dex-lan-SOE-pra-zole

Therapeutic Classification: antiulcer agents

Pharmacologic Classification: proton pump inhibitors

• Erosive esophagitis.
• Maintenance of healed erosive esophagitis and relief of heartburn.
• Treatment of heartburn from nonerosive gastroesophageal reflux disease (GERD).

• Binds to an enzyme in the presence of acidic gastric pH, preventing the final transport of hydrogen ions into the gastric lumen.

• Diminished accumulation of acid in the gastric lumen, with lessened acid reflux.

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 96–99%.

Metabolism/Excretion: Extensively metabolized by the liver, primarily by the CYP2C19 and CYP3A4 isoenzymes; the CYP2C19 isoenzyme exhibits genetic polymorphism (15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly ↑ dexlansoprazole concentrations and an ↑ risk of adverse effects); no active metabolites. No renal elimination.

Half-life: 1–2 hr.

(plasma concentrations)

*Reflects effects of delayed release capsule.

Contraindicated in:

• Hypersensitivity to dexlansoprazole or related drugs (benzimidazoles)
• Severe hepatic impairment
• Concurrent use of rilpivirine.

Use Cautiously in:

• Moderate hepatic impairment
• Patients using high doses for >1 yr (↑ risk of hip, wrist, or spine fractures and fundic gland polyps)
• Patients using therapy for >3 yr (↑ risk of vitamin B₁₂ deficiency)
• Pre-existing risk of hypocalcemia
• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Children <12 yr (safety and effectiveness not established); ↑ risk of heart valve thickening in children <2 yr
• Geri: Appears on Beers list. ↑ risk of Clostridioides difficile infection, pneumonia, GI malignancies, bone loss, and fractures in older adults. Avoid scheduled use for >8 wk in older adults unless for high-risk patients (e.g., oral corticosteroid or chronic NSAID use) or patients with erosive esophagitis, Barrett's esophagitis, pathological hypersecretory condition, or demonstrated need for maintenance therapy (e.g., failure of H₂ antagonist).

Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, cutaneous lupus erythematosus, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN).

F and E: hypocalcemia (especially if treatment duration 3 mo), hypokalemia (especially if treatment duration 3 mo), hypomagnesemia (especially if treatment duration 3 mo).

GI: abdominal pain, diarrhea, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), flatulence, fundic gland polyps, nausea, vomiting.

GU: acute tubulointerstitial nephritis.

Hemat: vitamin B₁₂ deficiency.

MS: bone fracture.
Misc: (INCLUDING ANAPHYLAXIS, ANGIOEDEMA, OR ACUTE TUBULOINTERSTITIAL NEPHRITIS)HYPERSENSITIVITY REACTIONS , systemic lupus erythematosus.

Drug-Drug:

• May ↓ absorption 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 ↑ levels of digoxin, methotrexate, and tacrolimus.
• May ↑ effect of warfarin.
• Hypomagnesemia and hypokalemia ↑ risk of digoxin toxicity.

• PO (Adults and Children 12 yr): Healing of erosive esophagitis: 60 mg once daily for up to 8 wk; Maintenance of healed erosive esophagitis: 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.

(Generic available)

• Delayed-release capsules: 30 mg; 60 mg;

• Assess patient routinely for epigastric or abdominal pain and for frank or occult blood in stool, emesis, or gastric aspirate.
• Monitor bowel elimination. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of CDAD.
• Monitor for signs and symptoms of decreased renal function (malaise, nausea, anorexia) periodically during therapy. If symptoms occur, discontinue dexlansoprazole and evaluate patient for acute tubulointerstitial nephritis.
• Monitor for severe cutaneous adverse reactions (SJS, TEN, DRESS). Discontinue dexlansoprazole at first signs or symptoms of severe skin reactions and consider further evaluation.

• May cause abnormal liver function tests, including ↑ AST, ALT, and ↑ or ↓ serum bilirubin.
  • May cause ↑ serum creatinine and BUN, ↑ blood glucose, and ↑ serum potassium, and ↓ serum magnesium levels. Consider monitoring magnesium and calcium levels prior to starting and periodically during therapy in patients with a pre-existing risk of hypocalcemia (hypoparathyroidism). Supplement with magnesium and/or calcium as necessary. If hypocalcemia is refractory to treatment, consider discontinuing therapy.
  • May cause ↓ platelet levels.
  • May also cause ↑ gastrin and total protein levels.
  • Monitor INR and prothrombin time in patients taking warfarin.

• Do not confuse Dexilant with duloxetine.
• PO: May be administered without regard to food. DNC: Swallow capsules whole or may be opened and sprinkled on 1 tbsp of applesauce and swallowed immediately, without crushing or chewing, for patients with difficulty swallowing.
  • Capsules may be opened and granules emptied into 20 mL water. Withdraw entire mixture into syringe; swirl gently to mix. Administer mixture into mouth or nasogastric tube immediately; do not save for later. Rinse syringe with 10 mL of water twice to ensure all medication administered.
  • Administer for shortest time possible to minimize risk of osteoporosis-related fractures and cutaneous or systemic lupus erythematosus.

• Instruct patient to take medication as directed for the full course of therapy, even if feeling better. Take missed doses as soon as remembered but not if just before next scheduled dose; do not double doses.
• Advise patient to avoid alcohol, products containing aspirin or NSAIDs, and foods that may cause an increase in GI irritation.
• Advise patient to report onset of black, tarry stools; diarrhea; or abdominal pain to health care professional promptly, especially if accompanied by fever or bloody stools. Do not treat with antidiarrheals without consulting health care professional.
• Advise patient to notify health care professional if signs and symptoms of hypomagnesemia (seizures, dizziness, abnormal or fast heartbeat, jitteriness, jerking movements or shaking [tremors], muscle weakness, spasms of the hands and feet, cramps or muscle aches, spasm of the voice box) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Decrease in abdominal pain, heartburn, gastric irritation, and bleeding in patients with GERD; may require up to 4 wk of therapy.
• Healing in patients with erosive esophagitis; may require up to 8 wk of therapy for healing and 6 mo of therapy for maintenance.

Dexilant