NSAIDs gastrointestinal system

NSAIDs are associated with gastrointestinal, renal, hepatic, and central nervous system toxicity and may increase blood pressure. NSAIDs that are selective for the cyclooxygenase-2 (COX-2) isozyme are less likely to cause gastrointestinal complications but may increase the risk of cardiovascular events. They are no more effective than nonselective NSAIDs. Selective agents should be reserved for patients at high risk of gastrointestinal complications and low risk for cardiovascular events. 

The effectiveness of ketoprofen at dosages of 100-300 mg/d is equivalent to that of other NSAIDs. In spite of its dual effect on prostaglandins and leukotrienes, ketoprofen is not superior to other NSAIDs in clinical efficacy. Its major adverse effects are on the gastrointestinal tract and the central nervous system (see common adverse effects above). 

Relief of pain after surgery can be achieved with a variety of techniques. An epidural infusion of a mixture of local anaesthetic and opioid provides excellent pain relief after major surgery such as laparotomy. Parenteral morphine, given intermittently by a nurse or by a patient-controlled system, will also relieve moderate or severe pain but has the attendant risk of nausea, vomiting, sedation and respiratory depression. The addition of regular paracetamol and a NSAID, given orally or rectally, will provide additional pain relief and reduce the requirement for morphine. NSAIDs are contraindicated if there is a history of gastrointestinal ulceration of if renal blood flow is compromised. 

ACE-I, indicates angiotensin converting-enzyme inhibitor BP, blood pressure CNS, central nervous system GI, gastrointestinal INR, international normalization ratio K+, potassium NSAID, non-steroidal anti-inflammatory drug SSRI, selective serotonin receptor inhibitor TCA, tricyclic antidepressant. 

The NSAID dexindoprofen has a similar adverse effect pattern to the parent drug, indoprofen. Gastrointestinal, nervous system, and skin reactions are the most frequent (1). 

Indometacin is the best-known and most thoroughly tested indoleacetic acid derivative. It is one of the most effective NSAIDs, and most of its toxic and therapeutic effects appear to be due to marked inhibition of prostaglandin sjmthesis. Because of its potency, its clinical efficacy is comparable, if not superior, to any other NSAID, but for precisely the same reason its adverse effects on the gastrointestinal tract and the nervous system inevitably limit its use. However, patients who tolerate it reasonably well are naturally not anxious to exchange it for any newer drugs with fewer problems but less potency. A meta-analysis of patients preference in 37 crossover comparisons of indometacin with newer NSAIDs did not provide evidence of a trend to replace indometacin with newer NSAIDs (1). 

Lonazolac, an arylacetic acid derivative, causes adverse effects like those of other NSAIDs. Gastrointestinal disturbances are followed in frequency by nervous system and skin reactions. The extent of gastrointestinal blood loss is similar to that with diclofenac (1). Cholestatic hepatitis has also been reported (SEDA-8, 106). 

Oral pH sensitive drug delivery systems are gaining importance because they are able to deliver the drag at specific part of the gastrointestine. Antibiotics, especially macrolide ones like erythromycin, enzymes and proteins are rapidly degraded by gastric juices. Others, such as acidic drugs like NSAID s (e.g., diclofenac, valproic acid, or acetylsalicylic acid) cause a local irritation of the stomach mucosa. 

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