Levomepromazine

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Structural formula
Levomepromazine structural formula m.  Stereochemie.png
General
Non-proprietary name Levomepromazine
other names

( R ) - [3- (2-Methoxyphenothiazin-10-yl) -2-methylpropyl] - N , N -dimethylamine

Molecular formula C 19 H 24 N 2 OS
External identifiers / databases
CAS number
EC number 200-495-5
ECHA InfoCard 100,000,450
PubChem 72287
ChemSpider 65239
DrugBank DB01403
Wikidata Q417204
Drug information
ATC code

N05 AA02

Drug class

Antipsychotic , phenothiazines

properties
Molar mass 328.47 g · mol -1
pK s value

9.19

solubility

practically insoluble in water (20 mg l −1 at 25 ° C)

safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances

Hydrochloride

07 - Warning

Caution

H and P phrases H: 302-317
P: 261-280-321-301 + 312-363-501
Toxicological data

1100 mg kg −1 ( LD 50ratoral )

As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Levomepromazine is a drug from the phenothiazine group that is used in psychopharmacotherapy . It is a low-potency (weak) antipsychotic that is more used as a sleep aid and sedation agent .

Action profile

As a low-potency neuroleptic , the sedating component is in the foreground of the spectrum of activity of levomepromazine; the antipsychotic properties are rather low. Indicated is Levomepromazin u. a. in psychomotor states of excitement, which is why it is often, popularly spoken, administered in the form of "tranquilizers".

Pharmacodynamics

Levomepromazine inhibits dopamine (D 2 and D 4 ) receptors, serotonin receptors (5HT 2A ) and histamine 1 receptors (H 1 ) as well as muscarinic acetylcholine receptors (ACh M )

Indications

Levomepromazine is approved for use in states of excitement that occur in the context of psychotic disorders or mania .

As a special feature of the phenothiazines, there is also the indication for the combination therapy of severe or chronic pain .

Although no randomized and controlled studies exist, levomepromazine is often used in palliative medicine for sedation in terminal agitation / restlessness and as a reserve drug for the treatment of nausea and vomiting.

Dosage forms, dosage

Levomepromazine is available in commercial preparations in the form of tablets and drops / oral solution and as a solution for injection.

The mean daily dose is 30–75 mg ( inpatient maximum 300 mg per day). The daily dose should be divided into several doses, with half or a larger part being administered in the evening.

Side effects

chemistry

The synthesis of levomepromazine is described in the literature. Levomepromazine is used exclusively enantiomerically pure in the ( R ) form.

Trade names

Monopreparations

Levium (D), Neurocil (D), Nozinan (A, CH), various generics (D)

See also

Individual evidence

  1. a b c Entry on levomepromazine in the ChemIDplus database of the United States National Library of Medicine (NLM) .
  2. a b LGC Standards: Levomepromazine Hydrochloride ( Memento from October 31, 2016 in the Internet Archive )
  3. Cochrane Database Syst Rev. 2015 Nov 2; (11): CD009420. doi : 10.1002 / 14651858.CD009420.pub3 .
  4. Specialist information Levomepromazin-neuraxpharm (solution for injection)
  5. Florian Holsboer, Gerhard founder, Otto Benkert: Manual of psychopharmacotherapy: with 155 tables . Springer, Heidelberg 2008, ISBN 978-3-540-20475-6 .
  6. ^ Pharmaceutical Substances , Axel Kleemann , Jürgen Engel, Bernd Kutscher and Dieter Reichert, 4th edition (2000) 2 volumes published by Thieme-Verlag Stuttgart, see there pages 1168–1169, ISBN 978-1-58890-031-9 ; online since 2003 with biannual additions and updates.