Pentasa - instructions for use, dose, side effects, contraindications

Composition:For 1 tablet:
active substance - mesalazine 500 mg, Excipients - microcrystalline cellulose 207 mg, povidone 25 mg, talc 9 mg, ethyl cellulose 6-9 mg, magnesium stearate 1 mg.

Description:The tablets are round in shape, white with a grayish shade of color with numerous inclusions of light brown color with a facet, risk and engraving "500 mg" on one side and "PENTASA" on the other.

Pharmacotherapeutic group:Antimicrobial and anti-inflammatory intestinal.

ATX: & nbsp

A.07.E.C.02 Mesalazine

A.07.E.C Aminosalicylic acid and its analogues

Pharmacodynamics:Mesalazine - 5-aminosalicylic acid - is an active component of sulfasalazine. The therapeutic effect of mesalazine after oral or rectal administration is largely due to local effects on inflamed intestinal tissue, rather than systemic action.
The therapeutic effect of mesalazine is manifested with local contact with the affected mucosa of the intestine.
Mesalazine inhibits leukocyte chemotaxis, reduces the production of cytokines and leukotriene, and also reduces the formation of free radicals in inflamed intestinal tissue. But the exact mechanism of the action of mesalazine is not fully understood.

Pharmacokinetics:Suction: After taking the tablet, the Pentasa® preparation breaks down into microgranules that act as independent forms of the sustained-release preparation. This provides a therapeutic effect of the Pentasa® preparation all the way from the duodenum to the rectum at any pH value.Microgranules reach the duodenum within an hour after taking the tablet. The time of passage of the drug through the small intestine averages 3-4 hours.
Distribution: about 30-50% of the dose is absorbed, mainly in the small intestine. The maximum concentration of mesalazine in plasma is reached 1 hour after administration and lasts up to 4 hours, gradually decreasing.
Metabolism: mesalazine is acetylated in the intestinal mucosa and in the liver, and also, to a small extent, enterobacteria, forming the main metabolite N-acetyl-5-aminosalicylic acid. 43% of mesalazine and 73-83% of the metabolite binds to plasma proteins. Mesalazine and its metabolite does not penetrate the blood-brain barrier, but penetrate into breast milk. The clearance of mesalazine is 18 l / h. When taking high doses (up to 1500 mg / day), a cumulative effect can be observed.
Excretion: the half-life of mesalazine from the plasma is approximately 40 minutes, the metabolite - about 70 minutes. Mesalazine and its metabolites are excreted from the body with urine and feces.

Indications:- Ulcerative colitis (exacerbation of mild to moderate ulcerative colitis, maintenance of remission and / or prolonged therapy of ulcerative colitis),
- Crohn's disease.

Contraindications:- Hypersensitivity to mesalazine and other components of the drug,
- Severe liver and / or kidney damage,
- Peptic ulcer of the stomach or duodenum,
- Hemorrhagic diathesis,
- The last 2-4 weeks of pregnancy and lactation,
- Children under 2 years.
If you have any of these diseases, consult a doctor before taking the drug.

Carefully:With caution, the drug should be prescribed to patients who are allergic to salicylates, since hypersensitivity reactions to sulfasalazine, as well as to patients with impaired lung function, in particular, with bronchial asthma, are possible.
Caution should be exercised when administering Pentasa® to patients with mild / moderate renal / hepatic insufficiency, since a decrease in the elimination rate and an increase in the systemic concentration of mesalazine increases the risk of kidney damage.

Pregnancy and lactation:The drug can be used during pregnancy, when the potential benefit of its use for the mother exceeds the possible risk of adverse effects on the fetus.In the last 2-4 weeks of pregnancy, the drug should be withdrawn.
Mesalazine penetrates the placental barrier and is excreted in breast milk. Therefore, while taking Pentasa®, breastfeeding should be discontinued.

Dosing and Administration:Tablets should be taken after eating without chewing. To facilitate swallowing, the tablet can be divided into several parts or dissolved in water or juice just before taking.
Ulcerative colitis
Acute period: 2 tablets 2-4 times a day.
Maintenance therapy: 1 tablet 2-3 times a day.
Crohn's disease
Acute period: 2 to 4 tablets 4 times a day.
Maintenance therapy: 2-4 tablets 2 times a day or 2-3 tablets 3 times a day.
Children
The dose is selected individually, usually 20-30 mg of mesalazine per 1 kg of body weight per day in several doses.

Side effects:Most often when using Pentasa®, there is diarrhea (3%), nausea (3%), abdominal pain (3%), headache (3%), vomiting (1%) and skin rashes (1%).

	Often (> 1% and <10%)	Rarely (> 0.01% and <1.0%)	Rarely (<0.01%, including isolated cases)
From the side bodies hematopoiesis			Eosinophilia, anemia, leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia
From the side immune systems			Hypersensitivity reactions, drug fever, angioedema
From the nervous system		Goalsaboutcircling	Peripheral neuropathy, benign intracranial hypertension
From the side of the cardiovascular system *		Myocarditis, pericarditis
From the respiratory system *			Shortness of breath, cough, allergic alveolitis, pulmonary eosinophilia, pulmonary infiltration, pneumonia, bronchospasm
From the digestive system	Diarrhea, pain in the belly, nausea, vomiting, flatulence	Increase content amylase, pancreatitis *	Exacerbation of colitis symptoms
From the hepatobiliary system			Increased levels of hepatic enzymes and bilirubin, hepatotoxicity * (hepatitis, hepatosis, cirrhosis, hepatic insufficiency)
From the skin	Hives, eczema		Photosensitivity, reversible alopecia

From the musculoskeletal system		Myalgia, arthralgia
From the side		Interstitial nephritis *,
urine		nephrotic syndrome, changes
excretory		color urine, transient renal
systems		failure
Other	Headache,
	fever

(*) The mechanism of development of adverse reactions, presumably, is allergic.
If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:Cases of overdose with Pentasa® are rare. Specific antidotes are absent. It is recommended to wash the stomach and take measures to enhance diuresis. In the case of the development of acidosis, alkalosis or dehydration, it is necessary to restore the acid-base and water-electrolyte balance. With signs of hypoglycemia, dextrose is recommended.

Interaction:With the simultaneous administration of Pentasa® with azathioprine or mercaptopurine, the risk of suppression of bone marrow function (leukopenia, thrombocytopenia, erythrocytopenia / anemia or pancytopenia) is increased. Simultaneous administration of Pentasa® and other drugs with nephrotoxicity, for example, non-steroidal anti-inflammatory drugs (NSAIDs) and azathioprine, increases the risk of side effects slowing down the absorption of cyanocobalamin (vitamin B₁₂), enhances hypoglycemic action of sulfonylurea derivatives, ulcerogenicity of glucocorticosteroids, toxicity of methotrexate, weakens furosemide activity,spironolactone, sulfonamides, rifampicin, enhances the effect of anticoagulants, increases the effectiveness of uricosuric drugs (tubular secretion blockers).

Special instructions:In case of acute symptoms of drug intolerance (muscle spasms, abdominal pain, fever, severe headache and skin rashes) or signs of liver and / or kidney dysfunction, Pentasa® should be stopped!
During the course of treatment with Pentasa®, creatinine should be monitored regularly in the blood.

Effect on the ability to drive transp. cf. and fur:In case of side effects (dizziness, nausea), it is not recommended to drive and other mechanisms requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Long-acting tablets 500 mg.

Packaging:10 tablets per blister of aluminum foil. By 2, 3, 5, 6, 9 or 10 blisters with instructions for use in a cardboard box.
For 50 tablets in a plastic bottle with a screw cap, sealed with a thermo film, in a cardboard box with instructions for use.On the cardboard pack, it is possible to apply a sticker (s) to control the first opening.

Storage conditions:At a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:3 years.
Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N010197

Date of registration:16.07.2010 / 07.08.2015

Expiration Date:Unlimited

The owner of the registration certificate:Fering International Center S.A.Fering International Center S.A. Switzerland

Manufacturer: & nbsp

FERRING INTERNATIONAL CENTER, S.A. Switzerland

Representation: & nbspFERRING PHARMACEUTICALS LLCFERRING PHARMACEUTICALS LLCRussia

Information update date: & nbsp2016-09-21

Illustrated instructions

Instructions

Pentasa (Pentasa)