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PubMed1977

Identification of nonpolar methotrimeprazine metabolites in plasma and urine by GLC-mass spectrometry.

Two metabolites of methotrimeprazine, the sulfoxide and the demethylated analog, were identified in extracts from patient plasma by combined GLC-mass spectrometry. Methotrimeprazine and its sulfoxide had similar mass spectra but different GLC retention times. In addition to the metabolites found in plasma, two other metabolites, the didesmethyl analog and the monodesmethyl sulfoxide, were identified in a urine extract.

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↗

PubMedDate not supplied

Identification of O-demethylated and ring-hydroxylated metabolites of methotrimeprazine (levomepromazine) in man.

Nonenzymatic FeCl2-catalyzed oxidation of methotrimeprazine (levomepromazine) yielded three ring-hydroxylated derivatives that had different GC retention times but almost identical mass spectra. Two of these, together with O-desmethylmethotrimeprazine, were identified by combined GC/MS in enzymatically hydrolyzed urine from four psychiatric patients, who had been treated with oral doses of methotrimeprazine. The mass chromatograms indicated that the three metabolites were formed in similar amounts. Small amounts of three other metabolites were also found in the urine after enzymatic hydrolysis. These were identified as O-desmethyl-N-monodesmethylmethotrimeprazine and two monohydroxy-N-monodesmethyl derivatives that had different GC retention times. None of those metabolites were found in unconjugated form in the urine.

Adult↗

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↗

PubMed2001

Methotrimeprazine in the treatment of agitation in acquired brain injury patients.

Medical management of the agitation associated with acquired brain injury (ABI) has been proble matic. At least 12 distinct drugs are currently recommended in the medical literature. In recent years, on the ABI in-patient rehabilitation unit, methotrimeprazine (MTZ) has come to be the preferred drug and is used routinely for effective treatment of agitation. The objective of this paper is to describe the use and safety of MTZ in the rehabilitation of ABI patients. A retrospective chart review of all patients discharged from the ABI unit over a course of 2 years was conducted. In addition to demographics such a aetiology of ABI, sex, age, length of stay, Glasgow Coma Scale, length of posttraumatic amnesia and others, a detailed analysis was made of the multidisciplinary progress notes to determine the daily agitation status and the daily use of psychotropic medication. All notes on side effects and adverse reactions were carefully documeneted. 120 first admission recent ABI patients were discharged in the 2 year study period. Of these, 69 (57%) had some level of agitation and 56 (48%) were treated with MTZ, in doses of 2-50 mg up to four times daily. Agitation was controlled in most cases. In only two cases were significant side effects noted. While MTZ has been used as a safe and effective neuroleptic in psychiatry for over 40 years, this is the first report of its use in treating agitation in ABI.

Adolescent↗

PubMedDate not supplied

Comparison of methotrimeprazine and meperidine as components of balanced anesthesia.

Methotrimeprazine (MTM) (0.5 mg/kg) and meperidine (1.5 mg/kg) was administered to four groups of 10 patients each. Two of these groups (I and II) received MTM or meperidine 12 minutes before, two other groups (III and IV), 3 minutes after, induction of thiopental anesthesia. N2O-O2 was administered after thiopental induction, and fractional doses of meperidine and muscle relaxants were used as required for maintenance of anesthesia. The preliminary administration of MTM or meperidine decreased the induction dose of thiopental by about 60 percent. When administered before thiopental, both had similar effects on heart rate, but whereas MTM moderately decreased, meperidine moderately increased systolic and diastolic blood pressure MTM had little or no effect on respiratory rate, which was significantly depressed by meperidine. When given after an induction dose of thiopental, the circulatory effects of MTM and meperidine were similar. Respiratory measurements were little affected by MTM but were markedly depressed by meperidine. The mug/kg/min maintenance doses of meperidine were about the same in the four groups. Postanesthetic recovery of consciousness was delayed in the two MTM groups. The incidence of postoperative nausea and vomiting was less in the MTM than in the meperidine groups. MTM appears to have several advantages over meperidine as a component of balanced anesthesia, but is not desirable if rapid postanesthetic recovery or early ambulation is important. Its use is indicated in patients in whom even transient respiratory depression is undesirable and in those in whom prolonged postoperative sedation is desired.

Adolescent↗

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↗

PubMedDate not supplied

[The algimetry evaluation by thermic and pressoric nociceptive stimulus in dogs pre treated with methotrimeprazine, midazolam and ketamine with or without butorphanol or buprenorphine].

PURPOSE: This study aimed at quantifies the pain in dogs under dissociative anesthesia, across thermal and pressoric stimulus and quantify the reasonable period between two different opioids analgesics. METHODS: In this study, 30 dogs were used and, divided into three groups of 10 animals each, in which the animals of GI received methotrimeprazine and midazolam put on the same syringe with ketamine. The animals of GII received the same treatment of GI but associated with butorphanol and finally the animals of GIII received the same treatment of GI but associated with buprenorphine. The routine parametric evaluations has been proceeded, although using the thermo algimetry measured in degrees C with the average of 52 degrees C and the pressoric algimetry in Kg. RESULTS: In the thermo algimetry, there has been significant difference in GI at the moments M0, M1, M4 and M5; in GII it was found at M0, M1, M5 and M6 and in GIII it was observed the significant at M0 and M1. It has also been shown in pressoric algimetry significant difference in GI at the moments M0, M2 and M3. Among GII it has observed significant difference at all moments and it has found at M0, M9 in GIII. Thus, it has observed significant differences between all groups; for such the M2 of GII smaller than the others; and M4, M5 of GIII bigger than GI and GII. In the assessment of all periods it was observed significant latent period bigger in GI, however, with reasonable period and short recovery in GII and GIII. In the order hand, the postural tonus recovery it was longer in GIII, followed by GII and finally GI. CONCLUSION: The used method for the measurement of algic stimulus was efficient, noticing a reasonable analgesic period of 3 hours for butorphanol and 6 hours for buprenorphine.

Analgesics↗

PubMed2003

Photochemistry and in vitro phototoxicity studies of levomepromazine (methotrimeprazine), a phototoxic neuroleptic drug.

The neuroleptic drug levomepromazine (1, previously known as methotrimeprazine) is photolabile under UV-A and UV-B light in aerobic conditions. Irradiation of a methanol solution of this drug produces one photoproduct, resulting from the oxidation of 1 to its sulfoxide parent. It is demonstrated that photodegradation occurs via type II mechanism involving irreversible trapping of self-photogenerated singlet molecular oxygen. 1 shows a photohemolytic effect on human erythrocytes and photoinducers lipid peroxidation.

Antipsychotic Agents↗

PubMed1979

Characterization of analgesic and activity effects of methotrimeprazine and morphine.

The interactions of Methotrimeprazine (MTM) with the CNS opiate receptor, with naloxone, and with morphine were investigated. MTM (16--256 nM) did not compete with 3H-naloxone for specific binding sites in mouse brain homogenates. In vivo, MTM induced analgesia was not antagonized by naloxone. After 14 days administration of MTM partial tolerance developed to the activity effect but not the analgesic effect. After 14 days administration of morphine, tolerance developed to both the activity effect and the analgesic effect.

Analgesics↗

PubMedDate not supplied