Picolax®

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

Composition:

active substance: sodium picosulfate,

1 tablet contains 5 mg or 7.5 mg of sodium picosulfate calculated as 100% anhydrous substance;

excipients: lactose monohydrate, maize starch, pregelatinized starch 1500, colloidal anhydrous silicon dioxide, magnesium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or almost white, flat cylindrical tablets with a score line and bevelled edge.

Pharmacotherapeutic group. Stimulant 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 colon, sodium picosulfate stimulates the mucosa, accelerates peristalsis, and promotes accumulation of water and electrolytes in the lumen of the colon. This results in stimulation of defecation, reduced transit time, and softening of stool.

Pharmacokinetics.

Absorption and distribution.

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

Biological transformation.

The active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), is formed following bacterial cleavage in the colon.

Elimination.

After conversion, only a small amount of BHPM is absorbed. After oral administration of 10 mg sodium picosulfate, 10.4% of the total dose is excreted as BHPM glucuronide in urine within 48 hours. In addition, BHPM is excreted in bile as glucuronide.

Relationship between pharmacokinetics and pharmacodynamics.

The onset of action of Picolax**®** usually occurs 6–12 hours after administration, depending on the release of the active metabolite (BHPM). The laxative effect of the drug does not correlate with plasma levels of the active metabolite.

Clinical characteristics.

Indications.

Constipation or conditions requiring facilitation of defecation.

Contraindications.

Hypersensitivity to the active substance, other triarylmethanes, or to any of the excipients of the medicine.

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, possible undiagnosed lactose intolerance (see section "Special warnings and precautions for use").

Interaction with other medicinal products and other forms of interaction.

Concomitant use of high doses of Picolax**®** and 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

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

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

Prolonged 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 long period, any recurrence of symptoms may be more pronounced.

Cases of dizziness and/or syncope temporally associated with the use of sodium picosulfate have been reported. Available information suggests that these events may correspond to defecation syncope (associated with the Valsalva maneuver) or may be related to a vasovagal response to abdominal pain.

Like other laxatives, the drug should not be used daily or for prolonged periods without identifying the cause of constipation.

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

The product contains lactose, which should be taken into consideration in patients with hereditary lactose intolerance.

Use during pregnancy or breastfeeding.

There are insufficient studies on the use of sodium picosulfate in pregnant women. For safety reasons, Picolax® should not be used during pregnancy, if possible.

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.

Studies evaluating effects on fertility have not been conducted.

Ability to affect reaction rate when driving or operating machinery.

Studies on the effect of Picolax® on the ability to drive or operate machinery have not been conducted.

However, patients should be warned about the possible development of adverse reactions such as dizziness and/or syncope, due to a vasovagal response (particularly abdominal cramps). If abdominal cramps occur, patients should avoid potentially hazardous activities such as driving or operating machinery.

Dosage and Administration

Adults: 5–10 mg once daily.

Children aged 4 years and older (only under medical supervision): 2.5–5 mg once daily.

Treatment should be initiated at the lowest dose. The dose may be adjusted up to the maximum recommended dose to achieve regular bowel movements. The maximum daily dose of 10 mg (for adults) or 5 mg (for children aged 4 years and older) must not be exceeded.

Picolax® should be taken at night. Bowel movement usually occurs 10–12 hours after administration of Picolax®.

Picolax® should not be used daily or for prolonged periods without identifying the underlying cause of constipation.

Children

Picolax® should be administered to children aged 4 years and older only under medical supervision.

Overdose

Overdose may result in loose stools (diarrhea), intestinal spasms, and clinically significant loss of fluids, potassium, and other electrolytes.

In acute overdose, adverse effects may be minimized or eliminated by induced emesis or gastric lavage performed shortly after ingestion of Picolax®. Rehydration and correction of electrolyte imbalances may be necessary. Antispasmodic agents may be used.

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

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

Side effects.

Skin and subcutaneous tissue disorders: angioneurotic edema, toxicoderma, rash, pruritus.

Immune system disorders: hypersensitivity reactions.

Nervous system disorders: dizziness, syncope. The occurrence of dizziness and syncope may be associated with a vasovagal reaction (such as abdominal spasm or defecation) (see section "Special precautions").

Gastrointestinal disorders: diarrhea, abdominal colic, abdominal pain, abdominal discomfort, vomiting, nausea.

Prolonged and excessive use of the drug may lead to loss of fluid, 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.

4 years.

Do not use 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 of children.

Packaging.

10 tablets per blister.

5 mg tablets: 1 blister per pack.

7.5 mg tablets: 1 or 3 blisters per pack.

Supply category. Over-the-counter.

Manufacturer.

JSC "Farmak".

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

74, Kyrylivska Street, Kyiv, 04080, Ukraine.