Class: GI agent
- Capsules 8 mcg
- Capsules 24 mcg
Lubiprostone, a locally acting chloride channel activator, activates CIC-2, a normal constituent of the luminal membrane of the human intestine, which enhances a chloride-rich intestinal fluid secretion without altering sodium and potassium serum concentrations. By increasing intestinal fluid secretion, lubiprostone increases intestinal motility, which facilitates the passage of stool and alleviates symptoms associated with chronic idiopathic constipation.
Low systemic bioavailability. The C max and mean AUC are 41.5 pg/mL and 57.1 pg•h/mL, respectively.
Protein binding is about 94%.
Extensively metabolized by carbonyl reductase.
Although not detectable in plasma, the t ½ ranges from 0.9 to 1.4 h. Elimination is 60% in urine and 30% in feces.
After a single oral dose of 24 mcg, peak levels occur at about 1.14 h.
Special PopulationsRenal Function Impairment
Has not been evaluated.Hepatic Function Impairment
Has not been evaluated.Gender
Indications and Usage
Treatment of chronic idiopathic constipation in adults; treatment of bowel syndrome with constipation in women 18 yr of age and older.
History of mechanical GI obstruction; hypersensitivity to any component of the product.
Dosage and AdministrationChronic Idiopathic Constipation
PO 24 mcg twice daily.Bowel Syndrome and Constipation
PO 8 mcg twice daily with food or water.
- Administer each dose with food and water to prevent or reduce nausea.
- Periodically assess need for continued therapy.
Store capsules at controlled room temperature (59° to 86°F).
None well documented.
Laboratory Test Interactions
None well documented.
Increased heart rate, syncope (postmarketing).
Headache (11%); dizziness (3%); fatigue (2%); asthenia, malaise (postmarketing).
Nausea (29%); diarrhea (12%); abdominal pain (8%); abdominal distention, flatulence (6%); abdominal discomfort, loose stools, vomiting (3%); dyspepsia (2%); dry mouth, stomach discomfort (1%).
Allergic-type reactions including rash, swelling, and throat tightness (postmarketing).
Muscle cramps or spasms (postmarketing).
Chest discomfort, edema (3%).
Category C .
Safety and efficacy not established.
ElderlyChronic idiopathic constipation
Efficacy similar in elderly patients compared with younger individuals. Elderly patients experienced a lower rate of nausea compared with younger patients.Bowel syndrome with constipation
Safety similar in elderly patients compared with younger individuals.
Do not administer to patients who have severe diarrhea.
Evaluate patients with symptoms suggestive of mechanical GI obstruction prior to initiating therapy.
Abdominal pain, anorexia, asthenia, chest discomfort, diarrhea, dizziness, dry mouth, dyspnea, flushing or hot flush, headache, hyperhidrosis, nausea, pallor, retching, stomach discomfort, syncope, vomiting.
- Advise patient to review the patient information leaflet carefully before starting therapy and to read and check for new information each time the medication is refilled.
- Advise patient to take each dose with food and water to reduce the frequency and severity of nausea.
- Advise patient that therapy will be periodically evaluated by health care provider to determine if medication needs to be continued.
- Advise patient that abdominal bloating, discomfort, and/or pain; nausea; diarrhea; and gas occur commonly during treatment and to notify health care provider if symptoms occur and are intolerable.
- Advise women of childbearing potential to use effective contraception while taking lubiprostone.
- Women who could become pregnant should have a negative pregnancy test prior to beginning therapy and should use effective contraception during treatment.
- Instruct patients to swallow the medication whole and not to break or chew capsules.
Copyright © 2009 Wolters Kluwer Health.