TABLE 2

Pharmacokinetic variables of clopidogrel, clopidogrel active cis-5-thiol metabolite, clopidogrel carboxylic acid, clopidogrel acyl-β-d-glucuronide, gemfibrozil, and gemfibrozil 1-O-glucuronide in 11 healthy volunteers after clopidogrel 300 mg or gemfibrozil 600 mg (fifth dose of twice daily dosing) ingested 1 hour before desloratadine 5 mg.

Data are given as median with range.

VariableClopidogrel or Gemfibrozil Phase
Clopidogrel
Cmax (ng/ml)2.88 (0.48–23.2)
tmax (h)1.5 (0.92–2.0)
t1/2 (h)3.4 (2.6–10)
 AUC0–12 h (ng × h/ml)11.7 (2.22–40.0)
Clopidogrel active metabolite
Cmax (ng/ml)23.2 (11.0–41.2)
tmax (h)0.92 (0.92–1.5)
t1/2 (h)1.8 (1.3–3.9)
 AUC0–12 h (ng × h/ml)34.6 (16.3–66.0)
Clopidogrel carboxylic acid
Cmax (ng/ml)9850 (7020–15,800)
tmax (h)1.5 (0.92–1.5)
t1/2 (h)4.2 (3.1–8.0)
 AUC0–12 h (ng × h/ml)35,400 (38,900–92,100)
Clopidogrel acyl-d-glucuronide
Cmax (ng/ml)3980 (1750–7390)
tmax (h)2.0 (1.5–3.0)
t1/2 (h)3.3 (2.7–4.0)
 AUC0–12 h (ng × h/ml)14,400 (10,900–35,800)
Gemfibrozil
Cmax (μg/ml)18.1 (14.3–29.1)
tmax (h)2.0 (1.5–4.0)
t1/2 (h)2.3 (1.7–2.7)
 AUC0–12 h (μg × h/ml)75.7 (56.5–130)
Gemfibrozil 1-O-glucuronide
Cmax (μg/ml)14.5 (10.2–20.3)
tmax (h)3.0 (1.5–6.0)
t1/2 (h)2.5 (1.7–3.4)
 AUC0–12 h (μg × h/ml)80.0 (46.2–147)