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PubMed1990

High-performance liquid chromatography of levomepromazine (methotrimeprazine) and its main metabolites.

The phenothiazine drug levomepromazine (methotrimeprazine) has five metabolites which previously have been identified in plasma from psychiatric patients. These are formed by sulphoxidation, N-demethylation, O-demethylation and aromatic hydroxylation in two different positions. A high-performance liquid chromatographic system is described for the analysis of levomepromazine and its main metabolites on a Supelcosil C18-DB column, based on ion-pair formation with sodium docecyl sulphate. The effects of variations in pH, buffer concentration, counter-ion concentration, temperature and concentration and composition of the organic solvent were examined. The six components may be analysed in 27.4 min at room temperature using 25 mM sodium dodecyl sulphate in 500 mM ammonium acetate buffer (pH 5.0)-5% v/v tetrahydrofuran in acetonitrile (50:50, v/v) as the mobile phase.

Acetates↗
PubMed2000

Neuroleptic malignant syndrome during olanzapine and levomepromazine treatment.

OBJECTIVE: To date only five reports of neuroleptic malignant syndrome (NMS) related to olanzapine exist. The first case report was published in November 1998. METHOD: We report the case of a 78-year-old woman suffering from chronic schizophrenia who developed a NMS while being treated with olanzapine and levomepromazine. Before this her medication had been unchanged for more than 2 years. RESULTS: When treated with olanzapine and levomepromazine, the patient had a fulminant NMS which was complicated with pneumonia. When the neuroleptic drug treatment was discontinued, the patient recovered. However, when this combination was restarted later due to severe agitation and hallucinations, the symptoms of NMS reappeared. CONCLUSION: This case report shows that the neuroleptic malignant syndrome can occur during olanzapine treatment as well as during treatment with conventional neuroleptics. This syndrome may develop even after a long and stable neuroleptic treatment.

Aged↗
PubMed1999

Levomepromazine (methotrimeprazine) and the last 48 hours.

Levomepromazine (previously known as methotrimeprazine) has a broad range of beneficial effects in the terminal phase of many illnesses, resulting from its combined antipsychotic, anxiolytic and sedative actions. Levomepromazine can safely be administered in a continuous subcutaneous infusion with most other commonly used drugs in palliative care.

Antipsychotic Agents↗
PubMed1976

[Hemodynamic study of postural regulation in the dog treated or not treated with levomepromazine].

Analysis of hemodynamic parameters in untreated and treated dogs (levomepromazine 5 mg/kg i.v.) during supine and erect position showed, 1) that the regulation of cerebral blood flow remained in the anaesthetized (pentobarbital 25 mg/kg i.v.) dogs ; 2) that the sympathetic reaction induced different effects in various vascular regions ; 3) that levomepromazine induced an impairement of the mechanisms involved in the regulation of the encephalic irrigation.

Animals↗
PubMedDate not supplied

Subcutaneous levomepromazine rescue (SLR) for high grade delayed chemotherapy-induced emesis (DCIE).

BACKGROUND: Delayed chemotherapy-induced emesis (DCIE) has significant patient and health economic impact. Up to 50% of patients on chemotherapy may develop DCIE. There is no accepted standard of care for DCIE. PATIENTS AND METHODS: A prospective observational study of patients with high grade DCIE needing admission to hospital over a 2-year period. Single cycle delayed anti-emetic failure (DAF) per patient is reported. Twenty-five mg/24 hours subcutaneous levomepromazine rescue (SLR) was used. Control of nausea and vomiting was recorded in 2 time-periods: 0 to 24 hours and 24 to 48 hours. RESULTS: Thirty-two patients (12 male, 20 female) required SLR. Median age 58 years (r. 35-76). Grade 0 nausea and vomiting (N and V) was attained within 24 hours in 75% and 81% of patients, respectively, and in 94% of patients for both by 48 hours. Side-effects of sedation and hypotension were mild. CONCLUSION: Levomepromazine has efficacious anti-emetic qualities in the rescue of patients with high grade DCIE needing hospital admission.

Adult↗
PubMed1982

Gas chromatographic mass spectrometric identification of O-demethylated and mono-hydroxylated metabolites of levomepromazine in blood from psychiatric patients by selected ion recording with high resolution.

An O-demethylated and two mono-hydroxylated metabolites of levomepromazine have previously been identified as conjugates in the urine from psychiatric patients. The three metabolites were identified in hydrolysed and nonhydrolysed plasma and erythrocytes from three patients by selected ion monitoring of the trimethylsilyl derivatives, with a mass spectrometric resolution of 5000. The three metabolites were mainly found as conjugates in the plasma, and smaller amounts were found unconjugated in the plasma and the erythrocytes.

Adult↗
PubMed1987

Nuclear magnetic resonance analysis of methotrimeprazine (levomepromazine) hydroxylation in humans.

Two monohydroxylated metabolites of methotrimeprazine (levomepromazine), which previously have been identified in plasma and urine from psychiatric patients, were synthesized by nonenzymatic, FeCl2-catalyzed oxidation, isolated, and purified by preparative reversed-phase HPLC. Mass spectrometric analysis gave identical spectra for the two compounds, but did not reveal the positions of the OH groups. However, 1H NMR spectroscopy at 200 MHz demonstrated that one of the compounds, which had the shortest GC retention time on an OV-17 column, was hydroxylated in the 3-position on the phenothiazine nucleus, and that the other derivative was hydroxylated in the 7-position. The metabolism of methotrimeprazine differs, therefore, from that of its congener chlorpromazine, which is hydroxylated mainly in the 7-position in humans.

Biotransformation↗
PubMed1986

Importance of oxidative polymorphism and levomepromazine treatment on the steady-state blood concentrations of clomipramine and its major metabolites.

The relationship between the debrisoquine oxidation status and the metabolism of clomipramine was studied in nine healthy volunteers (five rapid hydroxylators, three slow hydroxylators and one of intermediate status). The hydroxylation of clomipramine and demethylclomipramine were found to covary with that of debrisoquine, whereas demethylation of clomipramine seemed to be independent of the debrisoquine hydroxylation phenotype. The steady-state blood concentrations of clomipramine and its three main metabolites were measured in 122 depressed patients. Thirteen patients who concomitantly received a neuroleptic tended to have higher levels of demethylclomipramine and clomipramine, whereas the levels of the hydroxylated metabolites were hardly affected. Benzodiazepine co-administration did not modify the pharmacokinetics of clomipramine. The results suggest that benzodiazepines rather than levomepromazine should be used in depressed patients with anxiety and/or agitation in combination with the antidepressant treatment.

Adult↗
PubMedDate not supplied

Metabolism of levomepromazine in man.

The phenothiazine drug, levomepromazine (LM), is used in the treatment of psychiatric disorders and as an analgesic. A single 50 or 100 mg dose of LM was given to healthy male volunteers, and urine samples were collected for 24 h. The urine was treated with beta-glucuronidase, purified by solid-phase extraction, and analyzed on a GC-MS system for identification of LM metabolites. Mass spectra suggesting 14 different LM metabolites were obtained from the samples. Our of these, 13 spectra could be ascribed to specific metabolites, 5 of which have not previously been identified. All these 5 metabolites were hydroxylated at the phenothiazine nucleus. Although the applied method did not determine the positions of hydroxyl groups on phenothiazine nuclei. 3 of the 5 metabolites were identified as O-desmethyl 3-hydroxy LM, O-desmethyl 7-hydroxy LM, and N,O-didesmethyl 7-hydroxy LM, based on their chromatographic properties. In addition two metabolites, one being hydroxylated on the phenothiazine nucleus, and one being O-demethylated and hydroxylated on the nucleus, were found. It is suggested that these were 8-hydroxy LM and O-desmethyl 8-hydroxy LM. The concentrations of 3-hydroxy LM (free+conjugated) appeared to be much higher than the concentrations of any other metabolite in the samples.

Antipsychotic Agents↗
PubMed1993

Effects of zopiclone, flunitrazepam, triazolam and levomepromazine on the transient change in sleep-wake schedule: polygraphic study, and the evaluation of sleep and daytime condition.

1. The effects of zopiclone 10mg (ZP), flunitrazepam 1mg (FN), triazolam 0.25mg (TZ) and levomepromazine 5mg (LP) on two models of sleep-wake schedule change-6 hours advanced shift: (A-shift), and 6 hours delayed: (D-shift)--were investigated in 6 healthy volunteers using polysomnography. 2. In A-shift with placebo, TST, SEI, %SR and REM/NREM decreased. ZP, FN and TZ shortened SL. All drugs increased TST and SEI. TZ and LP increased %SR and REM/NREM. 3. In D-shift with placebo, TST decreased, SWSL was prolonged, %S3+4 decreased, and %SR and REM/NREM increased. All drugs increased TST. ZP and LP shortened SWSL. All drugs increased %SWS. ZP, FN and TZ decreased %SR. ZP and FN decreased REM/NREM. 4. Daytime mental and physical conditions were worse than usual on more than half of the days in A- and D-shift. LP and FN caused some inadequate conditions on the following days. Significantly higher REM/NREM was observed in the nights before the days with worse mental conditions in D-shift, and lower REM/NREM in the nights before the days with worse physical conditions in A-shift. 5. It is concluded that TZ and ZP are superior to the others for A-shift and D-shift, respectively.

Adult↗
PubMed2006

Possible levomepromazine-clozapine interaction: two case reports.

OBJECTIVE: To report and comment upon two cases of suspected pharmacological interaction between the "classical" neuroleptic levomepromazine (LMP) and the "atypical" antipsychotic clozapine (CLZ). CASE SUMMARY: The patients who simultaneously took the two drugs had unusually low plasma levels of CLZ and its metabolites, even though they took high doses of CLZ. The patients were considered "non-responders" to the treatment by the psychiatrist. When LMP was withdrawn from the therapy, plasma concentrations of CLZ returned to therapeutic levels and one of the two patients experienced the anticipated therapeutic response. DISCUSSION: No information can be found in the literature regarding possible interactions between LMP and CLZ. However, the results of the two cases reported herein point out to a possible lack of therapeutic efficacy of CLZ therapy during this kind of polypharmacy. CONCLUSION: While two cases are too few to draw any conclusion, it would be prudent on the part of psychiatrists to consider a possible drug interaction in patients receiving both CLZ and LMP who fail to respond to the therapy.

Adolescent↗
PubMed2005

The use of levomepromazine in Hyperemesis Gravidarum resistant to drug therapy--a case series.

Hyperemesis Gravidarum (HG) is a potentially serious complication of early pregnancy, which may rarely be severe enough to warrant termination of pregnancy. HG requires prompt treatment with intravenous fluids, thiamine supplementation and appropriate anti-emetic therapy. Anti-histamines such as promethazine are favoured as first-line agents, with prochlorperazine being used as a second-line drug. However, there is no clear data as to the most appropriate drug if these are ineffective. A case series of six women who presented with HG resistant to drug treatment is described. In these cases, levomepromazine 6.25mg tds was used to control HG. Five pregnancies progressed leading to live born infants with no evidence of congenital anomaly. One pregnancy resulted in an intra-uterine death with no external or ultrasound evidence of congenital anomaly. The role of phenothiazines in the pharmacological management of HG is discussed.

Adolescent↗
PubMed1998

A risk for obstruction of the airways in the parenteral use of levomepromazine with benzodiazepine.

Arrhythmogenic effects of phenothiazines appear to be associated with sudden death, whereas respiratory complications have received little attention. In this report we describe 5 cases with accompanying obstruction of the airways after intramuscular injections of levomepromazine (LPZ), a potent sedative phenothiazine, in combination with intravenous injections of benzodiazepine (BZ) during a 3-month period in a psychiatric intensive care unit. Two out of 5 cases were unpredictable because obstruction of the airways occurred 2 hours or more after the last injection. As compared with patients who received parenteral (intravenous or intramuscular) injections during the same period, the dose of intramuscular LPZ was significantly large in the 5 cases with obstruction of the airways. All 5 of these cases received intramuscular LPZ 0.52 mg/kg or more. In contrast, there was no patient with obstruction of the airways who received only intramuscular LPZ, the combination of LPZ and HDL, or BZ and HDL. The occurrence of obstruction of the airways among patients who received both intramuscular LPZ and intravenous BZ was significantly higher than among patients who received other drug regimes. These preliminary results suggest that the intramuscular use of LPZ with intravenous BZ may be a risk for obstruction of the airways.

Adult↗
PubMed1983

Levomepromazine elimination in patients during active and sham hemodialysis.

The effect of active and sham dialysis on the plasma concentration of levomepromazine was studied in seven schizophrenic patients undergoing hemodialysis treatment in a double-blind crossover study. Samples of blood were collected before, after 2 h and 5 h of treatment, and once a week during the treatment program. The plasma concentrations decreased during both active and sham dialysis. The data indicate that there was no significant difference in the elimination of the drug between active and sham hemodialysis.

Adult↗
PubMed1992

Is levomepromazine a useful drug in treatment-resistant schizophrenia?

Levomepromazine (LMP) unexpectedly improved 16 of 23 chronic treatment-resistant schizophrenic patients who were hospitalized in most cases for at least 2 years and who manifested positive symptoms, irritability and, in many cases, restlessness, hostility, uncooperativeness, poor concentration and aggressive behavior. Improvement led to discharge in 7 (6 to a foster home), placement on a waiting list for a foster home in 4 and improved behavior and autonomy in 5 patients. Five subjects developed seizures and 1 agranulocytosis. Whether improvement with LMP is caused by unique antischizophrenic properties or by diminished liability to induce side effects such as akathisia, a formal controlled study of LMP in treatment-resistant schizophrenia is merited.

Adult↗
PubMed1993

Resolution of chlorpromazine-induced cutaneous pigmentation following substitution with levomepromazine or other neuroleptics.

Eleven chronic schizophrenic patients with abnormal skin pigmentation associated with neuroleptic treatment were withdrawn from chlorpromazine (CPZ), which was replaced by levomepromazine (n = 4), trifluoperazine (n = 1) or thioproperazine (n = 1) as the sole neuroleptic, by a combination of these phenothiazines (n = 4) or with haloperidol plus pipotiazine (n = 1). Seven patients showed complete resolution of abnormal skin pigmentation over a period of 1-5 years and 4 markedly improved over 2.0-2.6 years of follow-up. Our observations suggest that neuroleptic-induced abnormal skin pigmentation is (i) predominantly, if not exclusively, a side effect of CPZ and (ii) reversible, providing that CPZ is withdrawn and sufficient time is allowed to elapse.

Adult↗
PubMed1993

Levomepromazine receptor binding profile in human brain--implications for treatment-resistant schizophrenia.

The receptor binding profile of levomepromazine (LMP) in human brain was compared with that of clozapine (CLOZ) and chlorpromazine (CPZ). LMP showed significantly greater binding affinity for both alpha-1 and serotonin-2 binding sites than either CLOZ or CPZ, and significantly greater binding to alpha-2 sites than CPZ. A potent pharmacological effect at these receptor sites may explain the beneficial effect of LMP on psychotic symptoms and akathisia in treatment-resistant schizophrenia recently described in 2 open studies. LMP requires further appraisal as a potentially useful neuroleptic in the management of treatment-resistant schizophrenia.

Adolescent↗