MICROLAX SORBITOL CITRATE AND SODIUM LAURILSULFOACETATE S rectal in single-dose container 12Single-dose-containers-can/5ml

Rectal solution in single-dose container.

Crystallisable sorbitol at 70 %.................................................................................................................. 4,4650 g

Sodium citrate..................................................................................................................................... 0,4500 g

Sodium laurilsulfoacetate at 70 %.................................................................................................... 0,0645 g

For one single-dose container.

6,45 g = 5 ml of rectal solution

Excipient(s) with known effect: sorbic acid

Excipients:

Symptomatic treatment of occasional constipation.

Reserved for adults.

Dosage

1 single-dose container per day.

The dose should be administered 5 to 20 minutes before the expected effect.

Method of administration

Rectal route.

Break the tip.

Insert the full length of the cannula into the rectum and expel the entire contents of the tube by pressure, withdraw the cannula without releasing pressure on the tube.

• Hypersensitivity to the active substances or to any of the excipients listed in section Composition.

• Intestinal obstruction and abdominal pain of unknown aetiology.

• Concomitant treatment with sodium sulfo cation-exchange resin (see section Interactions).

• Concomitant treatment with calcium sulfo cation-exchange resin (see section Interactions).

Warnings

Prolonged use is not recommended. If symptoms persist for more than a few days or worsen, medical advice is required.

Drug treatment of constipation is only an adjunct to hygienic-dietary treatment:

• enrichment of the diet with vegetable fibres and fluids;

• advice on physical activity and re-education of defecation.

Precautions for use

It is recommended to avoid the use of this medicine in cases of hemorrhoidal flare-ups, anal fissures, or hemorrhagic proctocolitis.

It is recommended to exercise extreme caution in patients with inflammatory or ulcerative diseases affecting the colon or in patients suffering from acute gastrointestinal disorders.

This medicine contains sorbic acid, which may cause local skin reactions (for example, contact dermatitis).

Contraindicated combinations

+ Sodium sulfo-cationic resin (oral and rectal routes of sorbitol or resin)

Risk of colonic necrosis, possibly fatal.

+ Calcium sulfo-cationic resin (oral and rectal routes of sorbitol or resin)

Risk of colonic necrosis, possibly fatal.

Any other medicine administered rectally should be used at a distance from MICROLAX, as it may be eliminated by the gastrointestinal tract without having been absorbed.

Pregnancy

There are no adequate data on pregnant women, and no well-controlled clinical study has been conducted in these patients.

Under normal conditions of use, no effect on pregnancy is expected, as systemic exposure to the product is likely to be limited.

As a result, use of this medicine should only be considered during pregnancy if necessary.

Breast-feeding

There is no data to determine whether sorbitol, sodium citrate and sodium laurilsulfoacetate are excreted in breast milk.

Under normal conditions of use, no effect on breastfed newborns/infants is expected, as systemic exposure to the product is likely to be limited.

Consequently, use of this medicine during breastfeeding should only be considered if necessary.

Fertility

Studies conducted in rats and rabbits (only with sorbitol) showed no effect on fertility (see section Preclinical safety).

This medicine has no or negligible influence on the ability to drive and use machines.

The following table describes the adverse effects that have been reported during post-marketing use with sorbitol, sodium citrate and sodium laurilsulfoacetate. The frequency of adverse effects is defined using the following convention:

• Very common (≥ 1/10)

• Common (≥1/100, < 1/10)

• Uncommon (≥ 1/1000, < 1/100)

• Rare (≥ 1/10000, < 1/1000)

• Very rare (< 1/10000)

• Frequency not known (cannot be estimated from the available data).

System organ	Adverse effects
Frequency
Immune system disorders
Frequency not known	Anaphylactic reaction
	Hypersensitivity reactions (such as urticaria)
Gastrointestinal disorders
Frequency not known	Abdominal paina
	Anorectal discomfort
	Liquid stools

   a : includes abdominal discomfort, abdominal pain and upper abdominal pain.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reaction via the national reporting system: National Agency for the Safety of Medicines and Health Products (ANSM) and the network of Regional Centres of Pharmacovigilance - Website:https://signalement.social-sante.gouv.fr/.

No cases of overdose have been reported during post-marketing use or in the scientific literature. However, prolonged use may give rise to anal burning sensations and, exceptionally, congestive proctitis.

Pharmacotherapeutic class: ENEMA, ATC code: A06AG11 (A: alimentary tract and metabolism).

Mechanism of action

Sodium citrate has an emollient effect on hard stools, linked to its penetration into the fecal bolus and the release of water. Sodium lauryl sulfoacetate improves the wetting and penetration capacities of the solution, and sorbitol increases the water-releasing effect of sodium citrate.

Onset of action: 5 to 20 minutes.

The active substances probably have limited systemic absorption and are eliminated in the stools.

Absorption

Sodium citrate

There is no study describing the absorption of sodium citrate following rectal administration in humans.

Sodium lauryl sulfoacetate

There is no study describing the absorption of sodium lauryl sulfoacetate following rectal administration in humans.

Sorbitol

Sorbitol is poorly absorbed by the gastrointestinal tract following rectal administration.

Distribution

There is no study describing the distribution of sodium citrate, sodium lauryl sulfoacetate and sorbitol following rectal administration in humans.

Biotransformation

There is no study describing the biotransformation of sodium citrate, sodium lauryl sulfoacetate and sorbitol following rectal administration in humans.

Elimination

Sodium citrate, sodium lauryl sulfoacetate and sorbitol are mainly eliminated in the feces.

The medicinal product showed negligible toxicity in dogs following repeated clinical (rectal) administration. A safety pharmacology study in dogs was carried out following intravenous administration of 1,33 mmol/kg/h of citrate solution (composed of a mixture of citric acid and sodium citrate with a molar ratio of 1 : 5,25). A decrease in blood pressure and a prolongation of the QT interval were observed: these are explained by a reduction in the blood Ca2+ level due to the chelating action of citrate (the citrate level tolerated intravenously in conscious dogs is 0,33 mmol/kg/h). Given the posology of the medicinal product, it is considered that chelation of blood Ca2+ does not represent a clinical risk for patients.

Data available in the literature have shown that the active substances generally presented low toxicity in repeated-dose oral administration studies.

No adverse effects were reported for sodium citrate in repeated-dose toxicity studies at doses up to 1 500 mg/kg/day. The repeated-dose toxicity study of sodium lauryl sulfoacetate in rats revealed no signs of systemic toxicity at doses up to 75 mg/kg/day. Repeated-dose toxicity studies conducted in rats demonstrated that sorbitol was well tolerated.

Sodium citrate and sorbitol showed no genotoxic effects in in vitro and in vivo tests. Sodium lauryl sulfoacetate showed no genotoxic effects in in vitro tests.

Sodium citrate and sodium lauryl sulfoacetate had no carcinogenic effect in rats. According to long-term dietary studies conducted in rats, sorbitol had no carcinogenic effect.

Sodium citrate did not cause a teratogenic effect in rats. No teratogenic effect was reported following oral administration of 1 000 mg/kg/day of sodium lauryl sulfoacetate in rats. Sorbitol did not cause a teratogenic effect in rabbits and rats after incorporation into food (up to 20% sorbitol).

Oral treatment with sodium citrate showed no reprotoxic effect in rats. In a reproduction and developmental toxicity study conducted in rats, no effect on growth, fertility and reproductive capacity was observed after oral administration of doses of sodium lauryl sulfoacetate up to 1 000 mg/kg/day. In non-clinical studies conducted in rats exposed to sorbitol through food, no treatment-related effect was reported in terms of mating capacity, pregnancy, reproductive performance, newborns or histopathology.

3 years.

No special precautions for storage.

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

Marketing authorisation (AMM)

CIP 3400956207244 (50 single-dose containers/5 mL). CIP 3400934968754 (4 single-dose containers/5 mL). CIP 3400934968815 (12 single-dose containers/5 mL).

Not reimbursed by social security (4 single-dose containers/5 mL, 12 single-dose containers/5 mL).
Hospital model(s) (50 single-dose containers/5 mL).
Collection.