Pantoprazole

Protonix | Pantoloc

FDA ApprovedGastrointestinal AgentsProton Pump Inhibitors
FDA: 2000Half-life: 1 hourPregnancy: Category B

Overview

Proton pump inhibitor for gastric acid suppression, used in GERD, erosive esophagitis, and Zollinger-Ellison syndrome.

Indications

  • Gastroesophageal reflux disease (GERD)
  • Erosive esophagitis
  • Zollinger-Ellison syndrome
  • H. pylori eradication (combination)

Contraindications

  • Hypersensitivity to substituted benzimidazoles
  • Concomitant use with rilpivirine

Classification

Mechanism of Action

Irreversibly inhibits H+/K+ ATPase (proton pump) in gastric parietal cells, suppressing basal and stimulated gastric acid secretion.

Pharmacodynamics

Produces dose-dependent inhibition of gastric acid. Maximum effect at day 2-3 of once-daily dosing.

Pharmacokinetics

Absorption
Rapid absorption. Enteric-coated tablet delays onset.
Distribution
Protein binding 98%. Volume of distribution 11-24 L.
Metabolism
Hepatic via CYP2C19 (major), CYP3A4. Polymorphic metabolism.
Excretion
Renal (71%), fecal (18%).
Half-life
1 hour
Bioavailability
77%
Protein Binding
98%

Dosage

Typical dosage: 20-40mg once daily

Available Forms

  • Tablet (delayed-release)
  • Granules
  • IV injection

Side Effects

Common

  • Headache
  • Diarrhea
  • Nausea
  • Abdominal pain
  • Flatulence

Serious

  • C. difficile-associated diarrhea
  • Bone fractures (long-term)
  • Hypomagnesemia

Rare

  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus

Drug Interactions

moderate

PPIs may increase methotrexate levels by inhibiting renal elimination.

moderate

Less interaction than omeprazole, but some CYP2C19 inhibition possible.

Warnings

Pregnancy

Category B

Toxicity

LD50 >4000 mg/kg (oral, rat)

Overdose

No specific symptoms expected. Treatment: supportive care.

References

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