词条 | Loxoprofen |
释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 462094150 | IUPAC_name = (RS)-2- | image = Loxoprofen.svg | width = 250px | image2 = Loxoprofen 3D.png | chirality = Racemic mixture | tradename = | Drugs.com = {{drugs.com|international|loxoprofen}} | pregnancy_category = | legal_status = Red Stripe (Brazil) | routes_of_administration = Oral, transdermal | bioavailability = | protein_bound = 97% | metabolism = Hepatic glucuronidation | elimination_half-life = 75 minutes | excretion = Renal | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 68767-14-6 | ATC_prefix = M01 | ATC_suffix = AE | PubChem = 3965 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3828 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3583H0GZAP | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08149 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 76172 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 19299 | C=15 | H=18 | O=3 | molecular_weight = 246.302 g/mol 304.314 g/mol (sodium salt as the dihydrate) | SMILES = O=C2C(Cc1ccc(cc1)C(C(=O)O)C)CCC2 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C15H18O3/c1-10(15(17)18)12-7-5-11(6-8-12)9-13-3-2-4-14(13)16/h5-8,10,13H,2-4,9H2,1H3,(H,17,18) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = YMBXTVYHTMGZDW-UHFFFAOYSA-N }}Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) in the propionic acid derivatives group, which also includes ibuprofen and naproxen among others. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006.[1] It was patented in 1977 and approved for medical use in 1986.[2] PharmacokineticsLoxoprofen is a prodrug. It is quickly converted to its active trans-alcohol metabolite following oral administration, and reaches its peak plasma concentration within 30 to 50 minutes. Mechanism of actionAs most NSAIDs, loxoprofen is a non-selective cyclooxygenase inhibitor, and works by reducing the synthesis of prostaglandins from arachidonic acid. InteractionsLoxoprofen should not be administered at the same time as second-generation quinolone antibiotics such as ciprofloxacin and norfloxacin, as it increases their inhibition of GABA and this may cause seizures.[3] It may also increase the plasma concentration of warfarin, methotrexate, sulfonylurea derivatives and lithium salts, so care should be taken when loxoprofen is administered to patients taking any of these drugs.[3] Brand namesIt is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, in Argentina as Oxeno, in India as Loxomac, and in Thailand as Japrolox. References1. ^{{cite press release | url = http://www.daiichisankyo.com/media_investors/media_relations/press_releases/detail/005643.html | title = Percutaneous Absorption-Type Analgesic and Anti-inflammatory Drug Loxonin Poultice 100mg Receives Approval for Manufacture | author = Daiichi Sankyo Co. | date = January 24, 2006 | accessdate = 2007-04-19 | publisher = Doctor's Guide Global Edition}} {{Commons category}}{{NSAIDs}}{{Prostanoidergics}}2. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=521 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA521 |language=en}} 3. ^1 {{cite web | url = http://bulas.cxpass.net/index.asp?C=A&V=66506F737449443D36323834266163743D73686F7752656164436F6D6D656E7473 | title = LOXONIN - Bula do Medicamento [Label Information] | year = 2007 | accessdate = 2007-04-19 | publisher = Centralx|language=pt}} 5 : Nonsteroidal anti-inflammatory drugs|Prodrugs|Cycloalkanones|Propionic acids|Daiichi Sankyo |
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