Picosulfate-sofarma

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PICO-SULFATE-SOPHARMA (PICOSULFATE-SOPHARMA)

Composition:

Active substance: sodium picosulfate;

1 ml of solution contains 7.5 mg of sodium picosulfate;

Excipients: sorbitol solution, non-crystallizing (E 420); citric acid monohydrate; sodium citrate; sodium benzoate (E 211); purified water.

Pharmaceutical form. Oral drops, solution.

Main physicochemical properties: clear, colorless or slightly yellowish solution.

Pharmacotherapeutic group.

Contact laxatives. Sodium picosulfate. ATC code A06AB08.

Pharmacological properties.

Pharmacodynamics.

The active substance, sodium picosulfate, is a locally-acting laxative from the triarylmethane group. After bacterial transformation in the colon, it stimulates the colonic mucosa, inducing peristalsis, which in turn leads to accumulation of water and electrolytes in the intestinal lumen. As a result, defecation is promoted, intestinal transit time is reduced, and stools are softened.

As a laxative acting specifically on the colon, sodium picosulfate stimulates the natural evacuation process of the lower gastrointestinal tract. Therefore, sodium picosulfate does not interfere with digestion and does not cause accumulation of calories or other nutrients in the small intestine.

Pharmacokinetics.

Absorption and distribution

After oral administration, sodium picosulfate reaches the colon without significant absorption in the gastrointestinal tract. As a result, enterohepatic recirculation is avoided.

Biotransformation

Sodium picosulfate is converted into the active laxative component (BHRM, bis-(p-hydroxyphenyl)-pyridyl-2-methane) via bacterial transformation in the colon.

Elimination

After transformation, only small amounts of BHRM are detected in the colonic wall and in the liver, which are almost completely conjugated to form the inactive glucuronide of BHRM. Within 48 hours after oral administration of 1 mg of sodium picosulfate, 10.4% of the total dose is excreted in urine as BHRM glucuronide.

Overall urinary excretion decreases with higher doses of sodium picosulfate.

Pharmacokinetic–pharmacodynamic relationship

The effect usually occurs 6–12 hours after administration, corresponding to the release of the active substance (BHRM).

There is no direct or inverse relationship between the laxative effect and the plasma concentration of the active component.

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 medicinal product;
• dynamic or mechanical intestinal obstruction;
• severe abdominal pain and/or acute surgical abdomen which may be accompanied by fever (e.g., appendicitis), nausea and vomiting;
• acute inflammatory bowel diseases;
• severe dehydration;
• rare hereditary disorders that may be incompatible with any of the excipients of the medicinal product (see section "Special precautions for use");
• children under 4 years of age.

Interaction with other medicinal products and other forms of interaction.

Concomitant intake of excessively high doses of sodium picosulfate with diuretics or adrenocorticosteroids may increase the risk of electrolyte imbalance.

Electrolyte imbalance may lead to increased sensitivity to cardiac glycosides.

Concomitant use of antibiotics may reduce the laxative effect of the medicinal product.

Special precautions for use

In patients suffering from chronic constipation, a complete diagnostic evaluation should be performed to determine the underlying cause of constipation.

Like all laxatives, Picosulfate-Sofarma should not be taken daily or for prolonged periods without identifying the cause of constipation. Prolonged and excessive use may lead to fluid and electrolyte imbalance and hypokalemia. Discontinuation of the medicinal product may result in recurrence of symptoms. If the product has been used for chronic constipation over a long period, any recurrence of constipation symptoms may be more pronounced.

Cases of dizziness and/or malaise (syncope) have been reported in patients taking the medicinal product. Available details of these cases suggest that these events were related to defecation syncope (associated with the Valsalva maneuver) or vasovagal response (vascular reaction) to abdominal pain secondary to constipation, but not necessarily to the use of sodium picosulfate itself.

The medicinal product contains sorbitol. 1 ml of drops contains 642.86 mg of sorbitol, corresponding to 857.3 mg of sorbitol in the maximum recommended daily dose for the treatment of adults and children aged 10 years and older. One drop contains 43 mg of sorbitol. Sorbitol is a source of fructose. This medicinal product should not be used in patients with rare hereditary fructose intolerance.

Use during pregnancy or breastfeeding

Pregnancy

There are no adequate and well-controlled studies in pregnant women. Animal studies have demonstrated reproductive toxicity of the drug when administered at daily doses of 10 mg/kg and higher. For safety reasons, the medicinal product should not be used during pregnancy, if possible.

Breastfeeding

Clinical data indicate that neither the active moiety of sodium picosulfate (BHRM, bis-(p-hydroxyphenyl)-pyridyl-2-methane) nor its glucuronides are excreted in breast milk of healthy lactating women. Therefore, the medicinal product Picosulfate-Sofarma can be used during breastfeeding.

Fertility

Clinical studies on 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 influence the speed of reactions when driving or operating machinery

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

However, patients should be advised that they may experience dizziness or nausea due to vasovagal reactions (e.g., abdominal cramps). If patients experience abdominal cramps, they should avoid potentially hazardous activities such as driving vehicles or operating machinery.

Method of Administration and Dosage

Method of Administration

For oral use. The medication can be taken with or without liquid. The recommended dose should be taken in the evening to induce defecation the following morning. After administration of the drops, bowel movement usually occurs approximately 10–12 hours later. Treatment should be initiated with the lowest recommended dose. The dose may be increased up to the maximum daily dose to achieve regular defecation. The maximum daily dose must not be exceeded. The medication should not be used continuously (daily) or for prolonged periods without identifying the cause of constipation.

Dosage

1 ml of oral drops solution contains sodium picosulfate 7.5 mg (=15 drops).

Adults and children aged 10 years and older: 10–20 drops (5–10 mg) once daily.

Children aged 4 to 10 years: 5–10 drops (2.5–5 mg) once daily.

Children.

The medication should be used in children aged 4 years and older only under medical supervision.

Overdose

Symptoms

When high doses are used, watery stools (diarrhea), abdominal cramps, and clinically significant loss of fluid, potassium, and other electrolytes may occur.

Cases of colonic mucosal ischemia have been reported following administration of doses significantly higher than those recommended for routine relief of constipation.

Sodium picosulfate, like other laxatives, in cases of chronic overdose, may cause chronic diarrhea, abdominal pain, hypokalemia, secondary hyperaldosteronism, and nephrolithiasis. Chronic abuse of laxatives has also been associated with renal tubular damage, metabolic alkalosis, and muscle weakness due to hypokalemia.

Treatment

Absorption may be minimized or prevented shortly after ingestion of Picosulfate-Sofarma by inducing vomiting or gastric lavage. If necessary, fluid intake and correction of electrolyte imbalances should be administered. This is particularly important for elderly patients and adolescents.

Spasmolytic agents may help alleviate symptoms.

Adverse Reactions

Adverse reactions to the medicinal product are classified according to system organ classes. The following frequency classification is used: 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 the available data).

Immune system disorders: frequency not known* – hypersensitivity.

Nervous system disorders: uncommon – dizziness; frequency not known* – syncope.

Dizziness and syncope occurring after administration of sodium picosulfate are consistent with a vasovagal reaction (e.g., abdominal cramps, defecation).

Gastrointestinal disorders: very common – diarrhea; common – abdominal cramps, abdominal pain, gastric discomfort; uncommon – vomiting, nausea.

Skin and subcutaneous tissue disorders: frequency not known* – skin reactions such as angioneurotic edema, drug rash, pruritus.

* These adverse reactions were observed during post-marketing experience. The frequency of occurrence is no higher than uncommon, with a 95% probability, but could be lower. An accurate estimation of frequency cannot be made, as the adverse reaction did not occur during clinical trials within the database of 1020 patients.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

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

Storage conditions.

Keep out of the reach of children.

Store below 30 °C.

Packaging.

15 ml of solution in a glass bottle with an applicator dropper and cap.

1 bottle per cardboard box.

Availability classification. Over-the-counter.

Manufacturer: JSC "Sofarma".

Manufacturer's address and place of business.

16 Iliensko Shose Str., Sofia, 1220, Bulgaria.

2800, Sandanski, Industrial Zone, Bulgaria.