Anti-Inflammatory/Analgesic Combination of Alpha
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United States Patent (19) 11 Patent Number: 5,955,504 Wechter Et Al
USOO5955504A United States Patent (19) 11 Patent Number: 5,955,504 Wechter et al. (45) Date of Patent: Sep. 21, 1999 54 COLORECTAL CHEMOPROTECTIVE Marnett, “Aspirin and the Potential Role of Prostaglandins COMPOSITION AND METHOD OF in Colon Cancer, Cancer Research, 1992; 52:5575–89. PREVENTING COLORECTAL CANCER Welberg et al., “Proliferation Rate of Colonic Mucosa in Normal Subjects and Patients with Colonic Neoplasms: A 75 Inventors: William J. Wechter; John D. Refined Immunohistochemical Method.” J. Clin Pathol, McCracken, both of Redlands, Calif. 1990; 43:453-456. Thun et al., “Aspirin Use and Reduced Risk of Fatal Colon 73 Assignee: Loma Linda University Medical Cancer." N Engl J Med 1991; 325:1593-6. Center, Loma Linda, Calif. Peleg, et al., “Aspirin and Nonsteroidal Anti-inflammatory Drug Use and the Risk of Subsequent Colorectal Cancer.” 21 Appl. No.: 08/402,797 Arch Intern Med. 1994, 154:394–399. 22 Filed: Mar 13, 1995 Gridley, et al., “Incidence of Cancer among Patients With Rheumatoid Arthritis J. Natl Cancer Inst 1993 85:307-311. 51) Int. Cl. .......................... A61K 31/19; A61K 31/40; Labayle, et al., “Sulindac Causes Regression Of Rectal A61K 31/42 Polyps. In Familial Adenomatous Polyposis” Gastroenterol 52 U.S. Cl. .......................... 514/568; 514/569; 514/428; ogy 1991 101:635-639. 514/416; 514/375 Rigau, et al., “Effects Of Long-Term Sulindac Therapy On 58 Field of Search ..................................... 514/568, 570, Colonic Polyposis” Annals of Internal Medicine 1991 514/569, 428, 416, 375 11.5:952-954. Giardiello.et al., “Treatment Of Colonic and Rectal 56) References Cited Adenomas With Sulindac In Familial Adenomatous Poly U.S. -
Comparing the Effects of Salts of Diclofenac and Almioprofen with Aspirin on Serum Electrolytes, Creatinine and Urea Levels in Rabbits
Comparing the effects of salts of diclofenac and almioprofen with aspirin on serum electrolytes, creatinine and urea levels in rabbits Nawazish-i-Husain Syed*, Farnaz Zehra, Amir Ali Rizvi Syed, Sabiha Karim and Farrakh Zia Khan University College of Pharmacy, University of the Punjab, Lahore, Pakistan Abstract: The effects of diclofenac sodium, diclofenac potassium, alminoprofen and aspirin on serum electrolytes (serum Na+ and K+), urea and creatinine were compared in rabbits in acute and chronic phases of treatment. The data suggested that all the four drugs markedly increased the serum electrolytes, urea and creatinine levels in both post- treatment phases. In conclusion, present study does not present any advantage of diclofenac sodium over diclofenac potassium at electrolyte levels on short and long term treatment. Nevertheless, current data support the evidence of renal function impairment by all the four drug therapies used in the present study, which is generally caused by NSAIDS. Keywords: NSAIDs, renal function, serum electrolytes. INTRODUCTION were given fodder twice daily, while water was available ad libitum. Throughout the study, environmental Inflammatory diseases including rheumatoid arthritis and conditions remained constant. Rabbits were divided into osteoarthritis are initially treated with non-steroidal anti- five groups, each of six animals. Same group of animals inflammatory drugs (NSAIDS) (Patrono and Rocca, were used for acute and chronic phases of the study. In 2009). Previously, steroids were prescribed to manage the both studies, rabbits of each group were orally chronic inflammatory diseases, however, due to their administered diclofenac Na+, diclofenac K+, severe adverse effects, NSAIDS has become the first alminoprofen, acetyl salicylic acid in a doses of 2.5mg, choice to treat these diseases. -
Table S1: Sensitivity, Specificity, PPV, NPV, and F1 Score of NLP Vs. ICD for Identification of Symptoms for (A) Biome Developm
Table S1: Sensitivity, specificity, PPV, NPV, and F1 score of NLP vs. ICD for identification of symptoms for (A) BioMe development cohort; (B) BioMe validation cohort; (C) MIMIC-III; (D) 1 year of notes from patients in BioMe calculated using manual chart review. A) Fatigue Nausea and/or vomiting Anxiety Depression NLP (95% ICD (95% CI) P NLP (95% CI) ICD (95% CI) P NLP (95% CI) ICD (95% CI) P NLP (95% CI) ICD (95% CI) P CI) 0.99 (0.93- 0.59 (0.43- <0.00 0.25 (0.12- <0.00 <0.00 0.54 (0.33- Sensitivity 0.99 (0.9 – 1) 0.98 (0.88 -1) 0.3 (0.15-0.5) 0.85 (0.65-96) 0.02 1) 0.73) 1 0.42) 1 1 0.73) 0.57 (0.29- 0.9 (0.68- Specificity 0.89 (0.4-1) 0.75 (0.19-1) 0.68 0.97 (0.77-1) 0.03 0.98 (0.83-1) 0.22 0.81 (0.53-0.9) 0.96 (0.79-1) 0.06 0.82) 0.99) 0.99 (0.92- 0.86 (0.71- 0.94 (0.79- 0.79 (0.59- PPV 0.96 (0.82-1) 0.3 0.95 (0.66-1) 0.02 0.95 (0.66-1) 0.16 0.93 (0.68-1) 0.12 1) 0.95) 0.99) 0.92) 0.13 (0.03- <0.00 0.49 (0.33- <0.00 0.66 (0.48- NPV 0.89 (0.4-1) 0.007 0.94 (0.63-1) 0.34 (0.2-0.51) 0.97 (0.81-1) 0.86 (0.6-0.95) 0.04 0.35) 1 0.65) 1 0.81) <0.00 <0.00 <0.00 F1 Score 0.99 0.83 0.88 0.57 0.95 0.63 0.82 0.79 0.002 1 1 1 Itching Cramp Pain NLP (95% ICD (95% CI) P NLP (95% CI) ICD (95% CI) P NLP (95% CI) ICD (95% CI) P CI) 0.98 (0.86- 0.24 (0.09- <0.00 0.09 (0.01- <0.00 0.52 (0.37- <0.00 Sensitivity 0.98 (0.85-1) 0.99 (0.93-1) 1) 0.45) 1 0.29) 1 0.66) 1 0.89 (0.72- 0.5 (0.37- Specificity 0.96 (0.8-1) 0.98 (0.86-1) 0.68 0.98 (0.88-1) 0.18 0.5 (0-1) 1 0.98) 0.66) 0.88 (0.69- PPV 0.96 (0.8-1) 0.8 (0.54-1) 0.32 0.8 (0.16-1) 0.22 0.99 (0.93-1) 0.98 (0.87-1) NA* 0.97) 0.98 (0.85- 0.57 (0.41- <0.00 0.58 (0.43- <0.00 NPV 0.98 (0.86-1) 0.5 (0-1) 0.02 (0-0.08) NA* 1) 0.72) 1 0.72) 1 <0.00 <0.00 <0.00 F1 Score 0.97 0.56 0.91 0.28 0.99 0.68 1 1 1 *Denotes 95% confidence intervals and P values that could not be calculated due to insufficient cells in 2x2 tables. -
What Are the Acute Treatments for Migraine and How Are They Used?
2. Acute Treatment CQ II-2-1 What are the acute treatments for migraine and how are they used? Recommendation The mainstay of acute treatment for migraine is pharmacotherapy. The drugs used include (1) acetaminophen, (2) non-steroidal anti-inflammatory drugs (NSAIDs), (3) ergotamines, (4) triptans and (5) antiemetics. Stratified treatment according to the severity of migraine is recommended: use NSAIDs such as aspirin and naproxen for mild to moderate headache, and use triptans for moderate to severe headache, or even mild to moderate headache when NSAIDs were ineffective in the past. It is necessary to give guidance and cautions to patients having acute attacks, and explain the methods of using medications (timing, dose, frequency of use) and medication use during pregnancy and breast-feeding. Grade A Background and Objective The objective of acute treatment is to resolve the migraine attack completely and rapidly and restore the patient’s normal functions. An ideal treatment should have the following characteristics: (1) resolves pain and associated symptoms rapidly; (2) is consistently effective; (3) no recurrence; (4) no need for additional use of medication; (5) no adverse effects; (6) can be administered by the patients themselves; and (7) low cost. Literature was searched to identify acute treatments that satisfy the above conditions. Comments and Evidence The acute treatment drugs for migraine generally include (1) acetaminophens, (2) non-steroidal anti-inflammatory drugs (NSAIDs), (3) ergotamines, (4) triptans, and (5) antiemetics. For severe migraines including status migrainosus and migraine attacks refractory to treatment, (6) anesthetics, and (7) corticosteroids (dexamethasone) are used (Tables 1 and 2).1)-9) There are two approaches to the selection and sequencing of these medications: “step care” and “stratified care”. -
Horsemen's Information 2016和文TGP 1 薬物修正後 E
[Conditions] 1 Date December 29 (Tue), 2020 2020 Oi Racetrack, Race 10 2 Location TCK, Oi Racetrack 3 Race The 66th Running of Tokyo Daishoten (GI) 4 Eligibility Thoroughbreds, 3 years old & up 5 Full Gate 16 horses 6 Foreign Runners Selected by the selection committee from among the pre-entered horses. 7 Distance 2,000m, 1 1/4 mile (Right-handed, dirt course) 8 Weight 3 years old: 121.5 lbs,4 years old & up: 125.5 lbs, Female: 4.4 lbs less For 3 year-old-horses from the southern hemisphere, reduce 4.4 lbs from the above weight. 9 Purse Unit: 1,000 JPY Prize Purse & Bonus money Running Record 1st place 6th place allowances prize *1 prize *2 1st place 2nd place 3rd place 4th place 5th place or lower Owner 80,000 28,000 16,000 8,000 4,000 300 300 50 1,600 Trainer 880 70 60 50 40 30 30 80 Jockey 120 110 100 80 70 60 30 80 Groom 80 70 60 50 40 30 30 80 Rider 30 30 80 *1 Paid for the runner who broke the previous record and also set the best record during the race. *2 Prize equivalent to the amount listed in the table above is presented. *3 1 USD= 105.88 JPY (As of August,2020) 10 Handling of Late Scratch No allowance is paid in the case of a late scratch (including cancelation of race due to standstill in a starting gate) approved by TCK, Stewards, and Starter. However, if the chairman of the race meeting operation committee deems that the horse is involved in an accident not caused by the horse, the owner is given an running allowance. -
Acemetacin.Pdf
Methods and Findings in Experimental and Clinical Pharmacology 2010, 32(2): ???-??? THOMSON REUTERS Copyright © 2010 Prous Science, S.A.U. or its licensors. All rights reserved. CCC: 0379-0355/2010 DOI: 10.1358/mf.2010.32.2.1423883 ORIGINAL ARTICLE ACEMETACIN ANTINOCICEPTIVE MECHANISM IS NOT RELATED TO NO OR K+ CHANNEL PATHWAYS. M. Gil-Flores1, M.I. Ortiz2, G. Castañeda-Hernández1 and A.E. Chávez-Piña1 1Departamento de Farmacología, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, México, D.F., México. 2Área Académica de Medicina del Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Pachuca, Hidalgo, México SUMMARY Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID) used for the treatment of acute gout and inflammation. However, its use is limited due to side effects. Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical tri- als. The aim of this study was to examine if the systemic administration of acemetacin involved the sequential participation of nitric oxide (NO) or K+ channel pathways to confer its antinociceptive effect, as compared to indomethacin. The antinociceptive effect of both drugs was studied with the formalin test. Equimolar doses of acemetacin or indomethacin were administered orally. The intraplantar administra- tion of either L-NAME, glibenclamide, apamin or charybdotoxin plus indomethacin or acemetacin was studied using the formalin test and the anti-inflammatory and antihyperalgesic effects were measured. The antinociceptive effect of acemetacin or indomethacin was not sig- nificantly different when pretreatment with L-NAME, glibenclamide, apamin or charybdotoxin was done. The antihyperalgesic and anti- inflammatory effects were also similar for both indomethacin and acemetacin. -
Short Reports
Br Med J (Clin Res Ed): first published as 10.1136/bmj.287.6395.798 on 17 September 1983. Downloaded from 798 BRITISH MEDICAL JOURNAL VOLUME 287 17 SEPTEMBER 1983 SHORT REPORTS analgesic properties. The usual daily dosage is 400 mg. The amount Piroxicam poisoning of fentiazac absorbed after gastric lavage would probably be small and of little importance. Piroxicam is a potent non-steroidal anti-inflammatory drug. Ex- The main signs were altered consciousness and muscle twitchings. perience with overdosage is limited. We describe a patient who took The exact causes of these were unknown, but griseofulvin has been a large dose of piroxicam. associated with dizziness, mental confusion, irritability, and impaired coordination.2 Side effects of piroxicam have occasionally included headache and dizziness, although their incidences in double blind Case report comparative studies have been lower than those reported with indomethacin.3 Thus the drowsiness and muscle twitchings could not A 25 year old Chinese man weighing 46 kg was admitted to hospital be definitely attributed to piroxicam. about two hours after ingesting 56 capsules of 10 mg piroxicam, 97 tablets Gastrointestinal bleeding is usually the major side effect of most of 125 mg griseofulvin, and about 10 tablets of 100 mg fentiazac. He had been drugs. Piroxicam seemed to be well suffering from psoriatic arthropathy affecting both knee and ankle joints non-steroidal anti-inflammatory and had been taking piroxicam 30 mg daily for nine months. Other anal- tolerated since the patient did not complain of gastric discomfort or gesics, including aspirin, paracetamol, fentiazac, and indomethacin, had gastrointestinal bleeding despite a history of gastric erosions. -
Binding of Nonsteroidal Anti-Inflammatory Drugs to DPPC: Structure and Thermodynamic Aspects
4132 Langmuir 2008, 24, 4132-4139 Binding of Nonsteroidal Anti-inflammatory Drugs to DPPC: Structure and Thermodynamic Aspects Marlene Lu´cio,*,†,⊥ Frank Bringezu,‡,|,⊥ Salette Reis,† Jose´ L. F. C. Lima,† and Gerald Brezesinski§,⊥ REQUIMTE, Faculdade de Farma´cia, UniVersidade do Porto, Rua Anı´bal Cunha, 4099-030 Porto, Portugal, Institute of Medical Physics and Biophysics, UniVersity of Leipzig, Ha¨rtelstrasse 16, D-04103 Leipzig, Germany, and Max-Planck Institute of Colloids and Interfaces, Research Campus Golm, Am Mu¨hlenberg 1, D-14476 Potsdam, Germany ReceiVed NoVember 16, 2007. In Final Form: January 8, 2008 The effect of nonsteroidal anti-inflammatory drugs (NSAIDs) on the phase transition and phase properties of 1,2-dipalmitoylphosphatidylcholine (DPPC) has been investigated in both 2D (monolayers at the air/water interface) and 3D (multilayers in lipid/water dispersions) model systems. The 2D membrane models have been characterized by means of pressure-area isotherms and grazing incidence X-ray diffraction (GIXD) measurements. Differential scanning calorimetry (DSC) and simultaneous small- and wide-angle X-ray diffraction have been applied to lipid aqueous dispersions. All NSAIDs studied altered the main transition temperature of the gel to liquid-crystalline phase transition, with the arylacetic acid derivatives (acemetacin and indomethacin) showing the largest effects. A comparison of the results reveals distinct structural features of the membrane models after interaction with the NSAID. All drugs induced perturbations in the lipid liquid-crystalline phase, suggesting a major change in the hydration behavior of DPPC. Again, the largest effects on the structural parameters are found for the arylacetic acid derivatives. The results obtained in the different model systems give indications of the role of the membrane/NSAID interactions that might also be important for NSAID gastric injury. -
Download Product Insert (PDF)
PRODUCT INFORMATION Acemetacin Item No. 29615 CAS Registry No.: 53164-05-9 Cl Formal Name: 1-(4-chlorobenzoyl)-5- methoxy-2-methyl-1H- indole-3-acetic acid, O carboxymethyl ester N MF: C21H18ClNO6 FW: 415.8 O OH Purity: ≥98% O Supplied as: A crystalline solid O Storage: -20°C O Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Acemetacin is supplied as a crystalline solid. A stock solution may be made by dissolving the acemetacin in the solvent of choice, which should be purged with an inert gas. Acemetacin is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of acemetacin in ethanol is approximately 3 mg/ml and approximately 25 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of acemetacin can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of acemetacin in PBS, pH 7.2, is approximately 0.5 mg/ml. We do not recommend storing the aqueous solution for more than one day. Description Acemetacin is a non-steroidal anti-inflammatory drug (NSAID) and a prodrug form of indomethacin 1 (Item No. 70270). It reduces zymosan-induced thromboxane B2 (TXB2; Item No. 19030) and prostaglandin E2 (PGE2; Item No. 14010) production in isolated rat whole blood and stomach, respectively, when administered at doses ranging from 2.7 to 83.8 µmol/kg. -
Suprofen | Medchemexpress
Inhibitors Product Data Sheet Suprofen • Agonists Cat. No.: HY-B0270 CAS No.: 40828-46-4 Molecular Formula: C₁₄H₁₂O₃S • Molecular Weight: 260.31 Screening Libraries Target: PGE synthase Pathway: Immunology/Inflammation Storage: Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month SOLVENT & SOLUBILITY In Vitro DMSO : ≥ 100 mg/mL (384.16 mM) * "≥" means soluble, but saturation unknown. Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 3.8416 mL 19.2079 mL 38.4157 mL Stock Solutions 5 mM 0.7683 mL 3.8416 mL 7.6831 mL 10 mM 0.3842 mL 1.9208 mL 3.8416 mL Please refer to the solubility information to select the appropriate solvent. In Vivo 1. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.5 mg/mL (9.60 mM); Clear solution 2. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (9.60 mM); Clear solution 3. Add each solvent one by one: 10% DMSO >> 90% corn oil Solubility: ≥ 2.5 mg/mL (9.60 mM); Clear solution BIOLOGICAL ACTIVITY Description Suprofen (TN-762) is a non-steroidal anti-inflammatory drug (NSAID). IC₅₀ & Target PGE synthase[1]. In Vitro Suprofen (TN-762) is an NSAID. Suprofen (TN-762) is an ibuprofen-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic. suprofen was clinically effective but the Page 1 of 2 www.MedChemExpress.com differential suppression of prostanoids favors 200mg which spares 6-keto PGF1a[1]. -
Contrasting Effects of Diclofenac and Ibuprofen on Active Imatinib Uptake Into Leukaemic Cells British Journal of Cancer, 2012; 106(11):1772-1778
PUBLISHED VERSION Wang, Jueqiong; Hughes, Timothy Peter; Kok, Chung Hoow; Saunders, Verity Ann; Frede, Amity; Groot- Obbink, Kelvin Stuart; Osborn, M.; Somogyi, Andrew Alexander; D'Andrea, Richard James; White, Deborah Lee Contrasting effects of diclofenac and ibuprofen on active imatinib uptake into leukaemic cells British Journal of Cancer, 2012; 106(11):1772-1778 © 2012 Cancer Research UK From twelve months after its original publication, this work is licensed under the Creative Commons Attribution-NonCommercial-Share Alike 3.0 Unported License. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-sa/3.0/ The electronic version of this article is the complete one and can be found online at: http://www.nature.com/bjc/journal/v106/n11/full/bjc2012173a.html PERMISSIONS http://www.nature.com/bjc/authors/submit.html#open BJC publishes BJC OPEN articles under a Creative Commons Attribution-Non commercial-Share Alike 3.0 Unported licence. This licence allows users to: share - to copy, distribute and transmit the work remix - to adapt the work Under the following conditions: attribution - users must attribute the work in the manner specified by the author or licensor (but not in any way that suggests an endorsement ) non commercial - users may not use this work for commercial purposes share alike - If users alter, transform, or build upon this work, they may distribute the resulting work only under the same or similar license to this one 20th May 2013 http://hdl.handle.net/2440/72375 British Journal of Cancer -
Fenbufen | Medchemexpress
Inhibitors Product Data Sheet Fenbufen • Agonists Cat. No.: HY-B1138 CAS No.: 36330-85-5 Molecular Formula: C₁₆H₁₄O₃ • Molecular Weight: 254.28 Screening Libraries Target: COX; Caspase Pathway: Immunology/Inflammation; Apoptosis Storage: Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month SOLVENT & SOLUBILITY In Vitro DMSO : 50 mg/mL (196.63 mM; Need ultrasonic) H2O : 0.67 mg/mL (2.63 mM; Need ultrasonic) Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 3.9327 mL 19.6634 mL 39.3267 mL Stock Solutions 5 mM 0.7865 mL 3.9327 mL 7.8653 mL 10 mM 0.3933 mL 1.9663 mL 3.9327 mL Please refer to the solubility information to select the appropriate solvent. In Vivo 1. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: 2.5 mg/mL (9.83 mM); Suspended solution; Need ultrasonic 2. Add each solvent one by one: 10% DMSO >> 90% corn oil Solubility: ≥ 2.5 mg/mL (9.83 mM); Clear solution BIOLOGICAL ACTIVITY Description Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].