Clonazolam |
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Please be aware of the high incidence of deaths due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances. |
| Clonazolam | |||||||||||||||||||||||||||||
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| Molecular structure of Clonazolam | |||||||||||||||||||||||||||||
| Chemical Nomenclature | |||||||||||||||||||||||||||||
| Common names | Clonazolam, Clonitrazolam | ||||||||||||||||||||||||||||
| Systematic name | 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-s-triazolo- (4,3-a)-(1,4)-benzodiazepine | ||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||
| Psychoactive class | Depressant | ||||||||||||||||||||||||||||
| Chemical class | Benzodiazepine | ||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||
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| Summary sheet: Clonazolam |
Clonazolam (also known as Clonitrazolam) is a medium-duration psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, and amnesic effects. Clonazolam, like other benzodiazepines, binds to specific sites on the GABA receptor. Clonazolam is a novel research chemical derivative of the FDA-approved drugs clonazepam (Klonopin, Rivitrol) and alprazolam (Xanax).
Clonazolam has a fast onset of action and symptomatic relief. Subjective reports suggest the onset to be between 20 - 60 minutes.
Contents
Chemistry
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.
Pharmacology
Benzodiazepines produce their sedative effects by binding to one of the benzodiazepine sites on GABAA receptors, the most prolific inhibitory receptor within the body. This increases the conductivity of sodium through the receptor's trans-membrane channel. The GABA molecule and receptor system inhibits neuron firing throughout the nervous system, often manifesting as sedating, anxiolytic, and hyponotic effects.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
The physical effects of clonazolam can be broken down into several components which progressively intensify proportional to dosage.
These are described below and generally include:
- 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.
- Respiratory depression
- Dizziness
- Muscle relaxation
- Motor control loss
Cognitive effects
The cognitive effects of clonazolam can be broken down into several components which progressively intensify proportional to dosage. The general head space of clonazolam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.
The most prominent of these cognitive effects generally include:
- Amnesia
- Anxiety suppression
- Thought deceleration
- Disinhibition
- Information processing 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.
Paradoxical effects
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%).[1][2]These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[3][4]
Recipes and preparation methods
- 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 solution and dose it accurately based upon the methodological instructional guide linked here.
Toxicity and harm potential
Lethal dosage
The LD50 of clonazolam is unknown, but it is not unreasonable to presume that clonazolam, like other common benzodiazepines, is well tolerated. Benzodiazepines are not toxic by themselves. If adequate life support systems (including aspirators) are applied upon overdose, one has a good chance of recovery.
As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.
Tolerance and addiction potential
Tolerance will develop to the sedative-hypnotic effects within a couple of days.[5] 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.
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 seizure following discontinuation of benzodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.
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.
- 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 also 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.
- 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.
Legal issues
- United Kingdom: Clonazolam is not currently described in the Misuse of Drugs Act. As such, it is legal to sell or possess for analytical purposes. The distribution of clonazolam is legal when used for reasons other than human consumption.
Preparation methods
Preparation methods for this compound within our preparation index include:
See also
References
- ↑ 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
- ↑ Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535