Last update 04 Nov 2024

Levomepromazine

Last update 04 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(-)-(2R)-3-(2-methoxy-10H-phenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine, (-)-10-(3-(Dimethylamino)-2-methylpropyl)-2-methoxyphenothiazine, 2-Methoxytrimeprazine

+ [21]

Target

adrenergic receptor

Mechanism

adrenergic receptor antagonists(Adrenergic receptors antagonists)

Therapeutic Areas

Other Diseases

Active Indication

Bipolar DisorderDepressive DisorderSchizophrenia

Inactive Indication

Behavioural disorders

Originator Organization

Sanofi-Aventis Participations SAS

Active Organization

Kyowa Pharmaceutical Industry Co., Ltd.

Mitsubishi Tanabe Pharma Corp.

Inactive Organization

Immunex Corp.

Drug Highest PhaseApproved

First Approval Date

JP (27 May 1960),

Bipolar DisorderDepressive DisorderSchizophrenia

Regulation-

Structure

Molecular FormulaC19H25ClN2OS

InChIKeyODLGFPIWRAEFAN-PFEQFJNWSA-N

CAS Registry1236-99-3

Clinical Trials associated with Levomepromazine

NCT02374567 / TerminatedPhase 3IIT

Pharmacovigilance in Gerontopsychiatric Patients

The purpose of this multicenter-study is to investigate safety of psychopharmacological treatment and rates of adverse drug reactions in gerontopsychiatric inpatients. Elderly people are at higher risk for developing side effects under pharmacological treatment due to an altered metabolic situation, higher comorbidity rates and often polypharmacy. Furthermore gerontopsychiatric patients can often not articulate their symptoms clearly, for example due to pronounced cognitive impairment.
The aim of the study is to gain valid data of possible adverse drug reaction rates, their potential risk factors and outcome, as well as medical prescription practises.
To assess these outcomes an intensive pharmacovigilance-monitoring will be conducted at the five participating study sites.
At Baseline demographic data, previous and present disorders, use of drugs, previous and present medication, quality of life, cognitive function, physical examination results, laboratory results and ECG will be assessed.
Afterwards patients are visited weekly and screened for possible adverse drug reactions. All adverse drug reactions will be coded in the MedDRA-system.
In case of a possible serious adverse drug reaction serum levels of all psychotropic substances applicated will be assessed. Drug combinations will be analysed using an established advanced bioinformatic tool (mediQ). Diagnosis, medication intake and possible adverse drug reactions are documented continually.
2 weeks after discharge from the ward, patients will be contacted by phone to assess catamnestic data.

Start Date01 Jan 2015

Sponsor / Collaborator

Hannover Medical School

NCT02582736 / CompletedNot ApplicableIIT

Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data

The purpose of this study is to determine whether the use of atypical antipsychotic medication increases the risk of hospitalization for a hyperglycemic emergency.
The investigators will carry out separate population-based cohort studies using administrative health databases in eight jurisdictions in Canada and the UK. Cohort entry will be defined by the initiation of a new antipsychotic medication. Follow-up will continue until hospitalization for a hyperglycemic emergency or the end of 365 days. The results from the separate sites will be combined to provide an overall assessment of the risk of hyperglycemic emergencies among new users of various antipsychotic drugs.

Start Date01 Apr 2012

Sponsor / Collaborator

Canadian Institutes of Health Research

NCT03019887 / CompletedNot ApplicableIIT

Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction in Patients Undergoing High-dose Antipsychotic Therapy

To reduce antipsychotics to under 1000mg in patients with schizophrenia taking more than 1000mg/day and to evaluate relationship between relapse and cognitive function.

Start Date01 Apr 2011

Sponsor / Collaborator

Juntendo University

100 Clinical Results associated with Levomepromazine

100 Translational Medicine associated with Levomepromazine

100 Patents (Medical) associated with Levomepromazine

745

Literatures (Medical) associated with Levomepromazine

01 Sep 2024·Legal Medicine

An autopsy case of intoxication caused by drug interaction with multiple psychotropic drugs, fluvoxamine, levomepromazine, and trihexyphenidyl

Article

Author: Yamashita, Tadayoshi ; Kinoshita, Hiroshi ; Murase, Takehiko ; Tanaka, Etsuko ; Takei, Sella ; Tsutsui, Kunihiko ; Jamal, Mostofa ; Abe, Hiroko ; Kawahara, Sachiko

A case of death due to combined use of multiple drugs is reported, and the pharmacokinetic interactions are discussed. A woman in her thirties was found dead in her home. A medico-legal autopsy found no findings suggestive of injury or natural disease. Toxicological analysis using liquid chromatography tandem mass spectrometry (LC-MS/MS) identified a toxic level of fluvoxamine (0.947 µg/mL), and concentrations greater than the therapeutic levels of levomepromazine (0.238 µg/mL) and trihexyphenidyl (0.225 µg/mL) were present, while bromazepam, haloperidol, sulpiride, and 7-aminoflunitrazepam were within or below their therapeutic ranges. Fluvoxamine is mainly metabolized by cytochrome P450 2D6 (CYP2D6), and levomepromazine is a potent CYP2D6 inhibitor. A high concentration of levomepromazine may increase the blood fluvoxamine level. Since the combined use of levomepromazine and fluvoxamine induces seizures, it may have been involved in causing the subject's death. In addition, combined use of trihexyphenidyl may potentiate anticholinergic effects of fluvoxamine overdose, including convulsions and coma. It was concluded that the cause of the subject's death was the interaction of multiple drugs.

01 Sep 2024·BMJ supportive & palliative care

Anticipatory prescribing in community end-of-life care

Article

Author: Ross, Joy ; Lee, Charlotte ; Tran, Theresa Tammy

Objectives:

Our work aims to critically review the use of anticipatory medicines in our inner-city hospice community population and whether our current practices are fit for purpose.

Methods:

Retrospective audit of community palliative care patients at the end-of-life prescribed anticipatory medicines within a 3-month period. Anticipatory charts and case notes reviewed. Intervention included updating local guidelines, local teaching for medical and non-medical prescribers and sharing results nationally. Eighteen months later, reaudit was performed assessing impact.

Results:

In total, 76 patients included. 75/76 (99%) were prescribed an analgesic, antiemetic, antisecretory and anxiolytic. 49/76 (64%) were administered ‘as required’ medications at home. Haloperidol was the favoured antiemetic (88%), costing our hospice ~£2000/month. Case note review highlighted prescribing and administration issues. Reaudit showed a reduction in prescriptions of antisecretory (by 57%) and antiemetic (by 50%), with a wider range of antiemetics (levomepromazine 47%, haloperidol 35%, cyclizine 14%, metoclopramide 3%) indicating individualised prescribing. Those without an antiemetic prescribed did not later require one dispensing.

Conclusion:

Our work challenges the orthodoxy that an analgesic, antiemetic, antisecretory and anxiolytic medication must always be included for effective anticipatory prescribing. Antiemetics may not be universally required and individualised prescribing was cost-effective and safe at a local level. Further work evaluating the impacts of altered practice on patients, caregivers, professionals and in other community settings is required.

01 Sep 2024·AQUATIC TOXICOLOGY

Comparative in vitro hepatic clearances of commonly used antidepressants, antipsychotics, and anti-inflammatory agents in rainbow trout liver S9 fractions

Article

Author: Pätsi, Jade ; Ollikainen, Elisa ; Sikanen, Tiina M ; Pihlaja, Tea L M

Residues of human pharmaceuticals are widely detected in surface waters and can be taken up by and bioaccumulate in aquatic organisms, especially fish. One of the key challenges in assessing the bioaccumulation potential of ionizable organic compounds, such as the pharmaceuticals, is the lack of empirical data for biotransformation. In the present study, we assessed the in vitro intrinsic clearances (CL_INT) of twelve pharmaceuticals, individually and some additionally as mixtures, in rainbow trout (Oncorhynchus mykiss) liver S9 fractions (RT-S9) adhering to the OECD test guidance 319B. The test substances included four anti-inflammatory agents (diclofenac, ibuprofen, ketoprofen, naproxen), seven antidepressants/antipsychotics (citalopram, haloperidol, levomepromazine, mirtazapine, risperidone, sertraline, venlafaxine) and the O-desmethyl metabolite of venlafaxine. Quantifiable intrinsic clearances were detected for diclofenac, ibuprofen, naproxen, levomepromazine, and sertraline. Apart from diclofenac, the in vitro clearances of the other four pharmaceuticals were shown to be critically dependent on the cytochrome P450 (CYP) metabolism. Therefore, we also determined the half-maximal inhibitory concentrations (IC₅₀) of the same twelve pharmaceuticals toward CYP1A-like (7-ethoxyresorufin-O-deethylation, EROD) and CYP3A-like (benzyloxy-4-trifluoromethylcoumarin-O-debenzyloxylation, BFCOD) activities in RT-S9 using IC₅₀ shift assay. As a result, levomepromazine and sertraline were identified as the most potent inhibitors of both EROD and BFCOD activity (unbound IC₅₀ < 10 µM each), followed by citalopram and haloperidol (10 µM < IC₅₀ < 100 µM). Additionally, mirtazapine was a selective EROD inhibitor (IC₅₀ ∼ 30 µM). The inhibitory impacts of haloperidol and sertraline were indicatively time dependent. Finally, we carried out intrinsic clearance assays with mixtures of diclofenac, ibuprofen, naproxen, levomepromazine, and sertraline to examine the impacts of EROD and BFCOD inhibitions on their in vitro CL_INT in RT-S9. Our in vitro data suggests that the intrinsic clearances of ibuprofen, levomepromazine, and sertraline in rainbow trout can be significantly reduced as the result of P450 inhibition by pharmaceutical mixtures, whereas the clearances of diclofenac and naproxen are less impacted.

News (Medical) associated with Levomepromazine

13 Jul 2022

·endpts.com

Sanofi CEO Paul Hudson offloads two portfolios to German pharma company in continued effort to prune products

Sanofi warned earlier this year that some serious cuts were in order. CEO Paul Hudson made good on that promise this week, pruning more than a dozen marketed products. Germany-based Neuraxpharm revealed yesterday that it struck a deal for Sanofi’s CNS and pain and vascular disease portfolios. While the companies are keeping the financial terms under wraps for now, Neuraxpharm did say it’s swallowing 17 products representing 38 brands, including neuroleptics Nozinan and Tiapridal, anxiety med Tranxene and antipsychotics Dogmatil and Largactil. Within the pain and vascular portfolio, Neuraxpharm is getting pain narcotic Topalgic and Trental, which is used to improve blood flow. Neuraxpharm expects that the new products will boost sales to about $600 million this year. “There is significant growth potential in the pharmaceutical sector, especially in the CNS market driven by an aging population and an increasing awareness of mental health,” CEO Jörg-Thomas Dierks said in a news release. “With the upcoming acquisition, we will not only strengthen our presence in Europe, but also lay the ground for further expanding our international presence.” The new drugs will contribute to a portfolio of CNS drugs, as well as generics and consumer healthcare products such as nutraceuticals and probiotics, according to Neuraxpharm’s website. The company has main offices in Germany and Spain, with additional locations throughout Europe. Hudson has been on a mission to reshape Sanofi since he took the helm in 2019. He said earlier this year that nothing is off the table when it comes to restructuring, and has already culled a handful of programs. During the Q1 call, EVP of general medicines Olivier Charmeil said the company is looking to shave the general medicines unit down to about 125 product families, either by divesting or discontinuing programs. That’s a big difference from late 2019 and early 2020, when the unit boasted more than 350 product families. The company also revealed in its Q4 results that it plans on axing about 6,000 jobs in an effort to become more “agile.” Execs said at the time that they were aiming for a headcount of around 90,000 by the end of the year.

Generic DrugAcquisition

12 Jul 2022

·www.prnewswire.com

Neuraxpharm to increase branded business through upcoming acquisition of established products from Sanofi

Neuraxpharm, the central nervous system (CNS) specialist, to acquire two portfolios of established products for CNS disorders, pain and vascular diseases DUSSELDORF, Germany and BARCELONA, Spain, July 12, 2022 /PRNewswire/ -- Neuraxpharm Group ("Neuraxpharm") today announced that it has entered into a definitive agreement to acquire two product portfolios for CNS disorders, pain and vascular diseases from Sanofi. With the upcoming acquisition, Neuraxpharm will strengthen its position as a leading European specialty pharmaceutical company focused on CNS. The well-established products that Neuraxpharm will acquire are marketed globally in more than 50 countries. The first portfolio combines 15 products addressing CNS disorders and ranging across psychiatry and neurology. The second portfolio includes two products in pain and vascular diseases. Following the acquisition of these new portfolios, Neuraxpharm's annual gross sales will be around EUR 0.6 billion. The products benefit patients across a large spectrum of diseases including depression, anxiety, psychosis, alcohol dependence, myasthenia gravis and Parkinson disease. The CNS portfolio notably includes Nozinan®, Tranxene®, Tiapridal®, Dogmatil®, Largactil®. The pain and vascular portfolio includes Topalgic® and Trental®. Combined, both portfolios include 17 molecules representing 38 brands. These global brands will further solidify Neuraxpharm's position as a leading CNS pharmaceutical company in Europe and increase the company's global footprint and business. Dr. Jörg-Thomas Dierks, CEO of Neuraxpharm, said: "There is significant growth potential in the pharmaceutical sector, especially in the CNS market driven by an ageing population and an increasing awareness of mental health. This phenomenon is a global trend. With the upcoming acquisition, we will not only strengthen our presence in Europe, but also lay the ground for further expanding our international presence." About the Group Neuraxpharm – the European CNS specialist Neuraxpharm is a leading European specialty pharmaceutical company focused on the treatment of central nervous system disorders (CNS) with a direct presence in 19 countries. Backed by funds advised by Permira, Neuraxpharm has a unique understanding of the CNS market built over 35 years. With its focus on CNS, Neuraxpharm develops and commercializes established brands, value added medicines, generics, Consumer Healthcare products, medical cannabis and beyond-the-pill solutions and is continuously striving to offer a wide range of effective, high quality and affordable CNS treatment options in Europe. Present with its products in more than 50 countries, Neuraxpharm also manufactures pharmaceutical products and active pharmaceutical ingredients in its own manufacturing sites, Lesvi and Inke, in Spain. For more information please visit SOURCE Neuraxpharm

Generic DrugAcquisition

100 Deals associated with Levomepromazine

External Link

KEGG	Wiki	ATC	Drug Bank
-	Levomepromazine	N05AA02	DB01403

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Bipolar Disorder	JP	Kyowa Pharmaceutical Industry Co., Ltd.	27 May 1960
Depressive Disorder	JP	Kyowa Pharmaceutical Industry Co., Ltd.	27 May 1960
Schizophrenia	JP	Kyowa Pharmaceutical Industry Co., Ltd.	27 May 1960
Behavioural disorders	US	Immunex Corp.	-

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