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At least 19 recordsLinked to original sources
PubMed1976

[Changes in drug elimination under the influence of perazine therapy (author's transl)].

In 8 male patients who were treated with perazine for a schizophrenic psychosis (200-800 mg/die), the elimination rate of phenazone was investigated. Simultaneously determinations of plasma levels of perazine and desmethylperazine were carried out. The average half-life of phenazone was 27.0 h in perazine-treated patients and 11.2 h in controls. Correspondingly, the clearance of phenazone decreased from 47.0 ml/min to 18.9 ml/min under perazine, both differences being highly significant. The amount of 4-OH-phenazone, the principal hydroxylated metabolite excreted in the urine, was 66 mg/24 h in the perazine group, and significantly different from the results obtained in the control group: 185 mg/24 h. In contrast the urinary excretion of the unchanged phenazone increased from 29 to 40 mg/24 h under perazine. The results are interpreted to demonstrate inhibition of drug hydroxylation in the liver by perazine treatment.

Antipsychotic Agents↗
PubMed1991

[Zotepine versus perazine in patients with paranoid schizophrenia: a double-blind controlled trial of its effectiveness].

The dibenzothiepine zotepine is a new potential "atypical" neuroleptic exhibiting powerful antiserotonergic and antidopaminergic properties. The efficacy of zotepine was evaluated in a double-blind controlled trial versus the tricyclic neuroleptic perazine in 41 patients suffering mainly from the paranoid-hallucinatory type of schizophrenia. The key outcome variable was the extent of mental disturbance as defined by the total score of the BPRS. Additional outcome variables were GAS and CGI. In addition, adverse reactions and extrapyramidal side effects were assessed according to the FSUCL scale and the Gerlach and AIMS rating scale, respectively. Additional variables recorded were blood pressure, heart rate and routine laboratory parameters as well as electrocardiogram and electroencephalogram. In the first two days, standard equivalent doses of both drugs were administered. Thereafter, doses were administered as required. The efficacy of both substances was compared after 7, 14 and 28 days of treatment. Both drugs showed a similar antipsychotic efficacy. Under zotepine treatment a 55% improvement of the BPRS total score was observed while perazine led to a 41% BPRS score reduction. After 7 days the zotepine group was significantly more improved than the perazine group, possibly due to a dosing effect in the perazine group. In the zotepine group, fewer adverse reactions and a better benefit/risk index were observed although the differences between the two treatment groups did not reach levels of statistical significance. There were no drug-specific abnormal laboratory findings. Thus, in the present study there was no significant difference between zotepine and perazine with respect to antipsychotic efficacy and side-effect rates. However, zotepine showed a trend to a better benefit/risk index at the end of treatment.

Adult↗
PubMed1978

[Relationship between perazine serum concentration and clinical results in long-term treated schizophrenic outpatients (author's transl)].

The perazine serum concentration was determined with a new gaschromatographic method in 33 schizophrenic outpatients of our psychiatric catamnestic unit who had received perazine for a period of 18 years. A very high constancy of the perazine serum level could be demonstrated by repeated measurements. A close connection existed between perazine dosage and perazine serum level. Both findings suggest a very good complicance of these patients. Serum levels were correlated positively with the intensity of the psychopathologic symptoms as well as with the frequency of side-effects, particularly with slight changes of liver enzymes.

Adolescent↗
PubMed1979

[Specific binding of perazine, a piperazine side-chain phenothiazine drug, to a serum protein (author's transl)].

A binding of perazine to a serum protein of 48 000 D was determined by gel filtration. The affinity constant of the perazine-protein complex was found to be 5.42 X 10(6) mol/l corresponding to a specific binding of 70 ng/ml serum. This result may gather clinical relevance with regard to the "CNS-bioavailability" and individual response to perazine, the average therapeutic serum concentrations having been shown to range between appr. 50 and 200 ng/ml serum. A specific binding of perazine to human or bovine albumine could not be detected.

Antipsychotic Agents↗
PubMed1977

Thin-layer and gas-liquid chromatographic procedures for the determination of perazine and its metabolites in human body fluids.

The quantitative determination of perazine, a neuroleptic drug, and its metabolites in body fluids is difficult in view of the low concentrations to be expected under therapeutic conditions as well as of the problem of convenient detectors. Different methods for extraction and measurement of perazine concentration in blood samples are discussed, with special consideration of partition coefficients and the properties of the chromatographic systems (thin-layer and gas-liquid chromatography). A new and simple method for rapid gas chromatographic determination of perazine is presented.

Antipsychotic Agents↗
PubMed1991

[Effectiveness and tolerance of zotepine in a double-blind comparison with perazine in schizophrenic patients].

40 inpatients suffering from a schizophrenia (ICD-9) were treated with either zotepine or perazin. The study was continued for a period of 28 days. Assessment of clinical efficacy was effected via BPRS, AMDP, CGI and SANS; tolerance was assessed by means of Simpson's scale. In addition, EEG, ECG and laboratory controls were conducted. The overall therapeutic efficacy was good, and it was not possible to distinguish one group from the other, i.e. both substances were equally effective, judged by means of the psychopathometric tools that were at our disposal. In 11 patients of the zotepine group and in 9 patients of the perazin group, slight extrapyramidal symptoms were observed. No clinically relevant changes were seen in EEG, ECG and laboratory controls in both groups.

Adult↗
PubMed1978

Determination of perazine serum levels by gas liquid chromatography under clinical routine conditions.

A quantitative gas liquid chromatographic method for the determination of serum levels of perazine (10-[3'-(1''-methyl-4''-piperazinyl)-propyl]-phenothiazine) is described. Perazine is used as a neuroleptic drug. The main problem consists in optimizing the chromatographic system. A sensitivity of appr. 60--150 nmol/1 (20--50 microgram/1) serum is achieved. Examples of optimization, analyses with patient samples, and the reproducibility of the results are presented.

Antipsychotic Agents↗
PubMedDate not supplied

Kinetics of drug decomposition. Part 46. Photooxidation and photolysis of some perazine derivatives.

The rate and type of the photochemical degradation of perazine derivatives in acidic aqueous solutions depends upon the nature of the substituent at C2 atom. Free perazine degrades by two parallel reactions, namely a fast reversible first-order photooxidation and a slow zero-order photolysis. An introduction of the substituent in the C2 position results frequently in the elimination of one of these reactions.

Antipsychotic Agents↗
PubMed1976

Gas-liquid chromotographic determination of perazine, thioridazine and thioridazine metabolites in human plasma.

A gas-liquid chromatographic method for the detection of perazine, thioridazine and its major metabolites in human plasma is presented. Repeated extraction, an internal standard and a temperature program with flame ionization detection make possible accurate and reproducible results with patients on therapeutic doses of these drugs. Examples of chromatograms after extraction of plasma are given.

Antipsychotic Agents↗
PubMedDate not supplied

Formation of sulfone metabolites from chlorpromazine and perazine in man.

Didesmethylchlorpromazine sulfone [gamma-(2-chlorophenothiazinyl-10)-propylamine sulfone] has been isolated from the urine of a patient under continuous chlorpromazine therapy and identified by mass spectrometry. The same compound was present in organs of rats after injection of the corresponding sulfide. The Cl-free analogue, gamma-(phenothiazinyl-10)-propylamine sulfone, was excreted by patients receiving perazine and by a volunteer after ingestion of the primary amine sulfoxide.

Adult↗
PubMedDate not supplied

Chemical characterization of decomposition products of drugs. Part 6. Mass spectrometry of some perazine derivatives.

Mass spectra of perazine, prochlorperazine, tiethylperazine, trifluperazine, butaperazine and thioproperazine were obtained. All possible fragmentation routes were discussed. The mechanism of fragmentations, their similarities and differences within the investigated group of compounds were established. The Hammett type relationship was found between the intensities of some ions and the kind of substituents at the C2 position. The utility of mass spectra for the prediction of drug stability was demonstrated.

Antipsychotic Agents↗