Guttalax, drops 7.5 mg/ml, 30 ml

Pharmacodynamics

The active substance – sodium picosulfate – is a laxative of triarylmethane group. As local laxative sodium picosulfate after bacterial cleavage in large intestine has stimulating effect on mucosa of large intestine, increasing peristalsis, contributes to accumulation of water and electrolytes in large intestine. This leads to stimulation of the act of defecation, reduction of evacuation time and softening of stools.

Sodium picosulfate, being a laxative acting at the level of the large intestine, stimulates the natural process of evacuation of contents from the lower parts of the GI tract. Therefore, sodium picosulfate has no effect on digestion or absorption of caloric foods or essential nutrients in the small intestine.

Pharmacokinetics

Absorption is insignificant, the drug is almost completely metabolized in the intestinal wall and liver to inactive glucuronide.

After oral administration, sodium picosulfate enters the large intestine; absorption of the drug is negligible, which rules out its enterohepatic circulation. Breakdown of sodium picosulfate occurs in the distal colon to form the active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane. The time of development of the laxative effect of the drug is determined by the rate of release of the active metabolite and usually is 6-12 hours after application (on average 10 hours).

A small part of the drug enters systemic blood stream. There is no correlation between the laxative effect of the active metabolite and its concentration in blood serum.

After oral administration of 10 mg of the drug about 10.4% of the total dose is excreted by the kidneys as glucuronide after 48 hours.

Higher doses of the drug are generally less excreted by the kidneys.

Indications

As a laxative in the following cases:

Constipation due to atony and hypotonia of the colon (including. In old age, in bed-ridden patients, after operations, after childbirth and during lactation);

Constipation caused by taking medication;

Stool regulation in hemorrhoids, proctitis, anal fissures (for softening the stool consistency);

Disease of gallbladder, irritable bowel syndrome with predominant constipation;

constipation caused by gut dysbacteriosis, dietary disorders.

Active ingredient

Composition

How to take, the dosage

Ingestion. In order to get a laxative effect in the morning hours, the drug should be taken the night before.

The following dosage regimen is recommended: adults and children over 10 years of age – 10-20 drops/day (5-10 mg/day); children 4-10 years of age – 5-10 drops/day (2.5-5 mg/day); under 4 years of age – 0.25 mg/kg/day (this corresponds to 1 drop of the drug (0.5 mg of sodium picosulfate)/2 kg/day).

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. The maximum recommended daily dose should not be exceeded.

The drug does not need to be dissolved in liquid.

Interaction

Diuretics or GCS increase the risk of electrolyte imbalance (hypokalemia) with high doses of Guttalax®.

The electrolyte imbalance may increase sensitivity to cardiac glycosides.

The co-administration of the drug and antibiotics may decrease the laxative effect of the drug.

Special Instructions

Do not use the drug daily without medical advice for more than 10 days. Prolonged use of high doses of the drug may lead to fluid loss, electrolyte imbalance, hypokalemia.

Dizziness and fainting have been observed in patients taking Guttalax®. Analysis showed that these cases were associated with fainting while defecating (or fainting caused by straining while defecating), or with a vasovagal reaction to abdominal pain, which may be due to constipation and is not necessarily related to taking the drug.

1 ml of drops contains 0.45 g of sorbitol. The maximum recommended daily dose for the treatment of adults and children 4-10 years old contains 0.6 g and 0.3 g of sorbitol, respectively.

The drug has no taste, so children can be added to food. Children should only take the drug as prescribed by their doctor.

The effect on the ability to drive or operate machinery. Special clinical studies of the effect of the drug on the ability to drive and operate machinery have not been conducted. 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

Hypersensitivity to sodium picosulfate or other ingredients of the drug;

intestinal obstruction or obstructive bowel disease;

acute abdominal disease, including appendicitis, or severe abdominal pain that may be accompanied by nausea, vomiting, or elevated body temperature;

acute inflammatory bowel disease;

serious dehydration;

fructose intolerance.

Side effects

Gastrointestinal disorders: discomfort, nausea, vomiting, abdominal cramps and pain, diarrhea.

Nervous system disorders: dizziness and fainting that occur after taking the drug may be associated with a vasovagal reaction (e.g., straining during defecation, abdominal cramps).

Immune system disorders: hypersensitivity reactions.

Skin and subcutaneous tissue disorders: skin reactions (e.g., angioedema, skin rash, drug rash, skin itching).

Overdose

Symptoms: diarrhea, dehydration, decreased blood pressure, water-electrolyte imbalance, hypokalemia, convulsions are possible when taking high doses. In addition, there have been reports of cases of ischemia of the colon muscles associated with doses of Guttalax® significantly higher than those recommended for normal treatment of constipation.

Guttalax, like other laxatives, in chronic overdose may lead to chronic diarrhea, abdominal pain, hypokalemia, secondary hyperaldosteronism, and urolithiasis. Renal tubular damage, metabolic alkalosis, and muscle weakness associated with hypokalemia may develop due to chronic laxative abuse.

Treatment: to reduce absorption of the drug after ingestion – induction of vomiting or gastric lavage. It may be necessary to replenish fluids and correct electrolyte balance, as well as prescription of antispasmodic agents.

Similarities