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酮咯酸：修订间差异

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'''酮咯酸'''（{{lang-en|Ketorolac}}，也稱為克多羅多克）以商品名Toradol和Biorolac等在市面銷售，是一種用於治療[[疼痛]]的[[非類固醇類抗發炎藥]] (NSAID)。<ref name="researchgate.net">{{cite journal | vauthors = Mallinson T |title=A review of ketorolac as a prehospital analgesic |journal=Journal of Paramedic Practice |date=2017 |volume=9 |issue=12 |pages=522–526 |url=https://www.researchgate.net/publication/321640488 |access-date=2018-06-02 |language=en |doi=10.12968/jpar.2017.9.12.522 |doi-access=free }}</ref><ref name=AHFS2019/>特別用於治療中度至重度疼痛用途。<ref name=BNF76/>建議治療時間不超過六天，<ref name=AHFS2019/>在[[瑞士]]的建議治療時間為不超過兩天。<ref>{{Cite web |url=https://compendium.ch/product/30303-tora-dol-inj-los-30-mg-ml/mpro |title=TORA-DOL Inj Lös 30 mg/ml |date=2022-03-01 |website=Kompendium |language=de |quote=Die Behandlung mit Ampullen ist bei akuten und schweren Schmerzzuständen angezeigt und sollte nicht länger als 2 Tage dauern.}}</ref>它透過[[口服給藥|口服]]、[[鼻腔給藥|鼻腔]]、[[靜脈注射]]或[[肌肉注射]]的方式給藥，另有[[眼藥水]]的形式。<ref name=AHFS2019/><ref name=BNF76>{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=1144, 1302–1303|edition=76}}</ref>給藥後一小時內開始作用，持續時間達八小時。<ref name=AHFS2019/>
'''酮咯酸'''（[[INN]]：ketorolac）或音译'''克多羅多克'''，以商品名 Toradol、Biorolac 等等銷售，是一種用於治療[[疼痛]]的[[非類固醇類抗發炎藥]]（NSAID），属非选择性[[环氧合酶]]抑制剂<ref name="researchgate.net">{{cite journal |vauthors=Mallinson T |title=A review of ketorolac as a prehospital analgesic |journal=Journal of Paramedic Practice |date=2017 |volume=9 |issue=12 |pages=522–526 |url=https://www.researchgate.net/publication/321640488 |access-date=2018-06-02 |language=en |doi=10.12968/jpar.2017.9.12.522 |doi-access=free |archive-date=2018-06-05 |archive-url=https://web.archive.org/web/20180605033254/https://www.researchgate.net/publication/321640488_A_review_of_ketorolac_as_a_prehospital_analgesic |dead-url=no }}</ref><ref name=AHFS2019/>。特別用於治療中度至重度疼痛用途<ref name=BNF76/>。建議治療時間不超過六天<ref name=AHFS2019/>，在[[瑞士]]的建議治療時間為不超過兩天<ref>{{Cite web |url=https://compendium.ch/product/30303-tora-dol-inj-los-30-mg-ml/mpro |title=TORA-DOL Inj Lös 30 mg/ml |date=2022-03-01 |website=Kompendium |language=de |quote=Die Behandlung mit Ampullen ist bei akuten und schweren Schmerzzuständen angezeigt und sollte nicht länger als 2 Tage dauern. |access-date=2024-02-07 |archive-date=2023-06-07 |archive-url=https://web.archive.org/web/20230607181444/https://compendium.ch/product/30303-tora-dol-inj-los-30-mg-ml/mpro |dead-url=no }}</ref>。它透過[[口服給藥|口服]]、[[鼻腔給藥|鼻腔]]、[[靜脈注射]]或[[肌肉注射]]的方式給藥，另有[[眼藥水]]的形式<ref name=AHFS2019/><ref name=BNF76>{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=1144, 1302–1303|edition=76}}</ref>。給藥後一小時內開始作用，持續時間達八小時<ref name=AHFS2019/>。


常見的副作用包括[[昏睡|嗜睡]]、[[頭暈]]、腹痛、腫脹和[[噁心]]。<ref name=AHFS2019/>嚴重的副作用有[[上消化道出血]]、[[腎衰竭]]、[[心臟病]]、[[支氣管痙攣]]、[[心臟衰竭]]和[[過敏性休克]]。<ref name=AHFS2019/>不建議個體在[[妊娠|懷孕]]後期或[[母乳哺育|哺乳]]期間使用。<ref name=AHFS2019/>酮咯酸發揮作用的方式是透過阻斷[[環氧合酶]] 1和 2（COX1和COX2）而減少[[前列腺素]]產生。<ref name=AHFS2019/><ref name=Daily2019>{{cite web |title=DailyMed - ketorolac tromethamine tablet, film coated |url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2837a082-3a34-6f81-5e43-45a70295686b |website=dailymed.nlm.nih.gov |access-date=2019-04-14}}</ref>
常見的副作用包括[[昏睡|嗜睡]]、[[頭暈]]、腹痛、腫脹和[[噁心]]。<ref name=AHFS2019/>嚴重的副作用有[[上消化道出血]]、[[腎衰竭]]、[[心臟病]]、[[支氣管痙攣]]、[[心臟衰竭]]和[[過敏性休克]]。<ref name=AHFS2019/>不建議個體在[[妊娠|懷孕]]後期或[[母乳哺育|哺乳]]期間使用。<ref name=AHFS2019/>酮咯酸發揮作用的方式是透過阻斷[[環氧合酶]] 1和 2（COX1和COX2）而減少[[前列腺素]]產生。<ref name=AHFS2019/><ref name=Daily2019>{{cite web |title=DailyMed - ketorolac tromethamine tablet, film coated |url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2837a082-3a34-6f81-5e43-45a70295686b |website=dailymed.nlm.nih.gov |access-date=2019-04-14 |archive-date=2020-08-13 |archive-url=https://web.archive.org/web/20200813001442/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2837a082-3a34-6f81-5e43-45a70295686b |dead-url=no }}</ref>


此藥物於1976年獲得[[專利]]，並於1989年獲得批准用於醫療用途。<ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=521 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA521 |language=en}}</ref><ref name=AHFS2019>{{cite web |title=Ketorolac Tromethamine Monograph for Professionals |url=https://www.drugs.com/monograph/ketorolac-tromethamine.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |access-date= 2019-04-13 |language=en}}</ref>它有[[非處方藥]]的形式出售。<ref name=BNF76/>此藥物在2020年是美國最常使用處方藥中排名第249，開立的處方箋超過100萬張。<ref>{{cite web | title = The Top 300 of 2020 | url = https://clincalc.com/DrugStats/Top300Drugs.aspx | website = ClinCalc | access-date = 2022-10-07}}</ref><ref>{{cite web | title = Ketorolac - Drug Usage Statistics | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Ketorolac | access-date = 2022-10-07 }}</ref>
此藥物於1976年獲得[[專利]]，並於1989年獲得批准用於醫療用途。<ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=521 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA521 |language=en}}</ref><ref name=AHFS2019>{{cite web |title=Ketorolac Tromethamine Monograph for Professionals |url=https://www.drugs.com/monograph/ketorolac-tromethamine.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |access-date=2019-04-13 |language=en |archive-date=2019-04-08 |archive-url=https://web.archive.org/web/20190408214139/https://www.drugs.com/monograph/ketorolac-tromethamine.html |dead-url=no }}</ref>它有[[非處方藥]]的形式出售。<ref name=BNF76/>此藥物在2020年是美國最常使用處方藥中排名第249，開立的處方箋超過100萬張。<ref>{{cite web | title = The Top 300 of 2020 | url = https://clincalc.com/DrugStats/Top300Drugs.aspx | website = ClinCalc | access-date = 2022-10-07 | archive-date = 2017-03-16 | archive-url = https://web.archive.org/web/20170316102646/https://clincalc.com/DrugStats/Top300Drugs.aspx | dead-url = no }}</ref><ref>{{cite web | title = Ketorolac - Drug Usage Statistics | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Ketorolac | access-date = 2022-10-07 | archive-date = 2024-02-29 | archive-url = https://web.archive.org/web/20240229213617/https://clincalc.com/DrugStats/Drugs/Ketorolac | dead-url = no }}</ref>


由於酮咯酸導致上消化道出血和腎衰竭，造成一系列死亡案例，而於1993年有[[德國]][[鎮痛藥]]市場撤出。<ref>{{Cite web |url=https://www.arznei-telegramm.de/html/1993_08/9308084_02.html |title=Abverkauf von Ketorolac (TORATEX) gestoppt |year=1993 |language= |trans-title=Sale of Ketorolac (TORATEX) stopped}}</ref>最初此藥物引入德國時，因其副作用被認為輕很多，不會產生任何[[物質依賴]]，一次劑量有效時間達7-8小時（[[嗎啡]]只有3-4小時），而經常被誤用作疼痛治療中的[[類阿片]]藥物替代品。由於酮咯酸是一種非常有效的前列腺素抑制劑，會削弱腎臟對[[血管收縮]]相關效應而產生的防禦能力（例如失血或[[內源]]性[[兒茶酚胺]]濃度較高時）。<ref>{{Cite web |url=https://www.arznei-telegramm.de/html/1993_06/9306061_05.html |title=Warnhinweis: Wie lange noch Analgetikum Ketorolac (Toratex)? |publisher=Arznei-Telegramm |year=1993 |language=de |trans-title=Warning notice: How long anymore analgesic Ketorolac (Toratex)?}}</ref>
由於酮咯酸導致上消化道出血和腎衰竭，造成一系列死亡案例，而於1993年有[[德國]][[鎮痛藥]]市場撤出。<ref>{{Cite web |url=https://www.arznei-telegramm.de/html/1993_08/9308084_02.html |title=Abverkauf von Ketorolac (TORATEX) gestoppt |year=1993 |language= |trans-title=Sale of Ketorolac (TORATEX) stopped |access-date=2024-02-07 |archive-date=2023-10-03 |archive-url=https://web.archive.org/web/20231003042337/https://www.arznei-telegramm.de/html/1993_08/9308084_02.html |dead-url=no }}</ref>最初此藥物引入德國時，因其副作用被認為輕很多，不會產生任何[[物質依賴]]，一次劑量有效時間達7-8小時（[[嗎啡]]只有3-4小時），而經常被誤用作疼痛治療中的[[類阿片]]藥物替代品。由於酮咯酸是一種非常有效的前列腺素抑制劑，會削弱腎臟對[[血管收縮]]相關效應而產生的防禦能力（例如失血或[[內源]]性[[兒茶酚胺]]濃度較高時）。<ref>{{Cite web |url=https://www.arznei-telegramm.de/html/1993_06/9306061_05.html |title=Warnhinweis: Wie lange noch Analgetikum Ketorolac (Toratex)? |publisher=Arznei-Telegramm |year=1993 |language=de |trans-title=Warning notice: How long anymore analgesic Ketorolac (Toratex)? |access-date=2024-02-07 |archive-date=2023-03-24 |archive-url=https://web.archive.org/web/20230324114422/https://www.arznei-telegramm.de/html/1993_06/9306061_05.html |dead-url=no }}</ref>


==醫療用途==
==醫療用途==
[[File:Ketorolac (Toradol).jpg|thumb|left|於[[俄羅斯]]販售的酮咯酸。]]
[[File:Ketorolac (Toradol).jpg|thumb|left|於[[俄羅斯]]販售的酮咯酸。]]


酮咯酸用於短期治療中度至重度疼痛。<ref name="researchgate.net"/>因為它可能會導致腎臟損傷，<ref name = "Henry_2016" />{{rp|280}}通常施用時間不會超過五天。<ref name=Vallertand>{{cite book | vauthors = Vallerand AH |publisher= F.A. Davis Company |location= Philadelphia |year= 2017 |title= Davis's Drug Guide for Nurses|page=730 | isbn = 9780803657052}}</ref><ref name=PDR/><ref name=AHFS>{{cite web |title= Ketorolac-tromethamine |url= https://www.drugs.com/monograph/ketorolac-tromethamine.html |work= The American Society of Health-System Pharmacists|access-date=3 April 2011}}</ref><ref name = "Henry_2016">{{cite book | vauthors = Henry N | title = RN pharmacology for nursing : review module | publisher = Assessment Technologies Institute | location = Overland Park, KS | year = 2016 | isbn = 978-1-56533-573-8 }}</ref>{{rp|291}}
酮咯酸用於短期治療中度至重度疼痛。<ref name="researchgate.net"/>因為它可能會導致腎臟損傷，<ref name = "Henry_2016" />{{rp|280}}通常施用時間不會超過五天。<ref name=Vallertand>{{cite book | vauthors = Vallerand AH |publisher= F.A. Davis Company |location= Philadelphia |year= 2017 |title= Davis's Drug Guide for Nurses| url = https://archive.org/details/davissdrugguidef0000vall_u2j2 |page=[https://archive.org/details/davissdrugguidef0000vall_u2j2/page/730 730] | isbn = 9780803657052}}</ref><ref name=PDR/><ref name=AHFS>{{cite web |title= Ketorolac-tromethamine |url= https://www.drugs.com/monograph/ketorolac-tromethamine.html |work= The American Society of Health-System Pharmacists |access-date= 3 April 2011 |archive-date= 2019-04-08 |archive-url= https://web.archive.org/web/20190408214139/https://www.drugs.com/monograph/ketorolac-tromethamine.html |dead-url= no }}</ref><ref name = "Henry_2016">{{cite book | vauthors = Henry N | title = RN pharmacology for nursing : review module | url = https://archive.org/details/rnpharmacologyfo0000unse | publisher = Assessment Technologies Institute | location = Overland Park, KS | year = 2016 | isbn = 978-1-56533-573-8 }}</ref>{{rp|291}}


酮咯酸與撲熱息痛（[[乙醯胺酚]]）一起服用可有效控制新生兒疼痛，它不會像類阿片藥物那樣抑制[[呼吸]]。<ref name="MartinJimenez2017">{{cite journal | vauthors = Martin LD, Jimenez N, Lynn AM | title = A review of perioperative anesthesia and analgesia for infants: updates and trends to watch | journal = F1000Research | volume = 6 | pages = 120 | year = 2017 | pmid = 28232869 | pmc = 5302152 | doi = 10.12688/f1000research.10272.1 | doi-access = free }}</ref>酮咯酸也是類阿片藥物的佐劑，可增強疼痛緩解作用。它也用於治療婦女的[[經痛]]。<ref name = "Henry_2016" />{{rp|291}} 此藥物也因可減輕發炎而用於治療特發性[[心包炎]]。<ref name="SchwierTran2016">{{cite journal | vauthors = Schwier N, Tran N | title = Non-Steroidal Anti-Inflammatory Drugs and Aspirin Therapy for the Treatment of Acute and Recurrent Idiopathic Pericarditis | journal = Pharmaceuticals | volume = 9 | issue = 2 | pages = 17 | date = March 2016 | pmid = 27023565 | pmc = 4932535 | doi = 10.3390/ph9020017 | doi-access = free }}</ref>
酮咯酸與撲熱息痛（[[乙醯胺酚]]）一起服用可有效控制新生兒疼痛，它不會像類阿片藥物那樣抑制[[呼吸]]。<ref name="MartinJimenez2017">{{cite journal | vauthors = Martin LD, Jimenez N, Lynn AM | title = A review of perioperative anesthesia and analgesia for infants: updates and trends to watch | journal = F1000Research | volume = 6 | pages = 120 | year = 2017 | pmid = 28232869 | pmc = 5302152 | doi = 10.12688/f1000research.10272.1 | doi-access = free }}</ref>酮咯酸也是類阿片藥物的佐劑，可增強疼痛緩解作用。它也用於治療婦女的[[經痛]]。<ref name = "Henry_2016" />{{rp|291}} 此藥物也因可減輕發炎而用於治療特發性[[心包炎]]。<ref name="SchwierTran2016">{{cite journal | vauthors = Schwier N, Tran N | title = Non-Steroidal Anti-Inflammatory Drugs and Aspirin Therapy for the Treatment of Acute and Recurrent Idiopathic Pericarditis | journal = Pharmaceuticals | volume = 9 | issue = 2 | pages = 17 | date = March 2016 | pmid = 27023565 | pmc = 4932535 | doi = 10.3390/ph9020017 | doi-access = free }}</ref>
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在全身性使用時，可透過口服、[[口腔黏膜吸收|舌下]]、肌肉注射、靜脈注射和{{le|鼻腔噴霧|nasal spray}}方式給藥。<ref name=Vallertand/>通常的做法是先透過肌肉注射或靜脈注射，<ref name="researchgate.net"/>繼而採口服給藥。<ref name=Vallertand/><ref name="MartinJimenez2017"/>
在全身性使用時，可透過口服、[[口腔黏膜吸收|舌下]]、肌肉注射、靜脈注射和{{le|鼻腔噴霧|nasal spray}}方式給藥。<ref name=Vallertand/>通常的做法是先透過肌肉注射或靜脈注射，<ref name="researchgate.net"/>繼而採口服給藥。<ref name=Vallertand/><ref name="MartinJimenez2017"/>


酮咯酸也用作眼藥水。在眼科手術期間幫助緩解疼痛，<ref name="Saenz-de-ViteriGonzalez-Salinas2016">{{cite journal | vauthors = Gonzalez-Salinas R, Guarnieri A, Guirao Navarro MC, Saenz-de-Viteri M | title = Patient considerations in cataract surgery - the role of combined therapy using phenylephrine and ketorolac | journal = Patient Preference and Adherence | volume = 10 | pages = 1795–1801 | year = 2016 | pmid = 27695298 | pmc = 5029911 | doi = 10.2147/PPA.S90468 | doi-access = free }}</ref>且可有效治療眼部發[[癢]]。<ref name=Karch>{{cite book | vauthors = Karch A |page = 272| title = Focus on nursing pharmacology | publisher = Wolters Kluwer | location = Philadelphia | year = 2017 | isbn = 9781496318213 }}</ref>無足夠的證據顯示非類固醇抗發炎藥有助於預防[[黃斑水腫]]。<ref name="LimLim2016">{{cite journal | vauthors = Lim BX, Lim CH, Lim DK, Evans JR, Bunce C, Wormald R | title = Prophylactic non-steroidal anti-inflammatory drugs for the prevention of macular oedema after cataract surgery | journal = The Cochrane Database of Systematic Reviews | volume = 2016 | pages = CD006683 | date = November 2016 | issue = 11 | pmid = 27801522 | pmc = 6464900 | doi = 10.1002/14651858.CD006683.pub3 | url = http://discovery.ucl.ac.uk/1529414/ }}</ref><ref name="SivaprasadBunce2012">{{cite journal |vauthors=Wingert AM, Liu SH, Lin JC, Sridhar J |date=December 2022 |title=Non-steroidal anti-inflammatory agents for treating cystoid macular oedema following cataract surgery |journal=The Cochrane Database of Systematic Reviews |volume=2022 |issue= 12|pages= CD004239|doi=10.1002/14651858.CD004239.pub4 |pmid=36520144|pmc=9754896 }}</ref>酮咯酸眼藥水也用於治療[[角膜刮傷]]而引起的疼痛。<ref name="Wakai">{{cite journal | vauthors = Wakai A, Lawrenson JG, Lawrenson AL, Wang Y, Brown MD, Quirke M, Ghandour O, McCormick R, Walsh CD, Amayem A, Lang E, Harrison N | display-authors = 6 | title = Topical non-steroidal anti-inflammatory drugs for analgesia in traumatic corneal abrasions | journal = The Cochrane Database of Systematic Reviews | volume = 2017 | pages = CD009781 | date = May 2017 | issue = 5 | pmid = 28516471 | pmc = 6481688 | doi = 10.1002/14651858.CD009781.pub2 }}</ref>
酮咯酸也用作眼藥水。在眼科手術期間幫助緩解疼痛，<ref name="Saenz-de-ViteriGonzalez-Salinas2016">{{cite journal | vauthors = Gonzalez-Salinas R, Guarnieri A, Guirao Navarro MC, Saenz-de-Viteri M | title = Patient considerations in cataract surgery - the role of combined therapy using phenylephrine and ketorolac | journal = Patient Preference and Adherence | volume = 10 | pages = 1795–1801 | year = 2016 | pmid = 27695298 | pmc = 5029911 | doi = 10.2147/PPA.S90468 | doi-access = free }}</ref>且可有效治療眼部發[[癢]]。<ref name=Karch>{{cite book | vauthors = Karch A |page = [https://archive.org/details/focusonnursingph0000karc/page/272 272]| title = Focus on nursing pharmacology | url = https://archive.org/details/focusonnursingph0000karc | publisher = Wolters Kluwer | location = Philadelphia | year = 2017 | isbn = 9781496318213 }}</ref>無足夠的證據顯示非類固醇抗發炎藥有助於預防[[黃斑水腫]]。<ref name="LimLim2016">{{cite journal | vauthors = Lim BX, Lim CH, Lim DK, Evans JR, Bunce C, Wormald R | title = Prophylactic non-steroidal anti-inflammatory drugs for the prevention of macular oedema after cataract surgery | journal = The Cochrane Database of Systematic Reviews | volume = 2016 | pages = CD006683 | date = November 2016 | issue = 11 | pmid = 27801522 | pmc = 6464900 | doi = 10.1002/14651858.CD006683.pub3 | url = http://discovery.ucl.ac.uk/1529414/ | access-date = 2024-02-07 | archive-date = 2021-08-28 | archive-url = https://web.archive.org/web/20210828134945/https://discovery.ucl.ac.uk/id/eprint/1529414/ | dead-url = no }}</ref><ref name="SivaprasadBunce2012">{{cite journal |vauthors=Wingert AM, Liu SH, Lin JC, Sridhar J |date=December 2022 |title=Non-steroidal anti-inflammatory agents for treating cystoid macular oedema following cataract surgery |journal=The Cochrane Database of Systematic Reviews |volume=2022 |issue= 12|pages= CD004239|doi=10.1002/14651858.CD004239.pub4 |pmid=36520144|pmc=9754896 }}</ref>酮咯酸眼藥水也用於治療[[角膜刮傷]]而引起的疼痛。<ref name="Wakai">{{cite journal | vauthors = Wakai A, Lawrenson JG, Lawrenson AL, Wang Y, Brown MD, Quirke M, Ghandour O, McCormick R, Walsh CD, Amayem A, Lang E, Harrison N | display-authors = 6 | title = Topical non-steroidal anti-inflammatory drugs for analgesia in traumatic corneal abrasions | journal = The Cochrane Database of Systematic Reviews | volume = 2017 | pages = CD009781 | date = May 2017 | issue = 5 | pmid = 28516471 | pmc = 6481688 | doi = 10.1002/14651858.CD009781.pub2 }}</ref>


使用酮咯酸期間，臨床醫師會監測不良反應表現，經常化驗例如[[肝功能測試|肝功能]]、{{le|出血時間|bleeding time}}、及[[尿素氮]]、血清[[肌酸酐]]和[[電解質]]水平，協助識別潛在的併發症。<ref name=Vallertand/><ref name=PDR>{{cite book | title = Physician's Desk Reference 2017 | pages = S–474–5|publisher = PDR, LLC| location = Montvale, New Jersey | year = 2017 | isbn = 9781563638381| title-link = Physicians' Desk Reference}}</ref>
使用酮咯酸期間，臨床醫師會監測不良反應表現，經常化驗例如[[肝功能測試|肝功能]]、{{le|出血時間|bleeding time}}、及[[尿素氮]]、血清[[肌酸酐]]和[[電解質]]水平，協助識別潛在的併發症。<ref name=Vallertand/><ref name=PDR>{{cite book | title = Physician's Desk Reference 2017 | pages = S–474–5|publisher = PDR, LLC| location = Montvale, New Jersey | year = 2017 | isbn = 9781563638381| title-link = Physicians' Desk Reference}}</ref>
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==不良影響==
==不良影響==
常見（>10%）的副作用是嗜睡。不常見（<1%）的副作用有{{le|感覺異常|paresthesia}}、出血時間延長、注射部位疼痛、[[紫癜|紫斑]]、出汗、思維異常、眼淚增加、[[水腫]]、[[面色蒼白]]、口乾、味覺異常、[[頻尿症|頻尿]]、肝酵素升高、發癢以及其他症狀。酮咯酸會降低[[血小板]]功能。<ref name = "Henry_2016" />{{rp|279}}
常見（>10%）的副作用是嗜睡。不常見（<1%）的副作用有[[感覺異常]]、出血時間延長、注射部位疼痛、[[紫癜|紫斑]]、出汗、思維異常、眼淚增加、[[水腫]]、[[面色蒼白]]、口乾、味覺異常、[[頻尿症|頻尿]]、肝酵素升高、發癢以及其他症狀。酮咯酸會降低[[血小板]]功能。<ref name = "Henry_2016" />{{rp|279}}


潛在致命的不良反應雖然不常見，但包含有中風、心肌梗塞、上消化道出血、[[史蒂芬斯－強森症候群]]、{{le|中毒性表皮壞死鬆解症| toxic epidermal necrolysis}}和過敏性休克。就安全性而言，酮咯酸被評估為較[[醋氯芬酸]]、[[塞來昔布]]和[[布洛芬]]（均為非類固醇抗發炎藥）具有相對較高的風險。<ref name="SchwierTran2016" />
潛在致命的不良反應雖然不常見，但包含有中風、心肌梗塞、上消化道出血、[[史蒂芬斯－強森症候群]]、{{le|中毒性表皮壞死鬆解症| toxic epidermal necrolysis}}和過敏性休克。就安全性而言，酮咯酸被評估為較[[醋氯芬酸]]、[[塞來昔布]]和[[布洛芬]]（均為非類固醇抗發炎藥）具有相對較高的風險。<ref name="SchwierTran2016" />
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如果個體在懷孕晚期服用酮咯酸，會導致嬰兒[[動脈導管]]過早收縮，與所有非類固醇抗發炎藥物的作用相同。<ref name=Vallertand/><ref name=PDR/>
如果個體在懷孕晚期服用酮咯酸，會導致嬰兒[[動脈導管]]過早收縮，與所有非類固醇抗發炎藥物的作用相同。<ref name=Vallertand/><ref name=PDR/>


[[美國食品藥物管理局]] (FDA) 於2020年10月要求更新所有非類固醇抗發炎藥物的{{le|藥品標籤|Drug labelling}}，標明這類藥物對未出生嬰兒可能會產生腎臟問題，而導致[[羊水]]過低的風險。<ref name="FDA PR 20201015" /><ref name="FDA safety 20201015" />標籤建議孕婦在懷孕20週或之後避免使用非類固醇抗發炎藥物。<ref name="FDA PR 20201015">{{cite press release | title=FDA Warns that Using a Type of Pain and Fever Medication in Second Half of Pregnancy Could Lead to Complications | website=U.S. [[Food and Drug Administration]] (FDA) | date= 2020-10-15 | url=https://www.fda.gov/news-events/press-announcements/fda-warns-using-type-pain-and-fever-medication-second-half-pregnancy-could-lead-complications | access-date=2020-10-15}} {{PD-notice}}</ref><ref name="FDA safety 20201015">{{cite web | title=NSAIDs may cause rare kidney problems in unborn babies | website=U.S. Food and Drug Administration | date= 2017-07-21 | url=https://www.fda.gov/drugs/drug-safety-and-availability/fda-recommends-avoiding-use-nsaids-pregnancy-20-weeks-or-later-because-they-can-result-low-amniotic | access-date= 2020-10-15}} {{PD-notice}}</ref>
[[美國食品藥物管理局]] (FDA) 於2020年10月要求更新所有非類固醇抗發炎藥物的{{le|藥品標籤|Drug labelling}}，標明這類藥物對未出生嬰兒可能會產生腎臟問題，而導致[[羊水]]過低的風險。<ref name="FDA PR 20201015" /><ref name="FDA safety 20201015" />標籤建議孕婦在懷孕20週或之後避免使用非類固醇抗發炎藥物。<ref name="FDA PR 20201015">{{cite press release | title=FDA Warns that Using a Type of Pain and Fever Medication in Second Half of Pregnancy Could Lead to Complications | website=U.S. [[Food and Drug Administration]] (FDA) | date=2020-10-15 | url=https://www.fda.gov/news-events/press-announcements/fda-warns-using-type-pain-and-fever-medication-second-half-pregnancy-could-lead-complications | access-date=2020-10-15 | archive-date=2020-10-16 | archive-url=https://web.archive.org/web/20201016180003/https://www.fda.gov/news-events/press-announcements/fda-warns-using-type-pain-and-fever-medication-second-half-pregnancy-could-lead-complications | dead-url=no }} {{PD-notice}}</ref><ref name="FDA safety 20201015">{{cite web | title=NSAIDs may cause rare kidney problems in unborn babies | website=U.S. Food and Drug Administration | date=2017-07-21 | url=https://www.fda.gov/drugs/drug-safety-and-availability/fda-recommends-avoiding-use-nsaids-pregnancy-20-weeks-or-later-because-they-can-result-low-amniotic | access-date=2020-10-15 | archive-date=2020-10-17 | archive-url=https://web.archive.org/web/20201017014419/https://www.fda.gov/drugs/drug-safety-and-availability/fda-recommends-avoiding-use-nsaids-pregnancy-20-weeks-or-later-because-they-can-result-low-amniotic | dead-url=no }} {{PD-notice}}</ref>


==交互作用==
==交互作用==
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==作用機轉==
==作用機轉==
多克羅克多在化學上是一種[[羧酸]]衍生物，透過抑制[[環氧合酶]] 1和 2，非選擇性阻斷前列腺素合成。前列腺素在體內充當平滑肌收縮/鬆弛和調節發炎的信使。抑制前列腺素合成可預防發炎。<ref>{{Cite web|url=https://pubchem.ncbi.nlm.nih.gov/compound/3826|title=Ketorolac| work = PubChem| publisher = National Center for Biotechnology Information, U.S. National Library of Medicine |language=en|access-date= 2020-04-18}}</ref>此藥物的抗發炎、解熱和鎮痛作用的主要機轉是透過競爭性阻斷環氧合酶（COX）來抑制前列腺素合成。多克羅克多是一種非選擇性環氧合酶抑制劑。<ref>{{cite journal | vauthors = Lee IO, Seo Y | title = The effects of intrathecal cyclooxygenase-1, cyclooxygenase-2, or nonselective inhibitors on pain behavior and spinal Fos-like immunoreactivity | journal = Anesthesia and Analgesia | volume = 106 | issue = 3 | pages = 972–7, table of contents | date = March 2008 | pmid = 18292448 | doi = 10.1213/ane.0b013e318163f602 | s2cid = 5894373 | doi-access = free }}</ref>它被認為是第一代的非類固醇抗發炎藥（NSAID）。<ref name = "Henry_2016" />{{rp|279}}
多克羅克多在化學上是一種[[羧酸]]衍生物，透過抑制[[環氧合酶]] 1和 2，非選擇性阻斷前列腺素合成。前列腺素在體內充當平滑肌收縮/鬆弛和調節發炎的信使。抑制前列腺素合成可預防發炎。<ref>{{Cite web|url=https://pubchem.ncbi.nlm.nih.gov/compound/3826|title=Ketorolac|work=PubChem|publisher=National Center for Biotechnology Information, U.S. National Library of Medicine|language=en|access-date=2020-04-18|archive-date=2020-08-13|archive-url=https://web.archive.org/web/20200813183146/https://pubchem.ncbi.nlm.nih.gov/compound/3826|dead-url=no}}</ref>此藥物的抗發炎、解熱和鎮痛作用的主要機轉是透過競爭性阻斷環氧合酶（COX）來抑制前列腺素合成。多克羅克多是一種非選擇性環氧合酶抑制劑。<ref>{{cite journal | vauthors = Lee IO, Seo Y | title = The effects of intrathecal cyclooxygenase-1, cyclooxygenase-2, or nonselective inhibitors on pain behavior and spinal Fos-like immunoreactivity | url = https://archive.org/details/sim_anesthesia-and-analgesia_2008-03_106_3/page/972 | journal = Anesthesia and Analgesia | volume = 106 | issue = 3 | pages = 972–7, table of contents | date = March 2008 | pmid = 18292448 | doi = 10.1213/ane.0b013e318163f602 | s2cid = 5894373 | doi-access = free }}</ref>它被認為是第一代的非類固醇抗發炎藥（NSAID）。<ref name = "Henry_2016" />{{rp|279}}


==歷史==
==歷史==
克多羅克多是美國唯一受廣泛使用的靜脈注射非類固醇抗發炎藥。<ref name="MartinJimenez2017"/>
克多羅克多是美國唯一受廣泛使用的靜脈注射非類固醇抗發炎藥。<ref name="MartinJimenez2017"/>


位於[[加利福尼亞州]][[帕羅奧圖]]的{{le|Syntex|Syntex}}藥廠於2006年左右開發眼科用藥Aulous（愛克樂眼藥水），<ref>{{Cite web|title=Acular (Ketorolac Tromethamine): Uses, Dosage, Side Effects, Interactions, Warning|url=https://www.rxlist.com/acular-drug.htm|access-date=2021-05-06|website=RxList|language=en}}</ref>目前由美國全球性藥品公司{{le|Allergan|Allergan, Inc.}}取得銷售授權。<ref>{{cite web | title = Label: ACULAR® Eye Drops (ketorolac trometamol) | url = https://allergan-web-cdn-prod.azureedge.net/allergan/allergannewzealand/media/allergannewzealand/products/acular-nz-cmi.pdf | date = December 2011 }}</ref><ref>{{cite web | title = Label: ACULAR® (ketorolac tromethamine ophthalmic solution) | url = https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019700s028lbl.pdf | work = Allergan, Inc. | publisher = U.S. Food and Drug Administration }}</ref>
位於[[加利福尼亞州]][[帕羅奧圖]]的{{le|Syntex|Syntex}}藥廠於2006年左右開發眼科用藥Aulous（愛克樂眼藥水），<ref>{{Cite web|title=Acular (Ketorolac Tromethamine): Uses, Dosage, Side Effects, Interactions, Warning|url=https://www.rxlist.com/acular-drug.htm|access-date=2021-05-06|website=RxList|language=en|archive-date=2024-02-24|archive-url=https://web.archive.org/web/20240224233950/https://www.rxlist.com/acular-drug.htm|dead-url=no}}</ref>目前由美國全球性藥品公司{{le|Allergan|Allergan, Inc.}}取得銷售授權。<ref>{{cite web | title = Label: ACULAR® Eye Drops (ketorolac trometamol) | url = https://allergan-web-cdn-prod.azureedge.net/allergan/allergannewzealand/media/allergannewzealand/products/acular-nz-cmi.pdf | date = December 2011 | access-date = 2024-02-07 | archive-date = 2021-09-24 | archive-url = https://web.archive.org/web/20210924221743/https://allergan-web-cdn-prod.azureedge.net/allergan/allergannewzealand/media/allergannewzealand/products/acular-nz-cmi.pdf | dead-url = no }}</ref><ref>{{cite web | title = Label: ACULAR® (ketorolac tromethamine ophthalmic solution) | url = https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019700s028lbl.pdf | work = Allergan, Inc. | publisher = U.S. Food and Drug Administration | access-date = 2024-02-07 | archive-date = 2024-04-16 | archive-url = https://web.archive.org/web/20240416185248/https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019700s028lbl.pdf | dead-url = no }}</ref>


人們於2007年因此藥物副作用發生率很高而感到擔憂。導致對使用劑量和最長使用時間予以限制。在[[英國]]，僅能在醫院開始使用此藥物，但並不排除在住院前護理和山區救援行動中使用。<ref name="researchgate.net"/>當時也發佈有使用劑量指南。<ref>{{cite journal | title = Ketoprofen and ketorolac: gastrointestinal risk | journal = MHRA Drug Safety Update | date = October 2007 | volume = 1 | issue = 3 | pages = 3–4 | publisher = Medicines and Healthcare products Regulatory Agency (MHRA) | url = https://webarchive.nationalarchives.gov.uk/ukgwa/20150110161836mp_/http://www.mhra.gov.uk/home/groups/pl-p/documents/publication/con2032519.pdf }}</ref>
人們於2007年因此藥物副作用發生率很高而感到擔憂。導致對使用劑量和最長使用時間予以限制。在[[英國]]，僅能在醫院開始使用此藥物，但並不排除在住院前護理和山區救援行動中使用。<ref name="researchgate.net"/>當時也發佈有使用劑量指南。<ref>{{cite journal | title = Ketoprofen and ketorolac: gastrointestinal risk | journal = MHRA Drug Safety Update | date = October 2007 | volume = 1 | issue = 3 | pages = 3–4 | publisher = Medicines and Healthcare products Regulatory Agency (MHRA) | url = https://webarchive.nationalarchives.gov.uk/ukgwa/20150110161836mp_/http://www.mhra.gov.uk/home/groups/pl-p/documents/publication/con2032519.pdf | access-date = 2024-02-07 | archive-date = 2023-01-26 | archive-url = https://web.archive.org/web/20230126163050/https://webarchive.nationalarchives.gov.uk/ukgwa/20150110161836mp_/http://www.mhra.gov.uk/home/groups/pl-p/documents/publication/con2032519.pdf | dead-url = no }}</ref>


由於擔心多克羅克多氨丁三醇（ketorolac trometamol，一種鹽形式（salt form，為一種化合物，由陽離子和陰離子結合而成）的多克羅克多副作用發生率高，導致其在一些國家遭到撤回（眼科製劑除外），而在其他國家，使用的劑量和最長治療持續時間已被要求減少。全世界於1990年到1993年期間有97起致命反應報告。<ref>{{cite journal | author = Committee on Safety of Medicines | title = Ketorolac: new restrictions on dose and duration of treatment. | journal = Current Problems in Pharmacovigilance | date = 1993 | volume = 19 | pages = 5–6 | url = }}</ref>
由於擔心多克羅克多氨丁三醇（ketorolac trometamol，一種鹽形式（salt form，為一種化合物，由陽離子和陰離子結合而成）的多克羅克多副作用發生率高，導致其在一些國家遭到撤回（眼科製劑除外），而在其他國家，使用的劑量和最長治療持續時間已被要求減少。全世界於1990年到1993年期間有97起致命反應報告。<ref>{{cite journal | author = Committee on Safety of Medicines | title = Ketorolac: new restrictions on dose and duration of treatment. | journal = Current Problems in Pharmacovigilance | date = 1993 | volume = 19 | pages = 5–6 | url = }}</ref>


此藥物的眼藥水配方於1992年獲得FDA批准。<ref>{{cite web|url=https://www.drugs.com/mtm/ketorolac-ophthalmic.html |title=Ketorolac ophthalmic medical facts from |publisher=Drugs.com |access-date=2013-10-06}}</ref>
此藥物的眼藥水配方於1992年獲得FDA批准。<ref>{{cite web |url=https://www.drugs.com/mtm/ketorolac-ophthalmic.html |title=Ketorolac ophthalmic medical facts from |publisher=Drugs.com |access-date=2013-10-06 |archive-date=2013-09-27 |archive-url=https://web.archive.org/web/20130927012914/http://www.drugs.com/mtm/ketorolac-ophthalmic.html |dead-url=no }}</ref>


鼻腔噴霧劑 (Sprix) 於2010年獲得FDA批准，<ref>{{cite web|url=https://www.drugs.com/sprix.html |title=Sprix Information from |publisher=Drugs.com |access-date=6 October 2013}}</ref>用於治療需要用到類阿片藥物的中度至中重度疼痛。
鼻腔噴霧劑 (Sprix) 於2010年獲得FDA批准，<ref>{{cite web |url=https://www.drugs.com/sprix.html |title=Sprix Information from |publisher=Drugs.com |access-date=6 October 2013 |archive-date=2013-09-17 |archive-url=https://web.archive.org/web/20130917105809/http://www.drugs.com/sprix.html |dead-url=no }}</ref>用於治療需要用到類阿片藥物的中度至中重度疼痛。


多克羅克多也在大學和職業運動場合中使用，報導稱會在[[國家美式足球聯盟]]和[[國家冰球聯盟]]競賽中常規使用。競技運動員，特別是從事接觸性運動的，通常被教練和/或隊友期望在受傷後繼續比賽，因此經常得依靠止痛藥協助。然而最近的研究顯示鼓勵球員在受傷狀態下比賽，往往會導致更嚴重的傷害。<ref>{{Cite magazine|url=https://www.si.com/nfl/2017/03/28/nfl-toradol-lawsuit-painkillers-nflpa-union-team-doctor-conflict-interest|title=Toradol Lawsuit: NFL Can't Outrun Legacy of Abuse| vauthors = Klemko R |magazine=Sports Illustrated|language=en-us|access-date=2020-04-18}}</ref><ref>{{cite journal | vauthors = Matava M, Brater DC, Gritter N, Heyer R, Rollins D, Schlegel T, Toto R, Yates A | display-authors = 6 | title = Recommendations of the national football league physician society task force on the use of toradol(®) ketorolac in the national football league | journal = Sports Health | volume = 4 | issue = 5 | pages = 377–383 | date = September 2012 | pmid = 23016110 | pmc = 3435943 | doi = 10.1177/1941738112457154 }}</ref>一批國家美式足球聯盟前球員於2017年對聯盟提起訴訟，指控聯盟准許球員濫用止痛藥的情事。<ref>{{Cite news| vauthors = Maese R |url=https://www.washingtonpost.com/sports/redskins/nfl-abuse-of-painkillers-and-other-drugs-described-in-court-filings/2017/03/09/be1a71d8-035a-11e7-ad5b-d22680e18d10_story.html|title=NFL abuse of painkillers and other drugs described in court filings|date=2017-03-09|newspaper=Washington Post|access-date=2020-04-18|language=en-US|issn=0190-8286}}</ref>迄2023年，此案仍在美國最高法院審理中。
多克羅克多也在大學和職業運動場合中使用，報導稱會在[[國家美式足球聯盟]]和[[國家冰球聯盟]]競賽中常規使用。競技運動員，特別是從事接觸性運動的，通常被教練和/或隊友期望在受傷後繼續比賽，因此經常得依靠止痛藥協助。然而最近的研究顯示鼓勵球員在受傷狀態下比賽，往往會導致更嚴重的傷害。<ref>{{Cite magazine|url=https://www.si.com/nfl/2017/03/28/nfl-toradol-lawsuit-painkillers-nflpa-union-team-doctor-conflict-interest|title=Toradol Lawsuit: NFL Can't Outrun Legacy of Abuse|vauthors=Klemko R|magazine=Sports Illustrated|language=en-us|access-date=2020-04-18|archive-date=2020-04-23|archive-url=https://web.archive.org/web/20200423072928/https://www.si.com/nfl/2017/03/28/nfl-toradol-lawsuit-painkillers-nflpa-union-team-doctor-conflict-interest|dead-url=no}}</ref><ref>{{cite journal | vauthors = Matava M, Brater DC, Gritter N, Heyer R, Rollins D, Schlegel T, Toto R, Yates A | display-authors = 6 | title = Recommendations of the national football league physician society task force on the use of toradol(®) ketorolac in the national football league | journal = Sports Health | volume = 4 | issue = 5 | pages = 377–383 | date = September 2012 | pmid = 23016110 | pmc = 3435943 | doi = 10.1177/1941738112457154 }}</ref>一批國家美式足球聯盟前球員於2017年對聯盟提起訴訟，指控聯盟准許球員濫用止痛藥的情事。<ref>{{Cite news|vauthors=Maese R|url=https://www.washingtonpost.com/sports/redskins/nfl-abuse-of-painkillers-and-other-drugs-described-in-court-filings/2017/03/09/be1a71d8-035a-11e7-ad5b-d22680e18d10_story.html|title=NFL abuse of painkillers and other drugs described in court filings|date=2017-03-09|newspaper=Washington Post|access-date=2020-04-18|language=en-US|issn=0190-8286|archive-date=2020-04-22|archive-url=https://web.archive.org/web/20200422190330/https://www.washingtonpost.com/sports/redskins/nfl-abuse-of-painkillers-and-other-drugs-described-in-court-filings/2017/03/09/be1a71d8-035a-11e7-ad5b-d22680e18d10_story.html|dead-url=no}}</ref>迄2023年，此案仍在美國最高法院審理中。


== 參見 ==
== 參見 ==
第131行： 第130行：
== 延伸閱讀 ==
== 延伸閱讀 ==
{{refbegin}}
{{refbegin}}
* {{cite book | title = AHFS drug information | publisher = American Society of Health-System Pharmacists | location = Bethesda, MD | year = 2011 | isbn = 9781585282609 }}
* {{cite book | title = AHFS drug information | url = https://archive.org/details/ahfsdruginformat0000unse_e1a5 | publisher = American Society of Health-System Pharmacists | location = Bethesda, MD | year = 2011 | isbn = 9781585282609 }}
* {{cite book| vauthors = Hamilton R |title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=9}}
* {{cite book| vauthors = Hamilton R |title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=9}}
* {{cite journal | vauthors = Handley DA, Cervoni P, McCray JE, McCullough JR | title = Preclinical enantioselective pharmacology of (R)- and (S)- ketorolac | journal = Journal of Clinical Pharmacology | volume = 38 | issue = 2S | pages = 25S–35S | date = February 1998 | pmid = 9549656 | doi = 10.1002/j.1552-4604.1998.tb04414.x | s2cid = 22508540 }}
* {{cite journal | vauthors = Handley DA, Cervoni P, McCray JE, McCullough JR | title = Preclinical enantioselective pharmacology of (R)- and (S)- ketorolac | journal = Journal of Clinical Pharmacology | volume = 38 | issue = 2S | pages = 25S–35S | date = February 1998 | pmid = 9549656 | doi = 10.1002/j.1552-4604.1998.tb04414.x | s2cid = 22508540 }}
* {{cite book | vauthors = Henry N | title = RN pharmacology for nursing : review module | publisher = Assessment Technologies Institute | location = Overland Park, KS | year = 2016 | isbn = 9781565335738 }}
* {{cite book | vauthors = Henry N | title = RN pharmacology for nursing : review module | url = https://archive.org/details/rnpharmacologyfo0000unse | publisher = Assessment Technologies Institute | location = Overland Park, KS | year = 2016 | isbn = 9781565335738 }}
* {{cite book | vauthors = Kizior R | title = Saunders nursing drug handbook 2017 | publisher = Elsevier | location = St. Louis, MO | year = 2017 | isbn = 9780323442916 }}<!--pp 666-669 -->
* {{cite book | vauthors = Kizior R | title = Saunders nursing drug handbook 2017 | url = https://archive.org/details/saundersnursingd0000kizi | publisher = Elsevier | location = St. Louis, MO | year = 2017 | isbn = 9780323442916 }}<!--pp 666-669 -->
{{refend}}
{{refend}}


== 外部連結 ==
== 外部連結 ==
* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/ketorolac | publisher = [[United States National Library of Medicine|U.S. National Library of Medicine]] | work = Drug Information Portal | title = Ketorolac }}
* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/ketorolac | publisher = [[United States National Library of Medicine|U.S. National Library of Medicine]] | work = Drug Information Portal | title = Ketorolac | access-date = 2024-02-07 | archive-date = 2020-06-17 | archive-url = https://web.archive.org/web/20200617074639/https://druginfo.nlm.nih.gov/drugportal/name/ketorolac | dead-url = no }}


{{模板:鎮痛藥
{{模板:鎮痛藥

2024年11月25日 (一) 20:10的最新版本

酮咯酸
臨床資料
商品名（英语：Drug nomenclature）Toradol、Acular（愛克樂眼藥水）、Sprix, 及其他
其他名稱Ketorolac tromethamine（一種鹽形式的克多羅多克）
AHFS/Drugs.comMonograph
MedlinePlusa693001
核准狀況
懷孕分級
  • 澳: C
给药途径口服給藥、舌下、肌肉注射、 靜脈注射、眼藥水及鼻腔給藥
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度80–100% (口服)，100% （靜脈注射/肌肉注射）
药物代谢肝臟
生物半衰期3.5到9.2小時（年輕成人患者）、
4.7至8.6小時（平均72歲患者）
排泄途徑腎: 91.4% (平均)
膽汁: 6.1% (平均)
识别信息
  • (±)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
CAS号74103-06-3  ☒N
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.110.314 編輯維基數據鏈接
化学信息
化学式C15H13NO3
摩尔质量255.27 g·mol−1
3D模型（JSmol（英语：JSmol））
手性外消旋體
  • O=C(c1ccc2n1CCC2C(=O)O)c3ccccc3
  • InChI=1S/C15H13NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13/h1-7,11H,8-9H2,(H,18,19) checkY
  • Key:OZWKMVRBQXNZKK-UHFFFAOYSA-N checkY

酮咯酸（INN：ketorolac）或音译克多羅多克，以商品名 Toradol、Biorolac 等等銷售，是一種用於治療疼痛的非類固醇類抗發炎藥（NSAID），属非选择性环氧合酶抑制剂[1][2]。特別用於治療中度至重度疼痛用途[3]。建議治療時間不超過六天[2]，在瑞士的建議治療時間為不超過兩天[4]。它透過口服、鼻腔、靜脈注射或肌肉注射的方式給藥，另有眼藥水的形式[2][3]。給藥後一小時內開始作用，持續時間達八小時[2]。

常見的副作用包括嗜睡、頭暈、腹痛、腫脹和噁心。[2]嚴重的副作用有上消化道出血、腎衰竭、心臟病、支氣管痙攣、心臟衰竭和過敏性休克。[2]不建議個體在懷孕後期或哺乳期間使用。[2]酮咯酸發揮作用的方式是透過阻斷環氧合酶 1和 2（COX1和COX2）而減少前列腺素產生。[2][5]

此藥物於1976年獲得專利，並於1989年獲得批准用於醫療用途。[6][2]它有非處方藥的形式出售。[3]此藥物在2020年是美國最常使用處方藥中排名第249，開立的處方箋超過100萬張。[7][8]

由於酮咯酸導致上消化道出血和腎衰竭，造成一系列死亡案例，而於1993年有德國鎮痛藥市場撤出。[9]最初此藥物引入德國時，因其副作用被認為輕很多，不會產生任何物質依賴，一次劑量有效時間達7-8小時（嗎啡只有3-4小時），而經常被誤用作疼痛治療中的類阿片藥物替代品。由於酮咯酸是一種非常有效的前列腺素抑制劑，會削弱腎臟對血管收縮相關效應而產生的防禦能力（例如失血或內源性兒茶酚胺濃度較高時）。[10]

醫療用途

[编辑]
於俄羅斯販售的酮咯酸。

酮咯酸用於短期治療中度至重度疼痛。[1]因為它可能會導致腎臟損傷，[11]:280通常施用時間不會超過五天。[12][13][14][11]:291

酮咯酸與撲熱息痛（乙醯胺酚）一起服用可有效控制新生兒疼痛，它不會像類阿片藥物那樣抑制呼吸。[15]酮咯酸也是類阿片藥物的佐劑，可增強疼痛緩解作用。它也用於治療婦女的經痛。[11]:291 此藥物也因可減輕發炎而用於治療特發性心包炎。[16]

在全身性使用時，可透過口服、舌下、肌肉注射、靜脈注射和鼻腔噴霧（英语：nasal spray）方式給藥。[12]通常的做法是先透過肌肉注射或靜脈注射，[1]繼而採口服給藥。[12][15]

酮咯酸也用作眼藥水。在眼科手術期間幫助緩解疼痛，[17]且可有效治療眼部發癢。[18]無足夠的證據顯示非類固醇抗發炎藥有助於預防黃斑水腫。[19][20]酮咯酸眼藥水也用於治療角膜刮傷而引起的疼痛。[21]

使用酮咯酸期間，臨床醫師會監測不良反應表現，經常化驗例如肝功能、出血時間（英语：bleeding time）、及尿素氮、血清肌酸酐和電解質水平，協助識別潛在的併發症。[12][13]

用藥禁忌

[编辑]

酮咯酸禁用於有過敏反應、對藥物過敏、對其他非類固醇抗發炎藥物交叉過敏、手術之前、有消化性潰瘍病史、上消化道出血、酒精不耐受、腎功能不全、腦血管出血、鼻息肉、血管性水腫和氣喘的患者。[12][13]建議患有心血管疾病、心肌梗塞、中風、心臟衰竭、凝血障礙、腎功能不全和肝功能不全的患者謹慎使用此藥物。[12][13]

不良影響

[编辑]

常見（>10%）的副作用是嗜睡。不常見（<1%）的副作用有感覺異常、出血時間延長、注射部位疼痛、紫斑、出汗、思維異常、眼淚增加、水腫、面色蒼白、口乾、味覺異常、頻尿、肝酵素升高、發癢以及其他症狀。酮咯酸會降低血小板功能。[11]:279

潛在致命的不良反應雖然不常見，但包含有中風、心肌梗塞、上消化道出血、史蒂芬斯－強森症候群、中毒性表皮壞死鬆解症（英语：toxic epidermal necrolysis）和過敏性休克。就安全性而言，酮咯酸被評估為較醋氯芬酸、塞來昔布和布洛芬（均為非類固醇抗發炎藥）具有相對較高的風險。[16]

如果個體在懷孕晚期服用酮咯酸，會導致嬰兒動脈導管過早收縮，與所有非類固醇抗發炎藥物的作用相同。[12][13]

美國食品藥物管理局 (FDA) 於2020年10月要求更新所有非類固醇抗發炎藥物的藥品標籤（英语：Drug labelling），標明這類藥物對未出生嬰兒可能會產生腎臟問題，而導致羊水過低的風險。[22][23]標籤建議孕婦在懷孕20週或之後避免使用非類固醇抗發炎藥物。[22][23]

交互作用

[编辑]

酮咯酸會與其他藥物產生交互作用。本妥昔林（英语：Probenecid）與酮咯酸一起服用會升高不良反應的可能性。與五羥色酮（英语：Pentoxifylline）一起服用會增加出血風險。與阿斯匹靈一起服用會降低療效。如果同時服用鉀補充劑、阿斯匹靈、其他非類固醇抗發炎藥、皮質類固醇或酒精，消化道問題會疊加，且更有可能發生。抗高血壓藥和利尿劑的有效性有降低可能。使用酮咯酸會使血清鋰濃度升高至中毒程度。如果同時服用酮咯酸和化療藥物和免疫抑制劑氨甲蝶呤，會增加後者毒性的風險。

服用酮咯酸，同時服用氯吡格雷、頭孢哌酮、丙戊酸、頭孢替坦（英语：cefotetan）、依替菲巴肽（英语：eptifibatide）、替羅非班（英语：tirofiban）和替洛比丁（英语：ticlopidine）時，出血風險會增加。同時服用抗凝劑和血栓溶解（英语：Thrombolysis）藥物也會增加出血的可能性。用於治療癌症的藥物會在放射治療時與酮咯酸相互作用。當酮咯酸與環孢素一起服用時，腎臟毒性的風險會增加。[12][13]

一些草藥補充劑也會與酮咯酸發生交互作用。它與高麗參、丁子香、薑、山金車、短舌匹菊、當歸、洋甘菊和銀杏一起服用會增加出血風險。[12][13]

作用機轉

[编辑]

多克羅克多在化學上是一種羧酸衍生物，透過抑制環氧合酶 1和 2，非選擇性阻斷前列腺素合成。前列腺素在體內充當平滑肌收縮/鬆弛和調節發炎的信使。抑制前列腺素合成可預防發炎。[24]此藥物的抗發炎、解熱和鎮痛作用的主要機轉是透過競爭性阻斷環氧合酶（COX）來抑制前列腺素合成。多克羅克多是一種非選擇性環氧合酶抑制劑。[25]它被認為是第一代的非類固醇抗發炎藥（NSAID）。[11]:279

歷史

[编辑]

克多羅克多是美國唯一受廣泛使用的靜脈注射非類固醇抗發炎藥。[15]

位於加利福尼亞州帕羅奧圖的Syntex（英语：Syntex）藥廠於2006年左右開發眼科用藥Aulous（愛克樂眼藥水），[26]目前由美國全球性藥品公司Allergan（英语：Allergan, Inc.）取得銷售授權。[27][28]

人們於2007年因此藥物副作用發生率很高而感到擔憂。導致對使用劑量和最長使用時間予以限制。在英國，僅能在醫院開始使用此藥物，但並不排除在住院前護理和山區救援行動中使用。[1]當時也發佈有使用劑量指南。[29]

由於擔心多克羅克多氨丁三醇（ketorolac trometamol，一種鹽形式（salt form，為一種化合物，由陽離子和陰離子結合而成）的多克羅克多副作用發生率高，導致其在一些國家遭到撤回（眼科製劑除外），而在其他國家，使用的劑量和最長治療持續時間已被要求減少。全世界於1990年到1993年期間有97起致命反應報告。[30]

此藥物的眼藥水配方於1992年獲得FDA批准。[31]

鼻腔噴霧劑 (Sprix) 於2010年獲得FDA批准，[32]用於治療需要用到類阿片藥物的中度至中重度疼痛。

多克羅克多也在大學和職業運動場合中使用，報導稱會在國家美式足球聯盟和國家冰球聯盟競賽中常規使用。競技運動員，特別是從事接觸性運動的，通常被教練和/或隊友期望在受傷後繼續比賽，因此經常得依靠止痛藥協助。然而最近的研究顯示鼓勵球員在受傷狀態下比賽，往往會導致更嚴重的傷害。[33][34]一批國家美式足球聯盟前球員於2017年對聯盟提起訴訟，指控聯盟准許球員濫用止痛藥的情事。[35]迄2023年，此案仍在美國最高法院審理中。

參見

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延伸閱讀

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外部連結

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检索自“https://zh.wikipedia.org/zhwiki/w/index.php?title=酮咯酸&oldid=85100383”