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Active Ingredient: Mesalazine
Brand Name: Asacol

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What is Mesalazine

Mesalazine has an anti-inflammatory impact by inhibiting prostaglandin manufacturing within the intestine. The mesalazine merchandise has a pH-dependent and/or regulated launch system. Notice how the oral preparations release the drug in different ways. This is important for the different uses.

Mesalazine Drug Recommendation

When treating Crohn’s disease, the choice of medicine depends on where the irritation is, how big it is, how bad it is, how long it will last, and how well it worked before. Corticosteroids are used for remission induction and immunosuppressants for maintenance therapy. TNF-blockers can be used at any stage of the treatment.

Because the results of scientific studies don’t support their use enough, aminosalicylates aren’t used much anymore to treat Crohn’s disease. When treating ulcerative colitis, the choice of drug depends on where the irritation is, how big it is, how bad it is, how long it is expected to last, and how well a previous treatment worked. Corticosteroids are used for remission induction and immunosuppressants as maintenance remedies. Aminosalicylates and TNF-blockers can be used at any time during the treatment.

When selecting an aminosalicylate, mesalazine is the most well-liked. Sulfasalazine causes extra-negative effects, and olsalazine is liable to cause diarrhoea. Due to their different ways of going off, the different preparations shouldn’t be swapped out right away. Mesalazine suppositories are only used if the condition is solely proctitis.

Asacol Indications

Oral (adults and youngsters over 6 years)

  • all preparations: delicate to reasonable ulcerative colitis, each within the acute section and to stop recurrences.
  • Pentasa: Crohn’s illness, each within the acute section and to stop recurrences (in all intestinal areas).
  • Asacol, Salofalk pill and a few generic mesalazine gastro-resistant tablets:
    • Crohn’s illness, each within the acute section and to stop relapses, if the illness is proscribed to the colon.

Rectal (adults)

  • ulcerative proctitis;
  • for Salofalk enema additionally: (relapse prophylaxis of) distal ulcerative colitis.
  • for Pentasa enema additionally: proctosigmoiditis, left-sided colitis.
  • for Salofalk foam: remedy of delicate ulcerative colitis, localized within the sigmoid and rectum, within the acute section.

What Should You Discuss To Your Doctor Before Using This Medicine

  • Being pregnant
    • Mesalazine passes via the placenta.
    • Teratogenesis: No proof of harmfulness. After long-term use of a excessive dosage (2-4g per day orally), neonatal renal failure and hydrops foetalis have been reported as soon as. Mesalazine is absorbed from the gastrointestinal tract to a restricted extent.

  • Lactation
    • Transition in breast milk: Sure, to a minor extent.
    • Pharmacological impact: Acute diarrhoea has been reported sporadically as a consequence of toddler hypersensitivity.

  • Contraindications
    • extreme hepatic impairment;
    • extreme renal impairment (creatinine clearance < 30 ml/min);
    • present peptic ulcer;
    • hypersensitivity to salicylates.

Mesalazine Drug Interactions

Mesalazine may be released less when the pH level in the intestine is lowered with a drug like lactulose. On theoretical grounds, the following interactions will be anticipated as a result of salicylate part:

  • the hypoglycaemic impact of the sulphonylurea derivatives may very well be elevated;
  • methotrexate may very well be extra poisonous;
  • the motion of furosemide and spironolactone and the tuberculostatic impact of rifampicin may very well be lowered;
  • the chance of gastric misery brought on by glucocorticosteroids may very well be elevated.

If it is taken with a vitamin K antagonist, the anticoagulant effect may be lessened, so the INR needs to be checked more often. When different nephrotoxic drugs, like NSAIDs and azathioprine, are used together, the risk of kidney-damaging side effects goes up. This means that kidney function needs to be checked more often.

inhibits thiopurine methyltransferase. Co-treatment with azathioprine, 6-mercaptopurine, or tioguanine will increase the chance of myelosuppressive effects; check blood often and often.

Mesalazine Dosage

Because the launch profiles are different, the different preparations shouldn’t be swapped with each other.

  1. Ulcerative Colitis
    • Adults (incl. aged)
      • orally:
        • Asacol:
          • acute section 2.4-4.8 g/day in 3-4 doses,
          • upkeep dosage 800-2400 mg/day in 3 doses.

        • Mesalazine gastro-resistant:
          • acute section 2-4.5 g/day in 3-4 doses after meals;
          • upkeep dose max. 500 mg 3×/day.

        • Mezavant:
          • acute section 2.4-4.8 g 1×/day swallowed complete with meals. The best dose is really helpful in sufferers who don’t reply to the decrease dose. Assess efficacy after 8 weeks utilizing the best dose.
          • Upkeep dosage 2.4 g 1×/day.

        • Pentasa pill or controlled-release granule:
          • acute section as much as 4 g/day, abruptly or in a number of doses per day;
          • upkeep dosage individually e.g. 2 g/day. Don’t chew the granules.

        • Salofalk Granu-Stix:
          • acute section 1.5-3 g 1×/day ideally within the morning or 500-1000 mg 3×/day;
          • upkeep dosage 500 mg 3×/day or 3 g 1×/day ideally within the morning. Don’t chew granules.

        • Salofalk gastro-resistant:
          • acute section 2-4.5 g/day in 3-4 doses swallowed complete after meals;
          • upkeep dosage max. 500 mg 3×/day.

        • Yaldigo: acute section as much as 4.8 g/day in 1-3 doses, swallowed complete with (a glass of) water, with or with out meals, till remission is achieved; upkeep dosage 1.6 g 1×/day.

      • Rectal:
        • Pentasa enema: 1 g/100 ml for the night time for 2-4 weeks.
        • Salofalk foam: 2 administrations for the night time; presumably give the second administration, after defecation of the primary dose, later at night time or early within the morning.
        • Salofalk enema:
          • acute section 2 g/30 g 2×/day or 4 g/60 g by night time;
          • upkeep dosage 2 g/30 g or 2 g/60 g by night time or 4 g/60 g each different day or each two days.
    • Youngsters 6-18 years
      • Oral:
        • Asacol, Mesalazine gastro-resistant, Pentasa, Salofalk: Typically, it is suggested to offer half of an grownup dose for physique weight as much as 40 kg, above 40 kg the conventional grownup dose.

    • Youngsters 10-18 years (with physique weight > 50 kg)
      • Oral:
        • Mezavant:
          • acute section (first 8 weeks): 2.4-4.8 g 1×/day swallowed complete with meals;
          • upkeep dose 2.4 g 1×/day. The 1200 mg tablets should not appropriate for youngsters < 10 years or ≤ 50 kg.

  2. Crohn’s illness
    • Adults (incl. aged)
      • orally:
        • Asacol:
          • acute section most 4.8 g/day in 3-4 doses
          • upkeep dose most 2.4 g/day in 3 doses.
        • Mesalazine gastro-resistant (some producers):
          • acute section as much as 4.5 g/day in 3-4 doses after meals
          • upkeep dose as much as 3 g/day in 3-4 doses.
        • Pentasa pill or managed launch granulate:
          • acute section 2-4 g/day in a number of doses
          • upkeep dosage as much as 2 g/day. Don’t chew granules.
        • Salofalk pill:
          • cute section as much as 4.5 g/day in 4 doses swallowed complete after meals;
          • upkeep dosage as much as 2 g/day in 3 doses.
    • Youngsters 6-18 years
      • Oral:
        • Asacol, Mesalazine gastro-resistant, Pentasa, Salofalk pill: Typically, it is suggested to offer half of an grownup dose for a physique weight as much as 40 kg, above 40 kg the conventional grownup dose. For instance, for the:
          • acute section 30-50 mg/kg/day in numerous doses, max. 75 mg/kg/day and 4 g/day
          • upkeep section 15-30 mg/kg/day in numerous doses, max. 2 g/day.

  3. Ulcerative Proctitis
    • Adults (incl. aged)
      • Rectal:
        • Pentasa enema: 1 g/100 ml at night time for 2-4 weeks.
        • Salofalk enema: acute section 2 g/30 g 2×/day; upkeep dosage 2 g/30 g by night time.
        • Pentasa suppository: 1 g 1-2×/day.
        • Mesalazine and Salofalk suppository: acute section 500 mg 3×/day or 1 g 1×/day at bedtime; upkeep dose 250 mg 3×/day.

  4. Administration: Suppository or enema ought to ideally be administered after defecation to stop the drug from leaving the physique prematurely.

Signs of Overdose

  • signs of salicylate poisoning might happen
  • resembling gastrointestinal results
  • acidosis or alkalosis
  • hyperventilation
  • pulmonary oedema
  • dehydration
  • hypo-/hyperglycaemia
  • hypothermia
  • central nervous system problems

Mesalazine Precautions

  1. Controls: Decide renal operate, blood rely and liver operate parameters previous to remedy and recurrently throughout remedy.
  2. Renal toxicity: Use in renal impairment just isn’t really helpful, use with warning in circumstances of proteinuria and elevated blood urea. If renal operate decreases throughout remedy take into account renal toxicity of mesalazine.
  3. Nephrolithiasis: Kidney stones have been reported, together with these composed of 100% mesalazine. It is suggested to make sure sufficient fluid consumption.
  4. Haematological results: Within the occasion of extreme blood dyscrasia resembling haemorrhage, bruising, purpura, anaemia or sore throat, discontinue remedy instantly.
  5. Comorbidity: Warning in case of hepatic insufficiency, in case of bronchial asthma (as a consequence of hypersensitivity response) and in situations which will result in myocarditis or pericarditis.
  6. Intolerance syndrome: If an acute intolerance syndrome happens, discontinue remedy instantly.
  7. Critical pores and skin reactions: Instantly stop remedy within the occasion of extreme pores and skin reactions, resembling rash, lesions of the mucous membranes and/or different indicators of hypersensitivity.
  8. Asacol: Pill wraps might happen within the stool.
  9. Analysis information: There are restricted information on efficacy in youngsters aged 6 to 18 years. Attributable to inadequate efficacy and security information, the usage of enemas, foams and suppositories and the 1200 or 1600 mg controlled-release tablets just isn’t really helpful in youngsters < 18 years of age.

Asacol Side Effects

  • headache
  • Dyspepsia, stomach ache, nausea, vomiting, diarrhoea, flatulence
  • Improve in transaminases and bilirubin
  • Backache, arthralgia
  • Pores and skin rash, itching
  • Fatigue, asthenia, fever
  • Hypertension
  • Rectal discomfort, rectal irritation and itching, urge
  • Dizziness, tremour, drowsiness, paraesthesia
  • Hypotension
  • Tinnitus
  • Earache
  • Sore throat
  • Tachycardia
  • Myalgia
  • Rectal polyp, acute pancreatitis
  • Facial oedema
  • Zits, urticaria, alopecia
  • Chest ache
  • Improve in lipase, amylase and eosinophils
  • Renal failure
  • Photosensitivity
  • Myocarditis, pericarditis
  • Cholestatic hepatitis

Disclaimer

Information concerning psychotic disorders, included in the review of Mesalazine, is used exclusively for the informative features and should not be considered an alternative to licenced healthcare or a referral to the well-being treatment distributor.

 

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Frequently asked questions

  1. What is Mesalazine Asacol?

    Mesalazine is an anti-inflammatory drug that acts on the lining of the gut to treat ulcerative colitis, proctosigmoiditis, and proctitis. It also reduces inflammation, tissue damage, and diarrhoea. Mesalazine becomes active in the small intestine just before it enters the large intestine.

  2. What to do if you miss a dose?

    If you forget to take a dose of Mesalazine, you should take it as soon as you remember. However, if it is almost time for your next dose, you should skip the dose you missed and go back to your regular dosing schedule. You should never double your doses.

  3. How to store Mesalazine?

    Keep at a temperature between 20 and 25 degrees Celsius (68 and 77 degrees Fahrenheit).

  4. What are the side effects of Mesalazine Asacol?

    The most common adverse reactions include cramping, fever, dyspepsia, jaundice, exacerbation of abdominal colitis, severe abdominal pain, and exacerbation of abdominal colitis. Colic, fever, nasopharyngitis, headache, and severe abdominal pain are also reported.

  5. What are the Contraindications?

    People who are hypersensitive to any of the ingredients, sensitive to salicylates or aminosalicylates, or renally sensitive to sulfasalazine are not allowed to take mesalazine. Mesalazine is also contraindicated in people who have severe hepatic impairment, acute or chronic interstitial nephritis, gastric or duodenal ulcer, or a tendency to bleed easily.

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