LANSOPRAZOLE
Clinical safety rating: safe
Animal studies have demonstrated safety
Proton pump inhibitor that inhibits gastric acid secretion by binding to the H+/K+ ATPase enzyme (proton pump) in gastric parietal cells, preventing the final step of acid production.
| Metabolism | Primarily metabolized by CYP2C19 and CYP3A4 to inactive metabolites; undergoes significant first-pass metabolism. |
| Excretion | Renal (14-23% as metabolites); biliary/fecal (major route, ~60% as metabolites and parent drug). |
| Half-life | Terminal elimination half-life: 1.5-2 hours (increased to 3-6 hours in elderly, hepatic impairment). |
| Protein binding | 97% bound to albumin. |
| Volume of Distribution | 0.3 L/kg (indicates distribution into total body water). |
| Bioavailability | Oral: 80-90% (first-pass metabolism minimal). |
| Onset of Action | Oral: 1-2 hours (single dose); IV: 30 minutes. |
| Duration of Action | Acid suppression persists >24 hours due to prolonged binding to proton pumps; dosing once daily. |
15-30 mg orally once daily; 30 mg IV over 30 minutes once daily (when oral not possible).
| Dosage form | CAPSULE, DELAYED REL PELLETS |
| Renal impairment | No dose adjustment required in renal impairment. Hemodialysis does not remove lansoprazole; no supplemental dose needed. |
| Liver impairment | Moderate to severe hepatic impairment (Child-Pugh B or C): reduce dose to 15 mg orally once daily. |
| Pediatric use | 1-11 years (≤30 kg): 15 mg orally once daily; >30 kg: 30 mg orally once daily. 12-17 years: 15-30 mg orally once daily. |
| Geriatric use | No specific dose adjustment, but consider lower starting dose (15 mg daily) due to decreased hepatic function and prolonged half-life in elderly. |
| 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 | Lansoprazole is excreted in human milk, but the M/P ratio is not well established. Limited data show low levels in breast milk; likely compatible with breastfeeding. Use with caution in premature infants or neonates. |
| Teratogenic Risk | In the first trimester, limited data suggest no major increase in congenital malformations (minor risk or none). Second and third trimesters: no specific fetal toxicity reported; however, consider potential for hypocalcemia and reduced vitamin B12 absorption with prolonged use. |
■ FDA Black Box Warning
None.
| Common Effects | erosive esophagitis |
| Serious Effects |
["Hypersensitivity to lansoprazole or any component of the formulation.","Concomitant use with rilpivirine-containing products."]
| Precautions | ["Increased risk of Clostridium difficile-associated diarrhea, bone fracture (hip, wrist, spine) with long-term use, hypomagnesemia with prolonged treatment, vitamin B12 deficiency with chronic use, and acute interstitial nephritis.","May mask symptoms of gastric malignancy.","Interaction with clopidogrel: potential reduced antiplatelet effect (controversial)."] |
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| Fetal Monitoring | Maternal monitoring: For long-term use, monitor magnesium levels, vitamin B12 levels, and bone density. Fetal monitoring: Routine obstetric ultrasound; no specific additional monitoring required. |
| Fertility Effects | No known adverse effects on fertility in humans. In animal studies, no impairment of fertility observed. |