Lubiprostone
Brand names,
Lubiprostone
Analogs
Lubiprostone
Brand Names Mixture
Lubiprostone
Chemical_Formula
C20H32F2O5
Lubiprostone
RX_link
No information avaliable
Lubiprostone
fda sheet
Lubiprostone
msds (material safety sheet)
Lubiprostone
Synthesis Reference
No information avaliable
Lubiprostone
Molecular Weight
390.462 g/mol
Lubiprostone
Melting Point
No information avaliable
Lubiprostone
H2O Solubility
Practically insoluble
Lubiprostone
State
Solid
Lubiprostone
LogP
4.453
Lubiprostone
Dosage Forms
Capsule (24 µg)
Lubiprostone
Indication
For the treatment of chronic idiopathic constipation in the adult population.
Lubiprostone
Pharmacology
Chronic idiopathic constipation is generally defined by infrequent or difficult passage of stool. The signs and symptoms associated with chronic idiopathic constipation (i.e., abdominal pain or discomfort, bloating, straining, and hard or lumpy stools) may be the result of abnormal colonic motility that can delay the transit of intestinal contents and impede the evacuation of rectal contents. One approach to the treatment of chronic idiopathic constipation is the secretion of fluid into the abdominal lumen through the activation of chloride channels in the apical membrane of the gastrointestinal epithelium. 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
Absorption
Lubiprostone has low systemic availability following oral administration and concentrations of lubiprostone in plasma are below the level of quantitation (10 pg/mL).
Lubiprostone
side effects and Toxicity
In a definitive Phase 1 cardiac repolarization study, 51 patients were administered a single oral dose of 144 mcg of lubiprostone, which is 6 times the normal single administration dose. Thirty-nine (39) of the 51 patients experienced an adverse event. The adverse events reported in >1% of this group included the following: nausea (45.1%), vomiting (27.5%), diarrhea (25.5%), dizziness (17.6%), loose or watery stools (13.7%), headache (11.8%), retching (7.8%), abdominal pain (5.9%), flushing or hot flush (5.9%), dyspnea (3.9%), pallor (3.9%), stomach discomfort (3.9%), syncope (3.9%), upper abdominal pain (2.0%), anorexia (2.0%), asthenia (2.0%), chest discomfort (2.0%), dry mouth (2.0%), hyperhidrosis (2.0%), skin irritation (2.0%) and vasovagal episode (2.0%).
Lubiprostone
Patient Information
No information avaliable
Lubiprostone
Organisms Affected
Humans and other mammals