Dulcolax^® (Tablets) Instructions for Use

Marketing Authorization Holder

A. Nattermann and Cie., GmbH (Germany)

Manufactured By

Delpharm Reims (France)

ATC Code

A06AB02 (Bisacodyl)

Active Substance

Bisacodyl (Rec.INN registered by WHO)

Dosage Form

Dulcolax®

Tablets, enteric-coated, 5 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Tablets, enteric-coated, sugar-coated, beige-yellow in color, round, biconvex, with a smooth, even, shiny surface and a white core.

Excipients: corn starch, glycerol 85%, modified corn starch, lactose, magnesium stearate.

Enteric coating composition: sucrose, talc, acacia gum, titanium dioxide, methacrylic acid and methyl methacrylate copolymer (1:2) (Eudragit S100), methacrylic acid and methyl methacrylate copolymer (1:1) (Eudragit L100), castor oil, magnesium stearate, macrogol (polyethylene glycol) 6000, yellow iron oxide dye (E172), white beeswax, carnauba wax, shellac.

10 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Laxative drug that stimulates intestinal peristalsis

Pharmacotherapeutic Group

Laxative

Pharmacological Action

A laxative drug, a derivative of diphenylmethane. As a local laxative with an anti-resorptive effect, Bisacodyl after hydrolysis in the colon increases the secretion of water and electrolytes in the colon, accelerates and enhances its peristalsis. This leads to stimulation of the defecation act, reduction of evacuation time, and softening of the stool.

The time to onset of the laxative effect of the drug is 6-12 hours.

Bisacodyl, being a laxative acting at the level of the colon, stimulates the natural evacuation process in the lower gastrointestinal tract. Therefore, Bisacodyl does not affect the digestion or absorption of caloric food or essential nutrients in the small intestine.

Pharmacokinetics

Absorption and Distribution

Absorption is negligible. Enteric-coated tablets are resistant to the action of gastrointestinal juice. Bisacodyl is released in the colon with the formation of an active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane, which has an irritant effect on the colonic mucosa.

C_max of the active metabolite in plasma after drug administration is reached in 4-10 hours, the laxative effect develops in 6-12 hours. There is no correlation between the laxative effect of bisacodyl and the plasma concentration of the active metabolite.

Metabolism and Excretion

The drug is almost completely metabolized in the intestinal wall and liver to an inactive glucuronide. Metabolism occurs under the action of enzymes of the colonic mucosa.

T_1/2 is about 16.5 hours. Excretion of the active metabolite occurs mainly with feces (up to 51.8%), about 10.5% is excreted in urine.

Indications

As a laxative in the following cases

• Constipation due to colonic hypotonia (including chronic);
• Preoperative preparation, postoperative treatment;
• Preparation for instrumental and radiological examinations;
• Medical conditions requiring facilitation of defecation.

ICD codes

Dosage Regimen

Tablets are taken orally with a sufficient amount of liquid.

For constipation, adults and children over 10 years are prescribed 1-2 tablets (5-10 mg). It is recommended to start with the lowest dose. To achieve regular stool, the dose can be increased to the maximum recommended (10 mg). The maximum recommended daily dose should not be exceeded.

Children aged 4-10 years – 1 tablet (5 mg). The maximum recommended daily dose (5 mg) should not be exceeded.

To achieve a laxative effect in the morning, it is recommended to take the drug the night before.

The drug should not be taken together with products that reduce acidity in the upper gastrointestinal tract, such as milk, antacids, or proton pump inhibitors, to avoid premature dissolution of the enteric coating.

For preparation for examinations, pre- and postoperative treatment, medical conditions that require facilitation of defecation, Dulcolax^® should be used under medical supervision.

It is recommended to take 2 tablets at night one day before the examination and 2 tablets at night before the operation or examination. Use in combination with suppositories is possible. For adults, in addition to 2-4 tablets taken the day before, administration of 1 suppository in the morning is recommended.

Adverse Reactions

The most frequently reported adverse reactions during the use of the drug are abdominal cramping pain and diarrhea.

From the digestive system: cramping pain or discomfort in the abdominal area, diarrhea (dehydration, muscle weakness, cramps, decreased blood pressure), nausea, vomiting, a small amount of blood in the stool, anorectal discomfort, colitis.

From the nervous system: dizziness, fainting. These side effects occurring after drug use are associated with a vasovagal reaction (i.e., due to intestinal spasm, straining during defecation).

From the immune system: hypersensitivity, angioedema, anaphylactic reactions.

Contraindications

• Intestinal obstruction;
• Obstructive intestinal diseases;
• Acute diseases of the abdominal organs, including appendicitis;
• Acute inflammatory bowel diseases;
• Severe abdominal pain accompanied by nausea and vomiting, which may be a symptom of a more serious condition;
• Severe dehydration;
• Children under 4 years of age;
• Hypersensitivity to bisacodyl or excipients.

One tablet (5 mg) contains 33.2 mg of lactose. The maximum recommended daily dose of tablets for adults and children over 10 years for the treatment of constipation and for radiographic examination contains 66.4 mg and 132.8 mg of lactose, respectively. Patients with rare hereditary galactose intolerance, e.g., galactosemia, should not take the drug.

One tablet (5 mg) contains 23.4 mg of sucrose. The maximum recommended daily dose of tablets for adults and children over 10 years for the treatment of constipation and for radiographic examination contains 46.8 mg and 93.6 mg of sucrose, respectively. Patients with rare hereditary fructose intolerance should not take the drug.

The drug should be prescribed with caution to patients with hepatic and/or renal impairment.

Use in Pregnancy and Lactation

During long-term experience with the drug, no adverse events during pregnancy have been identified. However, due to the lack of studies, the use of the drug Dulcolax^® during pregnancy is recommended only in cases where the potential benefit to the mother outweighs the possible risk to the fetus.

Bisacodyl is not excreted in breast milk.

During pregnancy and breastfeeding, the drug should be used only after consultation with a specialist.

No clinical studies on the effect of the drug on fertility have been conducted.

Use in Hepatic Impairment

The drug should be prescribed with caution to patients with liver diseases.

Use in Renal Impairment

The drug should be prescribed with caution to patients with kidney diseases.

Pediatric Use

Contraindicated in children under 4 years of age.

Special Precautions

The drug, like all laxatives, should not be used regularly or for a long period of time without establishing the causes of constipation. Long-term use of high doses of the drug can lead to fluid loss, electrolyte imbalance, hypokalemia.

Fluid loss through the intestines can lead to dehydration, which may be accompanied by symptoms such as thirst and oliguria. Dehydration can be harmful to the body (e.g., in renal failure, in elderly patients), therefore, if the above symptoms occur, the drug should be discontinued and can be resumed only under medical supervision.

Patients may experience a small amount of blood in the stool. This manifestation is usually mild and resolves on its own.

Dizziness and/or fainting have been observed in patients taking Dulcolax^®. Analysis has shown that these cases were associated with fainting during defecation (or fainting caused by straining during defecation) or with a vasovagal response to abdominal pain, which could be due to constipation and are not necessarily related to drug intake.

1 tablet (5 mg) corresponds to 0.006 XE (Bread Units).

Children should take the drug after consultation with a doctor.

Effect on the ability to drive vehicles and operate machinery

No specific clinical studies on the effect of the drug on the ability to drive a car and operate machinery have been conducted. Despite this, patients should be informed that they may experience dizziness and/or fainting due to a vasovagal reaction (i.e., during intestinal spasm). If patients experience intestinal spasm, they should avoid potentially hazardous activities, including driving vehicles or operating machinery.

Overdose

In acute overdose, the following are possible: diarrhea, dehydration, decreased blood pressure, disturbance of water-electrolyte balance, hypokalemia, convulsions.

In chronic overdose: chronic diarrhea, abdominal pain, hypokalemia, hyperaldosteronism, urolithiasis. Due to chronic abuse of laxatives, renal tubular damage, metabolic alkalosis, and muscle weakness associated with hypokalemia may develop.

Treatment should be symptomatic. There is no specific antidote. To reduce drug absorption after oral administration, vomiting can be induced or gastric lavage can be performed. Fluid replacement and correction of electrolyte balance, as well as the administration of antispasmodic agents, may be required.

Drug Interactions

Concomitant use of Dulcolax^® in high doses and diuretics or corticosteroids increases the risk of electrolyte imbalance (hypokalemia).

Electrolyte imbalance (hypokalemia) enhances the effect of cardiac glycosides.

Storage Conditions

The drug should be stored in a dry place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.