Pentas

Active material: Mesalazine
When ATH: A07EC02
CCF: The drug with anti-inflammatory action, used to treat Crohn's disease and ulcerative colitis
ICD-10 codes (testimony): K50, K51
When CSF: 11.13.01
Manufacturer: FERRING A/S (Denmark)

Pharmaceutical form, composition and packaging

Sustained-release tablets white with a grayish tint of color, with numerous intersperseds of light brown color, Correct round shape, chamfered, risk and inscription “500 mg” on one side and “Pentasa” – another.

Excipients: povidone, ethyl cellulose, magnesium stearate, talc, microcrystalline cellulose.

10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

The drug with anti-inflammatory action, used to treat Crohn's disease and ulcerative colitis.

Has a local anti -inflammatory effect, due to inhibiting the activity of neutrophilic lipoxygenase and synthesis of prostaglandins and leukotrienes. Slow down migration, degeneration, Fagocytosis of neutrophils, as well as the secretion of immunoglobulin lymphocytes.

Has an antibacterial effect in relation to E. coli and some cocks (manifests itself in the colon).

Has an antioxidant effect (due to the ability to contact free oxygen radicals and destroy their).

Reduces the risk of relapse in Crohn's disease, especially in patients with Ileite with a long duration of the disease.

The therapeutic effect of mesalazin is manifested as a result of local contact of the drug with the intestinal mucosa. After administration, the tablet breaks down into microgranulas, acting as independent forms of the drug with slow release of mesalazin. This provides the therapeutic effect of the drug from duodenum to the rectum at any pH values. Microcranulas reach the duodenum during the first hour after taking the tablet. The passage of the drug in an intact small intestine when administered orally is carried out during 3-4 no.

Pharmacokinetics

Absorption and distribution

About 30-50% The dose is absorbed, mainly, small intestine.

Binding a mesalazine with plasma proteins – 43%, and n-acetyl-5-aminosalicylic acid is 73-83%.

Mesalazine and its metabolites do not penetrate through the GEB. Cumulative properties occur when using high doses of the drug – 1500 mg / day.

Metabolism and excretion

Mesalazine is acetyline in the intestinal mucosa, in roasted and, to a small degree, – enterobacteria, Forming N-acetyl-5-aminosalicylic acid.

Clearance of mesalazin after V/in introduction at the dose 500 mg of 18.0 l / h.

Mesalazine and its metabolite are released with breast milk, urine and feces.

Testimony

- Nespetsificheskiy yazvennыy colitis;

- Crohn's disease.

Dosage regimen

Pentas tablets^® Swear, without chewing. To facilitate swallowing, the tablet can be divided into several parts or dissolved in input or juice immediately before taking.

The dose of the drug is selected individually.

The maximum daily dose is 6-8 g / day.

The average duration of treatment is 8-12 weeks. The maximum duration of treatment, including supportive and controversial therapy is not limited. The criterion for the effectiveness of the therapy is the achievement of clinical and endoscopic remission.

Side effect

From the digestive system: nausea, vomiting, heartburn, diarrhea, decreased appetite, abdominal pain, dry mouth, stomatitis, increase in liver transaminases, hepatitis, pancreatitis.

Cardio-vascular system: palpitations, tachycardia, increase or decrease in blood pressure, chest pain, breathlessness, perikardit, miokardit.

From the central and peripheral nervous system: headache, noise in ears, dizziness, polyneuropathy, tremor, depression.

From the urinary system: proteinuria, hematuria, oligurija, anurija, kristallurija, nephrotic syndrome.

From the hematopoietic system: eozinofilija, anemia (incl. hemolytic, megaloblastnaya, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoproteinemia.

Allergic reactions: skin rash, itch, dermatosis (pseudoaterromosity), bronchospasm.

Other: weakness, Mumps, lupus-like syndrome, oligospermatism, alopecia, decrease in production of tear fluid, photosensitivity.

Contraindications

- Blood disorders;

- Gastric ulcer and duodenal ulcer;

- Deficiency of glucose-6-fosfatdegidrogenazы;

- Gyemorragichyeskii diatyez;

- Severe renal insufficiency;

- Severe hepatic impairment;

- The latter 2-4 week of pregnancy;

- Lactation;

- Children up to age 2 years;

- Hypersensitivity to the drug.

FROM caution The drug should be used in the first trimester of pregnancy, with hepatic and / or renal insufficiency.

Pregnancy and lactation

Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.

Mesalazine penetrates through the placental barrier, but the limited experience in the use of the drug during pregnancy does not allow to evaluate possible side effects.

Mesalazine is released with breast milk in concentration below, than in the blood of women, Whereas metabolite (Acetyl-Mesalazin) found in a similar or higher concentration.

If necessary, use during lactation should decide the issue of termination of breastfeeding.

Cautions

Treatment of patients with impaired liver or kidneys is possible only after assessing the degree of their severity.

Throughout the course of treatment and, especially, At its beginning, the function of the kidney function should be regularly controlled (Creatinin level in the blood).

If pericarditis is suspected, myocarditis and changes in the formula of blood should be interrupted by treatment. Manifestations of the above adverse reactions can serve as pronounced pathological changes in the composition of the blood – increased bleeding, subcutaneous hemorrhage, sore throat and fever; In pericardials and/or myocardials – fever and pain behind the sternum combined with shortness of breath.

In some cases, an allergic reaction to sulfasalazine is possible to develop intolerance to the drug pentas^® (The risk of allergies to salicylates).

Patients, are “slow acetylators”, have an increased risk of side effects.

It is possible to stain urine and tear fluid in yellow-orange color, staining of soft contact lenses.

Effects on ability to drive vehicles and management mechanisms

The drug does not affect the ability to drive vehicles and management mechanisms.

Overdose

Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.

Treatment: gastric lavage, appointment of laxatives, simptomaticheskaya therapy.

Drug Interactions

With the simultaneous use of pentas^® enhances the hypoglycemic effect of sulfanilicochene derivatives, Ulcerogery GKS, toxicity of methotrexate and the action of anticoagulants.

With the simultaneous use of pentas ^®Weakens the activity of furosemide, spironolactone, sulfonamides, rifampicin.

With the simultaneous use of pentas^® increases the effectiveness of uricosuric drugs.

With the simultaneous use of pentas^® Slow down the absorption of cyancobalamin.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, place at a temperature not higher. Shelf life – 3 year.