dexlansoprazole

Brand: Dexilant

Prototype: omeprazole
Drug Class: proton pump inhibitor
Drug Family: GI agent
Subclass: R-enantiomer PPI with dual delayed-release
Organ Systems: gastrointestinal

Mechanism of Action

R-enantiomer of lansoprazole that irreversibly inhibits gastric H+/K+-ATPase. Unique dual-release formulation produces two plasma concentration peaks, extending acid suppression.

H+/K+-ATPase (proton pump)

Indications

  • GERD
  • erosive esophagitis (healing and maintenance)
  • non-erosive GERD

Contraindications

  • hypersensitivity to PPIs
  • concurrent rilpivirine use

Adverse Effects

Common

  • diarrhea
  • abdominal pain
  • nausea
  • flatulence

Serious

  • Clostridium difficile-associated diarrhea
  • hypomagnesemia
  • acute interstitial nephritis
  • bone fractures (long-term)

Pharmacokinetics (ADME)

Absorption dual delayed-release capsule yields two Tmax peaks (~1–2 h and 4–5 h); can be taken without regard to food
Distribution 96–99% protein bound
Metabolism hepatic via CYP2C19 (primary) and CYP3A4
Excretion renal and fecal
Half-life 1–2 hours
Onset 1–2 hours
Peak dual peak at 1–2 h and 4–5 h
Duration 24 hours
Protein Binding 96–99%
Vd moderate

Drug Interactions

Drug / Agent Mechanism Severity
atazanavir reduced absorption at increased gastric pH major
methotrexate PPI class effect on renal methotrexate clearance major
clopidogrel CYP2C19 inhibition reduces active metabolite of clopidogrel moderate

Nursing Considerations

  1. Unique advantage: capsule may be taken without regard to meals, improving patient adherence.
  2. Capsules may be opened and granules sprinkled on applesauce for patients unable to swallow whole; do not crush granules.
  3. Monitor serum magnesium in patients on long-term therapy or those also taking digoxin or diuretics.
  4. Educate patient that this formulation has two release phases to provide longer acid control throughout the day.

Clinical Pearls

  • The dual delayed-release technology delivers two separate absorption peaks, maintaining elevated gastric pH for a longer duration than standard PPIs.
  • Can be taken without regard to food, which is a practical advantage over other PPIs that require pre-meal dosing.

Safety Profile

Pregnancy generally-safe
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

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