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Diazepam

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Diazepam
Chemical Nomenclature
Common names Valium, Diastat, Mother's Little Helper, Apaurin
Substitutive name Diazepam
Systematic name 7-Chloro-1-methyl-5-phenyl-3H-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 1 mg
Light 2.5 - 5 mg
Common 5 - 15 mg
Strong 15 - 30 mg
Heavy 30 mg +
Duration
Total 4 - 8 hours
Onset 20 - 40 minutes
Peak 60 - 90 minutes
After effects 12 - 36 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
Depressants
Dissociatives
Stimulants

Diazepam, first marketed as Valium by Hoffmann-La Roche, is a benzodiazepine drug. It is commonly used to treat a wide range of conditions including anxiety, panic attacks, insomnia, seizures, muscle spasms, restless legs syndrome, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, opiate withdrawal syndrome, and Ménière's disease.

It may also be used before certain medical procedures (such as endoscopies) to reduce tension and anxiety and in some surgical procedures to induce amnesia. As an alternative, it may be used to hasten the onset of intravenous (IV) anaesthesia while reducing dose requirements or as the sole agent when IV anaesthesia is not available or is contraindicated.[1][2] It possesses anxiolytic, anticonvulsant, sedative, muscle relaxant, and amnestic properties. [3]

The pharmacological action of diazepam enhances the effect of the neurotransmitter GABA by binding to the benzodiazepine site on the GABAA receptor (via the constituent chlorine atom) leading to central nervous system depression.[4] Advantages of diazepam are a rapid onset of action[5] and high efficacy rates, which are important for managing acute seizures, anxiety attacks, and panic attacks. Benzodiazepines also have a relatively low toxicity in overdose.[6]

Diazepam is a core medicine in the World Health Organization's Essential Drugs List, the minimum medical needs for a basic health-care system.[7] Diazepam, first synthesized by Leo Sternbach,[8] has been one of the most frequently prescribed medications in the world since its launch in 1963.

Chemistry

This chemistry section is incomplete.

You can help by adding to it.

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.[9] As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of diazepam on the nervous system.

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 diazepam can be broken down into 5 components all of which progressively intensify proportional to dosage. These are described below and generally include:

  • Sedation - In terms of energy level alterations, diazepam is sedating and can result in an overwhelmingly lethargic state at appropriately high dosages. 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
  • Muscle relaxation - In comparison to Alprazolam (Xanax), diazepam has greater amounts of muscle relaxation.
  • Dizziness
  • Motor control loss

Cognitive Effects

The cognitive effects of diazepam can be broken down into 7 components all of which progressively intensify proportional to dosage. The general head space of diazepam 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 oral LD50 (lethal dose in 50% of the population) of diazepam is 720 mg/kg in mice and 1240 mg/kg in rats.[10] D. J. Greenblatt and colleagues reported in 1978 on two patients who had taken 500 and 2000 mg of diazepam, went into moderately deep comas, and were discharged within 48 hours without having experienced any important complications in spite of having high concentrations of diazepam and its metabolites esmethyldiazepam, oxazepam, and temazepam (according to samples taken in the hospital and as follow-up).[11]

Although not usually fatal when taken alone, a diazepam overdose is considered a medical emergency and generally requires the immediate attention of medical personnel. The antidote for an overdose of diazepam (or any other benzodiazepine) is flumazenil (Anexate). This drug is only used in cases with severe respiratory depression or cardiovascular complications. Because flumazenil is a short-acting drug and the effects of diazepam can last for days, several doses of flumazenil may be necessary. Artificial respiration and stabilization of cardiovascular functions may also be necessary.[12][13][14][15]

Overdoses of diazepam with alcohol, opiates and/or other depressants may be fatal.[16][17]

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days.[18] 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.[19] [20]

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 seizures following discontinuation of benzodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Diazepam is regulated in most countries as a prescription drug.

  • International: Diazepam is a schedule IV controlled drug under the Convention on Psychotropic Substances.[21]
  • UK: The drug is classified as a controlled drug and listed under Schedule IV, Part I (CD Benz POM) of the Misuse of Drugs Regulations 2001, allowing possession with a valid prescription. The Misuse of Drugs Act 1971 makes it illegal to possess the drug without a prescription and for such purposes it is classified as a Class C drug.[22]
  • Germany: Diazepam is classified as a prescription drug, or in high dosage, as a restricted drug (Betäubungsmittelgesetz, Anhang III).[23]

See also

References

  1. ↑ PubChem - Diazepam | http://pubchem.ncbi.nlm.nih.gov/compound/3016?from=summary#section=Top
  2. ↑ National Library of Medicine - Medical Subject Headings | http://www.nlm.nih.gov/cgi/mesh/2006/MB_cgi?mode=&term=Diazepam
  3. ↑ Benzodiazepine metabolism: an analytical perspective | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  4. ↑ Benzodiazepines in epilepsy: pharmacology and pharmacokinetics | http://www.ncbi.nlm.nih.gov/pubmed/18384456
  5. ↑ http://www.bjmp.org/content/benzodiazepines-revisited
  6. ↑ Benzodiazepine metabolism: an analytical perspective | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  7. ↑ WHO Model List (2005) | http://whqlibdoc.who.int/hq/2005/a87017_eng.pdf
  8. ↑ http://pubs.acs.org/doi/abs/10.1021/jo01069a069
  9. ↑ Benzodiazepine interactions with GABA receptors | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  10. ↑ http://www.drugs.com/diazepam.html
  11. ↑ Rapid recovery from massive diazepam overdose | http://www.ncbi.nlm.nih.gov/pubmed/357765
  12. ↑ http://www.inchem.org/documents/pims/pharm/pim181.htm
  13. ↑ http://www.drugs.com/diazepam.html
  14. ↑ Diazepam Injection | http://www.rxlist.com/diazepam-injection-drug/overdosage-contraindications.htm
  15. ↑ Barondes SH (2003). Better Than Prozac. New York: Oxford University Press. pp. 47–59. ISBN 0-19-515130-5.
  16. ↑ Barondes SH (2003). Better Than Prozac. New York: Oxford University Press. pp. 47–59. ISBN 0-19-515130-5.
  17. ↑ A survey of buprenorphine related deaths in Singapore | http://www.ncbi.nlm.nih.gov/pubmed/16879940
  18. ↑ Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535
  19. ↑ Clinical Pharmacology, Clinical Efficacy, and Behavioral Toxicity of Alprazolam: A Review of the Literature | http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00003.x/pdf
  20. ↑ The American Psychiatric Publishing Textbook of Substance Abuse Treatment | http://books.google.com/books?id=6wdJgejlQzYC&pg=PA222&hl=en#v=onepage&q&f=false
  21. ↑ International Narcotics Control Board (2003) | http://infoespai.org/wp-content/uploads/2014/12/green.pdf
  22. ↑ https://www.gov.uk/government/publications/controlled-drugs-list
  23. ↑ http://www.gesetze-im-internet.de/btmg_1981/anlage_iii_61.html
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