DEXILANT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEXILANT (DEXILANT).
Dexlansoprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of gastric parietal cells.
| Metabolism | Primarily metabolized by CYP2C19 and CYP3A4 to inactive metabolites. |
| Excretion | Renal (approximately 50% as inactive metabolites) and fecal (approximately 50% as inactive metabolites). |
| Half-life | Terminal elimination half-life is 1–2 hours in healthy subjects, but due to prolonged gastric acid suppression via irreversible binding to proton pumps, duration of action exceeds 24 hours. Half-life is not directly correlated with pharmacodynamic effect. |
| Protein binding | Approximately 96–98% bound to human plasma proteins, primarily albumin. |
| Volume of Distribution | Apparent volume of distribution is about 40 L (0.57 L/kg based on 70 kg), indicating distribution into total body water and some tissue binding. |
| Bioavailability | Oral bioavailability is approximately 30–40% due to first-pass metabolism. The delayed-release formulation protects the drug from gastric acid degradation. |
| Onset of Action | Oral (delayed-release capsule): Acid suppression begins within 1 hour, with maximal effect within 2–4 hours. |
| Duration of Action | Gastric acid suppression persists for >24 hours after a single dose, allowing once-daily dosing. Full effect on intragastric pH is achieved after 3–5 days of continued administration. |
30 mg orally once daily for up to 8 weeks; for healing esophagitis, 60 mg orally once daily for up to 8 weeks; maintenance 30 mg orally once daily.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; not studied in severe renal impairment (CrCl <30 mL/min), use caution. |
| Liver impairment | Child-Pugh A and B: no adjustment; Child-Pugh C: maximum dose 30 mg orally once daily. |
| Pediatric use | Not approved for pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use lowest effective dose for shortest duration due to potential increased risk of fractures and Clostridium difficile infection. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DEXILANT (DEXILANT).
| Breastfeeding | There is no information regarding the presence of dexlansoprazole in human milk, effects on the breastfed infant, or effects on milk production. Dexlansoprazole and its metabolites are excreted in milk in rats. The M/P ratio is unknown in humans. Because many drugs are excreted in human milk, caution should be exercised when DEXILANT is administered to a nursing woman. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for DEXILANT and any potential adverse effects on the breastfed child from DEXILANT or from the underlying maternal condition. |
| Teratogenic Risk | Dexlansoprazole (DEXILANT) is a proton pump inhibitor (PPI). Available data from epidemiologic studies over several thousand pregnant women do not indicate a significantly increased risk of major birth defects or other adverse pregnancy outcomes with PPI use, including dexlansoprazole. However, there is no human data for dexlansoprazole specifically; data are extrapolated from other PPIs. In animal reproduction studies, no adverse developmental effects were observed at doses up to 1.5 times the maximum recommended human dose (MRHD) based on AUC. Because animal studies are not always predictive of human response, dexlansoprazole should be used during pregnancy only if clearly needed. First-trimester exposure: No increased risk of major congenital malformations. Second and third trimesters: No specific risks identified; monitor for any potential effects on fetal growth and development (limited data). |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to dexlansoprazole or any component of the formulation","Concomitant use with rilpivirine-containing products"]
| Precautions | ["Gastric malignancy: Symptomatic response does not preclude presence of gastric malignancy","Acute interstitial nephritis observed in patients taking PPIs","Clostridium difficile-associated diarrhea: PPI use increases risk","Bone fracture: Long-term PPI use associated with increased risk of osteoporosis-related fractures","Hypomagnesemia: Reported with prolonged PPI use; monitor magnesium levels","Cyanocobalamin (Vitamin B12) deficiency: Long-term PPI use may reduce absorption","Interaction with methotrexate: Concomitant use may increase methotrexate toxicity","Interaction with rilpivirine: Contraindicated with products containing rilpivirine"] |
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| Fetal Monitoring | No specific clinical monitoring is routinely required for pregnant women receiving dexlansoprazole beyond standard prenatal care. As a PPI, chronic use may be associated with increased risk of Clostridium difficile-associated diarrhea and bone fracture; monitor for signs of these if therapy is prolonged. In pregnancy, monitor for potential vitamin B12 deficiency with long-term therapy. No fetal monitoring specific to dexlansoprazole is indicated. |
| Fertility Effects | There are no human data on the effect of dexlansoprazole on fertility. Animal studies in rats at doses up to 30 mg/kg/day (approximately 0.97 times the MRHD based on body surface area) showed no adverse effects on fertility or reproductive performance. |