Pharmacodynamics
In the large intestine, lactitol is broken down by intestinal flora into low-molecular organic acids, which leads to an increase in osmotic pressure in the large intestine, an increase in the volume of feces, their softening, easier bowel movements and normalization of intestinal function. The laxative effect usually occurs within 24 hours after using the drug (the delay is due to the passage of the drug through the gastrointestinal tract). At the beginning of the course of treatment, the laxative effect of the drug may be delayed; the effect may occur on the 2nd or 3rd day of its use.
In patients with hepatic encephalopathy or coma (or precoma), the effect is achieved due to the migration of ammonia from the blood into the large intestine (due to a decrease in pH, an increase in osmotic pressure in the intestinal lumen), removal of retained ammonium ions and other nitrogen-containing toxic substances from the colon. Lactitol inhibits proteolytic bacteria and increases the number of acidophilic bacteria.
Exportal
Exportal ®
(lat.
exportale
) - medicine, osmotic laxative, prebiotic. Exportal is produced in the form of sachets containing 10 g of powder of the active substance - lactitol monohydrate for the preparation of a solution for oral administration.
Indications for use Exportal
- constipation
- regulation of stool in case of hemorrhoids, in preparation for operations and after operations on the rectum, anal sphincters, perineum and in other situations
- hepatic encephalopathy
- hepatic coma and precoma
- hyperammonemia.
Method of application of exportal and dose
Exportal is taken orally during meals, mixed with various drinks: water, tea, coffee, juices or liquid food. Exportal should be taken once, the entire daily dose at once, in one dose. Daily dose of Exportal for constipation:
- children 1–6 years old – 2.5–5 g
- children 6–12 years old – 5–10 g
- children 12–16 years old – 10–20 g
- adults - 20 years
Exportal should cause one bowel movement per day.
After the onset of a stable laxative effect within several days of using Exportal, its dose can be reduced. A laxative effect is often achieved by taking half the above dose. Daily dose of Exportal for hepatic encephalopathy, hepatic precoma and coma, hyperammonemia
should be selected individually for each patient, depending on the severity of the disease and individual response to Eexportal, based on the fact that the initial daily dose should be 0.5–0.7 g per 1 kg of body weight. Exportal is taken three times a day, with meals, one third of the daily dose with meals. The dose is gradually selected to cause two “soft” bowel movements per day.
Side effects of Exportal
At the beginning of therapy with Exportal, there may be a feeling of discomfort in the abdomen and flatulence, which, as a rule, disappear with continued use of Exportal.
Comparison of Exportal with other laxatives
Exportal, compared to Forlax, has higher clinical efficacy in the treatment of chronic constipation in elderly and senile patients, fewer side effects and a faster response to therapy.
This is due to the more pronounced effect of Exportal on the motor activity of the colon, confirmed by electrogastroenterography data, as well as the normalization of the disturbed intestinal ecosystem, which was expressed by more significant changes in the concentration and qualitative composition of short-chain fatty acids, which are metabolites of the obligate microflora of the colon (Minushkin O.N. and etc.). Exportal has advantages over other laxatives, allowing its use in a wide variety of patient groups (Kolkhir V.K.):
- Exportal has a mild laxative effect and a stable effect from the use of the drug. Clinical studies confirm that with prolonged use and repeated repeated treatment, Exportal is not addictive, and therefore no upward dose adjustment is required
- lactitol is not broken down and not absorbed in the small intestine. Exportal has a low calorie content and does not affect blood glucose levels, so Exportal, unlike lactulose-based drugs, can be used in patients with diabetes
- Export can be taken by pregnant women and children over 1 year of age
- Exportal does not have a destructive effect on tooth enamel, since, unlike other substances, it does not reduce the pH level in the oral cavity and does not cause caries, which is important for long-term use of laxatives
- Exportal does not affect the excretion of calcium in the urine and the metabolism of bone tissue in terms of the concentration of parathyroid hormone, osteocalcin and alkaline phosphatase. At the recommended dosage, it also does not affect the concentration of phosphate and calcium in the blood.
- Exportal sachets contain only the active ingredient - lactitol and no other additional substances. Export can be stored for a long time and is convenient to use. To dissolve the drug, the patient can choose the most suitable drink for him.
- the taste of lactitol, according to more than 70% of many patients, is superior to the taste of lactulose
- Exportal is effective for chronic constipation of various etiologies, functional constipation, as a means of accelerating the restoration of defecation function and facilitating defecation after operations on the anal sphincter, and also as a drug necessary for softening stool for medical purposes, including hemorrhoids, preparation for operations and after operations on the rectum.
Exportal also has prebiotic properties: it selectively stimulates the growth of sugar-splitting bacteria that have a beneficial effect on human health - bifidobacteria and lactobacilli, including lactobacilli acidophilus, inhibits the growth of enterobacters and enterococci, and inhibits the adhesion of E. coli to epithelial cells. Lactitol, unlike lactulose, is not broken down by E. coli and is broken down by significantly fewer strains of Staphylococcus aureus and Clostridium perfringens (Kolkhir V.K.).
Contraindications to the use of Exportal
Lactitol intolerance, galactosemia, intestinal obstruction, suspected organic damage to the gastrointestinal tract, abdominal pain and rectal bleeding of unknown origin.
Professional medical publications concerning the use of Exportal in the treatment of gastrointestinal diseases:
- Minushkin O.N., Ardatskaya M.D., Voskoboynikova I.V., Kolkhir V.K. Exportal (Lactitol) is an effective and safe osmotic laxative // RZHGGK. - 2010. - T.20. - No. 5. - Adj. No. 36. — P. 118.
- Minushkin O.N., Ardatskaya M.D., Voskoboynikova I.V., Kolkhir V.K. Analysis of the clinical effectiveness of the drugs Exportal and Forlax // RZHGGK. - 2010. - T.20. - No. 5. - Adj. No. 36. — P. 118.
- Minushkin O.N. Chronic constipation // Medical advice. 2015. No. 13. pp. 100-105.
- Gasilina T.V., Belmer S.V. Issues of drug therapy for constipation of functional origin in children // Medical Council. 2015. No. 14. pp. 54–58.
- Ardatskaya M.D., Butorova L.I., Grigorieva Yu.V. et al. Clinical and metabolic effectiveness of lactitol in the treatment of chronic constipation (results of the non-interventional prospective observational program “Osmoaid”). Experimental and Clinical Gastroenterology 2018;150(2):149–160.
On the website GastroScan.ru in the “Literature” section there is a subsection “Laxatives”, containing publications for healthcare professionals regarding laxatives and their use.
Additional Information
Exportal (lactitol) has a low calorie content (2 kcal/g), does not affect blood glucose levels and can be used in patients with diabetes.
Exportal is a prescription medicine. Throughout the entire course of therapy with Exportal, increased fluid intake is desirable.
Exportal does not affect psychomotor functions associated with driving a car or operating machines and mechanisms.
According to the pharmacological index, Exportal belongs to the group “Laxatives”. For ATC - to the group “Osmotic laxatives”, code A06AD12.
Other trade names of drugs with the active substance lactitol: Lactitol monohydrate.
“Instructions for medical use of the drug Exportal” (pdf), powder for the preparation of a solution for oral administration. Exportal developer company:
CJSC FPK "FarmVILAR", Russia. In March 2015, the right to produce Exportal was sold to Valenta Pharm OJSC. Back to section
Directions for use and doses
Inside, during meals, mixing with various drinks (including water, tea, coffee, juices) or liquid food.
Constipation and dysbiosis. The drug should be taken once, the entire daily dose at once, in one go. Adults - 20 g/day (4 teaspoons of powder); children 12–16 years old - 10–20 g/day (2–4 teaspoons of powder); 6–12 years – 5–10 g/day (1–2 teaspoons of powder); 1–6 years – 2.5–5 g/day (0.5–1 teaspoon of powder).
The drug should induce stool once a day; After the onset of a stable laxative effect within several days of using the drug, its dose can be reduced. In some cases, half the recommended daily dose is sufficient to obtain the desired effect. The minimum course of therapy, after which you should consult a doctor, is 5 months. The use of the drug in children is recommended under medical supervision.
Regulating stool for medical purposes. 20 g of the drug, diluted in 1 liter of water, is taken 3 times (at 12, 15 and 18 hours) on the eve of medical procedures.
Hepatic encephalopathy, hepatic precoma and coma, hyperammonemia. The dose of the drug should be selected individually for each patient, depending on the severity of the disease and individual response to the drug. The initial daily dose is usually 0.5–0.7 g/kg. This dose is divided into 3 single doses. A dose should be selected that causes two soft stools per day.
Exportal® is more than just a laxative!
Exportal®
helps eliminate constipation and restore intestinal barrier function to protect the whole body from endotoxin aggression1,2.
The active ingredient, lactitol, belongs to the group of osmotic laxatives recommended by the Russian Gastroenterological Association and the Society of Children's Gastroenterologists, Nutritionists and Hepatologists as first-line drugs for the drug treatment of constipation1,2.
Lactitol attracts and retains water in the lumen of the colon. As a result, the contents of the colon soften to make bowel movements easier. 1.
Subsequently, lactitol is processed by bacteria that are beneficial to the human body and live in the large intestine, producing large amounts of butyric acid. Butyric acid “nourishes” the intestinal cells, which helps restore its barrier function to protect the body from the penetration of bacteria and their components (for example, endotoxins) from the intestinal lumen2,3.
In addition, lactitol “feeds” colon bacteria that are beneficial to the human body, thus restoring the microbiome (the prebiotic effect of lactitol, similar to the effect of dietary fiber)1.
Exportal®1
- Does not contain excipients, dyes or flavors;
- Tastes similar to table sugar but less sweet;
- Packaged in sachets, which are convenient to take with you;
- Acts only in the intestinal lumen;
Exportal® can be used1:
- children over 1 year old;
- pregnant and lactating women (if the potential benefit to the mother outweighs the potential risk to the fetus and child);
- patients with diabetes mellitus, because lactitol does not increase blood glucose levels;
- patients with liver diseases;
- To old people.
Directions for use: Exportal®1: 1 time per day, orally during meals, mixed with various drinks (water, tea, coffee, juices, etc.) or liquid food.
________________________________________________
1IMP Exportal LSR-003898/07
2Ardatskaya M.D. et al. Clinical and metabolic effectiveness of lactitol in the treatment of chronic constipation (results of the non-interventional prospective observational program “OSMOAID”) // Experimental and Clinical Gastroenterology. – 2021. – No. 2 (150).
3Ivashkin V. T. et al. Diagnosis and treatment of constipation in adults (Clinical recommendations of the Russian Gastroenterological Association and the Association of Coloproctologists of Russia) // Russian Journal of Gastroenterology, Hepatology, Coloproctology. – 2021. – T. 30. – No. 6. – pp. 69-85.
4Belmer S.V. et al. Functional disorders of the digestive organs in children. Recommendations of the Society of Pediatric Gastroenterologists, Hepatologists and Nutritionists. Part 2 // Russian Bulletin of Perinatology and Pediatrics. – 2021. – T. 65. – No. 5.
special instructions
Lactitol has a low calorie content (2 kcal/g), does not affect blood glucose levels and can be used in patients with diabetes.
Throughout the entire course of use of the drug, increased fluid intake is desirable.
Impact on the ability to drive vehicles and operate machinery. The use of the drug Exportal® does not affect psychomotor functions associated with driving a car or operating machines and mechanisms.
Exportal - an innovative laxative drug
About the article
18829
0
RMJ Appendix “Diseases of the Digestive Organs” No. 2 dated 01.09.2009 p. 80
Category: Digestive diseases
Author: Kolhir V.K.
For quotation:
Kolkhir V.K. Exportal is an innovative laxative drug. RMJ. 2009;2:80.
Chronic constipation. Today, this misfortune so aggravates the condition of millions of people around the world that it really is a socially significant problem. Moreover, due to the high frequency of occurrence, constipation is elevated to the rank of an independent disease.
According to modern concepts, chronic constipation can be defined as a chronic delay in bowel movement, characterized by a stool frequency of less than 3 times a week and accompanied by at least one of the following symptoms: a feeling of incomplete evacuation, a small amount and dense consistency of stool, and straining for at least a quarter of the time of defecation. According to medical statistics, chronic constipation is most common in young children and is one of the most common complaints in elderly patients. When treating constipation, both non-drug treatment methods are used (increasing physical activity, normalizing water balance and diet, playing sports, etc.) and treatment with laxatives. However, the choice of a laxative drug is often difficult when treating children, pregnant women, patients with diabetes mellitus and cardiovascular diseases, and elderly and senile patients. A significant breakthrough in the development of laxatives was made by the Russian pharmaceutical company, whose business activity has been going on for more than 10 years (the company was founded on the basis of the All-Russian Institute of Medicinal and Aromatic Plants in 1998). In the spring of 2009, the company introduced a new laxative to the Russian market - the drug Exportal®, the active ingredient of which is lactitol, which is a crystalline, non-hygroscopic and highly water-soluble powder with a sweetish, sugar-like taste. Abroad, laxatives based on lactitol have been used for many years and are one of the most popular means for treating constipation. In Russia, the drug Exportal® is produced only. Exportal® belongs to the group of osmotic laxatives. According to the mechanism of action, it differs from other similar drugs (with the exception of drugs based on lactulose) in that it is not the active substance itself that has osmotic properties, but the products of its metabolism in the colon, which are formed under the influence of certain types of bacteria that break down sugars. In the small intestine, Exportal® does not undergo significant enzymatic degradation and is not absorbed. Once in the colon, Exportal® is broken down by local bacteria to produce short-chain fatty acids, carbon dioxide and water. Since these substances are not absorbed, they increase osmotic pressure and make the intestinal contents more viscous by retaining water. Since Exportal® is a source of energy for colon bacteria that break down sugars, its use increases the mass of bacteria, and therefore the mass of intestinal contents, which has a positive effect on its emptying (Fig. 1). Many years of experience in use, as well as numerous tests of lactitol (the active ingredient of Exportal®) indicate its effectiveness, high level of safety and the absence of significant negative reactions. Exportal® has significant advantages over other laxatives, allowing its use in a wide variety of patient groups. 1. Exportal® has a mild laxative effect. The effect of using the drug is stable. Data from clinical studies confirm that with prolonged use and repeated repeated treatment, the drug is not addictive, and therefore no upward dose adjustment is required. 2. Since the active substance is not broken down or absorbed in the small intestine, Exportal® has a very low calorie content (2 Kcal/g) and does not affect blood glucose levels. In this regard, Exportal®, unlike lactulose-based drugs, can be used without restrictions in patients with diabetes. 3. Without restrictions, Exportal® can be used in pregnant women, as well as in children over the age of 1 year. 4. Exportal® does not have a destructive effect on tooth enamel, since, unlike other substances, it does not reduce the pH level in the oral cavity and does not cause the formation of caries, which is especially important during long-term use of laxatives. 5. Exportal® does not affect the excretion of calcium in the urine and the metabolism of bone tissue in terms of the concentration of parathyroid hormone, osteocalcin and alkaline phosphatase. At the dose used, it also does not affect the concentration of inorganic phosphate and calcium in the blood plasma. 6. The dosed dosage form of Exportal® in sachets (the drug is available in sachet packaging No. 20) contains only the pharmaceutical substance and does not contain any excipients or other additional substances. Exportal® in sachets does not require any measurements when dosing, is perfectly stored for a long time and is convenient to use (you can take a separate sachet with you for taking at work, etc.). To dissolve the drug, the patient himself can choose the most suitable drink for him, which is of no small importance if it is necessary to take the drug for a long time. For hospitals, a special form of release of the drug in 200 g containers has been developed, which allows the effective use of Exportal® in gastroenterological, surgical, therapeutic and other departments of hospitals. 7. The taste of lactitol is superior to that of lactulose, which was tested in clinical studies in 172 patients with constipation. After the first dose, more than 70% of patients chose lactitol based on taste. Exportal® is effective for chronic constipation of various etiologies, functional constipation, as a means of accelerating the restoration of defecation function and facilitating defecation after operations on the anal sphincter, as well as a drug necessary for softening stool for medical purposes (including for hemorrhoids, preparation before and after operations on the rectum, etc.). As evidenced by the results of a comparative clinical study of the laxative effect of substances such as lactitol (the active ingredient of the drug Exportal®) and lactulose, the effect of lactitol turned out to be more stable. Depending on the patient population, it was either not inferior to lactulose or was more effective. A comparative study was conducted of the effect of lactitol powder and lactulose powder in a daily dose of 10 g, as well as lactulose syrup (10 ml/day) and placebo on intestinal transport function in hospitalized patients. It was found that all laxatives studied approximately equally accelerate the movement of the capsule in the intestine and increase the rate of its movement to the greatest extent in the proximal part of the large intestine. Numerous clinical studies have determined the optimal doses of lactitol in different categories of patients suffering from constipation. In patients, the optimal daily dose of the drug, ensuring effectiveness and good tolerability of treatment, was 300 mg per 1 kg of body weight, which corresponds to an average dose of 20 g/day. After achieving the desired effect, it is possible to reduce the dose of the drug to 10 g/day. Much attention in trials of the active substance lactitol was paid to the treatment of constipation in elderly patients, in whom constipation occurs on average 1.8 times more often than in younger people, and in old people - 2.4 times more often. In some older people, intestinal motility is disrupted, abdominal muscles weaken, and significant changes in the composition of intestinal microorganisms occur, associated with a significant decrease in lactic acid bacteria. Such patients are shown laxatives that do not cause an increase in intra-abdominal pressure when straining (which is dangerous in case of myocardial infarction, severe arterial hypertension, aneurysm, venous thrombosis, retinopathy, hernia, rectal fissures, hemorrhoids, etc.), and also normalize the intestinal microflora. Studies have shown that the use of lactitol in elderly patients was effective and the drug was well tolerated by patients. For older people, the most effective dose was 20 mg/day. A single 20 mg dose has also been shown to be better tolerated than 2 10 mg doses. These results were confirmed in a study in which patients were treated for a year and lactitol remained effective at a constant dose. In pediatric practice, 5 clinical studies were conducted and the effect of lactitol in children was studied. The initial dose was individualized to achieve soft stools at least once daily. The effective dose ranged from 150 to 350 mg per 1 kg of body weight, and the effect was achieved in 71% of children. As a result, recommended dosages for children were established: • 1–6 years: 2.5–5 g (1/2–1 teaspoon of powder per day); • 6–12 years: 5–10 g (1–2 teaspoons of powder per day); • 12–16 years: 10–20 g (1–2 sachets or 2–4 teaspoons of powder per day). In a study of the laxative effect of lactitol in pregnant women, it was shown that in 80% of women the drug dose was 20 g/day. was enough to provide stool once a day in the morning. In all cases, the pregnancy ended normally. The side effects of lactitol correspond to what can be expected after taking the disaccharide, which enters the small intestine in an undigested form and is subsequently subjected to enzymatic breakdown by bacterial microflora. In the course of the studies, it was revealed that when using lactitol, such side effects as flatulence are less pronounced than with other lactulose-based laxatives. Side effects tend to weaken with long-term treatment, which is associated with changes in the composition of the colon microflora. It is advisable to take the daily dose of Exportal® at one time; this reduces the frequency and severity of intestinal side effects. In addition to the laxative, Exportal® has prebiotic properties: selectively stimulates the growth of sugar-splitting bacteria that have a beneficial effect on human health - Lactobacillus spp., Lactobacillus bifidus, Lactobacillus acidophilus, Bifidobacteria, inhibits the growth of proteolytic bacteria of the genera Enterobacteria and Enterococci, inhibits the adhesion of E. coli ) to epithelial cells. The effect of the drug leads to a shift in the composition of the colon microflora towards the predominance of bacteria that break down sugars. These bacteria are considered beneficial, especially bifidobacteria and lactobacilli, and increasing their numbers improves the overall well-being of patients. At a dose of 20 g/day. lactitol (the active ingredient of the drug Exportal®) significantly increased the number of lacto- and bifidobacteria and significantly reduced the content of aromatic substances and potentially carcinogenic enzymes in the colon. In a comparative study of the effect of lactitol and lactulose on probiotic and conditionally pathogenic and pathogenic bacteria, it was found that the effect of lactitol is more selective. In particular, unlike lactulose, it is not broken down by Escherichia coli (E. coli) and is broken down by significantly fewer strains of staphylococcus (St. aureus) and clostridia (Cl. perfringens). Another effect of Exportal® is associated with a selective effect on the intestinal microflora - an antiammonemic effect. In this regard, Exportal® is used as a drug for the treatment of hepatic encephalopathy, formed through a violation of the detoxification function of the liver and the direct release of toxic agents during the development of portal hypertension. Exportal® operates through several mechanisms. In particular, it is a source of energy for colon bacteria that break down sugars. Due to this, the number of such bacteria increases, and they inhibit the growth of bacteria that break down proteins, the activity of which leads to the formation of ammonia and endotoxins. When Exportal® breaks down, short-chain fatty acids are formed, which lower the pH in the large intestine. Under these conditions, ammonia is converted into ammonium ion NH4+, which is less absorbed and, as a result, the symptoms are weakened (Fig. 2). For the treatment of hepatic encephalopathy, Exportal® is prescribed in 1.5–3 times higher daily doses than for the treatment of constipation. Thus, the data from clinical trials and the practice of widespread medical use indicate that Exportal® is a safe laxative with a mild effect, effective for chronic and functional constipation of various etiologies, as well as a drug that accelerates the restoration of bowel function, improves and/or restoring intestinal microflora. In addition, Exportal® can be used as a treatment for hepatic encephalopathy, hepatic coma and precoma in a wide variety of patient groups. In medical practice, it is recommended to prescribe Exportal® to children and adults, pregnant women and patients suffering from diabetes.
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Exportal pores for oral administration pak 5g N6
Registration Certificate Holder
VALENTA PHARM (Russia)
Dosage form
Medicinal product – Exportale®
Description
Powder for solution for oral administration
white, crystalline.
1 pack
lactitol monohydrate 5 g
5 g - single-dose sachets (2) - strips (3) - cardboard packs. 5 g - single-dose sachets (2) - strips (6) - cardboard packs.
Indications
Constipation, stool regulation (including with hemorrhoids, preparation for operations and after operations on the rectum, anal sphincter and the adjacent area).
Hepatic encephalopathy, hepatic coma and precoma, hyperammonemia.
Contraindications for use
Galactosemia, intestinal obstruction, suspicion of organic damage to the gastrointestinal tract, abdominal pain, rectal bleeding of unknown origin, previous water and electrolyte imbalance, children under 1 year of age, hypersensitivity to lactitol.
pharmachologic effect
Laxative and hippoammonemic agent.
In the large intestine, lactitol is broken down by the intestinal flora into low-molecular organic acids that increase osmotic pressure, which helps to increase the volume of feces, soften them, and facilitate the act of defecation. The laxative effect occurs within 24 hours after use or on the 2-3rd day (due to the passage of lactitol through the gastrointestinal tract).
In hepatic encephalopathy or hepatic coma (or precoma), the effect is achieved through the transport of ammonia from the blood to the large intestine (due to a decrease in pH, an increase in osmotic pressure in the intestinal lumen) and the removal of ammonium ions and other nitrogen-containing toxic substances from the colon.
It has a prebiotic effect, restores its own intestinal microbiome.
Suppresses proteolytic bacteria and increases the number of acidophilic bacteria.
Drug interactions
When taken concomitantly with enteric pH-dependent release drugs, it should be taken into account that lactitol reduces intestinal pH.
Dosage regimen
Taken orally.
The dose and frequency of administration depend on age and indications for use.
Side effect
From the digestive system:
flatulence, abdominal pain, vomiting, diarrhea; very rarely - nausea, anal itching.
From the side of metabolism:
with long-term use in high doses in the treatment of hepatic encephalopathy, electrolyte imbalance may occur.
special instructions
Use with caution in patients with a tendency to disturb water and electrolyte balance.
During treatment, increased fluid intake is desirable.
The interval between doses of other medications is at least 2 hours.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - With caution.
Can be used during pregnancy and lactation in cases where the expected benefit of therapy for the mother outweighs the possible risk for the fetus or infant.
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
For hepatic encephalopathy, hepatic precoma and coma, the dose is set individually.
Use in children
Restrictions for children - With caution.
Contraindicated for use in children under 1 year of age.