Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles
In this study, we examined 26 clinically available antipsychotics to determine the extent to which they inhibit acetylcholine (ACh)-induced contraction in rat UBSM to predict the drugs that should not be used by elderly people to avoid urinary disorders. Of the 26 antipsychotics, six (chlorpromazine, levomepromazine (phenothiazines), zotepine (a thiepine), olanzapine, quetiapine, clozapine (multi-acting receptor targeted antipsychotics (MARTAs))) competitively inhibited ACh-induced contractions at concentrations corresponding to clinically significant doses. Further, 11 antipsychotics (perphenazine, fluphenazine, prochlorp...
Source: Biological and Pharmaceutical Bulletin - August 2, 2021 Category: Drugs & Pharmacology Authors: Keisuke Obara Yuka Matsuoka Naoya Iwata Yukako Abe Yohei Ikegami Nanako Shioda Yume Hattori Shoko Hamamatsu Kento Yoshioka Fumiko Yamaki Kazuhiro Matsuo Takashi Yoshio Yoshio Tanaka Source Type: research
Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles
In this study, we examined 26 clinically available antipsychotics to determine the extent to which they inhibit acetylcholine (ACh)-induced contraction in rat UBSM to predict the drugs that should not be used by elderly people to avoid urinary disorders. Of the 26 antipsychotics, six (chlorpromazine, levomepromazine (phenothiazines), zotepine (a thiepine), olanzapine, quetiapine, clozapine (multi-acting receptor targeted antipsychotics (MARTAs))) competitively inhibited ACh-induced contractions at concentrations corresponding to clinically significant doses. Further, 11 antipsychotics (perphenazine, fluphenazine, prochlorp...
Source: Biological and Pharmaceutical Bulletin - August 2, 2021 Category: Drugs & Pharmacology Authors: Keisuke Obara Yuka Matsuoka Naoya Iwata Yukako Abe Yohei Ikegami Nanako Shioda Yume Hattori Shoko Hamamatsu Kento Yoshioka Fumiko Yamaki Kazuhiro Matsuo Takashi Yoshio Yoshio Tanaka Source Type: research
Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles
In this study, we examined 26 clinically available antipsychotics to determine the extent to which they inhibit acetylcholine (ACh)-induced contraction in rat UBSM to predict the drugs that should not be used by elderly people to avoid urinary disorders. Of the 26 antipsychotics, six (chlorpromazine, levomepromazine (phenothiazines), zotepine (a thiepine), olanzapine, quetiapine, clozapine (multi-acting receptor targeted antipsychotics (MARTAs))) competitively inhibited ACh-induced contractions at concentrations corresponding to clinically significant doses. Further, 11 antipsychotics (perphenazine, fluphenazine, prochlorp...
Source: Biological and Pharmaceutical Bulletin - August 2, 2021 Category: Drugs & Pharmacology Authors: Keisuke Obara Yuka Matsuoka Naoya Iwata Yukako Abe Yohei Ikegami Nanako Shioda Yume Hattori Shoko Hamamatsu Kento Yoshioka Fumiko Yamaki Kazuhiro Matsuo Takashi Yoshio Yoshio Tanaka Source Type: research
A high-throughput screen identifies inhibitors of lung cancer stem cells
Biomed Pharmacother. 2021 May 24;140:111748. doi: 10.1016/j.biopha.2021.111748. Online ahead of print.ABSTRACTMetastasis is the main cause of cancer morbidity and mortality. Cancer stem cells (CSCs) are a rare subpopulation of cancer cells that can drive metastasis. The identification of CSC inhibitors and CSC-related genes is an alluring strategy for suppressing metastasis. Here, we established a simple and repeatable high-throughput CSC inhibitor screening platform that combined tumor sphere formation assays and cell viability assays. Human lung cancer cells were cocultured with 1280 pharmacologically active compounds (F...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - May 27, 2021 Category: Drugs & Pharmacology Authors: Xiaofei She Yaqun Gao Yan Zhao Yue Yin Zhewen Dong Source Type: research
A high-throughput screen identifies inhibitors of lung cancer stem cells
Biomed Pharmacother. 2021 May 25;140:111748. doi: 10.1016/j.biopha.2021.111748. Online ahead of print.ABSTRACTMetastasis is the main cause of cancer morbidity and mortality. Cancer stem cells (CSCs) are a rare subpopulation of cancer cells that can drive metastasis. The identification of CSC inhibitors and CSC-related genes is an alluring strategy for suppressing metastasis. Here, we established a simple and repeatable high-throughput CSC inhibitor screening platform that combined tumor sphere formation assays and cell viability assays. Human lung cancer cells were cocultured with 1280 pharmacologically active compounds (F...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - May 27, 2021 Category: Drugs & Pharmacology Authors: Xiaofei She Yaqun Gao Yan Zhao Yue Yin Zhewen Dong Source Type: research
A prospective, randomized, double-blind trial of intravenous chlorpromazine versus intravenous prochlorperazine for the treatment of acute migraine in adults presenting to the emergency department
CONCLUSIONS: Both chlorpromazine and prochlorperazine are efficacious treatments for acute migraine in adult patients presenting to the ED. This trial found no evidence of superiority of either agent over the other. Caution should be used when prescribing these medicines in the borderline hypotensive patient; in that circumstance, prochlorperazine should be preferentially used.PMID:33797074 | DOI:10.1111/head.14091 (Source: Headache)
Source: Headache - April 2, 2021 Category: Neurology Authors: Sarah E Hodgson Andrew M Harding Elyssia M Bourke David M Taylor Shaun L Greene Source Type: research
A prospective, randomized, double-blind trial of intravenous chlorpromazine versus intravenous prochlorperazine for the treatment of acute migraine in adults presenting to the emergency department
CONCLUSIONS: Both chlorpromazine and prochlorperazine are efficacious treatments for acute migraine in adult patients presenting to the ED. This trial found no evidence of superiority of either agent over the other. Caution should be used when prescribing these medicines in the borderline hypotensive patient; in that circumstance, prochlorperazine should be preferentially used.PMID:33797074 | DOI:10.1111/head.14091 (Source: Headache)
Source: Headache - April 2, 2021 Category: Neurology Authors: Sarah E Hodgson Andrew M Harding Elyssia M Bourke David M Taylor Shaun L Greene Source Type: research
A prospective, randomized, double-blind trial of intravenous chlorpromazine versus intravenous prochlorperazine for the treatment of acute migraine in adults presenting to the emergency department
CONCLUSIONS: Both chlorpromazine and prochlorperazine are efficacious treatments for acute migraine in adult patients presenting to the ED. This trial found no evidence of superiority of either agent over the other. Caution should be used when prescribing these medicines in the borderline hypotensive patient; in that circumstance, prochlorperazine should be preferentially used.PMID:33797074 | DOI:10.1111/head.14091 (Source: Headache)
Source: Headache - April 2, 2021 Category: Neurology Authors: Sarah E Hodgson Andrew M Harding Elyssia M Bourke David M Taylor Shaun L Greene Source Type: research
Non-interacting, Non-opioid, and Non-barbiturate Containing Acute Medication Combinations in Headache: A Pilot Combinatorics Approach Based on DrugBank Database
Conclusion: This list of headaches abortive medications without drug-drug interactions is a useful tool for clinicians seeking to more effectively manage refractory headaches by implementing a rational polypharmacy. (Source: Frontiers in Neurology)
Source: Frontiers in Neurology - February 17, 2021 Category: Neurology Source Type: research
Effectiveness of Standard Combination Therapy in Pediatric Migraine
A combination of parenteral medications (often referred to as Standard Combination Therapy or SCT) is frequently used in the treatment of acute migraine in the pediatric emergency department (PED). The primary aim of this study was to evaluate the 2-hour, 24 hour and 7- day impact of one such regimen on pain in children who present to the PED. SCT for purposes of our study is defined as a bolus of intravenous (IV) saline, and a combination of IV ketorolac, prochlorperazine and diphenhydramine. (Source: Pediatric Neurology)
Source: Pediatric Neurology - December 15, 2020 Category: Neurology Authors: Nirupama Kannikeswaran, Lavina Desai, Ahmad Farooqi, Lalitha Sivaswamy Tags: Research Paper Source Type: research
IV Amisulpride (Barhemsys) for Postoperative Nausea and Vomiting
Date: December 28, 2020
Issue #:
1614Summary:
The FDA has approved IV amisulpride (Barhemsys–
Acacia), a selective dopamine-2 and -3 (D2/D3) receptor
antagonist, for prevention and treatment of postoperative
nausea and vomiting (PONV) in adults. It is the first
antiemetic to be approved for rescue treatment of
PONV in patients who have symptoms despite receiving
antiemetic prophylaxis. Oral formulations of amisulpride
are available in Europe for treatment of schizophrenia
and acute psychotic episodes. (Source: The Medical Letter)
Source: The Medical Letter - November 10, 2020 Category: Drugs & Pharmacology Authors: admin Tags: Aloxi amisulpride Aprepitant Barhemsys Dexamethasone Dimenhydrinate Droperidol Emend Granisetron Histanil ondansetron Palonosetron Phenergan post-operative nausea and vomiting Prochlorperazine Promethazine Scopolamine Tra Source Type: research
New Drug Repositioning Candidates for T-ALL Identified Via Human/Murine Gene Signature Comparison
T-cell Acute Lymphoblastic Leukemia (T-ALL) is an aggressive subtype of leukemia for which important progress in treatment efficiency have been made in the past decades to reach a cure rate of 75%–80% nowadays. It is nevertheless mandatory to find new targets and active molecules for innovative therapeutic strategies as relapse is associated with a very dismal outcome. We designed an experimental workflow to highlight the conserved core pathways associated with leukemogenesis by confronting the gene expression profiles (GEPs) of human T-ALL cases to the GEP of a murine T-ALL representative model, generated by the conditi...
Source: Frontiers in Oncology - November 9, 2020 Category: Cancer & Oncology Source Type: research
Antiviral activity of chlorpromazine, fluphenazine, perphenazine, prochlorperazine, and thioridazine towards RNA-viruses. A review.
Abstract
In 2020 the whole world focused on antivirus drugs towards SARS-CoV-2. Most of the researchers focused on drugs used in other viral infections or malaria. We have not seen such mobilization towards one topic in this century. The whole situation makes clear that progress needs to be made in antiviral drug development. The first step to do it is to characterize the potential antiviral activity of new or already existed drugs on the market. Phenothiazines are antipsychotic agents used previously as antiseptics, anthelminthics, and antimalarials. Up to date, they are tested for a number of other disor...
Source: European Journal of Pharmacology - September 15, 2020 Category: Drugs & Pharmacology Authors: Otręba M, Kośmider L, Rzepecka-Stojko A Tags: Eur J Pharmacol Source Type: research
MAGraine: Magnesium compared to conventional therapy for treatment of migraines
Due to the healthcare burden associated with migraines, prompt and effective treatment is vital to improve patient outcomes and ED workflow. This was a prospective, randomized, double-blind trial. Adults who presented to the ED with a diagnosis of migraine from August of 2019 to March of 2020 were included. Pregnant patients, or with renal impairment were excluded. Patients were randomized to receive intravenous magnesium, prochlorperazine, or metoclopramide. The primary outcome was change in pain from baseline on a numeric rating scale (NRS) evaluated at 30 min after initiation of infusion of study drug. (Source: The A...
Source: The American Journal of Emergency Medicine - September 13, 2020 Category: Emergency Medicine Authors: Manar Kandil, Sabrin Jaber, Dharati Desai, Stephany Nunez Cruz, Nadine Lomotan, Uzma Ahmad, Michael Cirone, Jaxson Burkins, Marc McDowell Source Type: research
In vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review
In this study, we performed an extensive literature search to find and summarize all papers on the chosen phenothiazines and their potential in treating different types of cancerin vitro for further animal/clinical trials. Fluphenazine, perphenazine and prochlorperazine possess anticancer activity towards different types of human cancer. The antitumor activity is mainly mediated by an effect of the drugs on the cell cycle, proliferation or apoptosis. Possible molecular targets of phenothiazine derivatives are the drug's efflux pumps (ABCB1 and P ‐glycoprotein) and two parallel pathways (AKT and Wnt) regulated by the D2 r...
Source: Journal of Applied Toxicology - August 27, 2020 Category: Toxicology Authors: Micha ł Otręba,
Leon Kośmider Tags: REVIEW ARTICLE Source Type: research
