PROTON
PUMP INHIBITORS
Table
1: Doses and bioavailability of different PPIs [1]
Proton pump inhibitors (PPIs)
|
Doses recommended (mg)
|
Bioavailability (%)
|
|
Gastroduodenal ulcers*
|
Gastroesophageal Reflux Disease
(GERD)*
|
||
Dexlansoprazole
|
30 – 60
|
30 (OD – BD)
|
-
|
Esomeprazole
|
20 - 40
|
20 or 40 (OD)
|
64
|
Lansoprazole
|
15 – 30
|
30 (OD – BD)
|
85
|
Omeprazole
|
20 – 40
|
20 – 40 (OD – BD)
|
45
|
Pantoprazole
|
20 – 40
|
40 (OD – BD)
|
64
|
Rabeprazole
|
20
|
20 (OD – BD)
|
52
|
* TREAT GASTRODUODENAL ULCERS
X 4/52; TREAT GASTRIC ULCERS X 8/52
Table
2: Studies comparing different PPIs
Authors (year)
|
Title
|
Conclusion(s)
|
Klok RM et al. (2003) [2]
|
Meta analysis: comparing the efficacy
of PPIs in short term use
|
The significant difference may be
dose-dependent and not PPI-specific.
|
Edwards SJ et al. (2008) [3]
|
Systematic review of PPIs for the
acute treatment of reflux oesophagitis.
|
Esomeprazole has higher healing rates
than Omeprazole at week 4 and 8.
|
Pantoflickova et al. (2003) [4]
|
Acid inhibition on the first day of
dosing: comparison of 4 PPIs
|
Rabeprazole is the most potent acid
inhibitor during the first day of dosing.
|
Li XQ et al. (2004) [5]
|
Comparison of inhibitory effects of
the PPIs Omeprazole, Esomeprazole, Lansoprazole, Pantoprazole and Rabeprazole
on human CYP450 activity.
|
-Lansoprazole and Pantoprazole are the
most potent in-vitro inhibitors of CYP450.
-Esomeprazole has less inhibitory
potency than Omeprazole.
-Rabeprazole had lower inhibitory
potency than other PPIs.
|
Stedman CAM et al. (2001) [6]
|
Review article: comparison of the
pharmacokinetics, acid suppression and efficacy of PPIs
|
-Omeprazole increases in
bioavailability with repeated administrations.
-No significant interactions have been
reported for Pantoprazole as it has minimum CYP450 inhibition.
-Omeprazole and Lansoprazole showed more
drug interactions.
-Rabeprazole showed better acid
suppression than Omeprazole.
-Lansoprazole and Rabeprazole showed a
more rapid onset of maximal acid suppression than other PPIs.
-Lansoprazole showed earlier symptom
relief from oesophagitis and more rapid healing of duodenal ulcers.
-For peptic ulcer disease Rabeprazole
was more superior to Omeprazole.
|
H. pylori eradication rates were found to be of similar trends when different
proton pump inhibitors were used in triple therapy regimens. [6]
The studies in Table 2 show that
most PPIs are similar in its end point effect. It’s up to the physicians and pharmacists’
discretion to choose based on their preferences with regards to which type of
treatment they wish to target for which patient and at the same time to keep in
mind cost benefit ratio when treating.
References:
1. Adapted from: Wolfe MM, Sachs G. Acid suppression: Optimizing therapy for gastroduodenal ulcer healing, gastroesophageal reflux disease, and stress-related erosive syndrome. Gasteroenterology 2000; 118: S9.
2. Klok RM, et al. Meta analysis:
comparing the efficacy of PPIs in short term use. Aliment Pharmacol Ther. 2003;
17 (10): 1237-45.
3. Edwards
SJ et al. Systematic review of PPIs for the acute treatment of reflux
oesophagitis. Aliment Pharmacol Ther.
2008; 15(11): 1729-36.
4. Pantoflickova
et al. Acid inhibition on the first day of dosing: comparison of 4 PPIs. Aliment
Pharmacol Ther. 2003; 17 (12): 1507-14.
5. Li
XQ et al. Comparison of inhibitory effects of the PPIs Omeprazole,
Esomeprazole, Lansoprazole, Pantoprazole and Rabeprazole on human CYP450
activity. Aliment Pharmacol Ther. 2004; 32(8): 821-7.
6. Stedman CAM et al. Review article:
comparison of the pharmacokinetics, acid suppression and efficacy of PPIs. Aliment
Pharmacol Ther. 2000; 14(8): 963-78.
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