Dulcolax, 5 mg 30 pcs.

Pharmacodynamics

Laxative drug, derivative of diphenylmethane. As a local laxative with antiresorptive effect, after hydrolysis in the colon, bisacodyl increases secretion of water and electrolytes in the colon and accelerates and increases its peristalsis. This leads to stimulation of the act of defecation, reduction of evacuation time and softening of stools.

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

Bisacodyl being a laxative acting at the level of the large intestine, stimulates the natural process of evacuation in the lower parts of the gastrointestinal tract. Therefore, bisacodyl has no effect on digestion or absorption of caloric foods or essential nutrients in the small intestine.

Pharmacokinetics

Absorption and distribution

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

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

Metabolism and excretion

The drug is almost completely metabolized in the intestinal wall and liver to inactive glucuronide. Metabolism occurs under the influence of mucosal enzymes of the large intestine.

The T1/2 is about 16.5 hours. Excretion of active metabolite occurs mainly in the feces (up to 51.8%), about 10.5% is excreted in the urine.

Indications

As a laxative in the following cases:

Active ingredient

Composition

Active substances:

Bisacodyl 5 mg.

Auxiliary substances:

Corn starch – 8.3 mg,

Glycerol 85% – 0.2 mg,

soluble corn starch – 1.5 mg,

lactose – 34.9 mg,

magnesium stearate – 0.1 mg.

Composition of the enteric-soluble coating:

sucrose – 23.3819 mg, talc – 16.1608 mg, acacia gum – 1.9354 mg, titanium dioxide – 0.3995 mg, copolymer of methacrylic acid and methyl methacrylate (1:2) (Eudragit S100) – 2.2147 mg, copolymer of methacrylic acid and methyl methacrylate (1:1) (Eudragit L100) – 0.9866 mg, common castor seed oil (castor oil) – 0.9762 mg, magnesium stearate – 3.8225 mg, macrogol (polyethylene glycol) 6000 – 0,0462 mg, iron oxide yellow dye (E172) – 0.0657 mg, beeswax white – 0.0015 mg, carnauba wax – 0.003 mg, shellac – 0.006 mg.

How to take, the dosage

The tablets are taken orally with plenty of fluid.

In case of constipation, 1-2 tablets (5-10 mg) are prescribed for adults and children over 10 years of age. It is recommended to start with the lowest dose. In order to achieve regular stools, the dose may be increased to the maximum recommended dose (10 mg). The maximum recommended daily dose should not be exceeded.

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

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

The drug should not be taken with foods that lower acidity in the upper gastrointestinal tract, such as milk, antacids, or proton pump inhibitors, to avoid premature dissolution of the esophageal membrane.

Dulcolax® should be used under medical supervision in preparation for studies, pre- and post-operative treatment, and medical conditions that require relief of defecation.

The use of 2 tablets the night before the study and 2 tablets the night before the operation or study is recommended. It is possible to use in combination with suppositories. For adults, in addition to 2 to 4 tablets taken the night before, the administration of 1 suppository in the morning is recommended.

Interaction

The simultaneous use of Dulcolax in high doses and diuretics or GCS increases the risk of electrolyte imbalance (hypokalemia).

The electrolyte imbalance (hypokalemia) increases the effect of cardiac glycosides.

Special Instructions

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

Liquid loss through the intestine may 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, elderly patients), so if the above symptoms occur, the drug should be stopped and may only be restarted under medical supervision.

Patients may have a small amount of blood in the feces. This is usually mild and goes away on its own.

Dizziness and/or fainting have been observed in patients taking Dulcolax®. Analysis showed 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 were not necessarily related to taking the drug.

1 tablet (5 mg) corresponds to 0.006 IU.

Children should take the drug after consulting their doctor.

Impact on ability to drive and operate vehicles and other mechanisms requiring high concentration

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

Contraindications

Side effects

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

Digestive system disorders: spastic abdominal pain or discomfort, diarrhea (dehydration, muscle weakness, cramps, decreased BP), nausea, vomiting, a small amount of blood in the stool, anorectal discomfort, colitis.

Nervous system disorders: dizziness, fainting. These side effects occurring after using the drug are associated with vasovagal reaction (i.e., due to intestinal spasm, tension during defecation).

Immune system disorders: hypersensitivity, angioedema, anaphylactic reactions.

Overdose

Symptoms: in acute overdose – diarrhea, dehydration, BP decrease, water-electrolyte imbalance, hypokalemia, seizures are possible.

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

Treatment: should be symptomatic. There is no specific antidote. To reduce absorption of the drug after ingestion it is possible to induce vomiting or gastric lavage. It may be necessary to replenish fluids and correct electrolyte balance, as well as prescription of antispasmodic agents.

Pregnancy use

No adverse events in pregnancy have been observed during the long-term experience of using the drug. However, due to the lack of studies, the use of the drug Dulcolax® during pregnancy is recommended only if the potential benefit to the mother exceeds the possible risk to the fetus.

Bisacodyl is not excreted with the breast milk.

In pregnancy and during breast-feeding the drug may be used only after consultation with a specialist.

There have been no clinical studies of the effect of the drug on fertility.

Similarities