Dosing and uses of Dexilant, Kapidex (dexlansoprazole)
Adult dosage forms and strengths
delayed-release capsule
- 30mg
- 60mg
delayed-release oral disintegrating tablet (ODT)
- 30mg
Erosive Esophagitis
Capsule: Indicated for healing of all grades of erosive esophagitis (EE) and maintaining healing of Ee
ODT: Indicated for maintaining healing of Ee
Healing (capsule): 60 mg PO qDay for up to 8 weeks
Maintenance (capsule or ODT): 30 mg PO qDay for up to 6 months
Gastroesophageal Reflux Disease
Indicated for treating heartburn associated with symptomatic nonerosive GERd
Capsule or ODT: 30 mg PO qDay for 4 weeks
Dosage modifications
Hepatic impairment
- Milde (Child-Pugh A): Dose adjustment not necessary
- Moderate (Child-Pugh B): Not to exceed 30 mg/day
- Severe (Child-Pugh C): Not recommended
Pediatric dosage forms and strengths
delayed-release capsule
- 30mg
- 60mg
delayed-release oral disintegrating tablet (ODT)
- 30mg
Erosive Esophagitis
<12 years
- Safety and efficacy not established
>12 years
- Capsule: Indicated for healing of all grades of erosive esophagitis (EE) and maintaining healing of EE
- ODT: Indicated for maintaining healing of EE
- Healing (capsule): 60 mg PO qDay for up to 8 weeks
- Maintenance (capsule or ODT): 30 mg PO qDay for up to 6 months
Gastroesophageal Reflux Disease
<12 years
- Safety and efficacy not established
>12 years
- Indicated for treating heartburn associated with symptomatic nonerosive GERD
- Capsule or ODT: 30 mg PO qDay for 4 weeks
Dexilant, Kapidex (dexlansoprazole) adverse (side) effects
1-10%
Diarrhea (5%)
Abdominal pain (4%)
Nausea (3%)
URI (2-3%)
Vomiting (1-2%)
Flatulence (1%)
<1% (Selected)
Arrhythmia
Bradycardia
Barrett's esophagus
DVt
Dyspnea
Hepatomegaly
Hypertension
Paresthesia
Rectal hemorrhage
Vulvovaginal infection
Postmarketing Reports
Blurred vision
Oral edema
Facial edema
Anaphylactic shock (requiring emergency intervention)
Stevens-Johnsons syndrome
Toxic epidermal necrolysis (sometimes fatal)
Pharyngeal edema, throat tightness
Generalized rash
Leukocytoclastic vasculitis
Bone fracture
Warnings
Contraindications
Hypersensitivity reactions, including anaphylaxis and acute interstitial nephritis reported
PPIs are contraindicated with rilpivirine-containing products
Cautions
Proton pump inhibitors (PPIs) are possibly associated with increased incidence of Clostridium difficile-associated diarrhea (CDAD); consider diagnosis of CDAD for patients taking PPIs who have diarrhea that does not improve
May interfere with absorption of drugs for which pH is a determinant of oral bioavailability (eg, atazanavir)
Proton pump inhibitors may decrease the efficacy of clopidogrel by reducing the formation of the active metabolite
Gastric atrophy reported with long-term use of another proton pump inhibitor
Published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (>1 yr), high-dose therapy
Relief of symptoms does not eliminate the possibility of a gastric malignancy
Decreased gastric acidity increases serum chromogranin A (CgA) levels and may cause false-positive diagnostic results for neuroendocrine tumors; temporarily discontinue PPIs before assessing CgA levels
Therapy increases risk of Salmonella, Campylobacter, and other infections
Hypomagnesemia may occur with prolonged use (ie, >1 year); adverse effects may result and include tetany, arrhythmias, and seizures; in 25% of cases reviewed, magnesium supplementation alone did not improve low serum magnesium levels and the PPI had to be discontinued
Brand name changed from Kapidex to Dexilant
Daily long-term use (eg, >3 yr) may lead to malabsorption or a deficiency of cyanocobalamin
Acute interstitial nephritis reported in patients taking proton pump inhibitors (see Contraindications)
Serum chromogranin A (CgA) levels increase secondary to drug-induced decreases in gastric acidity; increased CgA level may cause false positive results in diagnostic investigations for neuroendocrine tumors; temporarily stop dexlansoprazole treatment at least 14 days before assessing CgA levels and consider repeating the test if initial CgA levels are high
Pregnancy and lactation
Pregnancy category: B
Lactation: Not known whether distributed into breast milk; discontinue nursing or drug
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Dexilant, Kapidex (dexlansoprazole)
Mechanism of action
R-enantiomer of lansoprazole; PPI; binds to H+/K+-exchanging ATPase (proton pump) in gastric parietal cells, resulting in blockage of acid secretion
Dual release formulation
Absorption
Peak plasma time: 1-2 hr and 4-5 hr (dual release)
Distribution
Protein bound: >96%
Vd: 40.3 L
Metabolism
Hydroxylation mainly by CYP2C19 and oxidation to sulfone by CYP3A4
Elimination
Half-life elimination: 1-2 hr
Excretion: Feces (48% as metabolites), urine (51% as metabolites)
Pharmacogenomics
Extensively metabolized in the liver by oxidation and reduction; oxidative metabolites are formed mainly by CYP2C19
Dexlansoprazole is the major circulating component regardless of CYP2C19 allele status
In extensive (*1/*1) and intermediate (*1/mutant) CYP2C19 metabolizers, 5-hydroxy dexlansoprazole is the major metabolite
In CYP2C19 poor metabolizers (mutant/mutant), dexlansoprazole sulfone is the major plasma metabolite (because of an increase in the alternate metabolic pathway via CYP3A4)
Systemic exposure of dexlansoprazole is generally higher in intermediate and poor metabolizers
Intermediate metabolizers: Mean dexlansoprazole Cmax and AUC values were up to 2 times higher than they were in extensive metabolizers
Poor metabolizers: Mean Cmax was up to 4 times higher and mean AUC was up to 12 times higher than they were in extensive metabolizers
Administration
Oral Administration
Capsule
- May take with or without food
- Swallow whole; do not chew
- May sprinkle capsule contents on applesauce
- 1. Place 1 TBSP of applesauce into a clean container
- 2. Open capsule and sprinkle intact granules on applesauce
- 3. Swallow applesauce and granules immediately, do not chew granules
- 4. Do not save applesauce and granules for later use
- Preparing capsule contents with water in oral syringe
- 1. Open the capsule and empty the granules into a clean container with 20 mL of water
- 2. Withdraw the entire mixture into a syringe
- 3. Gently swirl the syringe in order to keep granules from settling
- 4. Administer the mixture immediately into the mouth; do not save the water and granule mixture for later use
- 5. Refill the syringe with 10 mL of water, swirl gently, and administer
- 6. Refill the syringe again with 10 mL of water, swirl gently, and administer
- Preparing capsule contents with water for NG tube administration
- NG tube (≥16 French)
- 1. Open the capsule and empty the granules into a clean container with 20 mL of water
- 2. Withdraw the entire mixture into a catheter-tip syringe
- 3. Swirl the catheter-tip syringe gently in order to keep the granules from settling, and immediately inject the mixture through the NG tube into the stomach; do not save the water and granule mixture for later use
- 4. Refill the catheter-tip syringe with 10 mL of water, swirl gently, and flush the tube
- 5. Refill the catheter-tip syringe again with 10 mL of water, swirl gently, and administer
Oral disintegrating tablet
- Take at least 30 minutes before a meal
- Do not break or cut
- Place the tablet on the tongue, allow to disintegrate and swallow without water
- Do not chew microgranules
- May also be swallowed whole with water
- Avoid use of alcohol
- ODT with water in oral syringe
- 1. Place one tablet in an oral syringe and draw up 20 mL of water
- 2. Swirl gently to allow for a quick dispersal
- 3. After the tablet has dispersed, administer the contents immediately into the mouth; do not save the water and microgranule mixture for later use
- 4. Refill the syringe with approximately 10 mL of water, swirl gently, and administer any remaining contents
- 5. Refill the syringe again with approximately 10 mL of water, swirl gently, and administer any remaining contents
- Preparing ODT with water for NG tube administration
- 1. Place one tablet in a catheter-tip syringe and draw up 20 mL of water
- 2. Shake gently to allow for a quick dispersal
- 3. After the tablet has dispersed, swirl the catheter-tip syringe gently in order to keep the microgranules from settling, and immediately inject the mixture through the NG tube into the stomach; do not save the water and microgranule mixture for later use
- 4. Refill the catheter-tip syringe with approximately 10 mL of water, shake gently, and flush the tube
- 5. Refill the catheter-tip syringe again with 10 mL of water, swirl gently, and administer
Missed doses
- If a dose is missed, administer as soon as possible; however, if the next scheduled dose is due, do not take the missed dose, and take the next dose on time
- Do not take 2 doses at one time to make up for a missed dose
