LUBIPROSTONE
MECHANISM OF ACTION –
Lubiprostone acts by specifically activating CIC-2 chloride channels, which is a normal constituent of the apical membrane of the human intestine, in a protein kinase A action independent fashion. Activation of CIC-2 chloride channels causes an efflux of chloride ions into the lumen, which in turn leads to an efflux of sodium ions through a paracellular pathway to maintain isoelectric neutrality. As a result, water follows sodium into the lumen in order to maintain isotonic equilibrium, thereby increasing intestinal fluid secretion. By increasing intestinal fluid secretion, lubiprostone increases motility in the intestine, thereby increasing the passage of stool and alleviating symptoms associated with chronic idiopathic constipation.
PHARMACOLOGICAL ACTION –
Lubiprostone is a bicyclic fatty acid ( prostaglandin E1 derivative ) which acts by specifically activating CIC-2 chloride channels on the apical aspect of GIT epithelial cells, producing a chloride-rich fluid secretion.
These secretion soften the stool, increase motility , and promote spontaneous bowel movements.
THERAPEUTIC USES –
1. Lubiprostone is used for treating chronic constipation and constipation caused by opioid medicines in certain patients.
2. It is also used to treat irritable bowel syndrome ( IBD ) with constipation in women.
SIDE EFFECTS –
Nausea
Diarrhea
Headache
Frequent bowel movements
Fecal incontinence
Flatulence
Decreased appetite
Rashes
DRUG-DRUG INTERACTION –
Lubiprostone + Methadone = therapeutic efficacy of lubiprostone can be decreased .
Reference- Tripathi KD "Essential of medical pharmacology" 7th edition, page no- 675
MECHANISM OF ACTION –
Lubiprostone acts by specifically activating CIC-2 chloride channels, which is a normal constituent of the apical membrane of the human intestine, in a protein kinase A action independent fashion. Activation of CIC-2 chloride channels causes an efflux of chloride ions into the lumen, which in turn leads to an efflux of sodium ions through a paracellular pathway to maintain isoelectric neutrality. As a result, water follows sodium into the lumen in order to maintain isotonic equilibrium, thereby increasing intestinal fluid secretion. By increasing intestinal fluid secretion, lubiprostone increases motility in the intestine, thereby increasing the passage of stool and alleviating symptoms associated with chronic idiopathic constipation.
PHARMACOLOGICAL ACTION –
Lubiprostone is a bicyclic fatty acid ( prostaglandin E1 derivative ) which acts by specifically activating CIC-2 chloride channels on the apical aspect of GIT epithelial cells, producing a chloride-rich fluid secretion.
These secretion soften the stool, increase motility , and promote spontaneous bowel movements.
THERAPEUTIC USES –
1. Lubiprostone is used for treating chronic constipation and constipation caused by opioid medicines in certain patients.
2. It is also used to treat irritable bowel syndrome ( IBD ) with constipation in women.
SIDE EFFECTS –
Nausea
Diarrhea
Headache
Frequent bowel movements
Fecal incontinence
Flatulence
Decreased appetite
Rashes
DRUG-DRUG INTERACTION –
Lubiprostone + Methadone = therapeutic efficacy of lubiprostone can be decreased .
Reference- Tripathi KD "Essential of medical pharmacology" 7th edition, page no- 675
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