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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および心理学的障害のマネージメント management of psychiatric and psychologic disorders in patients with cancer

English Journal

Antipsychotics and mortality in first-onset schizophrenia: prospective Finnish register study with 5-year follow-up.

Kiviniemi M, Suvisaari J, Koivumaa-Honkanen H, Häkkinen U, Isohanni M, Hakko H.SourceSocial and Mental Health Services, City of Oulu, Finland; University of Oulu, Institute of Clinical Medicine, Psychiatry, Oulu, Finland. Electronic address: marjo.kiviniemi@oulu.fi.
Schizophrenia research.Schizophr Res.2013 Oct;150(1):274-80. doi: 10.1016/j.schres.2013.07.043. Epub 2013 Aug 14.
OBJECTIVE: Our aim was to assess the impact of the most commonly used typical and atypical antipsychotics on mortality of patients with first-onset schizophrenia.METHOD: We conducted a nationwide, register-based, five-year follow-up study of all patients presenting with first-onset of schizophrenia
PMID 23953217

Quantification of typical antipsychotics in human plasma by ultra-high performance liquid chromatography tandem mass spectrometry for therapeutic drug monitoring.

Gradinaru J, Vullioud A, Eap CB, Ansermot N.SourceUnit of Pharmacogenetics and Clinical Psychopharmacology, Center for Psychiatric Neurosciences, Department of Psychiatry, Lausanne University Hospital, Hospital of Cery, 1008 Prilly-Lausanne, Switzerland.
Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2013 Aug 7;88C:36-44. doi: 10.1016/j.jpba.2013.07.041. [Epub ahead of print]
A selective and sensitive method was developed for the simultaneous quantification of seven typical antipsychotic drugs (cis-chlorprothixene, flupentixol, haloperidol, levomepromazine, pipamperone, promazine and zuclopenthixol) in human plasma. Ultra-high performance liquid chromatography (UHPLC) wa
PMID 24036032

Photooxidation Mechanism of Levomepromazine in Different Solvents.

Piñero-Santiago LE, García C, Lhiaubet-Vallet V, Trzcionka J, Oyola R, Torres K, Leguillú J, Miranda MA.SourceDepartment of Chemistry, University of Puerto Rico at Humacao, Humacao, PR; Instituto de Tecnología Química UPV-CSIC, Universitat Politècnica de València, Valencia, Spain.
Photochemistry and photobiology.Photochem Photobiol.2013 Aug 3. doi: 10.1111/php.12147. [Epub ahead of print]
Unwanted photoinduced responses are well-known adverse effects of most promazine drugs, including levomepromazine (LPZ, Levoprome® or Nozinan® ). This drug is indicated in psychiatry primarily for the treatment of schizophrenia and other schizoaffective disorders. Levomepromazine's particular seda
PMID 23909411

Japanese Journal

SNRI milnacipranの向精神薬との併用時の血中濃度および肝薬物代謝酵素cytochrome P-450による薬物相互作用についての考察

細井律子
精神科 16(6), 584-587, 2010-06
NAID 40017161384

Improvement in antipsychotic-induced hyperprolactinemia with the addition of aripiprazole in schizophrenic patients

Mihara Kazuo,Nagai Goyo,Nakamura Akifumi,Fukuji Yasuhide,Suzuki Takeshi,Kondo Tsuyoshi
Clinical Neuropsychopharmacology and Therapeutics 1(0), 1-5, 2010
… The authors investigated the effect of aripiprazole coadministration on antipsychotic-induced hyperprolactinemia and associated symptoms in patients with schizophrenia.Method: The subjects were 9 patients (8 females, 1 male) with hyperprolactinemia induced by risperidone, olanzapine, haloperidol, zotepine, bromperidol, levomepromazine, and quetiapine; …
NAID 130000405620

脳波・筋電図の臨床急性期統合失調症に対するペロスピロン単剤治療とレボメプロマジン併用治療での聴覚性事象関連電位の変化

長澤達也,東間正人,菊知充 [他]
臨床脳波 50(9), 547-552, 2008-09
NAID 40016227635

Related Pictures

★リンクテーブル★

リンク元	「フェノチアジン誘導体」「レボメプロマジン」「methotrimeprazine」
拡張検索	「levomepromazine maleate」「levomepromazine hydrochloride」

「フェノチアジン誘導体」

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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