Levomepromazine

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Levomepromazine
Levomepromazine2DCSD.svg
Levomepromazine3DanJ.gif
Systematic (IUPAC) name
(2R)-3-(2-Methoxyphenothiazine-10-yl-)-N,N,2-trimethylpropanamine
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy cat. Only if clearly needed
Legal status Prescription Only (S4) (AU) POM (UK)
Routes Oral, seldom intramuscular
Pharmacokinetic data
Bioavailability approx. 50 to 60%
Metabolism Hepatic
Half-life ~ 20 hours
Excretion In feces and urine (metabolites), unchanged drug only 1%
Identifiers
CAS number 60-99-1 YesY
7104-38-3 (maleate),
1236-99-3 HCl)
ATC code N05AA02
PubChem CID 72287
DrugBank DB01403
ChemSpider 65239 YesY
UNII 9G0LAW7ATQ YesY
KEGG D00403 YesY
ChEBI CHEBI:6838 N
ChEMBL CHEMBL1764 YesY
Chemical data
Formula C19H24N2OS 
Mol. mass 328.47 g/mol
 N (what is this?)  (verify)

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's 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[edit]

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[edit]

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[edit]

  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. 
  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.  edit