Lansoprazole

Pronunciation: (lan-SO-pruh-zole)
Class: Helicobacter pylori agent, Proton pump inhibitor

Trade Names:
Prevacid
- Tablets, orally disintegrating, delayed-release 15 mg
- Tablets, orally disintegrating, delayed-release 30 mg
- Capsules, delayed-release 15 mg
- Capsules, delayed-release 30 mg
- Enteric-coated granules for oral suspension, delayed-release 15 mg
- Enteric-coated granules for oral suspension, delayed-release 30 mg

Trade Names:
Prevacid I.V.
- Injection 30 mg per vial

Prevacid FasTab (Canada)

Pharmacology

Suppresses gastric acid secretion by blocking “acid (proton) pump” within gastric parietal cells.

Pharmacokinetics

Absorption

Absorption is rapid. T _max is approximately 1.7 h. C _max and AUC are approximately proportional in doses from 15 to 60 mg single dose administration. Absolute bioavailability is over 80%. C _max and AUC decrease 50% if given 30 min after food.

Distribution

Protein binding (97%) is constant over the concentration range of 0.05 to 5 mcg/mL.

Metabolism

Extensively metabolized in the liver. Metabolites are hydroxylated sulfonyl and sulfone derivatives (very little activity).

Elimination

Significant biliary excretion of the metabolites. Mean t _½ is 1.9 to 2.9 h.

Special Populations

Hepatic Function Impairment

Mean t _½ prolonged to 3.2 to 7.2 h and AUC increased up to 500%; dose reduction is recommended in severe hepatic disease.

Elderly

Cl is decreased with t _½ increasing approximately 50% to 100%. Because mean t _½ remains between 1.9 to 2.9 h, repeated once daily dosing does not accumulate; no adjustment needed.

Indications and Usage

Oral Short-term treatment of active duodenal ulcer; to maintain healing of duodenal ulcers; short-term treatment of all grades of erosive esophagitis; maintenance of healing of erosive esophagitis; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; in combination with amoxicillin plus clarithromycin or amoxicillin alone (in patients intolerant or resistant to clarithromycin) for the eradication of H. pylori in patients with active or recurrent duodenal ulcers; short-term treatment and symptomatic relief of active benign gastric ulcer (including NSAID-associated gastric ulcer in patients who continue NSAID use and for reducing risk of NSAID-associated gastric ulcer in patients with a history of NSAID-associated gastric ulcer); treatment of heartburn and other symptoms of gastroesophageal reflux disease (GERD). IV Short-term treatment (up to 7 days) of all grades of erosive esophagitis.

Contraindications

Standard considerations.

Dosage and Administration

Duodenal Ulcer
Adults

PO 15 mg/day for 4 wk.

Duodenal Ulcer (Healed) Maintenance
Adults

PO 15 mg/day.

Erosive Esophagitis
Adults

PO 30 mg/day for up to 8 wk, an additional 8 wk may be helpful for patients who do not heal. For maintenance, use 15 mg/day. IV 30 mg/day for up to 7 days.

Children 12 to 17 yr of age

PO 30 mg/day for up to 8 wk.

Children 1 to 11 yr of age

PO For children weighing over 30 kg, give 30 mg/day for up to 12 wk; for children weighing 30 kg or less, give 15 mg/day for up to 12 wk.

Gastric Ulcer
Adults

PO 30 mg/day for up to 8 wk.

GERD
Adults

PO 15 mg/day for up to 8 wk.

Children 12 to 17 yr of age

PO Nonerosive GERD: 15 mg once daily for up to 8 wk.

Children 1 to 11 yr of age

PO For children weighing over 30 kg, give 30 mg/day for up to 12 wk; for children weighing 30 kg or less, give 15 mg/day for up to 12 wk.

H. pylori
Adults

PO 30 mg lansoprazole plus 500 mg clarithromycin and 1 g amoxicillin twice daily for 10 to 14 days, or 1 g amoxicillin alone tid for 14 days.

Pathological Hypersecretory Conditions
Adults

PO Initial dose 60 mg/day. Dosages up to 90 mg twice daily have been administered. Divide daily doses of more than 120 mg.

General Advice

• Administer prescribed oral dose before a meal.

Delayed-release capsule

• The 15 mg delayed-release capsule contains phenylalanine. Do not administer to patient with phenylketonuria without first discussing with health care provider.
• Caution patient to swallow capsule whole and not crush or chew the capsule.
• If patient has difficulty swallowing capsule, the capsule may be opened and the contents sprinkled on 1 Tbsp applesauce, Ensure pudding, cottage cheese, yogurt, or strained pears. The mixture should be swallowed immediately without chewing the granules. The contents of the capsule may also be emptied into 2 oz apple juice, orange juice, or tomato juice, mixed briefly, then swallowed immediately without chewing the granules. The glass should be rinsed with 2 or more volumes of juice, and the contents swallowed immediately.
• Do not mix granules with any other food or liquid other than those noted above.

Delayed-release orally disintegrating tablet

• Have patient place tablet on tongue and allow it to disintegrate, with or without water, until the particles can be swallowed. Caution patient not to chew the tablet or particles that are released.
• For patients having difficulty using the orally disintegrating tablet, the tablet can be placed in an oral syringe and mixed with 4 mL water (15 mg tablet) or 10 mL water (30 mg tablet). Shake syringe gently to allow for a quick dispersal and administer dispersed contents orally or via nasogastric tube (#8 French or greater) within 15 min. If dispersion was administered orally, refill syringe with 2 mL water (15 mg tablet) or 5 mL water (30 mg tablet), shake gently, and administer any remaining contents. If dispersion was administered via nasogastric tube, refill syringe with 5 mL water, shake gently, and flush the nasogastric tube.

Delayed-release oral suspension

• Open packet and empty contents into container containing 2 Tbsp water. Stir well and drink immediately without chewing granules. If any material remains after drinking, add more water, stir, and drink immediately.
• Do not mix oral suspension with any liquid other than water or with food.
• Do not administer oral suspension via enteral administration tubes.

IV

• Reconstitute IV preparation with 5 mL sterile water for injection, then further dilute in 50 mL sodium chloride 0.9% injection, lactated Ringer's injection, or dextrose 5% injection.
• Administer once daily by infusing over a period of 30 min using the inline filter provided.
• Flush the IV line before and after administration with sodium chloride 0.9% injection, lactated Ringer's injection, or dextrose 5% injection.
• Do not administer with other drugs or diluents.

Storage/Stability

Store delayed-release capsules, oral suspension, and orally disintegrating tablets at controlled room temperature (59° to 86°F).

IV

Store the powder for injection at 77°F; protect from light. Store the reconstituted solution for up to 1 h at 77°F. Store the admixture at 77°F for up to 24 h (sodium chloride 0.9%, lactated Ringer's injection) or up to 12 h (dextrose 5% injection).

Drug Interactions

Digoxin

Increased digoxin absorption, leading to elevated levels and increased risk of toxicity may occur.

Ketoconazole

Effects may be decreased by lansoprazole.

Sucralfate

May delay and reduce absorption; give lansoprazole at least 30 min before sucralfate.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (more than 1%).

Dermatologic

Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).

EENT

Speech disorder (postmarketing).

GI

Diarrhea (4%); abdominal pain (2%); constipation, nausea (1%); pancreatitis, vomiting (postmarketing).

Genitourinary

Urinary retention (postmarketing).

Hematologic-Lymphatic

Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia, thrombotic thrombocytopenic purpura (postmarketing).

Hepatic

Hepatotoxicity (postmarketing).

Miscellaneous

Injection site pain/reaction (IV, 1%); anaphylactoid reactions (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 1 yr of age. Safety and efficacy of lansoprazole IV has not been established in pediatric patients.

Hepatic Function

Consider dosage adjustment.

Patient Information

• Instruct patient to take each oral dose before a meal.
• Inform patients that antacids may be taken concurrently with lansoprazole.
• Remind patient that lansoprazole is to be taken every day as prescribed, not only when needed or symptoms are present.
• Advise patient not to change the dose or stop taking unless advised by health care provider.
• Advise patient to notify health care provider if symptoms do not improve or seem to be getting worse.
• Advise patient to immediately report bloody or coffee-ground-like vomit, or black tarry stools to health care provider.

• Delayed-Release Capsule
• Advise patient to swallow whole and not to crush or chew the capsule.
• Advise patient that if swallowing the capsule is difficult, the capsule may be opened and the contents sprinkled on 1 Tbsp applesauce, Ensure pudding, cottage cheese, yogurt, or strained pears. The mixture should be swallowed immediately without chewing the granules. Advise patient that the contents of the capsule may also be emptied into 2 oz apple juice, orange juice, or tomato juice, mixed briefly, then swallowed immediately without chewing the granules. Advise patient to then rinse the glass with 2 or more volumes of juice and swallow the contents immediately.
• Caution patient not to mix the contents of the capsule with any other food or liquid than those noted above.

• Delayed-Release Orally Disintegrating Tablet
• Instruct patient to place tablet on tongue and allow it to disintegrate, with or without water, until the particles can be swallowed. Caution patient not to chew the tablet or particles that are released.
• Advise patient or caregiver that if using the orally disintegrating tablet is difficult, the tablet can be placed in an oral syringe and mixed with 4 mL water (15 mg tablet) or 10 mL water (30 mg tablet). Advise patient or caregiver to shake syringe gently to allow for a quick dispersal and then administer the dispersed contents from the syringe within 15 min. Advise patient or caregiver to then refill the syringe with 2 mL water (15 mg tablet) or 5 mL water (30 mg tablet), shake gently, and administer any remaining contents.

• Delayed-Release Oral Suspension
• Advise patient to open packet and empty contents into container containing 2 Tbsp water. Ask patient to stir well and then drink immediately without chewing granules. If any material remains after drinking, advise patient to add more water, stir, and drink immediately.
• Caution patient not to mix oral suspension with any liquid other than water or with food.

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