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| Clinical data | |
|---|---|
| Trade names | Amitiza |
| Other names | RU-0211 SPI-0211 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607034 |
| License data | |
| Routes of administration | By mouth |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | Negligible |
| Protein binding | 94% |
| Metabolism | Extensive,CYP not involved |
| Eliminationhalf-life | Unknown (lubiprostone) 0.9–1.4 hours (main metabolite) |
| Excretion | Kidney (60%) and fecal (30%) |
| Identifiers | |
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| CAS Number | |
| PubChemCID | |
| IUPHAR/BPS | |
| DrugBank |
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| ChemSpider |
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| UNII | |
| KEGG |
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| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.107.168 |
| Chemical and physical data | |
| Formula | C20H32F2O5 |
| Molar mass | 390.468 g·mol−1 |
| 3D model (JSmol) | |
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Lubiprostone, sold under the brand nameAmitiza among others, is amedication used in the management ofchronic idiopathic constipation, predominantlyirritable bowel syndrome-associated constipation in women andopioid-induced constipation. The drug is owned byMallinckrodt and is marketed byTakeda Pharmaceutical Company.
The drug was developed bySucampo Pharmaceuticals and approved by theFood and Drug Administration (FDA) in 2006.[2][3][4] It was recommended for use in the UK by theNational Institute for Health and Care Excellence (NICE) in July 2014.[5]Health Canada approved the drug in 2015.[6] Lubiprostone received approval from the Food and Drug Administration in 2008, to treat irritable bowel syndrome withconstipation (IBS-C),[7] and in 2013, for the treatment of opioid-induced constipation in adults with chronic noncancer pain.[4] It is available as ageneric medication.[8]
Lubiprostone is a laxative used for the treatment of constipation, specifically:[9]
Lubiprostone has not been studied in children.[10][12] There is current research under way to determine the safety and efficacy in postoperative bowel dysfunction.
It comes in a liquid filled capsule and is available only with a doctor's prescription.[10] If one misses a dose it should be taken as soon as possible unless it is almost time for the next dose, in which case it should be skipped and the user should return to their regular dosing schedule.[10]
In clinical trials, the most common adverse event wasnausea (31%). Other adverse events (≥5% of patients) includeddiarrhea (13%),headache (13%),abdominal distension (5%),abdominal pain (5%),flatulence (6%),sinusitis (5%),vomiting (5%), andfecal incontinence (1%).
The FDA lists the following:[3]
For subjects with chronic idiopathic constipation taking Amitiza:
For opioid-induced constipation:
For subjects with irritable bowel syndrome with constipation:
A 2018 pooled analysis from threephase III, randomized, double-blind, placebo-controlled studies on usage for Opioid-Induced Constipation, found that the numbers of patients reporting adverse effects were similar in both the lubiprostone and placebo treatment groups for all opioid classes (P ≥ 0.125); however, gastrointestinal adverse effects were reported more frequently by those receiving lubiprostone than 2 of the 3 opioid groups. The most commonly reported TEAEs in the lubiprostone treatment groups were nausea (13.4%–18.1%), diarrhea (1.2%–13.9%), and abdominal pain (4.7%–5.6%). In the population overall, the greatest likelihood of experiencing the first episode of any of these three TEAEs was greatest in the first week of treatment and decreased thereafter.[4]
According to Medscape, the most common (>10%) were: Nausea, Diarrhea (7-12%), Headache (2-11%). Less common side effects (1-10%) included: Abdominal pain (4-8%), Abdominal distension (3-6%), Flatulence (4-6%), Vomiting (3%), Loose stools (3%), Edema (1-3%), Abdominal discomfort (1-3%), Dizziness (3%), Chest discomfort/pain (2%), Dyspnea (2%), Dyspepsia (2%), Fatigue (2%), Dry mouth (1%).[13]
The effects on pregnancy have not been studied in humans, but testing inguinea pigs resulted in fetal loss.[medical citation needed]
Lubiprostone is contraindicated in people exhibiting chronicdiarrhea,bowel obstruction, or diarrhea-predominantirritable bowel syndrome.[medical citation needed]
Lubiprostone is a bicyclicfatty acid[15] derived fromprostaglandin E1 that acts by specifically activatingClC-2 chloride channels on the apical aspect of gastrointestinalepithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase intestinal transit and decrease gastric emptying, and promote spontaneous bowel movements.[15]
Unlike manylaxative products, lubiprostone does not show signs ofdrug tolerance,chemical dependency, or altered serumelectrolyte concentration.[16]
Minimal distribution of the drug occurs beyond the immediate gastrointestinal tissues.[medical citation needed] Lubiprostone is rapidly metabolized byreduction/oxidation, mediated by carbonyl reductase.[medical citation needed] There is no metabolic involvement of the hepaticcytochrome P450 system.[medical citation needed] The measurable metabolite, M3, exists in very low levels in plasma and makes up less than 10% of the total administered dose.[medical citation needed]
Data indicate that metabolism occurs locally in thestomach andjejunum.[17]
The cost to theNHS was £29.68 per 24 mcg 28-cap pack as of April 2017.
Lubiprostone is available in the United States, Japan, Switzerland, India, Bangladesh, the United Kingdom, and Canada.[citation needed]
InBangladesh andIndia, lubiprostone is sold under the brand name Lubigut byZiska Pharmaceuticals, Lubilax byBeacon Pharmaceuticals, and under the brand name Lubowel bySun Pharmaceutical.[citation needed]
Lubiprostone is also used to treat irritable bowel syndrome with constipation... in women who are at least 18 years of age.
Lubiprostone is a safe and efficacious drug for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation, with limited adverse effects in 3 months of follow-up.
