Clonazepam - PsychonautWiki
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Fatal overdose may occur when benzodiazepines are combined with other depressants such as opiates, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Not to be confused with Clonazolam.
Summary sheet: Clonazepam
Clonazepam
Clonazepam.svg
Chemical Nomenclature
Common names Clonazepam, Klonopin, "K-Pins", Rivotril
Substitutive name Clonazepam
Systematic name 5-(2-Chlorophenyl)-7-nitro-2,3-dihydro-1,4-benzodiazepin-2-one
Class Membership
Psychoactive class Depressant
Chemical class Benzodiazepine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Bioavailability 90%[citation needed]
Threshold 0.10 mg
Light 0.25 - 0.5 mg
Common 0.5 - 1 mg
Strong 1 - 2 mg
Heavy 2 mg +
Duration
Total 8 - 12 hours
Onset 20 - 60 minutes
After effects 8 - 48 hours









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.

Interactions


Klonopin 0.5 mg.
Klonopin 1 mg

Clonazepam[2] (trade name Klonopin or Rivotril) is a long-acting psychoactive substance of the benzodiazepine class which produces anxiolytic, anticonvulsant, muscle relaxant, amnesic, sedative, depressant and hypnotic effects.[3] It is commonly used and FDA approved for the medical treatment of panic disorder, generalized anxiety disorder (GAD), and social anxiety disorder (SAD).

Clonazepam has an elimination half-life of 18 – 50 hours to 19 – 60 hours, and is generally considered to be a long-acting benzodiazepine. Clonazepam has an intermediate onset of action, with a peak blood level occurring one to four hours after oral administration.

It's worth noting that the sudden discontinuation of benzodiazepines can be potentially life-threatening for individuals using regularly for extended periods of time.[4] 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.[5]

Contents

Chemistry

Clonazepam 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 clonazepam is substituted at R8 with a nitro group, NO2-. Further, the diazepine ring is bonded at R5 to a 2-chlorinated phenyl ring. Clonazepam 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.[6] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of clonazepam 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.[7]

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated 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 are more likely to induce the full spectrum of effects. Likewise, adverse effects become much more likely with higher doses and may include serious injury or death.

Physical effects
 

Visual effects
 

Paradoxical effects
 

Cognitive effects
 

After effects
 

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

Additional experience reports can be found here:

Toxicity and harm potential

 
Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[13]

Clonazepam has a low toxicity relative to dose.[14] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

Clonazepam is 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.

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.[15] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Clonazopam presents cross-tolerance with all benzodiazepines, 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[16]. 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[17], however care is primarily supportive in nature.

Dangerous interactions

Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The list below includes some known dangerous combinations (although it cannot be guaranteed to include all of them). Independent research (e.g. Google, DuckDuckGo) 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.

  • 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.

Legal status

Internationally, clonazepam is included under the United Nations Convention on Psychotropic Substances in Schedule IV.[18]

  • Australia: Clonazepam is available by prescription only.[citation needed]
  • Brazil: Clonazepam is a "black stripe" drug, which are available by prescription only.[19]
  • Canada: Clonazepam is a Schedule IV drug.[citation needed]
  • Germany: Clonazepam is controlled under Anlage III BtMG (Narcotics Act, Schedule III) as of August 1, 1986.[20] It can only be prescribed on a narcotic prescription form, except preparations which contain up to 2 mg clonazepam in each dosage form and solutions that contain up to 0.25% and under 250 mg clonazepam in total per packaging unit.[21]
  • India: Clonazepam is Schedule H in India.[citation needed]
  • Israel: Clonazepam is available by prescription only.[citation needed]
  • Norway: Clonazepam is available by prescription only.[22]
  • Russia: Clonazepam is a Schedule III controlled substance as of April 2013.[23]
  • Switzerland: Clonazepam is a controlled substance specifically named under Verzeichnis B. Medicinal use is permitted.[24]
  • Turkey: Clonazepam is a 'green prescription' only substance[25] and illegal when sold or possessed without a prescription.[citation needed]
  • United Kingdom: Clonazepam is a Class C drug.[citation needed]
  • United States: Clonazepam is a Schedule IV substance.[citation needed]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. US Patent 3123529
  3. Ethyl beta-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in rats (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/6259533
  4. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  5. 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
  6. Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  7. 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
  8. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  9. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  10. Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
  11. Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
  12. Goyal, Sarita. "Drugs and Dreams." Indian Journal of Clinical Practice (n.d.): n. pag. Web. | http://medind.nic.in/iaa/t13/i3/iaat13i3p624.pdf
  13. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  14. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  15. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  16. Barbiturates and benzodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436
  17. Flumazenil, a benzodiazepine antagonist | https://www.ncbi.nlm.nih.gov/pubmed/8306565
  18. "List of Psychotropic Substances under International Control" (PDF). International Narcotics Control Board. Archived from the original (PDF) on December 19, 2013. Retrieved December 28, 2019. 
  19. Anvisa
  20. "Zweite Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften" (PDF) (in German). Bundesanzeiger Verlag. Retrieved December 26, 2019. 
  21. "Anlage III BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 26, 2019. 
  22. https://www.felleskatalogen.no/medisin/rivotril-roche-563568
  23. Постановление Правительства РФ от 04.02.2013 N 78 | https://www.consultant.ru/cons/cgi/online.cgi?req=doc&base=LAW&n=141744&dst=100005&date=02.12.2019
  24. "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020. 
  25. YEŞİL REÇETEYE TABİ İLAÇLAR | https://www.titck.gov.tr/storage/Archive/2019/contentFile/01.04.2019%20SKRS%20Ye%C5%9Fil%20Re%C3%A7eteli%20%C4%B0la%C3%A7lar%20Aktif%20SON%20-%20G%C3%9CNCEL_58b1ff4a-2e1c-4867-bad7-eec855d6162a.pdf