PICOLAX

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PicoLax® (Picolaх)

Composition:

Active substance: sodium picosulfate;

1 ml of the preparation contains 7.5 mg of sodium picosulfate calculated as 100% anhydrous substance (20 drops);

Excipients: sorbitol (E 420); sodium benzoate (E 211); citric acid monohydrate; sodium citrate; water for injections.

Pharmaceutical form. Oral drops.

Main physicochemical properties: clear, colourless or slightly yellow liquid.

Pharmacotherapeutic group.

Contact laxatives. ATC code A06A B08.

Pharmacological properties.

Pharmacodynamics.

Sodium picosulfate, the active ingredient of PicoLax**®**, is a locally-acting laxative of the triarylmethane group. After bacterial cleavage in the large intestine, sodium picosulfate stimulates the mucosa, accelerating peristalsis and promoting 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 is softened.

Pharmacokinetics.

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

The active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane, is formed following bacterial cleavage in the large intestine. The onset of action of PicoLax**®** usually occurs 6–12 hours after administration, depending on the release of the active metabolite. After oral administration, only a negligible amount of the drug may be detected in organs and body systems.

The laxative effect of the drug does not correlate with the plasma concentration of the active metabolite.

Clinical characteristics.

Indications.

Constipation or conditions requiring facilitation of defecation.

Like other laxatives, Picolax® should not be used daily or for prolonged periods without determining the cause of constipation.

Contraindications.

• Hypersensitivity to the active substance, other triarylmethanes, or any of the excipients of the medicine.
• Dynamic or mechanical intestinal obstruction.
• Severe painful and/or febrile abdominal conditions (e.g., appendicitis), potentially associated with nausea and vomiting.
• Acute inflammatory bowel diseases.
• Severe dehydration.
• Rare hereditary intolerance to any of the excipients of the medicine, for example, suspected undiagnosed fructose intolerance (see section "Special precautions").

Picolax® should be administered under medical supervision in conditions associated with disturbances in fluid and electrolyte balance (e.g., severe renal impairment).

Picolax® must not be administered to children under 4 years of age.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of high doses of Picolax® with diuretics or corticosteroids may increase the risk of electrolyte imbalance, which may lead to increased sensitivity to cardiac glycosides.

Concomitant use with antibiotics may reduce the laxative effect of Picolax®.

Special precautions for use

Patients suffering from chronic constipation should undergo a full diagnostic evaluation to determine the cause of constipation.

Prolonged and excessive use of the drug may lead to disturbances in fluid and electrolyte balance and to hypokalemia.

Discontinuation of Picolax® may result in recurrence of symptoms. If Picolax® has been used for chronic constipation over a prolonged period, any recurrence of symptoms may be more pronounced.

Cases of dizziness and/or syncope occurring in temporal association with sodium picosulfate administration have been reported. Available data suggest that these events are consistent with defecation-induced syncope (associated with the Valsalva maneuver) or related to a vasovagal response to abdominal pain.

Patients with rare hereditary fructose intolerance should not take this medicine, as it contains sorbitol.

This medicinal product contains less than 1 mmol/dose of sodium, i.e. it is practically sodium-free.

This medicinal product contains 2 mg of sodium benzoate per 1 ml (30 mg sodium benzoate in the 15 ml bottle, 60 mg sodium benzoate in the 30 ml bottle).

Use during pregnancy or breastfeeding.

Pregnancy

Adequate clinical studies in pregnant women have not been conducted. Animal studies have demonstrated reproductive toxicity of the drug when administered at daily doses of 10 mg/kg and higher. For safety reasons, Picolax® should be avoided during pregnancy if possible.

Breastfeeding

Clinical data indicate that neither the active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), nor its glucuronides pass into breast milk. Therefore, Picolax® can be used during breastfeeding.

Fertility

Clinical studies evaluating the effect of the drug on fertility in humans have not been conducted.

Animal studies did not demonstrate any effect of the drug on fertility.

Ability to affect reaction speed when driving vehicles or operating machinery.

Studies on the influence of the drug on the ability to drive vehicles or operate machinery have not been conducted. However, patients should be warned about the possibility of developing adverse reactions such as dizziness and/or syncope as a result of a vasovagal response (particularly abdominal cramps). If abdominal cramps occur, patients should avoid potentially hazardous activities such as driving vehicles or operating machinery.

Method of Administration and Dosage

The medication is dosed using the manufacturer's dispenser.

Adults: 13–27 drops (corresponding to 5–10 mg of sodium picosulfate);
Children aged 4 years and older (only on medical advice): 7–13 drops (corresponding to 2.5–5 mg of sodium picosulfate).

It is recommended to start with the lowest dose. The dose may be adjusted up to the maximum recommended dose to achieve regular bowel movements. The maximum daily dose of 27 drops (for adults) or 13 drops (for children aged 4 years and older) must not be exceeded.

Picolax**®** should be taken at night. Bowel movement occurs approximately 10–12 hours after administration. The medication can be taken with or without liquid.

This medication should not be used daily or for prolonged periods without determining the underlying cause of constipation.

Children

This medication is indicated for children aged 4 years and older.

Overdose

Overdose may lead to watery stools (diarrhea), intestinal spasms, and clinically significant loss of fluids, potassium, and other electrolytes.

In cases of acute overdose, effects may be minimized or eliminated by inducing vomiting or gastric lavage shortly after ingestion of Picolax® oral drops. Rehydration and correction of electrolyte imbalances may be necessary. Antispasmodic agents may be used.

Cases of colonic mucosal ischemia have been reported following administration of large doses of Picolax®, substantially exceeding the usual recommended doses for constipation.

Like other laxatives, prolonged overdose of Picolax® may result in chronic diarrhea and abdominal pain, hypokalemia, secondary hyperaldosteronism, and possibly kidney stone formation. With long-term abuse of laxatives, renal tubular damage, metabolic alkalosis, and muscle weakness due to hypokalemia have been reported.

Adverse reactions.

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

Skin and subcutaneous tissue disorders:

Frequency not known: skin reactions (angioedema, drug toxicoderma, rash, pruritus).

Immune system disorders:

Frequency not known: allergic reactions.

Nervous system disorders:

Uncommon: dizziness;

Frequency not known: syncope.

The occurrence of dizziness and syncope is likely related to vasovagal reactions (such as abdominal cramps or defecation) (see section "Special precautions").

Gastrointestinal disorders:

Very common: diarrhea;

Common: abdominal discomfort, abdominal pain, abdominal cramps;

Uncommon: vomiting, nausea.

Prolonged and excessive use of the drug may lead to fluid loss, potassium, and other electrolytes. This, in turn, may result in muscle weakness and impaired cardiac function, especially when the drug is used concomitantly with diuretics or corticosteroids.

Shelf life.

3 years.

Do not use the drug after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging.

15 ml or 30 ml in a bottle. 1 bottle per carton.

Pharmaceutical category.

Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's name and address of the place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.