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Lansoprazole; Uses, ,Dosage, Side Effects, Drug Interactions

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.

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.

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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

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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

Common

Less common

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

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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.