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Thioridazine Induces Apoptosis of Multidrug-Resistant Mouse Lymphoma Cells Transfected with the Human ABCB1 and Inhibits the Expression of P-Glycoprotein
ANTICANCER RESEARCH 31: 4201-4206 (2011) Thioridazine Induces Apoptosis of Multidrug-resistant Mouse Lymphoma Cells Transfected with the Human ABCB1 and Inhibits the Expression of P-Glycoprotein GABRIELLA SPENGLER1,3, JOSEPH MOLNAR1, MIGUEL VIVEIROS2,4 and LEONARD AMARAL2,3,4 1Institute of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Szeged, Hungary; 2Group of Mycobacteriology, Unit of Microbiology and 3Unit of Parasitology and Medical Microbiology (UPMM), Institute of Hygiene and Tropical Medicine, Universidade Nova de Lisboa, Lisboa, Portugal; 4Cost Action BM0701 (ATENS) of the European Commission, Brussels, Belgium Abstract. Aim: Chlorpromazine has activity against a large therapeutic aspects, and low availability of effective but also variety of cancer types. However, this phenothiazine produces costly forms of therapy (chemotherapy, radiotherapy). a plethora of serious side-effects. We have studied thioridazine Regardless of economic support, chemotherapy of cancer is (TZ), a phenothiazine neuroleptic that is much milder, for highly problematic, especially when therapy promotes the activity against multidrug-resistant (MDR) cancer cells, as development of multidrug resistance (MDR), hence cancer well as against the overexpressed ABCB1 transporter (P- becomes refractory not only to the initial chemotherapeutic glycoprotein) that is the cause for the MDR phenotype of these agent, but to many other anticancer drugs as well (1, 2). The cancer cells. Materials and Methods: MDR mouse T- development of an MDR phenotype of cancer cell has been lymphoma cells, transfected with the human gene ABCB1 that known for many decades to be due to the overexpression of codes for the transporter ABCB1, were incubated with TZ for transporters that extrude the anticancer agent before it various periods of time and examined for evidence of reaches its intended target (3). -
FDA Approved Drugs with Broad Anti-Coronaviral Activity Inhibit SARS-Cov-2 in Vitro
bioRxiv preprint doi: https://doi.org/10.1101/2020.03.25.008482; this version posted March 27, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-NC-ND 4.0 International license. FDA approved drugs with broad anti-coronaviral activity inhibit SARS-CoV-2 in vitro Stuart Weston1, Rob Haupt1, James Logue1, Krystal Matthews1 and Matthew B. Frieman*1 1 - Department of Microbiology and Immunology, University of Maryland School of Medicine, 685 W. Baltimore St., Room 380, Baltimore, MD, 21201, USA *Corresponding author. Email: [email protected] Key words: SARS-CoV-2, nCoV-2019, COVID-19, drug repurposing, FDA approved drugs, antiviral therapeutics, pandemic, chloroquine, hydroxychloroquine AbstraCt SARS-CoV-2 emerged in China at the end of 2019 and has rapidly become a pandemic with over 400,000 recorded COVID-19 cases and greater than 19,000 recorded deaths by March 24th, 2020 (www.WHO.org) (1). There are no FDA approved antivirals or vaccines for any coronavirus, including SARS-CoV-2 (2). Current treatments for COVID-19 are limited to supportive therapies and off-label use of FDA approved drugs (3). Rapid development and human testing of potential antivirals is greatly needed. A potentially quicker way to test compounds with antiviral activity is through drug re-purposing (2, 4). Numerous drugs are already approved for use in humans and subsequently there is a good understanding of their safety profiles and potential side effects, making them easier to test in COVID-19 patients. -
A Drug Repositioning Approach Identifies Tricyclic Antidepressants As Inhibitors of Small Cell Lung Cancer and Other Neuroendocrine Tumors
Published OnlineFirst September 26, 2013; DOI: 10.1158/2159-8290.CD-13-0183 RESEARCH ARTICLE A Drug Repositioning Approach Identifi es Tricyclic Antidepressants as Inhibitors of Small Cell Lung Cancer and Other Neuroendocrine Tumors Nadine S. Jahchan 1 , 2 , Joel T. Dudley 1 , Pawel K. Mazur 1 , 2 , Natasha Flores 1 , 2 , Dian Yang 1 , 2 , Alec Palmerton 1 , 2 , Anne-Flore Zmoos 1 , 2 , Dedeepya Vaka 1 , 2 , Kim Q.T. Tran 1 , 2 , Margaret Zhou 1 , 2 , Karolina Krasinska 3 , Jonathan W. Riess 4 , Joel W. Neal 5 , Purvesh Khatri 1 , 2 , Kwon S. Park 1 , 2 , Atul J. Butte 1 , 2 , and Julien Sage 1 , 2 Downloaded from cancerdiscovery.aacrjournals.org on September 29, 2021. © 2013 American Association for Cancer Research. Published OnlineFirst September 26, 2013; DOI: 10.1158/2159-8290.CD-13-0183 ABSTRACT Small cell lung cancer (SCLC) is an aggressive neuroendocrine subtype of lung cancer with high mortality. We used a systematic drug repositioning bioinformat- ics approach querying a large compendium of gene expression profi les to identify candidate U.S. Food and Drug Administration (FDA)–approved drugs to treat SCLC. We found that tricyclic antidepressants and related molecules potently induce apoptosis in both chemonaïve and chemoresistant SCLC cells in culture, in mouse and human SCLC tumors transplanted into immunocompromised mice, and in endog- enous tumors from a mouse model for human SCLC. The candidate drugs activate stress pathways and induce cell death in SCLC cells, at least in part by disrupting autocrine survival signals involving neurotransmitters and their G protein–coupled receptors. The candidate drugs inhibit the growth of other neuroendocrine tumors, including pancreatic neuroendocrine tumors and Merkel cell carcinoma. -
Light Scattering Studies of Amphiphilic Drugs Promethazine Hydrochloride and Imipramine Hydrochloride in Aqueous Electrolyte Solutions
12962 J. Phys. Chem. B 2008, 112, 12962–12967 Light Scattering Studies of Amphiphilic Drugs Promethazine Hydrochloride and Imipramine Hydrochloride in Aqueous Electrolyte Solutions Md. Sayem Alam,† Goutam Ghosh,‡ and Kabir-ud-Din*,† Department of Chemistry, Aligarh Muslim UniVersity, Aligarh-202 002, India, and UGC-DAE Consortium for Scientific Research, Trombay, Mumbai- 400 085, India ReceiVed: May 13, 2008; ReVised Manuscript ReceiVed: August 1, 2008 Two amphiphilic drugs, promethazine hydrochloride (PMT) and imipramine hydrochloride (IMP), have been studied using both static and dynamic light scattering techniques. Due to having rigid tricyclic hydrophobic moieties in their molecules, these drugs show interesting association behavior. The static light scattering (SLS) measurements show that the self-association commenced above a well-defined critical micellar concentration (cmc), which decreases with increasing NaBr concentration. The Gibbs energy of micellization, 0 ∆GM, in all cases, is negative. The colloidal stability of the system in terms of the interparticle interaction at different NaBr concentrations was studied using the dynamic light scattering (DLS) technique. The experimentally evaluated interparticle interaction parameter (kD) was compared with the Derjaguin-Landau- Verwey-Overbeek (DLVO) model. Interestingly, these two drugs with similar molecular structure show difference in their interparticle interactions, e.g., PMT showed complete agreement with the DLVO model whereas IMP showed clear deviation from this model at lower concentrations and agreement at higher concentrations of NaBr. 1. Introduction SCHEME 1: Molecular Structure of Promethazine Hydrochloride, PMT (a), and Imipramine Hydrochloride, Many drug molecules are amphiphilic and self-associate in IMP (b) a surfactant-like manner in aqueous environment to form small aggregates. -
HALDOL Decanoate 50 (Haloperidol)
HALDOL® Decanoate 50 (haloperidol) HALDOL® Decanoate 100 (haloperidol) For IM Injection Only WARNING Increased Mortality in Elderly Patients with Dementia-Related Psychosis Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. HALDOL Decanoate is not approved for the treatment of patients with dementia-related psychosis (see WARNINGS). DESCRIPTION Haloperidol decanoate is the decanoate ester of the butyrophenone, HALDOL (haloperidol). It has a markedly extended duration of effect. It is available in sesame oil in sterile form for intramuscular (IM) injection. The structural formula of haloperidol decanoate, 4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]-4 piperidinyl decanoate, is: Haloperidol decanoate is almost insoluble in water (0.01 mg/mL), but is soluble in most organic solvents. -
HIGH RISK MEDICATIONS As Specified by NCQA’S HEDIS Measure: Use of High Risk Medications in the Elderly
HIGH RISK MEDICATIONS as specified by NCQA’s HEDIS Measure: Use of High Risk Medications in the Elderly Description Prescription Antianxiety (includes • aspirin-meprobamate • meprobamate combination drugs) Antiemetics • scopolamine • trimethobenzamide Analgesics (includes • acetaminophen-diphenhydramine • ketorolac combination drugs) • diphenhydramine-magnesium salicylate Antihistamines (includes • APAP/dextromethorphan/diphenhydramine • dexchlorpheniramine-pseudoephedrine combination drugs) • APAP/diphenhydramine/phenylephrine • dextromethorphan-promethazine • APAP/diphenhydramine/pseudoephedrine • diphenhydramine • acetaminophen-diphenhydramine • diphenhydramine/hydrocodone/phenylephrine • atropine/CPM/hyoscyamine/PE/PPA/scopolamine • diphenhydramine-tripelennamine • carbetapentane/diphenhydramine/phenylephrine • diphenhydramine-magnesium salicylate • codeine/phenylephrine/promethazine • diphenhydramine-phenylephrine • codeine-promethazine • diphenhydramine-pseudoephedrine • cyproheptadine • hydroxyzine hydrochloride • dexchlorpheniramine • hydroxyzine pamoate • dexchlorpheniramine/dextromethorphan/PSE • phenylephrine-promethazine • dexchlorpheniramine/guaifenesin/PSE • promethazine • dexchlorpheniramine/hydrocodone/phenylephrine • tripelennamine • dexchlorpheniramine/methscopolamine/PSE Antipsychotic, typical • mesoridazine • thioridazine Amphetamines • amphetamine- • dextroamphetamine • pemoline dextroamphetamine • diethylpropion • phendimetrazine • benzphetamine • methamphetamine • phentermine • dexmethylphenidate • methylphenidate -
Determination of Thiazinamium, Promazine and Promethazine in Pharmaceutical Formulations Using a CZE Method Francisco J
Analytica Chimica Acta 535 (2005) 101–108 Determination of thiazinamium, promazine and promethazine in pharmaceutical formulations using a CZE method Francisco J. Lara, Ana M. Garc´ıa-Campana˜ ∗, Ferm´ın Ales-Barrero,´ Juan M. Bosque-Sendra Department of Analytical Chemistry, Faculty of Sciences, University of Granada, Avd. Fuente Nueva s/n, E-18071 Granada, Spain Received 26 July 2004; received in revised form 30 November 2004; accepted 30 November 2004 Available online 15 January 2005 Abstract We present the validation of a developed method using capillary zone electrophoresis (CZE) for quantitative analysis of three phenoth- iazines: thiazinamium methylsulphate (TMS), promazine hydrochloride (PMH) and promethazine hydrochloride (PTH) in pharmaceutical formulations. The influence of various parameters affecting the CZE separation (buffer pH and concentration, acetonitrile percentage, capil- lary temperature and applied voltage) was investigated by means of multivariate optimization using experimental designs so as to obtain the highest efficiency. The method allows the separation of the phenothiazines in 5.0 min at optimized conditions: 100 mM tris(hydroxymethyl)- aminomethane (Tris) buffer at a pH 8.0, 15% acetonitrile, capillary with 58.5 cm in length at 25 ◦C and a voltage of 30 kV.Detection occurred at 254 nm. Acceptable precision (relative standard deviation (R.S.D.) 5.3%) and linearity were achieved using the internal standard (IS) method. The limits of detection (LODs) were 2.8 gml−1 for TMS and 3.3 gml−1 for PMH and PTH. The method has been successfully applied in the analysis of pharmaceutical formulations. © 2004 Elsevier B.V. All rights reserved. Keywords: Capillary zone electrophoresis; Thiazinamium methylsulphate; Promazine; Promethazine; Pharmaceutical analysis 1. -
Neuromodulators for Functional Gastrointestinal Disorders (Disorders of Gutlbrain Interaction): a Rome Foundation Working Team Report Douglas A
Gastroenterology 2018;154:1140–1171 SPECIAL REPORT Neuromodulators for Functional Gastrointestinal Disorders (Disorders of GutLBrain Interaction): A Rome Foundation Working Team Report Douglas A. Drossman,1,2 Jan Tack,3 Alexander C. Ford,4,5 Eva Szigethy,6 Hans Törnblom,7 and Lukas Van Oudenhove8 1Center for Functional Gastrointestinal and Motility Disorders, University of North Carolina, Chapel Hill, North Carolina; 2Center for Education and Practice of Biopsychosocial Care and Drossman Gastroenterology, Chapel Hill, North Carolina; 3Translational Research Center for Gastrointestinal Disorders, University of Leuven, Leuven, Belgium; 4Leeds Institute of Biomedical and Clinical Sciences, University of Leeds, Leeds, United Kingdom; 5Leeds Gastroenterology Institute, St James’s University Hospital, Leeds, United Kingdom; 6Departments of Psychiatry and Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania; 7Departments of Internal Medicine and Clinical Nutrition, Institute of Medicine, Sahlgrenska Academy, University of Gothenburg, Gothenburg, Sweden; and 8Laboratory for BrainÀGut Axis Studies, Translational Research Center for Gastrointestinal Disorders, University of Leuven, Leuven, Belgium BACKGROUND & AIMS: Central neuromodulators (antide- summary information and guidelines for the use of central pressants, antipsychotics, and other central nervous neuromodulators in the treatment of chronic gastrointestinal systemÀtargeted medications) are increasingly used for treat- symptoms and FGIDs. Further studies are needed to confirm ment -
Promethazine-Chlorpromazine Combination in the Treatment of Unmanageable Psychotic Patients Armando R
Henry Ford Hospital Medical Journal Volume 17 | Number 4 Article 10 12-1969 Promethazine-Chlorpromazine Combination in the Treatment of Unmanageable Psychotic Patients Armando R. Favazza Follow this and additional works at: https://scholarlycommons.henryford.com/hfhmedjournal Part of the Chemicals and Drugs Commons, Life Sciences Commons, Medical Specialties Commons, Psychiatry and Psychology Commons, and the Public Health Commons Recommended Citation Favazza, Armando R. (1969) "Promethazine-Chlorpromazine Combination in the Treatment of Unmanageable Psychotic Patients," Henry Ford Hospital Medical Journal : Vol. 17 : No. 4 , 305-310. Available at: https://scholarlycommons.henryford.com/hfhmedjournal/vol17/iss4/10 This Article is brought to you for free and open access by Henry Ford Health System Scholarly Commons. It has been accepted for inclusion in Henry Ford Hospital Medical Journal by an authorized editor of Henry Ford Health System Scholarly Commons. Henry Ford Hosp. Med. Journal VoL 17, No. 4, 1969 Promethazine-chlorpromazine Combination in the Treatment of Unmanageable Psychotic Patients Armando R. Favazza, M.D.* Administering a combination of promethazine and chlorpromazine to patients with a "galloping psychosis" has an antipsychotic and tranquilizing effect which calms them down to a more manageable and less aggressive state. The drugs are chemically similar; promethazine's actions are strongly potentiated in the combina tion, so large doses must be given under careful supervision. Case histories demonstrate successful short term management of acutely psychotic, aggressive patients who were a danger to themselves and others. Acute, intense psychotic episodes common in the author's experience for can pose difficult problems for both some patients to receive massive doses the patient and those who care for him. -
Medications to Be Avoided Or Used with Caution in Parkinson's Disease
Medications To Be Avoided Or Used With Caution in Parkinson’s Disease This medication list is not intended to be complete and additional brand names may be found for each medication. Every patient is different and you may need to take one of these medications despite caution against it. Please discuss your particular situation with your physician and do not stop any medication that you are currently taking without first seeking advice from your physician. Most medications should be tapered off and not stopped suddenly. Although you may not be taking these medications at home, one of these medications may be introduced while hospitalized. If a hospitalization is planned, please have your neurologist contact your treating physician in the hospital to advise which medications should be avoided. Medications to be avoided or used with caution in combination with Selegiline HCL (Eldepryl®, Deprenyl®, Zelapar®), Rasagiline (Azilect®) and Safinamide (Xadago®) Medication Type Medication Name Brand Name Narcotics/Analgesics Meperidine Demerol® Tramadol Ultram® Methadone Dolophine® Propoxyphene Darvon® Antidepressants St. John’s Wort Several Brands Muscle Relaxants Cyclobenzaprine Flexeril® Cough Suppressants Dextromethorphan Robitussin® products, other brands — found as an ingredient in various cough and cold medications Decongestants/Stimulants Pseudoephedrine Sudafed® products, other Phenylephrine brands — found as an ingredient Ephedrine in various cold and allergy medications Other medications Linezolid (antibiotic) Zyvox® that inhibit Monoamine oxidase Phenelzine Nardil® Tranylcypromine Parnate® Isocarboxazid Marplan® Note: Additional medications are cautioned against in people taking Monoamine oxidase inhibitors (MAOI), including other opioids (beyond what is mentioned in the chart above), most classes of antidepressants and other stimulants (beyond what is mentioned in the chart above). -
Antipsychotics-2020.Pdf
© Mind 2020 Antipsychotics Explains what antipsychotics are used for, how the medication works, possible side effects and information about withdrawal. If you require this information in Word document format for compatibility with screen readers, please email: [email protected] Contents What are antipsychotics? ...................................................................................................................... 2 Could antipsychotics help me? .............................................................................................................. 5 How to take antipsychotics safely ......................................................................................................... 9 What dosage of antipsychotics should I be on? .................................................................................. 15 Antipsychotics during pregnancy and breastfeeding ........................................................................... 17 What side effects can antipsychotics cause? ....................................................................................... 20 What is a depot injection? ................................................................................................................... 30 How can I compare different antipsychotics? ..................................................................................... 31 Can I come off antipsychotics? ............................................................................................................ 41 Alternatives to antipsychotics -
Name of Medicine
HALDOL® haloperidol decanoate NEW ZEALAND DATA SHEET 1. PRODUCT NAME HALDOL haloperidol decanoate 50 mg/mL Injection HALDOL CONCENTRATE haloperidol decanoate 100 mg/mL Injection 2. QUANTITATIVE AND QUALITATIVE COMPOSITION HALDOL 50 mg/ml Haloperidol decanoate 70.52 mg, equivalent to 50 mg haloperidol base, per millilitre. HALDOL CONCENTRATE 100 mg/ml Haloperidol decanoate 141.04 mg, equivalent to 100 mg haloperidol base, per millilitre. For a full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM Injection (depot) HALDOL Injection (long acting) is a slightly amber, slightly viscous solution, free from visible foreign matter, filled in 1 mL amber glass ampoules. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications HALDOL is indicated for the maintenance therapy of psychoses in adults, particularly for patients requiring prolonged parenteral neuroleptic therapy. 4.2 Dose and method of administration Administration HALDOL should be administered by deep intramuscular injection into the gluteal region. It is recommended to alternate between the two gluteal muscles for subsequent injections. A 2 inch-long, 21 gauge needle is recommended. The maximum volume per injection site should not exceed 3 mL. The recommended interval between doses is 4 weeks. DO NOT ADMINISTER INTRAVENOUSLY. Patients must be previously stabilised on oral haloperidol before converting to HALDOL. Treatment initiation and dose titration must be carried out under close clinical supervision. The starting dose of HALDOL should be based on the patient's clinical history, severity of symptoms, physical condition and response to the current oral haloperidol dose. Patients must always be maintained on the lowest effective dose. CCDS(180302) Page 1 of 16 HALDOL(180712)ADS Dosage - Adults Table 1.