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Tripotassium dicitrato bismuthate: absorption and urinary excretion of bismuth in patients with normal and impaired renal function
Author(s) -
TREIBER G.,
GLADZIWA U.,
ITTEL T. H.,
WALKER S.,
SCHWEINSBERGS F.,
KLOTZ U.
Publication year - 1991
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1111/j.1365-2036.1991.tb00518.x
Subject(s) - renal function , creatinine , medicine , urine , bismuth , urology , excretion , urinary system , endocrinology , chemistry , organic chemistry
SUMMARY We have investigated the absorption and urinary excretion of tripotassium dicitrato bismuthate during a treatment course of 4 weeks in 7 patients with normal renal function (creatinine clearance 115 ± 29 ml/min; mean ± S. D.), in 7 patients with impaired renal function (creatinine clearance = 34 ± 19 ml/min) and in 4 dialysed patients. Following the first dose of tripotassium dicitrato bismuthate (216 mg bismuth b.d.), and after 2 and 4 weeks of treatment (dialysed patients received only 108 mg/b.d.), plasma and urine concentrations of bismuth were monitored for 2 and 24 h, respectively. After stopping therapy plasma and urine concentrations of bismuth were followed for 4 and 6 weeks, respectively. In all three groups of patients small amounts of bismuth (mean values 0.26 to 0.28% of dose) were rapidly (transient mean peak concentrations between 40 and 134 μg/L) reached within about 30 to 40 min, absorbed and alasma levels demonstrated a wide intra‐ and inter‐individual variability. Absorption profiles were not altered during the treatment course; however, the trough plasma concentration of bismuth demonstrated an about 3‐ to 5‐fold accumulation (correlated to creatinine clearance) from about 5 μg/L to 15 μ/L (normal renal function) or to 20–25 μ/L (impaired renal function). Pre‐study bismuth levels could be detected within 2 to 4 weeks after stopping therapy in all subjects whereas urinary concentrations were still elevated 6 weeks after the course of treatment. Our results indicate that tripotassium dicitrato bismuthate is absorbed in very low amounts during standard therapy. However, dependent on renal function, accumulation to non‐toxic levels does occur during a course of treatment. It appears prudent to halve tripotassium dicitrato bismuthate dosage in patients with severe renal insufficiency (creatinine clearance ± 20 ml/min) to avoid any possible toxic risks. In such patients monitoring of the plasma bismuth concentration might be helpful, especially if longer or repeated treatment is anticipated.