Gastrointestinal safety of NSAIDs and over-the-counter analgesics

被引:78
作者
Bjarnason, I. [1 ]
机构
[1] Kings Coll Hosp London, Dept Gastroenterol, London SE5 9RS, England
关键词
NONSTEROIDAL ANTIINFLAMMATORY DRUGS; SMALL-INTESTINAL INFLAMMATION; RHEUMATOID-ARTHRITIS; DOUBLE-BLIND; SMALL-BOWEL; BLOOD-LOSS; HIGH-RISK; IBUPROFEN; DAMAGE; COMPLICATIONS;
D O I
10.1111/ijcp.12048
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used. It is well recognised that they may adversely cause damage throughout the gastrointestinal tract and aggravate pre-existing disease. Their side effects on the upper gastrointestinal tract can be assessed by various means; each study type has different clinical connotations. Short-term use (less than 14 days) demonstrates dose-dependent damage of prescribed NSAIDs; the damage is proportional to the acidity of the drugs and not seen with Cyclooxygenase-2 (COX-2) selective inhibitors that have a pKa over 7.0. There have not been any serious outcomes, such as bleeding or perforation in these studies, and Helicobacter pylori (HP) plays no role in this damage. Long-term (3 months or more) endoscopy studies in patients show ulcer rates from 15%35% with the various NSAIDs, but serious outcomes are exceedingly rare. Epidemiological studies show an association between NSAID intake and serious events. Ibuprofen is consistently at the lower end of toxicity rankings, whereas ketorolac and azapropazone are the worst. The risk of bleeding is increased with advancing age, presence of HP, previous history of bleeding, anticoagulant use, etc. The mega-trials show that COX-2 selective agents halve the bleeding episodes, but NSAID-induced gastric bleeding is very rare usually, less than 1 in 200 subjects taking them for a year. Seventy percent of patients develop NSAID-enteropathy, which is associated with intestinal blood and protein loss and rarely strictures. Over-the-counter (OTC) use of ibuprofen and diclofenac is associated with symptomatic gastrointestinal side effects comparable with placebo. Ibuprofen is shown to be remarkably well tolerated at OTC doses in a number of studies. There are recent studies to suggest that OTC NSAIDs should be taken on a fasting stomach, not with food as commonly advocated.
引用
收藏
页码:37 / 42
页数:6
相关论文
共 38 条
  • [1] Determinants of the short-term gastric damage caused by NSAIDs in man
    Bjarnason, I.
    Scarpignato, C.
    Takeuchi, K.
    Rainsford, K. D.
    [J]. ALIMENTARY PHARMACOLOGY & THERAPEUTICS, 2007, 26 (01) : 95 - 106
  • [2] EFFECT OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS AND PROSTAGLANDINS ON THE PERMEABILITY OF THE HUMAN SMALL-INTESTINE
    BJARNASON, I
    WILLIAMS, P
    SMETHURST, P
    PETERS, TJ
    LEVI, AJ
    [J]. GUT, 1986, 27 (11) : 1292 - 1297
  • [3] CLINICOPATHOLOGICAL FEATURES OF NONSTEROIDAL ANTIINFLAMMATORY DRUG-INDUCED SMALL INTESTINAL STRICTURES
    BJARNASON, I
    PRICE, AB
    ZANELLI, G
    SMETHURST, P
    BURKE, M
    GUMPEL, JM
    LEVI, AJ
    [J]. GASTROENTEROLOGY, 1988, 94 (04) : 1070 - 1074
  • [4] BJARNASON I, 1987, LANCET, V2, P711
  • [5] SIDE-EFFECTS OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS ON THE SMALL AND LARGE-INTESTINE IN HUMANS
    BJARNASON, I
    HAYLLAR, J
    MACPHERSON, AJ
    RUSSELL, AS
    [J]. GASTROENTEROLOGY, 1993, 104 (06) : 1832 - 1847
  • [6] METRONIDAZOLE REDUCES INTESTINAL INFLAMMATION AND BLOOD-LOSS IN NONSTEROIDAL ANTIINFLAMMATORY DRUG-INDUCED ENTEROPATHY
    BJARNASON, I
    HAYLLAR, J
    SMETHURST, P
    PRICE, A
    GUMPEL, MJ
    [J]. GUT, 1992, 33 (09) : 1204 - 1208
  • [7] The murky world of the COX-2-selective agents
    Bjarnason I.
    Thjodleifsson B.
    [J]. InflammoPharmacology, 2005, 13 (4) : 381 - 393
  • [8] Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis.
    Bombardier, C
    Laine, L
    Reicin, A
    Shapiro, D
    Burgos-Vargas, R
    Davis, B
    Day, R
    Ferraz, MB
    Hawkey, CJ
    Hochberg, MC
    Kvien, TK
    Schnitzer, TJ
    Weaver, A
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 2000, 343 (21) : 1520 - 1528
  • [9] Celecoxib versus diciofenac plus omeprazole in high-risk arthritis patients: Results of a randomized double-blind trial
    Chan, FKL
    Hung, LCT
    Suen, BY
    Wong, VWS
    Hui, AJ
    Wu, JCY
    Leung, WK
    Lee, YT
    To, KF
    Chung, SCS
    Sung, JJY
    [J]. GASTROENTEROLOGY, 2004, 127 (04) : 1038 - 1043
  • [10] Celecoxib versus omeprazole and diclofenac in patients with osteoarthritis and rheumatoid arthritis (CONDOR): a randomised trial
    Chan, Francis K. L.
    Lanas, Angel
    Scheiman, James
    Berger, Manuela F.
    Nguyen, Ha
    Goldstein, Jay L.
    [J]. LANCET, 2010, 376 (9736) : 173 - 179