Lubiprostone

Indications

Lubiprostone is used for: Irritable Bowel Syndrome with Constipation (IBS-C), Chronic idiopathic constipation, Opioid-induced Constipation (OIC) in adults with chronic non-cancer pain

Adult Dose

Oral Chronic idiopathic constipation Adult: 24 mcg bid daily. Irritable Bowel Syndrome With Constipation 8 mcg twice daily. Opioid-Induced Constipation Treatment in patients with chronic noncancer pain 24 mcg bid daily. Hepatic impairment Mild: Dose adjustment not necessary Moderate (Child-Pugh B): Chronic idiopathic or opioid-induced constipation, 16 mcg PO q12hr; irritable bowel syndrome with constipation (IBS-C), no dosage adjustment required Severe (Child-Pugh C): Chronic idiopathic or opioid-induced constipation, 8 mcg PO q12hr; IBS-C, 8 mcg PO q24hr

Child Dose

Safety and efficacy not established

Renal Dose

Administration

Should be taken with food.

Contra Indications

History of mechanical GI obstruction.

Precautions

Safety has not been established in pregnant women. Not to be used in patients with severe diarrhoea. Lactation: Unknown whether drug is excreted in breast milk; because lubiprostone increases fluid secretion in the intestine and intestinal motility, monitor breastfeeding infants for diarrhea

Pregnancy-Lactation

Pregnancy Following oral administration, concentrations of lubiprostone in plasma are below the level of quantitation; however, one of the metabolites, M3, has measurable systemic concentrations Data are not available to inform a drug associated risk of adverse developmental outcomes Animal studies Animal studies did not show an increase in structural malformations; however, a doses dependent increase in fetal loss was observed in pregnant guinea pigs at 0.2-6 times the MRHD Lactation No data are available on the presence in human milk of the refect on milk production Animal studies Neither lubiprostone nor its active metabolite (M3) were present in milk of lactating rats When a drug is not present in animal milk, it is likely that the drug will not be present in human milk If present, lubiprostone may cause diarrhea in the breastfed infant lubiprostone may cause diarrhea on effect of breastfed infants

Interactions

Adverse Effects

Side effects of Lubiprostone : >10% Nausea (29%), Headache (12%), Diarrhea (11%) 1-10% Edema (3%), Chest discomfort (2%), Peripheral edema (1-3%), Fatigue (2%), Dizziness (3%), Flatulence (4-6%), Abdominal distress (3%), Dyspepsia (2%), Xerostomia (1%), Abdominal pain (4-8%), Loose stools (3%)

Mechanism of Action

Lubiprostone is a locally acting chloride channel activator that enhances a chloride-rich intestinal fluid secretion without altering sodium and potassium concentrations in the serum. Lubiprostone acts by specifically activating ClC-2, which is a normal constituent of the apical membrane of the human intestine. By increasing intestinal fluid secretion, Lubiprostone increases motility in the intestine, thereby facilitating the passage of stool and alleviating symptoms associated with chronic idiopathic constipation.