Protection from gastrointestinal side-effects by azapropazone by its incorporation into a glucose-sodium acid citrate formulation.
Addition of glucose and sodium citrate to azapropazone, in proportions of 1:1:1 by weight reduced gastric mucosal damage in rats and there was a trend towards reduction in radiolabelled faecal red cell loss in human volunteers compared with that with azapropazone alone. The glucose and citrate did not affect the pharmacokinetics of azapropazone, or its therapeutic efficacy. While no difference was observed in endoscopic injury and in symptomatic gastrointestinal complaints in a multicentre comparison in rheumatic patients, a striking reduction in symptoms was observed in those patients with a history of severe gastrointestinal intolerance to non-steroidal anti-inflammatory drugs.
Rainsford
K D
KD
Department of Biomedical Sciences, McMaster University, Faculty of Health Sciences, Hamilton, Ontario, Canada.
Dieppe
P A
PA
Pritchard
M H
MH
Rhodes
J
J
Leach
H
H
Russell
R I
RI
Walker
F S
FS
Upadhyay
R
R
Hort
J F
JF
D000293:Adolescent; D000328:Adult; D000368:Aged; D000818:Animals; D001032:Apazone / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D002951:Citrates / Q000008:administration & dosage / Q000627:therapeutic use*; D019343:Citric Acid; D016099:Endoscopy, Gastrointestinal; D005260:Female; D005753:Gastric Mucosa / Q000473:pathology; D005947:Glucose / Q000008:administration & dosage / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D008875:Middle Aged; D010437:Peptic Ulcer / Q000139:chemically induced / Q000517:prevention & control*; D051381:Rats; D011919:Rats, Inbred Strains; D016037:Single-Blind Method
D002951:Citrates; D019343:Citric Acid; D005947:Glucose; D001032:Apazone