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

Composition:per 1 bottle (100 ml):
active substance - mesalazine 1.0 g,
Excipients - disodium edetate dihydrate 20 mg, sodium disulfite 100 mg, sodium acetate trihydrate 630 mg, hydrochloric acid concentrated q.s. to pH 4.6-5.0, water purified to 100 ml.

Description:White or light yellow suspension.

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 rectal administration is largely due to local effects on the inflamed mucosa of the intestine than the systemic action. 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 used rectally, the Pentasa® suspension has a therapeutic effect in the distal parts of the intestine. Approximately 15-20% of the administered dose is absorbed. In patients with ulcerative colitis in the active phase, the degree of absorption is markedly lower than in patients in the stage of remission.
- distribution: About 50% of mesalazine and about 80% of its main metabolite (N-acetyl-5-amino-salicylic acid) bind to proteins. Mesalazine and its metabolite does not penetrate the blood-brain barrier, but penetrate into breast milk.
- metabolism: mesalazine is acetylated in the intestinal mucosa and in the liver, and also, to a small extent, enterobacteria, forming N-acetyl-5-amino-salicylic acid.
- excretion: Mesalazine and its metabolites are excreted from the body with urine and feces.

Indications:- Ulcerous proctosigmoiditis.
- Left ulcerative colitis.

Contraindications:- Hypersensitivity to salicylates and other components of the drug.
- Severe hepatic and / or renal failure.
- Hemorrhagic diathesis.
- Peptic ulcer of stomach or duodenum (in the phase of exacerbation).
- Children's age (due to insufficient data).
If you have any of these diseases, consult a doctor before taking the drug.

Carefully:With caution, the drug should be administered to patients who are hypersensitive to salicylates. In case of acute symptoms of intolerance of the drug (muscle spasms, abdominal pain, fever, severe headache and skin rashes) or signs of liver and / or kidney dysfunction, the suspension of Pentasa® should be discontinued.
Medical control is necessary for patients with impaired lung function, in particular, suffering from bronchial asthma.
Care should be taken when prescribing the Pentas® rectal suspension 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:The rectal suspension of Pentasa® can be used during pregnancy only if the expected benefit for the mother prevails over the potential risk to the fetus. The drug should be stopped for 2 to 4 weeks before delivery.
Mesalazine penetrates the placental barrier and is excreted in breast milk. Therefore, during treatment with Pentasa® suspension, breastfeeding should be discontinued.

Dosing and Administration:The drug is prescribed as an enema 1 time per day before bedtime. The daily dose is 1g. Before the procedure, it is recommended to empty the intestine.
Packaging must be opened immediately before use, shake the contents of the bottle and push the tip to the stop. Use immediately after shaking.To perform the procedure it is recommended to lie on one side and insert the tip of the bottle as far as possible into the rectum.
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 supportive and anti-relapse therapy, is unlimited.

Side effects:Diarrhea (3%), nausea (3%), abdominal pain (3%), headache (3%), vomiting (1%) and skin rashes (1%) are most common with the use of the Pentas® rectal suspension.

Often (from> 1/100 to <1/10

Rarely (from> 1/10000 to <1/1000)

Rarely

(from <1/10000, including isolated cases)

On the part of the organs of hematopoiesis

Eosinophilia, anemia, leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia

From the immune system			Reactions hypersensitivity
From the nervous system	Headache		Peripheral neuropathy
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 digestive systems	Diarrhea, abdominal pain, nausea, vomiting, flatulence	Increase content amylase, pancreatitis
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 motor support apparatus			Myalgia, arthralgia
From the urinary system			Interstitial nephritis *, nephrotic syndrome, changes in urine color, transient renal failure
Reactions at the site of administration		pain and irritation in the anus

(*) 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, inform the doctor about it.

Overdose:In case of an overdose, nausea, vomiting, weakness, drowsiness, and pulmonary edema may occur. However, cases of an overdose of Pentasa® especially with rectal administration are rare. Specific antidotes are absent.It is recommended to take measures to enhance diuresis.

Interaction:With simultaneous administration of a rectal suspension 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 a suspension of Pentas® and other drugs with nephrotoxicity, for example, non-steroidal anti-inflammatory drugs (NSAIDs) and azathioprine, increases the risk of developing adverse reactions from the kidneys. Mesalazine can enhance the effect of anticoagulants and hypoglycemic action of sulfonylurea derivatives, enhance the toxicity of methotrexate, glucocorticoids enhance the damaging action on the gastric mucosa, to reduce the effect of rifampicin and tuberculostatic uricosuric effect of probenecid and sulfinpyrazone and reduce diuretic effects of furosemide and spironolactone. With the simultaneous use of medications of mesalazine and digoxin, digoxin absorption is reduced.

Special instructions:During the entire course of treatment with the rectal suspension of Pentasa®, the concentration of creatinine in the blood should be monitored regularly.

Effect on the ability to drive transp. cf. and fur:When using the drug, it is advisable to use caution when driving a car and other mechanisms, as well as engaging in potentially dangerous activities, as its side effects (headache, dizziness and others) can reduce the concentration of attention and the speed of psychomotor reactions.

Form release / dosage:Rectal suspension 1 g / 100 ml.

Packaging:100 ml of suspension in a low-density polyethylene bottle with a low-density polyethylene tip equipped with a valve to allow the suspension to flow out in only one direction, in a hermetically sealed aluminum bag in an atmosphere of nitrogen.
For 7 bottles in bags with instructions for use in a pack of cardboard. The kit can also include plastic hygiene bags.

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:LP-002411

Date of registration:31.03.2014

Expiration Date:31.03.2019

The owner of the registration certificate: Ferring-Lechiva as Ferring-Lechiva as Czech Republic

Manufacturer: & nbsp

FERRING-LECIVA, a.s. Czech Republic

Representation: & nbspFERRING PHARMACEUTICALS LLCFERRING PHARMACEUTICALS LLCRussia

Information update date: & nbsp2016-09-20

Illustrated instructions

Instructions

Pentasa (Pentasa)