WordNet

drug (trade name Lorfan) that is related to morphine but that counteracts the respiratory depression produced by morphine poisoning but without affecting its analgesic effects (同)Lorfan
a salt or ester of tartaric acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/04/07 19:51:14」(JST)

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Levallorphan (INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote.^[1]^[2]^[3] It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR),^[4] and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia.^[5]

Levallorphan was formerly widely used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia (via KOR agonism). It is now less commonly employed for this purpose as the newer drug naloxone tends to be used instead. Levallorphan was also used in combination with opioid analgesics to reduce their side effects, mainly in obstetrics, and a very small dose of levallorphan used alongside an full agonist of the MOR can produce greater analgesia than when the latter is used by itself.^[6] The combination of levallorphan with pethidine (meperidine) was indeed used so frequently, a standardized formulation was made available, known as Pethilorfan.^[7]

As an agonist of the KOR, levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams.^[8]^[9]^[10]

References

^ J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 731–. ISBN 978-1-4757-2085-3.
^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0.
^ I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 164–. ISBN 978-94-011-4439-1.
^ Goodman & Gilman. The Pharmacological Basis of Therapeutics (10th ed.). McGraw Hill Medical Publishing. p. 602. ISBN 978-0-07-135469-1.
^ Codd, E. E.; Shank, R. P.; Schupsky, J. J.; Raffa, R. B. (September 1995). "Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception". The Journal of Pharmacology and Experimental Therapeutics 274 (3): 1263–1270. PMID 7562497.
^ Bullough, J. (1959). "Use of premixed pethidine and antagonists in obstetrical analgesia; with special reference to cases in which levallorphan was used" (pdf). British Medical Journal 2 (5156): 859–862. doi:10.1136/bmj.2.5156.859. PMC 1990381. PMID 13805887.
^ Williams, G.; Cope, I. (1962). "An evaluation of a combination of pethidine and levallorphan ("pethilorfan") in labour". The Medical Journal of Australia 49 (2): 499–503. PMID 14000851.
^ R.C.W. Hall (6 December 2012). Psychiatric Presentations of Medical Illness: Somatopsychic Disorders. Springer Science & Business Media. pp. 364–. ISBN 978-94-011-7677-4.
^ American Hospital Formulary Service Drug Information. authority of the Board of Directors of the American Society of Hospital Pharmacists. 1984. p. 664.
^ John B. Williams (1963). Narcotics. Wm. C. Brown Company. p. 203.

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English Journal

Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format.

Xia M1, Guo V, Huang R, Shahane SA, Austin CP, Nirenberg M, Sharma SK.
Cellular and molecular neurobiology.Cell Mol Neurobiol.2011 Aug;31(6):901-7. doi: 10.1007/s10571-011-9689-y. Epub 2011 May 20.
Opiates are not only potent analgesics but also drugs of abuse mainly because they produce euphoria. Chronic use of opiates results in the development of tolerance and dependence. Dr Marshall Nirenberg's group at the National Institutes of Health (NIH) was the first to use a cellular model system of
PMID 21598037

Sensitive determination of pentazocine in human tissues by high-performance liquid chromatography.

Imamura T1, Kudo K, Namera A, Yashiki M, Kojima T.
Legal medicine (Tokyo, Japan).Leg Med (Tokyo).2000 Aug;2(2):119-22.
The authors developed a simple, reliable and sensitive method for the determination of pentazocine in human solid tissues using high-performance liquid chromatography, combined with a three-step liquid-liquid extraction procedure. Levallorphan tartrate served as the internal standard. The extract wa
PMID 12935455

Liquid chromatography-fast atom bombardment mass spectrometry for detection and determination of pentazocine in human tissues.

Imamura T1, Kudo K, Namera A, Tokunaga H, Yashiki M, Jitsufuchi N, Kojima T.
Journal of chromatography. B, Biomedical sciences and applications.J Chromatogr B Biomed Sci Appl.1999 Aug 6;731(1):149-54.
A reliable and sensitive method was developed for the detection and determination of pentazocine in human solid tissues using liquid chromatography-dynamic fast atom bombardment (FAB) mass spectrometry, combined with a three-step liquid-liquid extraction procedure. Levallorphan tartrate served as an
PMID 10492001

「レバロルファン」

Levallorphan
Systematic (IUPAC) name
	(−)-17-allylmorphinan-3-ol
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
Legal status	℞ (Prescription only);
Identifiers
CAS Number	152-02-3
ATC code	none
PubChem	CID 5359371
IUPHAR/BPS	7209
DrugBank	DB00504
ChemSpider	4514267
UNII	353613BU4U
ChEMBL	CHEMBL1254682
Chemical data
Formula	C19H25NO
Molar mass	283.4079 g/mol
	SMILES Oc1ccc3c(c1)[C@@]24[C@H]([C@H](N(CC2)C\C=C)C3)CCCC4 ;
	InChI InChI=1S/C19H25NO/c1-2-10-20-11-9-19-8-4-3-5-16(19)18(20)12-14-6-7-15(21)13-17(14)19/h2,6-7,13,16,18,21H,1,3-5,8-12H2/t16-,18-,19-/m0/s1 ; Key:OZYUPQUCAUTOBP-WDSOQIARSA-N ;
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