COVID-19) Pandemic on National Antimicrobial Consumption in Jordan
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Interbiotech Entecavir
InterBioTech FT-XLS250 Entecavir Product Description Catalog #: XLS250, 5mg XLS251, 10mg XLS252, 50mg XLS253, 100mg AXAIV0, 1ml 10mM in DMSO. Catalog #: Name: Entecavir, Monohydrate Syn: BMS200475 monohydrate; SQ34676 monohydrate CAS : 209216-23-9 MW : 295.29 Formula : C12H17N5O4 Properties : DMSO : ≥ 50 mg/mL (169.33 mM) H2O : 2.8 mg/mL (9.48 mM) >99.5% Storage: Powder: -20°C (long term; possible at +4°C (2 years) (M) Also available: In solvent: -80°C (6 months) -20°C (1 month) Entecavir free form #RO893P/Q/R (Syn.: BMS200475; SQ34676) CAS No. : 142217-69-4; MW: 277.2 For Research Use Only Introduction Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell. IC50 & Target EC50:3.75 nM (anti-HBV, HepG2 cell)[1] In Vitro *Solubility : DMSO : ≥ 50 mg/mL (169.33 mM) H2O : 2.8 mg/mL (9.48 mM; Need ultrasonic and warming) *Preparation : 1mM = 1mg in 3.3865 mL Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1]. Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2]. P.1 InterBioTech FT-XLS250 In Vivo *Preparation : 1. Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution 2. -
Injectable PLGA Adefovir Microspheres; the Way for Long Term Therapy of T Chronic Hepatitis-B ⁎ Margrit M
European Journal of Pharmaceutical Sciences 118 (2018) 24–31 Contents lists available at ScienceDirect European Journal of Pharmaceutical Sciences journal homepage: www.elsevier.com/locate/ejps Injectable PLGA Adefovir microspheres; the way for long term therapy of T chronic hepatitis-B ⁎ Margrit M. Ayouba, , Neveen G. Elantounyb, Hanan M. El-Nahasa, Fakhr El-Din S. Ghazya a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt b Department of Internal Medicine, Faculty of Medicine, Zagazig University, Zagazig, Egypt ARTICLE INFO ABSTRACT Keywords: For patient convenience, sustained release Adefovir Poly-d,l-lactic-co-glycolic acid (PLGA) microspheres were Adefovir formulated to relieve the daily use of the drug which is a problem for patients treated from chronic hepatitis-B. Biodegradable microspheres PLGA microspheres were prepared and characterized by entrapment efficiency, particle size distribution and Poly-lactic-co-glycolic acid scanning electron microscopy (SEM). In-vitro release and in-vivo studies were carried out. Factors such as drug: Entrapment efficiency polymer ratio, polymer viscosity and polymer lactide content were found to be important variables for the preparation of PLGA Adefovir microspheres. Fourier transform infrared (FTIR) analysis and differential scanning calorimetry (DSC) were performed to determine any drug-polymer interactions. One way analysis of variance (ANOVA) was employed to analyze the pharmacokinetic parameters after intramuscular injection of the pure drug and the selected PLGA microspheres into rats. FTIR and DSC revealed a significant interaction between the drug and the polymer. Reports of SEM before and after 1 and 24 h release showed that the microspheres had nonporous smooth surface even after 24 h release. -
Highlights of Prescribing Information
HIGHLIGHTS OF PRESCRIBING INFORMATION --------------------------WARNINGS AND PRECAUTIONS-------------------- These highlights do not include all the information needed to use • New onset or worsening renal impairment: Can include acute VIREAD safely and effectively. See full prescribing information renal failure and Fanconi syndrome. Assess creatinine clearance for VIREAD. (CrCl) before initiating treatment with VIREAD. Monitor CrCl and ® serum phosphorus in patients at risk. Avoid administering VIREAD (tenofovir disoproxil fumarate) tablets, for oral use VIREAD with concurrent or recent use of nephrotoxic drugs. (5.3) VIREAD® (tenofovir disoproxil fumarate) powder, for oral use • Coadministration with Other Products: Do not use with other Initial U.S. Approval: 2001 tenofovir-containing products (e.g., ATRIPLA, COMPLERA, and TRUVADA). Do not administer in combination with HEPSERA. WARNING: LACTIC ACIDOSIS/SEVERE HEPATOMEGALY WITH (5.4) STEATOSIS and POST TREATMENT EXACERBATION OF HEPATITIS • HIV testing: HIV antibody testing should be offered to all HBV- infected patients before initiating therapy with VIREAD. VIREAD See full prescribing information for complete boxed warning. should only be used as part of an appropriate antiretroviral • Lactic acidosis and severe hepatomegaly with steatosis, combination regimen in HIV-infected patients with or without HBV including fatal cases, have been reported with the use of coinfection. (5.5) nucleoside analogs, including VIREAD. (5.1) • Decreases in bone mineral density (BMD): Consider assessment • Severe acute exacerbations of hepatitis have been reported of BMD in patients with a history of pathologic fracture or other in HBV-infected patients who have discontinued anti- risk factors for osteoporosis or bone loss. (5.6) hepatitis B therapy, including VIREAD. Hepatic function • Redistribution/accumulation of body fat: Observed in HIV-infected should be monitored closely in these patients. -
Hepsera, INN- Defovir Dipivoxil
SCIENTIFIC DISCUSSION This module reflects the initial scientific discussion for the approval of Hepsera. For information on changes after approvalplease refer to module 8B 1. Chemical, pharmaceutical and biological aspects Composition Hepsera is presented as an immediate release tablet containing 10 mg of adefovir dipivoxil, as active substance. The other ingredients in this formulation are commonly used in tablets Hepsera is supplied in high-density polyethylene bottle (HDPE), with silica gel desiccant canisters or sachets, and polyester fiber packing material. The closure system consists of a child-resistant polypropylene screw cap lined with an induction activated aluminium foil liner. Active substance Adefovir dipivoxil is an ester prodrug of the nucleotide analogue, adefovir. A structural modification of the parent drug has been carried out in order to increase the lipophilicity and to enhance the oral bioavailability of adefovir. The active substance is a white to off-white crystalline powder. It is soluble in ethanol, sparingly soluble in 0.1N HCl and very slightly soluble in water adjusted to pH 7.2 but relatively highly soluble at physiological pH. The active substance does not contain any chiral center and does not exhibit any optical isomerism. In laboratory studies the anhydrate crystal form has been observed to convert gradually into a dihydrate crystal form when adefovir dipivoxil was exposed to high humidity conditions (75% R.H., 25ºC) over an approximately one-month period. However, the only crystal form produced during the active substance synthesis and utilised in non-clinical and clinical studies has been the anhydrous crystal form. Adefovir dipivoxil undergoes also hydrolysis in aqueous solution and to a smaller degree in the solid state after exposure to humidity and heat for extended periods. -
Chapter 12 Antimicrobial Therapy Antibiotics
Chapter 12 Antimicrobial Therapy Topics: • Ideal drug - Antimicrobial Therapy - Selective Toxicity • Terminology - Survey of Antimicrobial Drug • Antibiotics - Microbial Drug Resistance - Drug and Host Interaction An ideal antimicrobic: Chemotherapy is the use of any chemical - soluble in body fluids, agent in the treatment of disease. - selectively toxic , - nonallergenic, A chemotherapeutic agent or drug is any - reasonable half life (maintained at a chemical agent used in medical practice. constant therapeutic concentration) An antibiotic agent is usually considered to - unlikely to elicit resistance, be a chemical substance made by a - has a long shelf life, microorganism that can inhibit the growth or - reasonably priced. kill microorganisms. There is no ideal antimicrobic An antimicrobic or antimicrobial agent is Selective Toxicity - Drugs that specifically target a chemical substance similar to an microbial processes, and not the human host’s. antibiotic, but may be synthetic. Antibiotics Spectrum of antibiotics and targets • Naturally occurring antimicrobials – Metabolic products of bacteria and fungi – Reduce competition for nutrients and space • Bacteria – Streptomyces, Bacillus, • Molds – Penicillium, Cephalosporium * * 1 The mechanism of action for different 5 General Mechanisms of Action for antimicrobial drug targets in bacterial cells Antibiotics - Inhibition of Cell Wall Synthesis - Disruption of Cell Membrane Function - Inhibition of Protein Synthesis - Inhibition of Nucleic Acid Synthesis - Anti-metabolic activity Antibiotics -
(MGH) COVID-19 Treatment Guidance
Version 8.0 4/28/2021 10:00AM © Copyright 2020 The General Hospital Corporation. All Rights Reserved. Massachusetts General Hospital (MGH) COVID-19 Treatment Guidance This document was prepared (in March, 2020-April, 2021) by and for MGH medical professionals (a.k.a. clinicians, care givers) and is being made available publicly for informational purposes only, in the context of a public health emergency related to COVID-19 (a.k.a. the coronavirus) and in connection with the state of emergency declared by the Governor of the Commonwealth of Massachusetts and the President of the United States. It is neither an attempt to substitute for the practice of medicine nor as a substitute for the provision of any medical professional services. Furthermore, the content is not meant to be complete, exhaustive, or a substitute for medical professional advice, diagnosis, or treatment. The information herein should be adapted to each specific patient based on the treating medical professional’s independent professional judgment and consideration of the patient’s needs, the resources available at the location from where the medical professional services are being provided (e.g., healthcare institution, ambulatory clinic, physician’s office, etc.), and any other unique circumstances. This information should not be used to replace, substitute for, or overrule a qualified medical professional’s judgment. This website may contain third party materials and/or links to third party materials and third party websites for your information and convenience. Partners is not responsible for the availability, accuracy, or content of any of those third party materials or websites nor does it endorse them. -
Anti-Inflammatory Effects of Amantadine and Memantine
Journal of Personalized Medicine Communication Anti-Inflammatory Effects of Amantadine and Memantine: Possible Therapeutics for the Treatment of Covid-19? Félix Javier Jiménez-Jiménez 1,* , Hortensia Alonso-Navarro 1 , Elena García-Martín 2 and José A. G. Agúndez 2 1 Section of Neurology, Hospital Universitario del Sureste, Arganda del Rey, E-28500 Madrid, Spain; [email protected] 2 University Institute of Molecular Pathology Biomarkers, UNEx. ARADyAL Instituto de Salud Carlos III, E-10071 Cáceres, Spain; [email protected] (E.G.-M.); [email protected] (J.A.G.A.) * Correspondence: [email protected]; Tel.: +34-636968395 Received: 2 October 2020; Accepted: 6 November 2020; Published: 9 November 2020 Abstract: We have reviewed current data on the anti-inflammatory effects of amantadine and memantine in clinical and in vivo models of inflammation, and we propose that these effects have potential interest for the treatment of the SARS-CoV-2 infection (COVID-19 disease). To that end, we performed a literature search using the PubMed Database from 1966 up to October 31 2020, crossing the terms “amantadine” and “memantine” with “inflammation” and “anti-inflammatory”. Amantadine and/or memantine have shown anti-inflammatory effects in chronic hepatitis C, in neuroinflammation induced by sepsis and by lipopolysaccharides, experimental models of multiple sclerosis, spinal cord injury, and respiratory diseases. Since the inflammatory response is one of the main pathogenetic mechanisms in the progression of the SARS-CoV-2 infection, anti-inflammatory effects of amantadine and memantine could be hypothetically useful in the treatment of this condition. This potential utility deserves further research. Keywords: amantadine; memantine; anti-inflammatory effects; SARS-Cov-2; COVID-19; therapy 1. -
Clinical Trial Details (PDF Generation Date :- Tue, 07 Sep 2021 08
PDF of Trial CTRI Website URL - http://ctri.nic.in Clinical Trial Details (PDF Generation Date :- Wed, 29 Sep 2021 20:12:22 GMT) CTRI Number CTRI/2020/12/029855 [Registered on: 16/12/2020] - Trial Registered Prospectively Last Modified On 30/03/2021 Post Graduate Thesis No Type of Trial Interventional Type of Study Biological Study Design Other Public Title of Study Phase III, Randomized, Controlled, Open-Label Study of Pegylated Interferon Alfa-2b With SARS-CoV-2 Scientific Title of A Phase III, Randomized, Controlled, Open-Label Study to Evaluate the Efficacy and Safety of Study Pegylated Interferon Alfa-2b In the Treatment of Adult Patients Diagnosed With SARS-CoV-2 (COVID-19). Secondary IDs if Any Secondary ID Identifier PEGI.20.005 Versoion 02,02 December 2020 Protocol Number Details of Principal Details of Principal Investigator Investigator or overall Name Dr Manjunath K Trial Coordinator (multi-center study) Designation Deputy General Manager Affiliation Cadila Healthcare Limited Address Zydus Research Center, Survey No. 396/403, Sarkhej-Bavla National Highway No.8A Moraiya, Ahmedabad - 382213 Ahmadabad GUJARAT 382213 India Phone Fax Email [email protected] Details Contact Details Contact Person (Scientific Query) Person (Scientific Name Dr Kevinkumar Kansagra Query) Designation General Manager Affiliation Cadila Healthcare Limited Address Zydus Research Center, Survey No. 396/403, Sarkhej-Bavla National Highway No.8A Moraiya, Ahmedabad - 382213 Ahmadabad GUJARAT 382213 India Phone Fax Email [email protected] Details Contact Details Contact Person (Public Query) Person (Public Query) Name Dr Balaji More Designation Senior General Manager Affiliation Cadila Healthcare Limited Address Zydus Research Center, Survey No. -
Antiviral Drug Resistance
Points to Consider: Antiviral Drug Resistance Introduction Development of resistance to antimicrobial agents (including antivirals) is considered to be a natural consequence of rapid replication of microorganisms in the presence of a selective pressure. I.e. it is a natural evolutionary event and should be an expected outcome of the use of antimicrobial agents. The speed with which such resistant organisms develop, and their ability to persist in the population, will be influenced by several factors including the extent to which the antimicrobial agent is used, and the viability of the new (mutated) resistant organism. Microorganisms may also differ naturally in their sensitivity to antimicrobial agents, and the existence of such insensitivity can have an impact on emergence of resistance in two ways. (i) It provides evidence that drug resistant organisms are viable, and could therefore emerge and persist in the population in response to drug use. (ii) Use of antimicrobial agents may create an environment in which pre‐existing insensitive strains may have a selective advantage and spread. Background to drug resistant influenza viruses 1 Adamantanes (amantadine, rimantidine) The existence of viruses resistant or insensitive to this class of antiviral agent is well documented. Many of the currently circulating strains of virus (both human and animal) lack sensitivity to these agents, and clinical use of amantadine or rimantadine has been shown to select for resistant viruses in a high proportion of cases, and within 2‐3 days of starting treatmenti. Such rapid emergence of resistance during treatment may explain the reduced efficacy of rimantidine or amantadine prophylaxis when the index cases were also treatedii. -
Prediction of Premature Termination Codon Suppressing Compounds for Treatment of Duchenne Muscular Dystrophy Using Machine Learning
Prediction of Premature Termination Codon Suppressing Compounds for Treatment of Duchenne Muscular Dystrophy using Machine Learning Kate Wang et al. Supplemental Table S1. Drugs selected by Pharmacophore-based, ML-based and DL- based search in the FDA-approved drugs database Pharmacophore WEKA TF 1-Palmitoyl-2-oleoyl-sn-glycero-3- 5-O-phosphono-alpha-D- (phospho-rac-(1-glycerol)) ribofuranosyl diphosphate Acarbose Amikacin Acetylcarnitine Acetarsol Arbutamine Acetylcholine Adenosine Aldehydo-N-Acetyl-D- Benserazide Acyclovir Glucosamine Bisoprolol Adefovir dipivoxil Alendronic acid Brivudine Alfentanil Alginic acid Cefamandole Alitretinoin alpha-Arbutin Cefdinir Azithromycin Amikacin Cefixime Balsalazide Amiloride Cefonicid Bethanechol Arbutin Ceforanide Bicalutamide Ascorbic acid calcium salt Cefotetan Calcium glubionate Auranofin Ceftibuten Cangrelor Azacitidine Ceftolozane Capecitabine Benserazide Cerivastatin Carbamoylcholine Besifloxacin Chlortetracycline Carisoprodol beta-L-fructofuranose Cilastatin Chlorobutanol Bictegravir Citicoline Cidofovir Bismuth subgallate Cladribine Clodronic acid Bleomycin Clarithromycin Colistimethate Bortezomib Clindamycin Cyclandelate Bromotheophylline Clofarabine Dexpanthenol Calcium threonate Cromoglicic acid Edoxudine Capecitabine Demeclocycline Elbasvir Capreomycin Diaminopropanol tetraacetic acid Erdosteine Carbidopa Diazolidinylurea Ethchlorvynol Carbocisteine Dibekacin Ethinamate Carboplatin Dinoprostone Famotidine Cefotetan Dipyridamole Fidaxomicin Chlormerodrin Doripenem Flavin adenine dinucleotide -
Novel Therapeutics for Epstein–Barr Virus
molecules Review Novel Therapeutics for Epstein–Barr Virus Graciela Andrei *, Erika Trompet and Robert Snoeck Laboratory of Virology and Chemotherapy, Department of Microbiology and Immunology, Rega Institute for Medical Research, KU Leuven, 3000 Leuven, Belgium; [email protected] (E.T.); [email protected] (R.S.) * Correspondence: [email protected]; Tel.: +32-16-321-915 Academic Editor: Stefano Aquaro Received: 15 February 2019; Accepted: 4 March 2019; Published: 12 March 2019 Abstract: Epstein–Barr virus (EBV) is a human γ-herpesvirus that infects up to 95% of the adult population. Primary EBV infection usually occurs during childhood and is generally asymptomatic, though the virus can cause infectious mononucleosis in 35–50% of the cases when infection occurs later in life. EBV infects mainly B-cells and epithelial cells, establishing latency in resting memory B-cells and possibly also in epithelial cells. EBV is recognized as an oncogenic virus but in immunocompetent hosts, EBV reactivation is controlled by the immune response preventing transformation in vivo. Under immunosuppression, regardless of the cause, the immune system can lose control of EBV replication, which may result in the appearance of neoplasms. The primary malignancies related to EBV are B-cell lymphomas and nasopharyngeal carcinoma, which reflects the primary cell targets of viral infection in vivo. Although a number of antivirals were proven to inhibit EBV replication in vitro, they had limited success in the clinic and to date no antiviral drug has been approved for the treatment of EBV infections. We review here the antiviral drugs that have been evaluated in the clinic to treat EBV infections and discuss novel molecules with anti-EBV activity under investigation as well as new strategies to treat EBV-related diseases. -
Multipurpose Tenofovir Disoproxil Fumarate Electrospun Fibers for the Prevention of HIV-1 and HSV-2 Infections
University of Louisville ThinkIR: The University of Louisville's Institutional Repository Electronic Theses and Dissertations 8-2016 Multipurpose tenofovir disoproxil fumarate electrospun fibers for the prevention of HIV-1 and HSV-2 infections. Kevin Tyo Follow this and additional works at: https://ir.library.louisville.edu/etd Part of the Other Chemicals and Drugs Commons, Polymer Chemistry Commons, Preventive Medicine Commons, and the Virus Diseases Commons Recommended Citation Tyo, Kevin, "Multipurpose tenofovir disoproxil fumarate electrospun fibers for the prevention of HIV-1 and HSV-2 infections." (2016). Electronic Theses and Dissertations. Paper 2486. https://doi.org/10.18297/etd/2486 This Master's Thesis is brought to you for free and open access by ThinkIR: The University of Louisville's Institutional Repository. It has been accepted for inclusion in Electronic Theses and Dissertations by an authorized administrator of ThinkIR: The University of Louisville's Institutional Repository. This title appears here courtesy of the author, who has retained all other copyrights. For more information, please contact [email protected]. MULTIPURPOSE TENOFOVIR DISOPROXIL FUMARATE ELECTROSPUN FIBERS FOR THE PREVENTION OF HIV-1 AND HSV-2 INFECTIONS By Kevin Tyo B.S. Virginia Tech, 2010 A Thesis Submitted to the Faculty of the School of Medicine of the University of Louisville In Partial Fulfillment of the Requirement for the Degree of Master of Science In Pharmacology and Toxicology Department of Pharmacology and Toxicology School of Medicine University of Louisville Louisville, KY August, 2016 MULTIPURPOSE TENOFOVIR DISOPROXIL FUMARATE ELECTROSPUN FIBERS FOR THE PREVENTION OF HIV-1 AND HSV-2 INFECTIONS By Kevin Tyo B.S.