Pentasa

General characteristics. Structure:

Active agent: месалазин (5-ACK) 500 mg

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

Pharmacological properties:

The drug with antiinflammatory action used for treatment of a disease Krone and NYaK.

Possesses the local antiinflammatory action caused by inhibition of activity of a neutrophylic lipoxygenase and synthesis of prostaglandins and leukotrienes. Slows down migration, degranulation, phagocytosis of neutrophils, and also secretion of immunoglobulins lymphocytes.
Possesses antibacterial action concerning colibacillus and some cocci (it is shown in a large intestine).
Has antioxidant effect (due to ability to contact free oxygen radicals and to destroy them).
Reduces risk of a recurrence at a disease Krone, especially patients with an ileitis with big duration have diseases.
Medical action of a mesalazin is shown as a result of local contact of drug with a mucous membrane of intestines. After intake the tablet breaks up to the microgranules operating as independent forms of drug with the slowed-down release of a mesalazin. It provides therapeutic effect of drug on an extent from duodenal to a rectum at any values рН. Microgranules reach a duodenum within the first hour after reception of a tablet. The drug passage on the unimpaired small bowel at intake is carried out during 3-4 h.

Pharmacokinetics. Absorption and distribution.
About 30-50% of the accepted dose are soaked up, mainly, in a small bowel.
Linkng of a mesalazin with proteins of plasma - 43%, and N-acetyl-5-aminosalicylic acid makes 73-83%.
Mesalazin and his metabolites do not get through GEB. Cumulative properties take place at use of high doses of drug - 1500 mg/days.

Metabolism and removal. Mesalazin is exposed to acetylation in a mucous membrane of intestines, in a liver and, in small degree, - enterobakteriya, forming N-acetyl-5-aminosalicylic acid.
The clearance of a mesalazin in/in introductions in a dose of 500 mg makes later 18.0 l/hour.
Mesalazin and his metabolite are allocated with breast milk, urine and a stake.

Indications to use:

— nonspecific ulcer colitis;
— disease Krone.

Route of administration and doses:

Tablets should be swallowed, without chewing. For simplification of a proglatyvaniye the tablet can be divided into several parts or to dissolve input or juice just before reception.
The dose of drug is selected individually.

Patients	Ulcer colitis		Disease Krone
	Aggravation stage	Maintenance therapy	Aggravation stage	Maintenance therapy
Adults	to 4 g/days in stages	2 g/days in stages	to 4 g/days in stages
Children	20-30 mg/kg/days in stages

The maximum daily dose of drug makes 6-8 g/days.

The average duration of treatment makes 8-12 weeks. The maximum duration of treatment, including the supporting and antirecurrent therapy is not limited. Criterion of efficiency of the carried-out therapy is achievement of kliniko-endoscopic remission.

Features of use:

Treatment of patients with abnormal liver functions or kidneys perhaps only after assessment of degree of their expressiveness.

During all course of treatment and, especially, at its beginning it is regularly necessary to control function of kidneys (creatinine level in blood).

At suspicion on development of a pericardis, myocarditis and changes of a blood count it is necessary to interrupt treatment. As manifestations of the above-stated side reactions can serve at the expressed pathological changes of composition of blood - the raised bleeding, hypodermic hemorrhages, a pharyngalgia and fever; at a pericardis and/or myocarditis - fever and pains behind a breast in combination with an asthma.

In certain cases allergic reaction to Sulfasalazinum development of intolerance and to the drug Pentasa® is possible (risk of an allergy to salicylates).

Patients, being "slow acetylizers", have the increased risk of development of side effects.

Coloring of urine and the lacrimal liquid in yellow-orange color, a prokrashivaniye of soft contact lenses is possible.

Influence on ability to driving of motor transport and to control of mechanisms
Drug does not influence ability to driving of motor transport and control of mechanisms.

Side effects:

From the alimentary system: nausea, vomiting, heartburn, diarrhea, a loss of appetite, abdominal pains, dryness in a mouth, stomatitis, increase in activity of hepatic transaminases, hepatitis, pancreatitis.

From cardiovascular system: a heart consciousness, tachycardia, increase or decrease in the ABP, pain behind a breast, an asthma, a pericardis, myocarditis.

From TsNS and peripheral nervous system: headache, sonitus, dizziness, polyneuropathy, tremor, depression.

From an urinary system: proteinuria, hamaturia, oliguria, anury, crystalluria, nephrotic syndrome.

From system of a hemopoiesis: eosinophilia, anemia (including hemolitic, megaloblastny, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoproteinemia.

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

Others: weakness, parotitis, volchanochnopodobny syndrome, oligospermatism, alopecia, reduction of products of the lacrimal liquid, photosensitization.

Interaction with other medicines:

At simultaneous use of Pentasa® strengthens hypoglycemic action of derivatives of sulfanylurea, GKS ultserogennost, toxicity of a methotrexate and effect of anticoagulants.

At simultaneous use of Pentasa® weakens activity of furosemide, Spironolactonum, streptocides, rifampicin.

At simultaneous use of Pentasa® increases efficiency of uricosuric drugs.

At simultaneous use of Pentasa® slows down cyanocobalamin absorption.

Contraindications:

— blood diseases;
— peptic ulcer of a stomach and duodenum;
— deficit glyukozo-6-fosfatdegidrogenazy;
— hemorrhagic diathesis;
— renal failure of heavy degree;
— liver failure of heavy degree;
— last 2-4 weeks of pregnancy;
— lactation period;
— children's age up to 2 years;
— hypersensitivity to drug components.

With care it is necessary to use drug in the I trimester of pregnancy, at a liver and/or renal failure.
Use of the drug PENTASA® at pregnancy and feeding by a breast
Use of drug at pregnancy is possible only in that case when the estimated advantage for mother surpasses potential risk for a fruit.
Mesalazin gets through a placental barrier, but limited experience of use of drug at pregnancy does not allow to estimate possible side effects.
Mesalazin is allocated with breast milk in concentration below, than in the woman's blood whereas the metabolite (acetyl-mesalazin) is found in similar or higher concentration.
In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Use at abnormal liver functions
Use of drug at a liver failure of heavy degree is contraindicated.

Use at renal failures
Use of drug at a renal failure of heavy degree is contraindicated.

Use for children
Drug is contraindicated to children up to 2 years.

Overdose:

Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.
Treatment: gastric lavage, purpose of purgatives, symptomatic therapy.

Storage conditions:

List B. Drug should be stored in unavailable to children, the place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets пролонгир. actions of 500 mg: 50 or 100 pieces.