Levomepromazine

Levomepromazine
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • Only if clearly needed
Routes of
administration		 Oral, seldom IM
ATC code N05AA02 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
Pharmacokinetic data
Bioavailability ~50–60%
Metabolism Hepatic
Biological 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)
PubChem (CID) 72287
IUPHAR/BPS 7603
DrugBank DB01403 N
ChemSpider 65239 YesY
UNII 9G0LAW7ATQ YesY
KEGG D00403 YesY
ChEBI CHEBI:6838 N
ChEMBL CHEMBL1764 YesY
ECHA InfoCard 100.000.450
Chemical and physical data
Formula C19H24N2OS
Molar mass 328.47 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Levomepromazine (INN, BAN, USAN), also known as methotrimeprazine, is a phenothiazine neuroleptic drug. It is sold in many countries under the generic name (levomepromazine) or under brand names such as Nozinan, Levoprome, Detenler, Hirnamin, Levotomin, Neurocil and many more. 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, particularly those of schizophrenia, and manic phases of bipolar disorder. It should only be used with caution in the treatment of agitated depressions, as it can cause akathisia as a side effect, which could worsen the agitation.[1][2]

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).[3]

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 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

  1. 1 2 3 4 5 6 Brayfield, A, ed. (13 December 2013). "Levomepromazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 12 May 2014.
  2. 1 2 3 4 5 6 7 8 9 10 11 Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.
  3. ↑ "Levomepromazine". Farmacotherapeutisch Kompas (in Dutch). Retrieved 5 October 2016.
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