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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/12/17 13:56:24」(JST)
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| Bioavailability | 100% |
| Protein binding | 92% |
| Metabolism | Hepatic, CYP extensively involved (mainly CYP3A4) |
| Biological half-life | 22 hours |
| Excretion | Renal (70%) and fecal (20%) |
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| ECHA InfoCard | 100.207.709 |
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| Formula | C18H15ClN2O2S |
| Molar mass | 358.842 g/mol |
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Etoricoxib (Arcoxia) is a selective COX-2 inhibitor from Merck & Co. Currently it is approved in more than 80 countries worldwide but not in the US, where the Food and Drug Administration (FDA) has required additional safety and efficacy data for etoricoxib before it will issue approval.
Contents
- 1 Therapeutic indications
- 2 Mechanism of action
- 3 Adverse effects
- 4 History
- 5 Brand names
- 6 References
Therapeutic indications
Etoricoxib is indicated for the treatment of rheumatoid arthritis, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain, and gout. Approved indications differ by country.
A Cochrane systematic review assessed the benefits of single-dose etoricoxib in reduction of acute post-operative pain in adults.[1] Single-dose oral etoricoxib provides pain relief post-operatively in adults and adverse events are similar to placebo in the studies included.[1] Etoricoxib given at a dose of 120 mg is as effective or even better than other analgesics that are commonly used.[1]
Mechanism of action
Like any other selective COX-2 inhibitor ("coxib"), etoricoxib selectively inhibits isoform 2 of the enzyme cyclooxygenase (COX-2). It has approximately 106-fold selectivity for COX-2 inhibition over COX-1. This reduces the generation of prostaglandins (PGs) from arachidonic acid. Among the different functions exerted by PGs, their role in the inflammation cascade should be highlighted.
Selective COX-2 inhibitors show less activity on COX-1 compared to traditional non-steroidal anti-inflammatory drugs (NSAID). This reduced activity is the cause of reduced gastrointestinal side effects, as demonstrated in several large clinical trials performed with different coxibs.[2][3]
Adverse effects
Like all other NSAIDs the COX-2 inhibitors too have their share of adverse effects. Fixed drug eruption and generalised erythema,[4] acute generalized exanthematous pustulosis (AGEP),[5] erythema multiforme like eruption[6] and drug induced pretibial erythema[7] are some serious side effects reported, besides the usual innocuous ones.
History
Some clinical trials and meta-analysis showed that treatment with some coxibs (in particular rofecoxib) led to increased incidence of adverse cardiovascular events compared to placebo. Because of these results, some drugs were withdrawn from the market (rofecoxib, in September 2004 and valdecoxib in April 2005). In addition, the United States Food and Drug Administration and the European Medicines Agency started revision processes of the entire class of both NSAIDs and COX-2 inhibitors.[8]
In April 2007, the FDA issued Merck a "non-approvable letter" for etoricoxib. The letter said Merck needs to provide more test results showing that the drug's benefits outweigh its risks before it has another chance of getting approved.
Brand names
Brand names for etoricoxib include:
- Arcoxia in Saudi Arabia, Sweden, Finland, Norway, Estonia, Germany, Lithuania, China, Hong Kong, Ireland, Israel, Jordan, Lebanon, Brazil, Malaysia, Singapore, Thailand, Guatemala, Mexico, Bulgaria, Philippines, Ecuador, Australia, New Zealand, Romania, South Africa, Trinidad & Tobago, United Arab Emirates, United Kingdom, Ukraine, Russian Federation, Netherlands
- Turox in United Arab Emirates
- Algix, Tauxib in Italy
- Etorix, Tory, Etoxib, Vargus in Bangladesh
- Arcox (by MAQ Life Sciences), Berrica, Starcox in Pakistan
- Exxiv in Portugal
- Etozox, Etospeed, Nucoxia and Etoshine in India
- Coxit in Jordan
References
- ^ a b c Clarke R, Derry S, Moore RA; Derry; Moore (2014). "Single dose oral etoricoxib for acute postoperative pain in adults". Cochrane Database Syst Rev. 5 (5): CD004309. doi:10.1002/14651858.CD004309.pub4. PMID 24809657. CS1 maint: Multiple names: authors list (link)
- ^ Bombardier, Claire; Laine, Loren; Reicin, Alise; Shapiro, Deborah; Burgos-Vargas, Ruben; Davis, Barry; Day, Richard; Ferraz, Marcos Bosi; Hawkey, Christopher J.; Hochberg, Marc C.; Kvien, Tore K.; Schnitzer, Thomas J. (2000). "Comparison of Upper Gastrointestinal Toxicity of Rofecoxib and Naproxen in Patients with Rheumatoid Arthritis". New England Journal of Medicine. 343 (21): 1520–8, 2 p following 1528. doi:10.1056/NEJM200011233432103. PMID 11087881.
- ^ Cannon, Christopher P; Curtis, Sean P; Fitzgerald, Garret A; Krum, Henry; Kaur, Amarjot; Bolognese, James A; Reicin, Alise S; Bombardier, Claire; Weinblatt, Michael E; Van Der Heijde, Désirée; Erdmann, Erland; Laine, Loren (2006). "Cardiovascular outcomes with etoricoxib and diclofenac in patients with osteoarthritis and rheumatoid arthritis in the Multinational Etoricoxib and Diclofenac Arthritis Long-term (MEDAL) programme: A randomised comparison". The Lancet. 368 (9549): 1771–1781. doi:10.1016/S0140-6736(06)69666-9. PMID 17113426.
- ^ Augustine M, Sharma P, Stephen J, Jayaseelan E. Fixed drug eruption and generalised erythema following etoricoxib. Indian J Dermatol Venereol Leprol. 2006;72:307–9. http://www.ijdvl.com/text.asp?2006/72/4/307/26732
- ^ Makela, L; Lammintausta, K (2008). "Etoricoxib-induced acute generalized exanthematous pustulosis". Acta Derm Venereol. 88: 200–1. doi:10.2340/00015555-0381.
- ^ Thirion, L; Nikkels, AF; Piérard, GE (2008). "Etoricoxib-induced erythema-multiforme-like eruption". Dermatology. 216: 227–8. doi:10.1159/000112930.
- ^ Kumar, P (2015). "Etoricoxib-induced pretibial erythema and edema". Indian Dermatol Online J. 6: S47–9. doi:10.4103/2229-5178.171046. PMC 4738517 . PMID 26904451.
- ^ The FDA concluded its revision on April 6, 2005: the final document can be found here. The EMA concluded its revision on June 27, 2005: the final document can be found here Archived April 6, 2008, at the Wayback Machine.
Nonsteroidal anti-inflammatory drugs (NSAIDs) (primarily M01A and M02A, also N02BA)
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UpToDate Contents
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- 1. COX-2選択的阻害剤：有害な心血管系への影響 cox 2 selective inhibitors adverse cardiovascular effects
- 2. COX-2阻害剤および胃十二指腸障害：大規模臨床試験 cox 2 inhibitors and gastroduodenal toxicity major clinical trials
- 3. COX-2選択的阻害剤の概要 overview of selective cox 2 inhibitors
- 4. 非ステロイド性抗炎症剤（NSAIDs）（アスピリンを含む）：アレルギー反応および偽アレルギー反応 nsaids including aspirin allergic and pseudoallergic reactions
- 5. 急性腰痛の治療 treatment of acute low back pain
English Journal
- Gastrointestinal safety of etoricoxib in osteoarthritis and rheumatoid arthritis: A meta-analysis.
- Feng X1, Tian M1, Zhang W2, Mei H2.
- PloS one.PLoS One.2018 Jan 10;13(1):e0190798. doi: 10.1371/journal.pone.0190798. eCollection 2018.
- PMID 29320568
- Regulator of calcineurin 1 modulates vascular contractility and stiffness through the upregulation of COX-2-derived prostanoids.
- García-Redondo AB1, Esteban V2, Briones AM3, Campo LSDD4, González-Amor M4, Méndez-Barbero N5, Campanero MR6, Redondo JM7, A MS8.
- Pharmacological research.Pharmacol Res.2018 Jan 5. pii: S1043-6618(17)31245-8. doi: 10.1016/j.phrs.2018.01.001. [Epub ahead of print]
- PMID 29309904
- Primary Hypertrophic Osteoarthropathy With SLCO2A1 Mutation in a Chinese Patient Successfully Treated With Etoricoxib.
- Sun F1, Guo L, Ye S.
- Journal of clinical rheumatology : practical reports on rheumatic & musculoskeletal diseases.J Clin Rheumatol.2017 Dec 12. doi: 10.1097/RHU.0000000000000647. [Epub ahead of print]
- PMID 29239930
Related Links
- ※この商品に関係するニュース記事へのリンクがページ最下部にあります。 「有効成分」 エトリコキシブ(Etoricoxib) 「同一成分含有商品」 アルコキシア（エトリコキシブ）90mg (30錠 ) 5300 円 Arcoxia (Etoricoxib) - 90mg (30 Tablets)
- Arcoxia（アルコキシア）は、現在、欧州、中南米、アジアの54カ国で発売されてるシクロオキシゲナーゼ－2（COX-2）抑制剤と呼ばれる抗炎症剤です。 胃腸障害の副作用が少なく、大腸癌の予防やアルツハイマー病に効果が期待されて ...
Related Pictures
★リンクテーブル★
| リンク元 | 「エトリコキシブ」 |
「エトリコキシブ」
- 英
- etoricoxib
- 同
- Arcoxia, Medal
- 関
- 非ステロイド性抗炎症薬
- コキシブ系非ステロイド性抗炎症薬;COX-2選択的阻害
- 販売されていない。