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Psychotropic Use during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Perphenazine, another a piperazine phenothiazine tranquilizer, is used to treat psychoses. At lower doses, it is used to treat nausea and vomiting. Birth defects were not increased in 63 infants whose mothers used perphenazine during the first trimester (Heinonen et al., 1977). Unpublished data indicated no increased frequency of birth defects in 140 infants exposed to this drug during the first trimester (Rosa, unpublished data, 1993). According to the Swedish Registry, the frequency of birth defects was not increased among 124 infants whose mothers took perphenazine during the first trimester (Kallen, 2019).
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Perphenazine is a typical antipsychotic drug of the piperazinyl phenothiazines used in the treatment of schizophrenia and manic phases of bipolar disorder (Hartung et al. 2005). Perphenazine is 10 to 15 times as potent as chlorpromazine, but it causes a high incidence of early and late extra-pyramidal side effects and tardive dyskinesia (Hartung et al. 2005). Perphenazine is primarily metabolized by CYP2D6 to N-dealkylperphenazine, perphenazine sulfoxide, and 7-hydroxyperphenazine (Figure 3.26), with the activity of the latter metabolite comparable with that of the parent in vitro (Olesen and Linnet 2000). Minor metabolic pathways may be N-oxidation and direct glucuronidation of the primary alcohol group. CYP2D6, 1A2, 3A4, and 2C19 are the most important contributors to N-dealkylation of perphenazine (Olesen and Linnet 2000). N-Dealkylperphenazine is usually present in vivo at concentrations 1.5 to 2 times that of the parent drug. In in vitro binding studies, N-dealkylperphenazine showed a higher affinity for 5-HT2A receptors than for D2 receptors to an extent comparable to that of some atypical neuroleptic agents.
MRCPsych Paper A1 Mock Examination 3: Questions
Published in Melvyn WB Zhang, Cyrus SH Ho, Roger Ho, Ian H Treasaden, Basant K Puri, Get Through, 2016
Melvyn WB Zhang, Cyrus SH Ho, Roger CM Ho, Ian H Treasaden, Basant K Puri
The following are findings from the Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE) study, except More patients taking second-generation antipsychotics continue the antipsychotic treatment compared with patients taking conventional antipsychotics.Olanzapine was the most effective in terms of the rates of discontinuation.The efficacy of the conventional antipsychotic agent perphenazine appeared similar to that of quetiapine, risperidone and ziprasidone.Olanzapine was associated with greater weight gain and increases in measures of glucose and lipid metabolism.Perphenazine was associated with more discontinuation for extrapyramidal effects.
A systematic review and meta‐analysis of maintenance treatment for psychotic depression
Published in Nordic Journal of Psychiatry, 2022
Ahmed Al-Wandi, Christoffer Holmberg, Mikael Landén, Axel Nordenskjöld
The optimal duration of maintenance treatment following remission is unclear. Rothschild et al. suggested that the majority of patients with psychotic unipolar depression do not need treatment with AP for more than 4 months [20]. This notion is based on a small uncontrolled study in which 30 patients with psychotic unipolar depression who had achieved remission were treated with fluoxetine and perphenazine for 3 months (plus 1 month of acute treatment). After that, the dose of perphenazine was tapered-off; 22/30 patients remained well until the end of the study 11 months later. The remaining 8/30 patients showed signs of impending relapse within 2 months of the tapering. All patients regained remission when perphenazine treatment was reinstated. When a new attempt was made to taper-off perphenazine, 3/8 patients once more presented with symptoms of impending relapse. On the other hand, a study by Naz et al. indicated that a high proportion of relapses may occur after 1 year, whether patients are obtaining treatment or not [21]. In their study, 60 patients who had achieved remission after an episode of psychotic unipolar depression were followed-up for 4 years, during which 26 patients relapsed. The median time for relapse was 50.0 weeks (interquartile range: 30.3–78.6 weeks). The authors concluded that treatment after achieving remission was not significantly associated with time-to-relapse. Since the optimal duration of maintenance treatment is not known, we suggest that future studies adhere to the protocol of Flint et al. with a follow-up time of at least 36 weeks.
Preparation, characterization, and in vivo evaluation of perphenazine-loaded nanostructured lipid carriers for oral bioavailability improvement
Published in Drug Development and Industrial Pharmacy, 2021
Zahra Saghafi, Mojdeh Mohammadi, Mohammad Mehdi Mahboobian, Katayoun Derakhshandeh
Perphenazine was obtained from Daroupakhsh Pharmaceutical Co. (Tehran, Iran). Amitriptyline (AT) was gifted from Arasto Pharmaceutical Chemicals Inc. (Tehran, Iran). Poloxamer 188 was purchased from Alfa Aesar A Johnson Matthey Co. (London, UK). Glyceryl monostearate 900 K and dynasan 118 were generous gifts from IOI Oleochemical Pharma Co. (Witten, Germany). Oleic acid was provided by Samchun Pure Chemicals Co., Ltd. (Seoul, Korea). Ammonium acetate was purchased from m Carlo Erba Reagents (Milan, Italy). Trichloroacetic acid, HPLC grade methanol, and acetonitrile were purchased from Merck (Darmstadt, Germany). Ultrapure water from a Millipore Direct-Q® 3 UV water purification system (Billerica, MA) was used throughout all experiments. All other reagents and chemicals were of analytical grade and used without further purification.
Pharmacokinetics and brain distribution studies of perphenazine-loaded solid lipid nanoparticles
Published in Drug Development and Industrial Pharmacy, 2021
Parnian Mohammadi, Reza Mahjub, Mojdeh Mohammadi, Katayoun Derakhshandeh, Ali Ghaleiha, Mohammad Mehdi Mahboobian
Perphenazine (PPZ) is a typical antipsychotic belonging to the class II of the biopharmaceutics classification system (BCS). This drug shows poor solubility and high permeability properties. PPZ is mainly prescribed for schizophrenia management and treating other psychiatric conditions like anxiety and manic episodes. The mechanism of action of PPZ is related to the postsynaptic dopamine 2 (D2) receptors blockade and lowering the excessively released dopamine neurotransmitter in the brain. By this mechanism, it reduces the positive symptoms of schizophrenia [6,7]. PPZ has an aqueous solubility of less than 100 µg/ml. The high lipophilicity of the PPZ molecule makes it barely dissolvable in the intestinal lumen, the main site of absorption, leading to a low bioavailability following the oral administration [8]. PPZ has an extensive hepatic first-pass metabolism and a variable systemic bioavailability [9].