Sulfasalazine or Pentasa, which is better? Some treatment features

The drug Sulfasalazine has powerful antimicrobial and anti-inflammatory effects. The medicine can also be used for diseases of the musculoskeletal system (for example, arthritis or ankylosing spondylitis).

Without strict indications, taking the drug is strictly prohibited: Sulfasalazine can have serious side effects, even with a short course of treatment. Before taking Sulfasalazine, you should always consult your doctor.

1 What is Sulfasalazine: general description

The drug Sulfasalazine belongs to the group of anti-inflammatory and antimicrobial drugs. It can be used in the treatment of various diseases of the musculoskeletal system (mostly severe).

It is also used for various autoimmune diseases, occurring with pronounced inflammatory phenomena. For example, with nonspecific ulcerative colitis or proctitis, with some forms of arthritis (including rheumatoid).

Composition of Sulfasalazine:

  • basic active substance– Sulfasalazine (500 mg in one tablet);
  • colloidal anhydrous silicon;
  • propylene glycol;
  • gelatinized starch;
  • hypromellose;
  • magnesium stearate;
  • titanium dioxide;
  • dyes with code E172 (iron oxide yellow 10).

During treatment with Sulfasalazine, constant monitoring (monitoring) of the patient's condition is required. The fact is that the drug quite often produces unwanted side effects, especially with long-term therapy.

1.1 Release form

There are two versions of Sulfasalazine: classic and with the prefix “EN”. Both versions of the drug have only one release form: tablets.

Regular Sulfasalazine tablets are film-coated and contain 500 mg of active ingredient. One package contains 50 yellow-brown tablets. The tablets are round, biconvex, and have beveled edges. There may be inclusions on the fracture.

Sulfasalazine EH tablets are coated with an enteric soluble coating and contain 500 mg of active ingredient. One package contains 50 tablets of yellow-brown or simply yellow color. The tablets are round, biconvex, have beveled edges and bad smell. The mass of the tablet at the break has a brownish-orange or orange color.

The tablets should be stored in their packaging, without removing them from the blisters, out of the reach of children and sun rays place. The optimal storage temperature is no more than 25 degrees.

1.2 How does it affect the body?

The drug represents its therapeutic effect And chemical structure a combination of sulfapyridine and 5-aminosalicylic acid. The smallest part of the drug is absorbed from the lumen of the colon and then evenly distributed throughout the connective tissues.

The tablet is coated with a film that dissolves under the influence of normal intestinal microflora. After the tablet film disintegrates, sulfapyridine and 5-aminosalicylic acid are released.

It is these substances that create a powerful anti-inflammatory and antimicrobial effect. In terms of anti-inflammatory activity, sulfapyridine is much better, since it has better absorption (about 30% of the dose taken is absorbed by the body).

Half-life products of components are excreted, including by the kidneys. This means that people with kidney diseases (including acute nephritis) either cannot take the drug at all or must take it with caution.

1.3 Where is Sulfasalazine sold and how much does it cost?

You can purchase Sulfasalazine either on specialized medical Internet portals or in pharmacies. The drug is available only with a prescription.

How much does Sulfasalazine cost? Standard packaging for 50 tablets (500 mg) costs 600-700 rubles. Sulfasalazine EH has a slightly higher cost: on average it is 670-750 rubles.

1.4 Sulfasalazine analogues: what can be replaced?

What can replace Sulfasalazine? Medicines for replacement great amount, but Mesacol and Methotrexate have proven themselves best. These are the best and most similar in price/effect analogues.

Other analogues of Sulfasalazine:

  1. Tablets Salazopyrine En-Tabs 500 mg.
  2. Asacol tablets 800 mg.
  3. Long-acting granules and Pentas tablets.
  4. Gastro-resistant granules and Salofalk suppositories, 250 and 500 mg.
  5. Rectal suspension and enteric tablets Samezil 400 and 800 mg.

Methotrexate is one of the best analogues Sulfasalazine

Prohibited independent choice Sulfasalazine and its replacement with analogues without consulting your doctor. In particular, you cannot replace the drug even in cases where the analogue is a drug with almost identical composition and dosage of use.

It is also impossible to replace the classic Sulfasalazine with a subtype with the prefix “EN” without consulting a doctor.

2 Indications: when is Sulfasalazine used?

The use of Sulfasalazine is justified in cases inflammatory diseases occurring with symptoms of microbial invasion, or the risk of infectious complications. Using the product as an analogue of an antibiotic is inappropriate and in some cases extremely dangerous.

Indications for use:

  • nonspecific ulcerative colitis or nonspecific ulcerative proctitis, occurring with mild or average degree severity (the drug is used to relieve exacerbations and as maintenance therapy in the remission phase of the disease);
  • Crohn's disease (only moderate or moderately severe forms of the disease during exacerbation, for full treatment of this disease the drug is not suitable);
  • rheumatoid arthritis with severe inflammatory processes that are not controlled by non-steroidal anti-inflammatory drugs (you can read about the use separately);
  • juvenile idiopathic chronic polyarthritis with resistance to treatment with non-steroidal anti-inflammatory drugs.

Sulfasalazine can be used in combination with various corticosteroid drugs and some antimicrobials (for example, the drug has good compatibility with Metronidazole).

2.1 Contraindications

Using Sulfasalazine correctly means making sure in advance that there are no contraindications. It is almost impossible to do this yourself; a comprehensive examination by doctors is necessary (at least at the level of studying biochemical parameters blood and urine).

Contraindications to Sulfasalazine:

  1. Individual intolerance to one or more components of the drug (presence of allergies).
  2. Acute form of porphyria and/or granulocytopenia.
  3. Severe deficiency of the enzyme glucose-6-phosphate dehydrogenase.
  4. The medication is prohibited for use by children under 5 years of age.
  5. Severe liver and/or kidney dysfunction, chronic renal or liver failure.
  6. Various types of anemia (including severe iron deficiency anemia), various diseases blood.
  7. Intestinal obstruction or compression of the urinary tract.
  8. Lactation period (breastfeeding). During pregnancy, the drug is used, but only under the strictest indications.
  9. The medication should be used with caution in case of systemic juvenile idiopathic-chronic polyarthritis (the development of serum-like reactions is possible).

Each of us has probably felt discomfort and pain in the abdomen and stomach. Sometimes they appear due to poor-quality food consumed the day before, and sometimes they can indicate the presence of a serious illness. For example, ulcerative colitis or Crohn's disease. Such ailments are rare, but they should absolutely not be neglected. Most often, doctors, having discovered such a pathology, prescribe the drug "Salofalk" to patients. Analogues, composition, instructions for use and reviews of the medicine - we will try to answer these questions in this article.

Release form and composition

The described drug is available in several forms. However, they all contain the same active ingredient - mesalazine. Only its dosage and some of the auxiliary components differ. We list the main types of forms:

  • Rectal suppositories - available in white, cream and dark brown color, which depends on the dosage of the drug. One suppository may contain 250 mg, 500 mg or 1 g of mesalazine. They are made in a torpedo shape. An auxiliary component is solid fat.
  • Tablets have a round, biconvex shape. Their color can vary from yellow to light brown. May contain 250 or 500 mg of active ingredient. Additional components - glycine, microcrystalline cellulose, silicon dioxide, magnesium stearate, dyes and others.
  • Granules - they are covered with a soluble coating and have a prolonged effect. They contain 500 mg of mesalazine. They are available in gray or white, round or cylindrical in shape. The shell consists of hypromellose, talc, magnesium stearate, silicon dioxide and vanilla flavor.

Sometimes in pharmacies you can also find less common forms of the drug "Salofalk" - rectal suspension or foam. The product is produced in cardboard boxes, where it is packed in blisters or plastic bottles. The medicine is produced in Germany.

Indications for use

The drug can be taken only after consultation with your doctor. It is sold in pharmacies strictly according to prescription. The drug "Salofalk" (its analogues and their indications for use may differ slightly) is prescribed for chronic ulcerative colitis or Crohn's disease. As a rule, it is used for cupping pain syndrome if the disease has worsened or is in acute form. It has an anti-inflammatory effect on organs gastrointestinal tract. In addition, it may be prescribed to prevent new exacerbations.

Suppositories and liquid suspensions are used when the disease has spread to the rectum and left side colon. In this case, tablets can be taken only during an exacerbation ulcerative colitis mild or moderate severity. If the patient's condition is severe, then use more effective methods treatment.

Possible side effects

The instructions for use call the drug "Salofalk" strong remedy, which has a significant impact on the human body. With him long-term use the patient may develop the following side effects:

  • allergic reactions associated with the patient’s sensitivity to any component of the drug - rash, redness of the skin and severe itching, may also experience fever, bronchospasms, symptoms acute pancreatitis, nephritis and systemic lupus erythematosus;
  • disorders of the gastrointestinal tract - nausea and vomiting, loss of appetite, diarrhea, extremely rarely jaundice, hepatitis may occur, sharp pains in the abdomen due to allergic inflammation of the intestines and dysfunction of bile secretion;
  • headaches and dizziness, sometimes taking the drug can provoke depression and sleep disturbances;
  • convulsions, tremor of the limbs and their paresthesia - extremely rare;
  • horse racing blood pressure, tachycardia, less often - shortness of breath and chest pain; nagging pain in muscles and joints;
  • anemia and bleeding disorders - extremely rare in some cases;
  • decrease in urine or complete absence, increasing the content of blood, proteins or salts in it.

If any of these symptoms appear, use of the drug should be stopped immediately and consult a doctor for treatment.

Who should not take the drug?

Unfortunately, this drug is not suitable for all patients. To prevent complications or exacerbations of other chronic diseases, be sure to consult a doctor before you start taking the medicine "Salofalk". Analogues or the selection of a more gentle medication in the presence of contraindications can only be prescribed by a specialist. We list the main pathologies for which the use of the medicine is strictly prohibited:

  • various blood diseases, especially if they are associated with blood clotting disorders;
  • stomach ulcer or duodenum, as well as gastritis, which is in the acute stage;
  • severe renal or liver failure, since the drug is excreted through these organs, so they may not be able to withstand the load;
  • phenylketonuria - in this case, only taking granules is prohibited;
  • hypersensitivity to any component of the drug;
  • hemorrhagic diathesis, complicated by a tendency to bleed.

In addition, the tablets are not recommended for use by children under 6 years of age. Instead, granules or suppositories are usually prescribed, which can be taken from 2-3 years. Doctors may prohibit taking medication if you have kidney or liver failure mild to moderate severity, if it is considered that the medicine may aggravate the course of the disease. It should also not be taken on early stages pregnancy, as well as during breastfeeding.

"Salofalk": instructions for use

The rules for taking this drug will depend entirely on the form in which the patient will use it. The decision on its choice should be made only by qualified specialist, which is based on the patient’s medical history and tests. As a rule, the patient should take up to 1-1.5 g of Salofalk per day.

Reviews of candles are called effective and easy to use. They should be used 3 times a day, 500 mg at any time, without combining their use with meals. At severe forms disease, the dose can be doubled. For prevention and long-term treatment it is reduced to 250 mg, but also taken 3 times a day. Children are prescribed half the adult dose.

Tablets and granules of the drug "Salofalk", analogues of which will be described in this article, are taken orally with a drink. big amount water. It is strictly forbidden to chew or bite them. The drug is taken in the morning, after lunch and in the evening, but always after a hearty meal. You can also take your entire daily dose after breakfast if you are being treated with granules.

If such symptoms appear, you should immediately contact a specialist. Doctors in such situations usually prescribe symptomatic treatment. The patient's stomach is washed and laxatives are prescribed. In case of severe intoxication, the patient is given forced diuresis - copious urine production is stimulated in order to eliminate toxic substances from the body.

The drug "Salofalk": Russian and foreign analogues

Since the described remedy is quite expensive, but you need to take it a long period, then not all patients can afford it. In addition, the medication may not be suitable for some people due to contraindications and side effects. Therefore, before starting treatment, responsible and economical patients always strive to find out about the availability of cheaper, usually domestic, similar drugs. The drug "Salofalk" has no Russian analogues. Nearest pharmaceutical company, which produces a similar product, is located in Belarus. However, even in this case, you can find budget medications, but you can change the medication you are taking only with the permission of your doctor.

We list the main analogues of "Salofalk" that can be bought in pharmacies:

  • Pentasa tablets and granules are a drug with a similar composition, produced in Switzerland;
  • "Budenofalk" is a drug from Germany, produced in the form of capsules;
  • "Mesakol" - inexpensive tablets with similar pharmacological effects, produced in Belarus;
  • drug "Mesalazole" - suppositories for rectal use, produced in Moldova;
  • Medicine "Remicade" - powder for intravenous administration, used in the treatment of similar diseases;
  • "Asacol" is available in tablet form.

"Pentasa", "Asakol", "Mesakol" or "Salofalk" - which is better? This question often worries patients suffering from the ailments described above. To answer this, let’s look at some analogues in more detail.

Medicine "Pentasa"

This medicine is practically no different from the drug we are describing. It is also prescribed for Crohn's disease or ulcerative colitis. They also have the same active ingredient. "Pentasa" is produced similarly - in the form of granules, tablets and rectal suppositories. The only significant difference is that the drug is prohibited from being taken in childhood, as well as in last weeks pregnancy. Unlike Salofalk, its side effects additionally include dry mouth, stomatitis, hair loss and decreased sexual function.

As a rule, reviews about this medicine are positive. Patients note its effectiveness, but write that it can only be taken under strict conditions good doctor, as it greatly affects the functioning of the kidneys and liver. In addition, the cost of the drug is significantly higher than its analogues. Therefore, when choosing between the drugs “Pentasa” or “Salofalk”, users choose the second option. It is almost 2 times cheaper than its analogue.

The drug "Budenofalk"

This medicine is similar pharmachologic effect, but is seriously different in composition. Its main component is budesonide, not mesalazine. Excipients also differ, for example, gelatin and lactose are present. It is usually prescribed for Crohn's disease, if it is not in a severe stage. The drug is produced in the form of dark pink capsules. At the same time, it has significantly fewer contraindications. It can also be used during pregnancy under the strict supervision of the attending physician. A German pharmaceutical company produces the drug Budenofalk. Suppositories, foam and suspensions - it is not available in these forms, so it is only suitable for oral administration.

Candles "Mesakol"

This is the most budget analogue of Salofalk. Its cost is about 1000 rubles. It is available in tablet form and contains the same active ingredient. It is forbidden to take it in childhood, during pregnancy and lactation. In general, Mesakol, released in Belarus, has practically no other differences.

The drug "Remicade"

An effective remedy for dealing with active form Crohn's disease, the drug is called "Remicade" instructions. Reviews confirm that it can quickly reduce inflammation of the gastrointestinal tract. It is available in powder form, which is diluted for intravenous administration. The main active ingredient is infliximab. As a rule, it is prescribed to patients for whom the effect of the drug "Salofalk" was not effective enough.

Tablets "Asacol"

One more good medicine against colitis and Crohn's disease is the drug "Asacol". It comes in the form of round tablets. It can be taken in the early stages of pregnancy, but under the supervision of a doctor. It is acceptable to use the product in childhood if the child is over 2 years old. Side effects and contraindications generally coincide with Salofalk.

Treatment is not complete without the use of antimicrobial drugs large quantity diseases. After all, these remedies help to cope either with the consequences of pathology, or with the cause of the development of the disease - microbes. This group of drugs is very extensive, and Sulfasalazine is one of these drugs, the instructions for use of which are discussed below.

Pharmacological affiliation of the drug

For an antimicrobial to work, its active ingredient must be certain substance, capable of fighting pathogens. The drug "Sulfasalazine" has quite positive reviews in the treatment of a certain group of diseases. IN medical practice This medicine belongs to the group of sulfonamides, which are the first chemotherapeutic drugs capable of fighting microorganisms that cause diseases.

In what form is the drug available?

The medicine "Sulfasalazine" has had quite positive reviews from patients and specialists for more than a decade. This drug is sold in pharmacies in the form of film-coated tablets.

What does the medicine consist of?

The drug "Sulfasalazine" contains one component, after which it is named - sulfasalazine (Sulfasalazinum). This substance belongs to sulfonamides. Other components included in the tablets antimicrobial drug, have only formative functionality, making up the mass of the tablet and its shell in the form of an enteric film.

How does the medicine work?

For the antimicrobial drug "Sulfasalazine", the instructions for use describe the prerequisites for prescribing it in treatment. They are based on the potential effect of the drug in solving certain problems that have arisen against the background of microbial activity. The drug works due to the action of one substance - sulfasalazine. It exhibits maximum activity in the intestines, helping to get rid of pathogens such as gonococci, diplococci, streptococci and coli. In the intestine, the drug goes through two phases of functional activity - in small intestine Sulfasalazine itself is absorbed in an amount of about 30%, the rest of the drug, passing into the large intestine, is metabolized into working components: 5-aminosalicylic acid, which has an anti-inflammatory effect, and sulfaperidine, which blocks the synthesis of folates in microbial cells, which has an antibacterial effect. Metabolites are excreted in feces and urine within 3 days.

For the drug "Sulfasalazine" the indications for use will be as follows:

This dispersion in the activity of the drug is not yet fully understood by specialists, although its positive effect both in the treatment of joints and in the treatment of intestinal problems is obvious from many years of practice.

When should you not take the product?

The antimicrobial drug "Sulfasalazine", like the vast majority of such drugs, has certain contraindications for use. These include:

  • anemia;
  • obvious disturbances in liver function;
  • disorders of the kidneys;
  • hypersensitivity to the components of the drug, including sulfonamides and salicylic acid derivatives;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • blood diseases;
  • porphyria.

This medicine is not prescribed for the treatment of diseases in children. younger age- up to 5 years, since research in this aspect has not been carried out and potential negative reaction child's body on medicinal substance not installed.

The drug should not be taken by pregnant women 6-9 months old, as well as by those who are breastfeeding a newborn. If it is necessary to carry out treatment with Sulfasalazine, then breast-feeding stop, transferring the baby to artificial nutrition.

Patients require maximum attention bronchial asthma and allergies who are prescribed treatment with this drug due to the potential for aggravation of the underlying disease.

How to take the drug?

For the drug "Sulfasalazine", the instructions for use recommend the following treatment regimens.

In therapy ulcerative colitis and granulomatous enteritis, otherwise called Crohn's disease, The treatment algorithm for adults and children over 16 years of age is the same:

  • the first day - use the drug four times in the amount of 0.5 grams per dose, that is, you need to take 2 grams of the drug per day;
  • second day - 1 gram 4 times a day;
  • starting from the third day, you need to take 6 to 8 grams of medicine per day, dividing them into 4 doses.

The exact dose and duration of treatment with this amount of the drug is determined by the attending physician. Once sharp clinical manifestations the diseases will subside, treatment is carried out in a maintenance daily dosage of 1.5-2 g, divided into 4 doses. It should be noted that such maintenance treatment with this drug is not recommended for children whose body weight is less than 65 kilograms. For adults, the duration of therapy is determined by the doctor, and it can last several months. For children under 16 years of age, the maximum daily dose, divided into 4 doses, is only 2 grams.

This drug can also be used in the treatment of rheumatoid arthritis, including juvenile arthritis. It is prescribed by the attending physician according to this algorithm. Adults and children over 16 years of age take the medicine at a dosage of 500 mg per day in the first week of treatment, in the second week 1000 mg per day, in the third - 1500 mg per day. Recommended daily amount The drug is divided into two or three servings. In some cases maximum amount daily dose may be 3 grams. Treatment in this case is a course of treatment, which can last more than six months, as determined by a specialist.

If it is necessary for a child to undergo Sulfasalazine therapy, the following recommendations should be taken into account:

  • children weighing more than 29 kilograms aged 6 to 8 years can take 1 tablet of the drug 2 times a day;
  • if the child’s weight is no more than 39 kilograms, and this is age from 8 to 12 years, then daily dosage makes 3 tablets - 1 in the morning, at lunch and in the evening;
  • if the body weight of a child 12-16 years old is in the range of 40-45 kilograms, then treatment is carried out either 1 tablet 3 times a day, or 2 tablets in 2 doses per day, the decision remains with the doctor.

In some cases, treatment with Sulfasalazine is indicated for ankylosing spondylitis. This occurs when therapy with non-steroidal anti-inflammatory drugs is ineffective and hormonal agents. Then this antibiotic becomes the basis of treatment, as it inhibits the processes of joint inflammation. This therapy is very long - from 3-6 months until the patient’s condition significantly improves. In this case, when the maximum daily dose of the drug is reached, the other drugs are first discontinued. medicines, and then there is a gradual withdrawal of Sulfasalazine. It should be remembered that this drug is not able to cure the disease itself, it only helps fight inflammatory manifestations in the joints, improving the patient’s quality of life, and therefore traditional therapy should be continued after 2-3 months.

In any treatment, Sulfasalazine tablets are taken immediately after meals with water.

Possible side effects

Like almost any other antimicrobial drug, Sulfasalazine has side effects. These include:

  • agranulocytosis;
  • anaphylactic shock;
  • hemolytic anemia;
  • anorexia;
  • ataxia;
  • transient infertility;
  • epigastric pain;
  • hallucinations;
  • hepatitis;
  • headache;
  • dizziness;
  • diarrhea;
  • jaundice skin, sclera, urine;
  • leukopenia;
  • fever;
  • flatulence;
  • kidney dysfunction;
  • sleep disorders;
  • peripheral neuropathy;
  • interstitial nephritis;
  • oligospermia is transient;
  • pancreatitis;
  • interstitial pneumonitis;
  • vomit;
  • Stevens-Johnson syndrome;
  • convulsions;
  • rash;
  • nausea;
  • thrombocytopenia;
  • fatigue;
  • photosensitivity;
  • noise in ears.

There is no specific antidote to this drug, so if necessary, treatment is symptomatic.

Drug overdose

One of antimicrobials, in demand in the treatment of diseases of the joints and gastrointestinal tract - "Sulfasalazine". Its use must be prescribed by a specialist and carried out in strict accordance with the dosage and regimen chosen by the attending physician.

In case of overdose or poisoning with this medicine, abdominal pain, dizziness, nausea, and vomiting occur. The patient needs health care, consisting of gastric lavage and forced diuresis. Specific symptomatic therapy is also necessary.

Possible joint treatment

In some cases, the drug "Sulfasalazine" is indicated for rheumatoid arthritis. The patient and the doctor prescribing it for use should remember that it enhances the effect of immunosuppressants, hepato- and nephrotoxic drugs, as well as cytostatics. "Sulfasalazine" inhibits the absorption of digoxin and folic acid, but enhances functional activity anticoagulants, anticonvulsants and oral hypoglycemic drugs.

Some treatment features

Sulfasalazine is widely used in the treatment of joint diseases. Its analogues, like the drug itself, require the use of large amounts of water during the course of treatment. But alcohol, despite the absence of a strict prohibition, should not be taken, as it is very potential danger serious liver damage.

What do they say about the drug?

Antimicrobial tablets "Sulfasalazine" reviews are mostly quite positive. Experts note the effective effect of the drug in the treatment of certain diseases, and patients note that the drug helped them get rid of painful sensations. The only drawback of the medicine, which many of those who took these pills talk about, is the frequent manifestation of dyspeptic symptoms - abdominal pain, flatulence, diarrhea. But the quality of treatment compensates for these side effects, notes the majority who left reviews about Sulfasalazine.

Are there any analogues?

For the antimicrobial drug "Sulfasalazine", analogues may contain both the same active substance, and its derivatives, for example, mesalazine. The synonym for the drug is “Salazopyrine”, but its analogues are “Pentasa”, “Asacol”, “Samezil”, “Mesakol” or the generic “Mesalazine”. For the drug "Sulfasalazine", the instructions for use indicate the dosage active component contained in tablets. The same applies to analogues. The specialist treating the patient will decide which specific drug to choose.

Antimicrobial drugs help solve many problems caused by pathogenic inhabitants of the microworld. One of them is Sulfasalazine. The instructions for its use contain all the information necessary for the doctor and the patient, and therefore must be read carefully. Following the recommendations of the instructions and the attending physician will help provide adequate and high-quality treatment for the existing problem.

Nonspecific ulcerative colitis is relatively rare disease. Nonspecific ulcerative colitis is a diffuse inflammation of the colon mucosa, initiated in the rectum and spreading proximally. The disease has a chronic undulating course with alternating exacerbations and remissions. However, over the past ten years there has been an increase in its incidence among both adults and children. At the same time, attention is drawn to the fact that the disease has become much younger and occurs already from 2 years of age. According to I.A. Bodnya (1986), of all cases, 0.9-12% are children aged 0 to 17 years. The prevalence of this disease among the European population is 5.8-14 per 100,000 population, in Russia 1-4.7 per 100,000, in Russian children 3.4 per 100,000 child population.

Regions characterized by high frequency ulcerative colitis include the UK, USA, Northern Europe, Australia. Low incidence is observed in Asia, Japan, and South America.

Ulcerative colitis is characterized by the presence of changes in chromosomes 6 and 12. The disease is also associated with the II.-1ra gene. Concordance for the proband with ulcerative colitis is 6.3% versus 58.3% with Crohn's disease.

This paper presents the results of a study of the clinical activity of drugs of two groups that were used in children and adolescents in the treatment of ulcerative colitis (UC) during exacerbation and subremission. We took two basic ones from the entire range of drugs used by pediatricians and gastroenterologists for the treatment of UC: sulfasalazine and mesalazine (mesacol).

The best known is sulfasalazine, which is used in children from 5 years of age at a dose of 50-80 mg. For 1 kg. body weight per day. This drug is not intended for rectal administration. When taken orally, a third of patients develop side effects associated with its constituent sulfapyridine. Side effects: headache, dizziness, dyspeptic symptoms: nausea, vomiting, diarrhea, abdominal pain, anorexia; admixture of blood in feces, necrotizing ulcerative colitis, interstitial pneumonitis, drug-induced hepatitis, agranulocytosis, leukopenia, thrombocytopenia, hemolytic anemia, photosensitivity of the skin, orange-yellow coloration of urine, allergic reactions: Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock.

Mesacol- a drug of the mesalazine group, practically devoid of side effects, “pure” 5-aminosalicylic acid. For delivery to the colon, it uses other transport systems without sulfapyridine. Mesacol is coated with Eudragit S. disintegrating at pH 7.0 or higher, salofalk is Eudragit I. dissolving at pH-6.0, pentaka is slowly released even earlier at pH below 6.0. Accordingly, any of these drugs can be used in the treatment of ulcerative colitis, but distal release Mesacol is much preferable.

Mesacol is prescribed from 2 years of age at a dose of 20-50 mg. per 1 kg of body weight per day. Moreover, mesacol is also used rectally in suppositories and enemas. According to many leading clinics, rectal forms of mesalazine (mesacol) have advantages over glucocorticoids (Kanshin O.A., Kanshin N.N. 2000).

It has been established that the tablets leave the stomach unchanged and their dissolution begins in the small intestine 120-180 minutes after administration, 170-230 minutes. The tablets dissolve completely. This process is not affected by changes in the pH of the environment caused by food or other drugs.

The release of mesacol occurs in the terminal section small intestine and in the large intestine. In tablets, the active substance (mesalazine) is protected by a coating that is resistant to gastric juice. Dosage form is manufactured in such a way that mesalazine begins to be slowly released only in the terminal part of the small intestine and in the colon.

Due to the relatively low degree of absorption of mesalazine and its rapid conversion to N-acetyl-5-ASA already in the intestinal mucosa, the concentration of mesalazine in the blood plasma remains relatively small; after a single dose of mesacol at a dose of 240 mg, the concentration of mesalazine is 0.5-1.5 mcg/ml. Plasma protein binding of mesalazine is 43%, N-acetyl-5-ASA - 75-83%. IN breast milk 0.1% mesalazine is supplied (in the form of N-acetyl-5-ASA).

In the intestinal mucosa and liver, mesalazine is metabolized to N-acetyl-5-ASA. T1/2 of mesalazine is 0.5-2 hours, depending on the dose taken, clearance is 300 ml/min. Mesalazine is excreted by the kidneys, mainly in the acetylated form.

The number of observed patients was 18, aged from 2 to 19 years. There were 11 men, 7 women. All patients were diagnosed with mild UC - 4, moderate - 13 and 1 severe. 7 patients had left-sided lesions of the colon, 10 had distal lesions in the form of proctosigmoiditis, and 1 had subtotal lesions of the colon.

The patients were divided into 2 groups: group 1 received sulfasalazine, and group 2 received mesacol. Both drugs were prescribed at a therapeutic dose. Treatment was carried out for 1 month.

The criteria for assessing the effectiveness of drugs and their tolerability were: the dynamics of the main clinical symptoms, data laboratory research(total blood, urine, feces (coprogram), biochemical blood parameters, endoscopic data (RRS and colonoscopy).

As a result of therapy with two drugs in two groups, we noted the onset of clinical and endoscopic remission of UC in the 1st group 1 (11.1%) people, in the 2nd group 6 (66.6%) patients, which we assessed as as an excellent effect, in 4 (44.4%) in the 1st group and in the 2nd 5 (55.5%) people, clinical remission was noted in the presence of a minimal degree of activity of the process according to the endoscopic picture - good effect and in 2 (11.1%) in the 1st group, 0 patients in the 2nd group, a satisfactory effect was noted when the process subsided according to clinical and endoscopic data.

Clinical symptoms of UC before and after treatment with sulfasalazine and mesacol

Symptoms

Before treatment

Treatment
sulfasalazine

Treatment
mesacol

Stool frequency
1-3
3-5
Stool consistency
Decorated
Mushy 38,8 11,2
Liquid
False urges
1-3
4-6
Blood in stool
Mucus in stool
Stomach ache
Fever
Anemia iron deficiency.

Studies have shown a visible advantage of mesacol. The drug is well tolerated. Mesacol is effective for mild, moderate and severe forms of UC. Oral intake mesacola effectively induces and maintains remission in mild and moderate activity UC and can be successfully used as a basic therapy for UC. In case of a moderate course of the process, the initial dose of mesacol should be no lower than 40-50 mg per 1 kg of body weight. In group 1 (sulfasalazine was used), side effects were noted in the form of headache in 5 patients, nausea in 7 patients, increased indirect bilirubin in 3 patients, leukopenia in 2 patients and allergic pinpoint rash in 1 patient.

Benefits of mesacol:

  • GMP quality;
  • Possibility of appointment from 2 years;
  • wide popularity of the active substance;
  • proven effectiveness;
  • anti-inflammatory effect specifically in the intestines;
  • minimalization side effects(eg in comparison with sulfasalazine);
  • does not change skin color (compared to sulfasalazine);
  • not noted negative influence on reproductive function in men (unlike sulfasalazine).

Conclusions: we believe that in pediatric practice the use of mesacol is a priority and much more effective, the effect of the drug is less toxic and it can be prescribed from the age of two, which is at this moment necessary due to the development of the disease at an earlier age.

Children's Gastroenterology Center. (Head, doctor of higher education qualification category V.L. Zemlyakov)