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Lubiprostone (rINN, marketed under the trade name Amitiza among others) is a drug used in the management of chronic idiopathic constipation, particularly the constellation of intestinal constipation associated with syndrome in women and opioids-induced constipation.

Initially approved by the Food and Drug Administration (FDA) in 2006 and recommended for use in the United Kingdom by the National Institute for Health and Care Excellence (NICE) in 2014. This is expensive in 2017, with costs to the NHS being Ã, £ 29, 68 per 24mg 28-cap pack as of April 2017.


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Medical use

Lubiprostone is used for the treatment of chronic constipation of unknown causes in adults, as well as irritable bowel syndrome associated with constipation in women.

Lubiprostone is approved for treating chronic idiopathic constipation (CIC) in adults.

Lubiprostone is also approved for treating opioid-induced constipation, in adults with chronic non-cancer pain. The effectiveness of lubiprostone has not been established in patients taking diphenylated opioids (eg, methadone).

Lubiprostone is approved for treating irritable bowel irritation syndrome (IBS-C) in women 18 years and older.

On November 12, 2014, lubiprostone has not been studied in children. There is currently research to determine the safety and efficacy of postoperative bowel dysfunction.

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Adverse effects

In clinical trials, the most common side effect was nausea (31%). Other side effects (> = 5% of patients) include diarrhea (13%), headache (13%), abdominal distension (5%), abdominal pain (5%), flatulence (6%), sinusitis (5% vomiting (5%) and fecal incontinence (1%).

Contraindications

No recent data is used in people with liver or kidney complications. The effects on pregnancy have not been studied in humans but testing on guinea pigs produces fetal loss. Amitiza is not approved for use in children. Lubiprostone is contraindicated in patients who exhibit chronic diarrhea, intestinal obstruction, or diarrheal bowel irritation syndrome.

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Action mechanism

Lubiprostone is a bicyclic fatty acid derived from prostaglandin E1 which acts to actively activate the ClC-2 chloride channel on the apical aspects of gastrointestinal epithelial cells, resulting in the secretion of chloride-rich liquids. This secretion softens the stool, improves motility, and promotes spontaneous bowel movement (SBM).

Constipation symptoms such as pain and bloating usually improve within a week, and SBM can occur in one day.

Lubiprostone Prevents Nonsteroidal Anti-Inflammatory Drugâ€
src: jpet.aspetjournals.org


Pharmacokinetics

Unlike many laxatives, lubiprostone shows no signs of tolerance, dependence, or altered serum electrolyte concentrations. No rebound effects after withdrawal treatment, but gradually returning to the frequency of pre-treatment bowel movement should be expected.

Minimal drug distribution occurs outside the immediate gastrointestinal tissues. Lubiprostone is rapidly metabolized by reduction/oxidation, mediated by carbonyl reductase. There is no metabolic involvement of the liver cytochrome P450 system. Measurable metabolites, M3, are present in very low levels in plasma and make up less than 10% of the total dose administered.

Data show that metabolism occurs locally in the abdomen and jejunum.

a50246853ex99-1.htm
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Society and culture

Legal status

Lubiprostone received approval from the Food and Drug Administration in 2008 to treat intestinal irritation syndrome with constipation (IBS-C) and is available only through prescription. In 2014, the drug is available in the United States, Japan, Switzerland, India and the UK; Reviews by Health Canada begin at the end of 2014.

Brand name

In Bangladesh and India, lubiprostone is marketed under the trade name Lubilax by Beacon Pharmaceuticals Limited, and under the trade name Lubowel by SunPharma.

a50246853ex99-1.htm
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References


Lubiprostone Prevents Nonsteroidal Anti-Inflammatory Drugâ€
src: jpet.aspetjournals.org


External links

  • Official Site

Source of the article : Wikipedia

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