Salofalk

General characteristics. Structure:

Suppositories rectal - 1 soup.

Active agent: месалазин - 250 mg, 500 mg.

Excipients: sodium docusate — 0/2 mg; fat firm — 1830/1680 mg; cetyl alcohol — 0/18 mg.

Suspension rectal - 1 enema.

Active agent: месалазин - 2 g / 30 ml, 4 g / 60 ml.

Excipients: the water purified — 27,5791/55,1582 g; Kalii acetas — 0,123/0,246; potassium disulphite — 0,1404/0,2808 g; a butt xanthane — 0,075/0.15 g; carbomer — 0,0225/0,045 g; Natrium benzoicum — 0,03/0,06; sodium ethylaminoacetate — 0,03/0,06; nitrogen gaseous.

Foam rectal dosed - 1 апплик.

Active agent: месалазин - 1 g.

Excipients: propylene glycol — 3,4364 g; sodium disulphite — 0,05 g; polysorbate of 60 — 0,0364 g; dinatrium эдетат — 0,0136 g; cetostearyl alcohol — 00091 g; propellant (propane of 7%, / isobutane of 88% / butane of 5% under pressure of 2,5 bars) — 0,176 g.

Pharmacological properties:

Pharmacodynamics.

Possesses the local antiinflammatory action caused by inhibition of a neutrophylic lipoxygenase and synthesis of PG and leukotrienes. Slows down migration, degranulation, phagocytosis of neutrophils, and also secretion of immunoglobulins lymphocytes. Possesses antibacterial action concerning colibacillus and some cocci. Has antioxidant effect due to ability to contact free oxygen radicals and to destroy them. It is important to consider what месалазин possesses only local antiinflammatory action as works locally in an epithelial and submucous layer of a mucous membrane of a large intestine. Therefore indicators of system bioavailability and concentration of a mesalazin in plasma are not important in respect of its therapeutic effectiveness, and serve more likely as factors of assessment of its safety.

Pharmacokinetics.

Absorption.

The greatest absorption of a mesalazin happens in a straight line and a colon.

Metabolism.

Mesalazin is metabolized as a presistemny way in a mucous membrane of intestines, and a system way in a liver, turning into pharmacological inactive N-acetyl-5-aminosalicylic acid (N-Ats-5-ASK). The nature of acetylation does not depend on acetylating patient's phenotype. In small degree acetylation can be carried out due to action of bacterial microflora of a large intestine. Communication with proteins of plasma of a mesalazin and N-Ats-5-ASK makes respectively 43 and 78%.

Removal.

Mesalazin and his metabolite N-Ats-5-ASK are removed through intestines (the main part,> 90%), is removed by kidneys to 7% (0,6% of the general dose are removed in the form of a mesalazin and to 6,3% — in the form of N-Ats-5-ASK metabolite), extent of removal of drug with bile is minimum.

Indications to use:

- aggravation of distal forms of ulcer colitis of average and easy severity;

- maintenance of remission of distal forms of ulcer colitis (long therapy).

Route of administration and doses:

Rektalno.

Suppositories rectal.

Adults. On the 2nd soup. on 250 mg or 1 soup. on 500 mg 3 times a day. At severe forms of a disease the dose can be doubled.

At the prolonged supporting treatment and for prevention of a recurrence — on 1 soup. on 250 mg 3 times a day.

Children. At body weight to 40 kg about a half of the dose recommended for adults is appointed (on 1 soup. on 250 mg 3 times a day); at body weight over 40 kg — a usual dose for adults.

Suspension rectal.

Contents of one tank are entered rektalno 1 time a day before going to bed (previously it is recommended to clear intestines). The daily dose makes 30–50 mg/kg. The maximum daily dose makes 3 g.

For prevention of a recurrence oral administration of Salofalk in the form of tablets in a dose of 15-30 mg/kg/days is recommended. The daily dose has to be divided into 2 receptions.

Foam rectal dosed.

If the doctor it is not offered differently, at adults and children 12 years are more senior drug usually is used once a day before going to bed (1 dose corresponds to 2 applications/pressing). If it is difficult to keep such volume of foam in a gut, the drug should be administered in two stages: 1 time for the night, and 1 more time — at night or early in the morning (after defecation).

For achievement of the best result administration of drug after bowel emptying (defecation) is recommended.

At the time of introduction drug Salofalk foam rectal, has to be the room temperature (20–25 °C).

1. To densely install the applicator on a cylinder head

2. To stir up a cylinder during 20 with for hashing of its contents.

3. At the first use to remove a protective uvula from the basis of the dosing head.

4. To turn a cap that the semicircular cut on a safety ring appeared on one line with a nozzle.

5. To place an index finger on a cap and to turn a cylinder upside down.

6. To enter the applicator into a rectum as it is possible more deeply. It is the best of all to put at the same time a leg on a chair or a stool. To enter the first part of a dose of drug to press a cap against the stop and to release slowly. To enter the second part of a dose of drug, again to press a cap and to release slowly. To wait 10–15 with, then to slowly take the applicator from a rectum.

7. After administration of foam to remove the applicator and to throw out it, having packed into a plastic package. For each new introduction of a dose of drug, it is necessary to use the new applicator.

8. After the procedure to wash up hands. It is necessary to try not to empty intestines till next morning.

At receipt in hospital or consultations with other doctors it is necessary to report to them about use of this drug.

The therapeutic effect is reached at regular use of drug Salofalk foam rectal.

Duration of a course of treatment is selected the doctor individually.

As a rule, the aggravation of easy forms of ulcer colitis can be stopped during 4–6 weeks. After this term it is recommended to visit the attending physician for the solution of a question of purpose of a peroral form of a mesalazin for a maintenance therapy.

Features of use:

For all rectal forms.

Before an initiation of treatment and in the course of its carrying out at the discretion of the attending physician it is necessary to determine parameters of a functional condition of a liver (such as activity of ALT or nuclear heating plant). Monitoring procedure is recommended usually in 14 days after an initiation of treatment, then 2-3 more times at an interval of 4 weeks.

If results of analyses are normal, it is necessary to conduct control researches each 3 months. If emergence of additional symptoms is noted, control researches need to be carried out immediately.

For foam rectal in addition.

Contents of a container are under high pressure. The cylinder should not be subjected to impact of a sunlight and to heat to temperature more than 50 °C. To open and puncture a cylinder, and also to burn the empty used cylinders inadmissibly. Not to use near naked flame or the heated objects.

Influence on ability to drive the car or to perform the works demanding the increased speed of physical and mental reactions. Impact of drug on ability to driving and control of mechanisms is not registered.

Side effects:

Typical side effects (arise less than at 1 of 10 patients):

- discomfortable feelings in an abdominal cavity.

Unusual side effects (arise less than at 1 of 100 patients):

- discomfort in an anus, irritation in scopes, painful desires to bowel emptying.

Rare side effects (arise less than at 1 of 1000 patients)

From a nervous system: headache, dizziness.

From a GIT: abdominal pain, diarrhea, abdominal distention, nausea and vomiting.

Very rare side effects (arise less than at 1 of 10000 patients)

From blood and lymphatic system: the fever, a pharyngalgia, an indisposition connected with disturbance of quantity of blood cells. Changes of quantity of blood cells (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia).

From immune system: allergic dieback, medicinal fever, bronchospasm, peri-and myocarditis, acute pancreatitis, allergic alveolitis, system lupus erythematosus, pan-colitis.

From a nervous system: numbness and a pricking in brushes and feet (peripheral neuropathy).

From a liver and biliary tract: changes of functional parameters of a liver (increase in level of transaminases and parameters of a cholestasia), hepatitis, cholestatic hepatitis.

From skin and hypodermic fabrics: alopecia (hair loss).

From skeletal and muscular system and connecting fabric: mialgiya, arthralgia.

From kidneys and urinary tract: renal failures, including – acute and chronic intersticial nephrite, a renal failure.

From reproductive system: oppression of formation of spermatozoa (it is recovered after drug phase-out).

If any of the specified phenomena proceeds hard, or there were phenomena which are not specified in this instruction, it is necessary to report about it to the doctor.

Interaction with other medicines:

It is not described.

Contraindications:

- hypersensitivity to salicylic acid and its derivatives or other components of drug;

- blood diseases;

- a peptic ulcer of a stomach and duodenum in an aggravation stage;

- deficit glyukozo-6-fosfatdegidrogenazy;

- hemorrhagic diathesis;

- heavy renal/liver failure;

- lactation period;

- last 4 weeks of pregnancy;

- children's age (up to 2 years).

With care: diseases of lungs, including bronchial asthma.

Overdose:

Symptoms: nausea, vomiting, weakness, drowsiness.

Treatment: symptomatic therapy.

Storage conditions:

In the place protected from light, at a temperature not above 25 °C.

To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Suppositories rectal, 250 or 500 mg. On the 5th soup. in the blister the laminated PVH/PENP; on 2 or 6 blisters in a pack cardboard.

Suspension of rectal, 2 g / 30 ml or 4 g / 60 ml. On 30 or 60 ml in the white, round contracting bottles from dense PE closed by the greased tip of the rectal applicator and a protective cover. The bottle is placed in planimetric packaging from the film thermowelded by PVC and the paper laminated with an aluminum covering. 7 bottles of PE placed in planimetric packaging in a cardboard pack.

The foam rectal dosed 1 g / application. On 14 applications (7 doses) in the aluminum cylinder varnished from within, supplied with the portioning device in a set with the special applicators from PVC supplied with protective caps, and PE packages for the used applicators. The applicator is covered with the lubricant consisting of mix of white soft paraffin and a liquid paraffin (7:3). 1 cylinder, 14 applicators and 14 PE packages in a cardboard pack.