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Pharmacokinetic properties of proton pump inhibitors in adults

Pharmacokinetic properties of proton pump inhibitors in adults
Agent Regimen tested Oral bioavailability Time to peak
(hours)		 Cmax
(micrograms/mL)		 AUC0-24
(mg•h/L)		 Metabolism and clearance Half-life
(hours)*		 pKa
Dexlansoprazole 30 mg once daily Absorbed to a similar extent under fasting and fed conditions

1-2 (peak 1)

4-5 (peak 2)		 0.7 3.3 Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces 1-2 Not available
Esomeprazole 20 mg once daily

64% (single dose);

90% (after multiple doses if taken on an empty stomach; bioavailability is reduced by ~50% if taken with food)		 1-1.6 2.1 (micromol/L) 4.2 (micromol•h/L) Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces 1.2-2.5 4.0
Lansoprazole 30 mg once daily 85% (taken on an empty stomach; absorption is reduced by ~50% if taken with food) 1.5-3 0.5-1.0 3.2 Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in feces via bile and in urine 0.9-1.5 4.0
Omeprazole 20 mg once daily (delayed release capsule)

45% (single dose)

Varies by formulation; absorption is significantly increased after multiple doses		 0.5-3.5 0.7 3.3 Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and bile 0.5-3 4.0
Pantoprazole 40 mg once daily 77% 2-2.5 2.5 5.0 Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces via bile 1 (increased to 3.5-10 hours in CYP2C19 poor-metabolizers) 3.9
Rabeprazole 20 mg once daily 52% 2-5 0.4-0.48 0.9 Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces via bile 1-2 5.0
AUC0-24: cumulative systemic drug exposure as measured by the area under the plasma concentration versus time curve over 24 hours; Cmax: maximum plasma concentration; pKa: acid dissociation constant transformed by negative log; PPI: proton pump inhibitor.
* Duration of antisecretory effect of PPIs exceeds that predicted by drug half-life due to irreversible binding at site of action (ie, parietal proton pumps).
¶ PPIs are converted to their active form (ie, protonated) when pH of parietal cell is lower than pKa of the individual PPI (ie, in presence of gastric acidity). For detail, refer to accompanying text.
Δ Drug metabolism via hepatic CYP2C19 enzymes is polymorphic; thus, PPI systemic exposure (AUC0-24) can be increased several (ie, 2 to 12) times in patients who are intermediate or poor-metabolizers compared with those who are extensive-metabolizers (ie, most patients). 15-20% of persons of Asian descent are CYP2C19 poor-metabolizer phenotypes.
Prepared with data from: United States prescribing information available at US National Library of Medicine DailyMed website (https://dailymed.nlm.nih.gov/dailymed/index.cfm).
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