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Lansoprazole pharmacology, Lecture notes of Pharmacology

Lansoprazole pharmacological actions

Typology: Lecture notes

2020/2021

Uploaded on 06/21/2021

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Class: Proton-pump Inhibitors
- Antiulcer Agents
- Gastric Antisecretory Agents
- Acid-pump Inhibitors
Brands: Prevacid, Prevpac
Mechanism of action
Inhibits basal and stimulated gastric acid secretion
Concentrates in acid conditions of parietal cell secretory canaliculi; forms active
sulfenamide metabolite that irreversibly binds to and inactivates hydrogen-
potassium ATPase (proton or acid pump), blocking final step in secretion of
hydrochloric acid
Acid secretion is inhibited until additional hydrogen-potassium ATPase is
synthesized, resulting in prolonged duration of action
Lansoprazole is a racemic mixture of
R
- and
S
-isomers. Both isomers inhibit
hydrogen-potassium ATPase. Combined therapy with lansoprazole and
appropriate anti-infectives (i.e., amoxicillin, clarithromycin) can effectively
eradicate
H. pylori
infection.
Dosage
Pediatric Patients
GERD
Oral
Children 111 years of age: In those weighing ≤30 kg, 15 mg once daily for up to
12 weeks. In those weighing >30 kg, 30 mg once daily for up to 12 weeks.
LANSOPRAZOLE
-LAVANYA
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Class: Proton-pump Inhibitors

  • Antiulcer Agents
  • Gastric Antisecretory Agents
  • Acid-pump Inhibitors Brands: Prevacid, Prevpac

Mechanism of action

  • Inhibits basal and stimulated gastric acid secretion
  • Concentrates in acid conditions of parietal cell secretory canaliculi; forms active sulfenamide metabolite that irreversibly binds to and inactivates hydrogen- potassium ATPase (proton or acid pump), blocking final step in secretion of hydrochloric acid
  • Acid secretion is inhibited until additional hydrogen-potassium ATPase is synthesized, resulting in prolonged duration of action
  • Lansoprazole is a racemic mixture of R- and S-isomers. Both isomers inhibit hydrogen-potassium ATPase. Combined therapy with lansoprazole and appropriate anti-infectives (i.e., amoxicillin, clarithromycin) can effectively

eradicate H. pylori infection.

Dosage Pediatric Patients GERD Oral Children 1–11 years of age: In those weighing ≤30 kg, 15 mg once daily for up to 12 weeks. In those weighing >30 kg, 30 mg once daily for up to 12 weeks. LANSOPRAZOLE

  • LAVANYA

Dosage has been increased up to 30 mg twice daily after ≥2 weeks in patients remaining symptomatic. Children 12–17 years of age: 15 mg daily for up to 8 weeks. Treatment of Erosive Esophagitis Oral Children 1–11 years of age: In those weighing ≤30 kg, 15 mg once daily for up to 12 weeks. In those weighing >30 kg, 30 mg once daily for up to 12 weeks. Dosage has been increased up to 30 mg twice daily after ≥2 weeks in patients remaining symptomatic. Children 12–17 years of age: 30 mg daily for up to 8 weeks. Adults Gastroesophageal Reflux Chronic, lifelong therapy with proton-pump inhibitor is appropriate for many GERD patients. GERD Oral 15 mg once daily for up to 8 weeks. Treatment of Erosive Esophagitis Oral 30 mg once daily for up to 8 weeks. May give additional 8 weeks of therapy (up to 16 weeks for a single course) if not healed. If recurs, consider additional 8 weeks of therapy. Maintenance of Healing of Erosive Esophagitis Oral

NSAIA-induced Gastric Ulcer Treatment Oral 30 mg once daily for 8 weeks. Risk Reduction Oral 15 mg once daily for up to 12 weeks. Pathologic GI Hypersecretory Conditions (e.g., Zollinger-Ellison Syndrome) Oral 60 mg once daily initially. Adjust dosage according to patient response and tolerance; continue therapy as long as necessary. May require dosages of up to 90 mg twice daily. Administer daily dosages >120 mg in divided doses. Patients with Zollinger-Ellison syndrome have been treated for up to 4 years. Adverse Effects

  • In children 1–11 years of age, constipation and headache.
  • In children 12–17 years of age, headache, abdominal pain, nausea, dizziness.
  • In adults receiving oral lansoprazole, diarrhea, abdominal pain, nausea, constipation.

Uses for Lansoprazole

Gastroesophageal Reflux (GERD)

Short-term treatment of symptomatic GERD (e.g., heartburn). Short-term treatment of erosive esophagitis (endoscopically diagnosed) in patients with GERD. Maintain healing and decrease recurrence of erosive esophagitis.

Duodenal Ulcer

Short-term treatment of active duodenal ulcer (endoscopically or radiographically confirmed).

Treatment of Helicobacter pylori infection and duodenal ulcer disease. Used in

conjunction with amoxicillin and clarithromycin (triple therapy) or clarithromycin (dual therapy). Maintenance therapy following duodenal ulcer healing.

Gastric Ulcer

Short-term treatment and symptomatic relief of active benign gastric ulcer.

NSAIA-induced Gastric Ulcer

Short-term treatment of NSAIA-induced gastric ulcer in patients continuing NSAIA use. Risk reduction in patients with history of gastric ulcer who require NSAID treatment.

Formulations