Pico-Salax

White crystalline powder with a faint odour of orange.
The faint flavour of orange can still be detected even after reconstitution.
Each sachet contains the following active ingredients: Sodium picosulfate 10.0 mg, Light magnesium oxide 3.5 g, Anhydrous citric acid 12.0 g.
Each sachet also contains: Potassium hydrogen carbonate 0.5 g [equivalent to 5 mmol (195 mg) potassium], Lactose (as a component of the flavour).
Excipients/Inactive Ingredients: Potassium hydrogen carbonate; Sodium saccharin; Natural, spray dried orange flavour which contains acacia gum, lactose, ascorbic acid and butylated hydroxyanisole.

Pharmacotherapeutic group: Contact Laxatives. ATC code: A06A B58.
Pharmacology: Pharmacodynamics: Mechanism of action: Sodium picosulfate is hydrolyzed by colonic bacteria to form an active metabolite: bis-(p-hydroxyphenyl)- pyridyl-2-methane (BHPM), which acts directly on the colonic mucosa to stimulate colonic peristalsis.
Magnesium oxide and citric acid react to create magnesium citrate in solution, which is an osmotic agent that causes water to be retained within the gastrointestinal tract.
Pharmacodynamic effects: The stimulant laxative activity of sodium picosulfate together with the osmotic laxative activity of magnesium citrate produces a purgative effect which, when ingested with additional fluids, produces watery diarrhea that clears the bowel.
The product is not intended for use as a routine laxative.
Pharmacokinetics: Absorption: Sodium picosulfate, which is a prodrug, is converted to its active metabolite, BHPM, by colonic bacteria.
After administration of 2 sachets of PICO-SALAX separated by 6 hours, in 16 healthy subjects, sodium picosulfate reached a mean Cmax of 3.2 ng/mL at a median 8 hours (Tmax). After the first sachet, the corresponding value was 2.3 ng/mL at 2 hours. Magnesium oxide and citric acid react in solution to create magnesium citrate. Magnesium concentration value not corrected for baseline were 0.88 and 0.95 mmol/L at 4 and 10 hours, respectively. The baseline value was 0.75 mmol/L.
Distribution: The apparent volume (V/F) of sodium picosulfate was 3910 liters.
Biotransformation and Elimination: The fraction of the sodium picosulfate dose excreted unchanged in urine was 0.11%. Plasma levels of BHPM were low with 13 out of 16 subjects studied having plasma BHPM concentrations below the lower limit of quantification (0.1 ng/mL). Urinary samples show that the majority of excreted BHPM was in the glucuronide-conjugated form. The apparent clearance (CL/F) of sodium picosulfate was 463 L/h. The terminal half-life of sodium picosulfate was 7.4 hours.
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.
Pediatric population: The plasma concentration levels of sodium picosulfate and magnesium serum concentrations were comparable between adults and children. No dose adjustment is recommended for children in the 9 to 16-year age group due to the clinical effect and safety evaluation.

To clean the bowel prior to X-ray examination or endoscopy.
To clean the bowel prior to surgery when judged clinically necessary (see Precautions regarding open colorectal surgery).

Route of administration: Oral.
PICO-SALAX, supplied as a powder, must be reconstituted with cold water right before its use. There are two dosing regimens, each requires two separate dosing times: The preferred method is the "Split-Dose" method and consists of two separate doses: the first dose during the evening before the procedure and the second dose the next day, during the morning prior to the procedure.
The alternative method is the "Day Before" method and consists of two separate doses: the first dose during the afternoon or early evening before the procedure and the second dose 6 hours later during the evening before the procedure.
A low residue diet is recommended on the day prior to the hospital procedure. A clear liquid diet is recommended on the day of the procedure. To avoid dehydration it is important to follow the liquid intake recommendation as advocated together with the PICO-SALAX dosing whilst the effects of PICO-SALAX persist. Apart from the liquid intake together with the treatment regimen (PICO-SALAX + additional liquids), a normal, thirst driven intake of clear liquids is recommended. Clear liquids should include a variety of fruit juice without pulp, soft drinks, clear soup, tea, coffee (without milk, soy or cream) and water. Do not drink only water.
Additional fluids must be consumed after every dose in both regimens up until 2 hours before the time of the procedure. Instruct patients that if they experience severe bloating, distention, or abdominal pain following the first dose, delay the second dose until their symptoms resolve.
Directions for reconstitution: (a) Reconstitute the PICO-SALAX powder right before each administration. Do not prepare the solution in advance.
(b) Fill a cup with cold water (approximately 150 ml) and pour in the contents of one packet of PICO-SALAX powder.
(c) Stir for 2 to 3 minutes. The reconstituted PICO-SALAX solution may become slightly warm as the powder dissolves.
Adults: Split-Dose Dosing Regimen (Preferred Method): The Split-Dose regimen is the preferred dosing method. Instruct patients to take two separate doses in conjunction with fluids, as follows: Take the first dose during the evening before the procedure (e.g., 5:00 to 9:00 PM) followed by five 250 ml drinks (upper line on the dosing cup) of clear liquids before bed. Consume clear liquids within 5 hours.
Take second dose, the next day approximately 5 hours before the procedure followed by at least three 250 ml drinks of clear liquids before the procedure. Consume clear liquids within 5 hours up until 2 hours before the time of the procedure.
Day-Before Dosing Regimen (Alternative Method): The Day-Before regimen is the alternative dosing method for patients for whom the Split-Dosing is inappropriate. Instruct patients to take two separate doses in conjunction with fluids, as follows: Take the first dose in the afternoon or early evening (e.g., 4:00 to 6:00 PM) before the procedure followed by five 250 ml drinks (upper line on the dosing cup) of clear liquids before the next dose. Consume clear liquids within 5 hours.
Take the second dose approximately 6 hours later in the late evening (e.g., 10:00 PM to 12:00 AM), the night before the procedure followed by three 250 ml drinks of clear liquids before bed. Consume clear liquids within 5 hours.
Children: The first dose reconstituted in water as directed, taken before 8 am on the day before the procedure. Second dose 6 to 8 hours later.
1-2 years: ¼ sachet morning, ¼ sachet afternoon.
2-4 years: ½ sachet morning, ½ sachet afternoon.
4-9 years: 1 sachet morning, ½ sachet afternoon.
9 and above: adult dose.

Overdose would lead to profuse diarrhoea. Treatment is by general supportive measures and correction of fluid and electrolyte imbalance.

Hypersensitivity to the active substances or to any of the excipients listed in Description.
Congestive cardiac failure.
Gastric retention.
Gastrointestinal ulceration.
Toxic colitis.
Toxic megacolon.
Ileus.
Severe nausea and vomiting.
Acute surgical abdominal conditions such as acute appendicitis.
Known or suspected gastrointestinal obstruction or perforation.
Severe dehydration.
Rhabdomyolysis.
Hypermagnesemia.
Active inflammatory bowel disease.
In patients with severely reduced renal function, accumulation of magnesium in plasma may occur. Another preparation should be used in such cases.

Because a clinically relevant benefit of bowel cleansing prior to elective, open colorectal surgery could not be proven, bowel cleansers should only be administered before bowel surgery if clearly needed. The risks of the treatment should be carefully weighed against possible benefits and needs depending on surgical procedures performed.
An insufficient or excessive oral intake of water and electrolytes could create clinically significant, deficiencies, particularly in less fit patients. In this regard, patients with low body weight, children, the elderly, debilitated individuals and patients at risk of hypokalaemia or hyponatremia may need particular attention. Prompt corrective action should be taken to restore fluid/electrolyte balance in patients with signs or symptoms of hypokalaemia or hyponatremia.
Drinking only water to replace the fluid losses may lead to electrolyte imbalance which may in severe cases lead to complications such as seizures and coma. In rare cases, PICO-SALAX can cause severe or life-threatening electrolyte problems or impaired renal function in fragile or debilitated patients.
Care should also be taken in patients with recent gastrointestinal surgery as well as renal impairment, heart disease or inflammatory bowel disease.
Use with caution in patients on drugs that might affect water and/or electrolyte balance e.g. diuretics, corticosteroids, lithium (see Interactions).
PICO-SALAX may modify the absorption of oral medication and should be used with caution e.g. there have been isolated reports of seizures in patients on antiepileptics, with previously controlled epilepsy (see Interactions and Adverse Reactions).
The period of bowel cleansing should not exceed 24 hours because longer preparation may increase the risk of water and electrolyte imbalance.
This medicine contains 5 mmol (or 195 mg) potassium per sachet. This should be taken into consideration by patients with reduced kidney function or patients on a controlled potassium diet.
This medicine contains lactose as a component of the flavour. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
PICO-SALAX should not be used as a routine laxative.
Effects on Ability to Drive and Use Machines: Not relevant.

Pregnancy: There are no data with PICO-SALAX use in pregnant women to determine a drug-associated risk of adverse developmental outcomes.
In animal reproduction studies, no adverse developmental effects were observed in pregnant rats when sodium picosulfate, magnesium oxide, and anhydrous citric acid were administered orally at doses 1.2 times the recommended human dose based on body surface area during organogenesis.
PICO-SALAX should not be used during pregnancy unless the clinical condition of the woman requires treatment.
Breastfeeding: There is insufficient data on the use of PICO-SALAX in nursing mothers, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for PICO-SALAX and any potential adverse effects on the breastfed infant from PICO-SALAX.
Fertility: Studies with PICO-SALAX in animals have shown no impairment of fertility or embryo-fetal toxicity. In studies with sodium picosulfate alone, embryofetal toxicity has been observed in rats and rabbits at very high doses.

The most common adverse reactions are vomiting, nausea, abdominal pain and headache.
Hyponatraemia is rare but is the most commonly reported serious adverse reaction. Adverse reactions from spontaneous reports are presented by frequency category based on incidence in clinical trials when known. Frequency from spontaneous reports for adverse reactions never observed in clinical trials is based on an algorithm as recommended in the European Commission SmPC guideline, 2009, rev 2. (See table.)

Click on icon to see table/diagram/image

The absorption of other orally administered medicines (e.g. anti-epileptics, contraceptives, anti-diabetics, antibiotics) may be decreased during the treatment period (see Precautions).
Medicines with the potential to chelate with magnesium (e.g. tetracycline and fluoroquinolone antibiotics, iron, digoxin, chlorpromazine and penicillamine) should be taken at least 2 hours before and not less than 6 hours after administration of PICO-SALAX.
The efficacy of PICO-SALAX is lowered by bulk-forming laxatives.
Care should be taken with patients already receiving drugs which may be associated with hypokalaemia (such as diuretics or corticosteroids, or drugs where hypokalaemia is a particular risk i.e. cardiac glycosides). Caution is also advised when PICO-SALAX is used in patients on NSAIDs or drugs known to induce SIADH e.g. tricyclic antidepressants, selective serotonin re-uptake inhibitors, antipsychotic drugs and carbamazepine as these drugs may increase the risk of water retention and/or electrolyte imbalance.

Incompatibilities: Not applicable.

Store below 30°C. Store in the original package in order to protect from moisture.
Shelf-Life: 3 years. Once the sachet has been opened, use immediately and discard any unused powder or solution.

Laxatives, Purgatives

A06AB58 - sodium picosulfate, combinations ; Belongs to the class of contact laxatives.

NP