1- active ingredient
1mg prucalopride
2-mechanism of action
-Prucalopride, a first in class dihydro-benzofuran-carboxamide, is a selective, high affinity serotonin 5-HT4 receptor agonist with enterokinetic activities.
-Prucalopride alters colonic motility patterns via serotonin 5-HT4 receptor
-stimulation: it stimulates colonic mass movements, which provide the main propulsive force for defecation.
-The observed effects are exerted via highly selective action on 5-HT4 receptors
-prucalopride has >150-fold higher affinity for 5-HT4 receptors than for other receptors.
-Prucalopride differs from other 5-HT4agonists such as tegaserod and cisapride, which at therapeutic concentrations also interact with other receptors (5-HT1B/D and the cardiac human ether-a-go-go K+ or hERG channel respectively) and this may account for the adverse cardiovascular events that have resulted in the restricted availability of these drugs.
-Clinical trials evaluating the effect of prucalopride on QT interval and related adverse events have not demonstrated significant differences compared with placebo.
3-efficacy of the drug:-
-The primary measure of efficacy in the clinical trials is three or more spontaneous complete bowel movements per week
-a secondary measure is an increase of at least one complete spontaneous bowel movement per week.
- Further measures are improvements in *PAC-QOL (a quality of life measure)
and
*PAC-SYM (a range of stool,abdominal, and rectal symptoms associated with chronic constipation).
- Infrequent bowel movements, bloating, straining, abdominal pain, and defecation urge with inability to evacuate can be severe symptoms, significantly affecting quality of life.
-In three large clinical trials, 12 weeks of treatment with prucalopride resulted in a significantly higher proportion of patients reaching the primary efficacy endpoint of an average of ≥3 spontaneous complete bowel movements than withplacebo.
-There was also significantly improved bowel habit and associated symptoms, patient satisfaction with bowel habit and treatment, and HR-QOL in patients with severe chronic constipation, including those who did not experience adequate relief with prior therapies
(>80% of the trial participants).
- The improvement in patient satisfaction with bowel habit and treatment was maintained during treatment for up to 24 months
***prucalopride therapy was generally well tolerated.
4-contraindications
-resolor is contraindicated where there ishypersensitivity to the active substance or to any of the excipients, renal impairmentrequiring dialysis,
*intestinal perforation
or
*obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of theintestinal tract, such as Crohn's disease, andulcerative colitis and toxic megacolon and megarectum.
posted from Bloggeroid
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