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Fluocinonide/Fluticasone 1533 Fluorometholone Acetate (BANM, USAN, rINNM) ⊗ Preparations the hypothalamic-pituitary-adrenal axis to some degree. Others Acetato de fluorometolona; Fluorométholone, Acétate de; Proprietary Preparations (details are given in Part 3) have also found evidence of adrenal suppression with flutica- sone,2-5 particularly at high doses and in children,6 and the effect Fluorometholoni Acetas; Fluorometolon Asetat; U-17323. Fluor- Austria: Decoderm; Belg.: Decoderm; Ger.: Decoderm; Indon.: Deco- derm; Port.: Crinohermal; Swed.: Corticoderm†; Switz.: Decoderm. may be more marked with repeated than with single doses.4,6-8 A ometholone 17-acetate. Multi-ingredient: Arg.: Tri-Emcortina†; Austria: Decoderm Composi- number of cases of adrenal crisis have been associated with high- Флуорометолона Ацетат tum; Decoderm trivalent; Belg.: Decoderm Compositum; Braz.: dose inhaled fluticasone,9,10 including at least one fatality.6 It has C H FO = 418.5. Emecort†; Pan-Emecort†; Ger.: Candio-Hermal Plus; Crinohermal fem; been recommended that children using inhaled fluticasone at 24 31 5 Decoderm Comp; Decoderm tri; Sali-Decoderm; Vobaderm; Gr.: Antimy- CAS — 3801-06-7. cotic; Catrigel; Combi; Conazol; Domycotin; Edmudo; Expectein; Feminella; doses above 400 micrograms daily should have adrenal function ATC — C05AA06; D07AB06; S01BA07. Finicort; Flenazole; Fluniprol; Flunovon; Fosemyk; Fumicon; Micoflup; Mico- monitoring and a written plan for emergency corticosteroid re- ATC Vet — QC05AA06; QD07AB06; QS01BA07. gen; Mifler; Oxigon; Panderm; Panmyk; Sarmel; Verdal; Indon.: Decoderm placement therapy.6 Pharmacopoeias. In US. 3; Gentacortin; Switz.: Decoderm bivalent; Thai.: Supracortin 3†; UK: 1. Grahnén A, et al. An assessment of the systemic activity of sin- Acorvio Plus. USP 31 (Fluorometholone Acetate). gle doses of inhaled fluticasone propionate in healthy volun- teers. Br J Clin Pharmacol 1994; 38: 521–5. Profile 2. Clark DJ, et al. Comparative systemic bioactivity of inhaled Fluorometholone is a corticosteroid used for its glucocorticoid budesonide and fluticasone propionate in asthmatic children. Br activity (p.1490), usually as eye drops containing 0.1%, in the Fluticasone (BAN, rINN) ⊗ J Clin Pharmacol 1996; 42: 264P. treatment of allergic and inflammatory conditions of the eye. 3. Rohatagi S, et al. Dynamic modeling of cortisol reduction after Fluticasona; Fluticasonum. S-(Fluoromethyl) 6α,9-difluoro- inhaled administration of fluticasone propionate. J Clin Phar- Fluorometholone acetate is used similarly. macol 1996; 36: 938–41. 11β,17-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β- Fluorometholone is also used topically in the treatment of vari- 4. Clark DJ, Lipworth BJ. Adrenal suppression with chronic dos- ous skin disorders. carbothioate. ing of fluticasone propionate compared with budesonide in Флутиказон adult asthmatic patients. Thorax 1997; 52: 55–8. Prolonged use of ophthalmic preparations containing corticoster- 5. Eid N, et al. Decreased morning serum cortisol levels in chil- oids has caused raised intra-ocular pressure and reduced visual C22H27F3O4S = 444.5. dren with asthma treated with inhaled fluticasone propionate. function. When applied topically, particularly to large areas, CAS — 90566-53-3. Pediatrics 2002; 109: 217–21. when the skin is broken, or under occlusive dressings, corticos- ATC — D07AC17; R01AD08; R03BA05. 6. Paton J, et al. Adrenal responses to low dose synthetic ACTH (Synacthen) in children receiving high dose inhaled fluticasone. teroids may be absorbed in sufficient amounts to cause systemic ATC Vet — QD07AC17; QR01AD08; QR03BA05. Arch Dis Child 2006; 91: 808–13. effects (p.1490). The effects of topical corticosteroids on the skin 7. Lönnebo A, et al. An assessment of the systemic effects of sin- are described on p.1492. For recommendations concerning the gle and repeated doses of inhaled fluticasone propionate and in- correct use of corticosteroids on the skin, see p.1497. haled budesonide in healthy volunteers. Eur J Clin Pharmacol F S O 1996; 49: 459–63. Preparations 8. Wilson AM, et al. Adrenal suppression with high doses of in- H CH3 BP 2008: Fluorometholone Eye Drops; HO haled fluticasone propionate and triamcinolone acetonide in USP 31: Fluorometholone Cream; Fluorometholone Ophthalmic Suspen- OH healthy voluteers. Eur J Clin Pharmacol 1997; 53: 33–7. 9. Todd GRG, et al. Survey of adrenal crisis associated with in- sion; Neomycin Sulfate and Fluorometholone Ointment; Tobramycin and CH H H CH Fluorometholone Acetate Ophthalmic Suspension. 3 3 haled corticosteroids in the United Kingdom. Arch Dis Child 2002; 87: 457–61. Proprietary Preparations (details are given in Part 3) 10. Adverse Drug Reactions Advisory Committee (ADRAC). Flu- Arg.: Flarex; FML; Austral.: Flarex; Flucon; FML; Austria: Flarex†; Belg.: F H ticasone and adrenal crisis. Aust Adverse Drug React Bull 2003; Fluacort; Flucon; FML; Braz.: Florate; Flumex; Flutinol; Canad.: Flarex; FML; 22: 6. Also available at: http://www.tga.health.gov.au/adr/ Chile: Aflarex; Fluforte; Cz.: Efflumidex; Flarex; Flucon; Flumetol S†; Fluor- O aadrb/aadr0304.htm (accessed 06/05/04) opos; Denm.: Flurolon; Fin.: FML; Fr.: Flucon; Ger.: Efflumidex; Fluoro- Ophtal; Fluoropos; Isopto Flucon†; Gr.: Flucon; Fluxinam; FML; Talirax†; F Aspergillosis. The fungal infection aspergillosis has been re- Hong Kong: Flarex; Flucon; Flumetholon; FML; Hung.: Efflumidex; Flarex; ported in patients receiving inhaled1,2 and intranasal3 fluticasone. Flucon; India: Flomex; Flosef; Indon.: Flumetholon; Irl.: FML; Israel: Flarex; 1. Fairfax AJ, et al. Laryngeal aspergillosis following high dose in- FML; Ital.: Flarex; Fluaton; Flumetol; Flumetol Semplice†; Malaysia: Flarex; haled fluticasone therapy for asthma. Thorax 1999; 54: 860–1. FML†; Mex.: Flarex; Fluforte; Flumetol NF; Neth.: Flarex; FML; NZ: Fluticasone Furoate (BANM, USAN, rINN) ⊗ Flarex†; Flucon; FML; Philipp.: Flarex; Flulon; FML; Pol.: Flarex; Flucon; 2. Leav BA, et al. Invasive pulmonary aspergillosis associated with Port.: Flurop; FML; Rus.: Flarex (Фларекс); S.Afr.: Flucon; FML; Singa- Fluticasonum Furoas; Furoate de Fluticasone; Furoato de Flutica- high-dose inhaled fluticasone. N Engl J Med 2000; 343: 586. 3. Bratton RL, et al. Aspergillosis related to long-term nasal corti- pore: FML; Spain: FML; Isopto Flucon; Switz.: FML; Thai.: Flarex; Flu Oph; sona; GW-685698X. 6α,9-Difluoro-17-{[(fluoromethyl)sulfa- Flucon; FML; Turk.: Flarex; FML; UK: FML; USA: Eflone; Flarex; Fluor-Op†; costeroid use. Mayo Clin Proc 2002; 77: 1353–7. FML; Venez.: Aflarex; Flumetol. nyl]carbonyl}-11β-hydroxy-16α-methyl-3-oxoandrosta-1,4-dien- 17α-yl furan-2-carboxylate. Effects on the bones. For studies of the effects on bone of Multi-ingredient: Arg.: Delisan; Efemolina; FML Neo; Larsimal; Nesbil- inhaled fluticasone, compared with beclometasone, see p.1516. er†; Belg.: Infectoflam; Braz.: Flumex N; Chile: Fluforte N†; Cz.: Infecto- Флутиказон Фуроат flam†; Ger.: Cibaflam; Efemolin; Efflumycin†; Gr.: Efemoline; FML Neo; In- Effects on the muscles. Proximal myopathy has been report- C27H29F3O6S = 538.6. docort†; Luzin; Hong Kong: Efemoline; India: Flomex N; Ital.: Efemoline; ed in children receiving high-dose inhaled fluticasone;1 the pa- Flumeciclina; Flumetol Antibiotico†; Flumezina; Gentacort; Malaysia: CAS — 397864-44-7. Efemoline†; Infectoflam†; Mex.: Fluforte N; Fluorometil; Philipp.: Efemo- ATC — D07AC17; R01AD08; R01AD12; R03BA05. tients recovered after replacement of fluticasone with alternative line; Infectoflam; Port.: FML Neo; Neo-Preocil; S.Afr.: Efemoline; FML ATC Vet — QD07AC17; QR01AD08; QR01AD12; corticosteroid therapy. Neo; Singapore: Efemoline; Infectoflam; Spain: Bexicortil; Cortisdin Urea; QR03BA05. 1. De Swert LF, et al. Myopathy in children receiving high-dose Flugen; Fluorvas; Switz.: Efemoline; FML Neo; Infectoflam; Thai.: Efemo- inhaled fluticasone. N Engl J Med 2004; 350: 1157–9. line; FML Neo†; Infectoflam; Turk.: Efemoline; Flumetol; USA: FML-S. Fluticasone Propionate (BANM, USAN, rINNM) ⊗ CCI-18781; Fluticasone, propionate de; Fluticasoni propionas; Interactions Flutikasonipropionaatti; Flutikasonpropionat; Flutikason-propi- The interactions of corticosteroids in general are de- Fluprednidene Acetate (BANM, rINNM) ⊗ onát; Flutikazon Propiyonat; Flutikazono propionatas; Propionato scribed on p.1494. Acetato de fluprednideno; Fluprednidène, Acétate de; Flupred- de fluticasona. S-Fluoromethyl 6α,9α-difluoro-11β,17α-dihy- nideni Acetas; Fluprednylidene 21-Acetate. 9α-Fluoro- droxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carbothioate Pharmacokinetics 11β,17α,21-trihydroxy-16-methylenepregna-1,4-diene-3,20-di- 17-propionate. For a brief outline of the pharmacokinetics of corticos- one 21-acetate. Флутиказона Пропионат teroids, see p.1495. Флупреднидена Ацетат C25H31F3O5S = 500.6. Fluticasone propionate is poorly absorbed from the C24H29FO6 = 432.5. CAS — 80474-14-2. CAS — 2193-87-5 (fluprednidene); 1255-35-2 (flupredni- ATC — D07AC17; R01AD08; R03BA05. gastrointestinal tract and undergoes extensive first- dene acetate). ATC Vet — QD07AC17; QR01AD08; QR03BA05. pass metabolism; oral bioavailability is reported to be ATC — D07AB07. Pharmacopoeias. In Eur. (see p.vii) and US. ATC Vet — QD07AB07. only about 1%. Ph. Eur. 6.2 (Fluticasone Propionate). A white or almost white powder. Practically insoluble in water; slightly soluble in alco- ◊ References. hol; sparingly soluble in dichloromethane. Protect from light. 1. Mackie AE, et al. Pharmacokinetics of intravenous fluticasone OH propionate
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    Patentamt JEuropaischesJ European Patent Office @ Publication number: 0173 478 ^ ^ Office europeen des brevets EUROPEAN PATENT APPLICATION Application number: 85305552.3 © 'nt. CI ": A 61 K 35/78, A 61 K 31 /57 Dateof filing: 05.08.85 (A61K35/78, 31 :57),(A61K31/57, 31 :23, 31 :20) @ Priority: 15.08.84 GB 8420771 @ Applicant: EFAMOL LIMITED, Efamol House Woodbridge Meadows, Guildford Surrey GU1 1BA (GB) @ Date of publication of application: 05.03.86 @ Bulletin 86/10 efamol House woodbridge meadows, Guildford Surrey GU1 1BA (GB) @ Representative : Caro, William Egerton et al, J. MILLER & @ Designated Contracting States: AT BE CH DE FR GB IT CO. Lincoln House 296-302 High Holborn, London LILUNLSE WC1V7JH(GB) @ Treatment of skin disorders. A topical composition for skin treatment contains an anti- inflammatory glucocorticoid in combination with an essential fatty acid (EFA) of the n-6 or n-3 series or equivalent poly- unsaturated fatty acid, as such or in the form of a physio- logically acceptable derivative convertible in the body thereto. FIELD OF INVENTION The invention relates to compositions of y-linolenic acid and related materials with anti-inflammatory glucocorticoids and to the treatment of inflammatory skin disorders with them. BACKGROUND AND EXPLANATION OF INVENTION Much interest has been shown in recent years in essential fatty acid metabolism, especially in its relation to prosta- glandin (PG) metabolism and in particular to the balance of 1-series and 2-series PGs in the body. The main dietary essential fatty acid (EFA) utilised in the fully healthy human body is linoleic acid, but the Δ6- desaturase that converts it to the next acid in the n-6 series, namely y-linoleic acid (GLA) is at a low level of activity in many conditions.
  • Aspects of the Bioavailability of Topical Corticosteroid

    Aspects of the Bioavailability of Topical Corticosteroid

    - - ASPECTS OF THE BIOAVAILABILITY OF TOPICAL CORTICOSTEROID FORMULATIONS. A Thesis Submitted to RHOD ES UNIVERSITY in Partial Fulfilment of the Requirements for the Degree of MASTER OF SCIENCE by ASHLEY DENIS MAGNUS B.Pharm.(Rhodes) School of Pharmaceutical Sciences, Rhodes University, Grahamstown, South Africa. 6140 November 1978. - i - CONTENTS ABSTRACT iii ACKNOWLEDGEMENTS iv PREPARATIONS v STANDARDS vi INSTRUMENTA TION vii STRUCTURES viii 1. INTRODUCTION 1 1.1 BIOASSAYS USED TO ASSESS TOPICAL STEROID ACTIVITY 1 1. 2 TEE HUMAN VASOCONSTRICTOR ASSAY AS A MEASURE OF TOPICAL STEROID ACTIVITY 5 1 .2.1 Alcoholic Vasoconstrictor Studies 5 1.2.2 Studies of Vasoconstriction in Other Solvents 9 1.2.3 Studied of Vasoconstri ction in Formulated Products 10 1. 3 THE MECHANISM OF BLANCHING 1 6 1.4 THE SKIN AS A CORTICOSTEROID RESERVOIR 18 1. 5 TEE CORRELATION OF VASOCONSTRICTOR ACTIVITY WITE CLINICAL EFFICACY 19 1. 6 THE EFFECT OF EXTEMPORANEOUS DILUTION OF TOPICAL CORTICO- STEROID FORMULATIONS 20 1.6.1 Pharmaceutical Considerations 21 1.6.2 Bacteriological Consider ations 22 1.6.3 Biopharmaceutical Considerations 23 2. METHODS 24 2.1 TEE BLANCHING ASSAY 24 2.1 .1 Volunteers 24 2.1 . 2 Mode of Application 24 2 .1.3 Reading of Results 26 2.2 STATISTICAL EVALUATION 27 2 . 3 CALCULATION OF PERCENT TOTAL POSSIBLE SCORE (% TPS) 28 2.4 DETERMINATION OF AREA UNDER THE BLANCHING PROFILE 28 3. DISCUSSION 31 3 .1 TEE ASSESSMENT OF VARIABLES AFFECTING TEE BLANCHING ABILITY OF FORMULATED PRODUCTS 31 - ii - CONTENTS (continued)/ 3.1. 1 The Effect of the Amount of Formulated Product Applied to the Test Site 32 3.
  • SUPPLEMENTARY APPENDIX 4: Search Strategies Syntax Guide For

    SUPPLEMENTARY APPENDIX 4: Search Strategies Syntax Guide For

    SUPPLEMENTARY APPENDIX 4: Search Strategies Pubmed, Embase Perioperative Management - PubMed Search Strategy – March 6, 2016 Syntax Guide for PubMed [MH] = Medical Subject Heading, also [TW] = Includes all words and numbers in known as MeSH the title, abstract, other abstract, MeSH terms, MeSH Subheadings, Publication Types, Substance Names, Personal Name as Subject, Corporate Author, Secondary Source, Comment/Correction Notes, and Other Terms - typically non-MeSH subject terms (keywords)…assigned by an organization other than NLM [SH] = a Medical Subject Heading [TIAB] = Includes words in the title and subheading, e.g. drug therapy abstracts [MH:NOEXP] = a command to retrieve the results of the Medical Subject Heading specified, but not narrower Medical Subject Heading terms Boolean Operators OR = retrieves results that include at least AND = retrieves results that include all the one of the search terms search terms NOT = excludes the retrieval of terms from the search Perioperative Management PubMed Search Strategy – March 6, 2016 Search Query #1 ((((ARTHROPLASTY, REPLACEMENT, HIP[MH] OR HIP PROSTHES*[TW] OR HIP REPLACEMENT*[TIAB] OR HIP ARTHROPLAST*[TIAB] OR HIP TOTAL REPLACEMENT*[TIAB] OR FEMORAL HEAD PROSTHES*[TIAB]) OR (ARTHROPLASTY, REPLACEMENT, KNEE[MH] OR KNEE PROSTHES*[TW] OR KNEE REPLACEMENT*[TW] OR KNEE ARTHROPLAST*[TW] OR KNEE TOTAL REPLACEMENT*[TIAB]) OR (ARTHROPLAST*[TW] AND (HIP[TIAB] OR HIPS[TIAB] OR KNEE*[TIAB])) AND (("1980/01/01"[PDAT] : "2016/03/06"[PDAT]) AND ENGLISH[LANG])) NOT (((("ADOLESCENT"[MESH]) OR "CHILD"[MESH])