Pharmacological action of Dulcolax 

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

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

Bisacodyl, being a laxative that acts at the level of the colon, stimulates the natural evacuation process in the lower gastrointestinal tract. Therefore, bisacodyl has no effect on the digestion or absorption of high-calorie foods 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 to form the active metabolite, bis- (p-hydroxyphenyl) -pyridyl-2-methane, which is irritating to the colon mucosa.

Cmax of the active metabolite in the plasma after dosing is achieved after 4-10 hours, laxative effect develops after 6-12 hours. The relationship between the laxative effect of bisacodyl and concentration of the active metabolite in the plasma is absent.

Metabolism and excretion

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

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

Indications of the drug Dulcolax®

As a laxative in the following cases:

• constipation caused by hypotension of the large intestine (including chronic);

• preoperative preparation, postoperative treatment;

• preparation for instrumental and X-ray examinations;

• medical conditions that require easier bowel movements.

Dosage regimen of Dulcolax  

Tablets are taken orally with a sufficient amount of liquid.

For constipation, adults and children over 10 years old are prescribed 1-2 tablets. (5-10 mg). It is recommended to start with the lowest dose. In order to achieve regular bowel movements, the dose may be increased to the maximum recommended (10 mg). Do not exceed the maximum recommended daily dose.

Children aged 4-10 years old - 1 tab. (With 5 mg). Do not exceed the maximum recommended daily dose (5 mg).

To obtain a laxative effect in the morning, 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 enteric membrane.

In preparation for research, pre- and postoperative treatment, medical conditions that require relief of bowel movements, Dulcolax® should be used under medical supervision.

It is recommended to use 2 tabs. at night the day before the study and 2 tab. the night before surgery or research. Can be used in combination with suppositories. For adults, in addition to 2-4 tablets taken the day before, it is recommended to administer 1 suppository in the morning.

Contraindications to the use of

• intestinal obstruction;

• obstructive bowel disease;

• acute diseases of the abdominal organs, including appendicitis;

• acute inflammatory bowel disease;

• severe abdominal pain associated with nausea and vomiting, which may be a symptom of a more severe 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 of age for the treatment of constipation and for x-ray examination contains 66.4 mg and 132.8 mg of lactose, respectively. Patients with a rare hereditary galactose intolerance, such as 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 of age for the treatment of constipation and for X-ray 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 used with caution in patients with hepatic and / or renal impairment.

Application during pregnancy and lactation

During the long-term experience with the use of the drug, no adverse events have been identified during pregnancy. However, due to the lack of research, the use of 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 during breastfeeding, the drug can be used only after consulting a specialist.

Clinical studies of the effect of the drug on fertility have not been conducted.

Application for violations of liver function

The drug is prescribed with caution to patients with liver disease.

Application for impaired renal function

The drug is prescribed with caution to patients with kidney disease.

Use in children

Contraindicated in children under 4 years of age.

Special instructions

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

Loss of fluid through the intestines can lead to dehydration, which can be accompanied by symptoms such as thirst and oliguria. Dehydration can harm the body (for example, in case of renal failure, in elderly patients), therefore, with the above symptoms, the drug should be discontinued and can only be resumed under medical supervision.

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

Dizziness and / or fainting were observed in patients taking Dulcolax®. The analysis showed that these cases were associated with fainting during a bowel movement (or fainting caused by straining during a bowel movement) or with a vasovagal response to abdominal pain, which could be due to constipation and not necessarily drug-related.

1 tablet (5 mg) corresponds to 0.006 XE.

Children should take the drug after consulting a doctor.

Influence on the ability to drive vehicles and control mechanisms

Special clinical studies of the effect of the drug on the ability to drive and control mechanisms have not been conducted. However, patients should be advised that they may experience dizziness and / or fainting as a result of a vasovagal reaction (i.e., during bowel spasm). If patients have a bowel spasm, they should avoid potentially hazardous activities, incl. driving vehicles or operating machinery.

Overdose

In case of an acute overdose , the following are possible: diarrhea, dehydration, decreased blood pressure, imbalance in water and electrolyte balance, hypokalemia, convulsions.

In case of chronic overdose: chronic diarrhea, abdominal pain, hypokalemia, hyperaldosteronism, urolithiasis. Chronic laxative abuse can lead to renal tubular damage, metabolic alkalosis, and muscle weakness associated with hypokalemia.

Treatment should be symptomatic. There is no specific antidote. To reduce the absorption of the drug after ingestion, you can induce vomiting or gastric lavage. Fluid replenishment and electrolyte balance adjustments may be required, as well as antispasmodics.

Drug interactions

Simultaneous administration of Dulcolax in high doses and diuretics or GCS increases the risk of electrolyte imbalance (hypokalemia).

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

Side effects

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

From the digestive system: spastic pain or discomfort in the abdomen, 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 that occur after using the drug are associated with a vasovagal reaction (i.e., due to intestinal spasm, tension during bowel movements).

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