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. or 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. References DrugBank http://www.drugbank.ca/drugs/DB00448 http://www.drugbank.ca/drugs/DB00448#transporters http://www.drugbank.ca/drugs/DB00448#targets http://www.drugbank.ca/drugs/DB00448#enzymes https://www.drugs.com/lansoprazole.html https://www.drugs.com/cdi/lansoprazole-delayed-release-capsules.html https://www.drugs.com/prevacid.html HSDB https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+103577-45-3 ChemIDplus https://chem.nlm.nih.gov/chemidplus/sid/0103577453 ChemIDplus Chemical Information Classification https://chem.sis.nlm.nih.gov/chemidplus/chemidheavy.jsp DTP/NCI https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=758638 https://www.webmd.com/drugs/2/drug-11450-9143/lansoprazole-oral/lansoprazole-delayed-release-capsule-oral/details/list-contraindications https://online.epocrates.com/u/1031127/lansoprazole/Contraindications+Cautions EPA DSStox https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID4023200 Human Metabolome Database (HMDB) http://www.hmdb.ca/metabolites/HMDB0005008 ClinicalTrials.gov https://clinicaltrials.gov/ DailyMed https://dailymed.nlm.nih.gov/dailymed/search.cfm? https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=LANSOPRAZOLE LiverTox https://livertox.nlm.nih.gov/Lansoprazole.htm NCIt https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C29150 EU Community Register of Medicinal Products https://ec.europa.eu/health/documents/community-register/html/ho3061.htm European Chemicals Agency (ECHA) https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/178139 FDA Medication Guides https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020406s083,021428s031lbl.pdf#page=37 https://www.fda.gov/downloads/Drugs/DrugSafety/ucm088694.pdf FDA Orange Book https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm MassBank of North America (MoNA) http://mona.fiehnlab.ucdavis.edu/spectra/browse?inchikey=MJIHNNLFOKEZEW-UHFFFAOYSA-N PubMed Health http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0010860/ Show More