Regulax® picosulfate drops

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT REGULAX® PICOSULFATE DROPS

Composition:

Active substance: sodium picosulfate;

1 ml (20 drops) of solution contains sodium picosulfate monohydrate 7.5 mg (equivalent to sodium picosulfate 7.23 mg);

Excipients: sorbitol solution 70%, non-crystallizing; propylene glycol; purified water.

Pharmaceutical form. Oral drops, solution.

Main physicochemical properties: clear, colorless solution with a sweet, slightly bitter taste.

Pharmacotherapeutic group. Medicinal products used in the treatment of constipation. Stimulant laxatives. ATC code A06AB08.

Pharmacological properties.

Pharmacodynamics.

Sodium picosulfate, the active ingredient of the medicinal product REGULAX® PICOSULFATE DROPS, is a locally acting laxative of the triarylmethane group. After bacterial cleavage in the large intestine, sodium picosulfate stimulates the mucosa, accelerates peristalsis, and promotes accumulation of water and electrolytes in the lumen of the large intestine. As a result, defecation is stimulated, intestinal transit time is reduced, and stool softening occurs.

Pharmacokinetics.

Absorption and distribution.

After oral administration, sodium picosulfate reaches the large intestine without significant absorption.

Biotransformation and elimination.

After cleavage of sulfate esters by bacteria in the large intestine, a diphenolic laxative is formed, which is partially absorbed and, after conjugation, excreted with bile.

Relationship between pharmacokinetics and pharmacodynamics.

A small portion is excreted in urine as glucuronides; the majority is excreted in feces, both as free diphenols and as unchanged picosulfate. Information on plasma levels and protein binding is lacking. The onset of action of the medicinal product depends on the release of the active metabolite. The laxative effect of the medicinal product does not correlate with plasma levels of the active metabolite.

Clinical characteristics.

Indications.

For use in constipation or conditions requiring facilitation of defecation.

Like other laxatives, REGULAXâ PICOSULFATE DROPS should not be taken daily or for prolonged periods without identifying the cause of constipation.

Contraindications.

• Hypersensitivity to the active substance, other triarylmethanes, or to any of the excipients.
• Intestinal obstruction or acute abdominal disorders, e.g. appendicitis.
• Acute inflammatory bowel diseases.
• Acute abdominal pain associated with nausea and vomiting, which may indicate the aforementioned acute conditions.
• Severe dehydration.

REGULAXâ PICOSULFATE DROPS should be administered under medical supervision in conditions associated with disturbances in fluid and electrolyte balance (e.g. severe renal impairment).

Interaction with other medicinal products and other forms of interaction.

With prolonged use or use of high doses, hypokalemia may enhance the effect of cardiac glycosides. Potassium loss may be intensified when used concomitantly with diuretics or corticosteroids.

Since sodium picosulfate is metabolized into its active form by colonic bacteria, concomitant administration with antibiotics may result in reduced or absent laxative effect of REGULAXâ PICOSULFATE DROPS.

Special precautions for use

• Patients suffering from chronic constipation should undergo a complete diagnostic evaluation to determine the cause of constipation.
• The medicinal product should not be taken daily or for prolonged periods without first determining the cause of constipation. Prolonged or excessive use of the medicinal product may lead to disturbances in fluid and electrolyte balance and to hypokalemia.
• There have been reports of dizziness and/or loss of consciousness temporally associated with the use of sodium picosulfate: information on loss of consciousness during defecation (associated with Valsalva maneuver) or parasympathetic response to abdominal pain.
• REGULAXâ PICOSULFATE DROPS should be used under medical supervision in conditions associated with disturbances in water and electrolyte balance (e.g., severe renal dysfunction).
• After discontinuation of REGULAXâ PICOSULFATE DROPS, symptoms may recur. Recurrence of symptoms after prolonged use in chronic constipation may be associated with the presence of severe constipation.
• The medicinal product contains sorbitol; therefore, it should not be used in patients with hereditary fructose intolerance. REGULAXâ PICOSULFATE DROPS can be used by patients with diabetes mellitus, as it contains the sugar substitute sorbitol (1 ml of drops corresponds to 0.03 bread units (BU)). If you have an intolerance to certain sugars, consult your doctor before taking this medicinal product.

Use during pregnancy or breastfeeding

There are no clinical data on the use of sodium picosulfate during pregnancy; therefore, the medicinal product should not be used during pregnancy.

Clinical data indicate that neither the active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane, nor its glucuronides pass into breast milk. Therefore, REGULAXâ PICOSULFATE DROPS may be used during breastfeeding.

Fertility studies have not been conducted.

Effects on ability to drive and use machines

Studies on the effect on the ability to drive and operate machinery have not been conducted.

However, patients should be warned about possible vasovagal reactions (e.g., abdominal cramps) and/or adverse reactions such as dizziness and/or loss of consciousness. If abdominal cramps occur, patients should avoid potentially hazardous activities such as driving or operating machinery.

Method of Administration and Dosage

REGULAXâ PICOSULFATE DROPS should be taken orally as a single dose, preferably in the evening. The drops may be taken undiluted or mixed with a liquid.

The laxative effect usually occurs within 10–12 hours.

The recommended dose for adults is 14–27 drops (corresponding to 5–10 mg of sodium picosulfate). For children aged 4 years and older (only on medical advice), the dose is 7–14 drops (corresponding to 2.5–5 mg of sodium picosulfate).

It is recommended to start with the lowest dose. The dose may be adjusted to the maximum recommended dose to achieve regular bowel movements. The maximum daily dose must not exceed 27 drops for adults or 14 drops for children aged 4 years and older.

REGULAXâ PICOSULFATE DROPS should not be used daily or for prolonged periods without identifying the underlying cause of constipation.

Children

REGULAXâ PICOSULFATE DROPS is contraindicated in children under 4 years of age.

In children aged 4 years and older, the medication should be used only on medical advice.

Overdose

Symptoms:
Ingestion of large doses may cause diarrhea and intestinal spasms, as well as clinically significant fluid, potassium, and other electrolyte losses.

Ischemia of the colonic mucosa has been reported following ingestion of sodium picosulfate in doses substantially higher than those recommended for the treatment of constipation.

Prolonged overdose may lead to chronic diarrhea, abdominal pain, hypokalemia, secondary hyperaldosteronism, and kidney stone formation. With long-term use, renal tubular damage, metabolic alkalosis, and muscle weakness due to hypokalemia may also occur.

Treatment:
Shortly after drug ingestion, absorption may be reduced or prevented by inducing emesis or performing gastric lavage.

Rehydration therapy should be administered (replacement of fluid and electrolyte losses).

The use of spasmolytic agents may be beneficial.

Adverse reactions

Adverse reactions are listed by frequency of occurrence: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1,000, < 1/100); rare (≥ 1/10,000, < 1/1,000); very rare (< 1/10,000); unknown (cannot be estimated from available data).

Gastrointestinal disorders:

very common – diarrhea;

common – flatulence, abdominal pain or abdominal colic, abdominal discomfort;

uncommon – nausea and vomiting.

Immune system disorders:

unknown – allergic reactions, including Quincke's edema and skin reactions (angioneurotic edema, toxicoderma, rash, pruritus).

Nervous system disorders:

uncommon – dizziness;

unknown – syncope. Dizziness and/or syncope associated with defecation (Valsalva manoeuvre) or a parasympathetic response to abdominal pain.

Prolonged use or use of high doses may lead to increased excretion of water, potassium and other electrolytes. This may result in cardiac disturbances and muscle weakness, particularly when used concomitantly with diuretics and corticosteroids.

Shelf life. 5 years.

Shelf life after first opening of the bottle – 6 months.

Storage conditions.

Store at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

20 ml in a dropper bottle; 1 dropper bottle per cardboard box.

Pharmaceutical category. Over-the-counter (no prescription required).

Manufacturer.

Krewel Meuselbach GmbH.

Manufacturer's address.

Krewelstrasse 2, 53783 Eitorf, Germany.