Picosen®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PICOSEN® (PICOSEN)

Composition:

Active substances: 1 capsule contains: sodium picosulfate 7.5 mg; dried leaf extract of senna (Cassiae folium extractum siccum) (4–6 : 1) (extraction solvent — 60% methanol, v/v) (excipient: glucose, spray-dried 1–30%) 10 mg;

Excipients: povidone K-25, lactose monohydrate, maize starch, magnesium stearate;

Hard gelatin capsule: gelatin, titanium dioxide (E 171), iron oxide (E 172), azorubine (E 122).

Pharmaceutical form. Capsules

Main physicochemical properties: capsules with red-brown body and cap.

Pharmacotherapeutic group. Stimulant laxatives. ATC code A06AB.

Pharmacological Properties

Pharmacodynamics.

PICOSEN® is a combined stimulant laxative. Sodium picosulfate is a locally acting laxative of the triarylmethane group, which, after bacterial cleavage in the colon, 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.

Senna glycosides inhibit fluid absorption and stimulate intestinal wall peristalsis.

Pharmacokinetics.

After oral administration, sodium picosulfate reaches the colon without significant absorption. The drug typically begins to act within 6–12 hours after administration, depending on the release of the active metabolite. After oral administration, only a negligible amount of the drug can 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, PICOSEN® should not be used daily or for prolonged periods without determining the cause of constipation.

Contraindications.

• Hypersensitivity to the active substances, other triarylmethanes, or to any of the excipients of the medicinal product;
• dynamic or mechanical intestinal obstruction, intestinal obstruction, abdominal pain of unknown origin, acute surgical diseases of abdominal organs (e.g., acute appendicitis, ulcerative colitis), acute inflammatory bowel diseases;
• acute abdominal pain accompanied by nausea and vomiting, which may indicate the aforementioned acute conditions, postoperative state following gastrointestinal surgery;
• Crohn’s disease, peritonitis, peptic ulcer of the stomach and duodenum, gastrointestinal bleeding;
• hemorrhoids, anal fissures;
• spastic colitis, hepatitis and organic liver damage, pancreatitis, diverticulitis;
• metrorrhagia;
• severe disturbances of water-electrolyte balance (severe dehydration);
• hereditary fructose intolerance;
• nephroso-nephritis, cystitis;
• incarcerated hernia.

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

Special precautions.

In patients suffering from chronic constipation, a full diagnostic evaluation should be performed to determine the cause of constipation if unknown.

Discontinuation of PICOSEN® may lead to recurrence of symptoms. If PICOSEN® has been used for chronic constipation over a prolonged period, any recurrence of symptoms may be more pronounced.

The medicinal product is intended for episodic use. Prolonged and excessive use may lead to disturbances in water or electrolyte balance, hypokalemia, and increased intestinal atony.

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

Interaction with other medicinal products and other forms of interaction.

Concomitant use of high doses of PICOSEN® with diuretics or corticosteroids increases the risk of electrolyte imbalance, which may lead to increased sensitivity to cardiac glycosides. Concomitant use with antibiotics may reduce the laxative effect of the medicinal product.

Special precautions for use

The gelatin capsule contains azorubine (E 122), which may cause allergic reactions.

PICOSEN® contains lactose and glucose; therefore, if a patient has been diagnosed with intolerance to certain sugars, he/she should consult a physician before taking this medicinal product.

Use during pregnancy or breastfeeding.

There are insufficient studies in pregnant women. For safety reasons, it is advisable to avoid using PICOSEN® during pregnancy.

Breastfeeding should be discontinued during treatment, because components of the drug may pass into breast milk and cause frequent, loose stools in the infant. However, under appropriate dosage conditions, the occurrence of adverse effects in the infant is unlikely.

Studies evaluating effects on fertility have not been conducted.

Effects on ability to drive and use machines.

Studies on the impact 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 vasovagal reactions (e.g., abdominal cramps). If abdominal cramps occur, patients should avoid potentially hazardous activities such as driving or operating machinery.

Dosage and Administration.

For adults and children aged 12 years and older, take 1 capsule once daily at bedtime to produce a bowel movement the following morning.

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

Children.

Do not administer this medicinal product to children under 12 years of age.

Overdose.

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

In acute overdose, the consequences may be minimized or eliminated by induced vomiting or gastric lavage performed shortly after ingestion of PICOSEN®. 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 sodium picosulfate, substantially exceeding the usual recommended doses for constipation.

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

Side effects

Side effects are listed by frequency of occurrence: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10,000 to < 1/1000), very rare (< 1/10,000), frequency not known (cannot be estimated from the available data).

Immune system disorders: frequency not known — allergic reactions.

Skin and subcutaneous tissue disorders: frequency not known — hypersensitivity reactions, including angioneurotic edema, skin rashes, urticaria, pruritus, localized and generalized exanthema, toxidermia.

Gastrointestinal disorders: frequency not known — dyspepsia, anorexia, pseudomelanosis of the intestine, diarrhea, flatulence, vomiting, nausea, abdominal cramps and pain, epigastric and perianal discomfort, which resolve upon dose reduction.

Water-electrolyte balance disorders: frequency not known — dehydration, hypokalemia, hypocalcemia. 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.

Renal and urinary disorders: frequency not known — change in urine color (red or brown depending on pH, clinically insignificant); with prolonged use/abuse — albuminuria, hematuria.

Nervous system disorders: frequency not known — dizziness, syncope. The occurrence of dizziness and syncope is likely related to vasovagal reactions (such as abdominal cramps or defecation) (see section "Special precautions").

Endocrine system disorders: frequency not known — hyperaldosteronism.

Other: frequency not known — cardiac disturbances, increased fatigue, fainting, somnolence, muscle weakness, cramps.

Shelf life. 3 years.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 ºC. Keep out of reach of children.

Packaging. 10 capsules in a blister; 1 or 3 blisters per carton.

Classification. Over-the-counter (without prescription).

Manufacturer.

LLC "DKP "Pharmaceutical Factory".

Manufacturer's address and place of business. 4, Korolyov St., Stanishivka, Zhytomyr District, Zhytomyr Oblast, 12430, Ukraine.