Regulax

INSTRUCTIONS for medical use of the medicinal product REGULAX® (REGULAX®)

Composition:

Active substances:

1 cube contains 0.71 g of senna leaf (sennaefolium) and 0.3 g of senna fruit (sennaefructus) (corresponds to 30 mg of hydroxyanthracene derivatives, calculated as sennoside B);

Excipients: citric acid anhydrous, mineral oil, glycerol monostearate, lemon flavoring (containing ethanol 96%), invert sugar syrup, sorbitol (E 420), sorbic acid, hard fat, propylene glycol, plum puree, fig paste.

Pharmaceutical form. Fruit cubes.

Main physicochemical characteristics: a paste-like cube of dark brown color with yellow fig granules, with a fruity odor and sweet aromatic taste.

Pharmacotherapeutic group. Stimulant laxatives. Senna glycosides.

ATC code A06AB06.

Pharmacological Properties

Pharmacodynamics

REGULAX® contains a mixture of senna fruit and senna leaf. Senna belongs to the group of stimulant laxatives containing anthranoids. The laxative effect is due to derivatives of 1,8-dihydroxyanthracene. The laxative action of sennosides, or more precisely their active metabolite rheinanthrone in the colon, is primarily associated with effects on colonic motility: inhibition of stationary contractions and stimulation of propulsive contractions. As a result, intestinal transit is accelerated and, consequently, the contact time between chyme and the intestinal wall is reduced, leading to decreased fluid resorption. In addition, water and electrolytes are secreted due to stimulation of active chloride secretion.

Pharmacokinetics

Systematic studies on the drug's kinetics are lacking.

Glycoside-bound sennosides (cassiosides) are prodrugs that are neither hydrolyzed nor absorbed in the upper gastrointestinal tract. By means of bacterial enzymes, they are cleaved in the colon to rheinanthrone. Rheinanthrone is the metabolite responsible for the laxative effect. Systemic availability of rheinanthrone is very low. In animal experiments, less than 5% of rhein and sennosides were excreted in urine as oxidized, partially conjugated derivatives. The majority of rheinanthrone (more than 90%) is found in feces, where it is tightly bound to intestinal contents and eliminated as polymeric compounds. A small amount of active metabolites of the rhein type enters breast milk. Laxative effects in breastfed infants have not been observed. Placental transfer of rhein in animal experiments was minimal.

Clinical characteristics.

Indications.

For short-term use in constipation.

Contraindications.

Hypersensitivity to the active substances or to other components of the medicinal product; intestinal obstruction (ileus); intestinal stenosis and atony; gastrointestinal bleeding; acute inflammatory bowel diseases (e.g. Crohn's disease, ulcerative colitis, appendicitis); abdominal pain of unknown origin; nausea, vomiting; severe dehydration of the body accompanied by loss of water and electrolytes; metrorrhagia, hemorrhoids, peritonitis, peptic ulcer of the stomach and duodenum, anal fissures, spastic colitis, incarcerated hernia, pancreatitis, hepatitis, nephritis, cystitis, diverticulitis, organic liver lesions.

Interaction with other medicinal products and other forms of interaction.

With prolonged use/abuse, potassium deficiency may enhance the effect of cardiac glycosides, as well as alter the effect of antiarrhythmic agents, drugs used in cardioversion (e.g. quinidine), and agents that prolong the QT interval.

Potassium loss may be intensified when used in combination with thiazide diuretics, adrenocortical hormones (corticosteroids), and liquorice root.

Also, consider medicinal products recently taken by the patient.

Special precautions for use.

REGULAX® should be used only if therapeutic effect cannot be achieved by dietary changes or by using agents that increase the volume of intestinal contents.

Patients taking cardiac glycosides, antiarrhythmic agents, drugs that prolong the QT interval, diuretics, adrenal cortex hormones (corticosteroids), or medications based on licorice root should consult a physician before starting REGULAX®.

If the cause of constipation is unknown or in the presence of acute or prolonged gastrointestinal symptoms (abdominal pain, nausea, and vomiting), as with initiation of any other laxative, a physician should determine the cause of constipation, since these symptoms may indicate intestinal obstruction.

When using laxatives on a daily basis, an examination should be performed to identify the underlying cause of constipation.

Prolonged use of this medication should be avoided, as long-term use of stimulant laxatives may lead to increased intestinal atony.

To prevent dependence, it is advisable to alternate REGULAX® with other laxatives and limit treatment duration to 1 week.

Adults suffering from fecal incontinence should avoid prolonged skin contact with feces by regularly changing pads (liners) during treatment with REGULAX®.

Caution is recommended in patients with kidney disease to prevent potential disturbances in electrolyte balance.

The product contains sugar syrup and therefore should not be used by patients with diabetes mellitus.

The product contains sorbitol and therefore should not be used by patients with rare hereditary fructose intolerance.

Use during pregnancy or breastfeeding.

Contraindicated.

Ability to influence reaction speed when driving or operating machinery.

No effect.

Dosage and Administration

For adults and children aged 12 years and older, the recommended dose is 1 cube once daily.

The cube should be thoroughly chewed and taken with an adequate amount of liquid, preferably a glass of water.

REGULAX®, fruit-flavored cubes, are best taken in the evening before bedtime. Laxative effect usually occurs within approximately 8 hours.

The lowest effective dose should be used to achieve soft bowel movement.

Maximum daily dose – 1 cube.

REGULAX®, fruit-flavored cubes, is intended for short-term use only.

Stimulant laxatives should not be used for more than 1–2 weeks without appropriate medical advice.

Children

Contraindicated in children under 12 years of age.

Overdose

Symptoms: The main clinical manifestations of laxative overdose are diarrhea, which may be accompanied in some cases by severe intestinal irritation and significant loss of water and electrolytes; vascular collapse and metabolic acidosis may occur. Electrolyte levels, particularly potassium, should be monitored, especially in elderly patients. Chronic use of high doses may lead to toxic hepatitis. Overdose may cause colicky abdominal pain and dyspepsia, requiring discontinuation of the medication. Prolonged high-dose use may result in atrophy of the smooth musculature of the colon and impaired innervation.

Treatment: Symptomatic management; rehydration therapy should be administered (replacement of fluid and electrolyte losses).

Side effects.

The frequency of occurrence of adverse reactions is defined as follows:

very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (< 1/10000); not known (cannot be estimated from the available data).

Immune system side effects:

Allergic reactions may occur, including pruritus, urticaria, and localized or generalized exanthema.

Metabolism and nutritional disorders:

Prolonged use or abuse of laxatives may lead to electrolyte loss, primarily potassium depletion.

Cardiovascular system side effects:

Potassium loss may lead to cardiac arrhythmias, especially when used concomitantly with cardiac glycosides, diuretics, and corticosteroid hormones.

Gastrointestinal side effects:

In isolated cases, spasmodic abdominal pain and diarrhea may occur; in such cases, the dose should be reduced. Digestive disturbances, bloating, diarrhea, and anorexia may occur. With prolonged use or abuse of laxatives, pigment deposition in the intestinal mucosa (pseudomelanosis) may be observed; this condition is benign and usually resolves after discontinuation of the drug.

Musculoskeletal and connective tissue side effects:

Potassium loss may lead to muscle weakness, particularly when used concomitantly with cardiac glycosides, diuretics, and corticosteroids, as well as increased fatigue and muscle cramps.

Renal and urinary tract side effects:

With prolonged use or abuse of laxatives, protein and blood may appear in the urine (proteinuria and hematuria), as well as hyperaldosteronism and hypocalcemia. Depending on the pH value, urine may be discolored by metabolites into a yellowish or reddish-brown color, which is clinically insignificant.

Shelf life. 3 years.

Storage conditions.

Store at temperatures not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

6 cubes (each cube in an individual aluminum foil pouch laminated with waxed paper embossed with Regulax®) in a cardboard box; in polypropylene film.

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

Manufacturer.

Krewel Meuselbach GmbH.

Manufacturer's address.

Krewelstrasse 2, 53783 Eitorf, Germany.