Mesacol

Anti-inflammatory treatment for intestinal diseases, produced by Krka, Novo place (Slovenia), known in the international register of pharmacological preparations called mesalazine, on the shelves of our pharmacies can be found as Samesil. It is this medication that will be discussed in this article. Its pharmacological characteristics, indications and contraindications to use, as well as the method of administration and recommended dosages will be considered.

Diseases of a proctological nature not only bring many unpleasant hours and days, but sometimes even months. After all, somehow the problems associated with the intestines - the small and large intestines - drive many people into the paint. They are ashamed to go to the clinic with their problems. And as a result, when the "early" or took first aid, the proctologist has to solve much more complicated tasks, removing the patient from a serious condition. Sometimes the patient can not always return to his former health. Solving many problems of proctological nature allows Samesil - a convenient modern anti-inflammatory drug, specially developed for the relief of intestinal diseases. Therefore, for the treatment to be easier and without complications, a qualified specialist should be consulted already when the unpleasant symptomatology has just appeared, then the result can be expected to be fast and favorable. You should not only engage in self-diagnosis and prescription of medications. This approach to treatment will lead to nothing good. In this case, the situation will only worsen, and time will be lost.

[1], [2]

Indications Mesacol

Due to its medicinal properties and the form of release, the indications for Samezil administration are reduced to such diseases:

1. Therapy and preventive treatment of ulcerative colitis.
2. Pathological changes of ulcerative nature, affecting the intestinal mucosa with a lesion of the rectum (ulceration proctitis).
3. Crohn's disease.
4. Nonspecific ulcerative colitis, accompanied by damage to the distal parts of the large intestine and rectum.

[3], [4]

Release form

Depending on the characteristics of the intestinal mucosa lesion and its accompanying pathologies, the form of release of the drug in question is somewhat different.

1. Samesel is available in the form of tablets, which are covered with a special shell that can dissolve only in the intestines, which makes it possible to "deliver" the medicine directly to the pathologically affected area. The tablet form of the drug is released by the concentration of the active active substance mesalazine (5-ASA) 400 mg or 800 mg. The skin of the drug has a brownish - reddish tinge, which allows the inclusion. Samesil itself is represented by a light gray mass. Auxiliary chemical compounds that support the high level of pharmacodynamics Samedil: sodium carboxymethyl, sodium lauryl sulfate, macrogol 6000, povidone, talc, starch, magnesium stearate, methacrylic acid copolymer, maltodextrin, triethyl acetate, sodium hydroxide, titanium dioxide. Tablets have a prolonged action.
2. The second type of release is the rectal suppository, which has a greyish-cream shade. The dosage of one unit of the drug is 500 mg of mesalazine (5-ASA). An accompanying substance is a solid fat.
3. Another form of the drug can be called a rectal suspension. This is a homogeneous creamy liquid, in 1 ml of which is 40 mg of mesalazine (5-ASA). The concomitant chemical compounds of this release form are: sodium edetate, sodium metabisulphite, tragacanth, distilled water, sodium benzoate, sodium acetate, xanthan gum. Samesel is packaged in seven containers that have a volume of 50 ml (2 g mesalazine) or 100 ml (4 g mesalazine). Together with the drug in the carton packs and applicator.

Pharmacodynamics

The drug in question is classified as an anti-inflammatory drug, showing its activity directly in the intestines of the patient, acting directly on the inflammatory mediators. Pharmacodynamics Samesil is due to the inhibition of the effectiveness of cyclooxygenase and neutrophilic lipoxygenase, as well as a reduction in the formation and development of leukotrienes and prostaglandins.

When the drug is injected, inhibition of motor activity, the destruction process of mast cell granules, as well as phagocytosis of neutrophils, is manifested by active capture and absorption of this form of leukocytes in the blood. Samesel effectively inhibits the secretion of Ig lymphocytes.

The drug in question has antibacterial characteristics that effectively cope with intestinal sticks and certain types of cocci that can be invaded in the large intestine. Due to the fact that mesalazine freely combines with free oxygen radicals (O ⁺² ) and leads to its destruction, Samesil shows high antioxidant characteristics.

Samesyl is well tolerated to the patient's organisms. Its administration reduces the likelihood of recurrence of the disease in Crohn's disease, especially in patients with ileitis (a nonspecific inflammatory disease affecting the ileum), as well as a prolonged course of the disease.

[5], [6]

Pharmacokinetics

Any form of the drug in question makes it possible to "deliver" the therapeutic volumes of mesalazine directly to the site of the pathology. Namely, these are the mucous layers of the rectum and sigmoid colon, the descending colon, up to the splenic zone.

Pharmacokinetics Samesil shows an average level of absorption. About a third - half of the drug is adsorbed to the intestinal mucosa, namely in the small intestine. Metabolites of mesalazine is N-acetyl-5-aminosalicylic acid.

The active substance undergoes acetylation (replacement of hydrogen atoms in organic compounds with an acetic acid residue), which occurs in the mucous layers of the intestine and liver.

The level of binding ability of N-acetyl-5-aminosalicylic acid with protein components of blood plasma corresponds to 85%, whereas mesalazine shows a relationship of only 43%.

Active active substance Samesila not only is able to pass through the blood-brain barrier, but is firmly established in breast milk during breast-feeding.

The given medicine is disposed of from the patient's organism, as in the majority, unchanged, and in the form of metabolites and with urine, and together with the calves.

The half-life of mesalazine (T _1/2 ) is determined by the figure from half an hour to an hour and a half, it all depends on the individual characteristics of the human body. The same parameter for the metabolite of N-acetyl-5-aminosalicylate is somewhat larger and ranges from five to ten hours.

[7], [8], [9]

Dosing and administration

The choice of dosage form is determined by the localization and scale of the affected area of the intestine. Only the attending physician can determine the form of administration, the way of administration and the dose of the prescribed drug. When used in the therapeutic therapy of Samesil in the form of a rectal suspension, the doctor can in parallel administer the administration of this drug in the form of tablets. Naturally, in this situation it is necessary to take into account the total amount of the drug delivered to the body of the patient. If this fact is not taken into account, the dosage is exceeded, which invariably leads to an overdose of mesalazine and an increase in the likelihood of toxic effects on kidney function.

The therapeutical dosage the doctor appoints individually individually to each patient, based on the clinical picture of the disease and its general health. If the therapeutic effectiveness is not observed during a month of drug therapy, it should be replaced by its analogue.

During the treatment, it is necessary to conduct the required hydration. If medical necessity arose, mesalazine may be taken concomitantly with metronidazole or preparations belonging to the group of corticosteroids.

Children, whose body weight has already reached 40 kg and adult patients, Samesil in the form of a rectal suspension, to achieve the expected efficacy, it is recommended to enter the patient immediately after evacuation of the intestine - eat after the defecation process.

1. To make it more convenient to conduct the procedure, the patient should lie on his left side and slightly bend his legs.
2. Before use, the vial of the medicated fluid should be shaken well, after which the applicator is inserted into the anus as far as possible.
3. Very carefully and slowly to squeeze out the suspension from the tube.
4. After the administration of the drug, it is necessary to lie down for half an hour, without changing the previously adopted position.
5. After the time has elapsed, make a few turns on the right side and back. This is necessary for better distribution of mesalazine in the gut.

The recommended dosage, for example, during the acute phase of ulcerative colitis is the administration of 100 ml of Samesil with an active substance concentration of 4 g per 100 ml, taken once a day. This form of admission is most effective if the administration occurs in the evening, just before going to bed.

If the patient, for some reason, is hard to keep the "large" amount of medicine in the gut, in such a situation it may be advisable to spread the dose in two 50 ml procedures. In this case, packing in 50 ml and active substance content of 2 g will be more convenient in application. The time of entry, with such a schedule, pharmacists recommend: the first procedure - just before bed, the second - preferably at night, after preliminary defecation.

The duration of the treatment course is preferably six to eight weeks.

As a preventive measure for relapsing ulcerative colitis, physicians recommend using a dosage of 50 ml (concentration of active ingredient 2 g), once during the day. The procedure and in this case it is desirable to do after evacuation of the intestine and at night. This approach to treatment is more effective, since the drug works on the affected area overnight.

The duration of preventive treatment is also six to eight weeks.

To small patients, whose weight has not yet reached 40 kg, the amount of Samesil is prescribed by the treating doctor, based on the activity of the inflammatory process and the place of its progression, as well as on the basis of the body weight of the baby.

 In case of diagnosing the acute form of ulcerative lesions of the intestinal mucosa, as well as Crohn's disease, the recommended amount of mesalazine is calculated according to the formula 30-50 mg per kilogram of the child's weight, divided into three procedures.

To prevent recurrence of the disease, this therapeutic dosage corresponds to the values of 15 to 30 mg per kilogram of the weight of the baby, separated by two or three procedures.

The method of carrying out the treatment procedure is similar to what was previously prescribed. As a rule, therapy of pathology during an exacerbation takes from eight to twelve weeks (two to three months).

Samesil in tablets is predominantly prescribed by the attending physician if distal proctosigmoiditis or proctitis is diagnosed.

If there is an exacerbation of the disease, the recommended dose is 0.4-0.8 g, taken three times throughout the day. The duration of the treatment course is usually eight to twelve weeks.

As a preventive measure to prevent recurrence of the disease, a slightly smaller dose is prescribed - 0.4-0.5 g three times a day (in the case of ulcerative colitis) or 1 g four times during the day (in case of Crohn's disease).

For small patients who are already two years old, the daily amount of the drug is calculated by the formula 20 - 30 mg per kilogram of the weight of the baby, which is divided into several receptions. Such graphite therapy can be maintained for several years. If the disease is severe, accompanied by complications, the daily amount of medication administered can be increased to a level of 3 to 4 g. But these numerical values should not be exceeded. Also, the maximum dosage should not be taken more than 8 - 12 weeks.

The tableted form of Samesel is administered orally, wholly, without chewing. The recommended time of entry is after eating with a large volume of water, or an hour before the proposed meal.

Samesil in the form of rectal suppositories (suppositories) is prescribed by 0.5 g (one suppository) three times a day - for adult patients. For children, the daily intake of the rectal suppository is calculated from the calculation: in the case of the acute phase of the disease as 40-60 mg per kilogram of the baby's weight, in the case of preventive measures, the daily amount of the drug is 20-30 mg per kilogram of the child's weight.

Against the backdrop of drug therapy, mesalazine should be constantly monitored the main characteristics of the blood, conducting a general analysis of it. Urine parameters, which are a characteristic of the kidneys, are regularly monitored.

If one of the techniques was missed, it is necessary to conduct the procedure at any convenient time, in case it does not work, then the missed amount is administered to the patient together with the next dose. If more than one dosage has not been taken, the medication should be continued on schedule, but it is absolutely necessary to consult your doctor.

In the event that a specialist begins to suspect that the patient develops acute intolerance to mesalazine, he cancels Samesil.

[15], [16], [17]

Use Mesacol during pregnancy

No matter how safe Samezil was considered, it is a medicine, and it is for its intended purpose to influence the human body. And this effect is not always directed. Therefore, referring to the peculiarities of the pharmacodynamics of the medicine in question, physicians believe that the use of Samesil during pregnancy is permissible only for irrefutable and obvious medical indicators for the female body. Only in this case, the specialist with special care can appoint Samesil, while constantly keeping the condition of the patient and her fetus under control.

It is advisable not to allow the medication to be administered early in the development of the embryo, this input is not permissible even in the last four weeks before childbirth, when the baby's body is already fully formed, but the use of mesalazine can provoke or exacerbate jaundice in a newborn baby. This is due to the fact that active substance Samesila is able to overcome the placental barrier. But since there are not enough results of the study of the consequences of taking the drug in question, it is difficult to assess possible side effects for the woman's organism and her unborn child.

In the light of the fact that mesalazine freely penetrates into breast milk, if it is necessary to carry out therapeutic treatment, it is necessary to raise the issue of stopping the feeding of the newborn with mother's milk, and transfer it to artificial feeding.

Contraindications

If a substance has an active effect on the human body, which in principle is required from an effective medicinal product, it is these pharmacological features that lead to the fact that the limitations to reception are determined. There are also contraindications to the use of Samezil, which are reduced to the following pathological changes:

• Increased individual intolerance of the patient's organism to the active substance and / or other components of the drug, including propylparabenam and methylparaben.
• Lack of glucose-6-phosphate dehydrogenase in the patient's body.
• Hypersensitivity of the mucosa to the procedure of enemation, when using the release form in the form of a suspension.
• Severe form of hepatic and / or renal dysfunction, available in a patient's history.
• Hemorrhagic diathesis.
• Ulcerous and erosive pathology, affecting the mucous membrane of the duodenum and stomach.
• Pregnancy, especially the first and last weeks of gestation.
• The period of feeding a newborn baby with breast milk.
• Children who have not yet reached the age of two.
• Rectal suspension is not recommended for use in patients with a history of bronchial asthma.

Regarding the influence of Samesil on the ability of an adequate reaction in the management of a vehicle patient or other potentially dangerous mechanisms, to date, no data are available.

[10], [11]

Side effects Mesacol

Advantageously, most drugs can cause accompanying pathological symptoms, which manifests itself with more or less intensity. The drug is considered quite well tolerated to the patient's organisms, but Samesil's side effects are nevertheless stipulated in the instructions attached to it.

• Increased fatigue rights.
• Puffiness.
• Vomiting.
• There may be pain symptoms in the throat, abdomen, as well as headaches.
• Exacerbation of asthma.
• The growth of body temperature.
• Symptoms of an allergic nature:
• Skin rashes.
• Itching sensation.
• Manifestations of lupus erythematosus.
• Burning.
• Dermatosis.
• Rarely, eosinophilic or interstitial pneumonia is rare.
• Sinusitis.
• Tachycardia.
• Very rarely, myocarditis or pericarditis.
• Vasodilatation - an increase in the lumen of the blood vessels, due to a decrease in muscle tone of the vascular wall.
• Symptoms of flatulence.
• Impairment or vice versa activation of appetite.
• Diarrhea.
• One can observe:
  • Increased hair loss on the head.
  • Hepatitis.
  • Exacerbation of pancreatitis, gastritis, cholecystitis or gastroenteritis.
  • Dryness of the skin, dry mouth, ulceration possible.
  • Urelic erythema (inflammation of the vessels of the skin and subcutaneous fat).
  • Manifestations of psoriasis and gangrenous pyoderma.
  • Dysuria is a violation of urination.
  • Tinnitus.
  • Multiple manifestations affecting the urinary system.
  • Ulcerative manifestations.
  • Exacerbation of kidney pathology.
  • Change in taste.
  • Appearance of shortness of breath.
  • Visual impairment.
  • Dizziness.
• Sharp mood changes.
• Unstable psychological level of the patient.
• Exacerbation of arthrosis manifestations.
• Change in blood pressure both in the direction of decrease, that and in the direction of its increase.
• Thrombocytopenia of leukopenia and lymphadenopathy.

Most of the above symptomatology is manifested in single cases and it is sufficient to reduce the dosage of Samesil so that the side symptoms disappear on their own. It is very rare cases when the treating physician has to completely remove this medication from the treatment protocol and introduce symptomatic therapy.

[12], [13], [14]

Overdose

The main amount of the drug is absorbed in the intestine, and only a small amount of it "seeps" into the blood. Therefore, there is a very small chance that an overdose of mesalazine will occur, causing an intoxication of the patient's body. But in view of the fact that the organism of each person is individual, nevertheless we will give the symptoms of overdose, which show salicylates at large dosages of intake, to which the given drug belongs:

1. Shortness of breath, respiratory depression, increase in the frequency of contraction of the diaphragm.
2. Strengthening of the sweat glands.
3. Redness of the skin.
4. Loss of consciousness.
5. The increased ventilation of lungs provokes the growth of respiratory alkalosis (imbalance of acid and alkali equilibrium), which, in turn, is transformed into metabolic acidosis (accumulation of endogenous acids in the tissues of the body).

If nevertheless it happened that signs of intoxication begin to appear, the treating doctor usually prescribes intravenous administration of electrolytic solutions, for example, such as sodium lactate or sodium bicarbonate. This will increase the diuresis (the amount of urine allocated for a certain period of time). Thanks to such correction, it is possible to increase the alkaline reserves of the patient's organism and improve the situation with excretion of components and metabolites of Samesil by the kidneys, together with urine.

To the therapeutic measures can be connected and hemodialysis. Specially developed antipode for the relief of this situation today does not exist.

Interactions with other drugs

The human body is a fragile vessel, to break the state of which is not very difficult. Therefore, when assigning any medication, especially in combination with other chemical compounds, it is necessary to clearly imagine what consequences can be expected from the joint administration of preparations of different pharmacological groups. The interaction of Samesil with other drugs has not been thoroughly studied, but certain recommendations on this issue can still be given.

Mesalazine, when administered together with drugs that are derivatives of sulfonylureas, enhance their characteristics, causing a decrease in blood sugar (glycemia). In this case, mesalazine encourages the toxicity of methotrexate.

Samesel provokes the development of ulcerogenicity in drugs belonging to the pharmacological group of glucocorticosteroids (GCS). The side symptomatology of taking this tandem is the formation of defects in the mucous membrane of the gastrointestinal tract. In case the patient has a history of ulcerative lesions of the mucosa, then there is a recurrence of the already existing ulcerative disease.

When working with diuretics (diuretics), for example, furosemide, spironolactone (potassium - and magnesium-saving diuretic), the work of diuretics is inhibited. The same is the result of the joint administration of Samesil with rifampicin, which belongs to the pharmacological group of antibiotics. Antibiotics lose their pharmacodynamic characteristics.

Mesalazine weakens the activity of sulfonamides , whereas the characteristics of anticoagulants, on the contrary, increase . The drug in question inhibits the ability of cyanocobalamin to be absorbed. With the simultaneous administration of active active substance Samesil and uricosuric medicines, there is an increase in renal clearance of the active metabolite of oxypurinol, and the blocking of tubular secretion is enhanced.

[18], [19], [20], [21], [22]

Storage conditions

Depending on how well the medicine is stored, its high pharmacological efficiency depends on the extent of the means considered in this article by the manufacturer. The storage conditions of Samesil, detailed in the instructions accompanying the drug, are not complex, but their clear keeping is simply necessary.

1. Samedil, produced in the form of tablets, must be kept throughout the period of permissible use in a cool place, where the room temperature does not exceed + 30 degrees.
2. Samedil, which is released in the form of a rectal suppository or rectal suspension, should be kept throughout the period of permissible use in a cool place, where the temperature values do not exceed + 25 degrees.
3. Keep mesalazine in a place inaccessible to small children.
4. The medicine should not be exposed to direct sunlight, it reduces its shelf life and reduces the quality of the drug itself.

[23]

Shelf life

By issuing any medicine to pharmacy counters, the manufacturer company must indicate the date of production and the final number on the package of the drug, after which the drug should not be used for therapeutic and preventive therapy. Since further the drug begins to lose its pharmacological characteristics, and, therefore, it is not necessary to expect high medication effectiveness from such a drug.

The period of expected effective work of Samesil differs depending on the form of its release:

• Shelf life of tablets covered with a dissolution in the intestine of the shell is three years;
• Samedil in the form of rectal suspension is suitable for use for two years after release;
• The medication in the form of rectal suppositories shows high efficacy within three years after the production date.

[24]