ESOMEPRAZOLE
ESOMEPRAZOLE
(Nexium®)
DOSING IN ADULTS
Erosive esophagitis (healing): Initial: 20-40 mg once daily for 4-8 weeks; if incomplete healing, may continue for an additional 4-8 weeks; maintenance: 20 mg once daily
Maintenance of healing of erosive esophagitis: 20 mg once daily; clinical trials evaluated therapy for ≤6 months
Symptomatic gastroesophageal reflux: 20 mg once daily for 4 weeks; may consider an additional 4 weeks of treatment if symptoms do not resolve
Peptic ulcer disease: Eradication of Helicobacter pylori: 40 mg once daily for 10 days; requires combination therapy
Prevention of NSAID-induced gastric ulcers: 20-40 mg once daily for up to 6 months
DOSING IN RENAL IMPAIRMENT No adjustment is necessary.
DOSING IN HEPATIC IMPAIRMENT
Mild-to-moderate hepatic impairment -No dosage adjustment needed.
Severe hepatic impairment -Dose should not exceed 20 mg/day.
DOSAGE FORMS
Capsule, delayed release, as magnesium:
Nexium®: 20 mg, 40 mg
Granules, for oral suspension, delayed release, as magnesium:
Nexium®: 10 mg/packet (30s); 20 mg/packet (30s); 40 mg/packet (30s)
ADMINISTRATION
Capsule: Should be swallowed whole and taken at least 1 hour before eating (best if taken before breakfast). Capsule can be opened and contents mixed with 1 tablespoon of applesauce. Swallow immediately; mixture should not be chewed or warmed.
Granules: Empty into container with 1 tablespoon of water and stir; leave 2-3 minutes to thicken. Stir and drink within 30 minutes. If any medicine remains after drinking, add more water, stir and drink immediately.
SIGNIFICANT ADVERSE REACTIONS
Abdominal pain
Headache
Hypertension
Chest pain
CONTRAINDICATIONS — Hypersensitivity to esomeprazole, substituted benzimidazoles (ie, lansoprazole, omeprazole, pantoprazole, rabeprazole), or any component of the formulation
DRUG INTERACTIONS
Antifungal agents : Proton pump inhibitors may decrease the absorption and thus the levels/effects of itraconazole and ketoconazole; avoid concomitant use.
Antiretroviral: Proton pump inhibitors may decrease the absorption of atazanavir and Indinavir.
CYP2C8 Substrates: may increase the levels/effects of CYP2C8 substrates. Example substrates include amiodarone, paclitaxel, pioglitazone, repaglinide, and rosiglitazone.
CYP2C19 inducers: May decrease the levels/effects of Nexium. Example inducers include aminoglutethimide, carbamazepine, phenytoin, and rifampin.
CYP2C19 substrates: May increase the levels/effects of CYP2C19 substrates. Example substrates include citalopram, diazepam, methsuximide, phenytoin, propranolol, and sertraline.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of rabeprazole. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
HMG-CoA reductase inhibitors: Proton pump inhibitors may increase the serum concentration of HMG-CoA reductase inhibitors; monitor for rhabdomyolysis.
Iron salts : Proton pump inhibitors may decrease the absorption.
Methotrexate: Proton pump inhibitors may decrease the excretion of methotrexate; monitor for increased toxic effects
PREGNANCY RISK FACTOR — B
LACTATION — Excretion in breast milk unknown/not recommended.