Pentasa tabs 500mg #100

Pentasa instruction

You can buy Pentasa here

Pentasa is an anti-inflammatory and antimicrobial intestinal drug with localization of action mainly in the intestine upon contact with the affected mucosa.

Release form and composition

Sustained-release tablets: round, chamfered, white with a grayish tint and numerous light brown blotches, on one side there is an engraving “500 mg” and a separation of risk, on the other side there is an engraving “PENTASA” (10 pieces each in aluminum blisters) foil, in a pack of cardboard 2, 3, 5, 6, 9 or 10 blisters; 50 pcs. in plastic bottles, in a pack of cardboard 1 bottle);
Each pack also contains instructions for the use of Pentasa.
Composition of 1 tablet:
    Active ingredient: mesalazine - 0.5 g;
    Auxiliary components: povidone, talc, microcrystalline cellulose, magnesium stearate, ethyl cellulose.

Pharmacodynamics

Mesalazine is an active component of sulfasalazine (5-aminosalicylic acid). The therapeutic effect of Pentasa after oral or rectal administration is more associated with local effects on the inflamed intestinal tissue than with its systemic effect.
The main effects of mesalazine are: inhibition of leukocyte chemotaxis, a decrease in the production of cytokines and leukotriene, as well as a decrease in the formation of free radicals in the inflamed intestinal tissue. However, the exact mechanism of action of the substance is not fully understood.
The therapeutic effect of mesalazine is manifested in local contact with the affected intestinal mucosa.

Pharmacokinetics

After oral administration, the tablet and granules disintegrate into microgranules, which act as independent forms of the drug with delayed release. Thanks to this, the therapeutic effect of Pentasa is provided throughout the entire length from the duodenum to the rectum at any pH. After taking the drug, the microbeads reach the duodenum in 60 minutes. The transit time of mesalazine through the small intestine is approximately 3-4 hours.
About 30-50% of the dose taken is absorbed in the small intestine (predominantly). The maximum plasma concentration of mesalazine is reached in 60 minutes and lasts up to 4 hours, gradually decreasing.
Mesalazine in the liver and intestinal mucosa undergoes acetylation (to a small extent, with the participation of enterobacteria), with the formation of the main metabolite - N-acetyl-5-aminosalicylic acid. 43% of mesalazine and 73–83% of the metabolite bind to plasma proteins. Mesalazine and its metabolite do not pass through the blood-brain barrier, but penetrate into breast milk. The clearance of the substance is 18 l / h. In the case of high doses (up to 1500 mg per day), a cumulative effect may be observed.
T1 / 2 (half-life) of mesalazine and metabolite from plasma - about 40 and 70 minutes, respectively. Excretion of the substance and metabolite is carried out with feces and urine.

Indications for use

Pentasa granules and tablets are taken for Crohn's disease and ulcerative colitis.
Rectal suppositories are used in case of ulcerative proctitis, one of the forms of ulcerative colitis with damage to the distal colon.
Pentasa rectal suspension is recommended for use with ulcerative proctosigmoiditis and left-sided ulcerative colitis.

Contraindications

Absolute:
    Hemorrhagic diathesis;
    Severe renal and / or liver dysfunction;
    Stomach ulcer or duodenal ulcer;
    Pregnancy (2-4 weeks before delivery);
    The period of breastfeeding (lactation);
    Children's age up to 2 years (for tablets), up to 6 years (for granules); Pentasa suspension and suppositories are contraindicated for use in pediatrics due to insufficient data;
    Hypersensitivity to mesalazine and / or other components.
Relative (Pentasa is used with caution due to the increased risk of complications):
    Allergy to salicylates (hypersensitivity reactions to sulfasalazine are possible);
    Dysfunctions of the lungs, in particular, bronchial asthma;
    Renal / hepatic insufficiency of mild to moderate severity (an increase in the systemic concentration of mesalazine and a decrease in the elimination rate increases the risk of kidney damage);
    Pregnancy (except for the period 2-4 weeks before childbirth) (Pentasa is used according to indications only if the potential benefit to the mother exceeds the possible risk of adverse effects for the fetus).

Instructions for use: method and dosage

Pentasa tablets are taken orally after a meal without chewing. If the patient cannot swallow the tablet whole, it is allowed to divide it into several parts, or to dissolve it in juice or water immediately before administration.
Recommended dosage for adults:
    Ulcerative colitis: with exacerbation - 2 pcs. 2-4 times a day; maintenance treatment - 1 pc. 2-3 times a day;
    Crohn's disease: with exacerbation - 2-4 pcs. 4 times a day; maintenance treatment - 2-4 pcs. 2 times a day or 2-3 pcs. 3 times a day.
An individual dose of mesalazine is selected for children, usually at the rate of 0.02-0.03 g / kg body weight per day in several doses.

Side effects

Side effects from the use of mesalazine from organs and systems, in accordance with the gradation - often -> 1% - <10%; rarely -> 0.01% - <1%; very rarely - <0.01%, including isolated cases:
    Hematopoietic organs: very rarely - anemia, leukopenia, eosinophilia, granulocytopenia, thrombocytopenia, pancytopenia, agranulocytosis;
    Immune system: very rarely - hypersensitivity reactions, Quincke's edema, drug fever;
    Nervous system: rarely - dizziness; very rarely - benign intracranial hypertension, peripheral neuropathy;
    Cardiovascular system: rarely - pericarditis, myocarditis;
    Respiratory system: very rarely - cough, shortness of breath, allergic alveolitis, lung infiltration, pulmonary eosinophilia, pneumonia, bronchospasm;
    Digestive system: often - diarrhea, abdominal pain, nausea, vomiting, flatulence; rarely - pancreatitis, increased amylase; very rarely - exacerbation of symptoms of colitis;
    Hepatobiliary system: very rarely - increased levels of bilirubin and liver enzymes, hepatotoxicity (hepatosis, hepatitis, liver failure, cirrhosis);
    Skin: often - eczema, urticaria; very rarely - reversible alopecia, photosensitivity;
    Musculoskeletal system: very rarely - arthralgia, myalgia;
    Urinary system: very rarely - nephrotic syndrome, interstitial nephritis, transient renal failure, urine discoloration;
    Other: often - fever, headache;
    Reactions at the injection site (suspension, suppositories): rarely - pain and irritation in the anus.
Most often, due to the use of mesalazine, there are: diarrhea, nausea, abdominal pain, headache - up to 3% of cases; vomiting and skin rashes - up to 1% of cases.
In case of aggravation of any side effects from those indicated in the instructions, or any other reactions not described in the instructions, it is required to seek the advice of your doctor.

Overdose

Cases of overdose, especially with rectal administration of Pentasa, are rare.
The main symptoms are vomiting, nausea, gastralgia, drowsiness, weakness.
Therapy: symptomatic in combination with control of kidney and liver function. In case of acidosis, dehydration or alkalosis, restoration of acid-base and water-electrolyte balance is required. With signs of hypoglycemia, glucose is indicated.
There is no specific antidote.

Special instructions

If acute signs of intolerance to Pentasa appear (such as muscle cramps, abdominal pain, fever, severe headache, skin rashes) or symptoms of impaired renal and / or liver function, therapy should be discontinued.
It is required to conduct regular monitoring of the creatinine in the blood throughout the entire time of application of any form of release of the drug Pentasa.
Staining of soft contact lenses, tear fluid and urine in yellow-orange color is allowed.
Influence on the ability to drive vehicles and complex mechanisms
Patients are advised to exercise caution when taking pills, granules and using a rectal suspension, driving vehicles and engaging in other potentially dangerous activities that require quick psychomotor reactions and increased concentration of attention, since they can be affected by Pentasa side effects such as nausea, weakness, dizziness, etc.

Pregnancy and lactation

    Pregnancy (2-4 weeks before delivery), lactation: therapy is contraindicated;
    Pregnancy (excluding the period 2–4 weeks before childbirth): Pentasa can be used only after assessing the ratio of expected benefits to possible risks.

Use in childhood

Age restrictions on the use of Pentasa in pediatrics, depending on the form of release:
    Tablets: up to 2 years;
    Granules: up to 6 years;
    Suppositories and suspension: up to 18 years.

With impaired renal function

For patients with severe renal impairment, mesalazine therapy is contraindicated.
For impaired renal function of mild to moderate severity, Pentasa should be used with caution.

With impaired liver function

Mesalazine therapy is contraindicated in patients with severe hepatic impairment.
In case of impaired hepatic function of mild to moderate severity, Pentasa should be used with caution.

Drug interaction

With simultaneous use with mesalazine:
    Azathioprine or mercaptopurine - increase the risk of suppressing bone marrow function (thrombocytopenia, leukopenia, pancytopenia, erythrocytopenia / anemia);
    Non-steroidal anti-inflammatory drugs (NSAIDs), azathioprine and other nephrotoxic drugs - increase the risk of side effects from the kidneys;
    Cyanocobalamin (Vitamin B12) - absorption slows down;
    Derivatives of sulfonylureas - increased hypoglycemic effect;
    Glucocorticosteroids (GCS) - increased ulcerogenicity;
    Methotrexate - increased toxicity;
    Furosemide, spironolactone, sulfonamides, rifampicin - activity is weakened;
    Anticoagulants - the action is enhanced;
    Tubular secretion blockers (uricosuric agents) - increased efficiency.

Terms and conditions of storage

Keep out of the reach of children, in a dry, dark place at temperatures up to 25 ° C.
Shelf life is 3 years.

Reviews

Most reviews of Pentasa indicate the high effectiveness of the drug. They note that in any form of release Pentasa demonstrates good tolerance, and its therapeutic effect develops rapidly.
Almost all patients indicate a high cost of the drug as a disadvantage.

Terms of sell

You don't need a prescription to buy Pentasa.