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Carbenoxolone: A Review of its Pharmacological Properties and Therapeutic Efficacy in Peptic Ulcer Disease

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Summary

Synopsis: Carbenoxolone sodium1 has been shown to accelerate the rate of healing of both gastric and duodenal ulcers, but its overall value in duodenal ulcer is probably less because of the high rate of natural remission of duodenal ulcers. Further studies are required to decide whether it should be used prophytactically to delay ulcer recurrence. Carbenoxolone may act by affecting both the proliferative activity of gastric epithelium and the differentiation of the epithelial cells to produce mucus (as well as favourably altering the physicochemical properties of mucus and by reducing peptic activity), factors which may be relevant to the prevention of acute gastric ulcers.

Some studies suggest that carbenoxolone adds to the effect of hospitalisation and bed rest on ulcer healing. Whether bed rest confers additional benefit to the drug’s ulcer healing effect in outpatients is also uncertain. There is no evidence that accelerated healing by carbenoxolone is associated with improved overall prognosis. Carbenoxolone is of greatest benefit in accelerating the healing of gastric ulcers in patients for whom hospitalisation is not possible or desirable, but it should only be used in the ambulatory patient when careful and regular observation of serum electrolytes (particularly potassium), blood pressure and weight is possible and when it is known that the patient will attend regular follow-up. Patients must be educated in the proper use of the drug. If severe mineralocorticoid-like toxic effects such as sodium and water retention and hypokalaemia appear, as they do in a variable proportion of patients but most frequently in those receiving excessive doses, carbenoxolone should be stopped and the complication treated; they respond to thiazide diuretics and potassium supplements, and probably to amiloride given in conjunction with a low dose of a thiazide diuretic. Treatment with carbenoxolone can continue with concurrent diuretic therapy in patients with less severe side-effects.

Optimum therapeutic effect in gastric ulcer with the least side-effects is achieved with a dosage of 100mg carbenoxolone tablets 3 times daily for the first week followed by 50mg 3 times daily thereafter, best taken before meals. A lower dosage is desirable in the elderly and in those with liver, cardiac or renal disease. Barium meal or preferably endoscopic examinations should be performed regularly and therapy continued until the ulcer is healed. Dosage for duodenal ulcer is 50mg 4 times daily, in special positioned-release capsules. These are best taken about 20 minutes before meals.

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    R. M. Pinder, R. N. Brogden, Phyllis R. Sawyer, T. M. Speight, Rosalind Spencer & G. S. Avery

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Various sections of the manuscript reviewed by: F. Avery Jones, Harley Street, London, England; S. Bank, Head, Gastrointestinal Clinic, Groote Schuur Hospital, Observatory, Cape, South Africa; J.H. Baron, Department of Surgery, Royal Postgraduate Medical School, Hammersmith Hospital, London, England; D. Birnbaum, Head, Gastroenterological Service, Hadassah University Hospital, Jerusalem, Israel; C.J. Edmonds, MRC Clinical Research Centre, Northwick Park Hospital, Harrow, Middlesex, England; W.P. Fung, Royal Perth Hospital, Perth, Australia; B.I. Hirschowitz, Professor and Director, Division of Gastroenterology, Department of Medicine, University of Alabama Medical Centre, Birmingham, Alabama, USA; M. Ishikawa, Tohoku University School of Medicine, Sendai, Japan; M.J.S. Langman, Professor of Therapeutics, University of Nottingham, City Hospital, Nottingham, England; D. V. Parke, Professor of Biochemistry, University of Surrey, Guildford, Surrey, England; D.W. Piper, Professor of Medicine, Royal North Shore Hospital of Sydney, St. Leonards, New South Wales, Austral ia; W. Sircus, Gastrointestinal Unit, Western General Hospital, Edinburgh, Scotland; F.M. Sullivan, Department of Pharmacology, Guy’s Hospital Medical School, London, England; G.M. Wilson, Regius Professor of the Practice of Medicine, Gardiner Institute, Western Infirmary, Glasgow, Scotland; J. Wolf, Chief of Staff, Veterans Administration Hospital, Bronx, New York, USA.

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Pinder, R.M., Brogden, R.N., Sawyer, P.R. et al. Carbenoxolone: A Review of its Pharmacological Properties and Therapeutic Efficacy in Peptic Ulcer Disease. Drugs 11, 245–307 (1976). https://doi.org/10.2165/00003495-197611040-00002

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