Proton pump inhibitors formulations

Drugs that may affect atazanavir include the following antacids and buffered medications, clarithromycin, didanosine (buffered formulation only), efavirenz, H2-receptor antagonists, indinavir, itraconazole, ketoconazole, nevirapine, proton pump inhibitors, rifampin, ritonavir, St. John s wort, tenofovir, voriconazole. 

Five proton pump inhibitors are available for clinical use omeprazole, lansoprazole, rabeprazole, pantoprazole, and esomeprazole. All are substituted benzimidazoles that resemble H 2 antagonists in structure (Figure 62-3) but have a completely different mechanism of action. Omeprazole is a racemic mixture of R- and S-isomers. Esomeprazole is the S-isomer of omeprazole. All are available in oral formulations. Esomeprazole and pantoprazole are also available in intravenous formulations (Table 62-2). 

Pancrelipase is available in both non-enteric-coated and enteric-coated preparations. Pancrelipase enzymes are rapidly and permanently inactivated by gastric acids. Therefore, non-enteric-coated preparations (eg, Viokase tablets or powder) should be given concomitantly with acid suppression therapy (proton pump inhibitor or H2 antagonist) to reduce acid-mediated destruction within the stomach. Encapsulated formulations contain acid-resistant microspheres (Creon) or microtablets (Pancrease, Ultrase). Enteric-coated formulations are more commonly used because they do not require concomitant acid suppression therapy. 

Proton pump inhibitors are administered as inactive prodrugs. To protect the acid-labile prodrug from rapid destruction within the gastric lumen, they are formulated as acid-resistant enteric-coated... 

Baldi F, Malfertheiner P. Lansoprazole fast disintegrating tablet a new formulation for an established proton pump inhibitor. Digestion 2003 67(l-2) l-5. 

Devlin JW, Welage LS, Olsen KM. Proton pump inhibitor formulary considerations in the acutely ill. Part 1 Pharmacology, pharmacodynamics, and available formulations. Ann Pharmacother 2005 Oct 39(10) 1667-1677. Epub 2005, 23 Aug. 

The proton pump inhibitors degrade in acidic environments and are therefore formulated in a delayed-release capsule or tablet formulation. Lansoprazole, esomeprazole, and omeprazole contain enteric-coated (pH-sensitive) granules in a capsule form. In patients unable to swallow the capsule or in pediatric patients, the contents of the capsule can be mixed in applesauce or placed in orange juice. If a patient has a nasogastric tube, the contents of an omeprazole capsule can... 

To prevent degradation of proton-pump inhibitors by acid in the gastric lumen, oral dosage forms are supplied in different formulations (1) enteric-coated drugs contained inside gelatin capsules (omeprazole, esomeprazole, and... 

DmochowskiR, Chen A, Sathyan G, MacDiarmid S, Gidwani S, Gupta S. Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of o -butynin and tolterockne. JClin Pharmacol (2005) 45, 961-8. 

Dabholkar AH, Han C, Paris MM, Perez MC, Atkinson SN, Peura DA. The 12-month safety profile of dexlansoprazole, a proton pump inhibitor with a dual delayed release formulation, in patients with gastro-oesophageal reflux disease. Aliment Pharmacol Ther 2011 33 366-77. 

Pilbrant A (1993) Formulation of proton pump inhibitors. In Current status on targeted drug delivery to the gastrointestinal tract. Capsugel Symposia series. Capsugel Library, Bomem, 35-42... 

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