Search
lubiprostone (Amitiza)
Indications:
- constipation
- constipation with irritable bowel syndrome [3]
- opioid-induced constipation [4]
Contraindications:
- history of mechanical gastrointestinal obstruction
Pregnancy category: C
Dosage:
- 24 ug BID with food
- 8 ug BID (irritable bowel syndrome)
Gelcap: 8, 24 ug
Pharmacokinetics:
- not absorbed appreciably
Adverse effects:
1) gastrointestinal
a) nausea 30%, dose-dependent
b) diarrhea 13.2%
c) abdominal distension (7.1%)
d) abdominal pain (6.7%)
e) gas (6.1%)
f) vomiting (4.6%)
g) loose stools (3.4%)
2) headache (13.2%)
3) dizziness (4.1%)
4) peripheral edema (3.8%)
5) dyspnea (2.4%)
6) arthralgia (3.1%)
Drug interactions:
1) no drug-drug interaction studies have been done
2) no cyt P450 interactions
3) little is absorbed, thus drug interactions unlikely
Mechanism of action:
1) lubiprostone is a prostone, a prostaglandin-like molecule
2) selective chloride channel activator
3) activates ClC-2 chloride channels in the small intestine
4) increases intestinal fluid secretion
5) increases intestinal motility
6) increases stool consistency
Notes:
- Amitiza costs over $200/month
- only about 14% of patients respond [2]
General
laxative
References
- Prescriber's Letter 13(4): 2006
Detail-Document#: 220422
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 15(6): 2008
Amitiza (Lubiprostone) for IBS with Constipation
Detail-Document#: 240606
(subscription needed) http://www.prescribersletter.com
- Drossman DA, Chey WD, Johanson JF et al
Clinical trial: lubiprostone in patients with constipation-
associated irritable bowel syndrome--results of two randomized,
placebo-controlled studies.
Aliment Pharmacol Ther. 2009 Feb 1;29(3):329-41
PMID: 19006537
- NEJM Knowledge+ Pain Management and Opioids: Recharge