Ketamine

| Ketamine | |
|---|---|
| INN | |
| Drug class | NMDA receptor antagonist; general anesthetic; dissociative hallucinogen; analgesic; antidepressant |
| Routes of administration | Any<ref>,
Ketamine as an adjuvant to opioids for cancer pain, The Cochrane Database of Systematic Reviews, Vol. 6(Issue: 9), pp. CD003351, DOI: 10.1002/14651858.CD003351.pub3, PMID: 28657160, PMC: 6481583, Full text, Accessed on: 10 September 2018.</ref><ref>, Perioperative Ketamine Administration for Thoracotomy Pain, Pain Physician, Vol. 20(Issue: 3), pp. 173–184, PMID: 28339431,</ref><ref name="MathewZarate2016">, Ketamine for Treatment-Resistant Depression: The First Decade of Progress. online version, Springer, ISBN 978-3-319-42925-0, Pages: 8–10, 14–22,</ref><ref name="MD">
Ketamine Hydrochloride: Martindale: The Complete Drug Reference(link). MedicinesComplete. Pharmaceutical Press. 9 January 2017. London, UK. Accessed 24 August 2017.
|
| Pregnancy category | |
| Bioavailability | * Intravenous: 100%<ref name="MathewZarate2016" />
Toxicological Aspects of Drug-Facilitated Crimes. online version, Elsevier Science, ISBN 978-0-12-416969-2, Pages: 87–,</ref>
Ketamine: use in anesthesia, CNS Neurosci Ther, Vol. 19(Issue: 6), pp. 381–9, DOI: 10.1111/cns.12072, PMID: 23521979, PMC: 6493613,</ref>
Rapid-acting antidepressant ketamine, its metabolites and other candidates: A historical overview and future perspective, Psychiatry and Clinical Neurosciences, Vol. 73(Issue: 10), pp. 613–627, DOI: 10.1111/pcn.12902, PMID: 31215725, PMC: 6851782,</ref> |
| Metabolism | Liver, intestine (oral):
Contribution of CYP3A4, CYP2B6, and CYP2C9 isoforms to N-demethylation of ketamine in human liver microsomes, Drug Metabolism and Disposition, Vol. 30(Issue: 7), pp. 853–8, DOI: 10.1124/dmd.30.7.853, PMID: 12065445,</ref>
|
| Elimination half-life | * Ketamine: 2.5–3 hours
|
| Excretion | * Urine: 91%
|
| Legal status | In general Rx-only |
| CAS Number | 6740-88-1 |
| PubChem | 3821 |
| DrugBank | DB01221 |
| ChemSpider | 3689 |
| KEGG | D08098 |
Ketamine is a dissociative anesthetic. It is a type of drug that is commonly administered by physicians to induce anesthesia during surgery or medical procedures. Ketamine can also be used as a painkiller and as a bronchodilator, which facilitates easier airflow into the lungs.<ref>,
Pharmacology for Anaesthesia and Intensive Care (3rd edition), Cambridge:Cambridge University Press, 2008, ISBN 978-0-521-70463-2,</ref>
Occasionally, ketamine use can lead to a specific type of hallucination that produces feelings of detachment from one's body and surroundings.<ref>Bergman, S. A.,
Ketamine: Review of its Pharmacology and Its Use in Pediatric Anesthesia, Anesthesia Progress, 1999, Vol. 46(Issue: 1), pp. 10–20, PMID: 10551055, PMC: 2148883,</ref> This property has made it a popular recreational drug despite its potentially severe side effects. For this reason, ketamine is not typically available as an over-the-counter drug.
Medical Use
In clinical settings, ketamine is most commonly administered via injection into a vein (intravenous) or a muscle (intramuscular).<ref name="lankenau">Lankenau SE, Sanders B, Bloom JJ, et al.,
First Injection of Ketamine Among Young Injection Drug Users (IDUs) in Three U.S. Cities, Drug and Alcohol Dependence, Vol. 87(Issue: 2–3), pp. 183–93, DOI: 10.1016/j.drugalcdep.2006.08.015, PMID: 16979848, PMC: 1852477,</ref>
While ketamine is not the preferred anesthetic in many cases due to its hallucinogenic effects, it offers distinct advantages. Unlike most other anesthetics that suppress respiration and necessitate the use of mechanical ventilation, ketamine does not significantly inhibit breathing.<ref name="heshmati">Heshmati F, Zeinali MB, Noroozinia H, Abbacivash R, Mahoori A,
Use of Ketamine in Severe Status Asthmaticus in the Intensive Care Unit, Iranian Journal of Allergy, Asthma, and Immunology, Vol. 2(Issue: 4), pp. 175–80, PMID: 17301376,</ref>
Ketamine is particularly valuable in situations where advanced medical equipment is unavailable, such as in war zones or emergency field medicine. (December 2013)
Side Effects
Short-Term Side Effects
Short-term side effects are experienced by approximately 40% of individuals and include:<ref name="Quibell">Quibell R, Prommer EE, Mihalyo M, et al.,
"Ketamine*", Journal of Pain and Symptom Management, Vol. 41(Issue: 3), pp. 640–649, DOI: 10.1016/j.jpainsymman.2011.01.001, PMID: 21419322,</ref>
- Dizziness
- Double vision
- Euphoria
- Blurred vision
- Difficulty expressing emotions
- High blood pressure
- Tachycardia (Fast heart rate)
- Nausea and vomiting
- Speech difficulties
- Nightmares
- Illusions
- Hallucinations
- Altered body image
- Memory and attention impairments.
Long-Term Side Effects
Long-term effects of ketamine are mostly observed in recreational users or from prolonged exposure in animal studies.<ref name=morgan11>Morgan, Celia J. A.,
Ketamine Use: A Review, Addiction, Vol. 107(Issue: 1), pp. 27–38, DOI: 10.1111/j.1360-0443.2011.03576.x, PMID: 21777321,</ref>
Urinary Tract Effects
Chronic ketamine use has been associated with urinary tract issues, including:
- Increased urgency to urinate
- Pain during urination with hematuria (blood in urine)
- Reduced bladder capacity<ref name=middela>Middela, S.,
Ketamine-Induced Vesicopathy: A Literature Review, International Journal of Clinical Practice, Vol. 65(Issue: 1), pp. 27–30, DOI: 10.1111/j.1742-1241.2010.02502.x, PMID: 21155941,</ref>
Neurological Effects
Frequent recreational use (more than 4 times a week) has been linked to impaired cognitive functions, including memory deficits and increased depression.<ref name="Addiction Users Study">,
Consequences of Chronic Ketamine Self-Administration Upon Neurocognitive Function and Psychological Wellbeing: A 1-Year Longitudinal Study, Addiction, 2009, Vol. 105(Issue: 1), pp. 121–33, DOI: 10.1111/j.1360-0443.2009.02761.x, PMID: 19919593,</ref>
Mechanism of Action
Ketamine functions as an NMDA receptor antagonist in the central nervous system (CNS). By inhibiting these receptors, ketamine prevents excessive excitatory neurotransmission, resulting in an anesthetic effect. Additionally, it produces sympathomimetic effects that help maintain blood pressure and airway reflexes. These properties make it a critical option for patients with shock or requiring emergency surgery.
Research
Treating Addiction
Studies have explored ketamine's role in managing alcohol addiction and opioid use disorder.<ref>
The Combination of Psychedelic and Aversive Approaches in Alcoholism Treatment - Eleusis(link). {{{website}}}. Eleusis.
</ref>
Antidepressant Effects
Preliminary studies suggest that a single dose of ketamine can significantly alleviate symptoms of treatment-resistant depression within hours, with effects lasting up to a week.<ref>NIH: "Experimental Medication Kicks Depression in Hours Instead of Weeks"</ref>
Recreational Use
Recreational users typically consume ketamine at sub-anesthetic doses. The dissociative effects, often referred to as a "K-hole," include hallucinations and a profound sense of detachment.<ref>
What Is a K-Hole?(link). {{{website}}}. VICE.
</ref> Chronic use, however, may lead to serious consequences such as bladder damage, cognitive decline, and psychological dependence.<ref>Morgan CJ, Curran HV,
Acute and Chronic Effects of Ketamine Upon Human Memory: A Review, Psychopharmacology, 2006, Vol. 188(Issue: 4), pp. 408–24,</ref>
References
<references/>
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The following are antidepressant subclasses and drugs MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine SNRIs Duloxetine, Levomilnacipran, Venlafaxine SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone |
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Ketamine
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Ketamine 2D Structure
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S-Ketamine 3D Structure
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