Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic group: Sodium picosulfate, combinations, ATC code: A06A B58.
The active components of CitraFleet are sodium picosulfate, a stimulant cathartic, active locally in the colon, and magnesium citrate which acts as an osmotic laxative by retaining moisture in the colon. The action is of a potent 'washing out' effect combined with peristaltic stimulation to clear the bowel prior to radiography, colonoscopy or surgery. The product is not intended for use as a routine laxative.

In a randomized, multicentre, rater-blinded study in adults, bowel cleansing prior to colonoscopy using two different regimens of CitraFleet was compared with that following Klean-Prep (each sachet containing 59 g polyethylene glycol 3350, 5.685 g anhydrous sodium sulfate, 1.685 g sodium bicarbonate, 1.465 g sodium chloride and 0.7425 g potassium chloride; to be dissolved in 1 litre of water) The treatment groups were: late prior-day CitraFleet (2 sachets, 5 hours apart during the afternoon and evening the day before colonoscopy, n=229); late prior-day Klean-Prep (4 sachets administered during the afternoon and evening the day before colonoscopy, n=227); same-morning CitraFleet (2 sachets, 3 hours apart on the morning before colonoscopy, n=56).
Bowel cleansing was assessed using a categorical scale (excellent, good, fair and poor).
Good/excellent cleansing was reported in 68.1% of patients on the late prior-day CitraFleet regimen (not statistically different from Klean-Prep), while a significantly higher proportion of patients had good/excellent cleansing with same-morning CitraFleet compared with either late prior-day regimen (p<0.05). Both CitraFleet regimens were rated as significantly easier to complete by patients than Klean-Prep (p<0.001). All regimens were well tolerated, with only       2.2% of patients on the late prior-day CitraFleet regimen having adverse drug reactions. There were no serious adverse drug reactions.

In a randomized, multicentre, rater-blinded study in adults, bowel cleansing prior to colonoscopy was compared using two different regimens of CitraFleet: split-dose (1 sachet in the evening the day before colonoscopy, and another sachet on the morning before colonoscopy, n=159); early prior-day regimen (1 sachet before 0800h the day before colonoscopy and another sachet 6-8 hours later, n=156). Bowel cleansing was assessed using a categorical scale (excellent, good, fair and poor). A significantly higher proportion of patients on the split-dose regimen had good/excellent cleansing (79.9% vs 30.8% for early prior-day, p<0.0001). Over 93% of patients in both groups rated the regimens as ‘easy’ or ‘very easy’ to take. Both regimens were well tolerated, with 1.9% and 2.5% of patients having adverse drug reactions in the split-dose and early prior-day groups, respectively. More patients in the split-dose group than in the early prior-day group reported nausea (23.3% vs 13.5%) and overall physical discomfort (29.6% vs 17.3%), while more patients in the early prior-day group reported hunger (46.2% vs 32.1% with split-dose).
There were no serious adverse drug reactions. Overall, changes in electrolyte levels and other laboratory parameters were minor in both groups.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

Both active components are locally active in the colon, and neither is absorbed in any detectable amounts.

In patients with severely reduced renal function, accumulation of magnesium in plasma may occur.