Lansoprazole (Monograph)

Brand names: Prevacid, Prevpac
Drug class: Proton-pump Inhibitors

Medically reviewed by Drugs.com on Jun 10, 2024. Written by ASHP.

Introduction

Acid- or proton-pump inhibitor; gastric antisecretory agent.

Uses for Lansoprazole

Gastroesophageal Reflux (GERD)

Short-term treatment of symptomatic GERD (e.g., heartburn).

Short-term treatment of erosive esophagitis (endoscopically diagnosed) in patients with GERD.

Maintain healing and decrease recurrence of erosive esophagitis.

Short-term self-medication for symptomatic relief of frequent (e.g., ≥2 days per week) heartburn in adults ≥18 years of age.

Duodenal Ulcer

Short-term treatment of active duodenal ulcer (endoscopically or radiographically confirmed).

Treatment of Helicobacter pylori infection and duodenal ulcer disease. Used in conjunction with amoxicillin and clarithromycin (triple therapy) or clarithromycin (dual therapy); has been used in other multidrug regimens^{† [off-label]}.

Maintenance therapy following duodenal ulcer healing.

Gastric Ulcer

Short-term treatment and symptomatic relief of active benign gastric ulcer.

NSAIA-induced Gastric Ulcer

Short-term treatment of NSAIA-induced gastric ulcer in patients continuing NSAIA use.

Risk reduction in patients with history of gastric ulcer who require NSAIA treatment.

Pathologic GI Hypersecretory Conditions

Long-term treatment of pathologic hypersecretory conditions (e.g., Zollinger-Ellison syndrome with or without multiple endocrine adenoma).

Crohn’s Disease-associated Ulcers

Some evidence for use of proton-pump inhibitors (e.g., omeprazole) for gastric acid suppressive therapy as an adjunct in the management of upper GI Crohn’s disease^{† [off-label]}, including esophageal, gastroduodenal, and jejunoileal disease.

Lansoprazole Dosage and Administration

Administration

Administer orally. Has been used administered IV (parenteral dosage form no longer commercially available in US).

If a dose is missed, administer the dose as soon as possible, unless it is almost time for the next dose. Do not double a dose to make up for a missed dose.

Administer orally before a meal.

Antacids may be used concomitantly as needed for pain relief.

Extemporaneously Compounded Oral Suspension

An extemporaneously compounded 3 mg/mL oral suspension of lansoprazole has been prepared using the commercially available capsules and an 8.4% sodium bicarbonate vehicle. An extemporaneous suspension also has been prepared by pulverizing one 30-mg enteric-coated microgranule tablet in 10 mL of Ora-Blend to provide a suspension containing 3 mg/mL.

Standardize 4 Safety

Standardized concentrations for an extemporaneously prepared oral suspension of lansoprazole have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care. Because recommendations from the S4S panels may differ from the manufacturer’s prescribing information, caution is advised when using concentrations that differ from labeling, particularly when using rate information from the label . For additional information on S4S (including updates that may be available), see [Web].

Table 1: Standardize 4 Safety Compounded Oral Liquid Standards for Lansoprazole252
Concentration Standards
3 mg/mL

Capsules

Swallow capsules intact; do not chew or crush.

Alternatively, open capsule and sprinkle contents on 1 tablespoonful of compatible foods (e.g., applesauce, Ensure pudding, cottage cheese, yogurt, strained pears) or mix with about 60 mL of appropriate juice (e.g., apple juice, orange juice, tomato juice); swallow immediately without chewing. If mixed with juice, rinse glass with ≥120 mL juice and swallow immediately to ensure complete dose ingestion. Do not mix with other foods or liquids.

Manufacturer recommends swallowing capsules for self-medication with a glass of water.

Orally Disintegrating Tablets

Do not break, cut, or chew orally disintegrating tablets. Place tablets on the tongue and allow to disintegrate (usually in <1 minute) with or without water; swallow particles without chewing.

To administer using an oral syringe, place 15- or 30-mg tablet in oral syringe, draw up about 4 or 10 mL, respectively, of water in the syringe, gently shake syringe to ensure rapid dispersal of particles, and administer within 15 minutes. To ensure complete consumption of dose, draw up an additional 2 mL (15-mg dose) or 5 mL (30-mg dose) of water in syringe, mix gently, and administer remaining contents.

NG Tube

Capsules: Open capsule and mix contents with about 40 mL apple juice and administer immediately (within 3–5 minutes) through NG tube; flush tube with additional apple juice. Do not mix with other liquids.

Orally disintegrating tablets: Place 15- or 30-mg tablet in syringe, draw up about 4 or 10 mL, respectively, of water in the syringe, gently shake syringe to ensure rapid dispersal of particles, and administer within 15 minutes through NG tube (8 French or larger). Draw up an additional 5 mL of water in syringe, mix gently, and flush NG tube with syringe contents.

Dosage

Pediatric Patients

Gastroesophageal Reflux

GERD

Oral

Children 1–11 years of age: In those weighing ≤30 kg, 15 mg once daily for up to 12 weeks. In those weighing >30 kg, 30 mg once daily for up to 12 weeks. Dosage has been increased up to 30 mg twice daily after ≥2 weeks in patients remaining symptomatic.

Children 12–17 years of age: 15 mg daily for up to 8 weeks.

Treatment of Erosive Esophagitis

Oral

Children 12–17 years of age: 30 mg daily for up to 8 weeks.

Adults

Gastroesophageal Reflux

Chronic, lifelong therapy with proton-pump inhibitor is appropriate for many GERD patients.

GERD

Oral

15 mg once daily for up to 8 weeks.

Treatment of Erosive Esophagitis

Oral

30 mg once daily for up to 8 weeks. May give additional 8 weeks of therapy (up to 16 weeks for a single course) if not healed. If recurs, consider additional 8 weeks of therapy.

Maintenance of Healing of Erosive Esophagitis

Oral

15 mg once daily. Not studied >1 year.

Self-medication for Frequent Heartburn

Oral

15 mg once daily in the morning for 14 days. Do not exceed recommended dosage or duration; do not administer more than 1 course every 4 months. May relieve symptoms within 24 hours, but 1–4 days may be required for complete relief.

Duodenal Ulcer

Treatment of Active Duodenal Ulcer

Oral

15 mg once daily for 4 weeks.

Treatment of Helicobacter pylori Infection and Duodenal Ulcer

Oral

Triple therapy: 30 mg every 12 hours for 10 or 14 days in conjunction with amoxicillin and clarithromycin.

Dual therapy: 30 mg every 8 hours for 14 days in conjunction with amoxicillin.

Maintenance of Duodenal Ulcer Healing

Oral

15 mg daily. Safety and efficacy beyond 1 year not established.

Gastric Ulcer

Benign Gastric Ulcer

Oral

30 mg once daily for up to 8 weeks.

NSAIA-induced Gastric Ulcer

Treatment

Oral

30 mg once daily for 8 weeks.

Risk Reduction

Oral

15 mg once daily for up to 12 weeks.

Pathologic GI Hypersecretory Conditions (e.g., Zollinger-Ellison Syndrome)

Oral

60 mg once daily initially. Adjust dosage according to patient response and tolerance; continue therapy as long as necessary. May require dosages of up to 90 mg twice daily. Administer daily dosages >120 mg in divided doses. Patients with Zollinger-Ellison syndrome have been treated for up to 4 years.

Special Populations

Hepatic Impairment

Consider dosage reduction in patients with severe hepatic impairment.

Renal Impairment

Lansoprazole dosage adjustment not necessary. Kit containing lansoprazole, amoxicillin, and clarithromycin (Prevpac) not recommended for use in patients with Cl_cr <30 mL/minute.

Geriatric Patients

Lansoprazole dosage adjustment not necessary.

Cautions for Lansoprazole

Contraindications

Known severe hypersensitivity to lansoprazole or any ingredient in the formulation.

Warnings/Precautions

Gastric Malignancy

Response to lansoprazole therapy does not preclude presence of occult gastric neoplasm.

Clostridium difficile Infection

Proton-pump inhibitors associated with possible increased (1.4–2.75 times) risk of Clostridium difficile infection, including C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis). Many patients also had other risk factors for CDAD. May be severe; colectomy and, rarely, death reported.

Use the lowest effective dosage and shortest duration of therapy appropriate for the patient's clinical condition.

Consider CDAD if persistent diarrhea develops and manage accordingly; initiate supportive therapy (e.g., fluid and electrolyte management), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.

Phenylketonuria

Each 15- or 30-mg Prevacid Solu-Tab™ orally disintegrating tablet contains aspartame, which is metabolized in the GI tract to provide 2.5 or 5.1 mg of phenylalanine, respectively.

Respiratory Effects

Administration of proton-pump inhibitors has been associated with an increased risk for developing certain infections (e.g., community-acquired pneumonia).

Bone Fracture

Several observational studies suggest that use of proton-pump inhibitors, particularly in high dosages (i.e., multiple daily doses) and/or for prolonged periods of time (i.e., ≥1 year), may be associated with increased risk of osteoporosis-related fractures of the hip, wrist, or spine. Magnitude of risk is unclear; causality not established. FDA is continuing to evaluate this safety concern.

Use the lowest effective dosage and shortest duration of therapy appropriate for the patient’s clinical condition.

Individuals at risk for osteoporosis-related fractures should receive an adequate intake of calcium and vitamin D; assess and manage these patients’ bone health according to current standards of care.

Hypomagnesemia

Hypomagnesemia, symptomatic and asymptomatic, reported rarely in patients receiving long-term therapy (≥3 months or, in most cases, >1 year) with proton-pump inhibitors, including lansoprazole. Serious adverse effects include tetany, seizures, tremors, carpopedal spasm, arrhythmias (e.g., atrial fibrillation, supraventricular tachycardia), and abnormal QT interval. Paresthesia, muscle weakness, muscle cramps, lethargy, fatigue, and unsteadiness may occur. Most patients required magnesium replacement and discontinuance of the proton-pump inhibitor. Hypomagnesemia resolved within 1 week (median) following discontinuance and recurred within 2 weeks (median) of rechallenge.

In patients expected to receive long-term proton-pump inhibitor therapy or in patients currently receiving digoxin or drugs that may cause hypomagnesemia (e.g., diuretics), consider measuring serum magnesium concentrations prior to initiation of prescription proton-pump inhibitor therapy and periodically thereafter.

Use of Combination Preparations

When kits containing lansoprazole and other agents (anti-infectives) are used, consider the cautions, precautions, and contraindications associated with the concomitant agent(s).

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk in rats; not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy of oral lansoprazole established for short-term treatment of symptomatic GERD and erosive esophagitis in patients 1–17 years of age.

Oral lansoprazole is not recommended in infants <1 year of age; the drug was no more effective than placebo in a controlled study in infants 1 month to <1 year of age with symptomatic GERD.

Safety and efficacy for self-medication of frequent heartburn not established in children <18 years of age.

Geriatric Use

No substantial differences in efficacy and safety of oral lansoprazole in geriatric patients relative to younger adults.

Hepatic Impairment

Increased systemic exposure (AUC) and decreased clearance. Consider dosage reduction in patients with severe hepatic impairment.

Common Adverse Effects

In children 1–11 years of age, constipation and headache. In children 12–17 years of age, headache, abdominal pain, nausea, dizziness. Pediatric adverse effect profile similar to that in adults.

In adults receiving oral lansoprazole, diarrhea, abdominal pain, nausea, constipation.

Drug Interactions

Metabolized by CYP2C19 and CYP3A.

Drugs Metabolized by Hepatic Microsomal Enzymes

Unlikely to have clinically important interaction with drugs metabolized by CYP3A, 1A2, 2C9, 2C19, 2D6.

Drugs that Cause Hypomagnesemia

Potential pharmacologic interaction (possible increased risk of hypomagnesemia). Consider monitoring magnesium concentrations prior to initiation of prescription proton-pump inhibitor therapy and periodically thereafter. (See Hypomagnesemia under Cautions.)

Specific Drugs

Drug	Interaction	Comments
Amoxicillin	No evidence of clinically important interaction
Antacids	Administered concomitantly with lansoprazole in clinical studies
Antipyrine	No evidence of clinically important interaction
Atazanavir	Possible altered oral absorption of atazanavir, resulting in decreased plasma atazanavir concentrations; possible loss of virologic response	Manufacturer of lansoprazole states that concomitant administration with atazanavir is not recommended Antiretroviral treatment-naive patients: If a proton-pump inhibitor is used concomitantly with atazanavir, administer ritonavir-boosted atazanavir (atazanavir 300 mg and ritonavir 100 mg once daily with food); administer the proton-pump inhibitor approximately 12 hours before ritonavir-boosted atazanavir For treatment-naive patients, dosage of proton-pump inhibitor should not exceed omeprazole 20 mg daily (or equivalent) Antiretroviral treatment-experienced patients: Concomitant use of proton-pump inhibitors with atazanavir not recommended
Clarithromycin	No evidence of clinically important interaction
Clopidogrel	Certain CYP2C19 inhibitors (e.g., omeprazole, esomeprazole) reduce exposure to clopidogrel’s active metabolite and decrease platelet inhibitory effects; potentially may reduce clopidogrel’s clinical efficacy. Dexlansoprazole, lansoprazole, or pantoprazole had less effect on clopidogrel's antiplatelet activity than did omeprazole or esomeprazole; Lansoprazole decreased exposure to the metabolite by about 14%; observed effects on metabolite exposure and clopidogrel-induced platelet inhibition not considered clinically important	Manufacturer of lansoprazole states clopidogrel dosage adjustment not required if used with recommended lansoprazole dosages Assess risks and benefits of concomitant proton-pump inhibitor and clopidogrel use in individual patients American College of Cardiology Foundation/American College of Gastroenterology/American Heart Association (ACCF/ACG/AHA) states that GI bleeding risk reduction with concomitant proton-pump inhibitor in patients with risk factors for GI bleeding (e.g., advanced age; concomitant use of warfarin, corticosteroids, or NSAIAs); H. pylori infection) may outweigh potential reduction in cardiovascular efficacy of antiplatelet treatment associated with a drug-drug interaction. In patients without such risk factors, ACCF/ACG/AHA states that risk/benefit balance may favor use of antiplatelet therapy without a proton-pump inhibitor. If concomitant therapy with a proton-pump inhibitor and clopidogrel is deemed necessary, consider using an agent with little or no CYP2C19-inhibitory activity; alternatively, consider using a histamine H₂-receptor antagonist (ranitidine, famotidine, nizatidine) but not cimetidine (also a potent CYP2C19 inhibitor)
Diazepam	No evidence of clinically important interaction
Digoxin	Hypomagnesemia (e.g., resulting from long-term use of proton-pump inhibitors) sensitizes the myocardium to digoxin and, thus, may increase risk of digoxin-induced cardiotoxic effects See table entry for gastric pH-dependent drugs	Consider monitoring magnesium concentrations prior to initiation of prescription proton-pump inhibitor therapy and periodically thereafter
Diuretics (i.e., loop or thiazide diuretics)	Possible increased risk of hypomagnesemia	Consider monitoring magnesium concentrations prior to initiation of prescription proton-pump inhibitor therapy and periodically thereafter
Fosamprenavir	Use of esomeprazole with fosamprenavir (with or without ritonavir) did not substantially affect concentrations of amprenavir (active metabolite of fosamprenavir)	No dosage adjustment required when proton-pump inhibitors used with fosamprenavir (with or without ritonavir)
Gastric pH-dependent drugs (e.g., ampicillin esters, digoxin, iron salts, ketoconazole)	Lansoprazole may alter drug absorption
Ibuprofen	No evidence of clinically important interaction
Indomethacin	No evidence of clinically important interaction
Lopinavir	Lopinavir/ritonavir: Omeprazole had no clinically important effect on plasma concentrations or AUC of lopinavir	No dosage adjustment required when proton-pump inhibitors used with lopinavir/ritonavir
Methotrexate	Possible delayed clearance and increased serum concentrations of methotrexate and/or its metabolite hydroxymethotrexate; possible methotrexate toxicity Reported mainly with high-dose methotrexate (300 mg/m² to 12 g/m²), but also reported with low dosages (e.g., 15 mg per week)	Manufacturer of lansoprazole recommends considering temporary discontinuance of proton-pump inhibitor therapy in some patients receiving high-dose methotrexate Some clinicians recommend withholding the proton-pump inhibitor for several days before and after administration of either high-dose or low-dose methotrexate or, alternatively, substituting a histamine H₂-receptor antagonist for the proton-pump inhibitor
Phenytoin	No evidence of clinically important interaction
Prednisone	No evidence of clinically important interaction
Propranolol	No evidence of clinically important interaction
Raltegravir	Omeprazole increased peak plasma concentration and AUC of raltegravir	No dosage adjustment recommended when proton-pump inhibitors used with raltegravir
Rilpivirine	Omeprazole decreased plasma concentrations and AUC of rilpivirine	Concomitant use of rilpivirine and proton-pump inhibitors contraindicated
Saquinavir	Ritonavir-boosted saquinavir: Omeprazole increased peak plasma concentration and AUC of saquinavir	Caution advised if proton-pump inhibitor used with ritonavir-boosted saquinavir; monitor for saquinavir toxicity
Sucralfate	Lansoprazole absorption delayed, bioavailability decreased	Administer at least 30 minutes before sucralfate
Tacrolimus	Possible increased concentrations of tacrolimus, particularly in transplant patients who are intermediate or poor metabolizers of CYP2C19 substrates
Theophylline	Minor increase in theophylline clearance	Usually not clinically important; may require theophylline dosage adjustment when lansoprazole is initiated or discontinued
Warfarin	May increase PT and INR	May need to monitor PT and INR

Lansoprazole Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract (absolute bioavailability >80%). Peak plasma concentrations attained about 1.7 hours after oral administration.

Onset

Increased gastric pH occurred within 1–2 or 2–3 hours after a single 30- or 15-mg oral dose, respectively.

Duration

Gastric acid secretion normalized over 2–4 days after discontinuance; no apparent rebound.

Food

Absorption (peak plasma concentration, AUC) decreased by 50–70% when administered 30 minutes after food. No substantial food effect when administered before meals.

Special Populations

Peak plasma concentration and time to peak plasma concentration in patients with renal impairment similar to healthy individuals.

Peak plasma concentrations were comparable in patients in Asian and US studies.

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.

Prolonged binding to gastric parietal proton pump enzyme.

Plasma Protein Binding

97%.

Special Populations

Severe renal impairment decreased plasma protein binding by 1–1.5% after administration of 60 mg dose.

Elimination

Metabolism

In parietal cell secretory canaliculi, thought to be transformed into 2 active sulfenamide metabolites not present in systemic circulation. Also metabolized in the liver by CYP3A and CYP2C19. Metabolites found in plasma are inactive.

Lansoprazole is a racemic mixture of R- and S-isomers. Plasma clearance of the R-isomer (dexlansoprazole) is slower than that of the S-isomer; plasma concentrations of the R-isomer are markedly higher than those of the S-isomer.

Elimination Route

Excreted principally in feces (about 67%) with remainder in urine; no unchanged drug excreted in urine.

Half-life

<2 hours.

Special Populations

Hepatic impairment increased plasma half-life to 3.2–7.2 hours.

Renal impairment decreased elimination half-life.

Stability

Storage

Oral

Capsules and Orally Disintegrating Tablets

25°C (may be exposed to 15–30°C).

Capsules for Self-medication

20–25°C; protect from high heat, humidity, and moisture.

Prevpac Kit

20–25°C. Protect from light and moisture.

Compatibility

Oral

Capsules

Immediately use extemporaneous mixtures of capsule contents and food or juice. (See Oral Administration under Dosage and Administration.)

Actions

Inhibits basal and stimulated gastric acid secretion.
Concentrates in acid conditions of parietal cell secretory canaliculi; forms active sulfenamide metabolite that irreversibly binds to and inactivates hydrogen-potassium ATPase (proton or acid pump), blocking final step in secretion of hydrochloric acid.
Acid secretion is inhibited until additional hydrogen-potassium ATPase is synthesized, resulting in prolonged duration of action.
Lansoprazole is a racemic mixture of R- and S-isomers. Both isomers inhibit hydrogen-potassium ATPase.
Combined therapy with lansoprazole and appropriate anti-infectives (i.e., amoxicillin, clarithromycin) can effectively eradicate H. pylori infection.

Advice to Patients

Importance of taking before a meal.
Importance of swallowing capsule intact, without crushing or chewing.
For orally disintegrating tablets, importance of allowing tablet to dissolve on tongue with or without water, then swallowing particles without chewing.
If capsule contents are mixed with food or juice, importance of immediately swallowing mixture without crushing or chewing.
Importance of advising patients that use of multiple daily doses of the drug for an extended period of time may increase the risk of fractures of the hip, wrist, or spine.
Risk of hypomagnesemia; importance of immediately reporting and seeking care for any cardiovascular or neurologic manifestations (e.g., palpitations, dizziness, seizures, tetany).
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs. Antacids may be used concomitantly as needed for pain relief.
Importance of women informing their clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients with phenylketonuria that orally disintegrating tablets contain aspartame.
Possible increased risk of Clostridium difficile infection; importance of contacting a clinician if persistent watery stools, abdominal pain, and fever occur.
Importance of following dosage instructions when lansoprazole is used for self-medication. Advise patients that they should use the drug for self-medication only as directed for no longer than 14 days of continuous use and that they should not exceed one course of therapy every 4 months.

Importance of discontinuing use as self-medication and consulting a clinician if heartburn persists or worsens, use of the drug for >14 days is needed, or >1 course of therapy is required every 4 months.
Self-medication with lansoprazole is not intended for immediate relief of heartburn; may relieve symptoms within 24 hours, but 1–4 days may be required for complete relief.
Advise patients to consult their clinician before using lansoprazole for self-medication if they have liver disease, have had heartburn for >3 months, or are experiencing heartburn with lightheadedness, dizziness, or sweating; chest or shoulder pain with shortness of breath, sweating, lightheadedness, or pain spreading to the arms, neck, or shoulders; frequent chest pain; frequent wheezing (especially with heartburn); unexplained weight loss; nausea or vomiting; or stomach pain.
Advise patients not to use lansoprazole for self-medication and to consult a clinician if they have difficulty or pain with swallowing, are vomiting blood, or have bloody or blackened stools.
Importance of informing patients of other important precautionary information. (See Cautions.)

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Lansoprazole
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules, delayed-release (containing enteric-coated granules)	15 mg*	Lansoprazole Delayed-Release Capsules
			Prevacid	Takeda
			Prevacid 24HR	Novartis
		30 mg*	Lansoprazole Delayed-Release Capsules
			Prevacid	Takeda
	Tablets, delayed-release (containing enteric-coated microgranules), orally disintegrating	15 mg	Prevacid SoluTab	Takeda
		30 mg	Prevacid SoluTab	Takeda

Lansoprazole Combinations
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Kit	4 Capsules, Amoxicillin (trihydrate) 500 mg (of amoxicillin) 2 Capsules, delayed-release (containing enteric-coated granules), Lansoprazole, 30 mg (Prevacid) 2 Tablets, film-coated, Clarithromycin, 500 mg (Biaxin Filmtab)	Prevpac	Takeda