DOCSLIB.ORG

RILPIVIRINE Antiretrovirals

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
RILPIVIRINE Antiretrovirals RILPIVIRINE antiretrovirals. immediately if you develop a rash while taking rilpivirine. In most cases, the rash Your dosage is: can be treated with anti-inflammatory drugs Other NAMES: Edurant™ or antihistamines. Consult your doctor or 25 mg white tablets pharmacist before taking any medications Why is this drug prescribed? to treat the rash. ____ tablet(s) (____mg) once daily Rilpivirine is an antiretroviral (anti-HIV) drug If you develop a severe rash, or a rash with that is part of the non-nucleoside reverse What should you do if you FORGET a symptoms such as fever, blistering, mouth transcriptase inhibitor (NNRTIs or Non dose? sores, red eyes, swelling, muscle or joint Nukes) family. It is used together with other aches and a general feeling of being unwell, antiretrovirals for the treatment of HIV-1 If you miss a dose of rilpivirine, and it is less STOP taking rilpivirine. Speak with your infection in adult patients who have never than 12 hours since the appointed time doctor immediately. taken HIV medications before (treatment- take it as soon as possible, with a meal; naïve adult patients). It may also be used then take your next dose at the scheduled Some people taking rilpivirine may together with other antiretrovirals in time. However, if it is more than 12 hours experience depression or mood changes. treatment-experienced adult patients, who since you missed your dose, do not take a Contact your doctor if you feel symptoms of have failed previous therapy, and have HIV- dose until your next regularly scheduled sadness or hopelessness, thoughts of 1 strains which are resistant to other dose. hurting yourself, anxiety or restlessness, or retrovirals and NNRTIs. Rilpivirine is used have had previous struggles with to delay the progression of HIV infection. By Why should you not forget to take this depression. using rilpivirine, your immune system + drug? should improve (increase in CD4 count) Other side effects people experience and you will be better protected against If you miss doses of rilpivirine, the amount include headache, trouble sleeping, and opportunistic infections. of HIV virus in your blood (known as the changes in body fat distribution. viral load) will start increasing again and Rilpivirine does not cure AIDS or completely your immune system will be further Your doctor will do blood tests regularly to kill the HIV virus, but helps to prevent damaged. A few missed doses can be see if there are any changes in your liver further damage by slowing down the enough for rilpivirine to stop being active, function, cholesterol and triglyceride levels. production of new viruses. Treatment with which is a phenomenon known as rilpivirine does not reduce the risk of resistance . When this happens, other It is important that you keep your doctor passing infection on to others. You will still antiretrovirals that work in a similar way as appointments and come for your be able to pass HIV by sexual contact, by rilpivirine may also become inactive. laboratory tests so that your progress blood transfer or by sharing needles. You Therefore, missing doses of rilpivirine can be followed. should always use appropriate precautions can decrease treatment options for the to prevent passing HIV on to others. future. Please do not stop rilpivirine without talking to your doctor first. HOW should this drug be taken? What ADVERSE EFFECTS can this drug What other PRECAUTIONS should you cause? What should you do about follow while using this drug? The recommended dose of rilpivirine is 25 mg once daily with a meal. Rilpivirine them? You must make sure that you are taking the should always be taken with a standard or right dose. If you take higher doses of high-fat meal together with other Some people taking rilpivirine may develop a mild to moderate rash. Tell your doctor rilpivirine than what is prescribed, you may increase the chance of having adverse 1-800-258-4263. Breastfeeding is NOT effects. If you take lower doses of rilpivirine recommended if you have HIV as you can than what is prescribed, the HIV virus may transmit the virus to your baby through your become resistant to rilpivirine. breast milk. Certain drugs can increase or decrease the How should this drug be STORED? effect of rilpivirine. Rilpivirine should be stored in a cool (15- ° The following drugs should not be taken 30 C) dry place, protected from light and with rilpivirine: well out of the reach of children, in its original bottle. Ensure that the drug has not Anticonvulsants (carbamazepine, expired by checking the expiry date (“EXP”) oxcarbazepine, phenobarbital, shown on the outside of the package. Do phenytoin) not remove the small dessicant packs Rifamycins (rifampin, rifabutin, included with your medication. RILPIVIRINE rifapentine) Proton pump inhibitors (e.g. Do not store in your bathroom or kitchen, as esomeprazole, lansoprazole, heat and moisture may cause the drug to omeprazole, pantoprazole, rabeprazole) be less active. Systemic dexamethasone (more than a MEDICATION single dose) If you have any questions or concerns St. John’s Wort ( Hypericum perforatum ) about this drug or if you are experiencing adverse effects, please FACT SHEET Also, rilpivirine might influence the effect of discuss them with your pharmacist, other drugs you are taking. Inform your doctor or nurse. doctor and pharmacist of all prescribed and non-prescribed drugs you are taking. As Write questions or concerns down to well, you should inform them of natural ensure they are addressed. products or recreational (street) drugs you are taking. If you wish to start a new drug or The following pharmacist is available to natural product, please consult with your answer questions: pharmacist before doing so. Pharmacist: __________________ Rilpivirine should NOT be taken if you Telephone: __________________ are pregnant. Please inform your doctor if you believe you are pregnant or if you wish to become pregnant in the near future. Reference: Product Monograph Edurant™ (rilpivirine). Your doctor can recommend an appropriate Janssen-Ortho Inc., Toronto, ON, Canada: 2011. Prepared treatment to help reduce the risk of passing by the Ontario HIV Pharmacy Professional Specialty Group, 2012. the HIV virus on to your baby. A registry has been established to follow patients who Additional medication fact sheets and updates may be found are exposed to rilpivirine during pregnancy. at: www.hivclinic.ca Your doctor may register you by calling .
Load more

Recommended publications
  • Emtricitabine, Rilpivirine, and Tenofovir Disoproxil Fumarate
    PATIENT & CAREGIVER EDUCATION Emtricitabine, Rilpivirine, and Tenofovir Disoproxil Fumarate This information from Lexicomp® explains what you need to know about this medication, including what it’s used for, how to take it, its side effects, and when to call your healthcare provider. Brand Names: US Complera Brand Names: Canada Complera Warning Hepatitis B has gotten worse when this drug was stopped in some people with hepatitis B. Close follow-up for a few months is needed when therapy is stopped in people who have hepatitis B. Do not stop taking this drug without calling your doctor. Hepatitis B testing needs to be done as you were told by the doctor. Talk with the doctor. What is this drug used for? It is used to treat HIV infection. Emtricitabine, Rilpivirine, and Tenofovir Disoproxil Fumarate 1/7 What do I need to tell my doctor BEFORE I take this drug? If you are allergic to this drug; any part of this drug; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had. If you have kidney disease. If you take any drugs (prescription or OTC, natural products, vitamins) that must not be taken with this drug, like some other drugs used for HIV or certain drugs used for seizures, infection, or stomach or bowel problems. There are many drugs that must not be taken with this drug. If you are breast-feeding. Do not breast-feed while you take this drug. This is not a list of all drugs or health problems that interact with this drug.
    [Show full text]
  • Antivirals: HIV –Cabotegravir/Rilpivirine (Cabenuva) Medical Policy No
    Antivirals: HIV –Cabotegravir/rilpivirine (Cabenuva) Medical policy no. 12.10.99.AB-1 Effective Date: June 1, 2021 Related medical policies: • 12.10.99 Antivirals- HIV Combinations • 12.10.99.AA Antivirals – HIV: emtricitabine-tenofovir (Descovy) Note: New-to-market drugs included in this class based on the Apple Health Preferred Drug List (AHPDL) are non-preferred and subject to this prior authorization (PA) criteria. Non-preferred agents in this class require an inadequate response or documented intolerance due to severe adverse reaction or contraindication to at least ONE preferred regimen. If a drug within this policy receives a new indication approved by the Food and Drug Administration (FDA), medical necessity for the new indication will be determined on a case-by-case basis following FDA labeling. To see the list of the current AHPDL, please visit: https://www.hca.wa.gov/assets/billers-and-providers/apple-health-preferred-drug-list.xlsx Before authorization of Cabenuva will be approved, documentation from TheraCom specialty pharmacy showing the patient has been established on Vocabria must be included. Documentation must include patient’s name, patient’s date of birth, NDC, quantity/days supply, and date patient received the medication. TheraCom Pharmacy contact information: TheraCom Mailing Address: TheraCom VIIV Specific Team numbers (Used to locate TheraCom in e-Prescribing systems) Phone: 1-844-276-6299 TheraCom Fax: 1-833-904-1881 345 International Blvd Ste 200 Brooks, KY 40109 Background: Human immunodeficiency virus (HIV) is a single-stranded RNA retrovirus that attacks the immune system, specifically CD4+ T-helper cells, causing a progressive decrease in CD4+ T cell count and increased susceptibility of a person to infections.
    [Show full text]
  • Injectable Antiretroviral Drugs: Back to the Future
    viruses Review Injectable Antiretroviral Drugs: Back to the Future Marco Berruti 1 , Niccolò Riccardi 2, Diana Canetti 3,4 , Sergio Lo Caputo 5 , Lucia Taramasso 6 and Antonio Di Biagio 1,6,* 1 Infectious Diseases Unit, Department of Health Sciences (DISSAL), University of Genoa, 16132 Genoa, Italy; [email protected] 2 Department of Infectious-Tropical Diseases and Microbiology, IRCCS Sacro Cuore Don Calabria Hospital, Negrar di Valpolicella, 37024 Verona, Italy; [email protected] 3 Clinic of Infectious Diseases, IRCCS San Raffaele Scientific Institute, 20097 Milan, Italy; [email protected] 4 School of Medicine, Vita-Salute San Raffaele University, 20097 Milan, Italy 5 Clinic of Infectious Diseases, Department of Clinical and Experimental Medicine, University of Foggia, 71122 Foggia, Italy; [email protected] 6 Infectious Diseases Unit, Department of Internal Medicine, Ospedale Policlinico San Martino IRCCS, 16132 Genoa, Italy; [email protected] * Correspondence: [email protected] Abstract: Current HIV treatment regimens provide sustained virologic suppression, at least partially restore the immune system and have limited side effects; however, they do not allow viral eradication and they are burdened by daily pill intake with a life-long commitment for the people living with HIV (PHIV). Injectable agents might represent a turning point in the care of PHIV, allowing less frequent administration of antiretroviral treatment (ART), more widespread use of pre-exposure prophylaxis (PrEP) and more stable drug levels in the blood, thus increasing the odds to get closer to end the HIV pandemic. The aim of this manuscript is to give a comprehensive review of injectable antiretrovirals that have been used in the past, which are available now, will be available in the future, and their role in the treatment of HIV infection Citation: Berruti, M.; Riccardi, N.; Canetti, D.; Lo Caputo, S.; Taramasso, Keywords: ART; injectable; HIV; antiretroviral; treatment; PrEP L.; Di Biagio, A.
    [Show full text]
  • Complera Pi.Pdf
    HIGHLIGHTS OF PRESCRIBING INFORMATION Patients should currently be on their first or second antiretroviral These highlights do not include all the information needed to use regimen prior to switching therapy. COMPLERA safely and effectively. See full prescribing Patients should have no current or past history of resistance to information for COMPLERA. any of the three components of COMPLERA. COMPLERA® (emtricitabine, rilpivirine, tenofovir disoproxil Additional monitoring of HIV-1 RNA and regimen tolerability is fumarate) tablets, for oral use recommended after replacing therapy to assess for potential virologic Initial U.S. Approval: 2011 failure or rebound. (1) -----------------------DOSAGE AND ADMINISTRATION----------------------- WARNING: LACTIC ACIDOSIS/SEVERE HEPATOMEGALY WITH STEATOSIS and POST TREATMENT ACUTE EXACERBATION Dose in patients 12 years of age and older: One tablet (containing OF HEPATITIS B 200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of See full prescribing information for complete boxed warning. tenofovir disoproxil fumarate) taken once daily with food. (2) Dose in renal impairment: Should not be administered in patients Lactic acidosis and severe hepatomegaly with steatosis, with estimated creatinine clearance below 50 mL per minute. (2) including fatal cases, have been reported with the use of nucleoside analogs, including tenofovir disoproxil With rifabutin coadministration, an additional 25 mg tablet of fumarate, a component of COMPLERA. (5.1) rilpivirine (Edurant) once per day is recommended
    [Show full text]
  • Estonian Statistics on Medicines 2016 1/41
    Estonian Statistics on Medicines 2016 ATC code ATC group / Active substance (rout of admin.) Quantity sold Unit DDD Unit DDD/1000/ day A ALIMENTARY TRACT AND METABOLISM 167,8985 A01 STOMATOLOGICAL PREPARATIONS 0,0738 A01A STOMATOLOGICAL PREPARATIONS 0,0738 A01AB Antiinfectives and antiseptics for local oral treatment 0,0738 A01AB09 Miconazole (O) 7088 g 0,2 g 0,0738 A01AB12 Hexetidine (O) 1951200 ml A01AB81 Neomycin+ Benzocaine (dental) 30200 pieces A01AB82 Demeclocycline+ Triamcinolone (dental) 680 g A01AC Corticosteroids for local oral treatment A01AC81 Dexamethasone+ Thymol (dental) 3094 ml A01AD Other agents for local oral treatment A01AD80 Lidocaine+ Cetylpyridinium chloride (gingival) 227150 g A01AD81 Lidocaine+ Cetrimide (O) 30900 g A01AD82 Choline salicylate (O) 864720 pieces A01AD83 Lidocaine+ Chamomille extract (O) 370080 g A01AD90 Lidocaine+ Paraformaldehyde (dental) 405 g A02 DRUGS FOR ACID RELATED DISORDERS 47,1312 A02A ANTACIDS 1,0133 Combinations and complexes of aluminium, calcium and A02AD 1,0133 magnesium compounds A02AD81 Aluminium hydroxide+ Magnesium hydroxide (O) 811120 pieces 10 pieces 0,1689 A02AD81 Aluminium hydroxide+ Magnesium hydroxide (O) 3101974 ml 50 ml 0,1292 A02AD83 Calcium carbonate+ Magnesium carbonate (O) 3434232 pieces 10 pieces 0,7152 DRUGS FOR PEPTIC ULCER AND GASTRO- A02B 46,1179 OESOPHAGEAL REFLUX DISEASE (GORD) A02BA H2-receptor antagonists 2,3855 A02BA02 Ranitidine (O) 340327,5 g 0,3 g 2,3624 A02BA02 Ranitidine (P) 3318,25 g 0,3 g 0,0230 A02BC Proton pump inhibitors 43,7324 A02BC01 Omeprazole
    [Show full text]
  • EDURANT with HIGHLIGHTS of PRESCRIBING INFORMATION Drugs with a Known Risk of Torsade De Pointes
    1 • Caution should be given to prescribing EDURANT with HIGHLIGHTS OF PRESCRIBING INFORMATION drugs with a known risk of Torsade de Pointes. (5.1) These highlights do not include all the information needed to • Depressive Disorders: Severe depressive disorders (depressed use EDURANT safely and effectively. See full prescribing mood, depression, dysphoria, major depression, mood information for EDURANT. altered, negative thoughts, suicide attempt, suicidal ideation) EDURANT (rilpivirine) [Tablets] have been reported. Immediate medical evaluation is recommended for severe depressive disorders. (5.2) Initial U.S. Approval: 2011 • Patients may develop redistribution/accumulation of body fat (5.3) or immune reconstitution syndrome. (5.4) --------------------INDICATIONS AND USAGE---------------------- EDURANT is a human immunodeficiency virus type 1 (HIV-1) ------------------------ADVERSE REACTIONS------------------------ specific, non-nucleoside reverse transcriptase inhibitor (NNRTI) The most common adverse drug reactions to EDURANT indicated: (incidence > 2%) of at least moderate to severe intensity In combination with other antiretroviral agents for the treatment of (> Grade 2) were depression, insomnia, headache and rash. (6) HIV-1 infection in treatment-naïve adult patients. To report SUSPECTED ADVERSE REACTIONS, contact The following points should be considered when initiating therapy Tibotec Therapeutics at 1-877-REACH-TT or 1-877-732-2488 with EDURANT: or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. • More EDURANT treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced -------------------------DRUG INTERACTIONS---------------------- virologic failure compared to subjects with HIV-1 RNA less • EDURANT should not be used in combination with NNRTIs. than 100,000 copies/mL at the start of therapy.
    [Show full text]
  • Emtricitabine/Rilpivirine/Tenofovir Alafenamide
    Odefsey® (emtricitabine/rilpivirine/tenofovir alafenamide) – New Drug Approval • On March 1, 2016, Gilead announced the FDA approval of Odefsey (emtricitabine/ rilpivirine/ tenofovir alafenamide), as a complete regimen for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in patients ≥ 12 years of age as initial therapy in those with no antiretroviral treatment history with HIV-1 RNA ≤ 100,000 copies per mL; or to replace a stable antiretroviral regimen in those who are virologically-suppressed (HIV-1 RNA < 50 copies/mL) for at least six months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Odefsey. • Odefsey is a fixed dose combination tablet containing emtricitabine and tenofovir alafenamide, both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTI), and rilpivirine, an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). • Gilead’s Genvoya® (elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide) was the first tenofovir alafenamide-based regimen that was recently FDA-approved. • The safety and efficacy of Odefsey is supported by clinical studies of rilpivirine-based therapy and emtricitabine/ tenofovir alafenamide-based therapy in a range of patients with HIV, including treatment- naïve adults and adolescents, virologically suppressed adults who switched from protease inhibitor-, NNRTI-, and integrase strand transfer inhibitor-based regimens, and virologically suppressed adults with mild-to-moderate renal impairment. • A bioequivalence study demonstrated that Odefsey achieved similar drug levels of emtricitabine and tenofovir alafenamide as Genvoya and similar drug levels of rilpivirine as Edurant® (rilpivirine). • Odefsey carries a boxed warning for lactic acidosis/severe hepatomegaly with steatosis and post- treatment acute exacerbation of hepatitis B.
    [Show full text]
  • Antiviral Activity and Safety of Long-Acting Cabotegravir Plus Long-Acting Rilpivirine Administered Every 2 Months in Hiv-Positi
    ANTIVIRAL ACTIVITY AND SAFETY OF LONG-ACTING CABOTEGRAVIR PLUS LONG-ACTING RILPIVIRINE ADMINISTERED EVERY 2 MONTHS IN HIV-POSITIVE PARTICIPANTS: RESULTS FROM THE POLAR STUDY Anthony Mills1, Gary J. Richmond2, Cheryl Newman3, Olayemi Osiyemi4, Jerry Cade5, Cynthia Brinson6, Jerome De Vente7, Nisha Andany8, David A. Margolis9, Kenneth C. Sutton9, Viviana Wilches10, Jeremy Roberts11, Cynthia McCoig12, Kati Vandermeulen13, William Spreen9 1Men’s Health Foundation, Los Angeles, CA, United States; 2Broward Health Medical Center, Broward Health Imperial Point, Fort Lauderdale, FL, United States; 3Augusta University Medical Center, Augusta, GA, United States; 4Triple O Research Institute PA, West Palm Beach, FL, United States; 5Wellness Center UMC of Southern Nevada, Las Vegas, NV, United States; 6Central Texas Clinical Research, Austin, TX, United States; 7Long Beach Education and Research Consultants, Long Beach, CA, United States; 8Sunnybrook Health Sciences Centre, Toronto, ON, Canada; 9ViiV Healthcare, Research Triangle Park, NC, United States; 10GlaxoSmithKline, Upper Providence, PA, United States; 11GlaxoSmithKline, Mississauga, ON, Canada; 12ViiV Healthcare, Tres Cantos, Spain; 13Janssen Research and Development, Beerse, Belgium IDWeek™ 2020; October 21–25, 2020; Virtual Financial Disclosures • The POLAR study was funded by ViiV Healthcare and Janssen Pharmaceuticals • Anthony Mills has received research funding and consulting fees from ViiV Healthcare, Gilead, Janssen Pharmaceuticals, and Merck Sharp & Dohme, and consulting fees from
    [Show full text]
  • Antiretrovirals and the Kidney in Current Clinical Practice: Renal Pharmacokinetics, Alterations of Renal Function and Renal Toxicity
    EDITORIAL REVIEW Antiretrovirals and the kidney in current clinical practice: renal pharmacokinetics, alterations of renal function and renal toxicity Jean C. Yombia,b, Anton Pozniakb, Marta Boffitob, Rachael Jonesb, Saye Khooc, Jeremy Levyd and Frank A. Poste Assessment of renal function in HIV-positive patients is of increasing importance in the context of ageing and associated comorbidities. Exposure to nephrotoxic medications is widespread, and several commonly used antiretroviral drugs have nephrotoxic potential. Moreover, specific antiretrovirals inhibit renal tubular transporters resulting in the potential for drug–drug interactions as well as increases in serum creatinine concentrations, which affect estimates of glomerular filtration rate in the absence of changes in actual glomerular filtration rate. This review explores the effects of antiretroviral therapy on the kidney and offers an understanding of mechanisms that lead to apparent and real changes in renal function. ß 2014 Wolters Kluwer Health | Lippincott Williams & Wilkins AIDS 2014, 28:621–632 Keywords: estimated glomerular filtration rate, HIV, kidney, pharmacokinetics, therapy, transporters Introduction and is an important risk factor for cardiovascular events and death [5–8]. Older age, black ethnicity, hypertension, The life expectancy of HIV-positive individuals exposed diabetes, low CD4þ cell count, hepatitis C virus (HCV) to combination antiretroviral therapy (cART) at the coinfection and high HIV RNA levels have been currently recommended CD4þ cell count threshold identified as risk factors for CKD, end-stage kidney approaches that of the general population [1]. As a disease and renal death [9–11], and specific antiretrovirals consequence of the widespread use of cART, ageing of [indinavir (IDV), tenofovir disoproxil fumarate (TDF), HIV-positive patients has been observed in many atazanavir (ATV) and lopinavir (LPV)] may further cohorts, with conditions such as cardiovascular disease, increase this risk [11–13].
    [Show full text]
  • Viewed and Approved the Final Manuscript
    Pasquau et al. BMC Infectious Diseases (2019) 19:207 https://doi.org/10.1186/s12879-019-3817-6 RESEARCH ARTICLE Open Access Effectiveness and safety of dual therapy with rilpivirine and boosted darunavir in treatment-experienced patients with advanced HIV infection: a preliminary 24 week analysis (RIDAR study) Juan Pasquau1* , Samantha E. de Jesus1, Piedad Arazo2, María J. Crusells3, María J. Ríos4, Fernando Lozano5, Javier de la Torre6, María J. Galindo7, Jorge Carmena8, Jesús Santos9, Carlos Tornero10, Guillermo Verdejo3, Gloria Samperiz2, Zaira Palacios4, Carmen Hidalgo-Tenorio1 and on behalf of the RIDAR Study Group Abstract Background: The objective was to analyze the effectiveness and safety of dual therapy with rilpivirine plus boosted- darunavir (RPV + bDRV) in real-life patients. Methods: Observational, retrospective, multi-center study in HIV+ patients who had received RPV + bDRV for 24 weeks to optimize/simplify their previous antiretroviral treatment. We determined the percentage of patients without virologic failure (2 consecutive viral loads > 50 copies/mL) at 24 weeks of treatment. Results: The study included 161 patients from 15 hospitals with median age of 49 years; 29.3% had previous AIDS stage and median CD4+ lymphocyte nadir of 170 cells/uL. They had been diagnosed with HIV for a median of 17 years and had received 14 years of ART, with five previous treatment combinations, and 36.6% had a history of virological failure. The reasons for the switch were simplification/optimization (49.7%), toxicity/intolerance (17.4%), or inadequate effectiveness of previous ART (10.6%). Baseline VL of 50–1000 copies/mL was recorded in 25.5% of the patients.
    [Show full text]
  • Design, Chemical Synthesis and Biological Evaluation of Potential New Antiviral Agents
    International Doctoral School in Biomolecular Sciences XXV Cycle Design, Chemical Synthesis and Biological Evaluation of Potential New Antiviral Agents Tutor Prof. Ines MANCINI University of Trento, Italy Ph.D. Thesis of Andrea DEFANT University of Trento, Italy 1 2 to my parents 3 4 Contents List of Abbreviations v List of Figures ix List of Schemes xii List of Tables xv Abstract 1 1. INTRODUCTION 3 1.1. Structure of HIV virion 4 1.2. HIV life cycle 6 1.3. Possible targets for anti-HIV agents and clinically used therapeutic agents 7 1.4. Reverse transcriptase enzyme 17 1.5. HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) 19 1.6. Drug design of new potential NNRTI molecules 25 2. MATERIAL AND METHODS 37 2.1. Computational approach 37 2.2. Chemistry 37 2.2.1 General 38 2.2.2 Instruments 38 2.2.3 Chemical procedures of synthesis 2.3. Biological assays 39 2.3.1. ELISA enzymatic assay 39 2.3.2. In vitro anti-HIV activity 39 2.3.3. In vitro antiviral activity 39 2.3.4. Antibacterial activity 40 3. RESULTS 43 3.1. Drug design 43 3.1.1. Docking calculation 45 3.1.1.1. Proteins preparation 45 3.1.1.2. Preparation of ligands 46 3.1.1.3. Molecular docking 47 3.1.1.4 ADME and drug-like properties prediction 50 i 3.2. Chemical synthesis and structural characterization of the new molecules 55 3.2.1. Precursors 29, 30 and 35 58 3.2.2. Tosylate precursors 59 3.2.2.1.
    [Show full text]
  • Usage of Antivirals and the Occurrence of Antiviral Resistance in Norway 2018
    REPORT 2019 Usage of Antivirals and the Occurrence of Antiviral Resistance in Norway 2018 RAVN Resistensovervåking av virus i Norge Resistance against Antivirals in Norway Usage of Antivirals and the Occurrence of Antiviral resistance in Norway 2018 RAVN Resistensovervåkning av virus i Norge Resistance against antivirals in Norway 2 Published by the Norwegian Institute of Public Health Division of Infection Control and Environmental Health Department for Infectious Disease registries October 2019 Title: Usage of Antivirals and the Occurrence of Antiviral Resistance in Norway 2018. RAVN Ordering: The report can be downloaded as a pdf at www.fhi.no Graphic design cover: Fete Typer ISBN nr: 978-82-8406-032-3 Emneord (MeSH): Antiviral resistance Any usage of data from this report should include a specific reference to RAVN. Suggested citation: RAVN. Usage of Antivirals and the Occurrence of Antiviral Resistance in Norway 2018. Norwegian Institute of Public Health, Oslo 2019 Resistance against antivirals in Norway • Norwegian Institute of Public Health 3 Table of contents Introduction _________________________________________________________________________ 4 Contributors and participants __________________________________________________________ 5 Sammendrag ________________________________________________________________________ 6 Summary ___________________________________________________________________________ 8 1 Antivirals and development of drug resistance ______________________________________ 10 2 The usage of antivirals in Norway
    [Show full text]