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 caused by atony and hypotension of the colon (including in old age, in bedridden patients, after operations, after childbirth and during lactation);

constipation caused by taking drugs;

regulation of stool for hemorrhoids, proctitis, anal fissures (to soften the consistency of stool);

gallbladder diseases, irritable bowel syndrome with a predominance of constipation;

constipation caused by intestinal dysbiosis and diet disorders.

Pharmacological effect

Pharmacological action
Pharmacological action – laxative.

Special instructions

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

Dizziness and fainting have been observed in patients taking Guttalax®. The analysis showed that these cases are associated with syncope with defecation (or syncope caused by straining to defecate), or with a vasovagal reaction to abdominal pain, which may be due to constipation, and is not necessarily related to 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 and 0.3 g of sorbitol, respectively.

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

Effect on the ability to drive a car or operate machinery. No special clinical studies have been conducted on the effect of the drug on the ability to drive a car or use machinery. However, patients should be advised that they may experience dizziness and/or fainting due to a vasovagal reaction (i.e. during bowel spasm). If patients experience intestinal spasms, they should avoid potentially hazardous activities, incl. driving vehicles or operating machinery.

Active ingredient

Sodium picosulfate

Composition

active substance:
sodium picosulfate monohydrate
0.75 g
excipients:

sodium benzoate – 0.2 g;

sodium citrate dihydrate – 0.15 g;

liquid sorbitol (non-crystallizing) – 64.37 g;

citric acid monohydrate – 0.14 g;

purified water – 49.89 g

Pregnancy

There are no reliable and well-controlled studies in pregnant women.

Long-term experience with use has not revealed a negative effect of the drug on pregnancy.

Taking the drug in the first trimester of pregnancy is contraindicated.

Studies on the effect of the drug on fertility have not been conducted. Preclinical studies did not reveal any teratogenic effects on reproduction.

With caution – in the second and third trimesters of pregnancy (as when using other laxatives), the drug can only be taken as prescribed by a doctor.

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

Contraindications

hypersensitivity to sodium picosulfate or other components of the drug;

intestinal obstruction or obstructive bowel disease;

acute diseases of the abdominal organs or severe abdominal pain, which may be accompanied by nausea, vomiting, fever, including appendicitis;

acute inflammatory bowel diseases;

severe dehydration;

fructose intolerance.

Side Effects

From the gastrointestinal tract: discomfort, nausea, vomiting, cramps and pain in the abdomen, diarrhea.

From the nervous system: dizziness and fainting that occur after taking the drug may be associated with a vasovagal reaction (for example, straining during bowel movements, abdominal cramps).

From the immune system: hypersensitivity reactions.

From the skin and subcutaneous tissues: skin reactions (for example, angioedema, skin rash, drug rash, pruritus).

Interaction

Diuretics or corticosteroids increase the risk of electrolyte imbalance (hypokalemia) when taking high doses of Guttalax®.

Electrolyte imbalance may increase sensitivity to cardiac glycosides.

The combined use of the drug and antibiotics may reduce the laxative effect of the drug.

Overdose

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

Guttalax, like other laxatives, in chronic overdose can 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 the absorption of the drug after oral administration, induce vomiting or gastric lavage. Fluid replacement and correction of electrolyte balance may be required, as well as antispasmodics.

Storage conditions

At a temperature not exceeding 30 °C (do not freeze).

Keep out of the reach of children.

Shelf life

3 years

Manufacturer

Instituto de Angeli S.r.L., Italy