Esomeprazole is a proton pump inhibitor that helps reduce the amount of gastric acid produced in the stomach.
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Esomeprazole achieves this by inhibiting an ion transport protein called H+/K+ ATPase that is present in the gastric parietal cells. The drug is cleared rapidly, with inactive metabolites such as 5-hydroxymethylesomeprazole and 5-carboxyesomeprazole mainly passed through the urine.
Indications
Esomeprazole is used in the short-term treatment of gastroesophageal reflux disease (GERD) to relieve inflammation and pain in the esophagus when patients are unable to take oral medications. This drug is also used both in the treatment of peptic and duodenal ulcers, as well as a preventative measure prior to endoscopy procedures to reduce the risk of these ulcers bleeding. Other uses of this drug include the prevention of gastric ulcers caused by non-steroidal anti-inflammatory drugs (NSAIDs) and treatment of the gastrointestinal ulcers associated with Crohn's disease.
Drug interactions
The term “drug interaction” refers to the effects that drugs have on each other when they interact in the body.
Esomeprazole is a competitive inhibitor of CYP2C19 and CYP2C9, both of which are enzymes in the cytochrome P450 family that are important in the metabolism and excretion of other drugs. Inhibition of these enzymes by esomeprazole could therefore alter the efficacy of drugs that rely on these enzymes for their metabolism, such as diazepam, which is a sedative and anxiolytic, as well as the blood thinner warfarin. If these drugs are used alongside esomeprazole, their concentration in the blood would rise and lead to drowsiness (caused by diazepam) or an increased tendency to bleed (caused by warfarin).
On the other hand, drugs that rely on conversion by CYP2C19 and CYP2C9 to become activated, as is the case with clopidogrel, may have a reduced therapeutic effect when used with esomeprazole. Furthermore, the absorption and efficacy of certain drugs depend on the presence of a certain amount of stomach acid. Since esomeprazole inhibits gastric acid, the effects of these drugs will be reduced, as is the case with ketoconazole and atazanavir.
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Additional examples of drugs that may interact with esomeprazole include:
- Anticoagulants such as cilostazol, methotrexate, digoxin, tacrolimus and saquinavir. When these drugs are taken simultaneously with esomeprazole, their risk of side effects may increase.
- Diuretics like furosemide or hydrochlorothiazide may increase the risk of low magnesium levels when used in combination with esomeprazole.
- Antifungals like voriconazole may increase the likelihood of esomeprazole having side effects.
- Natural remedies like St. John’s wort and ginkgo biloba may decrease the effectiveness of esomeprazole.
Food interaction
Certain food products can also alter the absorption of esomeprazole. Therefore, this drug should be taken at least an hour before eating any food so that absorption is not affected.
Interaction with medical conditions
Esomeprazole and the liver
Esomeprazole is primarily metabolized by the liver. No significant drug accumulation has been observed in patients with mild-to-moderate liver disease who take esomeprazole. However, significant plasma increases in esomeprazole have been observed among those with severe liver disease; therefore, a maximum daily dose of 20 mg is recommended for these patients.
Esomeprazole and the bones
Proton pump inhibitors have been shown to promote calcium loss from the bones, as well as impair the absorption of this mineral in the diet. Research also suggests that these drugs impair the absorption of magnesium, which is also required for bone mineralization. These side effects of esomeprazole mean the risk of osteoporosis is increased when taking this drug, particularly in women. It is therefore important for individuals to inform their doctor if they have osteoporosis or risk factors for the condition if esomeprazole is being considered as a treatment option.
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