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Levomepromazine

From Wikipedia, the free encyclopedia
Typical antipsychotic medication
Pharmaceutical compound
Levomepromazine
Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy
category
  • Only if clearly needed
Routes of
administration		Oral, seldomIM
Drug classTypical antipsychotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability~50–60%
MetabolismHepatic
Eliminationhalf-life~20 hours
ExcretionIn feces and urine (metabolites), unchanged drug only 1%
Identifiers
  • (2R)-3-(2-Methoxyphenothiazine-10-yl-)-N,N,2-trimethylpropanamine
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.000.450Edit this at Wikidata
Chemical and physical data
FormulaC19H24N2OS
Molar mass328.47 g·mol−1
3D model (JSmol)
  • O(c2cc1N(c3c(Sc1cc2)cccc3)C[C@H](C)CN(C)C)C
  • 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 checkY
  • Key:VRQVVMDWGGWHTJ-CQSZACIVSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Levomepromazine, also known asmethotrimeprazine, is aphenothiazineneurolepticdrug. Brand names include Nozinan, Levoprome, Detenler, Hirnamin, Levotomin and Neurocil. It is a low-potency antipsychotic (approximately half as potent aschlorpromazine) with stronganalgesic,hypnotic andantiemetic properties that are primarily used inpalliative care.[2][3]

Serious side effects includetardive dyskinesia,akathisia,abnormalities in the electrical cycle of the heart,low blood pressure and the potentially fatalneuroleptic malignant syndrome.[2][3]

As is typical of phenothiazine antipsychotics, levomepromazine is a "dirty drug", that is, it exerts its effects byblocking a variety ofreceptors, includingadrenergic receptors,dopamine receptors,histamine receptors,muscarinic acetylcholine receptors andserotonin receptors.[2][3]

Medical uses

[edit]

It can be used as an analgesic for moderate to severe pain in non-ambulant patients (the latter being because of its strong sedative effects).[4]

Levomepromazine is also used at lower doses for the treatment ofnausea andinsomnia.[2]

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 opioid analgesics such as hydromorphone.[2][3]

Levomepromazine is used for the treatment ofpsychosis, particularly those ofschizophrenia, andmanic phases ofbipolar disorder. It should only be used with caution in the treatment ofagitated depressions, as it can causeakathisia as a side effect, which could worsen the agitation.[2][3] A 2010systematic review compared the efficacy of levomepromazine with atypical antipsychotic drugs:

Levomepromazine versus atypical antipsychotic drugs for schizophrenia[5]
Summary

Data are few and not high quality making it impossible to be confident about the effects for schizophrenia.[5]

OutcomeFindings in wordsFindings in numbersQuality of evidence
Global state
Not much improved (CGI)
Follow-up: short-term		Levomepromazine may increase the risk of not seeing an improvement when compared with atypical antipsychotic drugs, but, at present there are only very limited data supporting this finding.RR 2.33 (1.11 to 4.89)Very low
Mental state
Any response (<20% decreasePANSS
Follow-up: short-term		At present it is not possible to be confident about the difference between people given levomepromazine and those receiving atypical antipsychotic drugs. There is very limited data to support this finding.RR 2.5 (0.93 to 6.72)Very low
Adverse events
ConstipationLevomepromazine may slightly reduce the risk of constipation but there is no clear difference between people given levomepromazine and those receiving atypical antipsychotics. These findings are based on data of low quality.RR 0.45 (0.07 to 2.94)Low
DizzinessLevomepromazine may increase the chance of experiencing dizziness when compared with atypical antipsychotic drugs. Data are based on low quality evidence.RR 2.59 (1.23 to 5.46)Low
DrowsinessThere is no clear difference for the outcome of 'drowsiness' between people given levomepromazine and those receiving atypical antipsychotic drugs. These findings are based on data of low quality.RR 0.62 (0.29 to 1.32)Low
Dry mouthDry mouth is no more or less common with levomepromazine compared with those receiving atypical antipsychotic drugs. These findings are based on data of low quality.RR 0.93 (0.45 to 1.95)Low
Extrapyramidal symptoms - Needing antiparkinsonian medicationLevomepromazine may reduce the risk of movement disorders but, with current data, there is no clear difference between people given levomepromazine and those receiving atypical antipsychotic drugs. These findings are based on data of very limited quality.RR 0.6 (0.16 to 2.2)Very low

Adverse effects

[edit]

The most common side effect isakathisia.[3] Levomepromazine has prominentsedative andanticholinergic/sympatholytic effects (dry mouth,hypotension,sinus tachycardia, night sweats) and may cause weight gain.[3] These side effects normally preclude prescribing the drug in doses needed for fullremission of schizophrenia, so it has to be combined with a more potent antipsychotic.[3] In any case, blood pressure andEKG should be monitored regularly.[3]

A rare but life-threatening side effect isneuroleptic malignant syndrome (NMS).[3] The symptoms of NMS include muscle stiffness, convulsions and fever.[3]

History

[edit]

The drug (under the name Nozinan) started clinical trials in France in 1956 and was studied in Canada 3 years later.[6]

References

[edit]
  1. ^Anvisa (2023-03-31)."RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese).Diário Oficial da União (published 2023-04-04).Archived from the original on 2023-08-03. Retrieved2023-08-16.
  2. ^abcdefBrayfield A, ed. (13 December 2013)."Levomepromazine".Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved12 May 2014.
  3. ^abcdefghijkJoint Formulary Committee (2013).British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press.ISBN 978-0-85711-084-8.
  4. ^"Levomepromazine".Farmacotherapeutisch Kompas (in Dutch). Archived fromthe original on 5 March 2016. Retrieved5 October 2016.
  5. ^abSivaraman P, Rattehalli RD, Jayaram MB (October 2010)."Levomepromazine for schizophrenia".The Cochrane Database of Systematic Reviews.2010 (10) CD007779.doi:10.1002/14651858.CD007779.pub2.PMC 3283151.PMID 20927765.
  6. ^Huot JM, Kristof AC (October 1959)."Levomepromazine (nozinan)-a new neuroleptic agent for treatment of senile patients".Canadian Medical Association Journal.81 (7):546–548.PMC 1831284.PMID 14405490.

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