- |||||||||| Trintellix (vortioxetine) / Lundbeck, Takeda, Dopergin (lisuride) / Bayer
Journal: DReAmocracy: A Method to Capitalise on Prior Drug Discovery Efforts to Highlight Candidate Drugs for Repurposing. (Pubmed Central) - May 25, 2024
Top-scored drugs for Alzheimer's Disease include agomelatine, mirtazapine and vortioxetine; for Parkinson's Disease, they include apomorphine, pramipexole and lisuride; for Huntington's, they include chlorpromazine, fluphenazine and perphenazine; and for Multiple Sclerosis, they include zonisamide, disopyramide and priralfimide. Overall, DReAmocracy is a methodology that focuses on leveraging the existing drug-related experimental and/or computational knowledge rather than a predictive model for drug repurposing, offering a quantified aggregation of existing drug discovery results to (1) reveal trends in selected tracks of drug discovery research with increased resolution that includes modes of action, targeted pathways and initial indications for the investigated drugs and (2) score new candidate drugs for repurposing against a selected disease.
- |||||||||| perphenazine / Generic mfg., fluphenazine / Generic mfg.
Thermal analysis of liquid state perphenazine and fluphenazine drugs | Poster Board #2204 (In-person; Poster Board #2204; Hall C (Ernest N. Morial Convention Center)) - Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_4858;
The compounds were synthesized by using known strategies (acid-base or metathesis reactions) and their identity and purity was determined using NMR spectroscopy. Their thermal behavior (melting points and/or glass transitions and decomposition temperatures) were determined using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA).
- |||||||||| lithium carbonate ER / Generic mfg.
Trial termination, HEOR: Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies (clinicaltrials.gov) - Feb 15, 2024
P=N/A, N=1037352, Terminated,
These data may reflect inappropriate prescribing practices in US nursing homes, and their association with 6-month mortality warrants further investigation. Completed --> Terminated; Per PI, this study is not a clinical trial and was inadvertently entered in the system
- |||||||||| perphenazine / Generic mfg., fluphenazine / Generic mfg.
Journal: Bile Is a Selective Elevator for Mucosal Mechanics and Transport. (Pubmed Central) - Dec 5, 2023
Drugs that interacted with bile also interacted with mucin but not vice versa. This study detailed the dynamics of mucus biomechanics under bile exposure and linked the ability of a drug to interact with bile to its abbility to interact with mucus.
- |||||||||| perphenazine / Generic mfg.
Trial completion date, Trial primary completion date: Evaluation of D3 Receptor Occupancy Using FLUORTRIOPRIDE ([18F]FTP) PET/CT (clinicaltrials.gov) - Jul 20, 2023
P1/2, N=30, Active, not recruiting,
The pathogenesis of depression is closely related to inflammation. Trial completion date: Jun 2023 --> Jun 2024 | Trial primary completion date: Jun 2023 --> Jun 2024
- |||||||||| lamotrigine liquid oral suspension / OWP Pharma
Seizures or Neuroleptic Malignant Syndrome: A Diagnostic Dilemma (Hall B Foyer, Exhibition Level Moscone South) - May 17, 2023 - Abstract #APA2023APA_864;
She has been on perphenazine 8 mg in the morning and and noon and 16 mg in the evening, aripiprazole 30 mg daily for schizophrenia and lamotrigine 100 mg in the morning and 125 mg in the evening and valproic acid 250 mg three times a day for seizures...However, once dantrolene 1 mg/kg was given, her rigidity relatively improved, possibly pointing towards a neuroleptic malignant syndrome despite its atypical presentation...Seizures arising from the occipital lobe, occipitotemporal, and occipitoparietal regions of the cortex are often epileptic hallucinations.The appearance of visual hallucinations during these 'shaky', seizure-like episodes does not necessarily preclude an epileptic cause of the hallucinations. Patient was advised to follow up with her outpatient psychiatrist for consideration of antipsychotic monotherapy rather than antipsychotic polypharmacy to avoid future possibilities of repeat neuroleptic malignant syndrome.
- |||||||||| Lodopin (zotepine) / Astellas
Retrospective data, Review, Journal: Long-term efficacy of antipsychotic drugs in initially acutely ill adults with schizophrenia: systematic review and network meta-analysis. (Pubmed Central) - May 9, 2023
In terms of overall symptoms, olanzapine was on average more efficacious than ziprasidone (standardized mean difference, SMD=0.37, 95% CI: 0.26-0.49), asenapine (SMD=0.33, 95% CI: 0.21-0.45), iloperidone (SMD=0.32, 95% CI: 0.15-0.49), paliperidone (SMD=0.28, 95% CI: 0.11-0.44), haloperidol (SMD=0.27, 95% CI: 0.14-0.39), quetiapine (SMD=0.25, 95% CI: 0.12-0.38), aripiprazole (SMD=0.16, 95% CI: 0.04-0.28) and risperidone (SMD=0.12, 95% CI: 0.03-0.21)...The differences between olanzapine and lurasidone, amisulpride, perphenazine, clozapine and zotepine were either small or uncertain...Concerning weight gain, the impact of olanzapine was higher than all other antipsychotics, with a mean difference ranging from -4.58 kg (95% CI: -5.33 to -3.83) compared to ziprasidone to -2.30 kg (95% CI: -3.35 to -1.25) compared to amisulpride. Our data suggest that olanzapine is more efficacious than a number of other antipsychotic drugs in the longer term, but its efficacy must be weighed against its side effect profile.
- |||||||||| Review, Journal: The role of phenothiazine derivatives in autophagy regulation: A systematic review. (Pubmed Central) - Mar 21, 2023
The final effect depends on the used concentration as well as the cell line. A further investigation of the mechanisms of autophagy regulation by phenothiazine derivatives is required to understand the biological actions, and to increase the therapeutic potential of this class of drugs.
- |||||||||| Review, Journal: Global occurrence and aquatic hazards of antipsychotics in sewage influents, effluent discharges and surface waters. (Pubmed Central) - Jan 17, 2023
In contrast, we observed elevated aquatic hazards for chlorpromazine (30.5%), aripiprazole (37.5%), and perphenazine (68.7%) in effluent discharges, and for chlorprothixene (35.4%) and flupentixol (98.8%) in surface waters. Elevated aquatic hazards for relatively understudied antipsychotics were identified, which highlight important data gaps for future environmental chemistry and toxicology research.
- |||||||||| perphenazine / Generic mfg., chlorpromazine / Generic mfg.
Review, Journal: Phenothiazines and their Evolving Roles in Clinical Practice: A Narrative Review. (Pubmed Central) - Nov 26, 2022
Low/mid potency phenothiazines such as chlorpromazine antipsychotic drugs that have been used to treat schizophrenia and schizophrenia-like disorders since the 1950s and are utilized in numerous disease states. The present investigation aims to elucidate the effects of phenothiazines in clinical practice.
- |||||||||| perphenazine / Generic mfg., nortriptyline / Generic mfg.
Journal: Synthesis and preliminary biological evaluation of gabactyzine, a benactyzine-GABA mutual prodrug, as an organophosphate antidote. (Pubmed Central) - Nov 4, 2022
The combined release of both compounds in the brain offers several advantages over the current OP poisoning treatment protocol: improved efficacy and safety profile (where the inhibitory properties of GABA are expected to counteract the anticholinergic cognitive adverse effects of benactyzine) and enhanced chemical stability compared to benactyzine alone. We present here preliminary results of animal studies, showing promising results with early gabactyzine administration.
- |||||||||| perphenazine / Generic mfg.
Journal: Rapid 18F- and 19F-Difluoromethylation via Desulfurative Fluorination of Transient N-, O-, and C-Linked Dithioles. (Pubmed Central) - Nov 2, 2022
We also introduce the 5,6-dimethoxy-1,3-benzodithiole (DMBDT) function, which undergoes sufficiently rapid desulfurative fluorination to additionally support 18 F-difluoromethylation. This new process is compatible with the wide range of functional groups typically encountered in medicinal chemistry campaigns and the use of [ 18 F]AgF is demonstrated in the production of 18 F-labelled derivatives of testosterone, perphenazine, and melatonin,58.0+/-2.2, 20.4+/-0.3 and 32.2+/-3.6 MBq/umol, respectively. We expect the DMBDT group and this 18 F/ 19 F-difluoromethylation process will inspire and support new efforts in medicinal and agrochemistry and radiotracer production.
- |||||||||| perphenazine / Generic mfg.
PK/PD data, Preclinical, Journal: Bile and excipient interactions directing drug pharmacokinetics in rats. (Pubmed Central) - Sep 12, 2022
Polymer-induced changes of bile colloids, e.g., by Eudragit E, reduced the flux of the bile interacting drug Perphenazine whereas bile non-interacting Metoprolol was not impacted...This study confirms the necessity to carefully select polymers for bile interacting drugs whereas non-bile interacting drugs are more robust in terms of excipient choice for formulation. The perspective of bile interaction may introduce interesting biopharmaceutical leverage for better performing oral formulations of tomorrow.
- |||||||||| perphenazine / Generic mfg., paroxetine / Generic mfg., quetiapine / Generic mfg.
Journal: Electroconvulsive Therapy (ECT) in Neuroleptic Malignant Syndrome (NMS) on an Intensive Care Unit (ICU) (Pubmed Central) - Jul 13, 2022
It was not until day 9 that a psychiatric consultation was undertaken, under the suspected diagnosis of NMS. On the same day ECT was performed, followed by a rapid remission of all clinical features and laboratory findings. Early consideration and application of ECT treatment for NMS on an ICU is life-saving.
- |||||||||| perphenazine / Generic mfg.
Trial completion date, Trial primary completion date: Evaluation of D3 Receptor Occupancy Using FLUORTRIOPRIDE ([18F]FTP) PET/CT (clinicaltrials.gov) - Jul 7, 2022
P1/2, N=30, Active, not recruiting,
Early consideration and application of ECT treatment for NMS on an ICU is life-saving. Trial completion date: Jun 2022 --> Jun 2023 | Trial primary completion date: Jun 2022 --> Jun 2023
- |||||||||| Zyprexa Relprevv (olanzapine pamoate long-acting injection) / Eli Lilly
Journal: Optimal Doses of Specific Antipsychotics for Relapse Prevention in a Nationwide Cohort of Patients with Schizophrenia. (Pubmed Central) - Jun 24, 2022
Our results suggest that olanzapine LAI is highly effective in dose ranges >0.9 DDD/day, and especially at 1.4-<1.6 DDDs/day (405 mg/4 weeks) associated with substantially lower risk of rehospitalization than any dose of any other antipsychotic. The current WHO standard dose definitions appear to be clearly too high for perphenazine and somewhat too high for risperidone.
- |||||||||| perphenazine / Generic mfg., prochlorperazine maleate / Generic mfg.
Journal: Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels. (Pubmed Central) - May 10, 2022
The results suggested that perphenazine and prochlorperazine may modulate the expression levels of multidrug resistance proteins (they decreased ABCB1 and increased ABCG2 expression), E-cadherin, α-tubulin and integrins, and could impair the migration and invasion of U-87 MG cells. In conclusion, the decrease in migratory and invasive ability following treatment with phenothiazine derivatives due to the increase in ABCG2 and E-cadherin expression, and decrease in α-tubulin and integrins expression, may suggest that research on perphenazine and prochlorperazine in the treatment of glioblastoma is worth continuing.
- |||||||||| Nitredon (nitrazepam) / Remedica
Journal: Development of an Analytical Method for Detection of Anesthetics and Sedatives in Fish. (Pubmed Central) - Apr 30, 2022
In conclusion, the decrease in migratory and invasive ability following treatment with phenothiazine derivatives due to the increase in ABCG2 and E-cadherin expression, and decrease in α-tubulin and integrins expression, may suggest that research on perphenazine and prochlorperazine in the treatment of glioblastoma is worth continuing. The most effective QuEChERS pretreatment method and conditions of LC-MS/MS for the analysis of anesthetics and sedatives in fish were established.
- |||||||||| Adempas (riociguat) / Bayer, Merck (MSD)
Trial completion, Trial completion date, Trial primary completion date: REPO-STROKE1: Possible Effects of Propylthiouracil, Riociguat and Perphenazine on Circulation of Healthy Volunteers (clinicaltrials.gov) - Mar 15, 2022
P1, N=8, Completed,
Mental health officers should accurately identify enrollees at a high risk of T2DM and take appropriate preventive measures to reduce the incidence of T2DM among patients with schizophrenia. Recruiting --> Completed | Trial completion date: Apr 2021 --> Feb 2022 | Trial primary completion date: Mar 2021 --> Feb 2022
- |||||||||| risperidone / Generic mfg.
Optimal Doses of Antipsychotics for Relapse Prevention in a Nation-Wide Cohort of Patients with Schizophrenia (Spadolini Pavilion Upper Floor) - Mar 11, 2022 - Abstract #SIRS2022SIRS_310;
Among the 15 most widely used antipsychotics, 13 had a U- or J-shaped dose-response curve, showing the lowest risks of relapse for doses of 0.6–<1.1 DDDs/day versus non-use of antipsychotics. The exceptions were oral perphenazine (aHR=0.72, 95% CI=0.68–0.76, <0.6 DDDs/day), and olanzapine-long-acting injectable (LAI) (aHR=0.17, 95%CI=0.11–0.25, 1.4–<1.6 DDDs/day), the latter of which had the lowest aHR of any antipsychotic.
- |||||||||| risperidone / Generic mfg.
Clinical, Journal: Antipsychotics Use Is Associated With Greater Adherence to Cardiometabolic Medications in Patients With Schizophrenia: Results From a Nationwide, Within-subject Design Study. (Pubmed Central) - Mar 3, 2022
The exceptions were oral perphenazine (aHR=0.72, 95% CI=0.68–0.76, <0.6 DDDs/day), and olanzapine-long-acting injectable (LAI) (aHR=0.17, 95%CI=0.11–0.25, 1.4–<1.6 DDDs/day), the latter of which had the lowest aHR of any antipsychotic. In this national database within-subject design study, current antipsychotic use was associated with substantially decreased risk of discontinuation of statins, anti-diabetics, antihypertensives, and beta-blockers, which might explain reduced cardiovascular mortality observed with antipsychotics in people with schizophrenia.
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