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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.
[Effect of a levopromazine-thymalin combination on the development of toxic edema and swelling in the brain].
The development of toxic edematous brain swelling in rats is accompanied by disproteinemia of the blood plasma and buildup of the gamma-globulin fraction. The administration of levopromazine (5 mg/kg), thymalin (1.2 mg/kg), or their combination reduces this disorder in the blood protein fractions. The antiedematous effect of the levopromazine--thymalin combination has an additive synergistic interaction.
[Clinical trials with levomepromazine].
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[Hair analysis as a document of oxcarbazepine therapy in fatal levomepromazine poisoning].
A development of contemporary analytical methods makes possible to use hairs in toxicological analysis for documentation history of drug administration. An undertaken subject has been illustrated by a suicidal fatal poisoning of 58-year-old man with a neuroleptic drug--levomepromazine. Toxicological analysis carried out by HPLC/APCI/MS, besides of standardized postmortem specimen as blood, urine, liver and cerebrospinal fluid included also victim hairs. As a result of analytical procedure levomepromazine at high concentrations was revealed, which may be responsible for death. Moreover, and antiepileptic drug--oxcarbazepine and two main metabolites at therapeutic concentrations were revealed parallel. In three 2-cm segments of hair oxcarbazepine and two metabolites were detected, levomepromazine, in contrary, was not detected in this specimen. Complex chemical-toxicological investigation confirmed information that victim was an epileptic patient and was treated with oxcarbazepine at least 6 months before death while toxic dose of levomepromazine, as one could suppose, he took to commit suicide.
Interactions between neuroleptics and CYP2C6 in rat liver--in vitro and ex vivo study.
The aim of the present study was to investigate the influence of classic and atypical neuroleptics on the activity of rat CYP2C6 measured as a rate of warfarin 7-hydroxylation. The reaction was studied in control liver microsomes in the presence of neuroleptics, as well as in microsomes of rats treated intraperitoneally for one day or two weeks (twice a day) with pharmacological doses (mg/kg) of the drugs (promazine, levomepromazine, thioridazine, perazine 10, chlorpromazine, haloperidol 0.3, risperidone 0.1, sertindole 0.05), in the absence of the neuroleptics in vitro. Some of the neuroleptics added in vitro to control liver microsomes decreased the activity of CYP2C6. Sertindole and levomepromazine (Ki = 25 and 31 microM, respectively) were the most potent inhibitors of the rat CYP2C6 among the drugs studied. Their effects were more pronounced than those of the other phenothiazines tested: thioridazine and chlorpromazine (Ki = 88 and 91 microM, respectively), promazine and perazine (Ki = 322 and 341 microM, respectively), risperidone (Ki = 414 microM) or haloperidol (Ki = 606 microM). The investigated neuroleptics--when given to rats in vivo for one day or two weeks--did not produce any indirect effect on CYP2C6 via other mechanisms, except for levomepromazine, which increased the activity of the enzyme after 24-h exposure. Therefore, the direct inhibitory effect of levomepromazine on CYP2C6 may be attenuated by an indirect mechanism at the beginning of the neuroleptic therapy. In summary, the obtained results show direct inhibitory effects of some phenothiazine neuroleptics and sertindole on the activity of CYP2C6 in vitro in rat liver microsomes. Considering relatively high pharmacological doses and therapeutic concentrations of phenothiazines, it seems that the inhibitory effect of levomepromazine (and other phenothiazines with Ki values below 100 microM) found in vitro may be of physiological and pharmacological importance in vivo.
Pharmacokinetic interaction between imipramine and antidepressant neuroleptics in rats.
Antidepressant neuroleptics, perazine (PZ), levomepromazine (LMZ) and flupenthixol (FPX) given to rats jointly with imipramine (IMI) for 2 weeks affected the plasma concentration of IMI only slightly but markedly elevated the concentration of its metabolite, desipramine (DMI). In the brain PZ significantly elevated both IMI and DMI concentrations while LMZ and FPX showed a tendency to increase the concentration of IMI and decrease the concentration of DMI. All three neuroleptics markedly decreased the DMI/IMI ratio in the brain and (except FPX) increased it in the plasma. Given alone for two weeks PZ, LMZ, FPX did not affect the levels of cytochromes P-450 and b-5 in liver microsomes. Chronic treatment with IMI significantly elevated the concentration of cytochrome P-450 in the liver and had a tendency to increase the concentration of cytochrome b-5. FPX, but not PZ or LMZ abolished this effect. Neuroleptics coadministered with IMI to rats did not affect the activity of the enzymes responsible for the IMI biotransformation as compared with IMI-treated animals. The neuroleptics added to the incubation mixture in vitro inhibited IMI hydroxylation noncompetitively. The demethylation was inhibited competitively by LMZ but noncompetitively by PZ and FPX. The inhibitory effect of neuroleptics on the hydroxylation was much more marked than that on the demethylation. FPX was the weakest inhibitor of IMI metabolism among the neuroleptics studied.
Levomepromazine versus chlorpromazine in treatment-resistant schizophrenia: a double-blind randomized trial.
OBJECTIVE: We compared the effect of levomepromazine (LMP) with chlorpromazine (CPZ) in treatment-resistant schizophrenia (TRS). METHODS: We carried out a double-blind, parallel group study (n = 19/arm) with balanced randomization in blocks of 4 and stratification by sex. Subjects entered a 30-week trial, of which phases I-III were open: phase I (wk 0-6) baseline; phase II (wk 7-9) stepwise transition to haloperidol (HAL), 30 mg/d, plus benztropine (BT), 4 mg/d; phase III (wk 10-15) HAL, 40-60 mg/d, plus BT, 4-6 mg/d; phase IV (wk 16-20) stepwise transition to LMP or CPZ (500 mg/d) following randomization; phase V (wk 21-28) stepwise increase of LMP or CPZ (600-1000 mg/d, dose reduction permitted) to establish optimum dose; and phase VI (wk 29-30) optimized dose maintained. Criteria for TRS were based on those established by Kane et al in 1988. The criterion for a response to treatment was a reduction of 25% or more in total Brief Psychiatric Rating Scale score. RESULTS: Both LMP (p = 0.007) and CPZ (p = 0.030) improved TRS relative to baseline. Although there was no significant difference between the 2 groups in treatment response at study end point, hierarchical linear modelling of longitudinal outcome revealed a significant (p = 0.006) advantage of LMP over CPZ for the BPRS total score. Ten of 19 participants on LMP and 8 of 19 on CPZ met the criterion for treatment response, and 9 of the 18 responders did so on 200-700 mg/d phenothiazine. The mean dose of responders was 710 (standard deviation [SD] 265) mg/d (LMP) and 722 (SD 272) mg/d (CPZ). Akathisia was associated with a nonresponse to phenothiazines (p = 0.010). BPRS scores increased significantly on HAL (p = 0.006). Two of 19 participants on LMP and 5 of 19 on CPZ withdrew early from the study. CONCLUSION: LMP and CPZ may be useful in the management of TRS. A modest advantage of LMP compared with CPZ was seen in longitudinal analysis. High doses of neuroleptics may contribute to TRS; reduction of neuroleptics to modest or moderate doses should be considered before categorizing a patient as treatment resistant.
Transfer of proteins to membranes facilitates both cyanogen bromide cleavage and two-dimensional proteolytic mapping.
We have found that the transfer of gel-fractionated proteins to membranes facilitates phosphopeptide mapping. Nitrocellulose proves to be an excellent matrix for both cyanogen bromide cleavage and proteolytic digestion. Digestion of p56lck bound to a nitrocellulose membrane with cyanogen bromide or trypsin generated patterns of phosphopeptides indistinguishable from those produced by digestion of p56lck eluted from a gel. Immobilon-P and nylon membranes can also be used for proteolytic mapping, but not for cyanogen bromide cleavage. Since the use of membrane-bound protein eliminates the need for elution and precipitation of the protein, analysis is rapid. In addition, the recovery of the peptides from proteins digested on membranes is better and more consistent than it is from eluted and precipitated proteins.
[Psychoneurological requirements in evaluating the functional state of cosmonauts in flight].
Selection and training of experts-psychoneurologists to be included into a team of operational medical monitoring are described. In regards to the capacity for synonymic paraphrasing, the conditions required for stability of individual opinions and their coincidence in different people are discussed. The capacity refers to the choice of the most suitable word among a number of synonyms. On this basis it is recommended to use similarity problems in appraising the function of an expert who involves verbal description of various events.
[Peripheral nerve involvement in a 47,XYY psychotic patient. Positive lymphoblastic transformation test with myelin and levopromazine].
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[The use of different physicochemical analysis methods for proving combined poisoning by aminazine, tizertsin and amitriptyline].
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[Malignant neuroleptic syndrome in a 15-year old girl after a single injection of a high-dose neuroleptic].
The malignant neuroleptic syndrome is a rare and fatal iatrogenic syndrome which requires rapid and effective symptomatic treatment in a somatic hospital, possibly in an intensive care unit. Relatively little medicine (neuroleptics) is employed in child psychiatry and the syndrome is, therefore, rare in child psychiatric departments. A well-defined syndrome is concerned and it is important to be able to recognise and diagnose this.
[Gene localization might make it possible to prevent schizophrenia].
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[The treatment of chronic pain with psychotropic drugs].
The results of long experience with psychotropic drugs in the treatment of chronic and severe pain resistant to ordinary therapy are reported. In 103 in-patients with chronic and severe pain caused by neurological conditions and treated with a combination of thymoleptics and neuroleptics, 82% showed a marked improvement. These encouraging results are compared with the results of other studies published in this field. The pharmacological basis of this good action is briefly discussed, together with the advantages of the use of psychotropic drugs and especially the combination of thymoleptics and neuroleptics. A clearcut dosage schedule for in- and out-patients using imipramine (Tofranil) or chlorimipramine (Anafranil) and haloperidol (Haldol) is established.
[Neuroleptic malignant syndrome].
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[Phenothiazine-induced pseudolymphoma].
A 59-year-old male patient developed lymphoma-like cutaneous infiltrates on the back and left side following treatment with levomepromazine (Neurocil) over many years. Complete remission after discontinuation of levomepromazine and its replacement by a drug of another chemical class (melperone, Eunerpan) confirmed the causative role of the phenothiazine in the development of pseudolymphoma.
[Comparative effect of psychotropic agents on orienting-motor responses and cerebral Na,K-ATPase activity in vivo].
Levomepromazine, chlorpromazine (10 and 30 mg/kg), etaperaxine, haloperidol (3 and 10 mg/kg) inhibited the exploratory-motor reactions of rats and the brain Na, K-ATPase activity an hour after their administration. The effects of tranquilizers as well as of antidepressants on the exploratory reactions and on the enzyme activity were not found to stand in a clearcut relation to each other. The stimulating effect of amphethamine (3 mg/kg) was accompanied by activation and suppressive action (10 mg/kg)--by inhibition of the enzyme. It is suggested that the inhibition of the brain Na, K-ATPase activity by psychotropic drugs may play a role in the mechanism of their sedative action.