Guttalax^® (Tablets, Drops) Instructions for Use

ATC Code

A06AB08 (Sodium picosulfate)

Active Substance

Sodium picosulfate (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Laxative drug

Pharmacotherapeutic Group

Drugs for the treatment of constipation; contact laxatives

Pharmacological Action

Mechanism of Action

Sodium picosulfate, being a laxative acting at the level of the colon, stimulates the natural process of evacuation of contents from the lower gastrointestinal tract. For this reason, Sodium picosulfate does not affect the digestion or absorption of caloric food or essential nutrients in the small intestine.

Pharmacodynamic Effects

The active substance – Sodium picosulfate – is a laxative of the triarylmethane group. As a local laxative, Sodium picosulfate, after bacterial cleavage in the colon, exerts a stimulating effect on its mucosa, enhancing peristalsis, and promotes the accumulation of water and electrolytes in the colon. This leads to stimulation of the defecation act, reduction of evacuation time, and softening of stool.

The effect of the drug Guttalax^® was studied in a randomized, double-blind, parallel-group study involving 367 patients with chronic constipation. The study results showed a significant enhancement of intestinal peristalsis during each of the four weeks of therapy compared to placebo (p< 0.0001). Serum potassium concentrations remained unchanged by the end of the study (4.4 mM) and corresponded to the physiological norm (3.6-5.3 mM).

Preclinical Safety Data

In vitro and in vivo studies did not reveal a genotoxic potential of sodium picosulfate.

Experimental studies on the carcinogenic potential of sodium picosulfate have not been conducted.

In embryotoxicity studies in rats and rabbits, the use of doses up to 100 mg/kg/day was not accompanied by signs of teratogenicity; however, such doses had an embryotoxic effect on rats and rabbits. The use of doses of 10 mg/kg/day and higher during fetal development and lactation reduced weight gain and increased the risk of offspring death. Fertility of male and female rats at doses up to 100 mg/kg/day was not impaired.

Pharmacokinetics

Absorption

After oral administration, Sodium picosulfate reaches the colon without significant absorption.

Distribution

Enterohepatic circulation of the drug is excluded.

Biotransformation

In the distal part of the colon, bacterial cleavage of sodium picosulfate occurs with the formation of the active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), which has a laxative effect.

Elimination

After cleavage, a small amount of BHPM is absorbed and then almost completely bound in the intestinal wall and liver to form an inactive glucuronide. After oral administration of sodium picosulfate at a dose of 10 mg (about 10.4% of the total dose), the drug is excreted in the urine as BHPM-glucuronide within 48 hours. When sodium picosulfate is used in higher doses, its renal excretion decreases.

Linearity/Non-linearity

The time to onset of the laxative effect of the drug is determined by the rate of release of the active metabolite (BHPM) and is 6-12 hours after administration (on average 10 hours).

An insignificant part of the drug enters the systemic circulation. There is no relationship between the laxative effect of the active metabolite and its serum concentration.

Indications

For adults and children aged 4 years and older as a laxative in the following cases

• Constipation due to atony and hypotension of the colon (including in the elderly, in bedridden patients, after surgery, after childbirth and during lactation);
• Constipation caused by medication use;
• For regulating stool in hemorrhoids, proctitis, anal fissures (to soften stool consistency);
• Gallbladder diseases, irritable bowel syndrome with predominant constipation;
• Constipation due to intestinal dysbiosis, dietary violations.

ICD codes

Dosage Regimen

Drops

The drug Guttalax^® is intended for oral administration.

Adults

It is recommended to start with the lowest dose. To achieve regular stool, the dose can be increased to the maximum recommended. The maximum recommended daily dose should not be exceeded. Since the drug does not cause habituation, the patient can individually adjust the intake: reduce the dose depending on individual needs or use the drug once as needed.

Children

The drug should be used in children only as prescribed by a doctor.

The recommended dose for children under 4 years is 0.25 mg/kg body weight/day.

Recommendations for Use

To achieve a laxative effect in the morning, the drug should be taken the night before.

The time to onset of the laxative effect of the drug is 6-12 hours after administration (on average 10 hours).

The drug does not necessarily need to be dissolved in liquid. It has no taste, so it can be added to food for children.

To restore the natural rhythm of defecation, along with taking the laxative, it is recommended to increase physical activity, sufficient intake of dietary fiber (20-25 g/day) and fluids (at least 2 liters).

Tablets

The drug is taken orally. The tablets must be taken with a sufficient amount of liquid (at least half a glass of water).

Adults

It is recommended to start with the lowest dose. To achieve regular stool, the dose can be increased to the maximum recommended. The maximum recommended daily dose should not be exceeded. Since the drug does not cause habituation, the patient can individually adjust the intake: reduce the dose depending on individual needs or use the drug once as needed.

Children

Children should take the drug only as prescribed by a doctor.

Children under 4 years

This dosage form should not be used in children under 4 years of age. For this age group of patients, the use of the drug Guttalax^® in the form of drops is possible.

Recommendations for Use

To achieve a laxative effect in the morning, the drug should be taken the night before.

The time to onset of the laxative effect of the drug is 6-12 hours after administration (on average 10 hours).

To restore the natural rhythm of defecation, along with taking the laxative, it is recommended to increase physical activity, sufficient intake of dietary fiber in the diet (20-25 g/day), and sufficient fluid intake (at least 2 liters).

Adverse Reactions

According to WHO principles, adverse reactions are classified according to their frequency 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), frequency unknown (frequency of adverse reactions cannot be determined from available data).

Contraindications

• Hypersensitivity to sodium picosulfate or to any of the excipients included in the drug;
• Intestinal obstruction or obstructive intestinal diseases;
• Acute diseases of the abdominal organs or severe abdominal pain that may be accompanied by nausea, vomiting, fever, including appendicitis;
• Acute inflammatory bowel diseases;
• Severe dehydration;
• First trimester of pregnancy.

Use in Pregnancy and Lactation

Pregnancy

There are no data from adequate and well-controlled studies in pregnant women. Long-term experience has not revealed a negative effect of the drug on pregnancy. Use of the drug in the first trimester of pregnancy is contraindicated; in the second and third trimesters of pregnancy, it should be used only as prescribed by a doctor.

Breastfeeding Period

The active metabolite and its derivatives (glucuronides) are not excreted in breast milk. Thus, the drug can be used during breastfeeding.

Fertility

Studies on the effect on human fertility have not been conducted. No effect on fertility was identified in preclinical studies.

Pediatric Use

Guttalax^® in tablet form should not be used in children under 4 years of age. For this age group of patients, the use of the drug Guttalax^® in the form of drops is possible.

The drug should be used in children only as prescribed by a doctor.

Geriatric Use

Used in elderly patients.

Special Precautions

For many patients suffering from constipation, there is no need to take the maximum dose daily – the regularly taken dose can be reduced depending on the patient’s individual needs or the drug can be used once as needed.

The drug should not be taken daily for more than 10 days without consulting a doctor. Long-term use of high doses of the drug can lead to fluid loss, electrolyte imbalance, and hypokalemia.

Stimulant laxatives, including Guttalax^®, do not contribute to weight loss.

Dizziness and fainting have occurred in patients taking Guttalax^®. Analysis has shown that these cases are related to fainting during defecation (or fainting caused by straining during defecation) or to a vasovagal reaction to abdominal pain, which may be due to constipation and is not necessarily related to drug intake.

The drug should be prescribed with caution in the second and third trimesters of pregnancy. In this case, as with the use of other laxatives, the drug should be taken only as prescribed by a doctor.

Children over 4 years should take the drug only as prescribed by a doctor.

Excipients

Patients with rare hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this drug.

Effect on Ability to Drive Vehicles and Operate Machinery

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

Overdose

Symptoms

When using the drug in high doses, diarrhea, dehydration, decreased blood pressure, water-electrolyte imbalance, hypokalemia, and convulsions are possible. In addition, there are reports of cases of colonic muscle ischemia associated with taking doses of Guttalax^® significantly exceeding those recommended for the usual treatment of constipation.

Guttalax^®, like other laxatives, with chronic overdose can lead to chronic diarrhea, abdominal pain, hypokalemia, secondary hyperaldosteronism, and urolithiasis. Due to chronic abuse of laxatives, renal tubular damage, metabolic alkalosis, and muscle weakness associated with hypokalemia may develop.

Treatment

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 antispasmodics, may be required.

Drug Interactions

With Diuretics or Corticosteroids

When used concomitantly with high doses of Guttalax^®, diuretics or corticosteroids increase the risk of electrolyte imbalance (hypokalemia). Electrolyte imbalance, in turn, can increase sensitivity to cardiac glycosides.

With Antibiotics

Concomitant use of Guttalax^® and antibiotics may reduce the laxative effect of the drug

Storage Conditions

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

Shelf Life

Shelf life – 3 years. Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is available without a prescription.

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.