| 词条 | Meloxicam |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 459437267 | IUPAC_name = 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide. | image = Meloxicam2DACS.svg | width = 250 | image2 = Meloxicam.png | tradename = Mobic, Metacam, others | Drugs.com = {{drugs.com|monograph|meloxicam}} | MedlinePlus = a601242 | pregnancy_AU = C | pregnancy_US = C | pregnancy_category = | legal_AU = S4 | legal_UK = POM | legal_US = Rx-only | routes_of_administration = By mouth | bioavailability = 89%[1] | protein_bound = 99.4%[1] | metabolism = Liver (CYP2C9 and 3A4-mediated)[1] | elimination_half-life = 20 hours[1] | excretion = Urine and faeces equally[1] | IUPHAR_ligand = 7220 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 71125-38-7 | ATC_prefix = M01 | ATC_suffix = AC06 | PubChem = 5281106 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00814 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 10442740 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = VG2QF83CGL | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00969 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 6741 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 599 | PDB_ligand = MXM | C=14 | H=13 | N=3 | O=4 | S=2 | molecular_weight = 351.403 g/mol | smiles = Cc1cnc(s1)NC(=O)C\\3=C(/O)c2ccccc2S(=O)(=O)N/3C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C14H13N3O4S2/c1-8-7-15-14(22-8)16-13(19)11-12(18)9-5-3-4-6-10(9)23(20,21)17(11)2/h3-7,18H,1-2H3,(H,15,16,19) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = ZRVUJXDFFKFLMG-UHFFFAOYSA-N }}Meloxicam, sold under the brand name Mobic among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation in rheumatic diseases and osteoarthritis.[1][7] It is taken by mouth.[2] It is recommended that it be used for as short of period as possible and at a low dose.[2] Common side effects include abdominal pain, dizziness, swelling, headache, and a rash.[2] Serious side effects may include heart disease, stroke, kidney problems, and stomach ulcers.[2] Use is not recommended in the third trimester of pregnancy.[2] It blocks cyclooxygenase-2 (COX-2) more than it blocks cyclooxygenase-1 (COX-1).[2] It is in the oxicam family of chemicals and is closely related to piroxicam.[2] Meloxicam was patented in 1977 and approved for medical use in the United States in 2000.[2][3] It was developed by Boehringer-Ingelheim, however is also available as a generic medication.[2] In the United States the wholesale cost per dose is less than US$0.02 as of 2018.[4] In the United Kingdom it costs about 0.13 pounds as of 2018.[1] In 2016 it was the 36th most prescribed medication in the United States with more than 21 million prescriptions.[5] Adverse effects{{See also|Nonsteroidal anti-inflammatory drug}}Meloxicam use can result in gastrointestinal toxicity and bleeding, headaches, rash, and very dark or black stool (a sign of intestinal bleeding). Like other NSAIDs, its use is associated with an increased risk of cardiovascular events such as heart attack and stroke.[6] It has fewer gastrointestinal side effects than diclofenac,[22] piroxicam,[7] naproxen,[8] and perhaps all other NSAIDs which are not COX-2 selective.[9] Although meloxicam inhibits formation of thromboxane A, it does not appear to do so at levels that would interfere with platelet function. A pooled analysis of randomized, controlled studies of meloxicam therapy of up to 60 days duration found that meloxicam was associated with a statistically significantly lower number of thromboembolic complications than the NSAID diclofenac (0.2% versus 0.8% respectively) but a similar incidence of thromboembolic events to naproxen and piroxicam.[10] Cardiovascular side effectsPersons with hypertension, high cholesterol, or diabetes are at risk for cardiovascular side effects. Persons with family history of heart disease, heart attack, or stroke must tell their treating physician as the potential for serious cardiovascular side effects is significant.[11][12] Mechanism of action{{Main|Non-steroidal anti-inflammatory drug}}Meloxicam blocks cyclooxygenase (COX), the enzyme responsible for converting arachidonic acid into prostaglandin H2—the first step in the synthesis of prostaglandins, which are mediators of inflammation. Meloxicam has been shown, especially at its low therapeutic doses, selectively to inhibit COX-2 over COX-1.[13] Meloxicam concentrations in synovial fluid range from 40% to 50% of those in plasma. The free fraction in synovial fluid is 2.5 times higher than in plasma, due to the lower albumin content in synovial fluid as compared to plasma. The significance of this penetration is unknown,[14] but it may account for the fact that it performs exceptionally well in treatment of arthritis in animal models.[15] Veterinary useMeloxicam is used in veterinary medicine, most commonly in dogs and cats, but also sees off-label use in other animals such as cattle and exotics.[16][17] Side effects in animals are similar to those found in humans; the principal side effect is gastrointestinal irritation (vomiting, diarrhea, and ulceration). Rarer but important side effects include liver and kidney toxicity. In healthy dogs given meloxicam, no perioperative adverse effects on the cardiovascular system have been reported at recommended dosages.[18] Perioperative administration of meloxicam to cats did not affect postoperative respiratory rate nor heart rate.[19] A peer-reviewed journal article cites NSAIDs, including meloxicam, as causing gastrointestinal upset and, at high doses, acute renal failure and CNS signs such as seizures and comas in cats. It adds that cats have a low tolerance for NSAIDs.[20][21] Meloxicam has been investigated as an alternative to diclofenac by the RSPB to prevent deaths of vultures.{{citation needed|date=October 2015}} PharmacokineticsIn dogs, the absorption of meloxicam from the stomach is not affected by the presence of food,[22] with the peak concentration (Cmax) of meloxicam occurring in the blood 7–8 hours after administration.[22] The half-life of meloxicam is approximately 24 hours in dogs.[22] In the koala (Phascolarctos cinereus), very little meloxicam is absorbed into the blood after oral administration (that is, it has poor bioavailability).[23] Legal statusUnited StatesSince 2003, meloxicam has been approved in the U.S. for use in dogs for the management of pain and inflammation associated with osteoarthritis, as an oral (liquid) formulation of meloxicam.[24] In January 2005, the product insert added a warning in bold-face type: "Do not use in cats."[25] An injectable formulation for use in dogs was approved by the FDA in November 2003.[26] In October 2004, a formulation for use in cats was approved for use prior to surgery only.[27] This is an injectable meloxicam, indicated for as a single, one-time dose only, with specific and repeated warnings not to administer a second dose.[28] In 2005, the U.S. Food and Drug Administration sent a Notice of Violation to the manufacturer for its promotional materials which included promotion of the drug for off-label use.[29] European UnionIn Europe, where the product has been available since the early 1990s,{{citation needed|date=October 2012}} it is licensed for other anti-inflammatory benefits including relief from both acute and chronic pain in dogs. In June 2007, an oral version of meloxicam was licensed for the long-term relief of pain in cats. Meloxicam is also licensed for use in horses, to relieve the pain associated with musculoskeletal disorders.[30] Other countriesAs of June 2008, meloxicam is registered for long-term use in cats in Australia, New Zealand, and Canada. References1. ^1 {{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=1112–1113|edition=76}} 2. ^1 2 3 4 5 6 7 8 9 {{cite web |title=Meloxicam Monograph for Professionals |url=https://www.drugs.com/monograph/meloxicam.html |website=Drugs.com |publisher=AHFS |accessdate=23 December 2018 |language=en}} 3. ^{{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=519 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA519 |language=en}} 4. ^{{cite web |title=NADAC as of 2018-12-19 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2018-12-19/g7bs-ahj4 |website=Centers for Medicare and Medicaid Services |accessdate=22 December 2018 |language=en}} 5. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}} 6. ^{{cite journal |vauthors=Stamm O, Latscha U, Janecek P, et al |title=Development of a special electrode for continuous subcutaneous pH measurement in the infant scalp |journal=Am. J. Obstet. Gynecol. |volume=124 |issue=2 |pages=193–5 |date=January 1976 |pmid=2012 |doi= 10.1016/S0002-9378(16)33297-5|url=}} 7. ^{{cite journal|doi= 10.1093/rheumatology/37.9.946|journal= The British Journal of Rheumatology|volume= 37|pages= 946–51|year= 1998|title= Improvement in gastrointestinal tolerability of the selective cyclooxygenase (COX)-2 inhibitor, meloxicam, compared with piroxicam: results of the Safety and Efficacy Large-scale Evaluation of COX-inhibiting Therapies (SELECT) trial in osteoarthritis|last1= Dequeker |first1= J|last2= Hawkey |first2= C|last3= Kahan |first3= A|last4= Steinbrück |first4= K|last5= Alegre |first5= C|last6= Baumelou |first6= E|last7= Begaud |first7= B|last8= Isomäki |first8= H|last9= Littlejohn |first9= G|last10= Mau |first10= J.|last11= Papazoglou |first11= S.|pmid=9783758|issue= 9|display-authors= 8}} 8. ^{{cite journal|journal= Rheumatology|volume= 35, Supplement 1|pages= 22–8|title= A Six-Month Double-Blind Trial to Compare the Efficacy and Safety of Meloxicam 7.5 mg Daily and Naproxen 750 mg Daily in Patients with Rheumatoid Arthritis|last1= Wojtulewski|first1= JA|last2= Schattenkirchner |first2= M|last3= Barceló |first3= P|last4= Le Loët |first4= X|last5= Bevis |first5= PJR|last6= Bluhmki |first6= E|last7= Distel |first7= M|doi=10.1093/rheumatology/35.suppl_1.22|year= 1996}} 9. ^1 {{cite journal|doi= 10.1093/rheumatology/37.9.937|title= Gastrointestinal tolerability of meloxicam compared to diclofenac in osteoarthritis patients|last1= Hawkey |first1= C|last2= Kahan |first2= A|last3= Steinbrück |first3= K|last4= Alegre |first4= C|last5= Baumelou |first5= E|last6= Bégaud |first6= B|last7= Dequeker |first7= J|last8= Isomäki |first8= H|last9= Littlejohn |first9= G|last10= Mau |first10= J.|last11= Papazoglou |first11= S|journal= Rheumatology|volume= 37|issue= 9|date=Sep 1998|pages= 937–945(9) |display-authors= 8}} 10. ^{{cite journal|pmid= 15234645|title= Gastrointestinal tolerability of meloxicam compared to diclofenac in osteoarthritis patients|last1= Singh |first1= G|last2= Lanes |first2= S|last3= Triadafilopoulos |first3= G|journal= Am J Med|volume= 117|issue= 9|year=2004|pages= 100–6|doi=10.1016/j.amjmed.2004.03.012}} 11. ^{{cite web |url=https://www.nlm.nih.gov/medlineplus/druginfo/meds/a601242.html|title=Medline Plus|publisher=Nlm.nih.gov|accessdate=15 November 2014}} 12. ^{{cite web |url=https://www.drugs.com/meloxicam.html|title=Drugs.com|publisher=Drugs.com|accessdate=15 November 2014}} 13. ^1 2 3 4 5 {{cite journal |last=Noble|first=S|author2=Balfour, JA|title=Meloxicam.|journal=Drugs|date=March 1996|volume=51|issue=3|pages=424–30; discussion 431–32|doi=10.2165/00003495-199651030-00007|pmid=8882380}} 14. ^{{cite web|url= https://www.drugs.com/pro/meloxicam.html|work= Drugs.com|accessdate= 17 March 2010|title= Meloxicam official FDA information, side effects, and uses|date= March 2010}} 15. ^{{cite journal|last1= Engelhardt |first1= G|last2= Homma |first2= D|last3= Schlegel |first3= K|last4= Utzmann |first4= R|last5= Schnitzler |first5= C|title= Anti-inflammatory, analgesic, antipyretic and related properties of meloxicam, a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance|journal= Inflammation Research|volume= 44|issue= 10|date=Oct 1995|doi= 10.1007/BF01757699|pages= 423–433|pmid= 8564518}} 16. ^Off-label use discussed in: Arnold Plotnick MS, DVM, ACVIM, ABVP, Pain Management using Metacam {{webarchive|url=https://web.archive.org/web/20110714025604/http://www.manhattancats.com/Articles/pain.html |date=2011-07-14 }}, and Stein, Robert, Perioperative Pain Management Part IV, Looking Beyond Butorphanol, Sep 2006, Veterinary Anesthesia & Analgesia Support Group. 17. ^For off-label use example in rabbits, see Krempels, Dana, Hind Limb Paresis and Paralysis in Rabbits, University of Miami Biology Department. 18. ^{{cite journal|last1=Boström|first1=IM|last2=Nyman|first2=G|last3=Hoppe|first3=A|last4=Lord|first4=P|title=Effects of meloxicam on renal function in dogs with hypotension during anaesthesia.|journal=Veterinary Anaesthesia and Analgesia|date=January 2006|volume=33|issue=1|pages=62–9|doi=10.1111/j.1467-2995.2005.00208.x|pmid=16412133}} 19. ^{{cite journal|last1=Höglund|first1=OV|last2=Dyall|first2=B|last3=Gräsman|first3=V|last4=Edner|first4=A|last5=Olsson|first5=U|last6=Höglund|first6=K|title=Effect of non-steroidal anti-inflammatory drugs on postoperative respiratory and heart rate in cats subjected to ovariohysterectomy.|journal=Journal of Feline Medicine and Surgery|volume=20|issue=10|date=1 November 2017|pages=980–984|doi=10.1177/1098612X17742290|pmid=29165006}} 20. ^{{cite web|url=http://veterinarymedicine.dvm360.com/toxicology-brief-10-most-common-toxicoses-cats?id=&sk=&date=&pageID=3 |title=Toxicology Brief: The 10 most common toxicoses in cats |publisher=Veterinarymedicine.dvm360.com |date=2006-06-01 |accessdate=2018-09-16}} 21. ^Merola, Valentina, DVM, DABT, and Dunayer Eric, MS, VMD, DABT, The 10 most common toxicoses in cats{{dead link|date=January 2018 |bot=InternetArchiveBot |fix-attempted=yes }}, Toxicology Brief, Veterinary Medicine, pp. 340–342, June, 2006. 22. ^1 2 {{cite journal|last1=Khan|first1=SA|last2=McLean|first2=MK|title=Toxicology of frequently encountered nonsteroidal anti-inflammatory drugs in dogs and cats|journal=The Veterinary Clinics of North America. Small Animal Practice|date=March 2012|volume=42|issue=2|pages=289–306, vi–vii|doi=10.1016/j.cvsm.2012.01.003|pmid=22381180}} 23. ^{{cite journal |last1=Kimble|first1=B.|last2=Black|first2=L. A.|last3=Li|first3=K. M.|last4=Valtchev|first4=P.|last5=Gilchrist|first5=S.|last6=Gillett|first6=A.|last7=Higgins|first7=D. P.|last8=Krockenberger|first8=M. B.|last9=Govendir|first9=M.|title=Pharmacokinetics of meloxicam in koalas (Phascolarctos cinereus) after intravenous, subcutaneous and oral administration|journal=Journal of Veterinary Pharmacology and Therapeutics|volume=36|issue=5|pages=486–493|doi=10.1111/jvp.12038|pmid=23406022|year=2013}} 24. ^{{cite web |url=http://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm118006.pdf|title=NADA 141-213: New Animal Drug Application Approval (for Metacam (meloxicam) 0.5 mg/mL and 1.5 mg/mL Oral Suspension)|date=April 15, 2003|publisher=US Food and Drug Administration|accessdate=24 July 2010}} 25. ^Metacam Client Information Sheet, product description: "Non-steroidal anti-inflammatory drug for oral use in dogs only", and in the "What Is Metacam" section in bold-face type: "Do not use in cats.", January 2005. 26. ^{{cite web |url=http://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm118026.pdf |title=Metacam 5 mg/mL Solution for Injection|publisher=Fda.gov|accessdate=15 November 2014}} 27. ^{{cite web |url=http://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm118027.pdf|title=Metacam 5 mg/mL Solution for Injection, Supplemental Approval|date=October 28, 2004|publisher=Fda.gov|accessdate=15 November 2014}} 28. ^See the manufacturer's FAQ on its website, and its clinical dosing instructions for cats. {{webarchive|url=https://web.archive.org/web/20080906211039/http://www.bi-vetmedica.com/product_sites/METACAMINCats/documents/Metacam_Inj_cats_label.pdf |date=2008-09-06 }} 29. ^US FDA Notice of Violation for off-label use promotion, April 2005. 30. ^{{cite book|editor1-last=Maddison|editor1-first=JE|editor2-last=Page|editor2-first=SW|editor3-last=Church|editor3-first=D|title=Small animal clinical pharmacology|date=2008|publisher=Saunders/Elsevier|location=Edinburgh|isbn=9780702028588|pages=301–302|edition=2nd|chapter=Meloxicam}} External links
9 : Nonsteroidal anti-inflammatory drugs|Benzothiazines|Carboxamides|Cat medications|Dog medications|Thiazoles|Veterinary drugs|RTT|Boehringer Ingelheim |
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