Pentasa

Pentasa – antiinflammatory and antimicrobic intestinal medicine with localization of action it is preferential in intestines at contact with the struck mucous.

Form of release and structure

• Tablets of the prolonged action: round, with a facet, white with a grayish shade and numerous light brown impregnations, on one party – an engraving of "500 mg" and dividing risk, on other party – an engraving of "PENTASA" (on 10 pieces in blisters from aluminum foil, in a pack of cardboard 2, 3, 5, 6, 9 or 10 blisters; on 50 pieces in plastic bottles, in a pack a cardboard 1 bottle);
• Granules of the prolonged action for intake: a cylindrical form, color from light brown to light gray (in bags from an aluminum foil / polyether / polyethylene of low density: on 1 g – 50, 60, 100, 120 or 150 pieces in a pack cardboard; on 2 g – 30, 50, 60 or 120 pieces in a pack cardboard);
• Suppositories rectal: oval, color from white with a yellowish-brown shade to white, with numerous light gray impregnations (on 5 or 7 pieces in blisters from aluminum foil, in packaging of 1, 2, 3, 4 or 6 blisters, 1 packaging in a pack cardboard, fingerstalls rubber hygienic can be included in the package);
• Suspension rectal: a suspension of white or light yellow color (on 100 ml in the bottles from polyethylene of low density corked by a tip with the valve providing a suspension effluence in one direction, hermetically soldered in the atmosphere of nitrogen in bags from aluminum foil; 7 bags of bottles in a pack cardboard, can be included in the package packages plastic hygienic).

Structure of 1 tablet:

• Active ingredient: месалазин – 0,5 g;
• Auxiliary components: povidone, talc, microcrystallic cellulose, magnesium stearate, ethyl cellulose.

Structure of 1 bag of granules:

• Active ingredient: месалазин – 1 g or 2 g;
• Auxiliary components: ethyl cellulose, povidone.

Composition of 1 suppository:

• Active ingredient: месалазин – 1 g;
• Auxiliary components: talc, macrogoal 6000, magnesium stearate, povidone.

Structure of 100 ml of suspension (1 bottle):

• Active ingredient: месалазин – 1 g;
• Auxiliary components: sodium disulphite, dinatrium of an edetat a dihydrate, acetate sodium trihydrate, the water purified (to 100 ml), the concentrated Acidum hydrochloricum to рН 4,6-5,0.

Indications to use

Tablets and Pentas's granules accept at a disease Krone and ulcer colitis.

Suppositories rectal apply in case of an ulcer proctitis, one of forms of ulcer colitis with defeat of distal departments of a large intestine.

Suspension rectal is recommended to use at an ulcer proctosigmoiditis and left-side ulcer colitis.

Contraindications

Absolute:

• Hemorrhagic diathesis;
• Heavy renal failures and/or liver;
• Stomach ulcer or duodenum;
• Pregnancy (in 2-4 weeks prior to delivery);
• Period of breastfeeding (lactation);
• Children's age up to 2 years (for tablets), up to 6 years (for granules); suppositories and suspension are contraindicated for use in pediatrics in connection with insufficiency of data;
• Hypersensitivity to a mesalazin and/or other components.

Relative (Pentasa is applied with care in connection with the increased risk of complications):

• Allergy to salicylates (reactions of hypersensitivity to Sulfasalazinum are possible);
• Dysfunctions of lungs, in particular, bronchial asthma;
• Renal/liver failure easy and moderate severity (increase in system concentration of a mesalazin and reduction in the rate of elimination increases risk of damage of kidneys);
• Pregnancy (except the period 2-4 weeks before childbirth) (drug is used according to indications, only in case of exceeding of potential advantage for mother over possible risk of adverse action for a fruit).

Route of administration and dosage

Tablets of the prolonged action
Pill is taken inside after meal, without chewing. If the patient cannot swallow a tablet entirely, it is allowed to divide it into several parts, or to dissolve in juice or water just before reception.

The recommended dosing mode for adults:

• Ulcer colitis: at an aggravation – 2 pieces 2-4 times a day; the supporting treatment – 1 piece 2-3 times a day;
• Disease Krone: at an aggravation – 2-4 pieces 4 times a day; the supporting treatment – 2-4 pieces 2 times a day or 2-3 pieces 3 times a day.

To children the individual dose of a mesalazin, usually at the rate of 0,02-0,03 g/kg of body weight a day in stages is selected.

Granules of the prolonged action
Granules accept inside after meal, without chewing. Contents of one bag should be poured out on language then to wash down with juice or water.

Daily dose of a mesalazin (is selected individually, it should be divided into several receptions):

• Adults: at an aggravation – to 4 g; the supporting treatment – 2-4 g;
• Children of 6 years and teenagers: at an aggravation – 0,02-0,03 g/kg of body weight, but no more than 4 g (the maximum single dose should not exceed 0,075 g/kg); the supporting treatment – 0,02-0,03 g/kg, maximum – no more than 2 g.

Reception of adult doses is also more recommended to children with body weight from 40 kg.

Duration of a course of therapy is determined by the attending physician.

Suppositories rectal
Rectal suppositories are intended for introduction to a rectum.

Manipulation is carried out after bowel emptying. It is necessary to use a rubber fingerstall for providing a gigiyenichnost of the procedure. For the purpose of introduction simplification suppository can be moistened with water then to enter into an anus before the termination of resistance of a muscular press. If for 10 minutes after introduction the candle leaves, it is required to repeat the procedure, using other suppository.

The recommended dosing: 1 pieces 1-2 times a day; the most admissible daily dose – 6-8 pieces.

Suspension rectal
Drug is used 1 time a day before going to bed in the form of an enema. It is desirable to empty intestines before holding a procedure.

The recommended daily dose – 1 g (1 bottle of 100 ml).

Just before use to open packaging, to shake up bottle contents. To tighten against the stop a tip with the valve providing a suspension effluence in one direction. To lay down sideways for implementation of the procedure and to accurately enter a tip as it is possible more deeply in a rectum.

The average duration of therapy by rectal drugs (suspension, suppositories) – 8-12 weeks, an indicator of its efficiency serves achievement of kliniko-endoscopic remission. The maximum duration of the course including the supporting and antirecurrent therapy is not limited.

Side effects

Side effects from use of a mesalazin from bodies and systems, according to gradation – it is frequent –> 1%-<10%; seldom –> 0,01%-<1%; very seldom – <0,01%, including isolated cases:

• Bodies of a hemopoiesis: very seldom – anemia, a leukopenia, an eosinophilia, a granulocytopenia, thrombocytopenia, a pancytopenia, an agranulocytosis;
• Immune system: very seldom – hypersensitivity reactions, a Quincke's edema, medicinal fever;
• Nervous system: seldom – dizziness; very seldom – benign intracranial hypertensia, a peripheral neuropathy;
• Cardiovascular system: seldom – a pericardis, myocarditis;
• Respiratory system: very seldom – cough, short wind, an allergic alveolitis, infiltration in lungs, a pulmonary eosinophilia, pneumonia, a bronchospasm;
• Alimentary system: often – diarrhea, an abdominal pain, nausea, vomiting, a meteorism; seldom – pancreatitis, increase in content of amylase; very seldom – an aggravation of symptoms of colitis;
• Gepatobiliarny system: very seldom – increase in level of bilirubin and liver enzymes, a hepatotoxic (a hepatosis, hepatitis, a liver failure, cirrhosis);
• Integuments: often – eczema, urticaria; very seldom – a reversible alopecia, a photosensitization;
• Musculoskeletal system: very seldom – an arthralgia, a mialgiya;
• Urinary system: very seldom – a nephrotic syndrome, intersticial nephrite, a tranzitorny renal failure, urine discolorations;
• Others: often – fever, a headache;
• Reactions in an injection site (suspension, suppositories): seldom – pain and irritation in an anus.

Most often owing to use of a mesalazin arise: diarrhea, nausea, an abdominal pain, a headache – to 3% of cases; vomiting and an enanthesis – to 1% of cases.

In case of aggravation of any side effects from specified in the instruction, or emergence of any other reactions which are not described in the instruction it is required to see behind consultation the attending physician.

Overdose cases mesalaziny are extremely rare (especially when using rectal means), its symptoms are: gastralgia, nausea, vomiting, drowsiness, weakness; the specific antidote does not exist.

Therapy is required to make fortunes a gastric lavage and to take measures for strengthening of a diuresis. At development of an alkalosis, acidosis or dehydration it is necessary to recover water and electrolytic and acid-base balance. In case of observation of signs of a hypoglycemia it is recommended to enter a dextrose.

Special instructions

At emergence of acute signs of intolerance of drug (such as muscular spasms, abdominal pains, fever, severe headache, skin rashes) or symptoms of a renal failure and/or a liver therapy needs to be interrupted.

It is required to carry out regular control of an indicator of creatinine to blood throughout all time of use of any form of production of drug of Pentas.

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

Patients are recommended to be careful at reception of tablets, granules and use of rectal suspension, managing vehicles and being engaged in other potentially dangerous types of activity which demand speed of psychomotor reactions and the increased concentration of attention as such side effects as nausea, weakness, dizziness, etc. can exert impact on them.

Medicinal interaction

At simultaneous use with mesalaziny:

• Azathioprinum or Mercaptopurinum – increase risk of suppression of function of marrow (thrombocytopenia, a leukopenia, a pancytopenia, erythrocytopenia/anemia);
• Non-steroidal anti-inflammatory drugs (NPVP), Azathioprinum and other nefrotoksichny means – increase risk of development of side effects from kidneys;
• Cyanocobalamine _{(B12 Vitamin)} – is slowed down absorption;
• Sulphonylurea derivatives – hypoglycemic action amplifies;
• Glucocorticosteroids (GKS) – the ultserogennost increases;
• The methotrexate – amplifies toxicity;
• Furosemide, Spironolactonum, streptocides, rifampicin – is weakened activity;
• Anticoagulants – action amplifies;
• Blockers of canalicular secretion (uricosuric means) – efficiency increases.

Terms and storage conditions

To store in unavailable to children, the dry, dark place at a temperature up to 25 °C.

Period of validity:

• Granules – 2 years;
• Tablets, suspension, suppositories – 3 years.