Composition, form of production and packaging
Foam rectal dosed from greyish-white to slightly reddish-violet, creamy, resistant.
1 application
mesalazine (5-ASA) 1 g
[PRING] 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, propellants (propane / isobutane / butane at a pressure of about 2.5 bar) 0.176 g.
14 applications (7 doses) - aluminum cylinders (1), lacquered from the inside, equipped with a dosing device, complete with special applicators made of PVC (14 pcs.), Equipped with protective caps and plastic bags (14 pcs.) For used applicators - packs cardboard .
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
The drug for rectal administration. 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.
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.
It is important to consider that mesalazine has only a local anti-inflammatory effect, since mesalazine 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
Suction
The greatest absorption of mesalazine occurs in the rectum and colon.
Metabolism
Mesalazine undergoes presystemic metabolism in the intestinal mucosa and systemic metabolism in the liver with the formation of a pharmacologically inactive metabolite of 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 connection with the 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 (main 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 metabolite N-Ac-5 -ASK), the degree of excretion of the drug with bile is minimal.
INDICATIONS
- exacerbation of distal forms of ulcerative colitis of moderate and mild degrees of severity;
- maintenance of remission of distal ulcerative colitis (long-term therapy).
DOSING MODE
The drug is applied rectally.
Adults and children over 12 years of age the drug is usually prescribed 1 time / day before bedtime (1 dose corresponds to 2 applications / strokes). If such a volume of foam is difficult for the patient to keep in the rectum, the drug should be administered in two stages: once a night, and once again - 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).
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, the doctor decides on the appointment of mesalazine for oral administration as maintenance therapy.
The therapeutic effect is achieved with regular use of the drug.
Rules of drug administration
At the time of administration, it is necessary that the salofalk rectal foam preparation be at room temperature (20-25 В° 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 tongue from the base 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 / application of the drug, push the cap all the way to the stop and slowly release. To enter the second part of the dose / application of the drug, 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. The patient should not empty the intestines until the next morning.
SIDE EFFECT
From the digestive system: very often (<1/10): a feeling of discomfort in the abdominal cavity; often (<1/100) - discomfort in the anus, irritation in the area of ​​application, painful urge to empty the intestine; rarely (<1/1000) - abdominal pain, diarrhea, bloating, nausea and vomiting.
From the liver and bile ducts: very rarely (<1/10 000) - changes in the functional parameters of the liver (increased levels of transaminases and parameters of cholestasis), hepatitis, cholestatic hepatitis.
From the side of the nervous system: rarely (<1/1000) - headache, dizziness; Very rarely (<1/10 000) - numbness and tingling in the hands and feet (peripheral neuropathy).
On the part of the blood and lymphatic system: very rarely (<1/10 000) - fever, sore throat, malaise associated with a violation of the number of blood cells, aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia.
From the side of the immune system: very rarely (<1/10 000) - allergic exanthema, drug fever, bronchospasm, peri- and myocarditis, acute pancreatitis, allergic alveolitis, systemic lupus erythematosus, pancolitis.
From the skin and subcutaneous tissues: very rarely (<1/10 000) - alopecia.
From the musculoskeletal system: very rarely (<1/10 000) - myalgia, arthralgia.
From the urinary system: very rarely (<1/10 000) - renal dysfunction, incl. acute and chronic interstitial nephritis, renal failure.
On the part of the reproductive system: very rarely (<1/10 000) - inhibition of sperm formation (restored after discontinuation of use of the drug).
The patient should consult a doctor if any of these adverse reactions occur severely, or if there are any other adverse reactions.
CONTRAINDICATIONS
- Blood diseases;
- Stomach ulcer in the phase of exacerbation;
- Duodenal ulcer in the phase of exacerbation;
- hemorrhagic diathesis;
- severe renal insufficiency;
severe hepatic impairment;
- deficiency of glucose-6-phosphate dehydrogenase;
- lactation period;
- the last 4 weeks of pregnancy;
- children's age till 12 years;
- hypersensitivity to the components of the drug;
- Hypersensitivity to salicylic acid and its derivatives.
Use with caution in lung diseases, incl. with bronchial asthma.
PREGNANCY AND LACTATION
When pregnant, suspected pregnancy, planning pregnancy, breastfeeding, patients should consult with their doctor.
Contraindicated in the last 4 weeks of pregnancy. Salofalk should be used during pregnancy only in cases where the potential benefit of therapy for the mother exceeds the possible risk to the fetus.
Do not use the drug during breastfeeding. The active substance and its metabolites can be excreted in breast milk. If it is necessary to prescribe Salofalka during lactation, the question of stopping breastfeeding should be resolved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under 12 years.
SPECIAL INSTRUCTIONS
Before the start 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). 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.
The contents of the container are under high pressure. The balloon should not be exposed to sunlight and heated to a temperature of more than 50 В° 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.
At hospitalization or consultations the patient should inform the doctor about application of Salofalk.
Impact on the ability to drive vehicles and manage mechanisms
Effects of the drug on the ability to drive vehicles and control mechanisms are not recorded.
OVERDOSE
Symptoms: nausea, vomiting, weakness, drowsiness.
Treatment: symptomatic therapy.
DRUG INTERACTION
Most of the possible drug interactions are based on theoretical assumptions.
With the simultaneous use of the drug with indirect anticoagulants, it is possible to enhance their effect: an increased risk of gastrointestinal bleeding.
When used simultaneously with GCS, there may be an increase in unwanted reactions from the stomach.
With simultaneous use with sulfonylureas, hypoglycemic effect may be increased.
With simultaneous use with methotrexate may increase the toxic effect of methotrexate.
When used simultaneously with probenecid, sulfinpyrazone, a reduction in the excretion of uric acid is possible.
With simultaneous use with spironolactone, furosemide, a weakening of the diuretic effect is possible.
When used simultaneously with rifampicin, the tuberculostatic effect may be weakened.
In patients who are simultaneously receiving treatment with azathioprine or mercaptopurine, the possible increase in the myelosuppressive effect of azathioprine and mercaptopurine should be borne in mind.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C; Do not freeze. Shelf life - 2 years.
After opening the container, it should be used within 12 weeks.
