Picoprep Mechanism of Action




Zuellig Pharma
Full Prescribing Info
Pharmacotherapeutic group: Contact Laxatives. ATC code: A06A B58.
Pharmacology: Pharmacodynamics: The active components of PICOPREP are sodium picosulfate and magnesium citrate. Sodium picosulfate is a locally acting stimulant cathartic, which after bacterial cleavage in the colon forms the active laxative compound, bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), which has a dual-action with stimulation of the mucosa of both the large intestine and of the rectum. Magnesium citrate acts as an osmotic laxative by retaining moisture in the colon. The combined action of the two substances is of a 'washing out' effect combined with peristaltic stimulation to clear the bowel.
The product is not intended for use as a routine laxative.
Pharmacokinetics: Sodium picosulfate and magnesium citrate, the two components of PICOPREP, are locally active, with minimal systemic exposure.
After administration of PICOPREP (2 sachets separated by 6 hours), picosulfate reached a mean levels of 2.3 and 3.2 ng/mL (Cmax) at a median of 2 and 8 hours (Tmax) after the first and second sachet, respectively. The corresponding values for magnesium were 0.88 and 0.95 mmol/L at 4 and 10 hours, respectively. The baseline value was 0.75 mmol/L.
The mean terminal half-life of picosulfate was 7.4 hours. The fraction of the sodium picosulfate dose excreted unchanged in urine was 0.11%. Plasma levels of BHPM were consistently low or undetectable and urinary samples showed that the majority of excreted BHPM was the glucuronide-conjugated form.
Clinical studies in bowel cleansing before colonoscopy have shown an increase from baseline to colonoscopy visit in serum magnesium of approximately 0.11 mmol/L (from 0.86 to 0.97 mmol/L). All changes in serum magnesium were transient and within normal limits, including in patients with mild to moderate renal impairment.
Toxicology: Preclinical Safety Data: Non-clinical data reveal no special hazard for humans based on conventional studies of repeated dose toxicity and genotoxicity.
Due to the very short treatment duration no long-term studies in animals have been performed.
Reproductive studies have shown no potential for impairment of fertility or harm to the foetus for sodium picosulfate and PICOPREP.
In a study on pre- and postnatal development, the NOAEL of PICOPREP was the mid dose of 750 mg/kg BID. The adverse effect that occurred in the 2000 mg/kg BID group (approximately 8 times the recommended human dose), was pup mortality, between lactation days 2 to 4 due to maternal toxicity.
Effects in reproductive and developmental toxicity studies with sodium picosulfate alone were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
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