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

Composition:For 1 suppository:
active substance - mesalazine 1 g, Excipients - macrogol 6000 519 mg, talc 4 mg, magnesium stearate 4 mg, povidone K-25 (K = 22-28) 50 mg.

Description:Suppositories are oval in shape, from white to white with a yellowish-brown hue of color, with numerous patches of light gray.

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 manifests itself in local contact with the affected mucosa. 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: Suppositories of Pentas® provide the creation of a high concentration of mesalazine in the distal part of the intestine and minimal systemic absorption (no more than 10%).
- distribution: 43% of mesalazine and 73-83% of its main metabolite of M-acetyl-5aminosalicylic acid bind to plasma proteins. Mesalazine and its metabolites do not penetrate the blood-brain barrier, but penetrate into the mother's milk.
- metabolism: mesalazine is acetylated in the intestinal mucosa, in the liver and, to a small extent, enterobacteria, forming N-acetyl-5-aminosalicylic acid
- excretion: mesalazine and its metabolites are excreted from the body with urine and feces.

Indications:Ulcerative colitis with damage to the distal parts of the colon (ulcerative proctitis).

Contraindications:- Hypersensitivity to the components of the drug,
- Severe liver and / or kidney damage,
- Peptic ulcer of the stomach or duodenum,
- Hemorrhagic diathesis,
- The preparation Pentasa® is contraindicated for use in pediatric practice.
If you have any of these diseases, consult a doctor before taking the drug.

Carefully:With caution, the drug should be given to patients who are allergic to sulfasalazine, since hypersensitivity reactions to salicylates are possible. Caution should be exercised when administering Pentasa® to patients with impaired hepatic and renal function, as reducing the elimination rate and increasing the systemic concentration of mesalazine increases the risk of kidney damage.

Pregnancy and lactation:Pentasa® preparation may be used during pregnancy only if the expected benefit 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, while taking Pentasa®, breastfeeding should be discontinued.

Dosing and Administration:1 suppository 1-2 times a day. The maximum daily dose is 6-8 suppositories.
Before the introduction of the suppository should be emptied the intestine.
To ensure hygienic manipulation, a rubber fingertip should be used.
The suppository is injected into the rectum until the resistance of the muscle pulp ceases. If within 10 minutes after the introduction of the suppository is withdrawn, then another suppository should be introduced. To facilitate the application, the suppository can be moistened with water.
The average duration of treatment is 8-12 weeks, the criterion for the effectiveness of treatment is the achievement of clinical endoscopic remission. The maximum duration of treatment, including maintenance and anti-relapse therapy, is unlimited.

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 single cases)
On the part of organs- hematopoiesis			Eosinophilia, anemia, leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia
From the side immune systems			Hypersensitivity reactions, drug fever, angioedema
From the nervous system		Dizzyande	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
From the side of the food processorьsystem	Diarrhea, pain in 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 side of the support impellent apparatus			Myalgia, arthralgia
From the urinary systems			Interstitial nephritis *, nephrotic syndrome, changes in urine color, transient renal failure
Other	Headache, fever

(*) The mechanism of development of adverse reactions, presumably, is allergic.
Local reactions can also be noted, such as itching, discomfort, and urge to defecate.
If any of the conditions indicated in the manual, side effects 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. Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness. Specific antidotes are absent.
Treatment is symptomatic in combination with control of liver and kidney function. In the case of the development of acidosis, alkalosis or dehydration it is necessary to restore acid-alkaline and water-electrolyte balance. With signs of hypoglycemia, you need to take glucose.

Interaction:Mesalazine enhances hypoglycemic effect of sulfonylurea derivatives, ulcerogenicity of glucocorticosteroids, toxicity of methotrexate. Pentasa® weakens the activity of furosemide, spironolactone, sulfonamides, rifampicin, enhances the effect of anticoagulants. Increases the effectiveness of tubular secretion blockers. Slows the absorption of cyanocobalamin (vitamin B₁₂).

Special instructions:Medical control is necessary for patients with impaired lung function, in particular, suffering from bronchial asthma. 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.
Staining of urine and tear fluid in yellow-orange color, as well as staining of soft contact lenses can be observed.

Effect on the ability to drive transp. cf. and fur:Pentasa® does not affect the ability to drive and operate machinery.

Form release / dosage:Suppositories rectal 1 g.

Packaging:5 suppositories rectal into a blister of aluminum foil. 2 or 3 blisters in the package together with instructions for use in a cardboard box.
7 suppositories rectal into the blister of aluminum foil. 2 or 4 blisters in a package together with instructions for use in a cardboard box. The kit can include rubber hygienic fingertips.

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 the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N010197 / 01

Date of registration:29.07.2010 / 19.05.2016

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)