「ケタミン」の版間の差分

提供：脳科学辞典
ナビゲーションに移動 検索に移動
細編集の要約なし
細編集の要約なし
32行目: 32行目:
* [[Intravenous therapy|Intravenous]]: 100%<ref name="MathewZarate2016" />
* [[Intravenous therapy|Intravenous]]: 100%<ref name="MathewZarate2016" />
* [[Intramuscular injection|Intramuscular]]: 93%<ref name="MathewZarate2016" />
* [[Intramuscular injection|Intramuscular]]: 93%<ref name="MathewZarate2016" />
* [[Subcutaneous injection|Subcutaneous]]: high<ref name="Mao2016">'''Jianren Mao'''<br>Opioid-Induced Hyperalgesia <br>CRC Press, April 2016</ref>
* [[Subcutaneous injection|Subcutaneous]]: high<ref name="Mao2016">'''Jianren Mao. (2016).'''<br>Opioid-Induced Hyperalgesia <br>CRC Press</ref>
* [[Epidural administration|Epidural]]: 77%<ref name="Kintz2014">'''Pascal Kintz. (2014).'''<br>Toxicological Aspects of Drug-Facilitated Crimes<br>Elsevier Science</ref>
* [[Epidural administration|Epidural]]: 77%<ref name="Kintz2014">'''Pascal Kintz. (2014).'''<br>Toxicological Aspects of Drug-Facilitated Crimes<br>Elsevier Science</ref>
* [[Intranasal administration|Intranasal]]: 8–50%<ref name="MathewZarate2016" /><ref name="pmid29736744"><pubmed> 29736744</pubmed></ref><ref name="sinner"><pubmed> 18175098 </pubmed></ref>
* [[Intranasal administration|Intranasal]]: 8–50%<ref name="MathewZarate2016" /><ref name="pmid29736744"><pubmed> 29736744</pubmed></ref><ref name="sinner"><pubmed> 18175098 </pubmed></ref>
* [[Sublingual administration|Sublingual]]: 24–30%<ref name="MathewZarate2016" /><ref name="Hashimoto2019"><pubmed>31215725</pubmed></ref>
* [[Sublingual administration|Sublingual]]: 24–30%<ref name="MathewZarate2016" /><ref name="Hashimoto2019"><pubmed>31215725</pubmed></ref>
* [[Rectal administration|Rectal]]: 11–30%<ref name="Nemeroff2017">
* [[Rectal administration|Rectal]]: 11–30%<ref name="Nemeroff2017">
'''Alan F. Schatzberg, Charles B. Nemeroff. (2017)'''<br>The American Psychiatric Association Publishing Textbook of Psychopharmacology, Fifth Edition<br>American Psychiatric Pub, pp550-.</ref>
'''Alan F. Schatzberg & Charles B. Nemeroff. (2017).'''<br>The American Psychiatric Association Publishing Textbook of Psychopharmacology, Fifth Edition<br>American Psychiatric Pub, pp550-.</ref>
<ref name=Zhang2018><pubmed> 30513009</pubmed> </ref>
<ref name=Zhang2018><pubmed> 30513009</pubmed> </ref>
* [[Oral administration|By mouth]]: 16–29%<ref name="Kintz2014" /><ref name="DickmanSchneider2016">'''Andrew Dickman, Jennifer Schneider. (2016)'''<br>The Syringe Driver: Continuous Subcutaneous Infusions in Palliative Care<br>Oxford University Press, pp. 114-</ref><ref name=Zhang2018 />
* [[Oral administration|By mouth]]: 16–29%<ref name="Kintz2014" /><ref name="DickmanSchneider2016">'''Andrew Dickman & Jennifer Schneider. (2016).'''<br>The Syringe Driver: Continuous Subcutaneous Infusions in Palliative Care<br>Oxford University Press, pp. 114-</ref><ref name=Zhang2018 />
| protein_bound = 12–47% (low)<ref name="Kintz2014" /><ref name="sinner" /><ref name="DowdJohnson2016">'''Frank J. Dowd, Bart Johnson, Angelo Mariotti. (2016)'''<br>Pharmacology and Therapeutics for Dentistry – E-Book<br>Elsevier Health Sciences, pp235–</ref>
| protein_bound = 12–47% (low)<ref name="Kintz2014" /><ref name="sinner" /><ref name="DowdJohnson2016">'''Frank J. Dowd, Bart Johnson & Angelo Mariotti. (2016).'''<br>Pharmacology and Therapeutics for Dentistry – E-Book<br>Elsevier Health Sciences, pp235–</ref>
| metabolism = [[Liver]] ([[demethylation|''N''-demethylation]]):<ref name="MathewZarate2016" /><ref><pubmed>12065445</pubmed></ref>
| metabolism = [[Liver]] ([[demethylation|''N''-demethylation]]):<ref name="MathewZarate2016" /><ref><pubmed>12065445</pubmed></ref>
* Major: [[CYP3A4]]
* Major: [[CYP3A4]]
89行目: 89行目:
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 742
| ChEMBL = 742
| synonyms = CI-581; CL-369; CM-52372-2<ref name="MortonHall2012">'''I. K. Morton, Judith M. Hall. (2012)'''<br>Concise Dictionary of Pharmacological Agents: Properties and Synonyms<br>Springer Science & Business Media, pp159–</ref>
| synonyms = CI-581; CL-369; CM-52372-2<ref name="MortonHall2012">'''I.K. Morton, & Judith M. Hall. (2012).'''<br>Concise Dictionary of Pharmacological Agents: Properties and Synonyms<br>Springer Science & Business Media, pp159–</ref>


<!--Chemical data-->
<!--Chemical data-->

2020年7月9日 (木) 22:36時点における版

ケタミン
(S)-Ketamine ball-and-stick model
Systematic (IUPAC) name
(RS)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexanone
Clinical data
Trade names Ketalar, others
AHFS/Drugs.com monograph
Licence data US Daily Med:link
Pregnancy cat. B3 (AU) ? (US)
Legal status Controlled (S8) (AU) Schedule I (CA) ? (UK) Schedule III (US) ℞ Prescription only
Routes Any[1][2][3]
Pharmacokinetic data
Bioavailability * Intravenous: 100%[3]

[10]

Protein binding 12–47% (low)[5][7][12]
Metabolism Liver (N-demethylation):[3][13]
Half-life * Ketamine: 2.5–3 hours[7][3]
  • Norketamine: 12 hours[14]
Excretion * Urine: 91%[3]
Identifiers
CAS number 6740-88-1 YesY
ATC code N01AX03
PubChem CID 3821
IUPHAR ligand 4233
DrugBank DB01221
ChemSpider 3689 YesY
UNII 690G0D6V8H YesY
KEGG D08098 YesY
ChEBI CHEBI:6121 YesY
ChEMBL CHEMBL742 YesY
Synonyms CI-581; CL-369; CM-52372-2[15]
Chemical data
Formula C13H16ClNO 
Mol. mass 237.725
Physical data
Melt. point 258–261 °C (496–502 °F)
 YesY (what is this?)  (verify)
  1. ↑ Bell, R.F., Eccleston, C., & Kalso, E.A. (2017).
    Ketamine as an adjuvant to opioids for cancer pain. The Cochrane database of systematic reviews, 6, CD003351. [PubMed:28657160] [PMC] [WorldCat] [DOI]
  2. ↑ Moyse, D.W., Kaye, A.D., Diaz, J.H., Qadri, M.Y., Lindsay, D., & Pyati, S. (2017).
    Perioperative Ketamine Administration for Thoracotomy Pain. Pain physician, 20(3), 173-184. [PubMed:28339431] [WorldCat]
  3. ↑ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 3.8 Frohlich, J., & Van Horn, J.D. (2014).
    Reviewing the ketamine model for schizophrenia. Journal of psychopharmacology (Oxford, England), 28(4), 287-302. [PubMed:24257811] [PMC] [WorldCat] [DOI]
  4. ↑ Jianren Mao. (2016).
    Opioid-Induced Hyperalgesia
    CRC Press
  5. ↑ 5.0 5.1 5.2 Pascal Kintz. (2014).
    Toxicological Aspects of Drug-Facilitated Crimes
    Elsevier Science
  6. ↑ Molero, P., Ramos-Quiroga, J.A., Martin-Santos, R., Calvo-Sánchez, E., Gutiérrez-Rojas, L., & Meana, J.J. (2018).
    Antidepressant Efficacy and Tolerability of Ketamine and Esketamine: A Critical Review. CNS drugs, 32(5), 411-420. [PubMed:29736744] [WorldCat] [DOI]
  7. ↑ 7.0 7.1 7.2 Sinner, B., & Graf, B.M. (2008).
    Ketamine. Handbook of experimental pharmacology, (182), 313-33. [PubMed:18175098] [WorldCat] [DOI]
  8. ↑ Hashimoto, K. (2019).
    Rapid-acting antidepressant ketamine, its metabolites and other candidates: A historical overview and future perspective. Psychiatry and clinical neurosciences, 73(10), 613-627. [PubMed:31215725] [PMC] [WorldCat] [DOI]
  9. ↑ Alan F. Schatzberg & Charles B. Nemeroff. (2017).
    The American Psychiatric Association Publishing Textbook of Psychopharmacology, Fifth Edition
    American Psychiatric Pub, pp550-.
  10. ↑ 10.0 10.1 Zhang, K., & Hashimoto, K. (2019).
    An update on ketamine and its two enantiomers as rapid-acting antidepressants. Expert review of neurotherapeutics, 19(1), 83-92. [PubMed:30513009] [WorldCat] [DOI]
  11. ↑ Andrew Dickman & Jennifer Schneider. (2016).
    The Syringe Driver: Continuous Subcutaneous Infusions in Palliative Care
    Oxford University Press, pp. 114-
  12. ↑ Frank J. Dowd, Bart Johnson & Angelo Mariotti. (2016).
    Pharmacology and Therapeutics for Dentistry – E-Book
    Elsevier Health Sciences, pp235–
  13. ↑ Hijazi, Y., & Boulieu, R. (2002).
    Contribution of CYP3A4, CYP2B6, and CYP2C9 isoforms to N-demethylation of ketamine in human liver microsomes. Drug metabolism and disposition: the biological fate of chemicals, 30(7), 853-8. [PubMed:12065445] [WorldCat] [DOI]
  14. ↑ Quibell, R., Prommer, E.E., Mihalyo, M., Twycross, R., & Wilcock, A. (2011).
    Ketamine*. Journal of pain and symptom management, 41(3), 640-9. [PubMed:21419322] [WorldCat] [DOI]
  15. ↑ I.K. Morton, & Judith M. Hall. (2012).
    Concise Dictionary of Pharmacological Agents: Properties and Synonyms
    Springer Science & Business Media, pp159–
「https://bsd.neuroinf.jp/w/index.php?title=ケタミン&oldid=44089」から取得