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Dexlansoprazole

Pronunciation

(deks lan SOE pra zole)

Index Terms

  • Kapidex
  • TAK-390MR

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule Delayed Release, Oral:

Dexilant: 30 mg, 60 mg [contains fd&c blue #2 aluminum lake]

Brand Names: U.S.

  • Dexilant

Pharmacologic Category

  • Proton Pump Inhibitor
  • Substituted Benzimidazole

Pharmacology

Proton pump inhibitor; decreases acid secretion in gastric parietal cells through inhibition of (H+, K+)-ATPase enzyme system, blocking the final step in gastric acid production

Distribution

Vd: 40.3 L

Metabolism

Hepatic via CYP2C19-mediated hydroxylation and CYP3A4-mediated oxidation; followed by reduction to sulfate, glucuronide, and glutathione conjugates (inactive)

Excretion

Urine (~51% as metabolites); feces (~48% as metabolites)

Time to Peak

Serum: Note: Two distinct peaks secondary to dual release formulation:

Peak 1: 1-2 hours

Peak 2: 4-5 hours

Half-Life Elimination

~1-2 hours; increased in the elderly

Protein Binding

~96% to 99%

Special Populations: Hepatic Function Impairment

Plasma exposure to the drug is ~2 times greater in patients with moderate hepatic impairment compared with subjects with healthy hepatic function.

Special Populations: Elderly

AUC is increased in the elderly.

Special Populations: Gender

Systemic exposure is higher in women than men.

Use: Labeled Indications

Erosive esophagitis: Healing of all grades of erosive esophagitis for up to 8 weeks; to maintain healing of erosive esophagitis and relief of heartburn for up to 6 months.

Gastroesophageal reflux disease: Treatment of heartburn associated with symptomatic nonerosive gastroesophageal reflux disease (GERD) for 4 weeks.

Contraindications

Hypersensitivity (eg, anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, urticaria) to dexlansoprazole, other substituted benzimidazole proton pump inhibitors or to any component of the formulation.

Dosage

Oral: Adults:

Erosive esophagitis (EE): Short-term treatment: 60 mg once daily for up to 8 weeks; maintenance of healed EE and symptomatic relief of heartburn: 30 mg once daily for up to 6 months. Note: Doses >30 mg do not provide additional benefit during maintenance phase.

Symptomatic GERD: Short-term treatment: 30 mg once daily for 4 weeks. Note: Doses >30 mg do not provide additional benefit during maintenance phase.

Dosage adjustment in renal impairment: No dosage adjustment necessary

Dosage adjustment in hepatic impairment:

Mild hepatic impairment (Child-Pugh class A): No dosage adjustment necessary

Moderate hepatic impairment (Child-Pugh class B): Consider a maximum dose of 30 mg once daily

Severe hepatic impairment (Child-Pugh class C): There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Administration

May be administered without regard to meals; some patients may benefit from premeal administration if symptoms do not adequately respond to postmeal dosing. Capsules should be swallowed whole; do not chew. Alternatively, patients who are unable to swallow capsules may open the capsule, sprinkle the intact granules onto 1 tablespoon of applesauce, and swallow intact granules immediately (do not chew granules). Do not save applesauce and granule mixture for later use. Capsules may also be opened for administration via NG tube or oral syringe.

NG tube (≥16 French): Open capsules and mix intact granules (not crushed) with 20 mL of water. Withdraw mixture into catheter-tip syringe; swirl syringe gently to prevent granules from settling and administer mixture immediately through NG tube (≥16 French) into the stomach. Refill syringe with 10 mL water, swirl gently, and flush NG tube; repeat. Do not save water and granule mixture for later use.

Oral syringe: Open capsules and mix intact granules (not crushed) with 20 mL water. Withdraw mixture into oral syringe; swirl syringe gently to prevent granules from settling and administer mixture immediately into the mouth. Refill syringe with 10 mL water, swirl gently, and administer; repeat. Do not save water and granule mixture for later use.

Dietary Considerations

Some patients may benefit from premeal administration if symptoms do not adequately respond to postmeal dosing.

Storage

Store at 25°C (77°F); excursions are permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Amphetamine: Proton Pump Inhibitors may increase the absorption of Amphetamine. Monitor therapy

Atazanavir: Proton Pump Inhibitors may decrease the serum concentration of Atazanavir. Management: See full drug interaction monograph for details. Consider therapy modification

Bisphosphonate Derivatives: Proton Pump Inhibitors may diminish the therapeutic effect of Bisphosphonate Derivatives. Monitor therapy

Bosutinib: Proton Pump Inhibitors may decrease the serum concentration of Bosutinib. Management: Consider alternatives to proton pump inhibitors, such as antacids or H2 receptor antagonists. Administer alternative agents more than 2 hours before or after bosutinib. Consider therapy modification

Cefditoren: Proton Pump Inhibitors may decrease the serum concentration of Cefditoren. Management: If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of PPIs can not be avoided. Consider therapy modification

Clopidogrel: Dexlansoprazole may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Management: Due to the possible risk for impaired clopidogrel effectiveness, clinicians should carefully consider the need for proton pump inhibitor therapy in patients receiving clopidogrel. Other acid-lowering therapies do not appear to share this interaction. Consider therapy modification

Cysteamine (Systemic): Proton Pump Inhibitors may diminish the therapeutic effect of Cysteamine (Systemic). Monitor therapy

Dabigatran Etexilate: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Monitor therapy

Dabrafenib: Proton Pump Inhibitors may decrease the serum concentration of Dabrafenib. Dabrafenib may decrease the serum concentration of Proton Pump Inhibitors. Management: Seek alternatives to the proton pump inhibitor when possible. If concomitant therapy cannot be avoided, monitor for diminished effects of both drugs. Consider therapy modification

Dasatinib: Proton Pump Inhibitors may decrease the serum concentration of Dasatinib. Management: Antacids (taken 2 hours before or after dasatinib administration) can be used in place of the proton pump inhibitor if some acid-reducing therapy is needed. Avoid combination

Delavirdine: Proton Pump Inhibitors may decrease the serum concentration of Delavirdine. Management: Chronic therapy with proton pump inhibitors (PPIs) should be avoided in patients treated with delavirdine. The clinical significance of short-term PPI therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Avoid combination

Dexmethylphenidate: Proton Pump Inhibitors may increase the absorption of Dexmethylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Dextroamphetamine: Proton Pump Inhibitors may increase the absorption of Dextroamphetamine. Specifically, the dextroamphetamine absorption rate from mixed amphetamine salt extended release (XR) capsules may be increased in the first hours after dosing. Monitor therapy

Erlotinib: Proton Pump Inhibitors may decrease the serum concentration of Erlotinib. Avoid combination

Fluconazole: May increase the serum concentration of Proton Pump Inhibitors. Monitor therapy

Gefitinib: Proton Pump Inhibitors may decrease the serum concentration of Gefitinib. Management: Avoid use of proton pump inhibitors (PPIs) with gefitinib when possible. If required, administer gefitinib 12 hours after administration of the PPI or 12 hours before the next dose of the PPI. Consider therapy modification

Indinavir: Proton Pump Inhibitors may decrease the serum concentration of Indinavir. Monitor therapy

Iron Salts: Proton Pump Inhibitors may decrease the absorption of Iron Salts. Exceptions: Ferric Carboxymaltose; Ferric Citrate; Ferric Gluconate; Ferric Pyrophosphate Citrate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Monitor therapy

Itraconazole: Proton Pump Inhibitors may decrease the serum concentration of Itraconazole. Consider therapy modification

Ketoconazole (Systemic): Proton Pump Inhibitors may decrease the serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase the serum concentration of Proton Pump Inhibitors. Consider therapy modification

Ledipasvir: Proton Pump Inhibitors may decrease the serum concentration of Ledipasvir. Management: Avoid the use of PPIs at doses greater than the equivalent of omeprazole 20 mg, avoid administration of PPIs within 2 hours prior to ledipasvir dosing, and avoid use of PPIs in combination with food. Consider therapy modification

Mesalamine: Proton Pump Inhibitors may diminish the therapeutic effect of Mesalamine. Proton pump inhibitor-mediated increases in gastrointestinal pH may cause the premature release of mesalamine from specific sustained-release mesalamine products. Management: Consider avoiding concurrent administration of high-dose proton pump inhibitors (PPIs) with sustained-release mesalamine products. Consider therapy modification

Methotrexate: Proton Pump Inhibitors may increase the serum concentration of Methotrexate. Monitor therapy

Methylphenidate: Proton Pump Inhibitors may increase the absorption of Methylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Ritalin LA brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): Proton Pump Inhibitors may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, the absorption of iron may be decreased. Monitor therapy

Mycophenolate: Proton Pump Inhibitors may decrease the serum concentration of Mycophenolate. Specifically, concentrations of the active mycophenolic acid may be reduced. Monitor therapy

Nelfinavir: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Nelfinavir. Proton Pump Inhibitors may decrease the serum concentration of Nelfinavir. Avoid combination

Nilotinib: Proton Pump Inhibitors may decrease the serum concentration of Nilotinib. Management: Avoid this combination when possible since separation of doses is not likely to be an adequate method of minimizing the interaction. Consider therapy modification

PAZOPanib: Proton Pump Inhibitors may decrease the serum concentration of PAZOPanib. Avoid combination

Posaconazole: Proton Pump Inhibitors may decrease the serum concentration of Posaconazole. Consider therapy modification

Raltegravir: Proton Pump Inhibitors may increase the serum concentration of Raltegravir. Monitor therapy

Rilpivirine: Proton Pump Inhibitors may decrease the serum concentration of Rilpivirine. Avoid combination

Riociguat: Proton Pump Inhibitors may decrease the serum concentration of Riociguat. Monitor therapy

Risedronate: Proton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate. Avoid combination

Saquinavir: Proton Pump Inhibitors may increase the serum concentration of Saquinavir. Monitor therapy

Tacrolimus (Systemic): Proton Pump Inhibitors may increase the serum concentration of Tacrolimus (Systemic). Management: Tacrolimus dose adjustment may be required. Rabeprazole, pantoprazole, or selected H2-receptor antagonists (i.e., ranitidine or famotidine) may be less likely to interact. Genetic testing may predict patients at highest risk. Consider therapy modification

Tipranavir: May decrease the serum concentration of Proton Pump Inhibitors. These data are derived from studies with Ritonavir-boosted Tipranavir. Monitor therapy

Voriconazole: May increase the serum concentration of Proton Pump Inhibitors. Proton Pump Inhibitors may increase the serum concentration of Voriconazole. Management: In patients receiving omeprazole 40 mg/day or greater, reduce omeprazole dose by half when initiating voriconazole. Monitor therapy

Adverse Reactions

2% to 10%:

Gastrointestinal: Diarrhea (5%), abdominal pain (4%), nausea (3%), flatulence (1% to 3%), vomiting (1% to 2%)

Respiratory: Upper respiratory tract infection (2% to 3%)

<2% (Limited to important or life-threatening): Abdominal distress, abnormal bowel sounds, abnormal dreams, abnormal stools, acne vulgaris, acute renal failure, anaphylaxis, anemia, angina pectoris, anorectal pain, anxiety, arthralgia, arthritis, aspiration, asthma, auditory hallucination, autoimmune hemolytic anemia, Barrett's esophagus, bezoar formation, biliary colic, blurred vision, bone fracture, bradycardia, bronchitis, cardiac arrhythmia, cerebrovascular accident, change in libido, chest pain, chills, cholecystitis (acute), cholelithiasis, chronic renal disease (Lazarus 2016), Clostridium difficile-associated diarrhea, colitis (microscopic), colonic polyps, constipation, constriction of the pharynx, cough, deafness, decreased serum bilirubin, deep vein thrombosis, delayed gastric emptying, depression, dermatitis, diabetes mellitus, dizziness, duodenitis, dysgeusia, dysmenorrhea, dyspareunia, dyspepsia, dysphagia, dyspnea, dysuria, edema (including oral, facial, and pharyngeal), enteritis, eructation, erythema, esophagitis, eye irritation, feeling abnormal, fever, gastric polyp, gastritis, gastroenteritis, gastrointestinal hypermotility, gastrointestinal perforation, gastrointestinal ulcer, goiter, halitosis, headache, hematemesis, hematochezia, hemorrhoids, hepatitis, hepatomegaly, hepatotoxicity (idiosyncratic) (Chalasani 2014), hiccups, hot flash, hypercalcemia, hyperglycemia, hyperkalemia, hyperlipidemia, hypermenorrhea, hypersensitivity, hypersensitivity angiitis, hypertension, hyperventilation, hypokalemia, hypomagnesemia, hyponatremia, hypothyroidism, immune thrombocytopenia, increased serum alkaline phosphatase, increased serum ALT, increased serum AST, increased serum bilirubin, increased serum creatinine, infection (Candida, herpes, influenza, vaginal, viral), insomnia, irritable bowel syndrome, joint sprain, lymphadenopathy, memory impairment, migraine, mucositis, mucus stools, myalgia, myocardial infarction, nasopharyngitis, neutropenia, nodule, oral bullae, otalgia, pain, painful defecation, palpitations, pancreatitis, paresthesia, pathological fracture due to osteoporosis, pharyngitis, pneumonia, proctitis, pruritus, psychomotor agitation, rectal hemorrhage, seizure, sinusitis, skin lesion, skin rash, Stevens-Johnson syndrome, sunburn, swelling of eye, tachycardia, thrombocytopenia, tinnitus, toxic epidermal necrolysis, transient ischemic attacks, tremor, urinary urgency, urticaria, vertigo, voice disorder, weakness, weight gain, xerostomia

Warnings/Precautions

Concerns related to adverse effects:

• Atrophic gastritis: Long-term omeprazole therapy has caused atrophic gastritis (by biopsy); this may also occur with dexlansoprazole.

• Carcinoma: No occurrences of enterochromaffin-like (ECL) cell carcinoids, dysplasia, or neoplasia (such as those seen in studies of rodents exposed to lansoprazole) have been reported in humans.

Clostridium difficile-associated diarrhea (CDAD): Use of proton pump inhibitors (PPIs) may increase risk of CDAD, especially in hospitalized patients; consider CDAD diagnosis in patients with persistent diarrhea that does not improve. Use the lowest dose and shortest duration of PPI therapy appropriate for the condition being treated.

• Fractures: Increased incidence of osteoporosis-related bone fractures of the hip, spine, or wrist may occur with proton pump inhibitor (PPI) therapy. Patients on high-dose (multiple daily doses) or long-term therapy (≥1 year) should be monitored. Use the lowest effective dose for the shortest duration of time, use vitamin D and calcium supplementation, and follow appropriate guidelines to reduce risk of fractures in patients at risk.

• Hypomagnesemia: Reported rarely, usually with prolonged PPI use of >3 months (most cases >1 year of therapy). May be symptomatic or asymptomatic; severe cases may cause tetany, seizures, and cardiac arrhythmias. Consider obtaining serum magnesium concentrations prior to beginning long-term therapy, especially if taking concomitant digoxin, diuretics, or other drugs known to cause hypomagnesemia; and periodically thereafter. Hypomagnesemia may be corrected by magnesium supplementation, although discontinuation of dexlansoprazole may be necessary; magnesium levels typically return to normal within 1 week of stopping.

• Interstitial nephritis: Acute interstitial nephritis has been observed in patients taking PPIs; may occur at any time during therapy and is generally due to an idiopathic hypersensitivity reaction. Discontinue if acute interstitial nephritis develops.

• Vitamin B12 deficiency: Prolonged treatment (≥2 years) may lead to vitamin B12 malabsorption and subsequent vitamin B12 deficiency. The magnitude of the deficiency is dose related and the association is stronger in females and those younger in age (<30 years); prevalence is decreased after discontinuation of therapy (Lam, 2013).

Disease-related concerns:

• Gastric malignancy: Relief of symptoms does not preclude the presence of a gastric malignancy.

• Gastrointestinal infection (eg, Salmonella, Campylobacter): Use of PPIs may increase risk of these infections.

• Hepatic impairment: Patients with moderate hepatic impairment (Child-Pugh class B) may require dosage reductions; no studies have been conducted in patients with severe hepatic impairment (Child-Pugh class C).

Concurrent drug therapy issues:

• Clopidogrel: Proton pump inhibitors (PPIs) may diminish the therapeutic effect of clopidogrel, thought to be due to reduced formation of the active metabolite of clopidogrel. The manufacturer of clopidogrel recommends either avoidance of both omeprazole (even when scheduled 12 hours apart) and esomeprazole or use of a PPI with comparatively less effect on the active metabolite of clopidogrel (eg, pantoprazole). Although lansoprazole exhibits the most potent CYP2C19 inhibition in vitro (Li, 2004; Ogilvie, 2011), an in vivo study of extensive CYP2C19 metabolizers showed less reduction of the active metabolite of clopidogrel when administered with lansoprazole/dexlansoprazole compared to esomeprazole/omeprazole (Frelinger, 2012). In contrast to these warnings, others have recommended the continued use of PPIs, regardless of the degree of inhibition, in patients with a history of GI bleeding or multiple risk factors for GI bleeding who are also receiving clopidogrel since no evidence has established clinically meaningful differences in outcome; however, a clinically-significant interaction cannot be excluded in those who are poor metabolizers of clopidogrel (Abraham, 2010; Levine, 2011). The manufacturer of dexlansoprazole states that no dosage adjustment is necessary for clopidogrel when used concurrently with approved doses.

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Dexlansoprazole is the R-enantiomer of lansoprazole. Information related to dexlansoprazole in pregnancy has not been located. Refer to the lansoprazole monograph for additional information. When treating GERD in pregnancy, PPIs may be used when clinically indicated (Katz, 2013).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, flatulence, rhinitis, rhinorrhea, or sternutation. Have patient report immediately to prescriber signs of hypomagnesemia, signs of renal impairment, severe dizziness, syncope, significant dyspepsia, osteodynia, chills, pharyngitis, excessive weight loss, intolerable diarrhea, abdominal cramps, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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