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Lorazepam

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Lorazepam
Chemical Nomenclature
Common names Lorazepam, Ativan, Orfidal, Lorsilan
Substitutive name Lorazepam
Systematic name (RS)-7-Chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-2H-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
Threshold 0.10 mg
Light 0.25 - 0.5 mg
Common 0.5 - 1.5 mg
Strong 1.5 - 2 mg
Heavy 2 - 3 mg +
Duration
Total 4 - 8 hours
Onset 5 - 30 minutes
Peak 1 - 3 hours
Offset 4 - 8 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

Lorazepam (trade name Ativan) is a intermediate-duration psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, anti-nausea and amnestic effects. Lorazepam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor. Lorazepam is used for the short-term treatment of anxiety, insomnia, acute seizures, and sedation of hospitalized patients.[1][2][3][4]

Chemistry

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory (or calming effects) of alprazolam on the nervous system.

Relative to other benzodiazepines, lorazepam is thought to have high affinity for GABA receptors, which may also explain its marked amnesic effects.[5] The anticonvulsant properties of lorazepam and other benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.[6]

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 Lorazepam can be broken down into 3 components all of which progressively intensify proportional to dosage. These are described below and generally include:

  • Sedation - In terms of energy level alterations, Lorazepam is 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.
  • Dizzness
  • Loss of motor control

Cognitive Effects

The cognitive effects of Lorazepam can be broken down into 6 components all of which progressively intensify proportional to dosage. The general head space of Lorazepam 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:

Toxicity and Harm Potential

Lethal dosage

The acute oral LD50 in mice is 1850 mg/kg.[7] As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

Tolerance and addition potential

Tolerance to benzodiazepine effects develops with regular use. This is desirable with amnesic and sedative effects, but undesirable with anxiolytic, hypnotic, and anticonvulsant effects. After four to six months of regular benzodiazepine use, evidence of continued efficacy declines. If regular treatment is continued for longer than this, dose increases may be necessary to maintain effects.

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.

  • International: The drug is a Schedule IV drug under the United Nations Convention on Psychotropic Substances.[8]
  • United States: Lorazepam is a Schedule IV drug under the Controlled Substances Act in the U.S.
  • Canada: It is a Schedule IV drug under the Controlled Drugs and Substances Act in Canada.
  • United Kingdom: It is a Class C, Schedule 4 Controlled Drug under the Misuse of Drugs Regulations 2001.[9]

See Also

References

  1. ↑ Benzodiazepines and their effects | http://www.benzo.org.uk/hindmarch.htm
  2. ↑ An Economic Evaluation of Propofol and Lorazepam for Critically Ill Patients Undergoing Mechanical Ventilation | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2763279/
  3. ↑ Status epilepticus: an evidence based guide | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1226249/
  4. ↑ Pharmacological Management of Acute Agitation | http://link.springer.com/article/10.2165%2F00003495-200565090-00003
  5. ↑ Benzodiazepine receptors mediate regional blood flow changes in the living human brain. | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC42301/
  6. ↑ Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. | http://www.ncbi.nlm.nih.gov/pubmed/2450203
  7. ↑ Material safety data sheet | http://www.drugbank.ca/system/msds/DB00186.pdf?1373674180
  8. ↑ List of psychotropic substances under international control | http://www.indiapost.gov.in/Pdf/Customs/List_of_Psychotropic_Substances.pdf
  9. ↑ 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
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