Lubiprostone

Generic Details

Generic Name

Lubiprostone

Other Names

  • Amitiza

Drug Class

  • Chloride Channel Activator

Chemical Formula

C20H32F2O5

Molecular Weight

390.5 g/mol

Mechanism of Action

  • Activates type 2 chloride channels in the gastrointestinal tract, leading to increased intestinal fluid secretion and motility

Indications

  • Chronic idiopathic constipation
  • Irritable bowel syndrome with constipation

Common Dosage Forms

  • Oral capsule

Typical Dosage

  • 24 mcg twice daily with food and water

Pediatric Dosage

  • Safety and efficacy not established in children

Geriatric Dosage

  • Dose adjustment may be required in elderly patients

Side Effects

  • Nausea
  • Diarrhea
  • Abdominal pain
  • Flatulence
  • Headache

Contraindications

  • Mechanical gastrointestinal obstruction

Pregnancy Category

  • Category C

Lactation Safety

  • Use caution; not recommended during breastfeeding

Drug Interactions

  • CYP3A4 inhibitors (e.g. ketoconazole) may increase exposure to lubiprostone

Overdose Symptoms

  • Nausea
  • Diarrhea

Antidote for Overdose

  • Symptomatic treatment

Storage Conditions

  • Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

Pharmacokinetics

  • Absorption: Poorly absorbed
  • Distribution: Mostly confined to the gastrointestinal tract
  • Metabolism: Metabolized in the stomach to active metabolite
  • Excretion: Mainly in the feces

Precautions

  • Monitor for severe diarrhea
  • Use with caution in patients with renal impairment

Warnings

  • May cause dehydration; ensure adequate fluid intake