Levomepromazine

Levomepromazine
Names
Trade namesNozinan, Levoprome, Detenler, Hirnamin, Levotomin, Neurocil, others
IUPAC name
  • (2R)-3-(2-Methoxyphenothiazine-10-yl-)-N,N,2-trimethylpropanamine
Clinical data
Drug classTypical antipsychotic
Main usesSchizophrenia, palliative care[1]
Side effectsLow blood pressure with standing, sleepiness, dry mouth, liver problems, dystonia[2][1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • Only if needed
Routes of
use		By mouth, IV, SC, IM[1]
Onset of action0.5 to 3 hr[2]
Duration of action8 hr[2]
External links
AHFS/Drugs.comInternational Drug Names
Legal
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
Pharmacokinetics
Bioavailability~50–60%
MetabolismLiver
Elimination half-life~20 hours
ExcretionIn feces and urine (metabolites), unchanged drug only 1%
Chemical and physical data
FormulaC19H24N2OS
Molar mass328.47 g·mol−1
3D model (JSmol)
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 checkY
  • Key:VRQVVMDWGGWHTJ-CQSZACIVSA-N checkY

Levomepromazine, also known as methotrimeprazine, is a medication used for schizophrenia and palliative care.[1] In palliative care it is used for restlessness, pain, and vomiting.[1] It may be used by mouth or by injection.[1] Effects generally begin around 0.5 to 3 hours and last for 8 hours.[2]

Side effects may include low blood pressure with standing, sleepiness, dry mouth, liver problems, and dystonia.[2][1] Serious side effect may include priapism, QT prolongation, and neuroleptic malignant syndrome.[2][1][3] It is an antipsychotic of the phenothiazine type.[2] It works by blocking a variety of receptors, including adrenergic, dopamine, histamine, muscarinic acetylcholine, and serotonin.[2]

Levomepromazine was patented in 1954 and come into medical use in the United State in 1957.[4] It is available as a generic medication.[1] In the United Kingdom 84 tablets of 25 mg costs the NHS about £20 as of 2020.[1] It has been widely used;[2] though is no longer commercially available in the United States.[5]

Medical uses

It is most commonly used in schizophrenia or palliative care.[1]

It can be used for moderate to severe pain in people who do not walk (this being because of its strong sedative effects).[6]

Levomepromazine is also used at lower doses for the treatment of nausea and insomnia.[7]

Levomepromazine is frequently prescribed and valued worldwide in palliative care medicine for its multimodal action, to treat intractable nausea or vomiting, and for 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.[7][8]

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.[7][8] A 2010 systematic review compared the efficacy of levomepromazine with atypical antipsychotic drugs:

Levomepromazine versus atypical antipsychotic drugs for schizophrenia[9]
Summary

Data are few and not high quality making it impossible to be confident about the effects for schizophrenia.[9]

Dosage

In schizophrenia the typical dose is 25 to 50 mg per day, though up to 1,000 mg per day may be used.[1]

It can be given once per day to three times per day.[2][1]

Side effects

The most common side effect is akathisia.[8] Levomepromazine has prominent sedative and anticholinergic/sympatholytic effects (dry mouth, hypotension, sinus tachycardia, night sweats) and may cause weight gain.[8] 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.[8] In any case, blood pressure and EKG should be monitored regularly.[8]

A rare but life-threatening side effect is neuroleptic malignant syndrome (NMS).[8] The symptoms of NMS include muscle stiffness, convulsions and fever.[8]

Pharmacology

It is a phenothiazine low-potency antipsychotic (approximately half as potent as chlorpromazine) with strong analgesic, hypnotic and antiemetic properties that are primarily used in palliative care.[7][8]

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 460. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  2. 1 2 3 4 5 6 7 8 9 10 Dietz, I; Schmitz, A; Lampey, I; Schulz, C (19 January 2013). "Evidence for the use of Levomepromazine for symptom control in the palliative care setting: a systematic review". BMC palliative care. 12: 2. doi:10.1186/1472-684X-12-2. PMID 23331515.
  3. ↑ "Levomepromazine Hydrochloride 25mg/ml Solution for Injection - Summary of Product Characteristics (SmPC) - (emc)". www.medicines.org.uk. Archived from the original on 28 August 2021. Retrieved 13 August 2021.
  4. ↑ Buschmann, Helmut; Holenz, Jörg; Párraga, Antonio; Torrens, Antoni; Vela, José Miguel; Díaz, José Luis (16 April 2007). Antidepressants, Antipsychotics, Anxiolytics, 2 Volume Set: From Chemistry and Pharmacology to Clinical Application. John Wiley & Sons. p. 502. ISBN 978-3-527-31058-6. Archived from the original on 28 August 2021. Retrieved 13 August 2021.
  5. ↑ "Drugs@FDA: FDA-Approved Drugs". www.accessdata.fda.gov. Archived from the original on 24 March 2021. Retrieved 13 August 2021.
  6. ↑ "Levomepromazine". Farmacotherapeutisch Kompas (in Nederlands). Archived from the original on 10 October 2016. Retrieved 5 October 2016.
  7. 1 2 3 4 Brayfield A, ed. (13 December 2013). "Levomepromazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Archived from the original on 28 August 2021. Retrieved 12 May 2014.
  8. 1 2 3 4 5 6 7 8 9 Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.
  9. 1 2 Sivaraman P, Rattehalli RD, Jayaram MB (October 2010). "Levomepromazine for schizophrenia". The Cochrane Database of Systematic Reviews. 10 (10): CD007779. doi:10.1002/14651858.CD007779.pub2. PMC 3283151. PMID 20927765.
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