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Proton pump inhibitor's (PPIs)
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Mechanism
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Mechanism of action and pharmacological effect - Proton inhibitors:
(1) Acts as a pro-drug and must be activated by exposure to acidic pH (< 5). (2) The activated species irreversibly binds to the H+, K+ - ATPase enzyme (proton pump) in the parietal cell apical membrane inhibiting it’s activity. New enzyme has to be synthesized to overcome the inhibition. (3) Has little effect on gastric acid volume and does not affect gastric motility. (4) Effective in decreasing gastric acid production by more than 95%. |
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esomeprazole (Nexium ®)
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Healing of Erosive Esophagitis: 20 - 40 mg once
daily x 4 to 8 weeks. May consider an additional 4-8 weeks of treatment
if patient is not healed. Maintenance of Healing of Erosive Esophagitis: 20 mg once daily. Symptomatic Gastroesophageal Reflux Disease: 20 mg once daily x 4 weeks. May consider an additional 4 weeks of treatment if symptoms do not resolve. Treatment of GERD (short-term): 20 mg or 40 mg IV once daily for </= 10 days. Change to oral therapy as soon as appropriate. H. pylori Eradication (Triple therapy): Nexium 40 mg qd x 10 days + Amoxicillin 1000 mg bid x 10 Days + Clarithromycin 500 mg bid for 10 days. [Supplied: 20, 40mg capsules. Injection (powder for reconstitution) 20 mg, 40 mg] |
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Lansoprazole (Prevacid ® )
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GERD: 15-30mg orally once daily before meal. Hypersecretory: Maximum: 180mg/day. Duodenal ulcer: 15 mg orally once daily x 4 weeks. Maintenance therapy: 15 mg once daily. Gastric ulcer: 30 mg orally once daily for up to 8 weeks. Erosive esophagitis: -Short-term treatment: 30 mg orally once daily for up to 8 weeks. Continued treatment for an additional 8 weeks may be considered for recurrence or for patients that do not heal after the first 8 weeks of therapy. -Maintenance therapy: 15 mg once daily. Alternatively: 30 mg IV once daily for up to 7 days. Patients should be switched to an oral formulation as soon as they can take oral medications. Hypersecretory conditions: Initially 60 mg orally once daily. Adjust dose based upon patient response and to reduce acid secretion to <10 mEq/hour (5 mEq/hour in patients with prior gastric surgery). Doses of 90 mg twice daily have been used. Administer doses >120 mg/day in divided doses Prevention of rebleeding in peptic ulcer bleed (unlabeled use): 60 mg IV, followed by 6 mg/hour infusion for 72 hours. Supplied: delayed release capsule: 15 mg, 30 mg. Oral suspension: 15 mg/packet, 30 mg/packet. Injection (powder for reconstitution): 30 mg. Orally-disintegrating tablet: 15 mg, 30 mg. |
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Omeprazole (Prilosec ® )
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Usual: 20-40mg orally once daily. Hypersecretory: 60mg once daily. Active bleeding (IV formulation of PPI not available): 40 mg po bid. If there is no rebleeding within 24 hours, the patient may be switched to oral omeprazole 20 mg/day. |
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Pantoprazole (Protonix ® )
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Adult (usual): Short-term treatment erosive esophagitis: 40 mg orally once daily for 8-16 weeks. Alternatively, 40 mg IV once daily infusion for 7-10 days. Gastroesophageal reflux disease (maintain healing erosive esophagitis): 40 mg orally once daily. Hypersecretory conditions: 80 mg IV infusion every 12 hours. Can increase to every 8 hours - Max: 240 mg/day. Alternatively: 40 mg orally twice daily. Max: 240 mg/day. Peptic ulcer: 40-80 mg orally once daily x 4-8 weeks. Prevention of rebleeding in peptic ulcer bleed (unlabeled use): 80 mg IV, followed by 8 mg/hour infusion for 72 hours [Supplied: Enteric coated tablet: 20, 40mg. Lyophilized powder: 40mg vial.] |
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Rabeprazole Sodium (Aciphex ®)
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Adult ((usual): 20 mg once daily. The recommended starting oral dose for the
treatment of hypersecretory conditions is 60mg once daily (may increase
up to 120 mg). Give on empty stomach before meals. Do not chew or crush. [Supplied: 20mg tab] |
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Treatment of bleeding peptic ulcers:
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Considering the available
data, the ideal pharmacologic therapy for patients with acute ulcer
bleeding appears to be an intravenous proton pump inhibitor started
immediately after endoscopic therapy. Although eprazole has
been the most extensively studied, other intravenous formulations of
proton pump inhibitors given in doses that are known to inhibit gastric
acid secretion are probably acceptable alternatives. Pantoprazole and
lansoprazole and esomeprazole are the only intravenous formulations
available in the United States. The suggested IV pantoprazole dose is 80
mg bolus followed by 8 mg/hr infusion. If there is no rebleeding within
24 hours, the patient may be switched to oral pantoprazole 40 mg/day or
omeprazole 20 mg/day. Oral dosing: Twice daily dosing (high dose) of an oral proton pump inhibitor may be a reasonable alternative if intravenous formulations are not available. While data are limited, oral administration of a proton pump inhibitor using standard doses in the acute bleeding setting may not affect bleeding risk since it may take several days to achieve adequate acid suppression. One of the largest and most rigorously conducted controlled trials conducted in India found that a high dose of oral omeprazole (40 mg PO BID) was associated with a decreased risk of recurrent bleeding in patients who had ulcers with a visible vessel or adherent clots who did not undergo endoscopic therapy. This study suggests that the theoretical limitation of oral dosing may in part be overcome by using high doses given twice daily. Another controlled trial involving patients at high risk for rebleeding suggested that patients treated with injection therapy may also benefit from oral omeprazole. |
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Disclaimer |
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Listed dosages are for - Adult patients ONLY. PLEASE READ THE
DISCLAIMER CAREFULLY BEFORE
ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE
TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.
GlobalRPH does not directly or indirectly practice medicine or provide
medical services and therefore assumes no liability whatsoever of any
kind for the information and data accessed through the Service or for
any diagnosis or treatment made in reliance thereon. David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc. |
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