Chronic idiopathic constipation

Tegaserod maleate (Zelnorm) is a partial serotonin (5-HT4) receptor agonist that causes an increase in peristaltic activity and intestinal secretion and moderation of visceral sensitivity. It increases the frequency of bowel movements and reduces abdominal discomfort, bloating, and straining. It is indicated for the treatment of patients younger than 65 years of age who experience chronic idiopathic constipation. The most common adverse effects include headache, abdominal pain, diarrhea, and nausea. 

Lubiprostone (Amitiza), a bicyclic acid oral agent, is approved for treatment of chronic idiopathic constipation in adults. It has not been studied in children. Lubiprostone acts locally on intestinal chloride channels and increases intestinal fluid secretion, resulting in increased intestinal motility and thereby increasing the passage of stool.6... 

C. R., Colonic motility in man features in normal subjects and in patients with chronic idiopathic constipation, Am. J. Gastroenterol. 1999, 94, 1760-1770. 

Besides constipation-related IBS, several studies have also suggested abnormalities of colonic bacterial composition in chronic idiopathic constipation [125]. Here again antibiotic treatment with vancomycin [126, 127], rova-mycin (in combination with diphetarsone, an amebicidal agent) [128,129] or erythromycin [130], which, however, displays a prokinetic activity [131, 132], proved to be capable of reversing long-lasting constipation. Furthermore, the efficacy in both clinical conditions of probiotics [133-135] lends further support to the pathogenic role of bowel flora. 

Celik AF, Tomlin J, Read NW The effect of oral vancomycin on chronic idiopathic constipation. Aliment Pharmacol Ther 1995 9 63-68. 

Lubiprostone is a chloride channel activator that acts locally on the gut to accelerate genitourinary transit time and delay gastric emptying. It is approved for chronic idiopathic constipation in adults. The dose is 24 mg capsule twice daily with food. Lubiprostone may cause headache, diarrhea, and nausea. 

FGIDs present with variable combinations of chronic or recurring GI symptoms not explained by overt biochemical or structural abnormalities and encompass conditions like functional dyspepsia (FD), irritable bowel syndrome (IBS) and chronic idiopathic constipation [1], A variety of mechanisms that could explain the etiology of FGIDs are currently under investigation and include, but are not limited to altered GI motility, visceral hypersensitivity and post-infectious abnormalities [2],... 

Chronic, idiopathic constipation - Short-term trials have shown an acceleration of intestinal transit in healthy individuals and in those with chronic constipation. Improvement in stool frequency in patients with chronic constipation has been... 

Chronic idiopathic constipation For the treatment of patients younger than 65 years of age with chronic idiopathic constipation. 

The efficacy of tegaserod for the treatment of IBS with constipation or chronic idiopathic constipation has not been studied beyond 12 weeks. 

Chronic idiopathic constipation The recommended dosage is 6 mg taken twice daily orally before meals. 

Elderly Patients 65 years of age and older who received tegaserod for chronic idiopathic constipation experienced a higher incidence of diarrhea and discontinuations because of diarrhea than patients younger than 65 years of age. Pregnancy Category B. Use during pregnancy only if clearly needed. 

Lubiprostone (Amitiza) [Laxative] Uses Chronic idiopathic constipation in adults Action Selective Cl channel activator Dose Adults. 24 meg PO bid w/ food Contra Mechanical GI obst Caution [C, /-] Severe D, severe renal or mod-severe hepatic impair Disp Gel, caps meg SE N, HA, D, GI distention, abd pain EMS Monitor for signs of electrolyte disturbances and h5rpovolemia d/t D OD May cause severe D, hypovolemia, and abd pain/cramps give IV fluids Lutropin Alfa (Luveris) [Hormone] Uses Inf ility Action Recombinant LH Dose 75 Units SQ w/ 75—150 Units FSH, 2 s arate inj max 14 d Caution [X, /M] Contra Primary ovarian failure, uncontrolled thyroid/adrenal dysfxn, intracranial lesion, AUB, hormone-dqjendent GU tumor, ovarian cyst, PRG Disp Inj SE HA, N, ovarian h5rpCTstimulation synd, breast pain, ovarian cysts T risk of multiple births EMS None OD Unlikely to cause life-threatening Sxs... 

Gnest JF, Varney SJ. Pharmacoeconomic impact of low-dose macrogol 3350 plus electrolytes compared with lactulose in the management of chronic idiopathic constipation among ambnlant patients in Belginm. Chn Dmg Investig 2004 24(12) 719-29. 

The standard pharmacokinetic parameters of the compound such as a half-life or bioavailability cannot be reliably calculated, because the concentrations in plasma are below lOpg/mL. As analogously expected from the results on the shift in keto-alcohol equilibrium of 16,16-difluoro-PGE2, it is rapidly metabolized by C-15 reduction mediated by the ubiquitously expressed carbonyl reductase. The metabolism followed by jS-oxidation and co-oxidation forms a mixture of a and fi epimers at the 15-hydroxy moiety as a sole measurable metabolite [46], In 2006, the US Food and Drug Administration approved the drug application for an oral treatment of chronic idiopathic constipation in adults, estimating that 4-5 million Americans are affected. Lubiprostone has also completed a phase II trial in constipation-predominant irritable bowel syndrome, and has been further evaluated for other bowel dysfunctions. 

Naloxone is being used to reverse the potentially lethal respiratory depression caused by neurolept analgesia or opioid overdose. Among other pharmacological effects, naloxone antagonizes the blood pressure drop in various forms of shock [29-32], reverses neonatal hypoxic apnoea [26], counteracts chronic idiopathic constipation [34], reduces the food intake in humans [35, 36] and shows beneficial effects in CNS injuries [37]. 

Cook, B.J., Lim, E., Cook, D., Hughes, J., Chow, C.W., Stanton, M.P., Bidarkar, S.S., Southwell, B.R. and Hutson, J.M. (2005) Radionudear transit to assess sites of delay in large bowel transit in children with chronic idiopathic constipation. Journal of Pediatric Surgery, 40, 478—483. 

Sucampo/ Treatment of chronic idiopathic constipation in adults... 

Lubiprostone is a water-insoluble heptanoic acid derivative used in the treatment of chronic idiopathic constipation in adults, and is solubilized in medium-chain triglyceride in 24 pg Amitiza soft gelatin capsules. The dose of lubiprostone is 24 pg (one capsule) twice daily with food. Amitiza should be stored at controlled room temperature and was approved in the USA in 2006. 

Tegaserod maleate is a GI agent that binds with high affinity to human 5-HT4 receptors, acting as an agonist at neuronal 5-HT4 receptors to trigger the release of neurotransmitters. Activation of 5-HT4 receptors in the GI tract stimulates peristaltic reflex and intestinal secretion, and inhibits visceral sensitivity. It is used for short-term treatment of women with irritable bowel syndrome (IBS) whose primary symptom is constipation and in treatment of patients younger than 65 years of age with chronic idiopathic constipation. 

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