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Annals of Emergency Medicine Nov 1991To compare the effectiveness of IM administration of methotrimeprazine, a non-narcotic, nonaddicting phenothiazine derivative, with that of a combination of meperidine... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
STUDY OBJECTIVE
To compare the effectiveness of IM administration of methotrimeprazine, a non-narcotic, nonaddicting phenothiazine derivative, with that of a combination of meperidine and dimenhydrinate in the treatment of severe migraine.
DESIGN
Double-blind, randomized, controlled trial.
SETTING
University hospital emergency department.
PARTICIPANTS
Consecutive adult patients with migraine who met eligibility criteria.
INTERVENTIONS
Random allocation to receive IM injections of either 37.5 mg methotrimeprazine (Levoprome, Nozinan) or 75 mg meperidine (Demerol) combined with 50 mg dimenhydrinate (Dramamine, Gravol).
MEASUREMENTS AND MAIN RESULTS
The 37 patients in each group who completed the study were similar in all demographic and clinical characteristics. There were no statistical differences in pain intensity one hour after treatment, change in pain intensity, or pain relief as measured on a visual-analog scale; need for additional analgesia; persistence of nausea or vomiting; adverse effects; or follow-up status, except for prolonged drowsiness, in the group receiving methotrimeprazine.
CONCLUSION
Methotrimeprazine is comparable to meperidine with dimenhydrinate for treating severe migraine and may be considered an effective, nonaddicting, IM alternative to narcotics for the management of this problem.
Topics: Adolescent; Adult; Dimenhydrinate; Double-Blind Method; Drug Evaluation; Drug Therapy, Combination; Female; Follow-Up Studies; Humans; Injections, Intramuscular; Male; Meperidine; Methotrimeprazine; Middle Aged; Migraine Disorders; Multivariate Analysis
PubMed: 1952306
DOI: 10.1016/s0196-0644(05)81471-4 -
JAMA Dec 1961
Topics: Analgesia; Analgesics; Anesthesia; Anesthesia and Analgesia; Methotrimeprazine; Pain Management; Tranquilizing Agents
PubMed: 14462565
DOI: 10.1001/jama.1961.03040480017004 -
Therapeutic Drug Monitoring 1982Methotrimeprazine (levomepromazine) has two major metabolites in man: N-monodesmethyl methotrimeprazine, which is pharmacologically active and almost as potent as the...
Methotrimeprazine (levomepromazine) has two major metabolites in man: N-monodesmethyl methotrimeprazine, which is pharmacologically active and almost as potent as the parent drug; and methotrimeprazine sulfoxide, which is much less active. Blood levels and the distribution between plasma and erythrocytes of methotrimeprazine and the two metabolites were studied in five psychiatric patients on oral methotrimeprazine and after incubation of the compounds in blood from healthy volunteers. The concentrations were measured separately in plasma and erythrocytes by gas chromatography with a nitrogen detector, and the concentrations in whole blood were calculated from the plasma and erythrocyte concentrations. In four of the five patients the blood levels of both metabolites were similar to or higher than the levels of the parent drug. A large interindividual variation was observed in the plasma-erythrocyte concentration ratios. The mean ratios in all individuals were 1.76, 0.57, and 3.02 for methotrimeprazine, N-monodesmethyl methotrimeprazine, and methotrimeprazine sulfoxide, respectively. The relatively high blood concentrations of N-monodesmethyl methotrimeprazine suggest that this metabolite may contribute significantly to the therapeutic action and side effects of oral treatment with methotrimeprazine.
Topics: Adult; Biotransformation; Chromatography, Gas; Erythrocytes; Female; Humans; Kinetics; Male; Mental Disorders; Methotrimeprazine; Middle Aged
PubMed: 7071908
DOI: 10.1097/00007691-198204000-00012 -
Journal of Pharmaceutical Sciences Jun 1972
Topics: Adult; Chromatography, Gas; Chromatography, Thin Layer; Dealkylation; Humans; Hydrogen-Ion Concentration; Infrared Rays; Male; Mass Spectrometry; Mental Disorders; Methods; Methotrimeprazine; Middle Aged; Spectrum Analysis; Sulfoxides; Ultraviolet Rays
PubMed: 5046109
DOI: 10.1002/jps.2600610618 -
Brain Injury Feb 2001Medical management of the agitation associated with acquired brain injury (ABI) has been proble matic. At least 12 distinct drugs are currently recommended in the... (Clinical Trial)
Clinical Trial
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.
Topics: Adolescent; Adult; Aged; Aged, 80 and over; Antipsychotic Agents; Brain Injuries; Female; Humans; Male; Methotrimeprazine; Middle Aged; Psychomotor Agitation
PubMed: 11260766
DOI: 10.1080/026990501458399 -
Journal of Forensic Sciences Nov 1996Fatal ingestion of methotrimeprazine is unusual, and while therapeutic drug levels are established as concentrations between 0.02 to 0.14 mg/L, fatal levels are not. The...
Fatal ingestion of methotrimeprazine is unusual, and while therapeutic drug levels are established as concentrations between 0.02 to 0.14 mg/L, fatal levels are not. The following describes a case of fatal suicidal ingestion of methotrimeprazine in which the measured concentration of methotrimeprazine in the blood was 4.1 mg/L. In addition, the major metabolites of methotrimeprazine, desmethylmethotrimeprazine, and methotrimeprazine sulfoxide were also measured at 2.0 and 1.8 mg/L, respectively. Methotrimeprazine and its metabolites were also measured in urine, bile, and vitreous humor. These results are compared with other case reports of methotrimeprazine fatalities reported in the literature.
Topics: Adult; Analgesics, Non-Narcotic; Chromatography, Gas; Fatal Outcome; Forensic Medicine; Humans; Male; Methotrimeprazine; Suicide
PubMed: 8914300
DOI: No ID Found -
South African Medical Journal =... Jun 1982
Topics: Adolescent; Adult; Humans; Male; Methotrimeprazine; Porphyrias
PubMed: 7089770
DOI: No ID Found -
Schizophrenia Bulletin Mar 2012
Meta-Analysis Review
Topics: Antipsychotic Agents; Humans; Methotrimeprazine; Psychotic Disorders; Schizophrenia
PubMed: 22114097
DOI: 10.1093/schbul/sbr174 -
Journal of Korean Medical Science Nov 2010Two schizophrenic patients who had been taking medication for a long period presented with visual disturbance of 6-month duration. Slit-lamp examination revealed fine,...
Two schizophrenic patients who had been taking medication for a long period presented with visual disturbance of 6-month duration. Slit-lamp examination revealed fine, discrete, and brownish deposits on the posterior cornea. In addition, bilateral star-shaped anterior subcapsular lens opacities, which were dense, dust-like granular deposits, were noted. Although we strongly suspected that the patient might have taken one of the drugs of the phenothiazine family, we were unable to obtain a history of medications other than haloperidol and risperidone, which were taken for 3 yr. We performed a drug profiling test using urine samples and detected methotrimeprazine. The patient underwent surgery for anterior subcapsular lens opacities. Visual acuity improved in both eyes, but the corneal deposits remained. We report an unusual case of methotrimeprazine-induced corneal deposits and cataract in a patient with psychosis, identified by using the urine drug profiling test.
Topics: Adult; Antipsychotic Agents; Cataract; Corneal Diseases; Female; Humans; Intellectual Disability; Male; Methotrimeprazine; Middle Aged; Schizophrenia; Visual Acuity
PubMed: 21060765
DOI: 10.3346/jkms.2010.25.11.1688 -
Molecular Pharmacology Mar 1982The 3-dimensional molecular structures of methotrimeprazine, methotrimeprazine sulfoxide, and chlorpromazine sulfoxide were examined by X-ray crystallography. Previous...
The 3-dimensional molecular structures of methotrimeprazine, methotrimeprazine sulfoxide, and chlorpromazine sulfoxide were examined by X-ray crystallography. Previous studies of their dopamine receptor binding affinities have indicated that both chlorpromazine sulfoxide and methotrimeprazine sulfoxide lack neuroleptic potency. The crystal structures of methotrimeprazine and its sulfoxide were similar to the previously published structure of chlorpromazine. The sulfoxide metabolite of chlorpromazine, on the other hand, had a different conformation of the side chain. A boat axial conformation of the sulfoxy group was found for both metabolites. The crystal structures suggest that the apparent loss of neuroleptic potency by biotransformation of the phenothiazine drugs to their ring sulfoxides is caused by the introduction of the sulfoxide group itself, and not by concurrent conformational changes in the rest of the molecule.
Topics: Animals; Antipsychotic Agents; Brain; Chlorpromazine; Methotrimeprazine; Models, Molecular; Molecular Conformation; Rats; Structure-Activity Relationship
PubMed: 6124878
DOI: No ID Found