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At least 109 records · Page 6Linked to original sources

Evaluation of long-term sedation in cheetah (Acinonyx jubatus) with perphenazine enanthate and zuclopenthixol acetate.

Two long-acting neuroleptics were used to tranquilize nine captive cheetahs (Acinonyx jubatus). Perphenazine enanthate (3.0 mg/kg) and zuclopenthixol acetate (0.6 mg/kg) were each administered to separate groups of three cheetahs in a double blind trial. Both products were administered together to a third group of three animals at the same dosages. Behavioral effect, duration of effect, and possible side effects were observed by a predefined protocol. Under standardized holding conditions, the cheetahs were observed 5 days before drug administration and 14 days after administration. Daily activity was defined and statistically evaluated by a U-test. A significant reduction of activity was observed after administration in all three trials. Zuclopenthixol acetate at 0.6 mg/kg alone and in combination with perphenazine enanthate caused inappetence, ataxia, extra pyramidal reactions, akathisia, and prolapse of the third eyelid. Zuclopenthixol acetate should not be used in cheetahs. Perphenazine enanthate did not cause inappetence, reduced appetite, or any of the previously mentioned side effects when used alone. It produced satisfactory tranquilization and is suitable and safe for cheetahs at 3.0 mg/kg. This dosage should be varied depending on health, age, and temperament of the individual cheetah.

Acinonyx↗

Effect of hypothalamic implantation of perphenazine on milk yield in goats.

The effects of perphenazine on galactopoiesis were studied in 52 goats in the phase of declining lactation (September-December). At the beginning of September, perphenazine (1 mg) was stereotaxically implanted into the hypothalamus, sham-implantations being performed on control animals. After the operation milk yield decreased and stabilized at a new starting level in most animals of both groups. The average weekly milk yield of the sham-implanted goats gradually fell during the experimental period. This progressive decline in yield was greatly reduced if perphenazine had been implanted in the median eminence (ME). No galactopoietic effects were observed when the implantation was localized outside the ME.

Animals↗

Comparison of the effect of the R2 phenothiazine ring substituent on fluphenazine and perphenazine interactions with cyclodextrins.

The effect of -CF3 R2 fluphenazine (FLF) and -Cl R2 perphenazine (PF) substituents on interactions of these phenothiazine derivatives with cyclodextrins (CD) was compared. Inclusion complexes of protonated and basic forms of FLF and PF with CDs were obtained in HCl 0.01 mol/L (pH 1.9 or 2.1), in phosphate buffer (pH 5.8) and in Britton-Robinson's buffer (pH 10.2) solutions and studied using spectral method. It was established. that the uncharged forms of both phenothiazine derivatives interact with CDs stronger than protonated molecules and that the perphenazine-CD inclusion complexes characterize greater apparent stability constants in comparison to adequate fluphenazine complexes. The thermodynamic parameters, estimated from linear Van't Hoff plot, suggest that the van der Waals forces accompanied by hydrophobic effects were operating in the investigated FLF-CD and PF-CD systems. The effect of pH and presence of CD on photostability of FLF or PF was also compared. The photochemical decomposition of both phenothiazine derivatives, in the absence and in the presence of CDs, proceeds according to the first order reaction. It was also established that independent on the charge of molecule, perphenazine was more stabile than fluphenazine and that the inclusion complexation with CDs improved the photostability of both drugs. The data of 2D NMR analysis suggest, that the aromatic portion of FLF and PF molecules, without R2 substituent, tend to the interior of CD.

Antipsychotic Agents↗

[Results of treatment of schizophrenic and schizoaffective patients with sulpiride (Eglonyl Alkaloid) in comparison with perphenazine (Perfenazin Spofa)].

In a three-week crossover controlled the authors administered alternately sulpiride and perphenazine with an intermittent placebo interval, to 40 hospitalized patients with acute exacerbation of schizophrenic and schizoaffective psychosis. According to evaluation recommended by Serejský significantly more complete remissions type AB were achieved especially in schizodepressive patients given sulpiride. The global score of BPRS and FKP scales after administration of the two tested neuroleptic drugs differed: sulpiride had a more favourable effect on depression, emotional withdrawal, reduced affectivity, slower motor activity, worry about the somatic state and hallucinations, while perphenazine gave better results in patients with reduced compliance, lack of cooperation, hostility and excitation. Sulpiride is well tolerated by the patients. Pharmacological parkinsonoid was observed only in cca half the patients, as compared with perphenazine and therefore also the need of correction by antiparkinsonian drugs was significantly smalled. The low incidence of extrapyramidal, hypnosedative and autonomous undesirable effects gave sulpiride the optimal position in our classification of 16 tested neuroleptic drugs. In one third of the patients no undesirable side--effects were observed.

Adolescent↗

Effect of different neuroleptics in tardive dyskinesia and parkinsonism. A video-controlled multicenter study with chlorprothixene, perphenazine, haloperidol and haloperidol + biperiden. Nordic Dyskinesia Study Group.

Thirty-three chronic psychiatric patients with tardive dyskinesia (TD) were included in a video-controlled multicenter study of the effect of chlorprothixene, perphenazine, haloperidol and haloperidol + biperiden in TD and parkinsonism. The drugs were given in a cross-over design in randomized order in dosages equipotent to the earlier neuroleptic treatment and administered for periods of 6 months with 6-week placebo periods before and after. A total of 55 treatment periods were completed; only seven patients were able to go through all three treatment phases (= 96 weeks). Perphenazine (20.5 mg/day), haloperidol (5.5 mg/day), and haloperidol (11 mg/day) + biperiden (7 mg/day) induced a moderate suppression of TD and at the same time produced a corresponding aggravation in parkinsonism. Chlorprothixene (142 mg/day) had only a slight TD reducing effect and did not change parkinsonism. Thus the TD suppressing effect was inversely related to the parkinsonian-inducing effect of the neuroleptics. Following withdrawal of the drugs, TD increased in some cases and decreased in others compared to the pretreatment level. No significant correlation was found between the intensity of the withdrawal TD and either drugs or preceding parkinsonism or TD suppression. Only in a subgroup of seven patients who consecutively received all three neuroleptics, perphenazine, but not haloperidol and chlorprothixene, produced a post-treatment aggravation which was correlated to the parkinsonsim and TD suppression during treatment. Independent of the neuroleptic given, the TD intensity increased significantly from the first to the third placebo period. This suggests that drug holidays are inappropriate to prevent TD induction/aggravation.

Adult↗

Dopaminergic antagonists potentiate the adenohypophyseal growth reaction to oestrogen: thioridazine is less effective than perphenazine.

The injection of oestradiol benzoate as an aqueous microcrystal suspension, in a dose of 1 mg twice a week, evokes a marked adenohypophyseal growth reaction in male rats. The reaction is potentiated by dopaminergic antagonists from the group of neuroleptics (specifically perphenazine and thioridazine). Elicitation of the same adenohypophyseal reaction required twice as much thioridazine (10 mg/rat per day) as perphenazine. Thyroxine inhibited the adenohypophyseal growth reaction to oestradiol. The serum polyphenol oxidase (ceruloplasmin) level rose after oestradiol and perphenazine and thioridazine slightly potentiated the increase.

Animals↗

[Treatment of Sydenham's chorea with perphenazine].

Symptomatic therapy in Sydenham's chorea has not been satisfactory. Perphenazine was tested as an alternative to diminish abnormal movements. A Syndenham's chorea comparative double-blind study (17 patients) using it, with reserpine and placebo as controls, was designed. Perphenazine was tried also in another open-study (13 patients with Syndenham's chorea). Out of the 2 groups, those which received perphenazine improved earlier and in a greater proportion than controls, with statistical significance (p is less than 0.01).

Adolescent↗

The influence of cyclizine and perphenazine on the emetic effect of meptazinol.

The effectiveness of 50 mg cyclizine and 2.5 mg perphenazine against the emetic sequelae of 100 mg meptazinol were studied in a randomized double-blind placebo-controlled trial. Three groups of 40 women received the opioid, together with an anti-emetic by i.m. injection, as premedication prior to minor gynaecological surgery. Beneficial or noxious effects were noted at standard time intervals and anaesthesia standardized as incremental methohexitone with nitrous oxide/oxygen. In the placebo group, 33 out of 40 subjects experienced either nausea or vomiting at some time after the opioid. Cyclizine, 50 mg, provided significant reduction of emetic tendency in both pre-operative and post-operative phases of the study with 22 out of 40 subjects experiencing nausea or vomiting overall. Perphenazine, 2.5 mg, showed no useful anti-emetic effect. Both anti-emetics increased the soporific effect of premedication at the 90-min interval. Subjects receiving perphenazine experienced significantly more dizziness than those of other groups.

Azepines↗

Dopaminergic modulation of the adenohypophyseal reaction to oestradiol: interaction of perphenazine with the thyroid hormones.

In male and female rats, oestradiol raises adenohypophyseal weight, the thyroxine-binding capacity of the adenohypophyseal proteins and the blood ceruloplasmin (polyphenol oxidase) level and reduces the ascorbic acid concentration in the hypothalamus. Simultaneous administration of the thyroid hormones inhibits all these reactions. The simultaneous administration of perphenazine (a dopaminergic neurone inhibitor) potentiates the adenohypophyseal and ceruloplasmin reaction, but does not modify the hypothalamic ascorbic acid reaction. Perphenazine combined with the thyroid hormones blocks the latters' inhibitory effect on the adenohypophyseal, ceruloplasmin and hypothalamic ascorbic acid reaction to oestradiol. The possible mechanisms by which perphenazine blocks the inhibitory effect of the thyroid hormones are discussed.

Animals↗

[The effect of serum monitoring on concentration of perphenazine and zuclopenthixole].

The effect of therapeutic drug monitoring (TDM), including pharmacokinetic guidance, was examined in 994 psychiatric patients treated with perphenazine (Trilafon) or zuclopentixol (Cisordinol). Before monitoring of the serum level, half of the serum concentrations from patients given perphenazine tablets (466 patients) was below the therapeutic level, and about one third was above. For perphenazine depot (208 patients), almost no patients had a serum concentration below the therapeutic level whereas 40% had concentrations above. For zuclopentixol tablets (231 patienter) and zuclopentixol depot (163 patients), about 60% of the patients had concentrations above the therapeutic level. For all four groups, it was found that slightly more than half of the patients with serum concentrations outside the therapeutic level was reexamined. The dosage was changed in most of these patients (80-90%) in order to bring the concentration within the therapeutic level. Half of those in whom the dose was changed obtained concentrations within the therapeutic level. It is concluded that since the recommendations for changes of the dosage is followed to a wide extent, the therapeutic drug monitoring service does influence the treatment significantly.

Clopenthixol↗

Some endocrine effects of two phenothiazine derivatives, chlorpromazine and perphenazine, in the female mouse.

The effects of chlorpromazine and perphenazine were studied with both immature and mature female mice. At a dose of 5 mg/kg daily, each drug delayed the onset of sexual maturity in immature animals. In mature mice, a daily dose of 10 mg/kg inhibited vaginal oestrus and reduced the weights of the ovaries, vagina and uterus. Each of the two drugs inhibited ovarian hypertrophy following unilateral ovariectomy, but only slightly diminished the responses to exogenous oestrogen and to exogenous gonadotrophin. In one experiment, pseudopregnancy, as shown by a positive deciduoma-test, was provoked by perphenazine, but this experiment could not be repeated. Chlorpromazine failed to evoke a positive deciduoma response. At a dose of 10 mg/kg, neither drug caused a fall in levels of adrenal ascorbic acid. In the rat, treatment for 1 week with 10 mg/kg daily of either drug led to a rise in pituitary gonadotrophic activity. It was concluded that both drugs inhibited the release of gonadotrophins by the pituitary gland, independently of any action in releasing corticotrophin.

Animals↗

A long-term cross-over pharmacokinetic study comparing perphenazine decanoate and haloperidol decanoate in schizophrenic patients.

The purpose of the study was to investigate clinical and pharmacokinetic parameters concerning perphenazine decanoate (PD) and haloperidol decanoate (HD) with an interval of 3 weeks during a study period of 51 weeks. This was done by using the available drug preparations in chronic schizophrenic patients in a randomised, double-blind, cross-over, multicentre study. In addition, an elimination phase of 6 weeks was added, when no IM injections of the depot drugs were given. Twenty-nine patients in a stable neuroleptic maintenance phase entered the study. The patients were rated during the trial according to the CPRS-SCHZ and CGI scales, the UKU side effect scale and serum concentrations of the drugs and prolactin were monitored. There was no significant difference between the drugs in antipsychotic efficacy or side effects. Thus, the doses were equipotent with regard to the CPRS-SCHZ scores. However, the patients' global improvement rating was higher for PD (52%) than for HD (39%) (P > 0.05). The elimination of both drugs was very slow. No interaction effects between PD and HD were observed. The serum levels of HD were in most patients lower than those recommended for acute-subacute treatment. The mean doses were 117 mg (0.29 mmol), range 20-313 mg PD and 120 mg (0.32 mmol), range 20-350 mg HD. The serum concentrations in nmol/L of perphenazine and haloperidol (week 24) were 0.8-15.9 and 2.3-46.7, respectively.

Adult↗

Comparison of lorazepam alone vs lorazepam, morphine, and perphenazine for cardiac premedication.

PURPOSE: To compare the effects of two premedication regimens on cardiorespiratory variables, sedation, and anxiety in patients scheduled for coronary artery bypass graft (CABG) surgery. METHODS: This was a prospective randomized, double-blind clinical trial. Sixty-eight patients were monitored for 1.5 hr before and 2.0 hr after premedication with lorazepam (0.03 mg.kg-1 sl), morphine (0.15 mg.kg-1 im), and perphenazine (0.05 mg.kg-1 im) [Group 1], or with lorazepam (0.03 mg.kg-1 sl) and saline (1.5 ml im) [Group 2]. All were continuously monitored with a 12-lead ECG ST monitors, respiratory inductive plethysmography (RIP), digital pulse oximetry, intra-arterial blood pressure, and arterial blood gas analysis. Sedation and anxiety scores were also recorded. RESULTS: The incidence and duration of myocardial ischaemia was low and similar in Groups 1 and 2. Patients in Group 1, but not in Group 2, had a greater number of events (P < 0.04) and duration (P < 0.02) of O2 desaturation; higher PaCO2 (P < 0.001), and more haemodynamic events (P < 0.006) after premedication when compared with baseline. There was no difference in RIP or ECG variables between the two groups. Following premedication, both groups reported reduced anxiety scores and elevated sedation scores (P < 0.01), with sedation greater in Group 1 than in Group 2 (P < 0.01). CONCLUSION: In CABG patients, premedication with lorazepam provides adequate anxiolysis and sedation, and the addition of morphine and perphenazine results in elevated PaCO2, arterial haemoglobin desaturation, and potentially adverse haemodynamic changes.

Aged↗

Electrophysiologic studies of perphenazine and protriptyline in a patient with psychotropic drug-induced ventricular fibrillation.

A 51 year old woman sustained ventricular fibrillation while receiving perphenazine and protriptyline. After successful resuscitation and clinical stabilization, cardiac electrophysiologic studies were performed before and after the administration of each of these medications. Perphenazine widened the ventricular echo zone and facilitated induction of short salvoes of ventricular tachycardia (repetitive ventricular response). Protriptyline also widened the ventricular echo zone and allowed easy induction of long runs of ventricular tachycardia. Both psychotropic agents increased the incidence of ventricular dysrhythmias in this patient. The electrophysiologic study is a useful technique in determining the interaction between psychotropic drugs and life-threatening arrhythmias; it may provide a means of identifying the patients with cardiac disease in whom administration of these agents may be fatal.

Major Depressive Disorder↗

Kinetic spectrophotometric method for determination of perphenazine based on monitoring the oxidation intermediate by applying a stopped-flow technique.

A novel and high-sensitive stopped-flow kinetic spectrophotometic method for the determination of perphenazine based on monitoring the variation of absorbance of the intermediate within a few seconds has been developed. The optimum conditions for various parameters on which the forming of the intermediate depends, were investigated. It was found that the initial reaction rate increased linearly with an increase in the perphenazine concentration in the range from 1.0 x 10(-5) to 1.6 x 10(-4)M. The detection limit was calculated to be 5.3 x 10(-6)M. The kinetics of the reaction was established by the aid of single-mixing or double-mixing stopped-flow techniques, a successive reaction model was proposed to analyze and simulate the reaction. The influence of both ascorbic acid and NADH on the time courses was also investigated.

Ascorbic Acid↗

Anodic coulometric detection with a glassy carbon electrode in combination with reversed-phase high-performance liquid chromatography. Determination of blood levels of perphenazine and fluphenazine.

A detector for liquid chromatography, based on anodic electrochemical oxidation at a glassy carbon electrode, is used in combination with reversed-phase liquid chromatography for the determination of the long-acting tricyclic psychotropic drugs fluphenazine and perphenazine in blood. Completely porous microparticulate silica material, modified so as to give a methyl silica, was used as the stationary phase and buffered mixtures of methanol and water as the mobile phase. The low detection limit and the selectivity of the coulometric detector made possible the determination of concentrations of 1-20 ppb of the compounds of interest. An extraction procedure was in order to obtain sufficient selectivity. Data for the precision, detection limit and yield of the extraction procedure are given. A number of serum levels of perphenazine after oral administration and of fluphenazine after i.m. doses of fluphenazine decanoate are stated.

Carbon↗

Simultaneous dissolution profiles of two drugs, sulfadiazine-trimethoprim and amitriptyline-perphenazine, in solid oral dosage forms by a FIA manifold provided with a single spectrophotometric detector.

The simultaneous determination of two dissolution profiles wih the aid of a flow injection analysis assembly has been applied to: (a) sulfadiazine-trimethoprim in tablets and (b) amitriptyline-perphenazine in sugar coated pills. The selected combinations are drugs which have overlapping UV-vis spectra. The officially proposed procedure from the pharmacopoeias has been adapted for the FIA methodology and derivative spectrophotometry and zero crossing. Preliminary experiments on the suitability of the simultaneous determination of both drugs were performed. The empirical profiles were adjusted by regression analysis using different approaches. The 3-parameter plot method was finally selected as the most suitable for the sulfadiazine-trimethoprim and the 4-parameter equation plot for amitriptyline-perphenazine.

Administration, Oral↗

Immediate effects of chlorpromazine and perphenazine following neuroleptic washout on word association of schizophrenic patients.

Reaction time and idiosyncrasy of word associations were examined in 30 schizophrenic patients, 2 h after administering a single dose of chlorpromazine, perphenazine or placebo. These patients were in the acute phase of their illness following 72 h cessation of oral neuroleptic treatment administered for 1-2 weeks. There was a statistically significant reduction in reaction times after administering perphenazine as compared to the placebo. Chlorpromazine showed some reduction in reaction times that was not statistically significant. Further study is needed to examine the relationship between such changes and other parameters, such as the patients' symptomatology and their social competence. Since many schizophrenic patients exhibit low or partial compliance, including patterns of intermittent taking of medication with a few days cessation, studies using such a model of a single dose of neuroleptic following several days withdrawal, may have clinical relevance. Another finding was a correlation between reaction time and the number of uncommon word associations produced. This correlation was beyond drug effect. Further study is needed to find out if such a correlation characterizes schizophrenic patients only.

Adolescent↗