Optumrx Premium Formulary Exclusions 2021

Total Page:16

File Type:pdf, Size:1020Kb

Optumrx Premium Formulary Exclusions 2021 Jan. 1, 2020 Premium Formulary Exclusions & Preferred Specialty Prior Authorization Requirements Therapeutic Category Excluded Medications Preferred Alternatives ALLERGIC REACTIONS epinephrine injection made by Anaphylaxis Treatment Auvi-Q (0.15mg, 0.3mg), Epi-Pen JR 0.15mg My lan, epinephrine injection, Epi-Pen 0.3mg ANALGESICS celecoxib, diflunisal, etodolac, Cambia fenoprofen, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, meclofenamate, meloxicam, Oral nabumetone, naproxen, Zorvolex oxaprozin, piroxicam, sulindac, tolmetin Non-Steroidal Anti- Inflammatory Agents Qmiiz ODT meloxicam Flector diclofenac patch Topical Pennsaid diclofenac solution diclofenac, ibuprofen, Other Sprix Nasal Spray meloxicam Opioid Apadaz, hydrocodone/acetaminophen, combinations Benzhydrocodone/acetaminophen oxycodone/acetaminophen hydromorphone HCl ER, Arymo ER, Kadian ER 200 mg, morphine sulfate ER, Nuc y nta ER, Oxycodone Pow der, Oral Long- oxymorphone HCl ER, Oxycodone ER ( M) , Xtampza ER, Acting Embeda, Hysingla ER, Zohydro ER Opioid OxyContin Analgesics Conzip, Tramadol ER 100mg, Pain tramadol 200mg, 300mg (M) Oral Short- codeine sulfate, Acting hydromorphone HCl, morphine Nucynta Opioid sulfate, oxycodone HCl, Analgesics oxymorphone HCl Transmucosal Abstral, Fentora, Fentanyl Citrate Fentanyl Buccal Tab (M), fentanyl citrate lozenge Analgesics Lazanda, Subsys (M) Co-branded product * Tier 3 pref erred 1 Existing utilizers of these medications will be allowed to continue on therapy. Grandfathering will not be provided for any other excluded drugs. Therapeutic Category Excluded Medications Preferred Alternatives ANTIBACTERIALS, ORAL Doryx MPC, Doxycycline Hyclate delayed release Oral Antibiotics doxycycline, minocycline 80mg, Minolira, Targadox ANTICONV ULSANT S Trokendi XR1 topiramate ER 1 Seizure Disorders Oxtellar XR oxcarbazepine IR lamotrigine ODT, lamotrigine Lamictal ODT Kit, Lamictal XR Kit XR ANTIFUNGAL S, ORAL Oral Antifungals Tolsura Itraconazole cap ANTIM IGRAINES amitriptyline, atenolol, divalproex sodium, nadolol, CGRP Antagonists Ajovy propranolol, timolol, topiramate, venlafaxine, Aimovig, Emgality rizatriptan ODT, sumatriptan Serotonin Receptor Agonists Onzetra Xsail, Zembrace Symtouch injection, sumatriptan nasal spray, zolmitriptan ODT ANTIPARKINS ON AGENTS Parkinson's Disease Gocovri, Osmolex ER amantadine ANTIPSYCHOTICS Schizophrenia Risperdal CONSTA, Risperdal injection risperidone injection ANTIV IRALS Ledipasvir-Sofosbuvir (M) , Sofosbuvir-Velpatasvir Hepatitis-C drugs Epclusa, Harvoni, Mavyret ( M) Please talk w ith your doctor HIV drugs Atripla1 about clinically appropriate options. AUTONOM IC & CENTRAL NERV OUS SYSTEM Interferon Beta Medications for Extavia1, Plegridy1 Avonex, Betaseron Multiple Sclerosis CARDIOV ASCULA R diltiazem hcl coated beads ER Cardizem LA 120mg 120mg Hypertension Inderal XL , Innopran XL propranolol ER Kapspargo metoprolol ER atorvastatin, fluvastatin, Cholesterol-Low ering lovastatin, pravastatin, Zypitamag Agents rosuvastatin, simvastatin, Livalo (M) Co-branded product * Tier 3 pref erred 1 Existing utilizers of these medications will be allowed to continue on therapy. Grandfathering will not be provided for any other excluded drugs. Therapeutic Category Excluded Medications Preferred Alternatives CORTICOSTEROI DS Oral Steroids Rayos prednisone Imiquimod cream 3.75% (M), Zyclara, Zyclara Actinic Keratosis Imiquimod 5% cream Pump DERMATOLOGIC AL AGENTS adapalene, adapalene/benzoyl peroxide, clindamycin gel/lotion/solution, Aktipak, Clindagel, Clindamycin phosphate 1% clindamycin/benzoyl peroxide, gel(M), Veltin Topical Acne Treatment erythromycin/benzoyl peroxide, tretinoin cream, Epiduo Forte, Onexton Adapalene lotion (M), Differin lotion adapalene Topical anesthetics ZTlido lidocaine patch Topical Antifungals Jublia terbinafine, Kerydin metronidazole cream/gel/lotion, Topical Antiinfectives Noritate cream Soolantra ALA Scalp lotion, Micort-HC c ream hydrocortisone Apexicon E cream fluocinonide, betamethasone Der ma-Smoothe/FS, Capex shampoo flucinolone acetonide scalp oil Cloderm cream clocortolone pivalate Cordran tape flurandrenolide flurandrenolide, hydrocortisone Desonate gel, Pandel cream valerate, triamcinolone Topical Corticosteroids acetonide betamethasone, clobetasol, Halobetasol foam(M), Lexette halobetasol cream/ointment fluticasone ointment, Halog cream/ointment halobetasol cream/ointment, triamcinolone Impoyz cream clobetasol Psorcon cream, Verdeso foam betamethasone, fluocinolone hydrocortisone valerate, Trianex ointment triamcinolone acetonide clobetasol proprionate, Ultravate lotion fluocinonide, halobetasol proprionate (M) Co-branded product * Tier 3 pref erred 1 Existing utilizers of these medications will be allowed to continue on therapy. Grandfathering will not be provided for any other excluded drugs. Therapeutic Category Excluded Medications Preferred Alternatives DERMATOLOGIC AL AGENTS Topical Plaque Psoriasis Sorilux calcipotriene Treatment DIABETES Examples: Abbott (FreeStyle, Precision), Blood Glucose Meters, Test Arkray(Glucocard), Bayer (Breeze, Contour), Lifescan (One Touch products) Strips and Control Solutions Nipro (TRUEtest, TRUEtrack), Roche (Accu- Chek) Continuous Glucose Freestyle Libre Dexcom Monitoring (CGM) Blood Sugar Regulators metformin HCl 24hr ER osmotic release, metformin ER (generic Miscellaneous metformin HCl 24hr ER modified release GLUCOPHA GE XR ) Dipeptidyl Peptidase-4 Alogliptin(M), Alogliptin w ith metformin(M), Janumet, Janumet XR, (DPP4) Inhibitors & Alogliptin w ith pioglitazone( M) , Kazano, Januvia, Jentadueto, Combinations Kombiglyze XR, Nesina, Onglyza, Oseni Jentadueto XR, Tradjenta Basal insulins Basaglar, Levemir, Tresiba Lantus, Toujeo Bydureon, Bydureon BCise, Glucagon-Like Peptide- Adlyxin, Tanzeum Byetta, Ozempic, Trulicity, 1(GLP1) Agonists Victoza Insulins Novolin Humulin Rapid-acting insulins Admelog, Apidra, Fiasp, Lispro, Novolog Humalog Sodium-glucose co- Invokamet, Invokamet XR, transporter (SGLT2) Farxiga, Segluromet, Steglatro, Xigduo XR Invokana, Jardiance, Synjardy, Inhibitors Synjardy XR SGLT2 and DPP4 QTERN, Steglujan Glyxambi Combinations ENDOC RI NE (OTHER) Estrogens Delestrogen 10mg/ml estradiol valerate Norditropin, Nutropin, Grow th Hormones Genotropin, Humatrope, Saizen, Zomacton Omnitrope Bravelle, Gonal-F, Gonal-F RFF Follistim AQ Infertility ganirelix (made by Cetrotide Organon/Merck) Nocturia Noctiva desmopressin, Nocdurna GASTROINTESTINAL diphenoxylate/atropine, Anti-Diarrheal Agents Motofen loperamide granisetron solution/tablet, Antiemetics Sancuso patch ondansetron ODT Anti-Inflammatory, famotidine w ith ibuprofen, Duexis, Vimovo Anti-Ulcer Agents omeprazole w ith naproxen Irritable Bow el Syndrome w ith Constipation/ Chronic Amitiza, Trulance Linzess Idiopathic Constipation (IBS- C/CIC) (M) Co-branded product * Tier 3 pref erred 1 Existing utilizers of these medications will be allowed to continue on therapy. Grandfathering will not be provided for any other excluded drugs. Therapeutic Category Excluded Medications Preferred Alternatives GASTROINTESTINAL Opioid-Induced Constipation Amitiza, Movantik, Relistor Symproic (OIC) Apriso, balsalazide, Inflammatory Bow el Disease Dipentum mesalamine Gavilyte-C, Gavilyte-H, PEG Golytely packets 3350 Laxatives Clenpiq, Plenvu, Prepopik, Moviprep Suprep Pancreatic Enzymes Pancreaze, Pertzye, Viokace Creon, Zenpep esomeprazole magnesium delayed release, lansoprazole, omeprazole, Proton pump inhibitors omeppi, omeprazole w ith sodium bicarbonate pantoprazole (cap, pow der pak) HEMATOLOGICAL Erythropoiesis-Stimulating Epogen, Procrit Aranesp, Retacrit Agents Immune globulin, 1 Panzyga Gammagard intravenous (IVIG) Long-Acting Granulocyte- Colony Stimulating Factor Fulphila Neulasta, Udenyca (G-CSFs) Short-Acting Granulocyte- Colony Stimulating Factor Granix, Neupogen Nivestym, Zarxio (G-CSFs ) IM M UNOM ODULATORS Interleukin-17 (IL-17) 1 Cosentyx Taltz* Inhibitor JAK Inhibitor Olumiant1 Xeljanz, Xeljanz XR TNF inhibitor Remicade Inflectra, Renflexis OPHTHALM IC latanoprost ophthalmic Vyzulta, Zioptan solution, Lumigan, Travatan Z Antiglaucoma Drugs Timoptic Ocudose timolol ophthalmic solution azelastine ophth sol, Mast cell stabilizers Pazeo olopatadine ophth sol Non-steroidal Anti- Bromsite, Ilevro, Nevanac Prolensa Inflammatory Agents OT HER Alkylating Agents Belrapzo, Bendamustine Bendeka, Treanda Antigout Agents Colchicine capsule/tablet, Mitigare Colcrys Clarinex Syrup desloratadine Antihistamines and combinations desloratadine w ith Clarinex-D pseudoephedrine (M) Co-branded product * Tier 3 pref erred 1 Existing utilizers of these medications will be allowed to continue on therapy. Grandfathering will not be provided for any other excluded drugs. Therapeutic Category Excluded Medications Preferred Alternatives OT HER Carnitine Deficiency Carnitor injection levocarnitine mometasone furoate, Corticosteroid nasal sprays Xhance Beconase AQ junel FE, larin FE, microgestin Oral Contraceptives Lo Loestrin FE, tarina FE Gel-One, Genvisc, Hyalgan, Hymovis, Monovisc, Osteoarthritis/Hyaluronic Orthovisc, Supartz FX, Synvisc, Synvisc-One, Durolane, Euflexxa, Gelsyn-3 acid injections Trivisc, Visco-3 Thyroid Agents Tirosint caps, solution levothyroxine RESPIRAT ORY Seebri, Tudorza Incruse Ellipta, Spiriva COPD: Inhaled Anticholinergics Yupelri Lonhala Magnair COPD: Long-Acting Beta Agonist/Long-Acting Bevespi, Utibron Anoro Ellipta, Stiolto Respimat Muscarinic Agonist Combination inhalers Cystic Fibrosis (inhaled Kitabis Pak, TOBI Podhaler,
Recommended publications
  • Native State Stabilization by Nsaids Inhibits Transthyretin Amyloidogenesis from the Most Common Familial Disease Variants
    Laboratory Investigation (2004) 84, 545–552 & 2004 USCAP, Inc All rights reserved 0023-6837/04 $25.00 www.laboratoryinvestigation.org Native state stabilization by NSAIDs inhibits transthyretin amyloidogenesis from the most common familial disease variants Sean R Miller, Yoshiki Sekijima and Jeffery W Kelly Department of Chemistry and The Skaggs Institute of Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA Transthyretin (TTR) tetramer dissociation and misfolding affords a monomeric amyloidogenic intermediate that misassembles into aggregates including amyloid fibrils. Amyloidogenesis of wild-type (WT) TTR causes senile systemic amyloidosis (SSA), whereas fibril formation from one of the more than 80 TTR variants leads to familial amyloidosis, typically with earlier onset than SSA. Several nonsteroidal anti-inflammatory drugs (NSAIDs) stabilize the native tetramer, strongly inhibiting TTR amyloid fibril formation in vitro. Structure-based designed NSAID analogs are even more potent amyloid inhibitors. The effectiveness of several NSAIDs, including diclofenac, diflunisal, and flufenamic acid, as well as the diclofenac analog, 2–[(3,5-dichlorophenyl) amino] benzoic acid (inhibitor 1), has been demonstrated against WT TTR amyloidogenesis. Herein, the efficacy of these compounds at preventing acid-induced fibril formation and urea-induced tetramer dissociation of the most common disease-associated TTR variants (V30M, V122I, T60A, L58H, and I84S) was evaluated. Homotetramers of these variants were employed for the studies within, realizing that the tetramers in compound heterozygote patients are normally composed of a mixture of WT and variant subunits. The most common familial TTR variants were stabilized substantially by flufenamic acid and inhibitor 1, and to a lesser extent by diflunisal, against acid-mediated fibril formation and chaotrope denaturation, suggesting that this chemotherapeutic option is viable for patients with familial transthyretin amyloidosis.
    [Show full text]
  • Acute Renal Failure Associated with Diflunisal J. G. WHARTON D. 0
    Postgrad Med J: first published as 10.1136/pgmj.58.676.104 on 1 February 1982. Downloaded from Postgraduate Medical Journal (February 1982) 58, 104-105 Acute renal failure associated with diflunisal J. G. WHARTON D. 0. OLIVER B.Sc., M.R.C.P. F.R.C.P., F.R.A.C.P. M. S. DUNNILL F.R.C.P., F.R.C.Path. Renal Unit, Churchill Hospital, and Department of Pathology, John Radcliffe Hospital, Oxford Summary eosinophils 224 x 106/1; ESR 30 mm/hr; urea 305 The case of a 44-year-old man with acute oliguric mmol/l; creatinine 1651 ,Lmol/l; potassium 6-43 renal failure due to tubulo-interstitial nephritis after mmol/l; serum amylase 88 Somogyi units; urine 3 months' diflunisal is reported. The possible mecha- contained no casts; no red cells but 10 neutrophils, nisms are discussed. no eosinophils and no growth. Antistreptolysin 0 titre 50 i.u./ml; IgG 16-5 g/l; IgA 3-8 g/l; IgM 1.1 g/l antinuclear factor negative; C3 122 mg/dl, C4 54Protected by copyright. Introduction mg/dl; hepatitis B surface antigen negative; chest Diflunisal has been reported as causing acute radiograph, cardiomegaly plus congestion; intra- allergic interstitial nephritis (Chan et al., 1980) venous urogram with tomograms, no obstruction, resulting in acute oliguric renal failure. A case of poor nephrogram. A renal biopsy showed tubulo- acute renal failure due to tubulo-interstitial nephritis interstitial nephritis with no eosinophil infiltrate. after 3 months of diflunisal is reported here. Recently, Diflunisal had been stopped 2 days before admission phenylakalonic acids with analgesic and anti- to this renal unit.
    [Show full text]
  • Salicylate, Diflunisal and Their Metabolites Inhibit CBP/P300 and Exhibit Anticancer Activity
    RESEARCH ARTICLE Salicylate, diflunisal and their metabolites inhibit CBP/p300 and exhibit anticancer activity Kotaro Shirakawa1,2,3,4, Lan Wang5,6, Na Man5,6, Jasna Maksimoska7,8, Alexander W Sorum9, Hyung W Lim1,2, Intelly S Lee1,2, Tadahiro Shimazu1,2, John C Newman1,2, Sebastian Schro¨ der1,2, Melanie Ott1,2, Ronen Marmorstein7,8, Jordan Meier9, Stephen Nimer5,6, Eric Verdin1,2* 1Gladstone Institutes, University of California, San Francisco, United States; 2Department of Medicine, University of California, San Francisco, United States; 3Department of Hematology and Oncology, Kyoto University, Kyoto, Japan; 4Graduate School of Medicine, Kyoto University, Kyoto, Japan; 5University of Miami, Gables, United States; 6Sylvester Comprehensive Cancer Center, Miami, United States; 7Perelman School of Medicine, University of Pennsylvania, Philadelphia, United States; 8Department of Biochemistry and Biophysics, Abramson Family Cancer Research Institute, Philadelphia, United States; 9Chemical Biology Laboratory, National Cancer Institute, Frederick, United States Abstract Salicylate and acetylsalicylic acid are potent and widely used anti-inflammatory drugs. They are thought to exert their therapeutic effects through multiple mechanisms, including the inhibition of cyclo-oxygenases, modulation of NF-kB activity, and direct activation of AMPK. However, the full spectrum of their activities is incompletely understood. Here we show that salicylate specifically inhibits CBP and p300 lysine acetyltransferase activity in vitro by direct *For correspondence: everdin@ competition with acetyl-Coenzyme A at the catalytic site. We used a chemical structure-similarity gladstone.ucsf.edu search to identify another anti-inflammatory drug, diflunisal, that inhibits p300 more potently than salicylate. At concentrations attainable in human plasma after oral administration, both salicylate Competing interests: The and diflunisal blocked the acetylation of lysine residues on histone and non-histone proteins in cells.
    [Show full text]
  • (Ketorolac Tromethamine Tablets) Rx Only WARNING TORADOL
    TORADOL ORAL (ketorolac tromethamine tablets) Rx only WARNING TORADOLORAL (ketorolac tromethamine), a nonsteroidal anti-inflammatory drug (NSAID), is indicated for the short-term (up to 5 days in adults), management of moderately severe acute pain that requires analgesia at the opioid level and only as continuation treatment following IV or IM dosing of ketorolac tromethamine, if necessary. The total combined duration of use of TORADOLORAL and ketorolac tromethamine should not exceed 5 days. TORADOLORAL is not indicated for use in pediatric patients and it is NOT indicated for minor or chronic painful conditions. Increasing the dose of TORADOLORAL beyond a daily maximum of 40 mg in adults will not provide better efficacy but will increase the risk of developing serious adverse events. GASTROINTESTINAL RISK Ketorolac tromethamine, including TORADOL can cause peptic ulcers, gastrointestinal bleeding and/or perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Therefore, TORADOL is CONTRAINDICATED in patients with active peptic ulcer disease, in patients with recent gastrointestinal bleeding or perforation, and in patients with a history of peptic ulcer disease or gastrointestinal bleeding. Elderly patients are at greater risk for serious gastrointestinal events (see WARNINGS). CARDIOVASCULAR RISK NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk (see WARNINGS and CLINICAL STUDIES). TORADOL is CONTRAINDICATED for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (see WARNINGS).
    [Show full text]
  • Arthritis Treatment Comparison Arthritis Treatment Comparison
    ARTHRITIS TREATMENT COMPARISON ARTHRITIS TREATMENT COMPARISON GENERIC OA of (BRAND) HOW SUPPLIED AS GA JIA JRA OA Knee PsA RA CHELATING AGENTS Penicillamine Cap: 250mg ✓ (Cuprimine) Penicillamine Tab: 250mg ✓ (Depen) CYCLIC POLYPEPTIDE IMMUNOSUPPRESSANTS Cyclosporine Cap: 25mg, 100mg; ✓ (Gengraf, Neoral) Sol: 100mg/mL CYCLOOXYGENASE-2 INHIBITORS Celecoxib Cap: 50mg, 100mg, ✓ ✓ ✓ ✓ (Celebrex) 200mg, 400mg DIHYDROFOLIC ACID REDUCTASE INHIBITORS Methotrexate Inj: 25mg/mL; ✓ ✓ Tab: 2.5mg Methotrexate Tab: 5mg, 7.5mg, ✓ ✓ (Trexall) 10mg, 15mg INTERLEUKIN RECEPTOR ANTAGONISTS Anakinra Inj: 100mg/0.67mL ✓ (Kineret) Tocilizumab Inj: 20mg/mL, ✓ ✓ (Actemra) 162mg/0.9mL GOLD COMPOUNDS Auranofin Cap: 3mg ✓ (Ridaura) Gold sodium thiomalate Inj: 50mg/mL ✓ ✓ (Myochrysine) HYALURONAN AND DERIVATIVES Hyaluronan Inj: 30mg/2mL ✓ (Orthovisc) Sodium hyaluronate Inj: 1% ✓ (Euflexxa) Sodium hyaluronate Inj: 10mg/mL ✓ (Hyalgan) Sodium hyaluronate Inj: 2.5mL ✓ (Supartz) HYLAN POLYMERS Hylan G-F 20 Inj: 8mg/mL ✓ (Synvisc, Synvisc One) KINASE INHIBITORS Tofacitinib Tab: 5mg ✓ (Xeljanz) MONOCLONAL ANTIBODIES Ustekinumab Inj: 45mg/0.5mL, ✓ (Stelara) 90mg/mL MONOCLONAL ANTIBODIES/CD20-BLOCKERS Rituximab Inj: 100mg/10mL, ✓ (Rituxan) 500mg/50mL (Continued) ARTHRITIS TREATMENT COMPARISON GENERIC OA of (BRAND) HOW SUPPLIED AS GA JIA JRA OA Knee PsA RA MONOCLONAL ANTIBODIES/TNF-BLOCKERS Adalimumab Inj: 20mg/0.4mL, ✓ ✓ ✓ ✓ (Humira) 40mg/0.8mL Golimumab Inj: 50mg/0.5mL, ✓ ✓ ✓ (Simponi) 100mg/mL Infliximab Inj: 100mg ✓ ✓ ✓ (Remicade) NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
    [Show full text]
  • Ketorolac Tromethamine Injection
    ! • unusual weight gain Ketorolac Tromethamine Injection, USP Rx only Table 1: Table of Approximate Average Pharmacokinetic Parameters (Mean ± SD) IV-Administration: In normal subjects (n=37), the total clearance of 30 mg IV-administered ketorolac tromethamine was Anaphylactoid Reactions 0.030 (0.017-0.051) L/h/kg. The terminal half-life was 5.6 (4.0-7.9) hours. (See Kinetics in Special Populations for use of • skin rash or blisters with fever FOR IV/IM USE (15 mg/mL and 30 mg/mL) Following Oral, Intramuscular and Intravenous Doses of Ketorolac Tromethamine As with other NSAIDs, anaphylactoid reactions may occur in patients without known prior exposure to ketorolac tromethamine. Oral† Intramuscular* Intravenous Bolus‡ IV dosing of ketorolac tromethamine in pediatric patients.) Ketorolac tromethamine should not be given to patients with the aspirin triad. This symptom complex typically occurs in • swelling of the arms and legs, hands and feet FOR IM USE ONLY (60 mg/2 mL (30 mg/mL) asthmatic patients who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm Pharmacokinetic CLINICAL STUDIES These are not all the side effects with NSAID medicines. Talk to your healthcare provider or Parameters 10 mg 15 mg 30 mg 60 mg 15 mg 30 mg after taking aspirin or other NSAIDs (see CONTRAINDICATIONS and PRECAUTIONS – Pre-existing Asthma). Emergency WARNING (units) Adult Patients help should be sought in cases where an anaphylactoid reaction occurs. pharmacist for more information about NSAID medicines. Bioavailability 100% In a postoperative study, where all patients received morphine by a PCA device, patients treated with ketorolac tromethamine IV Cardiovascular Effects Ketorolac tromethamine, a nonsteroidal anti-inflammatory drug (NSAID), is indicated for the short-term (up to 5 days (extent) in adults) management of moderately severe acute pain that requires analgesia at the opioid level.
    [Show full text]
  • Aspirin and Other Anti-Inflammatory Drugs
    Thorax 2000;55 (Suppl 2):S3–S9 S3 Aspirin and other anti-inflammatory drugs Thorax: first published as 10.1136/thorax.55.suppl_2.S3 on 1 October 2000. Downloaded from Sir John Vane Historical introduction inhibiting COX, thereby reducing prosta- Salicylic acid, the active substance in plants glandin formation, providing a unifying expla- used for thousands of years as medicaments, nation for their therapeutic actions and their was synthesised by Kolbe in Germany in 1874. side eVects. This also firmly established certain MacLagan1 and Stricker2 showed that it was prostaglandins as important mediators of eVective in rheumatic fever. A few years later inflammatory disease (see reviews by Vane and sodium salicylate was also in use as a treatment Botting7 and Vane et al8). COX first cyclises for chronic rheumatoid arthritis and gout as arachidonic acid to form prostaglandin (PG) well as an antiseptic compound. G2 and the peroxidase part of the enzyme then Felix HoVman was a young chemist working reduces PGG2 to PGH2. at Bayer. Legend has it that his father, who was taking salicylic acid to treat his arthritis, Discovery of COX-2 complained to his son about its bitter taste. Over the next 20 years several groups postu- Felix responded by adding an acetyl group to lated the existence of isoforms of COX. Then salicylic acid to make acetylsalicylic acid. Rosen et al,9 studying COX in epithelial cells Heinrich Dreser, the Company’s head of phar- from the trachea, found an increase in activity macology, showed it to be analgesic, anti- of COX during prolonged cell culture.
    [Show full text]
  • Ancient Anti-Inflammatory Drug Salicylic Acid Has Cancer-Fighting Properties 31 May 2016
    Ancient anti-inflammatory drug salicylic acid has cancer-fighting properties 31 May 2016 Scientists from the Gladstone Institutes have "The ability to repurpose drugs that are already identified a new pathway by which salicylic acid—a FDA-approved to be part of novel therapies for key compound in the nonsteroidal anti- cancer patients is incredibly exciting," said Nimer. inflammatory drugs aspirin and diflunisal—stops "We have conducted a clinical trial of salicylic acid inflammation and cancer. in patients with hematologic cancers and found it to be safe. Thus, this collaborative effort to develop In a study published in eLife, the researchers novel epigenetic therapies is an important next step found that both salicylic acid and diflunisal in our journey to find more effective treatment for suppress two key proteins that help control gene leukemia patients." expression throughout the body. These sister proteins, p300 and CREB-binding protein (CBP), The scientists are now pursuing a clinical trial that are epigenetic regulators that control the levels of will test the ability of salicylic acid to treat patients proteins that cause inflammation or are involved in with leukemia as part of novel combination cell growth. By inhibiting p300 and CBP, salicylic therapies. Other possible clinical applications for acid and diflunisal block the activation of these salicylic acid include other forms of cancer, type 2 proteins and prevent cellular damage caused by diabetes, inflammatory diseases, and even inflammation. This study provides the first concrete neurodegenerative disorders, such as Alzheimer's demonstration that both p300 and CBP can be disease. Prior Gladstone research showed that targeted by drugs and may have important clinical another drug containing salicylic acid prevented the implications.
    [Show full text]
  • Dolobid® (Diflunisal)
    9676203 TABLETS DOLOBID® (DIFLUNISAL) Cardiovascular Risk • NSAIDS may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. (See WARNINGS.) • DOLOBID is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (see WARNINGS). Gastrointestinal Risk • NSAIDS cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events. (See WARNINGS.) DESCRIPTION Diflunisal is 2', 4'-difluoro-4-hydroxy-3-biphenylcarboxylic acid. Its empirical formula is C13H8F2O3 and its structural formula is: Diflunisal has a molecular weight of 250.20. It is a stable, white, crystalline compound with a melting point of 211-213°C. It is practically insoluble in water at neutral or acidic pH. Because it is an organic acid, it dissolves readily in dilute alkali to give a moderately stable solution at room temperature. It is soluble in most organic solvents including ethanol, methanol, and acetone. DOLOBID* (Diflunisal) is available in 250 and 500 mg tablets for oral administration. Tablets DOLOBID contain the following inactive ingredients: cellulose, FD&C Yellow 6, hydroxypropyl cellulose, hydroxypropyl methylcellulose, magnesium stearate, starch, talc, and titanium dioxide. CLINICAL PHARMACOLOGY Action DOLOBID is a non-steroidal drug with analgesic, anti-inflammatory and antipyretic properties.
    [Show full text]
  • Ketorolac Tromethamine Injection, USP
    PRODUCT MONOGRAPH Pr Ketorolac Tromethamine Injection, USP 30 mg / mL single-dose vials 30 mg / mL in SimplistTM prefilled single use syringes For Intramuscular Administration Non-Steroidal Anti-Inflammatory Analgesic Agent Fresenius Kabi Canada Ltd. Date of Revision: 165 Galaxy Blvd, Suite 100 July 18, 2019 Toronto, ON M9W 0C8 Submission Control No.: 227928 Table of Contents PART I: HEALTH PROFESSIONAL INFORMATION ..........................................................3 SUMMARY PRODUCT INFORMATION ................................................................................3 INDICATIONS AND CLINICAL USE .....................................................................................3 CONTRAINDICATIONS ...........................................................................................................4 WARNINGS AND PRECAUTIONS .........................................................................................5 ADVERSE REACTIONS .........................................................................................................14 DRUG INTERACTIONS..........................................................................................................16 DOSAGE AND ADMINISTRATION .....................................................................................18 OVERDOSAGE ........................................................................................................................22 ACTION AND CLINICAL PHARMACOLOGY ....................................................................23 STORAGE
    [Show full text]
  • 3Q2021 Precision Formulary Exclusion List
    3Q2021 Precision Formulary Exclusion List Therapeutic Category Excluded Medications Preferred Alternatives ALLERGIC REACTIONS Anaphylaxis Treatment Auvi-Q, Epipen Jr 2-Pak 0.15 mg Epipen, epinephrine ANALGESICS celecoxib, diflunisal, flurbiprofen, Cambia, Zipsor, Zorvolex ibuprofen, indomethacin, ketorolac, meloxicam, piroxicam, sulindac Non-Steroidal Anti-Inflammatory Agents (Oral) Relafen, Relafen DS nabumetone Qmiiz ODT meloxicam Non-Steroidal Anti-Inflammatory Pennsaid, Voltaren gel diclofenac solution, diclofenac gel (Topical) Flector, Licart diclofenac patch Non-Steroidal Anti-Inflammatory Ketorolac Nasal Spray, Sprix Nasal diclofenac, ibuprofen, meloxicam (Other) Spray Skeletal Muscle Relaxant Norgesic Forte, Orphengesic Forte orphenadrine tab, aspirin Combinations Ozobax baclofen Kadian ER, Nucynta ER, Zohydro ER, Arymo ER, Hysingla ER, hydromorphone HCl ER, morphine sulfate Oxycontin, Embeda, Exalgo ER, MS Oral Long-Acting ER, oxymorphone HCl ER, Xtampza ER Contin, oxycodone ER, oxycodone Opioid Analgesics powder Conzip, tramadol ER 100mg, tramadol ER tablets 200mg and 300mg capsules codeine sulfate, hydromorphone hcl, Oral Short-Acting Opioid Analgesics Nucynta, Oxaydo, Qdolo morphine sulfate, oxycodone hcl, oxymorphone hcl, tramadol Abstral, Fentora, Lazanda, Subsys, Transmucosal Fentanyl Analgesics fentanyl citrate lozenge fentanyl citrate buccal tab Apadaz, hydrocodone/acetaminophen, Opioid Combinations benzhydrocodone/acetaminophen oxycodone/acetaminophen ANTICONVULSANTS Oxtellar XR oxcarbazepine IR Seizure Disorders Lamictal
    [Show full text]
  • Salicylate, Diflunisal and Their Metabolites Inhibit CBP/P300 and Exhibit Anticancer Activity
    Shirakawa et al. / 1 1 Salicylate, diflunisal and their metabolites inhibit CBP/p300 and exhibit anticancer activity 2 Kotaro Shirakawa1, 2, 7, Lan Wang3, 4, Na Man3, 4, Jasna Maksimoska5, Alexander W. Sorum6, Hyung W. 3 Lim1, 2, Intelly S. Lee1, 2, Tadahiro Shimazu1, 2, John C. Newman1, 2, Sebastian Schröder1, 2, Melanie Ott1, 2, 4 Ronen Marmorstein5, Jordan Meier6, Stephen Nimer3, 4 and Eric Verdin1, 2 5 From the 1Gladstone Institutes and 2Department of Medicine, University of California, San Francisco, 6 CA 94158, 3University of Miami, Coral Gables, FL 33124, 4Sylvester Comprehensive Cancer Center, 7 Miami, FL 33136, and 5Perelman School of Medicine, University of Pennsylvania, Abramson Family 8 Cancer Research Institute and Department of Biochemistry and Biophysics, Philadelphia, PA 19104, 9 6Chemical Biology Laboratory, National Cancer Institute, Frederick, MD 21702, 7Department of 10 Hematology and Oncology, Graduate School of Medicine, Kyoto University, Kyoto, Japan 11 Address for correspondence 12 Eric Verdin, M.D. 13 Gladstone Institutes/UCSF 14 1650 Owens Street 15 San Francisco, CA 94158 16 Tel: (415) 734-4808 17 Fax: (415) 355-0855 18 E-mail: [email protected] 19 Running title: Salicylate and diflunisal inhibit CBP/p300 acetyltransferases 20 Keywords: salicylate, histone acetyltransferase, acetylation, diflunisal 21 Shirakawa et al. / 2 22 Abstract 23 Salicylate and acetylsalicylic acid are potent and widely used anti-inflammatory drugs. They are thought 24 to exert their therapeutic effects through multiple mechanisms, including the inhibition of cyclo- 25 oxygenases, modulation of NF-κB activity, and direct activation of AMPK. However, the full spectrum of 26 their activities is incompletely understood.
    [Show full text]