- Postoperative nausea and vomiting (PONV) in patients undergoing colorectal surgery within an institutional enhanced recovery after surgery (ERAS) protocol: comparison of two prophylactic antiemetic regimens. [Journal Article]
- KJKorean J Anesthesiol 2019 May 17
- CONCLUSIONS: The incidence of PONV remains high despite most patients receiving 3 prophylactic antiemetic medications. Perphenazine can be considered a cost effective alternative as there was no significant difference in the effectiveness for oral aprepitant or perphenazine for prophylaxis of PONV in patients undergoing CRS within an ERP.
- A Compilation of Serum Concentrations of 12 Antipsychotic Drugs in a Therapeutic Drug Monitoring Setting. [Journal Article]
- TDTher Drug Monit 2019; 41(3):348-356
- CONCLUSIONS: For each antipsychotic drug, the results presented can serve as a reference tool for pharmacokinetic interpretation of the individual patient's serum drug level. The compiled serum concentrations and the C/D ratios can support the physician's decision when individualizing dosing and determining treatment strategies for a specific patient.
- Synthesis, biological evaluation and molecular modelling studies of 1,3,7,8-tetrasubstituted xanthines as potent and selective A2A AR ligands with in vivo efficacy against animal model of Parkinson's disease. [Journal Article]
- BCBioorg Chem 2019 Mar 19; 87:601-612
- In the present study, an attempt has been made to develop a new series of 1,3,7,8-tetrasubstituted xanthine based potent and selective AR ligands for the treatment of Parkinson's disease. Antagonisti…
In the present study, an attempt has been made to develop a new series of 1,3,7,8-tetrasubstituted xanthine based potent and selective AR ligands for the treatment of Parkinson's disease. Antagonistic interactions between dopamine and A2A adenosine receptors serve as the basis for the development of AR antagonists as potential drug candidates for PD. All the synthesized compounds have been evaluated for their affinity toward AR subtypes using in vitro radioligand binding assays. 1,3-Dipropylxanthine 7a with a methyl substituent at N-7 position represents the most potent compound of the series and displayed highest affinity (A2A, Ki = 0.108 µM), however incorporation of a propargyl group at 7-positon of the xanthine nucleus seems to be the most appropriate substitution to improve selectivity towards the A2A subtype along with reasonable potency. Antiparkinsonian activity has been evaluated using perphenazine induced catatonia in rats. Most of the synthesized xanthines significantly lowered the catatonic score as compared to control and displayed antiparkinsonian effects comparable to standard drug. All the synthesized compounds were subjected to grid-based molecular docking studies to understand the key structural requirements for the development of new molecules well-endowed with intrinsic efficacy and selectivity as adenosine receptor ligands. In silico studies carried out on newly synthesized xanthines provided further support to the pharmacological results.
- The role of weight gain in explaining the effects of antipsychotic drugs on positive and negative symptoms: An analysis of the CATIE schizophrenia trial. [Journal Article]
- SRSchizophr Res 2019; 206:96-102
- Second-generation antipsychotics are associated with moderate benefits in terms of improved schizophrenia symptoms, but also with higher rates of side-effects such as excessive weight gain (WG); a co…
Second-generation antipsychotics are associated with moderate benefits in terms of improved schizophrenia symptoms, but also with higher rates of side-effects such as excessive weight gain (WG); a consensus on their efficacy has not been reached. To date, no study has evaluated the interplay of treatments and side-effects in a single framework, which is a critical step to clarify the role of side-effects in explaining the efficacy of these antipsychotics. We used recent methods for mediation and interaction to clarify the role of WG in explaining the effects of second-generation drugs on schizophrenia symptoms. We used data from 1460 participants in the CATIE trial, assigned to either perphenazine (first-generation comparison drug), olanzapine, quetiapine, risperidone, or ziprasidone. The primary outcome was an individual's score on the Positive and Negative Syndrome Scale (PANSS) for symptoms of schizophrenia after 9 months, separately evaluated as positive (PANSS+), negative (PANSS-), and total PANSS score. WG after 6 months was investigated as a potential mediator and effect modifier. Results showed that, by limiting WG, patients would benefit of a considerably better improvement in terms of PANSS symptoms. In the scenario of weight change being controlled between -2% and 1% for all participants, patients assigned to olanzapine would experience the highest significant improvements in both PANSS+ (-2.66 points; 95% CI: -4.98, -0.35), PANSS- (-1.59; 95% CI: -4.31, 1.14), and total PANSS (-6.11; 95% CI: -13.13, 0.92). In conclusion, occurrence of excessive WG hampers the potentially beneficial effects of second-generation antipsychotics, thus suggesting future directions for treatment and interventions.
- Effects of Phenothiazines on Aldehyde Oxidase Activity Towards Aldehydes and N-Heterocycles: an In Vitro and In Silico Study. [Journal Article]
- EJEur J Drug Metab Pharmacokinet 2019; 44(2):275-286
- CONCLUSIONS: The five studied phenothiazine drugs showed dual inhibitory effects on AOX activity towards aldehydes and N-heterocycles as two major classes of enzyme substrates. Most of the interactions between the phenothiazine-related drugs and AOX in the binding pocket showed a hydrophobic nature.
- StatPearls: Antipsychotic Medications [BOOK]
- BOOKStatPearls Publishing: Treasure Island (FL)
- First-generation antipsychotics are dopamine receptor antagonists (DRA) and are known as typical antipsychotics. They include phenothiazines (trifluoperazine, perphenazine, prochlorperazine, acetophe…
First-generation antipsychotics are dopamine receptor antagonists (DRA) and are known as typical antipsychotics. They include phenothiazines (trifluoperazine, perphenazine, prochlorperazine, acetophenazine, triflupromazine, mesoridazine), butyrophenones (Haloperidol), thioxanthenes (thiothixene, chlorprothixene), dibenzoxazepines (loxapine), dihydroindole (molindone), and diphenylbutylpiperidines (pimozide).
- Lamotrigine Cross-Reactivity With Phencyclidine in Rapid Urine Toxicology in a Research Study. [Case Reports]
- PCPrim Care Companion CNS Disord 2018 Jul 26; 20(4)
- Electrochemically controlled fiber-in-tube solid-phase microextraction method for the determination of trace amounts of antipsychotic drugs in biological samples. [Journal Article]
- JSJ Sep Sci 2018; 41(18):3598-3606
- In this study, a novel 'fiber-in-tube' configuration was applied to electrochemically controlled fiber-in-tube solid-phase microextraction of antipsychotic drugs (perphenazine and chlorpromazine) fro…
In this study, a novel 'fiber-in-tube' configuration was applied to electrochemically controlled fiber-in-tube solid-phase microextraction of antipsychotic drugs (perphenazine and chlorpromazine) from biological samples. To prepare an electrochemically controlled fiber-in-tube solid-phase microextraction column, first eight stainless-steel wires were placed into the stainless-steel column. Then, a nanostructured Cu-Cr-Al ternary layered double hydroxide/polythiophene coating was prepared on the inner surface of the stainless-steel tube and on the surfaces of the stainless-steel wires by a facile in situ electrodeposition method. The nanostructured coating exhibited enhanced long lifetime, good mechanical stability, high porosity, and large specific surface area compared with polythiophene and Cu-Cr-Al layered double hydroxide coatings. Under the optimal conditions, the limits of detection were in the range of 0.07-0.8 μg/L. This method showed good linearity for perphenazine and chlorpromazine in the ranges of 0.3-300 and 0.2-300 μg/L, respectively, with coefficients of determination more than 0.9982. The inter- and intra-assay precisions (RSD%, n = 3) were in the ranges of 3.0-5.1 and 2.5-4.5% at three concentration levels of 5, 25 and 50 μg/L, respectively. Finally, the method was applied for the analysis of the drugs in human urine and plasma samples.
- Aripiprazole-induced atrial fibrillation in a patient with concomitant risk factors. [Case Reports]
- ECExp Clin Psychopharmacol 2018; 26(5):509-513
- Aripiprazole is an atypical antipsychotic drug with a polypharmacological mechanism of action and a favorable tolerability profile. Its major indications are schizophrenia and mania in adults and ado…
Aripiprazole is an atypical antipsychotic drug with a polypharmacological mechanism of action and a favorable tolerability profile. Its major indications are schizophrenia and mania in adults and adolescents. Here we present the case of a 43-year-old Caucasian man with schizophrenia who developed atrial fibrillation (AF) after starting aripiprazole treatment. Prior to this treatment, he had never received any antipsychotic drugs. On admission to our inpatient unit, he showed severe psychotic symptoms and was started on aripiprazole with a rapid titration regimen (15 mg on the first day and then 15 mg twice daily thereafter) in combination with lorazepam (2.5 mg thrice a day). On the third day, the patient exhibited vomiting and an irregular pulse. An electrocardiogram (ECG) revealed new-onset AF with rapid ventricular response. Aripiprazole was discontinued and cardioversion was obtained with intravenous amiodarone. A different antipsychotic treatment was thus started (perphenazine 12 mg/d), which led to symptom remission without any relevant adverse effects. During the 2-year follow-up observation, neither psychotic symptoms nor ECG abnormalities were detected. Besides aripiprazole, other co-occurring factors might have contributed to the onset of AF in our patient, namely hypertension, low-grade diastolic dysfunction, chronic inflammatory disease, CYP2D6 polymorphism, corticosteroid and antiulcer treatment, and a family loading for myocardial infarction. In conclusion, our case study suggests that although aripiprazole has fewer cardiovascular effects than other antipsychotic drugs, in the presence of concomitant risk factors, high dose, and rapid titration regimen, regular monitoring of clinical parameters and ECG is highly recommended. (PsycINFO Database Record (c) 2018 APA, all rights reserved).
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- Drugs and Lactation Database (LactMed): Perphenazine [BOOK]
- BOOKNational Library of Medicine (US): Bethesda (MD)
- Limited information indicates that maternal doses of perphenazine up to 24 mg daily produce low levels in milk. Very limited long-term follow-up data indicate no adverse developmental effects when ot…
Limited information indicates that maternal doses of perphenazine up to 24 mg daily produce low levels in milk. Very limited long-term follow-up data indicate no adverse developmental effects when other phenothiazines are used alone. Monitor the infant for excessive drowsiness during breastfeeding and for developmental milestones, especially if other antipsychotics are used concurrently.