関: levomepromazine

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/05 08:42:47」(JST)

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Levomepromazine (INN, BAN, USAN), also known as methotrimeprazine (common use in America; sold as Nosinan, Nozinan, Levoprome) is an phenothiazine neuroleptic drug. It is a low-potency antipsychotic (approximately half as potent as chlorpromazine) with strong analgesic, hypnotic and antiemetic properties that is primarily used in palliative care.^[1]^[2]

Serious side effects include tardive dyskinesia, akathisia, abnormalities in the electrical cycle of the heart, low blood pressure and the potentially fatal neuroleptic malignant syndrome.^[1]^[2]

As is typical of phenothiazine antipsychotics, levomepromazine is a "dirty drug", that is, it exerts its effects by blocking a variety of receptors, including adrenergic receptors, dopamine receptors, histamine receptors, muscarinic acetylcholine receptors and serotonin receptors.^[1]^[2]

Medical uses

Levomepromazine is used for the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder. It should be used only with caution in the treatment of agitated depressions, as it can cause akathisia as a side effect, which could worsen the agitation.^[1]^[2]

Levomepromazine is also used at lower doses for the treatment of nausea and insomnia.^[1]

Levomepromazine is frequently prescribed and valued worldwide in palliative care medicine for its multimodal action, to treat intractable nausea or vomiting, and for severe delirium/ agitation in the last days of life. Palliative care physicians will commonly prescribe it orally or via subcutaneous syringe drivers in combination with more potent opiate analgesics such as Hydromorphone.^[1]^[2]

Adverse effects

The most common side effect is akathisia.^[2] Levomepromazine has prominent sedative and anticholinergic/sympatholytic effects (dry mouth, hypotension, sinus tachycardia, night sweats) and may cause weight gain.^[2] These side effects normally preclude prescribing the drug in doses needed for full remission of schizophrenia, so it has to be combined with a more potent antipsychotic.^[2] In any case, blood pressure and EKG should be monitored regularly.^[2]

A rare but life-threatening side effect is neuroleptic malignant syndrome (NMS).^[2] The symptoms of NMS include muscle stiffness, convulsions and fever.^[2]

References

^ ^a ^b ^c ^d ^e ^f Brayfield, A, ed. (13 December 2013). "Levomepromazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 12 May 2014.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.

PubChem Substance Summary: Levomepromazine National Center for Biotechnology Information.
NOZINAN - Lévomépromazine Doctissimo Guides des Medicaments
[1]Grampians Palliative Care Team Publication May 2010 (Victoria, Australia)
[2] Palliative Care Guidelines, Scotland, UK

UpToDate Contents

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1. 苦痛緩和のための鎮静 palliative sedation
2. 癌患者における精神学的障害のマネージメント management of psychiatric disorders in patients with cancer
3. 緩和ケア：評価および吐気、嘔吐の管理 palliative care assessment and management of nausea and vomiting
4. 緩和ケア：末期腎不全 palliative care end stage renal disease

English Journal

Autophagy induction enhances TDP43 turnover and survival in neuronal ALS models.

Barmada SJ1, Serio A2, Arjun A3, Bilican B4, Daub A3, Ando DM5, Tsvetkov A6, Pleiss M7, Li X8, Peisach D8, Shaw C9, Chandran S4, Finkbeiner S10.
Nature chemical biology.Nat Chem Biol.2014 Aug;10(8):677-85. doi: 10.1038/nchembio.1563. Epub 2014 Jun 29.
Amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) have distinct clinical features but a common pathology--cytoplasmic inclusions rich in transactive response element DNA-binding protein of 43 kDa (TDP43). Rare TDP43 mutations cause ALS or FTD, but abnormal TDP43 levels and locali
PMID 24974230

The cytochrome P450-catalyzed metabolism of levomepromazine: a phenothiazine neuroleptic with a wide spectrum of clinical application.

Wójcikowski J1, Basińska A2, Daniel WA2.
Biochemical pharmacology.Biochem Pharmacol.2014 Jul 15;90(2):188-95. doi: 10.1016/j.bcp.2014.05.005. Epub 2014 May 16.
The aim of the present study was to identify cytochrome P450 isoenzymes (CYPs) involved in the 5-sulfoxidation and N-demethylation of the aliphatic-type phenothiazine neuroleptic levomepromazine in human liver. Experiments were performed in vitro using cDNA-expressed human CYP isoforms (Supersomes 1
PMID 24841887

Practice and documentation of palliative sedation: a quality improvement initiative.

McKinnon M1, Azevedo C2, Bush SH3, Lawlor P3, Pereira J3.
Current oncology (Toronto, Ont.).Curr Oncol.2014 Apr;21(2):100-3. doi: 10.3747/co.21.1773.
BACKGROUND: Palliative sedation (ps), the continuous use of sedating doses of medication to intentionally reduce consciousness and relieve refractory symptoms at end of life, is ethically acceptable if administered according to standards of best practice. Procedural guidelines outlining the appropri
PMID 24764700

Japanese Journal

ヘッドスペース固相ミクロ抽出/ガスクロマトグラフィーによるフェノチアジン系薬物の検出

Seno Hiroshi,Kumazawa Takeshi,Ishii Akira,Nishikawa Masanobu,Watanabe Kanako,Hattori Hideki,Suzuki Osamu
1996-01-31
… Phenothiazine drugs, such as promazine, chlorpromazine, triflupromazine, trimeprazine and methotrimeprazine, have been found extractable from whole blood and urine by headspace solid phase microextraction (SPME). …
NAID 120005314019

フェノチアジン系薬剤急性中毒２例における血中濃度動態

小山和弘,菊野隆明,猪芳亮,市来嵜潔,村越功治,城川裕美,石井漱一
医療 50(11), 772-775, 1996
フェノチアジン系薬物急性中毒2例に対してHPLCにより血中濃度を測定した.症例1: 69歳女性, レボメプロマジンを推定3000mg服用し, 服用から約17時間後に昏睡状態で入院した. レボメプロマジン血中濃度が2018ng/mlあり, 入院後心停止状態になった. 蘇生後血液吸着を行い血中濃度が35ng/mlまで低下したが症状の改善はなかった.症例2: 58歳女性, チオリダジンを推定1000mg …
NAID 130004315346

The use of etorphine/methotrimeprazine and midazolam as an anaesthetic technique in laboratory rats and mice

WHELAN G.
Lab Anim 28, 70-77, 1994
NAID 30027887082

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リンク元	「メトトリメプラジン」

「メトトリメプラジン」

Levomepromazine
Systematic (IUPAC) name
	(2R)-3-(2-Methoxyphenothiazine-10-yl-)-N,N,2-trimethylpropanamine
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	Only if clearly needed;
Legal status	AU: Prescription Only (S4); UK: Prescription-only (POM);
Routes of; administration	Oral, seldom intramuscular
Pharmacokinetic data
Bioavailability	approx. 50 to 60%
Metabolism	Hepatic
Biological half-life	~ 20 hours
Excretion	In feces and urine (metabolites), unchanged drug only 1%
Identifiers
CAS Registry Number	60-99-1 ; 7104-38-3 (maleate),; 1236-99-3 HCl)
ATC code	N05AA02
PubChem	CID: 72287
IUPHAR/BPS	7603
DrugBank	DB01403
ChemSpider	65239
UNII	9G0LAW7ATQ
KEGG	D00403
ChEBI	CHEBI:6838
ChEMBL	CHEMBL1764
Chemical data
Formula	C19H24N2OS
Molecular mass	328.47 g/mol
	SMILES O(c2cc1N(c3c(Sc1cc2)cccc3)C[C@H](C)CN(C)C)C ;
	InChI InChI=1S/C19H24N2OS/c1-14(12-20(2)3)13-21-16-7-5-6-8-18(16)23-19-10-9-15(22-4)11-17(19)21/h5-11,14H,12-13H2,1-4H3/t14-/m1/s1 ; Key:VRQVVMDWGGWHTJ-CQSZACIVSA-N ;
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英: methotrimeprazine
関: レボメプロマジン

[MD-1] ^ ^a ^b ^c ^d ^e ^f Brayfield, A, ed. (13 December 2013). "Levomepromazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 12 May 2014.

[BNF-2] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.

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methotrimeprazine