Acemetacin in Acute and Chronic Pain Management

Authors

  • Barkin Berk Department of Pharmaceutical Chemistry, School of Pharmacy, Altinbas University, Turkey

Abstract

Acemetacin is the carboxymethyl ester of indomethacin and is a pro-drug precursor compound, in other words, a prodrug. The pharmacologically active metabolite of acemetacin is also indomethacin. Acemetacin exerts its potent non-steroidal anti-inflammatory effects in the body as indomethacin. It is known that acemetacin is not only a prodrug of indomethacin, but also an agent with gastric protective mechanisms, possibly involving a reduction in leukocyte adhesion, and that acemetacin exerts gastric protective effects by exhibiting less efficacy on the COX-1 enzyme in the gastric mucosa compared to direct indomethacin use. It is clear that acemetacin is a valuable NSAID for acute and chronic pain.

Keywords: Acemetacin, indomethacin, non-steroidal anti-inflammatory drugs.

Keywords:

Acemetacin, indomethacin, non-steroidal anti-inflammatory drugs

DOI

https://doi.org/10.22270/jddt.v13i6.5834

Author Biography

Barkin Berk, Department of Pharmaceutical Chemistry, School of Pharmacy, Altinbas University, Turkey

Department of Pharmaceutical Chemistry, School of Pharmacy, Altinbas University, Turkey

References

Wada Y, Nakamura M, Kogo H, Aizawa Y: Inhibitory effect of acemetacin, a prodrug of indomethacin, on prostaglandin E2 release from inflamed synovial tissue. Jpn J Pharmacol. 1984 Apr; 34(4):468-70. (PubMed ID 6587139) https://doi.org/10.1016/S0021-5198(19)52303-4

https://titck.gov.tr/storage/Archive/2023/kubKtAttachments/TTCKOnaylKBACETUDL_7af02bcd-24d9-46ae-ab1f-6b28176f7ca6.pdf.(son erişim tarihi 10.05.2023)

Chou CT, Tsai YY. A double-blind, randomized, controlled parallel group study avaluating the efficacy and safety of acemetacin fort he management of osteoarthritis. Int J Clin Pharm Res 2002; 12:1-6. 2.

Acton A. (2011). Issues in Pharmacology, Pharmacy, Drug Research and Drug Innovation . ScholarlyEditions.

Sneader W. (2005). Drug discovery a history. Wiley https://doi.org/10.1002/0470015535

Chávez-Piña AE, McKnight W, Dicay M, Castañeda-Hernández G, Wallace JL. Mechanism underlying the anti-inflammatory activity and gastric safety of acemetacin. Br J Pharmacol 2007; 152(6):930-38. https://doi.org/10.1038/sj.bjp.0707451

Chávez-Piña AE, Vong L, McKnight W, Dicay M, Zanardo RC, Ortiz MI, Castañeda-Hernández G, Wallace JL. Lack of effects of acemetacin on signalling pathways for leukocyte adherence may explain its gastrointestinal safety. Br J Pharmacol. 2008 Nov; 155(6):857-64. Epub 2008 Aug 11. PMID: 18695646; PMCID: PMC2597236. https://doi.org/10.1038/bjp.2008.316

Şaş S, Kocak F, Kurt E, Tuncay F, Erdem H. Bilateral Transient Osteoporosis of the Hip: Case Report. J PMR Sci 2017; 20(2)

Şaş S, Erdem H.R, Tuncay F, Tokmak T.T. Os Trigonum Syndrome: Two Case Reports Focusing On Possible Risk Factors. Dicle Medical Journal. 2016; 43 (3):468-471. doi: https://doi.org/10.5798/diclemedj.0921.2016.03.0714

Şaş S, Kocak, F. Rehabilitation Outcomes of Painful Bipartite Patella Accompanying Spina Bifida Occulta: Two Case Reports. İzmir Kâtip Çelebi Üniversitesi Sağlık Bilimleri Fakültesi Dergisi 2018; 3(1):47-50

Ahi E.D., Özen S., Coşar S.N.S. Idiopathic Axillary Web Syndrome: A Case Report on a Rare Entity J PMR Sci. 2022; 25(1):119-22 https://doi.org/10.31609/jpmrs.2021-82996

Batmaz I., Sarıyıldız M.A., Dilek B., Ulu M.A., Verim S., Budulgan M., Çevık R. A Case of Spondyloepiphyseal Dysplasia Tarda Coexisting With Osteoporosis and Mimicking Spondyloarthropathy Turk J Phys Med Rehab 2013; 59:260-3

Eceviz E., Çevik H.B., Baysal Ö., Bulut G., Gülabi D., Çeçen G.S., Foot pain frequently associated with vitamin D deficiency: Bone Marrow Edema syndrome Medeniyet Medical Journal 2018; 33(4):263-268 https://doi.org/10.5222/MMJ.2018.11298

Güney A., Saka T., Uluöz M., Akkurt S., Karaoğlu S. Knee injuries in atletes. Turkiye Klinikleri J Orthop & Traumatol-Special Topics 2010; 3(1)

Saul PA, Korlipara K. Acemetacin and indomethacin in the treatment of rheumatoid arthritis: a double-blind comparative study in general practice. Curr Med Res Opin. 1991; 12(5):332-41. PMID: 2004546. https://doi.org/10.1185/03007999109112669

Siegmeth W, Bröll H, Schragl F. Acemetacin in der Behandlung schmerzhafter Arthrosen. Ergebnisse einer offenen Kurzzeitstudie über den Zeitpunkt des analgetischen Wirkungs- eintrittes und dessen Dauer [Acemetacin in the treatment of painful arthroses. Results of an open short-term study on the starting point of the analgesic effect and its duration]. Wien Med Wochenschr. 1984 Nov 30; 134(22):505-8. German. PMID: 6531936.

Valtonen EJ, Busson M. A comparative study on ibuprofen (Brufen) and indomethacin in non-articular rheumatism. Scand J Rheumatol.1978; 7(3):183-187 https://doi.org/10.3109/03009747809095651

Gookin KS, Forman ES, Vecchio TJ, Wiser WL, Morrison JC. Comparative efficacy of ibuprofen, indomethacin, and placebo in the treatment of primary dysmenorrhea. South Med J. 1983; 76(11):1361-1362, 1367. https://doi.org/10.1097/00007611-198311000-00008

Videman T, Osterman K. Double-blind parallel study of piroxicam versus indomethacin in the treatment of low back pain. Ann Clin Res. 1984; 16(3):156-160.

Moore RA, Derry S, Mason L, McQuay HJ, Edwards J. Single dose oral indometacin for the treatment of acute postoperative pain. Cochrane Database of Systematic Reviews 2004; 4. Art. No.: CD004308. https://doi.org/10.1002/14651858.CD004308.pub2

Kikui S, Sugiyama H, Miyahara J, Ota K, Danno D, Kashiwaya Y, Takeshima T. [Acemetacin, a Prodrug of Indomethacin, Is Effective for Treatment of Hemicrania Continua: A Japanese Case Report]. Brain Nerve. 2022 Oct; 74(10):1215-1219. Japanese. https://doi.org/10.11477/mf.1416202213 . PMID: 36198648.

Bemanalizadeh M, Baghaei Oskouei H, Hadizadeh A, Dakkali MS, Qahremani R, Mansouri V. Paroxysmal hemicrania in children and adolescents: A systematic review. Headache. 2022; 62(8):952-966. Epub 2022 Jul 14. PMID: 35833494. https://doi.org/10.1111/head.14354

Newman LC. Effective management of ice pick pains, SUNCT, and episodic and chronic paroxysmal hemicrania. Curr Pain Headache Rep 2001; 5:292-9. https://doi.org/10.1007/s11916-001-0046-6

Fuh JL, Kuo KH, Wang SJ. Primary stabbing headache in a headache clinic. Cephalalgia 2007; 27:1005-9. https://doi.org/10.1111/j.1468-2982.2007.01365.x

Dodick DW. Indomethacin-responsive headaches syndromes. Curr Pain Headache Rep 2004; 8:19-26. https://doi.org/10.1007/s11916-004-0036-6

Headache Classification Comittee of the International Headache Society (IHS). The International Classification of Headache Disorders. 3th edition (beta version). Cephalalgia 2013; 33(9):749-57.

https://doi.org/10.1177/0333102413485658

Cutrer FM, De Lange J. Cough, Exercise, and Sex Headaches. Neurol Clin 2014; 32:433-50. https://doi.org/10.1016/j.ncl.2013.11.012

Wang SJ & Fuh JL. The "Other" Headaches: Primary Cough, Exertion, Sex, and Primary Stabbing Headaches. Curr Pain Headache Rep 2010; 14:41-6. https://doi.org/10.1007/s11916-009-0083-0

Akyol A, Yeter Amasyalı S, Şair A, Özkul A. Headache Assocıated Wıth Sexual Actıvıty: A Current Overvıew Accompanıed By Cases. Turkish Journal of Cerebrovascular Diseases 2017; 23(2): 62-67. https://doi.org/10.5505/tbdhd.2017.92063

Cutrer FM, DeLange J. Cough, Exercise, and Sex Headaches. Neurol Clin 2014; 32:433- 50. https://doi.org/10.1016/j.ncl.2013.11.012

Frese A, Rahmann A, Gregor N, Biehl K, Husstedt IW, Evers S. Headache associated with sexual activity: prognosis and treatment options. Cephalalgia 2007; 27:1265-70. https://doi.org/10.1111/j.1468-2982.2007.01449.x

Mathew NT. Indomethacin responsive headache syndromes. Headache 1981; 21:147-50. 16. https://doi.org/10.1111/j.1526-4610.1981.hed2104147.x

Cutrer FM, Boes CJ. Cough, exertional, and sex headaches. In: Evans RW, ed. Neurologic Clinics North America. Secondary Headache Disorders, vol.22: Elsevier: Saunders Publishers; 2004. p.133-49. https://doi.org/10.1016/S0733-8619(03)00092-6

Diamond S. Prolonged exertional headache: its clinical characteristics and response to indomethacin. Headache 1982; 22:96-8. https://doi.org/10.1111/j.1526-4610.1982.hed2203096.x

Slavik RS, Rhoney DH. Indomethacin: A review of its cerebral blood flow effects and potential use for controlling intracranial pressure in traumatic brain injury patients. Neurol Res 1999; 21:491-9. https://doi.org/10.1080/01616412.1999.11740964

Lanteri-Minet M. Hypnic headache.Headache 2014; 54(9):1556-9. https://doi.org/10.1111/head.12447

Liang JF, Wang SJ. Hypnic headache: a review of clinical features, therapeutic options and outcomes. Cephalalgia 2014; 34(10):795- 805. https://doi.org/10.1177/0333102414537914

Sözütek A., Deniz V. Postoperative Analgesia Turkiye Klinikleri J Gen Surg-Special Topics 2012; 5(1):100-3

Neugirg R, Penners R. Klinische Prüfung von Acemetacin bei Kindern und Jugendlichen [Clinical trials with acemetacin on children and adolescents (author's transl)]. Arzneimittelforschung. 1980; 30(8A):1451-4. German. PMID: 7191316.

Eti E, Özden İ, Sazak Öveçoğlu H. Postoperatif ağrı. Ersev H, editör. Endodontide Acil Durumların Yönetimi. 1. Baskı. Ankara: Türkiye Klinikleri; 2022. p.32-9.

Eder A, Watzek G. Treatment of a patient with severe osteoporosis and chronic polyarthritis with fixed implant-supported prosthesis: a case report. Int J Oral Maxillofac Implants. 1999 Jul-Aug; 14(4):587-90. PMID: 10453676

Published

2023-06-04
Statistics
Abstract Display: 775
PDF Downloads: 645
PDF Downloads: 158

How to Cite

1.
Berk B. Acemetacin in Acute and Chronic Pain Management. J. Drug Delivery Ther. [Internet]. 2023 Jun. 4 [cited 2026 Jan. 21];13(6):18-22. Available from: https://jddtonline.info/index.php/jddt/article/view/5834

How to Cite

1.
Berk B. Acemetacin in Acute and Chronic Pain Management. J. Drug Delivery Ther. [Internet]. 2023 Jun. 4 [cited 2026 Jan. 21];13(6):18-22. Available from: https://jddtonline.info/index.php/jddt/article/view/5834