Celecoxib
From Ganfyd
rINN: Celecoxib
Other Names
Celebrex®
Pharmacological Information
Pharmacology Images
Web information on Celecoxib
Mechanism of Action
Predominant Cox II inhibition
Relevant Clinical Literature
UK Guidance
Regulatory Literature
Other Literature
Please read pharmacological data limitations
Other Wikis
Medpedia on Celecoxib (Less technical, good quality control)
Wikipedia on Celecoxib (Less technical, ? quality control)
Contents |
Introduction
Clinical Use
Indications
- Indicated for pain, particularly of joints, particularly caused by inflammatory arthritides.
- A number of other potential indications have been explored which can be regarded as experimental or unproved:
Administration
Oral
Clinical Issues
Safety profile now well understood
Contra-indications
- Active peptic ulceration
- Severe heart failure (hazard ratio of any use in those diagnosed to have any heart failure of death = 1.75 (1.63-1.88))[4]
Cautions and Interactions
- Cardiovascular disease
- Cerebrovascular disease
- Very similar to any other NSAID
Side effects
- Cardiovascular events in the case of celecoxib is directly related to dose and frequency of dosing level 1a[5]. Most other NSAIDs have not been studied so intensively.
Commoner important
- Upper gastro-intestinal. All NSAIDs are associated with serious gastrointestinal side effects. For non-selective NSAIDs these were most common with azapropazone and least common with Ibuprofen. Selective cyclo-oxygenase-2 inhibitors are associated with a lower risk of gastrointestinal side effects
- Dyspepsia
- Haemorrhage
- Renal failure (especially in combination with diuretics and drugs acting on angiotensin system)
- Fluid retention
Rarer Important
- Cardiovascular events. This may be related to degree of cyclo-oxygenase-2 inhibition
- Asthma
- In chronic heart failure all NSAIDS have a dose-dependent increase in risk of death and increased risk of hospitalization with some such as diclofenac and coxibs having higher hazard ratios[6]
List of NSAID side-effects - many rare
Some NSAIDs are more likely to cause these side-effects than others but they all appear to be class side-effects
- Gastro-intestinal
- Gastritis
- Duodenitis
- Duodenal ulcer
- Gastric ulcer
- Oesophagitis
- Oesophageal ulcer
- Intestinal stricture
- Haemorrhage
- Colitis
- Diarrhoea
- Nausea
- Renal
- Failure
- Fluid retention/Oedema
- Papillary necrosis
- Interstitial fibrosis
- Hypersensitivity reactions
- Asthma
- Pulmonary eosinophilia
- Rashes
- Stephen-Johnson syndrome
- Toxic epidermal necrolysis
- Photosensitivity
- Nervous system
- Headache
- Dizziness
- Vertigo
- Nervousness
- Depression
- Drowsiness
- Insomnia
- Hearing disturbances
- Tinnitus
- Aseptic meningitis
- Aggravate Parkinsonism
- Other
- Haematuria
- Hepatic damage
- Alveolitis
- Pancreatitis
Special advice
In the context of its use in so called multimodal analgesia in combination with pregabalin it has been subject to research fraud[7].
Pharmacology
Its potential for inducing apoptosis[8] has lead to active derivatives such as OSU-03012 being developed[9].
References
- ↑ Tfayli A, Yang J, Kojouri1 K, Kesserwan C, Jafari M, Ozer H. Neoadjuvant Therapy with Celecoxib to Women with Early Stage Breast Cancer. Neoplasma. 2008; 55(2):122-126.
- ↑ Koo BK, Kim YS, Park KW, Yang HM, Kwon DA, Chung JW, Hahn JY, Lee HY, Park JS, Kang HJ, Cho YS, Youn TJ, Chung WY, Chae IH, Choi DJ, Oh BH, Park YB, Kim HS. Effect of celecoxib on restenosis after coronary angioplasty with a Taxus stent (COREA-TAXUS trial): an open-label randomised controlled study. Lancet. 2007 Aug 18; 370(9587):567-74.(Link to article – subscription may be required.)
- ↑ ADAPT Research Group Lyketsos CG, Breitner JC, Green RC, Martin BK, Meinert C, Piantadosi S, Sabbagh M. Naproxen and celecoxib do not prevent AD in early results from a randomized controlled trial. Neurology. 2007 May 22; 68(21):1800-8.(Link to article – subscription may be required.)
- ↑ Gislason GH, Rasmussen JN, Abildstrom SZ, Schramm TK, Hansen ML, Fosbøl EL, Sørensen R, Folke F, Buch P, Gadsbøll N, Rasmussen S, Poulsen HE, Køber L, Madsen M, Torp-Pedersen C Increased Mortality and Cardiovascular Morbidity Associated With Use of Nonsteroidal Anti-inflammatory Drugs in Chronic Heart Failure Arch Intern Med. 2009;169(2):141-149
- ↑ Solomon SD, Wittes J, Finn PV, Fowler R, Viner J, Bertagnolli MM, Arber N, Levin B, Meinert CL, Martin B, Pater JL, Goss PE, Lance P, Obara S, Chew EY, Kim J, Arndt G, Hawk E. Cardiovascular Risk of Celecoxib in 6 Randomized Placebo-Controlled Trials. The Cross Trial Safety Analysis. Circulation. 2008 Mar 31.(Epub ahead of print) (Link to article – subscription may be required.)
- ↑ Gislason GH, Rasmussen JN, Abildstrom SZ, Schramm TK, Hansen ML, Fosbøl EL, Sørensen R, Folke F, Buch P, Gadsbøll N, Rasmussen S, Poulsen HE, Køber L, Madsen M, Torp-Pedersen C Increased Mortality and Cardiovascular Morbidity Associated With Use of Nonsteroidal Anti-inflammatory Drugs in Chronic Heart Failure Arch Intern Med. 2009;169(2):141-149
- ↑ Retraction notice Anesthesia and analgesia accessed from http://www.anesthesia-analgesia.org/ on 15.03.2009
- ↑ Andrews P, Zhao X, Allen J, Li F, Chang M. A comparison of the effectiveness of selected non-steroidal anti-inflammatory drugs and their derivatives against cancer cells in vitro. . 2007 Apr 20.(Epub ahead of print) (Link to article – subscription may be required.)
- ↑ Zhang S, Suvannasankha A, Crean CD, White VL, Johnson A, Chen CS, Farag SS. OSU-03012, a Novel Celecoxib Derivative, Is Cytotoxic to Myeloma Cells and Acts through Multiple Mechanisms. . 2007 Aug 15; 13(16):4750-4758.(Link to article – subscription may be required.)
