Instruction for use: Salofalk

Active substance Mesalazine

ATX Code A07EC02 Mesalazine

Pharmacological group

Antimicrobial and anti-inflammatory intestinal [NSAIDs - Salicylic acid derivatives]

Nosological classification (ICD-10)

K51 Ulcerative colitis

Colitis acute ulcerative, Colitis ulcerative, Ulcerative-necrotic colitis, Colitis ulcerative-hemorrhagic nonspecific, Colitis ulcerative and trophic, Colitis ulcerative idiopathic, Colitis ulcerative nonspecific, Nonspecific ulcerative colitis, Proctocolitis ulcers, Hemorrhagic purulent rectoxitis, Rectoccolitis ulcerative-hemorrhagic

Composition

Suppositories rectal 1 supp.

active substance:

mesalazine 250 mg

500 mg

auxiliary substances (250 mg): fat solid - 1830 mg

auxiliary substances (500 mg): docusate sodium - 2 mg; fat solid - 1680 mg; cetyl alcohol - 18 mg

Rectal suspension 1 enema

active substance:

mesalazine 2 g / 30 ml

4 g / 60 ml

auxiliary substances: xanthan gum - 0,075 / 0,15 g; carbomer (carbopol 974) - 0.0225 / 0.045 g; disodium edetate dihydrate - 0.03 / 0.06 g; sodium benzoate - 0.03 / 0.06 g; potassium disulphite - 0.1404 / 0.2808 g; potassium acetate - 0.123 / 0.246 g; purified water - 27.5791 / 55.1582 g

Foam rectal dosed 1 application.

active substance:

mesalazine 1 g

auxiliary substances: propylene glycol - 3.4364 g; sodium disulphite - 0.05 g; polysorbate 60 - 0.0364 g; disodium edetate - 0.0136 g; cetostearyl alcohol 0.0091 g; Propellant (propane / isobutane / butane at a pressure of 2.5 bar) - 0.176 g

Description of dosage form

Suppositories rectal: torpedovidnye, from white to cream color, homogeneous consistency, with intact, even surface.

Rectal suspension: homogeneous suspension from light gray to brown color, free of foreign inclusions.

Foam rectal dosed: creamy persistent foam from greyish-white to slightly reddish-violet.

pharmachologic effect

Pharmacological action - anti-inflammatory local.

Pharmacodynamics

Has a local anti-inflammatory effect due to inhibition of COX and neutrophilic lipoxygenase and synthesis of PG and LT. Slows migration, degranulation, phagocytosis of neutrophils, as well as secretion of Ig lymphocytes. It has antibacterial action against Escherichia coli and some cocci. It has an antioxidant effect due to the ability to bind to free oxygen radicals and destroy them. Mesalazine has a local anti-inflammatory effect because it acts locally in the epithelial and submucous layer of the colon mucosa. Therefore, the indicators of systemic bioavailability and the concentration of mesalazine in plasma are not important in terms of its therapeutic effectiveness, but rather serve as a factor in assessing its safety.

Pharmacokinetics

Absorption. The greatest absorption of mesalazine occurs in the rectum and colon.

Metabolism. Mesalazine is metabolized both by the pre-systemic route in the intestinal mucosa, and systemically in the liver, turning into pharmacologically inactive N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA). The nature of acetylation does not depend on the acetylating phenotype of the patient. To a small extent, acetylation can be carried out by the action of bacterial microflora of the colon. The binding to plasma proteins of mesalazine and N-Ac-5-ASA is 43% and 78%, respectively.

Excretion. Mesalazine and its metabolite N-Ac-5-ASA are excreted through the intestine (the major part,> 90%), up to 7% of the kidneys (0.6% of the total dose is excreted in the form of mesalazine and up to 6.3% in the form of a metabolite N-Ac-5-ASA), the degree of excretion of the drug with bile is minimal.

Indications

exacerbation of distal forms of ulcerative colitis of moderate and mild severity;

maintenance of remission of ulcerative colitis.

Contraindications

Common for all dosage forms

hypersensitivity to the components of the drug and other derivatives of salicylic acid;

severe renal / hepatic insufficiency.

For suppositories of rectal and rectal suspension

children's age till 18 years.

With caution: impaired breathing (especially bronchial asthma); hypersensitivity to sulfasalazine; impaired liver function; deficiency of glucose-6-phosphate dehydrogenase.

For rectal suppositories additionally

peptic ulcer of the stomach and duodenum in the phase of exacerbation;

hemorrhagic diathesis (with a tendency to bleeding).

With caution: impaired renal function.

For foam rectal dosed additionally

children under 12 years.

With caution: lung disease, incl. bronchial asthma.

pregnancy and lactation

Sufficient data on the use of the drug Salofalk in pregnant women do not. However, data on the use of mesalazine in several pregnant women indicate that there is no undesirable effect of mesalazine on pregnancy or fetus / newborn health.

Studies on animals in which mesalazine was administered orally do not indicate a direct or indirect adverse effect on pregnancy, embryo / fetal development, childbirth and postpartum development.

The drug Salofalk should be used during pregnancy only in those cases when the potential benefit of its use for the mother exceeds the possible risk to the fetus.

When breastfeeding, Salofalk should not be used - the active substance and its metabolites can penetrate into breast milk. If it is necessary to prescribe Salofalk during lactation, the question of stopping breastfeeding should be solved.

Side effects

Common for three dosage forms

Against the background of the use of mesalazine, the following side effects were observed, systematized according to the organ system and frequency of occurrence.

The assessment of adverse events is based on the following classification: often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000; <1/1000); very rarely (<1/10000).

On the part of the blood and lymphatic system: very rarely - pathological parameters of blood elements (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia).

From the nervous system: rarely - headache, dizziness; very rarely - peripheral neuropathy.

From the heart: rarely - myocarditis, pericarditis.

From the respiratory, thoracic and mediastinal organs: very rarely - allergic and fibrotic reactions from the lungs (including shortness of breath, cough, bronchospasm, alveolitis, pulmonary eosinophilia, pulmonary infiltrates, pneumonitis).

From the digestive tract: rarely - abdominal pain, diarrhea, bloating, nausea, vomiting; very rarely - acute pancreatitis.

From the side of the kidneys and urinary tract: very rarely - impaired renal function, incl. acute and chronic interstitial nephritis, renal failure.

From the skin and subcutaneous tissues: very rarely - alopecia.

From the musculoskeletal system and connective tissue: very rarely - myalgia, arthralgia.

From the immune system: very rarely - hypersensitivity reactions, for example, allergic exanthema, drug fever, lupus erythematosus, pancolitis.

From the liver and bile ducts: very rarely - increased activity of transaminases and cholestasis parameters), cholestatic hepatitis.

From the side of the reproductive system: very rarely - oligospermia (reversible).

For foam rectal dosed additionally

Complications of a general nature and reaction at the injection site: often - discomfort; infrequent - discomfort in the anus; irritation at the injection site, painful urge to defecate.

Interaction

Studies of the interaction of the drug Salofalk with other drugs have not been conducted.

Patients who are simultaneously receiving treatment with azathioprine, 6-mercaptopurine or thioguanine should be aware of the possible increase in the myelosuppressive effect of azathioprine and 6-mercaptopurine or thioguanine.

The use of mesalazine together with anticoagulants, for example warfarin, may reduce the anticoagulant effect of mesalazine.

Dosing and Administration

Rectally.

Rectal suppositories

For the treatment of exacerbations of ulcerative colitis: adults, 2 soups. 3 times a day (corresponding to 1500 mg of mesalazine per day).

As maintenance therapy in the period of remission: adults, 1 supp. 3 times a day (corresponding to 750 mg of mesalazine per day).

The duration of treatment is determined by the doctor.

Rectal suspension

Adults and elderly people: in patients with symptoms of acute inflammation, 60 ml of the suspension is injected into the intestine as an enema once a day before bedtime (it is recommended to clean the intestine first).

If the patient has difficulties with the introduction of large amounts of liquid, the dose of the drug can be divided into 2 divided doses, 30 ml of suspension in the morning and evening.

The duration of use is determined by the doctor.

1. Shake the vial well for at least 30 seconds before use to ensure a good mixing of the suspension.

2. Remove the protective cap from the applicator. Keep the container upright so that its contents do not spill.

3. Lie on your left side, stretching your left leg and bending the right knee to facilitate the introduction of rectal suspension and increase the effectiveness of the enema.

4. Insert the tip of the applicator deep into the rectum.

5. To direct a tip of a vial a little downwards, then slowly and in regular intervals to squeeze out a vial or flask.

6. After emptying the vial slowly remove the applicator.

7. After applying the drug, stay in the same position for at least 30 minutes.

Rectal Dosed Foam

If the doctor is not prescribed otherwise, in adults and children over 12 years of age the drug is usually applied 1 time a day before bedtime (1 dose corresponds to 2 applications / strokes). If it is difficult to keep such a volume of foam in the gut, the drug should be administered in two stages: 1 time at night and 1 time at night or early in the morning (after defecation).

To achieve the best result, it is recommended to administer the drug after bowel movement (defecation).

At the time of administration, the drug Salofalk is rectal, should be at room temperature (20-25 ° C).

1. Attach the applicator tightly to the cylinder head.

2. Shake the can for 20 seconds to mix its contents.

3. For first use, remove the protective tab from the bottom of the dosing head.

4. Turn the cap so that the semicircular cutout on the safety ring is aligned with the nozzle.

5. Place the index finger on the cap and turn the cylinder upside down.

6. Introduce the applicator into the rectum as deeply as possible. It is best to put your foot on a chair or a stool. In order to enter the first part of the dose of the drug, press the cap to the stop and slowly release. To enter the second part of the dose, press the cap again and release slowly. Wait 10-15 seconds, then slowly remove the applicator from the rectum.

7. After the introduction of foam, remove the applicator and discard it, packed in a plastic bag. For each new dose of the drug, a new applicator should be used.

8. Wash hands after the procedure. You should try not to empty your bowels until the next morning.

When you go to the hospital or consult with other doctors, tell them about the use of this drug.

The therapeutic effect is achieved with the regular use of the drug Salofalk rectal foam.

The duration of the course of treatment is selected by the doctor individually.

As a rule, exacerbation of mild forms of ulcerative colitis can be stopped within 4-6 weeks. At the end of this period, it is recommended that you visit the attending physician to decide on the appointment of an oral form of mesalazine for maintenance therapy.

Overdose

Cases of an overdose have not been revealed. In case of an overdose, symptomatic treatment is performed.

special instructions

Common for three dosage forms

Before the beginning of treatment and in the process of its conduct, at the discretion of the attending physician, the following tests should be performed: blood test (general blood test, liver functional status indicators (such as ALT and AST activity), plasma creatinine content) and urinalysis. Conducting a follow-up examination is usually recommended 14 days after the start of treatment and then 2-3 times with an interval of 4 weeks. If the results obtained correspond to the norms of values, then it is sufficient to carry out these analyzes every 3 months. If additional symptoms appear, follow-up examinations should be performed immediately.

For rectal suppositories additionally

Care should be taken in patients with impaired liver function.

Treatment of patients with known hypersensitivity to drugs containing sulfasalazine, can begin only under close medical supervision. When symptoms of acute intolerance, such as spasms, acute abdominal pain, fever, severe headaches and skin rash should be discontinued immediately.

In patients with impaired renal function, the use is not recommended. If, during treatment, there is a decrease in kidney function, the manifestation of nephrotoxicity associated with mesalazine should be assumed.

In patients with lung diseases, in particular bronchial asthma, careful monitoring is necessary during the treatment.

For rectal suspension additionally

The drug Salofalk rectum suspension contains potassium disulphite, it can cause allergic reactions with symptoms of anaphylaxis and bronchial spasms (bronchospasm), in particular in patients with bronchial asthma or with allergic reactions in the anamnesis.

Patients with the above conditions should be under close medical supervision.

The drug Salofalk rectally contains sodium benzoate, so it can provoke hypersensitivity reactions (in particular in the form of skin, eye and mucous membrane irritation).

For foam rectal dosed additionally

Salofalk rectal foam should not be used in patients with impaired renal function. The possibility of renal toxicity due to the action of mesalazine should be considered when worsening with kidney function.

The condition of patients with pulmonary diseases, in particular asthma, should be closely monitored during treatment with the drug Salofalk rectal foam.

Patients with a history of undesirable drug reactions to drugs containing sulfasalazine, should be kept under close medical supervision at the time of starting treatment with the drug Salofalk rectally.

If the drug causes acute intolerance reactions, such as colic in the abdomen, acute abdominal pain, fever, severe headache and rash, therapy should be immediately withdrawn.

In some cases, hypersensitivity reactions, mainly in the form of problems with breathing, can also be observed in people who do not suffer from asthma due to the presence of sulfite.

This drug contains propylene glycol, which can cause lactic acidosis, hyperosmolarity, hemolysis and CNS depression. There may be slight or mild skin irritation due to the action of propylene glycol.

The drug contains cetostearyl alcohol, which can cause local skin reactions (eg contact dermatitis).

The contents of the container are under high pressure. The container should not be exposed to sunlight and heated to a temperature of more than 50 ° C.

To open and puncture the cylinder, and also to burn empty used cylinders is inadmissible.

Do not use near open flames or hot objects.

Influence on ability to drive vehicles, mechanisms

For suppositories rectal and rectal suspension additionally. The drug does not affect the management of vehicles and the maintenance of moving mechanisms. When the described undesirable phenomena (including dizziness) should be refrained from performing these activities.

For foam rectal dosed additionally. The effect of the drug on the ability to drive and control mechanisms is not recorded.

Form of issue

Suppositories rectal, 250 or 500 mg. By 5 soups. in a laminated PVC / LDPE blister; on 2 or 6 bl. in a pack of cardboard.

Rectal suspension, 2 g / 30 ml, 4 g / 60 ml. For 30 or 60 ml in white, round compressible vials of dense PE, closed with a lubricated tip of the rectal applicator and a protective cap. The bottle is placed in a contoured package of heat-sealed PVC film and paper laminated with an aluminum coating. 7 fl. PE, placed in a contoured package, in a cardboard bundle.

Foam rectal dosed, 1 g / applique. For 14 applications (7 doses) in an aluminum bottle lacquered from the inside, equipped with a dosing device, complete with special PVC applicators, equipped with protective caps, and PE bags for used applicators. The applicator is coated with a lubricant consisting of a mixture of white soft paraffin and vaseline oil (7: 3). 1 bottle, 14 applicators and 14 PE bags in a cardboard bundle.

Conditions of leave from pharmacies

On prescription.

storage conditions

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life

Rectal Dosed Foam 1 g / applique. - 2 years. After opening the container it should be used within 12 weeks.

Rectal suspension 2 g / 30 ml - 2 years.

Rectal suspension 4 g / 60 ml - 2 years.

suppositories rectal 250 mg - 3 years.

suppositories rectal 500 mg - 3 years.

Do not use after the expiry date printed on the package.