Bisacodyl-pharmex

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT BISACODYL-PHARMEX (BISACODYL-PHARMEX)

Composition:

active substance: bisacodyl;

1 rectal suppository contains 10 mg of bisacodyl;

excipients: solid fat, microcrystalline wax.

Pharmaceutical form. Rectal suppositories.

Main physicochemical properties: smooth suppositories of white to creamy color. On longitudinal section, absence of inclusions is observed; funnel-shaped depression and air channel are permissible.

Pharmacotherapeutic group.

Medicinal products used in constipation. Contact laxatives. Bisacodyl.

ATC code A06AB02.

Pharmacological Properties

Pharmacodynamics

Bisacodyl is a stimulant laxative that enhances colonic peristalsis through irritation of the mucosa or direct stimulation of nerve endings in the submucosal and mucosal nerve plexuses.

Pharmacokinetics

Bisacodyl is poorly absorbed from the gastrointestinal tract; moreover, it affects electrolyte absorption. As a result, the increased osmotic pressure in the intestinal lumen retains more water, leading to softening of the stool and facilitating its passage through the colon. In addition, the increased stool volume stimulates peristalsis and promotes defecation.

Bacterial enzymes in the colon metabolize bisacodyl into its active compound—diphenol—which undergoes conjugation during the first pass through the liver with glucuronic or sulfuric acid and is returned to the intestine via enterohepatic circulation. This process prolongs the drug's effect.

Absorption of bisacodyl after intrarectal administration is minimal. The absorbed bisacodyl undergoes deacetylation in the liver to form a phenolic derivative, which is subsequently excreted in the urine. The portion remaining in the colon is excreted in feces.

Clinical characteristics.

Indications.

Short-term symptomatic treatment of constipation, including habitual constipation and chronic constipation in bedridden patients and elderly patients; prior to diagnostic procedures, surgical and obstetric interventions, as well as in the pre- and postoperative period.

Contraindications.

Hypersensitivity to bisacodyl and to other components of the medicinal product.

Intestinal obstruction.

Acute abdominal conditions, including appendicitis and acute inflammatory bowel diseases.

Severe abdominal pain associated with nausea and vomiting, which may indicate the aforementioned serious conditions.

Severe dehydration.

Anal fissures or ulcerative proctitis with mucosal damage.

Interaction with other medicinal products and other forms of interaction.

Bisacodyl enhances the effect of cardiac glycosides due to reduction in serum potassium levels. It also enhances the potassium-depleting effect of diuretics and glucocorticoids.

Concomitant use of bisacodyl with other laxatives may intensify gastrointestinal adverse reactions.

Special precautions for use.

Duration of treatment

Like other laxatives, bisacodyl should not be used continuously for more than 5 days without identifying the cause of constipation. Prolonged and excessive use of the drug may lead to fluid and electrolyte imbalance, as well as hypokalemia.

Fluid loss in the intestine

Fluid loss in the intestine may cause dehydration, the symptoms of which may include thirst and oliguria. Bisacodyl should be discontinued in patients suffering from intestinal fluid loss that may lead to dangerous dehydration (e.g., in renal insufficiency, elderly patients) and may be restarted only under medical supervision (see section "Side effects").

Long-term use may lead to habit formation, whereby defecation becomes possible only after administration of a laxative.

Gastrointestinal disorders

There have been isolated reports of abdominal pain and bloody diarrhea following bisacodyl use. Some cases were associated with ischemia of the colonic mucosa. In some patients, blood in the stool may appear, which is generally mild in nature and does not require treatment (see section "Side effects").

Suppositories are not recommended for patients with anal fissures, proctitis, or ulcerative hemorrhoids, as this may cause pain and local irritation. Do not use in patients with obstructive intestinal disorders or acute conditions such as appendicitis, as well as in patients with inflammatory bowel diseases.

Dizziness, syncope

Dizziness and/or syncope may occur in patients using bisacodyl.

Based on available information about these cases, it can be assumed that these events are related to defecation syncope (or syncope associated with straining during defecation) or vasovagal response to abdominal pain, which may be associated with constipation prompting the use of a laxative.

Elderly patients

Frequent use of bisacodyl in elderly patients may exacerbate asthenia and cause orthostatic hypotension and coordination disorders related to fluid and electrolyte loss.

Local reactions

Pain and local irritation may occur with suppository use, especially in the presence of anal fissures and ulcerative proctitis.

The drug does not promote weight loss.

The hard fat base may reduce the effectiveness of latex products (e.g., condoms).

Use during pregnancy or breastfeeding

Bisacodyl is not recommended during pregnancy, especially during the first trimester, except when the expected benefit to the mother outweighs the potential risk to the fetus; use should only be under a physician's advice. Adequate controlled clinical studies in pregnant women have not been conducted. Long-term experience with the drug does not indicate harmful effects during pregnancy.

Bisacodyl is not recommended during breastfeeding, except when the expected benefit to the mother outweighs the potential risk to the infant; use should only be under a physician's advice. There are no data on whether bisacodyl is excreted in breast milk.

Ability to influence reaction speed when driving or operating machinery

Studies on the ability to affect reaction speed when driving or operating machinery have not been conducted. However, patients should be advised that, due to the possible occurrence of dizziness and/or syncope, they should refrain from driving and operating machinery.

Method of Administration and Dosage.

The medicinal product is intended for rectal use. Before administration, the suppository should be removed from the blister pack.

Bisacodyl should be used only for the treatment of adult patients: 1 suppository once daily, usually in the morning. The treatment duration should not exceed 7 days.

Children.

The drug must not be used in children.

Overdose.

Administration of bisacodyl in high doses may cause diarrhea, abdominal cramps, and clinically significant loss of potassium and electrolytes.

Prolonged use of laxatives may lead to chronic diarrhea, abdominal pain, hypokalemia, secondary hyperaldosteronism, and nephrolithiasis. Cases of renal tubular damage, metabolic alkalosis, and muscle weakness as a consequence of hypokalemia have been reported.

Treatment: fluid replacement and correction of electrolyte imbalance (especially in hypokalemia). This is particularly important for elderly and young patients. Spasmolytics may be prescribed if necessary.

Side effects

The frequency of adverse reactions is classified as follows: 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

Rare: Hypersensitivity and allergic reactions, including angioneurotic edema and anaphylactic reactions.

Metabolism and nutrition disorders

Rare: Dehydration.

Nervous system disorders

Uncommon: Dizziness, fainting. These adverse effects occurring after administration of the drug are associated with a vasovagal reaction (i.e. due to intestinal spasm, straining during defecation).

Rare: Syncope.

Gastrointestinal disorders

Common: Discomfort, abdominal pain, cramps, nausea, and diarrhea.

Uncommon: Blood in stools, vomiting, abdominal discomfort, anorectal discomfort.

Rare: Colitis, including ischemic colitis.

Local reactions (reactions at the site of administration, including pain and irritation)

Frequency not known: The use of suppositories may be accompanied by pain and local irritation, especially in the presence of anal fissures and ulcerative colitis.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

5 suppositories per strip, 2 strips per carton.

Classification. Over-the-counter.

Manufacturer.

LLC "FARMEKS GROUP".

Manufacturer's address and location of business activity.

100, Shevchenka Street, Boryspil, Kyiv Oblast, Ukraine, 08301.