Generic

Lubiprostone

Indications

Irritable Bowel Syndrome with Constipation is treated with Lubiprostone (IBS-C).

Adults with Chronic Idiopathic Constipation (CIC).

Constipation caused by opioids in adult patients with chronic, non-cancer pain.

Pharmacology

Lubiprostone is a chloride-channel activator that works locally to promote intestinal secretion. It does this by increasing intestinal motility, which aids stool passage and relieves the symptoms of chronic idiopathic constipation.

Lubiprostone works by triggering a protein kinase reaction that activates ClC-2 chloride channels, which are found in the apical membrane of the human intestine. A style that is unaffected by motion. When ClC-2 chloride channels are activated, chloride ions are effluxed into the lumen, which is followed by sodium ions being effluxed through a paracellular pathway to preserve isoelectric neutrality. As a result, water takes after sodium into the lumen in arrange to preserve isotonic balance, in this manner expanding intestinal liquid emission. By expanding intestinal liquid secretion, lubiprostone increments motility within the digestive tract, in this manner expanding the entry of stool and lightening side effects related with incessant idiopathic stoppage. Actuation of ClC-2 chloride channels may too invigorate the recuperation of muscosal barrier function by reestablishing tight intersection protein complexes within the digestive tract. Fix clamp cell considers in human cell lines have demonstrated that the lion's share of the useful natural action of lubiprostone and its metabolites is watched as it were on the apical (luminal) parcel of the gastrointestinal epithelium.

Dosage & Administration

Irritable Bowel Syndrome with Constipation: The recommended dose is 8 mcg twice daily orally with food and water.

Dosage in patients with hepatic impairment: Dosage adjustment is not required for patients with moderately impaired hepatic function. For patients with severely impaired hepatic function, the recommended starting dose is 8 mcg once daily. If tolerated then dose can be increased to 8 mcg twice

Chronic Idiopathic Constipation and Opioid-induced Constipation: The recommended dose is 24 mcg twice daily orally with food and water.

Dosage in patients with hepatic impairment: For patients with moderately impaired hepatic function, the recommended starting dose is 16 mcg twice daily. For patients with severely impaired hepatic function, the recommended starting dose is 8 mcg twice daily.

Interaction

Lubiprostone's efficacy may be reduced in patients using diphenylheptane opioids in a dose-dependent manner.

Contraindications

Lubiprostone is not recommended for anyone who have a mechanical gastrointestinal obstruction, whether they know it or not.

Side Effects

Diarrhea, a sense of fullness or pressure in the stomach, nausea, stomach pain, abdominal or stomach edema Dyspnea.

Pregnancy & Lactation

Category C pregnancy. Whether lubiprostone is excreted in human milk is unknown. Human milk-fed infants should be watched for diarrhea because lubiprostone increases fluid secretion in the intestine and intestinal motility. When Lubiprostone is given to a nursing mother, it should be done with caution.

Precautions & Warnings

Nausea is a possible side effect of taking Lubiprostone. Food taken at the same time as Lubiprostone may help to alleviate nausea symptoms.

Lubistone should not be given to patients who are suffering from severe diarrhea.

Bowel Obstruction: Before starting Lubiprostone therapy in patients with symptoms that suggest a mechanical gastrointestinal obstruction, undertake a complete assessment to determine the absence of an obstruction.

Therapeutic Class

Other types of laxatives.

Storage Conditions

Store between 15-30° C.

Pharmaceutical Name

Incepta Pharmaceuticals Ltd.