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 • Mesalazine general information

      • Active – active substance / start: Mesalazinee

      • Mesalazine

Asacol Mesalazine 400 mg
Most popular brand: Asacol
Active ingredient: Mesalazine
Available dosage forms: 400 mg
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Mesalazine general information

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Topical NSAIDs are frequently utilized to ease musculoskeletal pain caused by sports-related injuries. Although NSAIDs are often taken orally, they could be administered intravenously, transdermally, and even rectally within the form of the suppository to ease pain. Ergo, taking selective NSAIDs will not alter the stomach lining, however at the exact time, they provide pain relief. Although prednisone is a powerful drug, it should be administered carefully. Either way, augmenting the dosage raises the danger of side results. At times, it may impact the blood platelets and therefore the blood clotting.

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Active – active substance / start: Mesalazinee

5 – amino salicylic acid; 5 – ASA; 5 – ASA; Mezavant; Mesakol; Mesalazine; Pentas; salazopiridazina; Salozinal; salofalk; Samezil; Candles with salazopiridazina; Tidokol.

Mesalazine – anti-inflammatory agent. It is used for the treatment of ulcerative colitis (UC) and Crohn’s disease of any location, chronic ulcerative inflammation of the rectum (ulcerative proctitis).

Active – active substance:
Mesalazine / 5 – aminosalicylic acid / 5 – ASA / Mesalazinee.

Dosage Forms:
Tablets.
rectal suppositories.
Enema (suspension).

Mesalazine

Properties / Action:
Mesalazine – anti-inflammatory agent, inhibits the activity of neutrophil lipoxygenase.
Mesalazinee inhibits the migration (chemotaxis), degranulation, neutrophil phagocytosis and the secretion of immunoglobulin by lymphocytes. Mesalazinee decreases the production of cytokinins and leukotrienes, inhibits the synthesis of prostaglandins.
Mesalazinee has an antioxidant effect, eliminates free radicals (due to the ability to bind to free oxygen radicals and destroy them).
Mesalazinee has an antibacterial effect against some cocci and Escherichia coli (manifested in the large intestine).
Mesalazinee has a pronounced therapeutic effect in patients with ulcerative colitis and Crohn’s disease.
The therapeutic effect of Mesalazinee appears as a result of the local contact of the drug with the intestinal mucosa.

Pharmacokinetics:
Depending on the application, the release of Mesalazinee occurs in the rectum and colon (suspension for rectal administration, suppositories) or in the terminal part of the small and large intestine (coated tablets enteric-coated).
After receiving the tablet disintegrates into microspheres act as independent forms of the drug sustained-release Mesalazinee. This provides the therapeutic effect of the drug on the way from the duodenum to the rectum at any pH. Microgranules reach the duodenum in the first hour after ingestion. Passage of the drug on the small intestine intact performed for 3 – 4 hours. About 20 – 50% and 50 – 80% of Mesalazinee microgranules released during passage through the small intestine and colon, respectively, thus enters the systemic circulation only about 10%.
About 10% of the dose of Mesalazinee, entering the body with suppositories is absorbed into the blood.
Mesalazinee is metabolized in the intestinal mucosa and in the liver is exposed to acetylation acetyl – Mesalazinee – N – acetyl – 5 – aminosalicylic acid (to a small extent with enterobacteria).
The connection to plasma proteins – 43%, and of N – acetyl – 5 – amino salicylic acid – 73 – 83%.
After intravenous administration, the half-life and acetyl Mesalazinee – plasma Mesalazinee 40 and 70 minutes respectively.
Mesalazinee and acetyl – Mesalazinee do not cross the blood – brain barrier and penetrate into breast milk.
Mesalazinee and its metabolites are excreted with urine and feces. Renal excretion (50%), mostly in the acetylated form through the intestines (40%). Clearance – 300 ml / min. It accumulates in renal failure.

Indications:
Ulcerative colitis (UC) and Crohn’s disease at any site (prevention and treatment of exacerbations).
Treatment of chronic ulcerative inflammation of the rectum (ulcerative proctitis) for suppositories and enemas.

Dosage and administration:
The choice of dosage form is mainly determined by the localization and extent of intestinal lesions

.

  • for common forms of tablets are used at the distal (proctitis, Proctosigmoiditis) – rectal form
  • .

  • an exacerbation of the disease – 400 – 800 mg 3 times a day, for 8 – 12 weeks
  • .

  • for the prevention of relapses – 400 – 500 mg 3 times a day, for several years.
    Tablets:
    The tablets should be taken whole, without chewing, after meals, drinking plenty of fluids. Do not chew the tablets! In the case where skipped once a pill, it must be taken at any time, or together with the next tablet to the following method.
    Ulcerative colitis:
    the acute stage:
    Adults: the dose is adjusted individually, normally – up to 4 g Mesalazinee per day in divided doses.
    Children: Dose selected individually – usually 20 – 30 mg Mesalazinee per 1 kg of patient body weight per day in divided doses.
    Maintenance therapy:
    Adults: Dose selected individually, usually 2 g Mesalazinee per day in divided doses.
    Children: dose adjusted individually, normally 20 – Mesalazinee 30 mg per 1 kg of patient body weight per day in divided doses.
    CROHN’S DISEASE:
    Step acute and maintenance treatment:
    Adults: the dose is adjusted individually, normally – up to 4 g Mesalazinee per day divided doses.
    Children: dose adjusted individually, normally 20 – Mesalazinee 30 mg per 1 kg of patient body weight per day in divided doses.
    suppositories and enemas suspension:
    should empty the bowel before the introduction of the suppository. To ensure the hygiene of manipulation, use a rubber fingertip. Suppository inserted into the rectum prior to the termination resistance of the muscular sphincter. If within 10 minutes after administration will indicate a suppository, the suppository should enter another. For ease of use, a suppository can be moistened with water. At night during exacerbations medication appropriate to prescribe enemas (previously recommended to clean the intestines).
  • Candles – 500 mg 3 times a day, and the slurry – 60 g of suspension (4 g Mesalazinee) 1 once a day at night
  • .

  • Children appoint a rate of candles: at an aggravation – 40 – 60 mg / kg / day; for the maintenance treatment – 20 – 30 mg / kg / day.

    Overdose:
    No cases of overdose were observed. Symptoms of overdose may be pronounced side effects: nausea, vomiting, gastralgia, weakness, drowsiness. Treatment is symptomatic: gastric lavage, the appointment of a laxative in combination with monitoring of renal function.

    Contraindications:
    Mesalazinee drugs are contraindicated in patients with:

  • severe impaired liver or kidney function;
  • hypersensitivity to salicylates, sulfonamides, or other ingredients of the drug;
  • peptic ulcer and duodenal ulcer;
  • deficiency of glucose – 6 – phosphate dehydrogenase;
  • hemorrhagic diathesis;
  • lactation, last 2 – 4 weeks of pregnancy;
  • children up to 2 years.

    Use during pregnancy and lactation:
    During pregnancy and lactation appoint Mesalazinee drugs should be only in those cases where the positive effect of its implementation outweigh the risk of possible side effects. Despite the fact that Mesalazinee crosses the placental barrier, what – or teratogenic effects on the fetus have been identified. Mesalazinee and its metabolites are partly excreted with the milk during lactation, however, reports of any – any adverse effect of the drug on infants have been reported.

    Side effects:
    Typically, therapy with Mesalazinee is well tolerated. However, from 1 – 3% of the patients may complain of pain in the abdomen, nausea, vomiting, loss of appetite, headache, diarrhea, and skin rash in the form of hives or eczema, fever.
    In some cases, after the introduction of the suppository into the rectum, there may be a feeling of irritation, itching and the urge to defecate.
    In rare cases, hypersensitivity reactions to the drug (skin rash, itching, dermatitis, bronchospasm and shortness of breath, eosinophilia).
    It rarely show any side effects include: pain in the muscles and joints, temporary hair loss, lupus-like syndrome, abnormal liver function (increased activity of “liver” transaminases, hepatitis) and renal (proteinuria, hematuria, oliguria, crystalluria, nephrotic syndrome), (peri -) myocarditis, pancreatitis and changes in the formula blood (leucopenia, granulocytopenia, thrombocytopenia, anemia), hypoprothrombinemia, disease, tinnitus, dizziness, insomnia, seizures, depression, hallucinations, photosensitivity.
    Some of the above displays can be regarded as symptoms of the disease.

    Special instructions and precautions:
    Mesalazine caution should be used in patients with liver disease and kidney failure with glucose – 6 – phosphate dehydrogenase, with allergic diseases and predisposition to them.
    The treatment of patients with impaired hepatic or renal function is possible only after an assessment of the degree of their severity. not recommended to use drugs Mesalazinee In severe renal insufficiency.
    In some cases, allergy to may develop from intolerance and to Mesalazinee.
    Control of peripheral blood picture, liver function and renal excretory function (blood creatinine levels) should be performed before the initiation of treatment and then monthly for the first three months of treatment.
    There may be tears and urine staining in yellow – orange staining of soft contact lenses.
    In the event of missed doses, the missed dose should be taken at any time or in conjunction with the next dose.
    Patients who are “slow acetylators” have an increased risk of adverse drug reactions.
    In rare cases, may develop (peri -) myocarditis and expressed blood count changes. If you suspect that these side effects you should stop treatment and contact your doctor. Manifestations of the above side effects are: in the case of marked pathological changes of the blood – increased bleeding, bruising, sore throat and fever, or, in the case of (peri -) myocarditis – fever and chest pain combined with shortness of breath.
    Not recommended for Mesalazinee formulations for the treatment of children under the age of 2 years.
    Admission Mesalazinee did not affect the ability to drive.

    Drug Interactions:
    Enhances hypoglycemic effect of sulfonylurea derivatives, corticosteroids and ulzerogennosti and side effects as furosemide, and, sulfonamides, rifampicin and, enhances the effect of anticoagulants, increases the effectiveness of uricosuric drugs (probenecid). It slows down the absorption of cyanocobalamin well.

    Storage:
    Mesalazinee suppositories should be stored in original packaging at room temperature (15 – 25 ° C).
    Mesalazinee tablets should be stored in original packaging at room temperature (15 – 25 ° C).
    Do not use the drug after the expiry date printed on the package.

    Dispensed by prescription.

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