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

Composition:Each tablet contains: mesalazine 250 mg
Auxiliary substances: sodium carbonate 110 mg, glycine 10 mg, povidone 10 mg, cellulose microcrystalline 50 mg, silicon dioxide colloid 5 mg, calcium stearate 5 mg, hypromellose 2.0 mg,methacrylic acid and methacrylate copolymer 1: 1 42.82 mg, talc 10.2 mg, titanium dioxide 1.2 mg, iron dye oxide yellow 0.6 mg, macrogol 4.98 mg, butyl methacrylate 0.9 mg.

Description:Round, biconvex tablets, covered with a film coat from light yellow to yellow-brown color.

Pharmacotherapeutic group:Anti-inflammatory intestinal.

ATX: & nbsp

A.07.E.C.02 Mesalazine

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

Pharmacodynamics:Has anti-inflammatory effect. Inhibits the synthesis of metabolites of arachidonic acid (prostaglandins), the activity of neutrophilic lipoxygenase, inhibits the migration, degranulation and phagocytosis of neutrophils, the secretion of immunoglobulins by lymphocytes; binds and destroys the free radicals of oxygen.

Pharmacokinetics:Biotransformation
Mesalazine is metabolized both by the pre-systemic route in the intestinal mucosa, and systemically in the liver, turning into pharmacologically inactive M-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-Ac-b-ASA is 43% and 78%, respectively.
Distribution
A combined pharmaco-cintigraphic / pharmacokinetic study demonstrated that when taken with food, Salofalk 250 mg tablets, coated with an enteric coating, dissolve after approximately 3-4 hours in the ileum. The average evacuation time of gastric contents was approximately 3 hours. After about 7 hours, the tablets reached the colon. Approximately 75% of the dose of mesalazine reaches the large intestine in a nonmetabolized form.
Absorption
Absorption of mesalazine is maximal in the proximal parts of the intestine and is minimal in the distal regions. The highest plasma concentration is reached after approximately 5 hours (in the ileum) and 500 mg of mesalazine are administered three times a day, provided the equilibrium is steady, is 2.1 ± 1.7 μg / ml for mesalazine and 2.8 ± 1, 7 μg / ml for its metabolite, N-Ac-5-ACK.
Excretion
Mesalazine and its metabolite N-Ac-5-ACK are excreted with feces (main part), through the kidneys (from 20% to 50%, depending on the method of use, the pharmacological preparation and the way of releasing mesalazine), and also with bile.N-Ac-5-ACK predominantly excreted with the kidneys. About 1% of the ingested dose of mesalazine is excreted in breast milk, mainly in the form of N-Ac-5-ACK. In long-term treatment with 250 mg Salofalk 250 mg tablets at a daily dose of 500 mg mesalazine (assuming steady equilibrium), the total rate of kidney excretion of mesalazine and N-Ac-5-ACK was approximately 55% (value obtained within 24 hours after the last dose ). The proportion of non-metabolized mesalazine was approximately 5%. The elimination half-life is 0.7-2.4 hours (1.4 ± 0.6 hours on the average) with 500 mg of mesalazine administered three times a day.

Indications:Treatment of exacerbations and prevention of relapses with ulcerative colitis and Crohn's disease.

Contraindications:Hypersensitivity to the components of the drug and other derivatives of salicylic acid, blood diseases, peptic ulcer of the stomach and duodenum, deficiency of glucose-6-phosphate dehydrogenase, hemorrhagic diathesis, severe renal / hepatic insufficiency, children's age (up to 6 years).

Carefully:Violation of the function of the liver and kidneys of mild and moderate severity, lung disease (especially bronchial asthma), patients with hypersensitivity to sulfasalazine.

Pregnancy and lactation:Sufficient data on the use of 250 mg Salofalk tablets in pregnant women does not exist. However, data on the use of mesalazine in several pregnant women indicate that there is no undesirable effect of mesalazine on pregnancy or on the health of the fetus / newborn.
Studies on animals, which mesalazine was administered orally, do not indicate the presence of direct or indirect adverse effects on pregnancy, embryo / fetal development, childbirth and postpartum development.
Salofalk tablets should be used during pregnancy only in cases where the potential benefit of using it for the mother exceeds the possible risk to the fetus.
Salofalk tablets can be used in women during lactation only if the potential effect of its use for 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:Take the drug strictly as directed by your doctor.
Adults. With ulcerative colitis for treatment of an exacerbation depending on the severity of the disease inside 2-4 tablets 250 mg 3 times a day (daily dose of 1.5 to 3.0 grams of mesalazine).In Crohn's disease, to treat an exacerbation, depending on the severity of the disease, 2-6 tablets 250 mg 3 times a day (daily dose of 1.5 to 4.5 grams of mesalazine).
For the prevention of recurrences with ulcerative colitis and Crohn's disease, the drug is prescribed at 2x250 mg 3 times a day, if necessary for several years.
Children (6 years and older). For treatment of exacerbation with ulcerative colitis and Crohn's disease, the dose is selected individually. The initial dose is 15-30 mg / kg / day, divided not a few techniques; the maximum dose is 75 mg / kg / day. The total daily dose should not exceed the maximum daily dose for adults.
For the prevention of recurrence, a dose of 15-30 mg / kg / day, divided into several doses, is used. The total daily dose should not exceed the recommended daily dose for adults.
The general recommendation is that up to 40 kg of body weight, a 1/2 day dose is used for adults (250 mg tablets 3 times a day should be used), more than 40 kg of body weight - a daily dose for adults - 500 mg 3 times a day .
Tablets should be taken whole, not liquid, morning, afternoon and evening 1 hour before meals and drink plenty of water.In the distal forms of ulcerative colitis, simultaneous rectal administration of the drug in the form of suppositories or enemas, foams is preferred.

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 (≥1/10,000; < 1/1,000)	Very rarely (<1 / 10,000)
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)
Infringements from 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, renal failure

Disturbances from the skin and subcutaneous tissue		Alopecia
Disturbances from musculoskeletal system and connective tissue		Myalgia, arthralgia
Immune system disorders		Reactions hypersensitivity, eg - allergic exanthema, medicinal fever, lupus syndrome, pancolitis
Disturbances from the liver and bile ducts		Changes in liver function (increased activity of transaminases and cholestasis parameters), hepatitis, cholestatic hepatitis
Disorders from the reproductive system		Oligospermia (reversible)

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

Interaction:Studies of the interaction of the drug Salofalk with other drugs have not been conducted.
In patients who are simultaneously receiving treatment with azathioprine, 6-mercaptopurine, or thioguanine, one should remember 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.

Special instructions:Before the beginning of treatment and in the process of it, at the discretion of the attending physician, it is necessary to determine the parameters of the functional state of the liver (such as ALT or ACT activity) and to control urine tests (by dipping test strips). 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 appointing Salofalk tablets to patients with lung diseases, in particular, bronchial asthma, it is necessary to carry out careful monitoring 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 treatment with Salofalkom tablets. If Salofalcom is treated with acute intolerance, such as convulsions, acute abdominal pain, fever, severe headache and rash, use of the drug should be stopped immediately. Note:
In rare cases, in patients who underwent resection of the large intestine / operation on the large intestine in the area of the ileocecal angle with the removal of the ileocecal flap, separation of Salofalk tablets in undissolved form with feces was noted in view of the excessively rapid passage through the intestine.
1 tablet Salofalk 250 mg contains 2.1 mmol (48 mg) of sodium. If the patient is on a diet with sodium content control, this should be taken into account.

Effect on the ability to drive transp. cf. and fur:The drug does not affect the management of vehicles and the maintenance of moving mechanisms. When these undesirable phenomena (such as dizziness, etc.) appear, one should refrain from performing these activities.

Form release / dosage:Tablets, covered with enteric film coating.

Packaging:For 10 tablets in aluminum / PVC / PVDC blister; for 5 or 10 blisters together with instructions for use in a pack of cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N013074 / 01

Date of registration:17.12.2007

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

Representation: & nbspDOCTOR FALK PHARMA GmbH DOCTOR FALK PHARMA GmbH Germany

Information update date: & nbsp2016-09-22

Illustrated instructions

Instructions

Salofalk (Salofalk)