Levomepromazine
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Non-proprietary name | Levomepromazine | |||||||||||||||||||||
other names |
( R ) - [3- (2-Methoxyphenothiazin-10-yl) -2-methylpropyl] - N , N -dimethylamine |
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Molecular formula | C 19 H 24 N 2 OS | |||||||||||||||||||||
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Drug information | ||||||||||||||||||||||
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properties | ||||||||||||||||||||||
Molar mass | 328.47 g · mol -1 | |||||||||||||||||||||
pK s value |
9.19 |
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solubility |
practically insoluble in water (20 mg l −1 at 25 ° C) |
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Toxicological data | ||||||||||||||||||||||
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
- Very common: especially at the start of treatment, with high doses or parenteral administration, increased fatigue, vegetative disorders with pronounced orthostatic dysregulation (reaction to changes in position), low blood pressure , tachycardia (persistently accelerated pulse) and ECG changes may occur.
- Common: extrapyramidal motor side effects such as early dyskinesia (tongue and throat cramps, torticollis, jaw muscle cramps, gaze cramps, stiffening of the back muscles), Parkinson's syndrome (hypomimia, tremor, rigidity, akinesia, hypersalivation), akathisia ( urge to move, inability to remain seated). In these cases, a dose reduction and co-medication with an anti-Parkinsonian drug such as Biperiden should be considered. Vegetative side effects such as accommodation disorders , dry mouth, a stuffy nose, increase in intraocular pressure , constipation and micturition disorders occur frequently, as do nausea, vomiting, diarrhea and loss of appetite.
- Uncommon: allergic reactions , allergic skin reactions and photosensitivity, also pigment deposits in the cornea and lens , severe liver dysfunction , drainage disorders of the bile, jaundice (jaundice), restlessness, agitation, drowsiness, depressive mood , lethargy, dizziness, exacerbation of psychotic symptoms , rare signs of excitation and confusion - particularly in combination with anticholinergic -wirksamen drugs - and cerebral seizures , as well as regulatory disturbances of body temperature.
chemistry
The synthesis of levomepromazine is described in the literature. Levomepromazine is used exclusively enantiomerically pure in the ( R ) form.
Trade names
Levium (D), Neurocil (D), Nozinan (A, CH), various generics (D)
See also
Individual evidence
- ↑ a b c Entry on levomepromazine in the ChemIDplus database of the United States National Library of Medicine (NLM) .
- ↑ a b LGC Standards: Levomepromazine Hydrochloride ( Memento from October 31, 2016 in the Internet Archive )
- ↑ Cochrane Database Syst Rev. 2015 Nov 2; (11): CD009420. doi : 10.1002 / 14651858.CD009420.pub3 .
- ↑ Specialist information Levomepromazin-neuraxpharm (solution for injection)
- ↑ Florian Holsboer, Gerhard founder, Otto Benkert: Manual of psychopharmacotherapy: with 155 tables . Springer, Heidelberg 2008, ISBN 978-3-540-20475-6 .
- ^ 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.