Salofalk rectal suppositories 500 mg strip No. 10

Instructions for Salofalk rectal suppositories 500 mg strip No. 10

Composition

active ingredient: mesalazine (5-aminosalicylic acid);

1 suppository contains 500 mg of mesalazine;

excipients: solid fat, cetyl alcohol, docusate sodium.

Dosage form

Rectal suppositories.

Main physicochemical properties: suppositories from white to cream color, torpedo-shaped, with a uniform consistency and an undamaged, smooth surface.

Pharmacotherapeutic group

Gastrointestinal tract and metabolism. Antidiarrheals, intestinal anti-inflammatory/antimicrobial drugs. Intestinal anti-inflammatory drugs. Aminosalicylic acid and similar agents. Mesalazine.

ATX code A07ES02.

Pharmacological properties

Pharmacodynamics

Mechanism of action

The mechanism of anti-inflammatory action is unknown. In vitro studies suggest that inhibition of lipoxygenase may play a role.

An effect on prostaglandin concentrations in the intestinal mucosa has also been demonstrated. Mesalazine (5-aminosalicylic acid/5-ASA) may also act as a scavenger of reactive oxygen species.

Mesalazine, when administered rectally, acts predominantly locally on the mucosa and submucosa of the intestines.

Pharmacokinetics

General properties of mesalazine

Absorption

Absorption of mesalazine is highest in the proximal part of the intestine and lowest in its distal part.

Biotransformation

Mesalazine is metabolized both presystemically in the intestinal mucosa and in the liver to the pharmacologically inactive N-acetyl-5-aminosalicylic acid (N-Acetyl-5-ASA). Acetylation is apparently independent of the acetylation phenotype of the patient. Some acetylation also occurs by the action of bacteria in the large intestine. The protein binding of mesalazine and N-Acetyl-5-ASA is 43% and 78%, respectively.

Excretion

Mesalazine and its metabolite N-Ac-5-ASA are excreted in the faeces (major part), renally (varying between 20% and 50%, depending on the type of administration, pharmaceutical form and route of release of mesalazine) and biliaryly (minor part). Renal excretion occurs mainly in the form of N-Ac-5-ASA. About 1% of the total orally administered dose of mesalazine is excreted in breast milk, mainly in the form of N-Ac-5-ASA.

Features of Salofalk suppositories

Distribution

Scintigraphic studies with technetium-labeled Salofalk suppositories have shown a peak distribution of the suppository, which has melted at body temperature, after 2–3 hours. Distribution is primarily limited to the rectum and rectosigmoid colon. Salofalk suppositories are therefore particularly suitable for the treatment of proctitis (ulcerative colitis of the rectum).

Absorption

Both after a single dose and after several weeks of therapy with 500 mg mesalazine in the form of Salofalk suppositories three times a day, the peak plasma concentration of 5-ASA varied from 0.1 to 1.0 μg/ml, while the range of the same indicator for the main metabolite N-Ac-5-ASA was from 0.3 to 1.6 μg/ml. In some cases, the peak plasma concentration of 5-ASA was reached within the first hour after administration.

Breeding

After a single dose of 500 mg mesalazine as a Salofalk suppository, approximately 11% (within 72 hours) and after several weeks or long-term therapy with 500 mg mesalazine as Salofalk suppositories three times a day, approximately 13% of the administered dose of 5-ASA was excreted in the urine. Approximately 10% of the administered single dose was excreted in the bile.

Indication

Treatment of exacerbations of ulcerative colitis limited to the rectum.

Contraindication

Hypersensitivity to mesalazine, to any of the components of the drug or to salicylates, gastric and duodenal ulcer in the acute stage, severe hepatic and/or renal failure, hemorrhagic diathesis.

Interaction with other medicinal products and other types of interactions

No specific drug interaction studies have been conducted.

In the case of simultaneous treatment with Salofalk and azathioprine, 6-mercaptopurine or thioguanine, the possible increase in the myelosuppressive effect of azathioprine, 6-mercaptopurine or thioguanine should be taken into account.

There is evidence that mesalazine may reduce the anticoagulant effect of warfarin.

Application features

At the discretion of the physician, blood tests (complete blood count; liver function tests such as ALT or AST; serum creatinine) and urine tests (test strips, sediment) should be performed before and during treatment. It is recommended that tests be performed approximately 14 days after the start of treatment and then 2–3 times at 4-week intervals.

If the test results are normal, routine checks can be done every 3 months, but if other additional symptoms appear, tests should be done urgently.

It should be used with caution in patients with impaired liver function.

If renal function impairment occurs during treatment, the toxicity of mesalazine on renal function should be taken into account.

Patients with lung diseases, in particular asthma, should be under the supervision of a doctor during the course of treatment with Salofalk suppositories.

Patients who have had hypersensitivity reactions to drugs containing sulfasalazine should be under medical supervision from the very beginning of the course of treatment with Salofalk suppositories. If acute symptoms of intolerance appear, such as cramps, acute abdominal pain, fever, severe headache and rash, therapy should be discontinued immediately.

Ability to influence reaction speed when driving vehicles or other mechanisms

The use of Salofalk, 250 mg or 500 mg suppositories, has no or only minor influence on the ability to drive or use machines.

Use during pregnancy or breastfeeding

Pregnancy

There are no adequate data from the use of Salofalk suppositories in pregnant women. However, data from a limited number of exposed pregnancies indicate no adverse effects of mesalazine on pregnancy or on the health of the fetus and/or newborn. No other epidemiological data are available for this product. Only one case of renal failure in the newborn has been reported following prolonged use of high doses of mesalazine (2-4 g orally) during pregnancy.

Animal studies with oral administration of mesalazine do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development.

Salofalk suppositories should be used during pregnancy only if the expected benefit outweighs the possible risk.

Lactation

N-acetyl-5-aminosalicylic acid and, to a lesser extent, mesalazine are excreted in breast milk. There is currently only limited experience of use in women during breastfeeding. Hypersensitivity reactions in the breastfed infant, such as diarrhoea, cannot be excluded. Therefore, Salofalk suppositories should be used during breastfeeding only if the expected benefit to the mother outweighs the possible risk to the infant. If diarrhoea develops in the breastfed infant, breastfeeding should be discontinued.

Method of administration and doses

If you use Salofalk suppositories three times a day, they are inserted into the rectum in the morning, afternoon, and evening before bedtime.

The desired therapeutic result can only be achieved with regular and continuous use of Salofalk suppositories.

The duration of use is determined by the doctor.

Treatment of ulcerative colitis flare-ups

Depending on the individual clinical need, 2 suppositories of Salofalk 250 mg or 1 suppository of Salofalk 500 mg are administered rectally 3 times a day (equivalent to 1500 mg of mesalazine per day).

Maintaining remission of ulcerative colitis

1 suppository of Salofalk 250 mg is administered rectally 3 times a day (equivalent to 750 mg of mesalazine per day).

Children

There is insufficient data on the use of this medicine in children.

Overdose

There are reports of rare cases of overdose (e.g. intentional suicide by taking a high oral dose of mesalazine) which do not indicate renal or hepatic toxicity. There is no specific antidote, treatment should be symptomatic and supportive.

Adverse reactions

The following adverse reactions have been observed after administration of mesalazine:

*More detailed information is provided in the "Application Features" section.

Photosensitivity

There have been reports of severe reactions in patients with skin conditions such as atopic dermatitis and atopic eczema.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after a medicinal product has been authorised is very important. This allows the benefit/risk balance of the medicinal product to be monitored continuously. Healthcare professionals are asked to report any suspected adverse reactions via the Bundesinstitut für Arzneimittel und Medizinprodukte (Federal Institute for Medicines and Medical Devices).

Pharmacovigilance Department

Kurt-Georg-Kiesinger-Allee 3

53175 Bonn

www.bfarm.de

Expiration date

3 years.

Do not use after the expiration date indicated on the package.

Storage conditions

Keep out of the reach of children. Store at a temperature not exceeding 30 ° C. Store in the original package in order to protect from light.

Packaging

5 suppositories in a strip, 2 strips in a cardboard box.

Vacation category

According to the recipe.

Producer

Dr. Falk Pharma GmbH.

Location of the manufacturer and its business address

Leinenweberstrasse 5, 79108 Freiburg, Germany.