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Lansoprazole is a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. Lansoprazole prodrug is converted to an active sulfonamide derivative in the acidic environment of the gastric parietal cell; the sulfonamide derivative binds to the gastric proton pump H+/K+ ATPase and forms a stable disulfide bond with the sulfhydryl group near the potassium-binding site on the luminal side, resulting in inactivation of the ATPase and a reduction in gastric acid secretion. This agent does not have anticholinergic or histamine H2 -receptor antagonistic properties.
Lansoprazole is a medication which inhibits the stomach’s production of acid. There is no evidence that its effectiveness is different from that of other PPIs. Lansoprazole, given through a nasogastric tube, effectively controls pH inside the stomach and is an alternative to intravenous pantoprazole in people who are unable to swallow solid-dose formulations. Lansoprazole is used to treat and prevent stomach and intestinal ulcers, erosive esophagitis (damage to the esophagus from stomach acid), and other conditions involving excessive stomach acid such as Zollinger-Ellison syndrome.
Mechanism of Action of Lansoprazole
Lansoprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but rather suppress gastric acid secretion by specific inhibition of the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, Lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus.
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Lansoprazole is a selective and irreversible proton pump inhibitor. In the acidic environment of the gastric parietal cell, lansoprazole is converted to active sulphenamide derivatives that bind to the sulfhydryl group of (H+, K+)-adenosine triphosphatase ((H+,K+)-ATPase), also known as the proton pump (H+,K+)-ATPase catalyzes the final step in the gastric acid secretion pathway. Lansoprazole’s inhibition of (H+, K+)-ATPase results in inhibition of both centrally and peripherally mediated gastric acid secretion. The inhibitory effect is dose-related. Lansoprazole inhibits both basal and stimulated gastric acid secretion regardless of the stimulus.
Indications of Lansoprazole
- For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.
- Bacterial Infection Due to Helicobacter Pylori (H. Pylori)
- GERD
- Barrett’s esophagus
- Gastritis/duodenitis
- Duodenal ulcer
- Aspiration pneumonia
- Erosive esophagitis
- Multiple endocrine adenomas
- NSAID-induced gastric ulcer
- Stomach ulcer
- Systemic mastocytosis
- Zollinger-Ellison syndrome
- Gastrointestinal Bleed
- Peptic ulcer disease
- Hypersecretory conditions
Therapeutic indications of Lansoprazole
- Lansoprazole is indicated for short-term (up to 8 weeks) treatment in patients with active benign gastric ulcer.
- Lansoprazole is indicated for short-term (up to 4 weeks) treatment for symptom relief and healing in patients with active duodenal ulcer. Lansoprazole also is indicated to maintain healing of duodenal ulcers. /Included in US product labeling
- Lansoprazole is indicated in combination with amoxicillin plus clarithromycin for the treatment of duodenal ulcer associated with Helicobacter pylori infection.
- Lansoprazole also is indicated in combination with amoxicillin in patients who are either allergic or intolerant to clarithromycin or in whom resistance to clarithromycin is known or suspected.
- Lansoprazole is indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
Contra-Indications of Lansoprazole
- Clostridium difficile infection
- Inadequate Vitamin B12
- low amount of magnesium in the blood
- Severe Liver Disease
- Interstitial Nephritis
- Osteoporosis
- Broken Bone
- CYP2C19 Poor Metabolizer
- Allergies to proton pump inhibitors
Dosage of Lansoprazole
Strengths: 15 mg; 30 mg; 3 mg/mL
Erosive Esophagitis
- Treatment: 30 mg orally once a day
- Duration of therapy: Up to 8 weeks
- Maintenance: 15 mg orally once a day
Duodenal Ulcer
- Treatment: 15 mg orally once a day
- Duration of therapy: Up to 4 weeks
- Maintenance: 15 mg orally once a day
Duodenal Ulcer Prophylaxis
- Treatment: 15 mg orally once a day
- Duration of therapy: Up to 4 weeks
- Maintenance: 15 mg orally once a day
Gastroesophageal Reflux Disease
- 15 mg orally once a day
- Duration of therapy: Up to 8 weeks
Gastric Ulcer
- 30 mg orally once a day
- Duration of therapy: Up to 8 weeks
Multiple Endocrine Adenomas
- Initial dose: 60 mg orally once a day
- Maintenance dose: 60 to 180 mg/day
Zollinger-Ellison Syndrome
- Initial dose: 60 mg orally once a day
- Maintenance dose: 60 to 180 mg/day
Helicobacter pylori Infection
Triple Therapy
- 30 mg orally 2 times a day, taken concomitantly with amoxicillin and clarithromycin
- Duration of therapy: 10 to 14 days
Dual Therapy
- 30 mg orally 3 times a day, taken concomitantly with amoxicillin
- Duration of therapy: 14 days
NSAID-Induced Gastric Ulcer
- 30 mg orally once a day
- Duration of therapy: Up to 8 weeks
Pediatric Gastroesophageal Reflux Disease
1 to 11 years
- Less than or equal to 30 kg: 15 mg orally once a day
- Greater than 30 kg: 30 mg orally once a day
- Duration of therapy: Up to 12 weeks
12 years and older
- 15 mg orally
Pediatric Erosive Esophagitis
1 to 11 years
- Less than or equal to 30 kg: 15 mg orally once a day
- Greater than 30 kg: 30 mg orally once a day
- Duration of therapy: Up to 12 weeks
12 to 17 years
- 30 mg orally once a day
- Duration of therapy: Up to 8 weeks
Side Effects of Lansoprazole
The most common
- Nausea and vomiting
- Severe stomach ache
- epigastric pain
- diarrhoea,
- anorexia,
- flatulence
- headache,
- dizziness,
- fainting, fast or pounding heartbeats;
- confusion, hallucinations;
Common
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Mouth sores
- Vaginal thrush
- Skin rash
- Headache
Less common
- Abdominal or stomach pain
- increased or decreased appetite
- joint pain
- nausea
- vomiting
- Anxiety
- constipation
- increased cough
- mental depression
- muscle pain
- rectal bleeding
Drug Interactions of Lansoprazole
Lansoprazole may interact with following drugs, supplements, & change the efficacy of the drug
- “azole” antifungals (e.g., itraconazole, ketoconazole, posaconazole)
- bisphosphonates (e.g., alendronate, risedronate)
- carbamazepine
- clopidogrel
- dasatinib
- dexamethasone
- fluvoxamine
- HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delavirdine, efavirenz, etravirine, nevirapine)
- methotrexate
- methylphenidate
- multivitamins with minerals
- mycophenolate
- nilotinib
- phenobarbital
- phenytoin
- “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
- warfarin
Pregnancy & Lactation of Lansoprazole
FDA Pregnancy Category B
Pregnancy
There are no adequate or well-controlled studies on the use of this medication by pregnant women. This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Breast-feeding
It is not known if lansoprazole passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
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