with other psychoactive substances during overdose.
Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABAA antagonist or they may consist of additional procedures such as adrenaline injections if other substances are involved; however, care is primarily supportive in nature.
Although many psychoactive substances are safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The following lists some known dangerous combinations, but may not include all of them. A combination that appears to be safe in low doses can still increase the risk of injury or death. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from Tripsit.
- Depressants (1,4-Butanediol, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Stimulants - It can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.
- Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
This legality section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
- Canada: All benzodiazepines are schedule IV in Canada. 
- United Kingdom: Clonazolam is a class C drug in the UK as of 31st May 2017 and is illegal to possess, produce or supply. 
- Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines which have central nervous system depressant activity (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/5165540
- Triazolobenzazepines, process and intermediates for their preparation and medicines containing them | https://www.google.com/patents/EP0072029B1
- Designer benzodiazepines: A new challenge (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26043347
- Characterization of the four designer benzodiazepines clonazolam, deschloroetizolam, flubromazolam, and meclonazepam, and identification of their in vitro metabolites | http://link.springer.com/article/10.1007%2Fs11419-015-0277-6
- Identification of main human urinary metabolites of the designer nitrobenzodiazepines clonazolam, meclonazepam, and nifoxipam by nano-liquid chromatography-high-resolution mass spectrometry for drug testing purposes. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/27071765
- A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
- 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
- Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
- 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
- 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
- Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
- A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
- 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
- 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
- The Misuse of Drugs Act 1971 (Amendment) Order 2017 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2017/634/made