DEXLANSOPRAZOLE
Clinical safety rating: safe
Animal studies have demonstrated safety
Proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell.
| Metabolism | Hepatic via CYP2C19 and CYP3A4; also via sulfotransferase (SULT2A1) and glutathione S-transferase (GST). |
| Excretion | Renal: 0% unchanged; metabolites eliminated via urine (51%) and feces (48%) |
| Half-life | 1-2 hours; clinical context: duration of acid suppression exceeds half-life due to binding to proton pumps |
| Protein binding | 97% bound; primarily to albumin |
| Volume of Distribution | 0.5-0.7 L/kg; indicates moderate tissue distribution |
| Bioavailability | Oral: 70-80% (fasting); food reduces peak concentration but area under curve unchanged |
| Onset of Action | Oral: 1-2 hours for symptom relief; maximal acid suppression in 2-4 hours |
| Duration of Action | 24 hours; due to prolonged binding to gastric H+/K+-ATPase, allowing once-daily dosing |
30 mg orally once daily for 4 weeks for healing of erosive esophagitis; maintenance therapy: 30 mg orally once daily for up to 6 months. For GERD: 30 mg orally once daily for 4 weeks.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dosage adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, maximum dose is 30 mg daily. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: maximum dose 30 mg daily. Child-Pugh Class C: not recommended. |
| Pediatric use | For children 1-11 years: weight <30 kg: 15 mg once daily for up to 8 weeks; weight ≥30 kg: 30 mg once daily for up to 8 weeks. For children 12-17 years: 30 mg once daily for up to 8 weeks for GERD; for healing of erosive esophagitis, 30 mg once daily for up to 8 weeks. |
| Geriatric use | No specific adjustment except to monitor for increased risk of Clostridioides difficile infection, bone fracture, and vitamin B12 deficiency with long-term use. Maximum daily dose should not exceed 30 mg. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Can reduce absorption of drugs requiring gastric pH for absorption (eg ketoconazole) May increase risk of Clostridium difficile-associated diarrhea and bone fractures with long-term use.
| Breastfeeding | Excreted in human milk at low levels (M/P ratio unknown). No adverse effects reported in breastfed infants. Use caution; consider risk versus benefit. |
| Teratogenic Risk | Category B. No evidence of teratogenicity in animal studies. Insufficient human data for first trimester; risk cannot be excluded. Second and third trimester: no known increased risk of major malformations. May cause hypocalcemia, skeletal fractures in offspring with prolonged use near delivery. |
■ FDA Black Box Warning
None
| Common Effects | erosive esophagitis |
| Serious Effects |
["Hypersensitivity to dexlansoprazole or any component of the formulation","Co-administration with rilpivirine"]
| Precautions | ["Atrophic gastritis (observed with long-term use)","Increased risk of osteoporosis-related fractures (hip, wrist, spine)","Hypomagnesemia (may require monitoring, especially in patients on prolonged therapy or with digoxin, diuretics)","Vitamin B12 deficiency (prolonged use)","Clostridium difficile-associated diarrhea","Lupus erythematosus (cutaneous or systemic) associated with PPIs","Potential interference with absorption of drugs dependent on gastric pH (e.g., ketoconazole, atazanavir, iron salts, erlotinib)","Acute interstitial nephritis (may occur at any time during therapy)","Cyanocobalamin (Vitamin B12) deficiency"] |
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| Fetal Monitoring | Monitor maternal serum gastrin levels if prolonged use; assess bone mineral density if therapy exceeds 1 year. Fetal monitoring not routinely indicated. |
| Fertility Effects | No data on human fertility effects. Animal studies show no impairment of fertility at therapeutic doses. |