Salofalk - instructions for use, dose, side effects, contraindications

Composition:In one dose (package) contains:
Active substance
Mesalazine (5-aminosalicylic acid) 500 mg or 1000 mg.
Auxiliary components
Core
Cellulose microcrystalline 200.0 mg / 400.0 mg, hypromellose 18.0 mg / 36.0 mg, silicon dioxide colloidal anhydrous 0.25 mg / 0.5 mg,eudragzhit NE 40 D [40% dispersion of methyl methacrylate and ethyl acrylate copolymer [2: 1] and 2% nonoxynol) in terms of dry matter 45.0 mg / 90.0 mg, magnesium stearate 7.75 / 15.5 mg, dry matter 33% emetic simethicone (consists of 92 % simethicone 7.7%, methylcellulose, 0.3% acid sorbic) 0.5 / 1.0 mg.
Inner shell of pellet
Gipromellose 2.0 mg / 4.0 mg, methacrylic acid and methyl methacrylate, copolymer [1: 1] (Eudrajit L 100) 75.0 mg / 150.0 mg, triethyl citrate 7.5 mg / 15.0 mg, talc 20.0 mg / 40.0 mg, magnesium stearate 5.0 mg / 10.0 mg , titanium dioxide 12.5 mg / 25.0 mg.
Outer sheath of granule
Carmellose sodium 15.0 mg / 30.0 mg, titanium dioxide 5.0 mg / 10.0 mg, aspartame 1.0 mg / 2.0 mg, citric acid anhydrous 3.0 mg / 6.0 mg, vanilla flavoring 2.0 mg / 4.0 mg, talc 5.5 mg / 11.0 mg, povidone K- 25 5.0 mg / 10.0 mg.

Description:Rounded particles of cylindrical or spherical shape (granules) are grayish white.

Pharmacotherapeutic group:Anti-inflammatory intestinal.

ATX: & nbsp

A.07.E.C.02 Mesalazine

A.07.E.C Aminosalicylic acid and its analogues

Pharmacodynamics:Has a local anti-inflammatory effect due to inhibition of neutrophilic lipoxygenase and the synthesis of prostaglandins and leukotrienes. Slows migration, degranulation, phagocytosis of neutrophils, as well as secretion of immunoglobulins by lymphocytes.Has antioxidant effects (due to the ability to bind to free oxygen radicals and destroy them). Mesalazine can also catch radicals formed from reactive oxygen compounds. The results obtained in in vitro studies indicate the possible role of inhibition of lipoxygenase. The effect on the content of prostaglandins in the intestinal mucosa is also shown. When taken orally mesalazine has a predominantly local effect in the intestinal mucosa and submucosal layer, acting from the side of the intestinal lumen. Therefore, it is important that mesalazine is available in the field of inflammation. The ratio of systemic bioavailability and mesalazine concentration in plasma is not significant in terms of therapeutic effectiveness, but rather serves as a factor affecting safety. To ensure the release of the active substance in the right place, it helps that the Salofalk pellets are resistant to gastric juice and are pH-dependent (due to the coating in the form of Eudrajit L) and delayed (due to the matrix structure of granules) release of mesalazine.

Pharmacokinetics:Biotraisformation
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-ACK). 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 connection with the plasma proteins of mesalazine and N-Au-5-ACK is 43% and 78%, respectively. Distribution
Due to the size of the granules (about 1 mm), transit from the stomach to the small intestine occurs quickly. Combined pharmaco-silica and pharmacokinetic study showed that the drug reaches the ileocecal region in about 3 hours, and the ascending colon section in about 4 hours. The total transit time for the large intestine is about 20 hours. Approximately 80% of the taken oral dose reaches the thick, sigmoid and rectum.
Absorption
The release of mesalazine from the pellets of Salofalk begins with a delay of 2-3 hours, the maximum concentration in the plasma is reached after 4-5 hours.
Systemic bioavailability of mesalazine after oral administration is approximately 15-25%.
Food intake slows down absorption for 1-2 hours, but does not change the rate and degree of absorption.
Elimination:
When mesalazine was taken at a dose of 500 mg x 3 times a day, the total elimination of mesalazine and N-Ac-5-ACK by the kidneys at a saturating concentration was about 25%. The excretion of the unmetabolized portion of mesalazine was less than 1% of the orally administered dose. The half-life in this study was 4.4 hours.

Indications:Exacerbation of ulcerative colitis of moderate and mild severity; maintenance of remission and / or long-term therapy of ulcerative colitis.

Contraindications:Hypersensitivity to the components of the drug and other derivatives of salicylic acid, severe renal / hepatic insufficiency, children's age (up to 6 years).

Carefully:Pregnancy (I trimester), renal / hepatic insufficiency of mild and moderate severity, lung disease (especially bronchial asthma).

Pregnancy and lactation:Salofalk in granules 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.
Salofalk in granules can be used in women during lactation only if the potential effect of its use on the mother exceeds the possible risk of adverse effects on the child. If a newborn breastfed has diarrhea, breastfeeding should be discontinued.

Dosing and Administration:To treat exacerbation of ulcerative colitis:
Depends on the clinical need for each individual case, 1 packet of 500-1000 mg mesalazine 3 times a day or 3 packets 1 time per day (corresponding to 1.5-3.0 g mesalazine per day).
To maintain remission of ulcerative colitis:
For 500 mg of mesalazine 3 times a day or 3 packets containing 500 mg of mesalazine or 1000 mg of mesalazine, once a day (corresponding to 1.5-3.0 g of mesalazine per day).
Children under 6 years:
Salofalk in granules should not be given to children under 6 years of age, since the experience of using the drug in patients of this age group is very limited.
Children over 6 years and adolescents:
When the disease worsens, depending on its severity, mesalazine is prescribed in a dose of 30-50 mg / kg of body weight per day with the distribution of the daily dose for 3 doses or for 1 reception.The maximum dose: 75 mg / kg of body weight per day. The total dose should not exceed the maximum dose for an adult (3.0 g mesalazine per day).
To maintain remission mesalazine is prescribed in a dose of 15-30 mg / kg of body weight per day: the daily dose can be divided into 2 doses.
Children with body weight up to 40 kg are usually recommended to appoint a half dose of adults, children with a body weight of more than 40 kg - a dose of adults.
Granules of Salofalk should not be chewed. The prescribed dose of Salofalk in granules should be taken in the morning, at lunchtime and in the evening or the entire dose once in the morning. Granules Salofalk should be put on the tongue and swallowed, without chewing, squeezed a lot of liquid.
As in the treatment of exacerbations of the inflammatory process, and with prolonged use to maintain remission, granules should be taken regularly and consistently, which allows to achieve the desired therapeutic effect. Exacerbation of ulcerative colitis usually subsides in 8-12 weeks, after which the dose of mesalazine in most patients can be reduced to 1.5 g per day.

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

Organs and Systems	Frequency, according to classification MedDRA
	Rarely (≥1/10000; < 1/1000)	Very rarely (<1/10000)
Violations of the blood and lymphatic system		Pathological parameters of blood elements (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia)
Disturbances from the nervous system	Headache, dizziness	Peripheral neuropathy
Heart Disease	Myocarditis, pericarditis
Disturbances from the respiratory, thoracic and mediastinal organs		Allergic and fibrotic reactions from the lungs (including dyspnea, cough, bronchospasm, alveolitis, pulmonary eosinophilia, pulmonary infiltrates, pneumonitis)
Disorders from the gastrointestinal tract	Abdominal pain, diarrhea, bloating, nausea, vomiting	Acute pancreatitis
Disorders from the kidneys and urinary tract		Impaired renal function, including acute and chronic interstitial nephritis, kidney failure
Disturbances from the skin and subcutaneous tissue		Alopecia
Disturbances from musculoskeletal system and connective tissue		Myalgia, arthralgia

Immune system disorders

Reactions

hypersensitivity, for example - allergic exanthema, drug fever, drug-induced lupus syndrome (drug syndrome of lupus erythematosus), pancolitis

Disturbances from the liver and bile ducts

Changes in liver function (increased activity of "liver" transaminases and parameters of cholestasis), hepatitis,

cholestatic

hepatitis

Disorders from the reproductive system

Oligospermia (reversible)

Overdose:Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.
Treatment: gastric lavage, laxative, symptomatic therapy.
In cases of overdose, if necessary, intravenous electrolyte solutions (forced diuresis) are administered.

Interaction:Studies of the interaction of mesalazine with other drugs have not been conducted.
In patients who are simultaneously receiving treatment with azathioprine, 6-mercaptopurine or thioguanine, the possible enhancement of the myelosuppressive effect of azathioprine, 6-mercaptopurine or thioguanine should be borne in mind.
The use of mesalazine together with anticoagulants, for example, warfarin, can reduce the anticoagulant effect of mesalazine.
Lactulose and other similar preparations that lower the pH of the intestinal contents may reduce the release of mesalazine from the granules due to a decrease in the pH due to the bacterial metabolism of lactulose.

Special instructions:Before the start of treatment and in the process of it, at the discretion of the attending physician, it is necessary to monitor the parameters of peripheral blood, determine the parameters of the functional state of the liver (such as ALT or ACT activity) and monitor urinalysis). The control is recommended usually 14 days after the start of treatment, then 2-3 more times with an interval of 4 weeks.
If the results of the tests are normal, control studies should be performed every 3 months. If additional symptoms appear, follow-up studies should be performed immediately.
If renal dysfunction has developed during treatment, one should think about the nephrotoxic effect of mesalazine.
When Salofalk is prescribed in granules, patients with lung diseases, in particular bronchial asthma, should be carefully monitored during treatment.
Patients who have had anamnestic indications of adverse reactions in the administration of drugs containing sulfasalazine, are subject to close monitoring during the initial period of Salofalk treatment in granules. If Salofalcom is treated with acute intolerance, such as convulsions, acute abdominal pain, fever, severe headache and rash, the drug should be discontinued immediately.
If you feel a serious deterioration in your overall health due to a fever, and / or inflammation of the pharynx and mouth, please notify your physician immediately. Symptoms may have been manifested by lowering the level of leukocytes in your blood (agranulocytosis). This can increase the risk of a serious infection. It is necessary to give a general blood test to determine if your symptoms are related to the action that this drug has on your blood.
When prescribing the drug to patients suffering from phenylketonuria, it should be remembered that Salofalk in granules contains aspartame (as a sweetener) at doses equivalent to the following amount of phenylalanine: 0.56 mg (Salofalk granules 500 mg), 1.12 mg (Salofalk granules 1000 mg).

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving a vehicle and engaging in potentially hazardous activities that require increased attention and speed of the psychomotor reaction.

Form release / dosage:Granules coated with enteric coating, prolonged action of 500 mg and 1000 mg.

Packaging:By 930 mg or 1860 mg in a polyethylene bag laminated with aluminum foil; 50 packets along with instructions for use are placed in a cardboard box.
By 930 mg or 1860 mg in a polyethylene bag laminated with aluminum foil; 50 bags along with the instructions for use are placed in a cardboard box and 2 cardboard packs No. 50 are enclosed by a cardboard box.

Storage conditions:Store in a dry place protected from light at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:4 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000158

Date of registration:13.01.2011 / 09.02.2016

Expiration Date:Unlimited

The owner of the registration certificate: Dr. Falk Farma GmbH Dr. Falk Farma GmbH Germany

Manufacturer: & nbsp

Dr.FALK PHARMA, GmbH Germany

Information update date: & nbsp2016-09-21

Illustrated instructions

Instructions

Salofalk (Salofalk)