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PubMedDate not supplied

[Quality of life in schizophrenic patients treated with classic and "old" atypical neuroleptics].

Subjective health-related quality of life was evaluated in 100 patients from day-hospital, treated for schizophrenia with classical (perazine, perphenazine, zuclopenthixol) or "old" atypical (klozapine, sulpiride) neuroleptics. No correlation was found between the clinical improvement (PANSS scale) and the quality of life (SF-36). After the treatment the improvement of the quality of life was significantly better in female than in male patients. In women more correlations were found between clinical improvement after treatment and the of quality of life domains. The general subjective health-related quality of life after treatment with classical and "old" atypical drugs did not differ. After the treatment those patients who received classical neuroleptics reported more physical complains but better improvement in the domain "role-emotional" than the subjects treated with "old" atypical drugs. Significant clinical improvement was found in patients treated with perazine, perphenazine and zuclopenthixol but not with clozapine or sulpiride. The presence and intensity of neuroleptic side-effects did not correlate with the quality of life. In patients who had more pronounced neuroleptic side-effects less favorable improvement was found in regard to those quality of life domains which included physical status as well as the evaluation of patients' mental health.

Adult↗
PubMedDate not supplied

Spectrofluorometric determination of 2- and 10-disubstituted phenothiazines.

Spectrofluorometric method for determination of promethazine hydrochloride, thioridazine hydrochloride and perazine dimaleate in the pure form and in drugs is described. Fluorescence excitation spectra of series of aqueous solutions were measured. The fluorescence signal was found to be a linear function of the promethazine hydrochloride (PTM) concentration in the range: 0.30-20.02 ppm, thioridazine hydrochloride (TR): (0.43-21.70 ppm and perazine dimaleate (PDM): 0.85-50.60 ppm. The excitation spectra were used for determination of phenothiazine derivatives in pharmaceutical formulations such as: Diphergan, Thioridazin and Pernazinum. The influence of K+, Na+, Mg2+ i Ca2+ cations on the fluorescence intensity of phenothiazine derivatives was also studied.

Antipsychotic Agents↗
PubMedDate not supplied

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.

Animals↗
PubMedDate not supplied

Clinical and pharmacological approach to the diagnosis of paranoid schizophrenia.

The aim of the study was finding out the correlations between some clinical and biological variables in paranoid schizophrenia. The group of 16 patients with paranoid schizophrenia, chosen in careful diagnostic procedure was treated with perazine during 4 weeks time. Before and during the treatment, the following parameters: psychopathology, serum perazine and prolactin concentration, dopamine-beta-hydroxylase activity and simple reaction time were measured. We found changes of those parameters caused by the treatment. The simple reaction time retardation was side-dependent before the treatment and not side-dependent after the treatment.

Adult↗
PubMed1988

In vitro inhibition of human platelet monoamine oxidase by phenothiazine derivatives.

Nineteen phenothiazines were tested for in vitro inhibition of human platelet type B monoamine oxidase (MAO). The inhibition potency was highly dependent on structures of their side chains. The inhibition was most potent for drugs with (hydroxyethyl-piperazinyl)propyl chains followed in decreasing order by those with (N-methylpiperazinyl)propyl, (2-dimethylamino-2-methyl)ethyl and 3-dimethylaminopropyl chains. Kinetic analyses were carried out for promazine, promethazine, perazine and perphenazine as representatives of each group; the four drugs showed competitive inhibition, and Ki values of 124, 31.4, 19.2 and 22.6 microM, respectively.

Blood Platelets↗
PubMed2001

Neuroleptics normalize increased release of interleukin- 1 beta and tumor necrosis factor-alpha from monocytes in schizophrenia.

Some recent reports show that schizophrenia is accompanied by changes in lymphocyte activity. This study investigated the activity of monocytes by determining their release of interleukin- 1 beta (IL- 1 beta) and tumor necrosis factor-alpha (TNF-alpha). Monocytes were immunomagnetically isolated from the peripheral blood of schizophrenic patients before and after neuroleptic medication and stimulated by lipopolisaccharide (LPS) in vitro. The monocytes of schizophrenic patients released significantly higher amounts of IL- 1 beta and TNF-alpha than those of healthy controls. Treatment with the typical neuroleptics haloperidol and perazine decreased the release of IL- 1 beta and TNF-alpha to the control levels. The study has shown that the activity of monocytes is increased in schizophrenia and that neuroleptic treatment normalizes this activity.

Adult↗
PubMed1986

Can changes in eye-contacts predict therapeutic outcome in schizophrenic patients undergoing neuroleptic treatment? Results of a preliminary study.

The proportion of interview time spent in eye-contacts was studied before the onset of and during neuroleptic treatment in a group of 24 male schizophrenic patients. A significant increase in eye-contacts after 14 days distinguished responders to neuroleptic treatment, while a tendency towards the same effect distinguished patients treated with haloperidol from those treated with perazine. Only in the subgroup of responders was there a significant relationship between increase in eye-contacts and reduction of psychopathologic symptoms, regardless of whether these values were compared for the same treatment days or whether early changes in eye-contacts were compared with final outcome of treatment after 28 days. Since the patient subgroups were rather small, the results should still be considered preliminary. A prospective study including more parameters of visual interaction, a larger patient sample, and a longer observation period is required.

Antipsychotic Agents↗
PubMed1984

The outpatient clinic for patients under chronic lithium or neuroleptic treatment as a phase-IV research tool.

Psychiatric drug treatment often means life-long therapy Controlled long-term drug trials in psychiatric patients over periods of more than three years, however, do not exist. Organisational and ethical reasons prohibit placebo controlled or even standard drug controlled trials over periods of one decade and more. The present paper illustrates the methodology and scientific significance of well-documented long-term follow-up studies by example of the structure and scientific results of two outpatient clinics: (1) a schizophrenic outpatient clinic taking care of approximately 200 patients of whom a subgroup has been treated with perazine for now 18 years on the average; (2) a lithium clinic taking care of approximately 100 actively participating patients.--It is suggested that this kind of "naturalistic" open trials, set up in accordance with conditions normally occurring in psychiatric practice, are a necessary complement to other controlled methodologes.

Adult↗
PubMed1983

The binding of chemically different psychotropic drugs to alpha 1-acid glycoprotein.

The clinical significance of the high-affinity binding of psychotropic compounds to alpha 1-acid glycoprotein (alpha 1-AGP) in human serum has not been established yet. However, this binding may be of considerable theoretical interest since glycoproteins play a prominent role in the structure of cell membranes. In order to elucidate the nature of the binding to alpha 1-AGP several typical psychotropic compounds (diazepam, haloperidol, imipramine, perazine, phenobarbital and phenytoin) were investigated by means of equilibrium dialysis. The results suggest that among the classical CNS-drugs only those with a tricyclic structure are bound to two binding sites. Possible reason for the widely differing binding of a series of drugs are discussed in terms of their different chemical structure.

Diazepam↗
PubMed2000

Valproate as an adjunct to neuroleptic medication for the treatment of acute episodes of mania: a prospective, randomized, double-blind, placebo-controlled, multicenter study. European Valproate Mania Study Group.

To compare the efficacy of sodium valproate administered as adjunct to neuroleptic medication for patients with acute mania with the efficacy of neuroleptics alone, the authors conducted a 21-day, randomized, double-blind, parallel-group, placebo-controlled trial. The study design closely reflected a clinical psychiatric setting in Europe where patients with acute mania commonly receive neuroleptic medication. In this trial, 136 hospitalized patients met the ICD-10 criteria for acute manic episodes; these patients received a fixed dose of 20 mg/kg of body weight of sodium valproate (Orfiril, Desitin Arzneimittel GmbH, Hamburg, Germany) orally, in addition to basic neuroleptic medication, preferably haloperidol and/or perazine. The primary outcome measure was the mean dose of neuroleptic medication (after conversion into haloperidol-equivalents) for the 21-day study period. Severity of symptoms was measured using the Young Mania Rating Scale (YMRS), the Global Assessment Scale, and the Clinical Global Impression Scale. Intent-to-treat analysis was based on 69 patients treated with valproate and 67 patients who received placebo. Groups were comparable with regard to demographic and clinical baseline data. Premature discontinuations occurred in only 13% of the patients. The mean neuroleptic dose declined continuously in the valproate group, whereas only slight variations were observed in the placebo group; the difference was statistically significant (p = 0.0007) for study weeks 2 and 3. The combination of neuroleptic and valproate proved superior to neuroleptics in attempts to alleviate manic symptoms. The proportion of responders (a 50% improvement rate shown on the YMRS) was higher for the combination with valproate than for the group receiving only neuroleptics (70% vs. 46%; p = 0.005). Adverse events consisted of those known for valproate or neuroleptics; the only adverse event was asthenia, which occurred more frequently with the combination therapy. Valproate represents a useful adjunct medication for the treatment of acute manic symptoms. Valproate is beneficial because it allows the administration of fewer neuroleptic medications and produces improved and quicker remission of manic symptoms.

Acute Disease↗
PubMed2001

[Neuroleptic malignant syndrome--case report].

We have reported the case of a 65-year-old woman treated with neuroleptics because of organic delusive disturbances. She was treated for about one month with risperidone (Rispolept) and perazine (Pernazinum). Around ten days before the patient was admitted to this ward, the following had been observed: rise in temperature up to 40 degrees C, progressive weakness and blood pressure (RR) fluctuationis. Despite the applied treatment, the patient died during the fourth of hospitalization on this ward. The diagnosis of neuroleptic malignant syndrome was made on the basis of the clinical picture accomplished whole of biochemical, figurative tests as well as on the conducted differential diagnostics.

Aged↗
PubMed2005

Acute psychosis with a mediastinal carcinoma metastasis.

BACKGROUND: Reversible schizophrenia-like syndromes have been reported to occur with small-cell carcinoma of the lung, thymoma, and hematological disorders. CASE REPORT: A 56-year-old man was admitted due to an acute psychosis characterized by delusions, agitation, and aggressive outbursts. His medical and psychiatric history was unremarkable. On treatment with olanzapine, valproic acid, and perazine there was only moderate improvement. Extensive checkup revealed an isolated mediastinal metastasis of an undifferentiated carcinoma. A primary tumor was not found. After removal of the metastasis, the psychosis remitted rapidly and completely, and the patient remained well on follow-up. CONCLUSIONS: Paraneoplastic syndromes may clinically present as acute psychoses and, in late-onset schizophreniform disorders with an atypical presentation, performing a tumor search should always be considered.

Acute Disease↗
PubMed1992

[Electroconvulsive therapy in treatment of acute life threatening catatonia in toxic epidermal necrolysis (Lyell syndrome)].

Toxic epidermal necrolysis (Lyell syndrome) developed in a 43-year woman treated with carbamazepine, perazine, and sulpiride for recurrent manic bipolar disorder. Five days after withdrawal of all psychotropic medication her psychiatric illness was exacerbated and a syndrome of lethal catatonia developed which was promptly treated with unilateral electroconvulsive therapy (ECT). Rapid remission of lethal catatonia after the first ECT treatment and of her affective disorder within days was achieved. According to clinical observations of the preneuroleptic era, early improvement of lethal catatonia following ECT may have been supported by concurrent high dose corticosteroid therapy for toxic epidermal necrolysis.

Adult↗
PubMedDate not supplied

Direct effects of neuroleptics on the activity of CYP2A in the liver of rats.

The aim of the present study was to investigate the influence of classic and atypical neuroleptics on the activity of rat CYP2A measured as a rate of testosterone 7alpha-hydroxylation. The reaction was studied in control liver microsomes in the presence of neuroleptics, as well as in microsomes of rats treated intraperitoneally (i.p.) 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. Most of the neuroleptics added in vitro to control liver microsomes decreased the activity of the rat CYP2A. Chlorpromazine (Ki = 11 microM) was the most potent inhibitor of the rat CYP2A among the studied drugs, whose effect was more pronounced than that of the other tested phenothiazines (Ki = 41-83 microM), haloperidol (Ki = 190 microM) or sertindole (Ki = 78 microM). Risperidone was not active in this respect. The investigated neuroleptics when given to rats in vivo for one day or two weeks--did not produce any indirect inhibitory effect on CYP2A via other mechanisms. The obtained results show direct inhibitory effects of phenothiazine neuroleptics on the activity of CYP2A in rat liver, which may be of physiological importance for the metabolism of testosterone, considering simultaneous inhibition of CYP2C11 and CYP3A by those drugs.

Animals↗
PubMedDate not supplied

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.

Administration, Oral↗
PubMedDate not supplied

[Comparative studies of various clinical and psychopharmacological parameters of schizoaffective psychosis and paranoid schizophrenia].

Two groups of male patients were investigated: 19 subjects with diagnosis of paranoid schizophrenia and 13 with schizoaffective psychosis (8 with both depressive and paranoid symptoms, 5 with manic and paranoid). All patients were treated with perazine in this same manner. During the consecutive stages of therapy the following parameters were examined and compared: clinical symptoms, DBH activity, plasma prolactin concentration and the simple reaction time task to auditory and visual stimuli. The noticeable changes, similarities and differences were described.

Adult↗
PubMed1988

Improved high-performance liquid chromatographic method for the determination of tiotixene in human serum.

The problem of accurate determination of tiotixene in body fluids is still challenging. Several methods have been published but most of them require a tedious, time-consuming sample preparation, are not specific enough and lack the necessary sensitivity or require highly sophisticated analytical devices. As carefully validated analytical methods represent the basis of conclusive clinical trials (e.g. evaluating bioavailability/bioequivalence), an assay was developed to fulfill these needs. The method present employs an HPLC system combined with a UV-detector and uses perazine as an internal standard. The achieved lower limit of detection in serum was 0.05 ng/ml and the calibration curves were linear in the range of 0.5-20 and 0.1-2.0 ng/ml, respectively. The chromatographic peaks were well resolved and the cis-/transisomers well separated. The imprecision and inaccuracy data typically ranged from 2 to 7%; the recovery from serum was always better than 80%. The assay has been successfully used for the determination of very low tiotixene serum levels during several clinical studies.

Calibration↗
PubMed1988

High-performance liquid chromatographic determination of trans-doxepin and desmethyldoxepin.

An improved high performance liquid chromatographic (HPLC) assay for the quantitative determination of trans-doxepin (I) and desmethyldoxepin (II) in body fluids is presented. This HPLC assay, employing a UV-detector and perazine (III) as an internal standard, provides a very sensitive and selective determination in the low ng/ml range. The lower limit of quantification was 0.426 ng/ml (I) and 0.50 ng/ml (II); respectively. The calibration curve was linear in the measured range of 0.426-34.08 ng/ml (I) and 0.50-40 ng/ml (II). In combination with the excellent precision and accuracy data (c.v. values typically lower than 5%) and a recovery exceeding 90% for both compounds, the method is well suited for quantitative determinations of plasma samples generated during clinical studies, eg. evaluating the pharmacokinetics and/or bioavailability/bioequivalence as well as evaluations of clinical response.

Antidepressive Agents, Tricyclic↗