Oesophageal damage

If a dosage form adheres to the oesophagus, a very concentrated solution of drug is presented to an extremely small area of the mucosa and it is not surprising that oesophageal injury can occur. Repeated insult to the mucosa can result in dysphagia and even stricture formation, both of which exacerbate the original problem. Drugs which are irritant to the gastric mucosa are often given as enteric coated formulations; however, failure of these coatings may result if units lodge in the oesophagus where the pH is near 7.

Medication induced oesophageal injury was first reported in 19701, and was reviewed 198323. During the period between 1960 and 1983, 221 cases were reported due to 26 different medications, and since then there have been numerous reports in the literature24 25. Antibiotics account for half the reported cases regardless of brand, although it has been reported for numerous other drugs including emepronium bromide, theophylline, doxycycline monohydrate and bisphosphonates26. This may reflect the various proportions of drugs which are prescribed, but this has not been studied. Endoscopic surveillance in healthy volunteer studies has shown that oesophagitis is detectable in 20% of subjects taking non-steroidal anti-inflammatories (NSAIDs)27. NSAIDS are also believed to have a causative role in oesophageal stricture in patients with gastro-oesophageal reflux28.

Drugs can cause local injury by a range of mechanisms including caustic or acidic effects, hyperosmotic effect, heat production, gastro-oesophageal reflux, impaired oesophageal clearance of acid and accumulation within the basal layer of the epithelium, in addition to any specific toxic effects caused by the drug.

Plasma Acetaminophen (pig ml1)


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