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 |
| Molecular Weight | 369.36 |
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 | Limited data; avoid unless clearly needed. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. |
| 2nd trimester | No evidence of risk from human studies; use only if clearly needed. |
| 3rd trimester | May be used if necessary; no known fetal risk. |
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.
| Placental transfer | Crosses placenta in animal studies; human data insufficient. |
| Breastfeeding | Excretion into human milk is unknown; however, dexlansoprazole is a proton pump inhibitor with high protein binding and short half-life, likely minimal excretion. Consider risk-benefit; alternatives may be preferred. |
■ FDA Black Box Warning
None
| Common Effects | erosive esophagitis |
| Serious Effects |
Hypersensitivity to dexlansoprazole or any component of the formulationConcomitant use with rilpivirine-containing products
| 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 |
| Food/Dietary |
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| Lactation Rating | L3 (Limited Data) or 'Probably Compatible' |
| 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. |
| 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. |
| Dexlansoprazole can be taken with or without food. The absorption is not significantly affected by food, so no specific dietary restrictions are required. However, high-fat meals may slightly delay absorption but do not reduce overall exposure. Avoid grapefruit products as they may inhibit CYP3A4, potentially increasing dexlanoprazole levels; however, clinical significance is low. Limit alcohol and caffeine as they may aggravate GERD symptoms. |
| Clinical Pearls | Dexlansoprazole is the R-enantiomer of lansoprazole with a dual delayed-release formulation providing prolonged acid suppression. Administer without regard to meals; do not crush or chew capsules. Onset of symptom relief is within hours but maximal acid suppression takes 2-4 days. For healing of erosive esophagitis, 8-week course is typical; maintenance therapy may be needed. Monitor for hypomagnesemia with prolonged use, especially in patients on diuretics. Consider CYP2C19 genetic testing if therapeutic failure occurs, as poor metabolizers have higher exposure. Avoid concomitant use with clopidogrel due to reduced efficacy of clopidogrel. Use with caution in patients with osteoporosis risk due to potential for increased fracture risk with long-term high-dose therapy. |
| Patient Advice | Take dexlanoprazole exactly as prescribed, usually once daily; it can be taken with or without food. · Swallow the capsule whole; do not crush, chew, or open it. If you have trouble swallowing, the capsule can be opened and the granules sprinkled on applesauce, then swallowed immediately. · If you miss a dose, take it as soon as you remember unless it is almost time for the next dose. Do not double the dose. · Common side effects include diarrhea, stomach pain, nausea, and headache. Contact your doctor if you experience severe diarrhea, joint pain, or a rash. · Long-term use may increase the risk of vitamin B12 deficiency, bone fractures (especially hip, wrist, or spine), and low magnesium levels. Notify your doctor if you have symptoms of low magnesium (muscle spasms, irregular heartbeat, seizures). · Do not take this medication with clopidogrel (Plavix) unless directed by your doctor, as it may reduce the effectiveness of clopidogrel. · Tell your doctor about all other medications you take, including over-the-counter drugs, supplements, and antacids. |