Korean J Gastroenterol.  1998 Nov;32(5):611-618.

Pharmacokinetics of Ranitidine in Patients with Liver Cirrhosis

• Chin YJ
• Earm JH
• Youn SJ
• Lee DH
• Jang IJ
• Sin SG

Abstract

BACKGROUND/AIMS: Approximately 50% of ranitidine is eliminated by hepatic metabolism, but the pharmacokinetics of ranitidine in patients with liver cirrhosis (LC) are poorly documented. This study was conducted to investigate the pharmacokinetic changes of ranitidine in patients with LC and to evaluate the possible contribution of the kinetic changes to the adverse CNS (central nercous system) effects of ranitiidine in patients with liver disease.
METHODS
The pharmacokinetics of single-dose ranitidine were studied in 12 patients with LC and 8 controls. After 150 mg of ranitidine was given by mouth, blood samples were collected at 1, 2, 3, 4, 5, 6, 8, 12 hours, and urine was also collected for 12 hours, Serum and urine concentrations of ranitidine were determined by HPLC method and the nizatidine was used as internal standard.
RESULTS
In patients with LC, AUC (area under curve) was significantly increased (p<0.05) and total clearance rate was significantly decreased (p<0.05). Renal clearance was significantly decreased (p<0.05) and half-life was significantly prolonged (p<0.05). Effective serum concentration was maintained more prolongedly.
CONCLUSIONS
These pharmacokinetic changes which were attributed to increase of bioavailability and decrease of renal clearance, may contribute partly to the adverse CNS reactions of ranitidine in patients with hepatic dysfunction. Therefore, the adjustment of ranitidine dose should be considered in patients with severe hepatic dysfunction.

Keyword

Ranitidine; Phaemacokinetics; Liver cirrhosis; Central nervous sustem; Adverse reaction

MeSH Terms

Area Under Curve
Biological Availability
Chromatography, High Pressure Liquid
Half-Life
Humans
Liver Cirrhosis*
Liver Diseases
Liver*
Metabolism
Mouth
Nizatidine
Pharmacokinetics*
Ranitidine*
Nizatidine
Ranitidine