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

Composition:For 1 sachet:
dosage of 1.0 g:
active substance - mesalazine 1000 mg; auxiliary substances - ethylcellulose 4 mg - 15 mg, povidone 50 mg.
dosage of 2.0 g:
active substance - mesalazine 2000 mg; auxiliary substances: ethylcellulose 8 mg - 30 mg, povidone 100 mg.

Description:Cylindrical granules from light gray to light brown in color.

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.
PENTASY® granules are mesalazine microgranules coated with ethyl cellulose. The therapeutic effect of mesalazine after oral 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: when administered orally, Pentasa® granules break down into microgranules acting 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 drug. 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. Mesalazine is determined in the plasma already after 15 minutes after administration, the maximum concentration is reached 1 hour after intake and remains up to 4 hours, gradually decreasing within 12 hours.
- 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-amino-salicylic 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.
- excretion: The clearance of mesalazine is 18 l / h. When taking high doses (up to 1500 mg / day), a cumulative effect can be observed. The half-life of mesalazine is approximately 40 minutes, the metabolite is about 70 minutes.
Mesalazine and its metabolites are excreted from the body with urine and feces.

Indications:- Ulcerative colitis
- Crohn's disease

Contraindications:- Hypersensitivity to salicylates and other components of the drug
- Severe hepatic or renal insufficiency
- Peptic ulcer of the stomach or duodenum
- Hemorrhagic diathesis
- Children under 6 years
If you have any of these diseases, consult a doctor before taking the drug.

Carefully:With caution, the drug should be given to patients with impaired lung function, in particular, with bronchial asthma.
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 Pentasa® preparation may be used during pregnancy only if the expected benefit for the mother prevails over the potential risk to 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, at the time of taking Pentasa® breastfeeding should be discontinued.

Dosing and Administration:Granules should be taken after meals without chewing. Pour the contents of one sachet into the tongue and drink with water or juice.
Children over 6 years and adolescents: dosage is selected individually.
The recommended dose in the acute period of 20 - 30 mg mesalazine per kilogram of body weight per day in divided doses, the maximum single dose not exceed 75 mg / kg, the maximum daily dose of not more than 4, the recommended maintenance dose is 20 - 30 mg / kg / day, the maximum daily dose is not more than 2 g. Children with a body weight of more than 40 kg are recommended to prescribe doses for adults.
Adults: dosage is selected individually. The recommended dose in the period of exacerbation to 4 g per day, divided into several doses, maintenance therapy 2 - 4 g per day, divided into several receptions.
The duration of therapy is determined by the attending physician.

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 (> 1/100 and <1/10

Rarely

(> 1/10000 and <1/1000)

Rarely

(<1/10000, including isolated cases)

On the part of the organs of hematopoiesis

Eosinophilia, anemia (including aplastic), leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia

From the side immune systems			Hypersensitivity reactions, drug fever, angioedema
From the nervous system		Dizziness	Peripheral neuropathy, benign intracranial hypertension (in patients at pubertal age)
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, interstitial lung disease
From the digestive system	Diarrhea, abdominal pain, nausea, vomiting, flatulence	Increase content amylase, pancreatitis *	Exacerbation of colitis symptoms
From the hepatobiliary system			Increased activity of hepatic enzymes and bilirubin, hepatotoxicity * (hepatitis, hepatosis, cirrhosis, hepatic insufficiency)
From the skin	Hives, erythema		Photosensitivity, reversible alopecia
From the side of the support impellent apparatus			Myalgia, arthralgia
From the side of the urine dividerьsystem			Interstitial nephritis *, nephrotic syndrome, changes in urine color, transient renal failure
Other	Headache, fever

(*) The mechanism of development of adverse reactions, presumably, is allergic.

If any of the side effects indicated in the instruction are aggravated, or you notice any other side effects not listed in the instructions, inform the doctor about it.

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, dehydration, hyperventilation or pulmonary edema, it is necessary to restore the acid-base and water-electrolyte balance. With signs of hypoglycemia, you need to take glucose.

Interaction:With the simultaneous administration of Pentasa® with azathioprine or 6-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 adverse reactions from the kidneys. Slows the absorption of cyanocobalamin (vitamin B₁₂), enhances the hypoglycemic effect of sulfonylurea derivatives, ulcerogenicity of glucocorticosteroids, toxicity of methotrexate, weakens the activity of furosemide, spironolactone, sulfonamides, rifampicin, probenicid and sulfinpyrazone, enhances the effect of anticoagulants, and increases the effectiveness of uricosuric drugs (tubular secretion blockers). With the simultaneous use of medications of mesalazine and digoxin, digoxin absorption is reduced.

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 discontinued.
During the entire course of treatment with Pentasa®, the concentration of creatinine in the blood should be monitored regularly.

Effect on the ability to drive transp.cf. and fur:Care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

Form release / dosage:Granules of prolonged action for ingestion of 1 g and 2 g.

Packaging:For 1 g or 2 g of granules in a bag of polyester / aluminum foil / low density polyethylene.
1 g: 50, 60, 100, 120 or 150 bags in a cardboard box with instructions for use.
2 grams: 30, 50, 60 or 120 bags in a cardboard box with instructions for use.

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

Shelf life:2 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002648

Date of registration:08.10.2014

Expiration Date:08.10.2019

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: & nbsp2016-09-20

Illustrated instructions

Instructions

Pentasa® (Pentasa)