dexlansoprazole (dex-lan-soe-pra-zole) Dexilant, Dexilant SoluTab

 Indications

Healing of erosive esophagitis (EE) (capsules only).

Maintenance of healed EE and relief of heartburn (capsules

and orally disintegrating tablets [ODTs]). Treatment

of heartburn from nonerosive gastroesophageal

reflux disease (GERD) (capsules and ODTs).

Action

Binds to an enzyme in the presence of acidic gastric pH,

preventing the final transport of hydrogen ions into the

gastric lumen. Therapeutic Effects: Diminished

accumulation of acid in the gastric lumen, with lessened

acid reflux.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 96–99%.

Metabolism and Excretion: Extensively metabolized

by the liver (CYP2C19 and CYP3A4 enzyme systems

are involved); the CYP2C19 enzyme system exhibits

genetic polymorphism; 15–20% of Asian patients

and 3–5% of Caucasian and Black patients may be

poor metabolizers and may have significantlyqdexlansoprazole

concentrations and anqrisk of adverse effects);

no active metabolites. No renal elimination.

Half-life: 1–2 hr.

TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK* DURATION

PO unknown 1–2 hr (1st);

4–5 hr

(2nd)

24 hr

*Reflects effects of delayed release capsule.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Severe hepatic

impairment; Concurrent use of rilpivirine; Lactation:

Lactation.

Use Cautiously in: Moderate hepatic impairment

(daily dose should not exceed 30 mg); Patients using

high doses for 1 year (qrisk of hip, wrist, or spine

fractures); Patients using therapy for 3 yr (qrisk of

vitamin B12 deficiency; Pedi: Children 12 yr (safety

and effectiveness not established).

Adverse Reactions/Side Effects

Derm: cutaneous lupus erythematosus. GI: CLOSTRIDIUM

DIFFICILE-ASSOCIATED DIARRHEA (CDAD), abdominal

pain, diarrhea, flatulence, nausea, vomiting. F and E:

hypomagnesemia (especially if treatment duration 3

mo). GU: acute interstitial nephritis. Hemat: vitamin

B12 deficiency. MS: bone fracture. Misc: HYPERSENSITIVITY

REACTIONS (including anaphylaxis), systemic lupus

erythematosus.

Interactions

Drug-Drug: Maypabsorption of drugs requiring

acid pH, including ketoconazole, itraconazole, atazanavir,

nelfinavir, rilpivirine, ampicillin esters,

iron salts, erlotinib, and mycophenolate mofetil;

concurrent use with rilpivirine contraindicated; avoid

concurrent use with atazanavir and nelfinavir. May

qlevels of digoxin, methotrexate, and tacrolimus.

Mayqeffect of warfarin. Hypomagnesemiaqrisk of

digoxin toxicity.

Route/Dosage

ODT formulation is NOT indicated for

healing of EE (two 30-mg ODTs are NOT

interchangeable with one 60-mg delayed

release capsule)

PO (Adults and Children 12 yr): Healing of EE

(capsules only)—60 mg once daily for up to 8 wk;

Maintenance of healed EE—30 mg once daily for up

to 6 mo (adults) and up to 16 wk (12–17 yr old);

GERD—30 mg once daily for 4 wk.

Hepatic Impairment

PO (Adults): Moderate hepatic impairment—daily

dose should not exceed 30 mg.

Availability (generic available)

Delayed release capsules: 30 mg, 60 mg. Orally

disintegrating tablets: 30 mg.