Clarinex - Clinical Pharmacology

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Renally Impaired:

Desloratadine pharmacokinetics following a single dose of 7.5 mg were characterized in patients with mild (n= 7; creatinine clearance 51-69 mL/ min/ 1.73 m 2 ), moderate (n= 6; creatinine clearance 34-43 mL/ min/ 1.73 m 2 ), and severe (n= 6; creatinine clearance 5-29 mL/ min/ 1.73 m 2 ) renal impairment or hemodialysis dependent (n= 6) patients. In patients with mild and moderate renal impairment, median Cmax and AUC values increased by approximately 1.2-and 1.9-fold, respectively, relative to subjects with normal renal function.

In patients with severe renal impairment or who were hemodialysis dependent, Cmax and AUC values increased by approximately 1.7-and 2.5-fold, respectively. Minimal changes in 3-hydroxydesloratadine concentrations were observed. Desloratadine and 3-hydroxydesloratadine were poorly removed by hemo-dialysis.

Plasma protein binding of desloratadine and 3-hydroxydesloratadine was unaltered by renal impairment. Dosage adjustment for patients with renal impairment is recommended (see DOSAGE AND ADMINISTRATION section).

Hepatically Impaired:

Desloratadine pharmacokinetics were characterized following a single oral dose in patients with mild (n= 4), moderate (n= 4), and severe (n= 4) hepatic impairment as defined by the Child-Pugh classification of hepatic function and 8 subjects with normal hepatic function.

Patients with hepatic impairment, regardless of severity, had approximately a 2.4-fold increase in AUC as compared with normal subjects. The apparent oral clearance of desloratadine in patients with mild, moderate, and severe hepatic impairment was 37%, 36%, and 28% of that in normal subjects, respectively. An increase in the mean elimination half-life of desloratadine in patients with hepatic impairment was observed. For 3-hydroxydesloratadine, the mean Cmax and AUC values for patients with hepatic impairment were not statistically significantly different from subjects with normal hepatic function. Dosage adjustment for patients with hepatic impairment is recommended (see