DOCSLIB.ORG

Ep 2554184 B1

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Ep 2554184 B1 (19) TZZ __T (11) EP 2 554 184 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 45/00 (2006.01) A61K 45/06 (2006.01) 26.10.2016 Bulletin 2016/43 A61K 31/137 (2006.01) A61K 31/222 (2006.01) A61K 31/4174 (2006.01) A61K 31/4415 (2006.01) (2006.01) (21) Application number: 11765663.7 A61P 17/00 (22) Date of filing: 30.03.2011 (86) International application number: PCT/JP2011/058071 (87) International publication number: WO 2011/125763 (13.10.2011 Gazette 2011/41) (54) PREVENTIVE AND/OR REMEDY FOR HAND AND FOOT SYNDROME MITTEL ZUR VERHINDERUNG UND/ODER HEILUNG DES HAND-FUSS-SYNDROMS AGENT PRÉVENTIF ET/OU REMÈDE POUR LE SYNDROME D’ENFLURE DOULOUREUSE DES MAINS ET DES PIEDS (84) Designated Contracting States: JP-A- 2008 506 674 JP-A- 2009 542 581 AL AT BE BG CH CY CZ DE DK EE ES FI FR GB JP-A- 2010 018 564 GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR • JACOBI U ET AL: "Release of doxorubicin in sweat: first step to induce the palmar-plantar (30) Priority: 31.03.2010 JP 2010082379 erythrodysesthesia syndrome?", ANNALS OF 08.11.2010 JP 2010250168 ONCOLOGY,KLUWER, DORDRECHT, NL, vol. 16, no. 7, 27 April 2005 (2005-04-27) , pages (43) Date of publication of application: 1210-1211, XP009134287, ISSN: 0923-7534, DOI: 06.02.2013 Bulletin 2013/06 10.1093/ANNONC/MDI204 • HEALD, R.C.: "Anticholinergic drugs as (73) Proprietor: ONO Pharmaceutical Co., Ltd. antiperspirants", AMERICAN PERFUMER AND Osaka-shi, Osaka 541-8526 (JP) COSMETICS, vol. 81, no. 10, 1966, pages 95-8, XP8058047, (72) Inventors: • WEBSTER-GANDY ET AL: "Palmar-plantar • ISHIZAKA, Kazuhiro erythrodysesthesia (PPE): A literature review Kanagawa 2138507 (JP) with commentary on experience in a cancer • NOMIZU, Tadashi centre", EUROPEAN JOURNAL OF ONCOLOGY Koriyama-shi NURSING, CHURCHILL LIVINGSTONE, Fukushima 963-8846 (JP) AMSTERDAM, NL, vol. 11, no. 3, 1 July 2007 • KITAO, Aya (2007-07-01), pages238-246, XP022136232, ISSN: Osaka-shi 1462-3889 Osaka 541-8526 (JP) • LOKESH JAIN ET AL: "Lack of Association Between Excretion of Sorafenib in Sweat and (74) Representative: Jones, Nicholas Andrew et al Hand-Foot Skin Reaction", Withers & Rogers LLP PHARMACOTHERAPY, vol. 30, no. 1, January 4 More London Riverside 2010 (2010-01), pages 52-56, XP055070331, ISSN: London, SE1 2AU (GB) 0277-0008, DOI: 10.1592/phco.30.1.52 • HEALD, R.C.: ’Anticholinergic drugs as (56) References cited: antiperspirants’ AMERICAN PERFUMER AND EP-A1- 2 368 549 WO-A2-2007/046102 COSMETICS vol. 81, no. 10, 1966, pages 95 - 98, WO-A2-2007/046102 WO-A2-2009/150408 XP008058047 Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 2 554 184 B1 Printed by Jouve, 75001 PARIS (FR) (Cont. next page) EP 2 554 184 B1 • M. L. HENSLEY ET AL.: ’Sunitinib malate in the • T. AHMAD ET AL.: ’Kinase Inhibition with BAY treatment of recurrent or persistent uterine 43-9006 in Renal Cell Carcinoma’ CLINICAL leiomyosarcoma: A Gynecologic Oncology CANCER RESEARCH vol. 10, 2004, pages 6388S Group phase II study’ GYNECOLOGIC - 6392S, XP002362669 ONCOLOGY vol. 115, 2009, pages 460 - 465, XP026733163 2 EP 2 554 184 B1 Description TECHNICAL FIELD 5 [0001] The present invention relates to an agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity. BACKGROUND ART 10 [0002] Hand-Foot Syndrome is a skin disease developed as a side effect of anti-cancer drug treatment and therefore is an indicator of dose limiting factor of anti-cancer drug. Favorite sites of Hand-Foot Syndrome are distal portions of the extremities, especially, palms, soles, and nails and it often appears at these sites with erythema or pigmentation. Patients with mild symptoms (grade 1 of Hand-Foot Syndrome judging criteria) would not be limited in activities of daily living, however in severe cases, patients would develop swelling or redness with pain (grade 2 of said criteria). In addition, 15 cornification or desquamation of palms and soles would become prominent, and sometimes skin fissure would be developed which is accompanied by hyperesthesia. Patients with such conditions might experience difficulty in holding things or in ambulation because of the pain (grade 3 of said criteria). [0003] Pathogenic mechanism of Hand-Foot Syndrome is currently unexplained. For example, there are some factors such as inhibition of proliferating ability of cutaneous basal cell, leakage of anti-cancer drug from blood vessels e.g( ., 20 see Patent Document 1), or secretion of anti-cancer drug from eccrine gland ( e.g., see Nonpatent Document 1), which are suggested as one of the possible causes of Hand-Foot Syndrome, however, causal connection between pathogenesis of the same and anti-cancer drug is yet unknown. [0004] As mentioned above, pathogenic mechanism of Hand-Foot Syndrome is unknown and therefore no prevention method or treatment method is established. Current treatment method of Hand-Foot Syndrome is mainly symptomatic 25 treatment relying on empirical treatment such as: resting limbs, or in the situation of severe swelling, cooling limbs or elevating limbs; local treatment using external formulation such as urea ointment, heparinoid preparation or vitamin ointments for moisturizing purpose; local treatment using topical steroid with anti-inflammatory effect; systemic treatment using internal remedy such as prednisolone, dexamethasone, or pyridoxine hydrochloride (Vitamin B6) (e.g., see Non- patent Document 2); and for treatments of symptoms on nail, washing, protecting with gauze, taping, onychoplasty, 30 artificial nail, cryosurgery, and so on. [0005] In addition to the above, for example, following treatments are suggested; usage of local DMSO for the treatment of Hand-Foot Syndrome caused by liposomal doxorubicin (e.g., see Patent Document 1), usage of dihydropyrimidine dehydrogenase, thymidine phosphorylase, and/or uridine phosphorylase enzyme inhibitor for the treatment of Hand- Foot Syndrome caused by fluorouracil or its precursor (e.g., see Patent Document 2), and usage of cyclin-dependent 35 kinase II inhibitor for prevention and/or reduction of severity of epithelial cytotoxicity side effects including Hand-Foot Syndrome caused by chemotherapy and/or radiation therapy (e.g., see Patent Document 3). [0006] However, effects of aforementioned treatments are not satisfactory. [0007] In addition, there are cases where administration of responsible agents might have to be interrupted as there is no means to treat such symptoms. Nevertheless, for example, at Phase 2 clinical study of capecitabine in Japan, it 40 is reported that the period for recovery of Hand-Foot Syndrome for patients with the highest Hand-Foot Syndrome judging criteria grade of 3 after interruption is about two to three months in average e.g( ., see Nonpatent Document 3), which shows the fact that it takes a long time for its recovery even with interruption. [0008] Thus more effective drug product with instant results is demanded. [0009] On the other hand, as for Hand-Foot Syndrome, there are some reports indicating the connectivity of its patho- 45 genesis with sweat. For example, Patent Document 4 discloses adhesive skin patch for patients under anti-cancer drug treatment, which contains an adhesive base, and at least one compound selected from the group consisting of oil, polyhydric alcohol, and hydrophilic high-molecular compound. In which, it is described that aforementioned skin adhesive patch is effective against Hand-Foot Syndrome by preventing sweat or sebum which contains such an anti-cancer drug to be stored in skin and by absorbing sweat or sebum which contains such an anti-cancer drug. However, this document 50 focused on the fact that use of certain skin adhesive patches to remove anti-cancer drug contained in sweat or sebum is effective for Hand-Foot Syndrome. Furthermore, in this document, anti-cancer drug that caused the pathogenesis of Hand-Foot Syndrome is not specified and it is not described in this document that which route of blood vessels and eccrine glands is important as a secretion pathway of anti-cancer drug to sweat or sebum. [0010] On the other hand, it is described in Nonpatent Document 1 that anti-cancer drug doxorubicin was detected in 55 the sweat from patients with Hand-Foot Syndrome who were administered with such a drug and that they were associated with hyperhidrosis, which implies the connectivity of Hand-Foot Syndrome with hyperhidrosis. However, it is not validated in this document the connectivity of pathogenesis of Hand-Foot Syndrome with drug substance in sweat. This document suggests usage of antiperspirant such as iontophoresis or aluminum chloride to suppress pathogenesis of Hand-Foot 3 EP 2 554 184 B1 Syndrome as the nature of this document is to associate Hand-Foot Syndrome with sweat. Although it has been five years since this document was published, it shows no successful experience of suppressing pathogenesis of Hand-Foot Syndrome using such antiperspirant. [0011] Currently, causal association between Hand-Foot Syndrome and secretion of drug substance into sweat is 5 being questioned (e.g., see Nonpatent Document 4). It was described in this document that drug substance was not detected in sweat from patients with Hand-Foot Syndrome caused by anti-cancer drug sorafenib administration, and therefore there is no relationship between Hand-Foot Syndrome caused by sorafenib and secretion of drug substance in sweat.
Load more

Recommended publications
  • United States Patent Office
    3,092,548 United States Patent Office Patented June 4, 1963 2 are the various side effects that occur in an appreciable 3,092,548 number of patients, the foremost of which are a blurring METHOD OF TREATING PEPTICULCERS WITH PANTOTHENECACD of vision, drowsiness and a general dry condition mani Albert G. Worton, Columbus, Ohio, assignor to The fested by a retarded salivation, reduction of perspiration Warren-Teed Products Company, Columbus, Ohio, a 5 and diminished urinary output. Other side effects which corporation of Ohio occur in some cases are glaucoma, stimulation of the cen No Drawing. Filed Oct. 27, 1960, Ser. No. 65,256 trol nervous system and in severe cases cardiac and respi 5 Claims. (Ci. 67-55) ratory collapse. These side effects increase to Some de gree with the increase in dosage. Despite the side effects This invention relates to preparation adapted for use O these compounds are fairly selective and highly effective in treating disorders of the gastro-intestinal tract, more in decreasing the volume and acidity of gastric secretion particularly in treating peptic ulcer, both of the duodenal and in reducing gastrointestinal motility. and gastric type, for hyperacidity, hypertropic gastritis, Understandably, the main problem in the past has been splenic flexure syndrome, biliary dyskinesia (postchole to provide a dosage of anticholinergic drug which will cystectomy syndrome) and hiatal hernia or other condi achieve the most beneficial results possible and yet mini tions where anticholinergic effect, either spasmolytic or mize the undesired side effects. One of the objects of antisecretory is indicated or where antiuicerogenic effect this invention is to provide novel compositions containing is indicated.
    [Show full text]
  • Regasta-Tab-Leaflet-Pakistan
    50mg Tablets DESCRIPTION Investigations : Increased AST (SGOT), increased ALT (SGPT), increased γ-GTP, Regasta (Itopride HCl) is a prokinetic benzamide derivative. It inhibits dopamine and increased alkaline phosphatase and increased bilirubin. have a gastrokinetic effect. Chemically, Itopride HCl is N-[4-[2-(Dimethylamino) ethoxy]benzyl]-3,4- CONTRAINDICATIONS dimethoxybenzamide monohydrochloride. Its molecular formula is C20H26N2O4.HCl and Itopride HCl is contraindicated in: the structural formula is: - Patients with known hypersensitivity to itopride HCl or any of the excipient of the product. 0 - Patient s in whom an increase in gastrointestinal motility could be harmful e.g., gastrointestinal hemorrhage, mechanical obstruction or perforation. N CH3 PRECAUTIONS H3C H N HCI - Itopride HCl should be used with caution since it enhances the action of acetylcholine. 0 0 CH3 Also, caution is advised in treatment of patients suffering from Parkinson's disease and conditions involving dopamine regulation issues. 0 - Itopride HCl should not be used aimlessly for a long term when no improvement of H3C Itopride HCl gastrointestinal symptoms is observed. Pregnancy and Nursing Mothers QUALITATIVE & QUANTITATIVE COMPOSITION Itopride HCl should be used in pregnant women or in women who may possibly be Regasta (Itopride HCl) is available for oral administration as: pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment. The safety of itopride HCl in pregnant women has not been established. Regasta Tablets 50mg It is ideal not to use itopride HCl in women during lactation, but if it is necessary, breast Each film-coated tablet contains: feeding should be avoided during the treatment of itopride HCl.
    [Show full text]
  • Isopropamide Iodide
    www.chemicalland21.com ISOPROPAMIDE IODIDE SYNONYMS (3-Carbamoyl-3,3-diphenylpropyl)diisopropylmethylammonium iodide; 2,2-Diphenyl-4- diisopropylaminobutyramide methiodide; 4-(Diisopropylamino)-2,2-diphenylbutyramide methiodide; gamma-(Aminocarbonyl)-N-methyl-N,N-bis(1-methylethyl)-gamma-phenylbenzenepropanaminium iodide; Iodure d'isopropamide; Ioduro de isopropamida; Isopropamide ioduro; Isopropamidi iodidum; Isoproponum iodide; PRODUCT IDENTIFICATION CAS RN 71-81-8 EINECS RN 200-766-8 FORMULA C23H33IN2O MOL WEIGHT 480.43 PHYSICAL AND CHEMICAL PROPERTIES PHYSICAL STATE white to off-white powder MELTING POINT 199 C BOILING POINT DENSITY SOLUBILITY IN WATER pH VAPOR DENSITY REFRACTIVE INDEX FLASH POINT GENERAL DESCRIPTION Isopropamide is a long-acting anticholinergic and antimuscarinic drug of quaternary ammonium structure. It is used in the form of the iodide, (also bromide or chloride) to treat peptic ulcer and to suppress gastric secretion other gastrointestinal disorders. Brands of Isopropamide drugs: Darbid Dipramide Isamide Marygin-M Piaccamide Priamide Priazimide Sanulcin Tyrimide Quaternary ammonium anticholinergics (Synthetic) ATC Code Product CAS RN. A03AB01 Benzilonium bromide 1050-48-2 A03AB02 Glycopyrrolate 596-51-0 A03AB03 Oxyphenonium 14214-84-7 A03AB04 Penthienate 22064-27-3 A03AB05 Propantheline 50-34-0 A03AB06 Otilonium bromide 26095-59-0 A03AB07 Methantheline 5818-17-7 Please mail us if you want to sell your product or need to buy some products) www.chemicalland21.com ISOPROPAMIDE IODIDE A03AB08 Tridihexethyl 60-49-1 A03AB09 Isopropamide 7492-32-2 A03AB10 Hexocyclium 6004-98-4 A03AB11 Poldine 596-50-9 A03AB12 Mepenzolic acid 25990-43-6 A03AB13 Bevonium 33371-53-8 A03AB14 Pipenzolate 13473-38-6 A03AB15 Diphemanil methylsulfate 62-97-5 A03AB16 (2-Benzhydryloxyethyl)diethyl-methylammonium iodide A03AB17 Tiemonium iodide 144-12-7 A03AB18 Prifinium bromide 4630-95-9 A03AB19 Timepidium bromide 35035-05-3 A03AB21 Fenpiverinium bromide 125-60-0 03AB53 Oxyphenonium, combinations STABILITY AND REACTIVITY STABILITY Stable under normal conditions.
    [Show full text]
  • The National Drugs List
    ^ ^ ^ ^ ^[ ^ The National Drugs List Of Syrian Arab Republic Sexth Edition 2006 ! " # "$ % &'() " # * +$, -. / & 0 /+12 3 4" 5 "$ . "$ 67"5,) 0 " /! !2 4? @ % 88 9 3: " # "$ ;+<=2 – G# H H2 I) – 6( – 65 : A B C "5 : , D )* . J!* HK"3 H"$ T ) 4 B K<) +$ LMA N O 3 4P<B &Q / RS ) H< C4VH /430 / 1988 V W* < C A GQ ") 4V / 1000 / C4VH /820 / 2001 V XX K<# C ,V /500 / 1992 V "!X V /946 / 2004 V Z < C V /914 / 2003 V ) < ] +$, [2 / ,) @# @ S%Q2 J"= [ &<\ @ +$ LMA 1 O \ . S X '( ^ & M_ `AB @ &' 3 4" + @ V= 4 )\ " : N " # "$ 6 ) G" 3Q + a C G /<"B d3: C K7 e , fM 4 Q b"$ " < $\ c"7: 5) G . HHH3Q J # Hg ' V"h 6< G* H5 !" # $%" & $' ,* ( )* + 2 ا اوا ادو +% 5 j 2 i1 6 B J' 6<X " 6"[ i2 "$ "< * i3 10 6 i4 11 6! ^ i5 13 6<X "!# * i6 15 7 G!, 6 - k 24"$d dl ?K V *4V h 63[46 ' i8 19 Adl 20 "( 2 i9 20 G Q) 6 i10 20 a 6 m[, 6 i11 21 ?K V $n i12 21 "% * i13 23 b+ 6 i14 23 oe C * i15 24 !, 2 6\ i16 25 C V pq * i17 26 ( S 6) 1, ++ &"r i19 3 +% 27 G 6 ""% i19 28 ^ Ks 2 i20 31 % Ks 2 i21 32 s * i22 35 " " * i23 37 "$ * i24 38 6" i25 39 V t h Gu* v!* 2 i26 39 ( 2 i27 40 B w< Ks 2 i28 40 d C &"r i29 42 "' 6 i30 42 " * i31 42 ":< * i32 5 ./ 0" -33 4 : ANAESTHETICS $ 1 2 -1 :GENERAL ANAESTHETICS AND OXYGEN 4 $1 2 2- ATRACURIUM BESYLATE DROPERIDOL ETHER FENTANYL HALOTHANE ISOFLURANE KETAMINE HCL NITROUS OXIDE OXYGEN PROPOFOL REMIFENTANIL SEVOFLURANE SUFENTANIL THIOPENTAL :LOCAL ANAESTHETICS !67$1 2 -5 AMYLEINE HCL=AMYLOCAINE ARTICAINE BENZOCAINE BUPIVACAINE CINCHOCAINE LIDOCAINE MEPIVACAINE OXETHAZAINE PRAMOXINE PRILOCAINE PREOPERATIVE MEDICATION & SEDATION FOR 9*: ;< " 2 -8 : : SHORT -TERM PROCEDURES ATROPINE DIAZEPAM INJ.
    [Show full text]
  • WITHOUTUS010307409B2 (12 ) United States Patent ( 10 ) Patent No
    WITHOUTUS010307409B2 (12 ) United States Patent ( 10 ) Patent No. : US 10 , 307 ,409 B2 Chase et al. (45 ) Date of Patent: Jun . 4 , 2019 ( 54 ) MUSCARINIC COMBINATIONS AND THEIR (52 ) U . S . CI. USE FOR COMBATING CPC . .. .. A61K 31/ 4439 (2013 . 01 ) ; A61K 9 /0056 HYPOCHOLINERGIC DISORDERS OF THE (2013 . 01 ) ; A61K 9 / 7023 ( 2013 . 01 ) ; A61K CENTRAL NERVOUS SYSTEM 31 / 166 ( 2013 . 01 ) ; A61K 31 / 216 ( 2013 . 01 ) ; A61K 31 /4178 ( 2013 .01 ) ; A61K 31/ 439 (71 ) Applicant: Chase Pharmaceuticals Corporation , ( 2013 .01 ) ; A61K 31 /44 (2013 . 01 ) ; A61K Washington , DC (US ) 31/ 454 (2013 .01 ) ; A61K 31/ 4725 ( 2013 .01 ) ; A61K 31 /517 (2013 .01 ) ; A61K 45 / 06 ( 72 ) Inventors : Thomas N . Chase , Washington , DC (2013 . 01 ) (US ) ; Kathleen E . Clarence -Smith , ( 58 ) Field of Classification Search Washington , DC (US ) CPC .. A61K 31/ 167 ; A61K 31/ 216 ; A61K 31/ 439 ; A61K 31 /454 ; A61K 31 /4439 ; A61K (73 ) Assignee : Chase Pharmaceuticals Corporation , 31 /4175 ; A61K 31 /4725 Washington , DC (US ) See application file for complete search history. ( * ) Notice : Subject to any disclaimer, the term of this (56 ) References Cited patent is extended or adjusted under 35 U . S . C . 154 (b ) by 0 days . U . S . PATENT DOCUMENTS 5 ,534 ,520 A 7 / 1996 Fisher et al. ( 21) Appl . No. : 15 /260 , 996 2008 /0306103 Al 12 /2008 Fisher et al. 2011/ 0021503 A1* 1/ 2011 Chase . .. A61K 31/ 27 ( 22 ) Filed : Sep . 9 , 2016 514 / 215 2011/ 0071135 A1 * 3 / 2011 Chase . .. .. .. A61K 31/ 166 (65 ) Prior Publication Data 514 / 215 2011 /0245294 Al 10 / 2011 Paborji et al.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
    US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig.
    [Show full text]
  • Muscarinic Acetylcholine Receptor
    mAChR Muscarinic acetylcholine receptor mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia. www.MedChemExpress.com 1 mAChR Inhibitors & Modulators (+)-Cevimeline hydrochloride hemihydrate (-)-Cevimeline hydrochloride hemihydrate Cat. No.: HY-76772A Cat. No.: HY-76772B Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the The general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other… gastrointestinal, urinary, and reproductive systems and other… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 1 mg, 5 mg AC260584 Aclidinium Bromide Cat. No.: HY-100336 (LAS 34273; LAS-W 330) Cat.
    [Show full text]
  • Anticholinergic Drugs Improve Symptoms but Increase Dry Mouth in Adults with Overactive Bladder Syndrome
    Source of funding: Evid Based Nurs: first published as 10.1136/ebn.6.2.49 on 1 April 2003. Downloaded from Review: anticholinergic drugs improve symptoms but Health Research Council of Aotearoa increase dry mouth in adults with overactive bladder New Zealand. syndrome For correspondence: Jean Hay-Smith, Hay-Smith J, Herbison P,Ellis G, et al. Anticholinergic drugs versus placebo for overactive bladder syndrome in adults. Dunedin School of Cochrane Database Syst Rev 2002;(3):CD003781 (latest version May 29 2002). Medicine, University of Otago, Dunedin, New QUESTION: What are the effects of anticholinergic drugs in adults with overactive Zealand. jean.hay-smith@ bladder syndrome? otago.ac.nz Data sources Parallel arm studies of anticholinergic drugs v placebo for overactive bladder syndrome in Studies were identified by searching the Cochrane adults at 12 days to 12 weeks* Incontinence Group trials register (to January 2002) Weighted event rates and reference lists of relevant papers. Anticholinergic Study selection Outcomes drugs Placebo RBI (95% CI) NNT (CI) Randomised or quasi-randomised controlled trials in Self reported cure or adults with symptomatic diagnosis of overactive bladder improvement (8 studies) 63% 45% 41% (29 to 54) 6 (5 to 8) syndrome, urodynamic diagnosis of detrusor overactiv- RRI (CI) NNH (CI) ity, or both, that compared an anticholinergic drug Dry mouth (20 studies) 36% 15% 138 (70 to 232) 5 (4 to 7) (given to decrease symptoms of overactive bladder) with Outcomes Weighted mean difference (CI) placebo or no treatment. Studies of darifenacin, emepronium bromide or carrageenate, dicyclomine Number of leakage episodes in 24 hours (9 − chloride, oxybutynin chloride, propiverine, propanthe- studies) 0.56 (–0.73 to –0.39) Number of micturitions in 24 hours (8 studies) −0.59 (–0.83 to –0.36) line bromide, tolterodine, and trospium chloride were Maximum cystometric volume (ml) (12 studies) 54.3 (43.0 to 65.7) included.
    [Show full text]
  • Urinary Antispasmodics TCO 02.2018
    Therapeutic Class Overview Urinary antispasmodics INTRODUCTION • Overactive bladder (OAB) is defined as urinary urgency, with or without urge incontinence, usually with frequency and nocturia, in the absence of a causative infection or pathological conditions. Urinary incontinence has been shown to greatly reduce quality of life in areas such as mental and general health in addition to physical and social functioning (American Urological Association 2019, Coyne et al 2008, Haab 2014, International Continence Society 2015). Children with OAB usually have detrusor overactivity as diagnosed through cystometric evaluation. Neurogenic detrusor overactivity is predominantly caused by a congenital neural tube defect in children (Austin et al 2016, Franco ○ et al 2020). • Behavioral therapies (eg, bladder training, bladder control strategies, pelvic floor muscle training and fluid management) are considered first-line treatment in all patients with OAB (American Urological Association 2019). • Urinary antispasmodics are used as first-line pharmacological therapy in OAB (American College of Obstetricians and Gynecologists 2015, American Urological Association 2019, Blok et al 2020, Burkhard et al 2018). Anticholinergic therapy has been frequently used in patients with neurogenic detrusor overactivity, but there are limited data in this specific population (Haab 2014). • The○ urinary antispasmodics used for the treatment of OAB belong to 2 classes of drugs, which include anticholinergic compounds known as muscarinic receptor antagonists, and the beta-3 adrenergic agonist (AR), mirabegron. The anticholinergic agents act as antagonists of acetylcholine at muscarinic cholinergic receptors, thereby relaxing smooth muscle in the bladder and decreasing bladder contractions. ○ . Oral immediate-release (IR) and extended-release (ER) formulations (LA, XL, and XR) are available for oxybutynin (Ditropan), tolterodine (Detrol), and trospium.
    [Show full text]
  • Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
    Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate.
    [Show full text]
  • Printed Formulary Catalog Basic
    Scripps Health Formulary July 2016 Foreword Pharmacy and Therapeutics Committee. MedImpact approves such multi- This document represents the efforts of the MedImpact Healthcare Systems source drugs for addition to the MAC list based on the following criteria: Pharmacy and Therapeutics (P & T) and Formulary Committees to provide physicians A multi-source drug product manufactured by at least one (1) nationally and pharmacists with a method to evaluate the safety, efficacy and cost-effectiveness marketed company. of commercially available drug products. A structured approach to the drug selection At least one (1) of the generic manufacturer’s products must have an “A” process is essential in ensuring continuing patient access to rational drug therapies. rating or the generic product has been determined to be unassociated with The ultimate goal of the Portfolio Formulary is to provide a process and framework to efficacy, safety or bioequivalency concerns by the MedImpact P & T support the dynamic evolution of this document to guide prescribing decisions that Committee. reflect the most current clinical consensus associated with drug therapy decisions. Drug product will be approved for generic substitution by the MedImpact P & T Committee. This is accomplished through the auspices of the MedImpact P & T and Formulary Committees. These committees meet quarterly and more often as warranted to ensure This list is reviewed and updated periodically based on the clinical literature and clinical relevancy of the Formulary. To accommodate changes to this document, pharmacokinetic characteristics of currently available versions of these drug updates are made accessible as necessary. products. As you use this Formulary, you are encouraged to review the information and provide If a member or physician requests a brand name product in lieu of an approved your input and comments to the MedImpact P & T and Formulary Committees.
    [Show full text]
  • Toviaz) Reference Number: ERX.ST.16 Effective Date: 09.01.17 Last Review Date: 08.17 Line of Business: Commercial [Prescription Drug Plan] Revision Log
    Clinical Policy: Fesoterodine (Toviaz) Reference Number: ERX.ST.16 Effective Date: 09.01.17 Last Review Date: 08.17 Line of Business: Commercial [Prescription Drug Plan] Revision Log See Important Reminder at the end of this policy for important regulatory and legal information. Description Fesoterodine (Toviaz®) is a muscarinic antagonist. FDA approved indication Toviaz is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Policy/Criteria Provider must submit documentation (which may include office chart notes and lab results) supporting that member has met all approval criteria It is the policy of health plans affiliated with Envolve Pharmacy Solutions™ that Toviaz is medically necessary when the following criteria are met: I. Initial Approval Criteria A. Step Therapy for Toviaz (must meet all): 1. Age ≥ 18 years; 2. Previous use of 2 formulary generic overactive bladder agents, each trialed for 30 days, unless all are contraindicated or clinically significant adverse effects are experienced; 3. Previous use of Myrbetriq and Vesicare, each trialed for 30 days, unless both are contraindicated or clinically significant adverse effects are experienced; 4. One of the aforementioned trials occurred within the past 6 months, unless all are contraindicated or clinically significant adverse effects are experienced; 5. Dose does not exceed 8 mg per day (1 tablet per day). Approval duration: 12 months II. Continued Therapy A. Step Therapy for Toviaz (must meet all): 1. Currently receiving medication via a health plan affiliated with Envolve Pharmacy Solutions or member has previously met initial approval criteria; 2. If request is for a dose increase, new dose does not exceed 8 mg per day (1 tablet per day).
    [Show full text]