Lubiprostone

Administration

• Type: Laxative
• Dosage Forms: CAP 8mcg, 24mcg
• Routes of Administration: Oral
• Common Trade Names: Amitiza

Adult Dosing

Chronic idiopathic constipation

• 24mcg PO BID

IBS, constipation predominant

• 8mcg PO BID

Constipation, opioid-induced

• 24mcg PO BID

Pediatric Dosing

Safety/efficacy not established in pediatric patients

Special Populations

• Pregnancy Rating: C
• Lactation risk: Risk of infant harm not expected based on minimal absorption.

Renal Dosing

• Adult: No adjustment
• Pediatric: Not available

Hepatic Dosing

• Adult:
  • Child-Pugh Class C: 8mcg qd
• Pediatric: Not available

Contraindications

• Allergy to class/drug
• GI Obstruction
• Diarrhea, severe

Adverse Reactions

Serious

• Diarrhea, severe
• Hypersensitivity reaction
• Syncope
• Hypotension

Common

• Nausea, headache, vomiting, dizziness
• Diarrhea
• Abdominal pain
• Flatulence
• Sinusitis
• UTI, URI
• Peripheral edema
• Arthralgia, fatigue, dyspnea

Pharmacology

• Half-life: 0.9-1.4h
• Metabolism: Stomach
• Excretion: Urine (60%), Feces (30%)

Mechanism of Action

• Activates CIC-2 chloride channels, increasing intestinal fluid secretion and motility
• Reduces intestinal permeability and stimulates recovery of mucosal barrier function