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Lorazepam: Difference between revisions
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| ''[[Lorazepam/Summary|Summary sheet: Lorazepam]]'' | | ''[[Lorazepam/Summary|Summary sheet: Lorazepam]]'' | ||
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'''Lorazepam''' (trade name '''Ativan''') is an intermediate-duration [[psychoactive]] | '''Lorazepam''' (trade name '''Ativan''') is an intermediate-duration [[psychoactive]] substance of the [[chemical class::benzodiazepine]] class which produces [[anxiolytic]], [[sedative]], [[hypnotic]], [[muscle relaxant]], [[anticonvulsant]], [[Nausea suppression|anti-nausea]], [[psychoactive class::depressant]] and [[amnestic]] effects. This compound is used for the short-term treatment of [[Anxiety|anxiety]], [[insomnia]], [[seizure|acute seizures]], and the sedation of hospitalized patients.<ref>Benzodiazepines and their effects | http://www.benzo.org.uk/hindmarch.htm</ref><ref>An Economic Evaluation of Propofol and Lorazepam for Critically Ill Patients Undergoing Mechanical Ventilation (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2763279/</ref><ref>Status epilepticus: an evidence based guide (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1226249/</ref><ref>Pharmacological Management of Acute Agitation | http://link.springer.com/article/10.2165%2F00003495-200565090-00003</ref> | ||
It's worth noting 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 for a prolonged period of time instead of stopping abruptly.<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's worth noting 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 for a prolonged period of time instead of stopping abruptly.<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> | ||
==Chemistry== | ==Chemistry== | ||
Lorazepam is a | Lorazepam is a substance 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>. Further, the benzodiazepine ring is bonded at R<sub>5</sub> to a 2-chlorinated phenyl ring. R<sub>7</sub> of the benzyl ring is also substituted with a chlorine group. Additionally, Lorazepam contains a hydroxy (OH-) group substituted at R<sub>3</sub>. It also contains an oxygen group double bonded to R<sub>2</sub> of its diazepine ring to form a ketone. This oxygen substitution at R<sub>2</sub> is shared with other benzodiazepine drugs with the suffix -azepam. | ||
==Pharmacology== | ==Pharmacology== | ||
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{{Preamble/SubjectiveEffects}} | {{Preamble/SubjectiveEffects}} | ||
===Physical effects=== | ===Physical effects=== | ||
*'''[[Effect::Sedation]]''' - In terms of energy level alterations, this | *'''[[Effect::Sedation]]''' - In terms of energy level alterations, this substance 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::Motor control loss]]''' | *'''[[Effect::Motor control loss]]''' | ||
*'''[[Effect::Muscle relaxation]] | *'''[[Effect::Muscle relaxation]] | ||
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Lorazepam 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]]]]. | Lorazepam 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 | It is strongly recommended that one use [[responsible substance use|harm reduction practices]] when using this drug. | ||
===Tolerance and addiction potential=== | ===Tolerance and addiction potential=== | ||
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==Legal issues== | ==Legal issues== | ||
*'''International:''' The | *'''International:''' The substance is a Schedule IV substance under the United Nations Convention on Psychotropic Substances.<ref>List of psychotropic substances under international control | http://www.indiapost.gov.in/Pdf/Customs/List_of_Psychotropic_Substances.pdf</ref> | ||
*'''United States:''' Lorazepam is a Schedule IV | *'''United States:''' Lorazepam is a Schedule IV substance under the Controlled Substances Act in the U.S. | ||
*'''Canada:''' It is a Schedule IV | *'''Canada:''' It is a Schedule IV substance under the Controlled Drugs and Substances Act in Canada. | ||
*'''United Kingdom:''' It is a Class C, Schedule 4 controlled | *'''United Kingdom:''' It is a Class C, Schedule 4 controlled substance under the Misuse of Drugs Regulations 2001.<ref>List of drugs currently controlled under | ||
the misuse of drugs legislation| https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/164222/controlled-drugs-list.pdf</ref> | the misuse of drugs legislation| https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/164222/controlled-drugs-list.pdf</ref> | ||
*'''Germany:''' Preparations containing more than 2.5 mg are controlled under Anlage 3 of the BtMG and require a prescription. | *'''Germany:''' Preparations containing more than 2.5 mg are controlled under Anlage 3 of the BtMG and require a prescription. | ||