Chapter 57- Proton Pump Inhibitors

Question 1

Proton Pump Inhibitors- Generic medications
(-zole)

Answer 1

Omeprazole (Prilosec)
Esomeprazole (Nexium)
Lansoprazole (Prevacid)
Dexlansoprazole (Kapidex)
Pantoprazole (Protonix)
Raberprazole (Aciphex)

Question 2

Proton Pump Inhibitors-MOA

Answer 2

Suppress the secretion of hydrochloric acid into the lumen of the stomach

Suppress gastric acid secretion by specifically inhibiting the hydrogen-potassium ATP enzyme system on the secretory surface of gastric parietal cells. This action blocks the final step of acid production, lowering the acid levels in the stomach.

Question 3

Proton Pump Inhibitors-Indications

Answer 3

Recommended for the short-term treatment of active duodenal ulcers, GERD, erosive esophagitis, and benign active gastric ulcers

Recommended for the long term treatment of pathological hyper-secretory conditions.

Recommended for maintenance therapy for healing of erosive esophagitis and ulcers

Recommended usage in combination with amoxicillin and clarithromycin for the treatment of H. pylori infection

Question 4

Proton Pump Inhibitors-Oral and IV forms

Answer 4

Esomeprazole
Lansoprazole
Pantoprazole

All available in ER oral forms and IV preparations

Question 5

Proton Pump Inhibitors-Oral forms only

Answer 5

Rabeprazole
Dexlansoprazole
Omeprazole

All available as ER oral forms only

Question 6

Proton Pump Inhibitors-Pharmacokinetics

Answer 6

These drugs are acid-labile and are rapidly absorbed from the GI tract, reaching peak levels in 3-5hr.

Extensive metabolism in the liver

Excreted in the urine

Omeprazole is fast acting and more quickly excreted than the other PPI’s

Esomeprazole is a longer acting PPI with a half-life of 60-90min and a duration of 17hr. It is not not broken down as rapidly in the liver as the parent drug (omeprazole)

There are no adequate studies about whether or not these drugs cross the placenta or enter breast milk

Question 7

Proton Pump Inhibitors-Contraindications & cautions

Answer 7

The safety and efficacy of these drugs have not been established for patients younger than 18 years of age, except for lansoprazole, which is the proton pump inhibitor of choice if one is needed for a child.

Question 8

Proton Pump Inhibitors-Adverse effects

Answer 8

The adverse effects associated with these drugs are related to their effects on the ATP pump of the parietal cells.

CNS effects of dizziness and headache are commonly seen. asthenia (loss of strength), vertigo, insomnia, apathy, and dream abnormalities may also be observed.

GI effects can include diarrhea, constipation, abdominal pain, acid rebound, nausea, vomiting, dry mouth, gastric cancer, and tongue atrophy.

Rash and alopecia

Arrhythmias and heart failure

Bone loss and hypomagnesemia

Cough, hoarseness, and pneumonia.

Question 9

Proton Pump Inhibitors-Drug to drug interactions

Answer 9

There is a risk of increased serum levels and increased toxicity of benzo’s, phenytoin, and warfarin.

Decreased levels of theophylline and ketoconazole have been reported when combined with these drugs.

Sucralfate is not absorbed well in the presence of these drugs and doses should be spaced at least 30 min apart

Increased risk of CV events if PPI’s are combined with clopidogrel due to possible interference with the effectiveness of clopidogrel’s anti-platelet MOA.

Question 10

Proton Pump Inhibitors-Pre/post medication assessment

Answer 10

Administer the drug before meals

Monitor the patient’s nutritional status, the use of small frequent meals may be helpful if GI upset is a problem

Arrange for medical follow-up if symptoms are not resolved after 4-8 weeks of therapy