Prevacid (Lansoprazole)

(British Approved Name, US Adopted Name, rINN)

What Is Prevasid (Lansoprazole)?

Lansoprazole is a proton pump inhibitor (PPI) medication that reduces stomach acid production. It belongs to a class of drugs that work by inhibiting the proton pump in the stomach lining, specifically the H+/K+ ATPase enzyme, which is responsible for the final step in acid production. By reducing stomach acid, lansoprazole is effective in treating conditions where excess acid can cause problems, such as gastroesophageal reflux disease (GERD), peptic ulcers, and other acid-related disorders.

Lansoprazole works by inhibiting the proton pump in the stomach lining, reducing the production of gastric acid.

Lansoprazole is typically taken orally, usually before meals. It is available in different formulations, including delayed-release capsules and orally disintegrating tablets. The duration of treatment with lansoprazole can vary based on the specific condition being treated. Short-term use may be appropriate for conditions like peptic ulcers, while long-term maintenance therapy may be recommended for GERD.

Common side effects may include headache, nausea, abdominal pain, and diarrhea. These side effects are generally mild and temporary.

Long-term use of PPIs like lansoprazole has been associated with certain risks, including potential changes in bone density, kidney disease, and the risk of certain infections. Regular monitoring may be recommended.

Lansoprazole can interact with other medications, and you must inform your healthcare provider about all the medications and supplements you are taking.

Using lansoprazole under a healthcare professional’s guidance is crucial, and the treatment dosage and duration will be determined based on the specific condition being treated. Discuss your questions or concerns about lansoprazole with your healthcare provider for personalized advice and information.

Pharmacokinetics

Lansoprazole is rapidly absorbed after oral doses, with peak plasma concentrations achieved after about 1.5 to 2 hours. Bioavailability is reported to be 80% or more even with the first dose, although the drug must be given in an enteric-coated form since lansoprazole is unstable at acid pH. Food slows the absorption of lansoprazole and reduces the bioavailability by about 50%.

It is extensively metabolized in the liver, primarily by cytochrome P450 isoenzyme CYP2C19 to form 5-hydroxyl-lansoprazole and by CYP3A4 to form lansoprazole sulfone. Metabolites are excreted mainly in feces via the bile; about 15 to 30% of a dose is excreted in the urine. The plasma elimination half-life is around 1 to 2 hours, but the duration of action is much longer. Lansoprazole is about 97% bound to plasma protein. Clearance is decreased in elderly patients and hepatic impairment.

Metabolism

As for omeprazole, the cytochrome P450 isoenzyme CYP2C19 (S-mephenytoin hydroxylase) is involved in the hydroxylation of lansoprazole, and individuals who are deficient in this enzyme are poor metabolizers of lansoprazole. The effect of this genetic polymorphism on lansoprazole may be less than the effect on omeprazole.

Clinical Studies

Prevacid is administered as capsules containing enteric-coated granules of lansoprazole. It is absorbed rapidly, reaching peak plasma concentrations within about 1.7 hours. Bioavailability exceeds 80%. Plasma half-life is 1.5 hours. Food diminishes peak plasma concentration and the area under the concentration-time curve (AUC). Lansoprazole is 97% bound to plasma proteins. The drug undergoes extensive hepatic metabolism. Despite a short plasma half-life, the drug’s inhibitory effect on gastric acid secretion lasts about 24 hours.
In a clinical trial involving 284 patients, healing rates after two weeks for duodenal ulcers were 42.4% with 15 mg lansoprazole/day, 35.6% with 30 mg/day, and 39.1% with 60 mg/day, compared with 11.3% for placebo. After four weeks, the respective healing rates with lansoprazole were 89.4%, 91.7%, and 89.9%, compared with 46.1% for placebo. In a second trial with 280 patients, the healing rates at four weeks with lansoprazole were 92.3% with 15 mg/day and 80.3% with 30 mg/day, compared with 70.5% for 300 mg ranitidine and 47.5% for placebo. (Lanza Fetal. Am J Gastroenterol. 1994; 89: 1191-1200.)
In a trial of lansoprazole in 269 patients with erosive esophagitis, the healing rate at eight weeks ranged from 90.9% with 15 mg/day to 95.4% with 30 mg/day, compared with 52.5% for placebo. In another trial, the healing rate was 92.1% with 30 mg/day, compared with 69.9% for ranitidine 150 mg twice daily. Lansoprazole has been found to promote healing in more than 80% of patients whose initial treatment with H2-receptor antagonists had failed.
Lansoprazole has been well-tolerated in clinical use. Adverse events occurring in more than 1% of patients have included abdominal pain (1.8%), diarrhea (3.6%), and nausea (1.4%). Lansoprazole does not interact with other drugs, but coadministration with sucralfate can slow and reduce the absorption of lansoprazole.
Prevacid is supplied as 15-mg pink-and-green capsules and 30-mg pink-and-black capsules. The recommended adult dosage for duodenal ulcers is 15 mg daily before food for four weeks. The recommended dosage for erosive esophagitis is 30 mg daily before food for up to 8 weeks. If healing does not occur, or if erosive esophagitis recurs, an additional eight weeks of treatment may be helpful. An initial dosage of 60 mg a day is recommended for hypersecretory conditions, with adjustments to suit individual patient needs. Doses greater than 120 mg a day should be given in divided doses.

Uses

• GERD: Lansoprazole is commonly prescribed for treating GERD, a condition where stomach acid flows back into the esophagus, causing irritation and symptoms such as heartburn.
• Peptic Ulcers: Lansoprazole can promote the healing of peptic ulcers in the stomach or duodenum.
• Zollinger-Ellison Syndrome: This is a rare condition characterized by pancreatic or duodenum tumors that produce excessive amounts of gastrin, leading to increased stomach acid. Lansoprazole is used to control acid production in such cases.

Administration

Lansoprazole is a proton pump inhibitor with actions and uses similar to those of omeprazole. It is used in treating peptic ulcer disease and other conditions where inhibiting gastric acid secretion may be beneficial.

Lansoprazole is usually given orally as capsules, dispersible tablets, or suspension containing enteric-coated granules. Once daily regimens are taken before food in the morning. An intravenous formulation is also available.

To relieve acid-related dyspepsia, intermittent courses of lansoprazole may be given in doses of 15 or 30 mg once daily for 2 to 4 weeks. In treating gastro-oesophageal reflux disease, the dose is 15 to 30 mg once daily for 4 to 8 weeks. After that, maintenance therapy can be continued with 15 or 30 mg once daily, according to response. In patients unable to take oral therapy, lansoprazole may be given by intravenous infusion to treat erosive oesophagitis for up to 7 days; a dose of 30 mg over 30 minutes daily is recommended. Lansoprazole is given for the treatment of peptic ulcer disease in the UK in doses of 30 mg once daily. Treatment is continued for 2 to 4 weeks for duodenal and 4 to 8 weeks for gastric ulcer. In the USA, a dose of 15 mg daily for four weeks is recommended for duodenal ulcers, and 30 mg once daily is given for up to 8 weeks for gastric ulceration.

When appropriate, 15 mg daily may be used as maintenance therapy to prevent relapse of duodenal ulcer. Lansoprazole may be combined with antibacterials in one-week triple therapy regimens to eradicate Helicobacter pylori. Effective regimens include lansoprazole 30 mg twice daily combined with clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily or combined with clarithromycin 250 mg twice daily and metronidazole 400 mg twice daily lansoprazole with amoxicillin and metronidazole has also been used. In patients with NSAID-associated ulceration, a dose of 30 mg daily for 4 to 8 weeks is recommended; 15 to 30 mg daily may be used as prevention for patients who require continued NSAID treatment. In the treatment of pathological hypersecretory states such as the Zollinger-Ellison syndrome, the initial dose is 60 mg once daily, adjusted as required. Doses of up to 90 mg twice daily have been used. Daily doses greater than 120 mg should be given in divided doses.

In the USA, children aged 1 to 11 years may be given lansoprazole for the short-term treatment of erosive oesophagitis and symptomatic gastro-oesophageal reflux disease. Children weighing 30 kg or less should be given 15 mg once daily, and those weighing more than 30 kg are given 30 mg daily for up to 12 weeks. Doses of up to 30 mg twice daily have been used. In children aged from 12 to 17 years, lansoprazole 30 mg once daily for up to 8 weeks may be used for erosive oesophagitis, and 15 mg once daily for up to 8 weeks may be used for symptomatic gastro-oesophageal reflux disease. Although not licensed for children in the UK, the BNFC recommends comparable oral daily doses of 0.5 to 1 mg/kg in children up to 30 kg weight and 15 or 30 mg once daily in those over 30 kg.

Doses of lansoprazole may need to be reduced in patients with hepatic impairment (see below).

How to Take

Lansoprazole capsules should be swallowed whole and not crushed or chewed. Lansoprazole dispersible tablets should be placed on the tongue and allowed to disintegrate, and the resultant granules swallowed alternatively, the tablets may be swallowed whole with a glass of water. The tablets should not be crushed or chewed. The tablets may also be dispersed in a small amount of water and given via an oral syringe or a nasogastric tube.

Lansoprazole granules for oral suspension should be reconstituted in water and swallowed immediately. Where the suspension formulation is unavailable, the capsules (enteric-coated granules) can be sprinkled on a small amount of soft food (such as yogurt or apple sauce) or mixed with a bit of fruit juice and swallowed. For administration via a nasogastric tube, the contents of a capsule may be mixed with 40 mL of apple juice. Additional apple juice may be used to flush the tube.

Administration in Hepatic Impairment

Exposure to lansoprazole is increased in patients with hepatic impairment. Licensed product information recommends that patients with moderate to severe liver disease should be supervised, and the daily dose should be reduced by 50%.

Adverse Effects and Precautions

Lansoprazole can be associated with specific adverse effects and precautions like other medications. It’s essential to use this medication under the guidance of a healthcare professional who can assess the potential risks and benefits for your specific health condition. Here are some of the adverse effects and precautions associated with lansoprazole.

Adverse Effects

1. Gastrointestinal Effects: Common side effects include nausea, vomiting, abdominal pain, and diarrhea. These effects are usually mild and temporary.
2. Central Nervous System Effects: Some individuals may experience headaches or dizziness.
3. Bone Health: Long-term use of proton pump inhibitors (PPIs), including lansoprazole, has been associated with a potential increased risk of bone fractures, particularly in the hip, wrist, and spine. This risk may be higher in individuals who take high doses of PPIs or use them for an extended period.
4. Clostridium difficile Infection: Prolonged use of PPIs may increase the risk of developing Clostridium difficile-associated diarrhea, a severe colon infection.
5. Kidney Disease: Some studies suggest an association between long-term PPI use and an increased risk of kidney disease. Regular monitoring of kidney function may be advisable.

Precautions

1. Pregnancy and Breastfeeding: Lansoprazole is generally considered safe during pregnancy and breastfeeding. However, discussing its use with a healthcare provider to weigh the potential benefits against any potential risks is essential.
2. Liver Disease: Individuals with severe liver disease may require dosage adjustments, as lansoprazole is metabolized in the liver.
3. Hypomagnesemia: Prolonged use of PPIs has been associated with low magnesium levels in the blood (hypomagnesemia). This can lead to symptoms such as muscle spasms, irregular heartbeat, and seizures.
4. Interactions with Other Medications: Lansoprazole can interact with certain medications, including warfarin, clopidogrel, and certain antifungal medications. Inform your healthcare provider about all the medications and supplements you are taking.
5. C. difficile Infection: Prolonged use of PPIs may increase the risk of Clostridium difficile infection. If diarrhea occurs, especially if it is persistent or severe, contact your healthcare provider.

It’s crucial to take lansoprazole as prescribed by your healthcare provider and to inform them of any symptoms or concerns you may have. Regular check-ups and monitoring may be recommended, especially for long-term use. Do not stop or adjust the medication dosage without consulting your healthcare provider.

Interactions

Like other medications, lansoprazole can interact with various drugs, potentially affecting their effectiveness or increasing the risk of side effects. To ensure safe and appropriate use, it’s essential to inform your healthcare provider about all the medications, supplements, and over-the-counter drugs you are taking. Here are some interactions to be aware of:

1. Warfarin (Anticoagulant): Lansoprazole may interact with warfarin, a blood thinner, potentially increasing the risk of bleeding. Regular monitoring of the International Normalized Ratio (INR) is advisable in individuals taking both medications.
2. Clopidogrel (Antiplatelet): There have been concerns about potential interactions between clopidogrel (Plavix), an antiplatelet medication, and PPIs like lansoprazole. The interaction may reduce the effectiveness of clopidogrel in some individuals. Consult with your healthcare provider regarding the use of these medications together.
3. Digoxin (Heart Medication): Lansoprazole may increase the absorption of digoxin, a medication used for heart conditions. Monitoring and adjustment of digoxin dosage may be necessary.
4. Antiretroviral Medications: Lansoprazole may reduce the absorption of certain antiretroviral medications used to treat HIV. These medications should be taken separately.
5. Ketoconazole and Itraconazole (Antifungals): Lansoprazole may reduce the absorption of ketoconazole and itraconazole, antifungal medications. Taking these medications at least 2 hours apart is advisable.
6. Methotrexate (Immunosuppressant): Lansoprazole may increase the levels of methotrexate, an immunosuppressant. Monitoring and adjustment of methotrexate dosage may be necessary.
7. Iron Supplements: Lansoprazole may reduce the absorption of iron supplements. Taking iron supplements at a different time of day may be recommended.
8. Sucralfate: Sucralfate, an aluminum-containing antacid, may reduce the absorption of lansoprazole. Taking these medications at least 30 minutes apart is advisable.
9. St. John’s Wort: St. John’s Wort may induce the metabolism of lansoprazole, potentially reducing its effectiveness.

Always consult your healthcare provider before starting, stopping, or adjusting the dosage of any medication. This information is not exhaustive, and individual responses to medications can vary. Your healthcare provider can provide personalized advice based on your health condition and medication regimen.

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: A-65006; AG-1749; Lansopratsoli; Lansoprazol; Lansoprazolum

BAN: Lansoprazole

USAN: Lansoprazole

INN: Lansoprazole [rINN (en)]

INN: Lansoprazol [rINN (es)]

INN: Lansoprazole [rINN (fr)]

INN: Lansoprazolum [rINN (la)]

INN: Ланзопразол [rINN (ru)]

Chemical name: 2-({3-Methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl)methyl} sulphinylbenzimidazole

Molecular formula: C16H14F3N3O2S =369.4

CAS: 103577-45-3

ATC code: A02BC03

Read code: y01JU

Pharmacopoeias. In Europe and the US.

European Pharmacopoeia, 6th ed. (Lansoprazole). A white or brownish powder. Practically insoluble in water, soluble in anhydrous alcohol, very slightly soluble in acetonitrile. It exhibits polymorphism. Store in airtight containers. Protect from light.

The United States Pharmacopeia 31, 2008(Lansoprazole). A white to brownish-white powder. Practically insoluble in water, freely soluble in dimethylformamide. Store in airtight containers at a temperature not exceeding 40°. Protect from light.

Preparations

The United States Pharmacopeia 31, 2008: Lansoprazole Delayed-Release Capsules.

Proprietary Preparations

Argentina: Isatecf Lanzopral Mesactol Ogasto

Australia: Zoton

Austria: Agopton Lansobene

Belgium: Dakar

Brazil: Anzoprol Lanogastro Lanz Lanzol Lanzopept Neozol Ogastro Prazol

Canada: Prevacid

Chile: Fudermex Gastride Lanzopral Ogasto Unival

Czech Republic: Lansone Lansoprol Lanzul

Denmark: Lanzo

Finland: Lanzo Zolt

France: Lanzor Ogast Ogastoro

Germany: Agopton Lanzor

Greece: Elcodil Lanciprol Lanso Laprazol

Hong Kong: Takepron

Hungary: Lansacid Lansogen Lansone Lansoptol Levant Protonexa Refluxon

India: Chexid Lancus Lanzol

Indonesia: Compraz Digest Gastrolan Inhipraz Lancid Lapraz Laproton Lasgan Laz Loprezol Nufaprazol Prazotec Prolanz Prosogan Protica Pysolan Solans Sopralan Ulceran

Ireland: Lanziop Lanzol Razolager Zomel Zoton Zotrole

Israel: Lanton Zoton

Italy: Lansox Limpidex Zoton

Japan: Prevacid Takepron

Malaysia: Prevacid

Mexico: Bonzol llsatec Imidex Keval Lafin Lanodizol Mavilan Mediprim Ogastro Olan Palatrin Pranix Safemar Uldapril Ulpax

Norway: Lanzo

New Zealand: Solox Zoton

Philippines: Lanzohex Prevacid Fylison

Poland: LansoLek Lanzostad Lanzul

Portugal: Alexin Dispepci Gastrex Gastrolanzo Gastroliber Lansox Lanzogastro Lapol Lizul Monolitum Ogasto Pampe Pepzol Ulcertec

Russia: Acrilans Epicur Helicol Lanzap

South Africa: Adco-Roznal Lancap Lansoloc Lanzor

Singapore: Prevacid

Spain: Bamalite Estomil Eudiges Lanzol Monolitum Opiren Pro Ulco Protoner

Sweden: Lanzo

Switzerland: Agopton

Thailand: Prevacid

Turkey: Aprazol Degastrol Helicol Lansazol Lansoprol Lansor Lanzedin Ogastro Opagis Vogast Zoprol

UAE: Lanfast

United Kingdom: Zoton

USA: Prevacid

Venezuela: Biolanz Gastrazol Lansovax Lanzapf Lanzol Lanzopral Ogastro

Multi-ingredient

Argentina: Helikar

Brazil: Anzopac H-Bacter Helicopac Helikar Lansodom Lansoprid Fylorikit Pyloripac Fyloritrat

Canada: Hp-Pac

Finland: Helipak A Helipak K Helipak T

India: Okalan D Pylokit

Mexico: Pylopac

Turkey: Helipak

UK- Heliclear HeliMet

USA: Prevpac

Used as on adjunct in:

USA: Prevacid NapraPAC