Salofalk

Salofalk is a drug belonging to a group of drugs that have anti-inflammatory and antimicrobial properties. It finds its application mainly in terms of treatment of ulcerative colitis, as well as Crohn's disease.

The impact of Salofalk on the human body is the local decrease in the intensity of inflammatory processes in the intestine. Such a beneficial therapeutic effect is reached due to the fact that the drug acts as an inhibitor against neutrophil lipoxygenase, and also helps to reduce the degree of activity with which leukotrienes and prostaglandins are synthesized. In addition, slows down the processes of neutrophil degranulation, migration and phagocytosis, and lymphocyte secretion of immunoglobulins.

In addition, Salofalk produces a pronounced antioxidant effect. This is due to the fact that by binding free oxygen radicals, the drug causes destruction of them. Mesalazine being the main component of this medication when it is taken orally, actualizes its effect in the intestinal mucosa, and also affects the submucosa, producing an effect from the intestinal lumen. Because of this, the availability of mesalazine in the area where inflammation is localized is very important.

In no small part contributes to ensuring the beginning of the action of the main active substance in precisely those areas of the body, where necessary, the fact that Salofalk-shaped granules show greater resistance to the effects of gastric juice. Granules also possess a matrix structure, which is provided with a delayed release of mesalazine to the corresponding necessary time interval.

Indications Salofalk

Indications for use Salofalk means the use of its various dosage forms depending on certain clinical cases of diseases and disorders of the functioning of the body.

So the drug is included in the list of appointments of medical measures for ulcerative colitis of nonspecific type in its distal forms. In this case, for the treatment, as well as for preventive purposes, to prevent exacerbation, it is advisable to use rectal suppositories.

Suspension rectal Salofalk is indicated in those cases if there is an exacerbation of ulcerative colitis, when the left colon and rectum are involved in pathological processes.

Tablets are the most justified dosage form of the drug for ulcerative colitis. As another case involving the use of Salofalk in this form it is necessary to mention Crohn's disease. This medication is intended for both prevention and treatment of exacerbations.

Ulcerative colitis of mild to moderate severity during the exacerbation phase requires the use of granules. They are also used in long-term therapeutic courses for ulcerative colitis, and in addition, with their help, this disease is maintained in a state of remission.

When there is an exacerbation of ulcerative colitis of the distal form in light and moderate severity, resort to the use of Salofalk in the form of a foam. In addition, this dosage form promotes the remission of distal ulcerative colitis by prolonged therapy.

Thus, the indications for the use of Salofalk are determined by a number of factors, among which the most significant are the localization and the magnitude of the lesion area occurring in the intestine. Based on this, a medical prescription is made to use the drug dosage form most applicable to the clinical picture of the disease in each specific case.

[1]

Release form

The form of release Salofalk differs quite a large variety: from tablets for oral administration, to medicines that are used rectally - suppositories and suspensions. The preparation is also presented in the form of a foam.

The most commonly used with nonspecific ulcerative colitis in common forms of it - total and subtotal, tablets are used. They have a round, convex form on both sides, the color is light yellow, which can vary in the range to light brown. The main constituent component - mesalazine 5-ASA may be present in the total amount of either 250 mg or 500 mg. It should be noted that the 500-milligram content of mesalazine tablets differ in oval form.

In both cases, there are a number of auxiliary substances in the formulation: butyl methacrylate, glycine, hypromelose, titanium dioxide, sodium carbonate, colloidal silicon dioxide, calcium stearate, talc, microcrystalline cellulose, iron oxide of yellow oxide.

Tablets are packed in blisters of 10 pcs. Blisters in a cardboard box, where they are placed together with the instructions for use can be 5 or 10 respectively.

Salofalk in the form of granules has a soluble pH-dependent shell Eudrajit L, which is why the release of the main active substance is slowed, which is due to this precisely at the desired destination. Granules of a white-gray hue have a rounded spherical or cylindrical shape. The content of mesalazine 5-ASA in granules is 500 mg. The inner shell is formed by hypromelose, a copolymer of methacrylic acid and methyl methacrylate, eurajite, triethyl cyrate, talc, magnesium stearate, titanium dioxide. In the outer shell there is the presence of caramellose sodium, titanium dioxide, aspartame, anhydrous citric acid, povidone K25-5, talc, vanilla flavor. Packages of polyethylene 930 or 1860 mg respectively, laminated with aluminum foil are in cardboard packs.

Rectal Suppositories Salofalk have a color from white to cream shade, they have an elongated shape, pointed on one side and a uniform consistency.

In one suppository contains mesalazine 5-ASA 500 mg. The presence of auxiliary substances is represented by fat solid, cetyl alcohol, sodium diokuzate. Suppositories are packed in blisters of 5 pcs. And placed in a box of cardboard.

Finally, the form of the preparation can be in the form of a foam dosed for rectal administration. It has a white-gray or reddish-violet shade, and has a persistent creamy consistency. Mesalazin 5-ASA in the first application is present in the amount of 1 g. Of the auxiliary substances there is the presence of propylene glycol, sodium disulfite, polysorbate, disodium edetate, cetostearyl alcohol, propellants. 7 doses, which is equal to 14 applications - one cylinder of aluminum lacquered inside, have a device for dosing. For this special 14 pieces are used. PVC applicators with protective caps. Under the used applicators are provided bags of polyethylene - 14 pcs. Packs of cardboard.

[2]

Pharmacodynamics

Pharmacodynamics Salofalk is characterized primarily by the anti-inflammatory effect of the drug. As a result of ingestion, the processes of synthesis of prostaglandins, which are metabolites of arachidonic acid, are inhibited. In the role of an inhibitor, he also speaks about the level of activity of neutrophil lipoxygenase, as well as immunoglobular secretion by lymphocytes. In addition, it causes a slowing of neutrophil migration, degranulation and phagocytosis.

Salofalk promotes the binding and destruction of free oxygen radicals. The main component of the drug - mesalazine is inherent in the ability to trap radicals arising from reactive oxygen compounds. In vitro studies indicate that it can be important in inhibiting lipoxygenase. It is established, in addition, that it affects the extent to which prostaglandins are present in the intestinal mucosa.

What is to be said about the way in which systemic bioavailability is correlated with the concentration in which mesalazine is present in the blood plasma is that this factor does not represent a significant value that is associated with therapeutic efficacy, but is mainly one of the factors that determine the level of safety.

Pharmacodynamics Salofalk is such that taking the drug orally contributes to the actualization of the local effect produced by mesalazine in the intestinal mucosa, which manifests itself from the side of the intestinal lumen. Proceeding from this, the availability of mesalazine in the localization of the inflammatory process seems to be important.

[3], [4], [5], [6], [7], [8], [9]

Pharmacokinetics

Pharmacokinetics Salofalk, as regards the absorption of the drug and its distribution in the body, manifests itself in the following. The release of mesalazine, the main active active ingredient, occurs in the terminal compartment in the large and small intestine.

The beginning of dissolution of Salofalk in the form of tablets in the small intestine occurs after a period of 110 to 170 minutes after they have been ingested. In order for them to completely dissolve after intake takes 165-225 minutes. The rate of dissolution in the most direct way can depend on changes in the acid-base balance of pH due to ingestion or taking other medications.

For the dosage form of the granules, a delay in time of 120-180 min is observed, which precedes the initiation of the release of mesalazine. To achieve in the blood plasma Cmax it is necessary from 4 to 5 hours. After the drug has been taken orally, there is approximately 15-25% systemic bioavailability of mesalazine. When the drug is taken after a meal, the onset of absorption is then delayed by 60-120 minutes, but the rate and extent of absorption remain unchanged.

The small size of the granules - about 1 mm facilitates the rapid transit of them from the stomach into the small intestine. Movement in the large intestine occurs over a total time of approximately 20 hours. At the same time, a thick, sigmoid colon receives about 80% of the dose taken orally.

Mesalazine undergoes metabolism in the intestinal mucosa (a pre-systemic pathway of metabolism), and in addition, the liver undergoes systemic metabolic processes that result in the formation of inactive pharmacologically N-acetyl-5-aminosalicylic acid. Acetylation has a character that does not depend on which acetylating phenotype in the patient, and may be related to the action of the bacterial microflora produced in the colon.

When mesalazine enters the body three times a day at a dose of 500 mg with a saturating concentration, approximately 25% of it, together with N-acetyl-5-aminosalicylic acid, is eliminated by the kidneys. The part of mesalazine that is not metabolised, in the amount of no more than 1% of the dose that was taken orally, is excreted. In this case, T1 / 2 is, as studies show, 4.4 h.

Pharmacokinetics Salofalk, when he was appointed for a single dose of 20 mg / kg in children aged about 6 to 16 years, was similar to pharmacokinetic features in adult patients. With regard to elderly patients, the pharmacokinetics of the drug have not been studied.

[10], [11], [12]

Dosing and administration

The method of administration and dosage of the drug, as well as its most appropriate dosage form, is selected on the basis of the localization and the area of the intestine that is affected.

In cases of common forms of diseases, as a rule, Salofalk is administered in tablets. In the case of distal forms, proctosigmoiditis, the proctitis is justified for use as a rectal medication.

The mode of taking tablets by adult patients provides a dose of 500 mg three times a day. Severe forms of diseases can cause the need to increase the dosage to 3-4 g per day in courses over a period of 8 to 12 weeks.

For children with a body weight not reaching 40 kg daily dose should be half that of adults, respectively - three times a day for 250 mg. Children with a body weight greater than 40 kg - 500 mg each.

As a preventive measure to avoid the possibility of relapse should be taken 3 times during the day for 250 mg of the drug. Such a policy course can have a length, if necessary - for several years.

Salofalk in the dosage form of granules is generally prescribed in the amount of 1-bag with a content of 500 to 100 mg of mesalazine for three doses during the day. Or 3 bags at a time, once a day, which is 1.5-3.0 grams. Children with a body weight of up to 40 kg should take a half dose of the drug, if the body weight of the child is more than 40 kg - Salofalk is prescribed in dosage as an adult.

Tablets and granules are taken orally, after eating, without chewing, and using for drinking a large amount of water.

Rectal suppositories of Salofalk should be administered to adults three times a day for the first dose - 500 mg or 2 to 25 mg, respectively. Severe forms of diseases suggest the possibility of doubling the dose.

As part of maintenance treatment, one suppository of 250 mg is prescribed three times a day. Children under 40 kg are shown a half daily dose of adults, and with an adult body weight of more than 40 kg, an adult dose.

Rectal suspension of the drug is injected from the 1st vial once a day before going to bed. Before this, it is desirable to clean the intestines. Dosage is determined as follows: 30-50 mg in terms of 1 kg of body weight. The maximum allowable amount per day is 3 grams.

Rectal Foam Salofalk is administered once a day before bedtime. 2 clicks on the applicator correspond to a single dose. In the event that the patient has difficulty maintaining this volume of foam in the rectum, it can be administered in several ways - one at bedtime and again at night or after an act of defecation early in the morning. For cupping with the use of foam exacerbations for ulcerative colitis in the lung forms, a 4-6 week treatment with such a dosage form may suffice.

Let's give a number of rules for using Salofalk in the form of foam.

At the time of administration, the foam should have a temperature corresponding to room temperature, that is, from 20 to 25 degrees Celsius.

The applicator is fixed on the cylinder head, after which it should be shaken for about 20 seconds to mix the contents.

If this is the first use, the protective tab at the bottom of the dosing head is removed.

The cap should be rotated in such a way that the nozzle is aligned with the semicircular notch on the safety ring.

With the index finger on the cap, the balloon is turned upside down.

The applicator is inserted into the rectum as deeply as possible. To do this, you can stand with your foot on some elevation, such as a stool or chair.

The first part of the dose (application) will be entered as a result of pressing the cap. When it comes to a stop, it is slowly released. For the second dose, this action should be repeated again. After waiting for 10-15 seconds, the applicator is removed from the rectum.

After the foam is introduced, the used applicator is pre-packed in a plastic bag and discarded.

With each subsequent dose of Salofalk in the foam, a new applicator is required.

The procedure should be followed by thorough hand washing. The patient should refrain from emptying the intestine until the next morning.

The method of administration and dose depend on a number of factors. Among them, one of the main medicinal forms of the drug is most expedient in each individual clinical case. Each of them has its own dosage features and a corresponding specific method, with which they achieve a therapeutic effect.

[17], [18]

Use Salofalk during pregnancy

The use of Salofalk during pregnancy, as well as the use of a variety of other medicines during that rather difficult period in which a woman carries a child, must carefully weigh and evaluate all the factors "For" and "Against". The main criterion for the expediency of the use of the drug must first of all be a comprehensive objective assessment of the degree of the expected positive effect for the future mother, taking into account all possible existing risks with regard to the processes of normal intrauterine growth and fetal development.

At the planning stage of the child, before the expected conception, medical specialists recommend, if there is such a possibility, to completely abandon the use of Salofalk, or to reduce the dosage in which it is applied to a minimum.

It is allowed to continue the course of treatment with the drug during the first trimester of pregnancy. However, the appointment of Salofalk in this case should be only on the basis of strict testimony.

On terms from 2 to 4 last weeks of pregnancy, it is necessary to stop taking the drug.

As for the period of lactation and lactation, it should be taken into account that in the composition of mother's milk may have a presence of about 0.1% of the dose. In view of this, if there is a rationale for the use of this medication by a nursing mother, the question of the possible need to stop breastfeeding becomes urgent. In particular, one of the factors that support the rejection of breastfeeding is the appearance of diarrhea in a baby.

As we see, the use of Salofalk during pregnancy, as well as during lactation and lactation, is possible mainly if it is expected to have a more significant positive effect for the mother than this drug is capable of producing any negative effect on the child during the fetal development and after birth.

Contraindications

Contraindications to the use of Salofalk in connection with the condition of various organs and systems in the patient's body can be summarized as follows.

First of all, we note that in the category of inadmissible to use the drug includes the existing violations of kidney function, which have a high degree of severity.

Equally, the inhibitory factor for the use of Salofalk is the presence of any expressed hepatic dysfunction. In this regard, it should also be noted that taking the drug is not recommended to combine with the regime of dietary nutrition in cases of liver disease.

In addition, gastroenterological contraindications include reflux-exophagitis, the presence of intestinal dysbiosis, gastric ulcer and duodenal ulcers at the stage of exacerbation.

Salofalk is excluded from the list of medications acceptable for prescribing to patients who have a tendency to bleeding - with hemorrhagic diathesis.

In addition, the cause of the inadmissibility of using Salofalk is the presence of an increased sensitivity of the patient to salicylic acid, along with its derivatives.

A cautious and carefully weighed approach requires that the drug be administered to those patients whose renal excretory function is impaired, there are violations of respiratory functions - especially for patients with bronchial asthma. Also a factor against the use of Salofalk is hypersensitivity to sulfasalazine and deficiency of glucose-6-phosphate dehydrogenase.

Categorical contraindications for the use of Salofalk exist for patients with children younger than 2 years of age.

[13], [14]

Side effects Salofalk

Side effects Salofalk find a mapping in the form of the development of all kinds of negative phenomena that can occur in various systems and organs of the human body.

So the reaction of the digestive system to the effect of the drug can be the appearance of pain in the abdomen, diarrhea, flatulence, loss of appetite, nausea and vomiting. In the blood there is an increased content of liver enzymes, in some cases, the development of hepatitis can be noted.

The central nervous system as a result of getting Salofalk into the body often gives a reaction in the form of headache, dizziness, and tinnitus. There is general weakness, sleep is disturbed, there is a tremor phenomenon, there may be seizures, there are paresthesias.

The cardiovascular system responds to taking the drug with hotel cases of tachycardia, arterial hypotension, or hypertension. In addition, there may appear shortness of breath, there may be pain in the sternum.

In the skeletal-muscular system, affected by the negative effects of Salofalk, occasionally the appearance of arthralgias and myalgias can be noted.

Possible violations of the hematopoietic system, manifested in rare cases of anemia, agranulocytosis, leukopenia and thrombocytopenia.

Adverse application of the drug can affect the processes of blood clotting - causing hypoprothrombinemia.

In the genitourinary system, due to the use of Salofalk, anuria, oliguria, hematuria, crystalluria, proteinuria can occur.

In some cases there is a decrease in the level of production of tear fluid, the phenomenon of alopecia.

Due to increased sensitivity, skin rashes may occur, itching, bronchospasm, fever and erythema may occur. Do not exclude the possibility of myocarditis and pericarditis, interstitial nephritis and nephrotic syndrome, acute pancreatitis.

At a certain confluence of circumstances, mesalazine is able to provoke a syndrome similar to systemic lupus erythematosus.

In the event that the side effects of Salofalk have a manifestation of acute signs of intolerance, an immediate cessation of its use is required.

[15], [16]

Overdose

Overdose of Salofalk with a dosage form of suppositories of rectal and rectal suspension has not been documented in any cases of application of the drug.

The probability of negative phenomena caused by this drug is mainly associated with taking it orally in the form of tablets as the most common form of it taking place in among medical appointments in a number of bowel diseases.

Symptomatics, manifested as a consequence of the negative impact on the body of critically exceeded doses of Salofalk, finds a mapping in the following.

There is the occurrence of attacks of nausea, vomiting occurs, gastralgia phenomena are observed characterized by painful contractions in the region of the stomach. There is a general decrease in the tone of the body, muscle weakness, drowsiness.

Treatment of an overdose of the drug Salofalk involves the provision of symptomatic therapeutic measures. Appoint funds that have a laxative effect, you may need to rinse your stomach. In addition, when there is an overdose of this drug, a justified measure may be the implementation of forced diuresis with infusion of electrolytic solutions.

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

Interactions with other drugs

The interaction of Salofalk with other drugs lies in the fact that in the process of its application in the complex simultaneously with such drugs as furosemide, rifampicin, spironolactone, sulfonamides, it leads to a decrease in their diuretic activity and effectiveness.

Salofalk causes an increase in the anticoaculant effect of coumarinic anticoagulants.

The next effect produced by the drug is that as a result of its effect, the effectiveness of uricosuric tubular secretion blockers increases, and the rate of cyanocobalamin absorption processes decreases.

With the simultaneous use of Salofalk and methotrexate, the latter has a stronger effect, its toxicity increases.

With respect to agents that are derivatives of sulfonylurea and possess antidiabetic properties, this drug helps to enhance the hypoglycemic effect that they produce.

The use of Salofalk in a single treatment course together with glucocorticosteroids can lead to an increase in the degree of adverse reactions manifested by the mucous membrane of the stomach.

Summing up, we will say that in some cases, the interaction of Salofalk with other drugs leads to an increase in the effect produced by them in the body, or, on the contrary, is able to act on them in an unfavorable manner. And on the other hand, the drug itself, entering into various interactions, can be both strengthened and weakened in its effectiveness. Therefore, all prescribed combinations of drugs, taking into account all their strengths and weaknesses, should be selected by a competent specialist in the field of medicine.

[23],

Storage conditions

Storage conditions of Salofalk stipulate that the drug should be in a place where it can not get into the hands of children, and also with a certain temperature regime - no more than 25 degrees Celsius. It must be allowed to freeze it.

[24], [25]

Shelf life

The shelf-life of the drug is different, depending on how it is presented to the drug form.

Tablets are suitable for use when they are stored under appropriate conditions - 3 years from the date of release. Granules - 4 years.

Suppositories rectal - 3 years. Rectal suspension is suitable for 2 years from the date of manufacture.

Foam - 2 years. Here, however, there is an important point - after the balloon was opened, the period of its use is 12 weeks.

[26], [27]