Mesacol

Pharmacology: Mesacol is designed to disintegrate and dissolve in the terminal portion of ileum. Thus, large amount of 5-aminosalicylic acid is made available at the desired site of action ie, distal ileum and large intestine, with minimal GI upset or systemic absorption. Very small amount of 5-aminosalicylic acid is absorbed from the large intestine. High levels of the drug continue to remain in the large intestine to exert its anti-inflammatory effect.
Teratogenicity: At doses 5-20 times the human dose (100-400 mg/kg in rats), reduced fetal weight, retarded ossifications and immaturity of fetal visceral organs has been noted in rats.

Treatment of ulcerative colitis and for prolongation of remission between acute attacks of ulcerative colitis and regional ileitis (Crohn's disease).

1-2 tab tid.
Acute: 800 mg tid (2.4 g/d) for 6 weeks (Max: 60 mg./kg./day).
Maintenance: 800 bid (1.6 g/d) for 6 months. Dosage reduced to 1.2 g/d for long term remission.

Nausea, vomiting, gastric distress, abdominal pain, weakness and drowsiness may be observed. Treatment includes gastric lavage, emesis, purgation, maintaining and monitoring renal function and other vital parameters.

Hypersensitivity to salicylates. Children <2 years.

Diarrhea, which appears to be dose-related, may occur. It may sometimes be difficult to distinguish it from diarrhea due to ulcerative colitis. Some of the absorbed 5-aminosalicylic acid or its metabolite may produce renal tubular damage. Care should be taken if renal tubular damage already exists; urinalysis, BUN and serum creatinine determination is advised. As Mesacol tablets will not disintegrate at lower pH, it should not be given with drugs that lower pH of stools.
Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Mesacol should be used only if the potential benefits justify the potential risks to the fetus.
Use in lactation: 5-Aminosalicylic acid is excreted in mother's milk. Caution should be exercised as diarrhea may occur in neonate. In lactating rats, doses from 100-400 mg/kg produced growth retardation in pups.
Use in children: Safety and effectiveness have not been completely established in this age group (see Contraindications). In children >2 years, 5-aminosalicylic acid may be used if the benefits outweigh the risk to the child.

GI: Diarrhea, nausea, abdominal pain, heartburn, anorexia, vomiting, stomatitis and dryness of mouth.
CNS: Headache, depression, vertigo, insomnia, fatigue, drowsiness, paresthesia, tremors and tinnitus.
Skin: Rash, itching, erythema and alopecia. There may be dryness of eyes.
CNS and Pulmonary: Very rare reports of pericarditis, heart block, hypertension, hypotension, chest pain, palpitation, tachycardia and shortness of breath.
GU: Dysuria, proteinuria, hematuria, oliguria, anuria, frequency and impotency are very rare.
Investigations: Elevated liver enzymes, neutropenia, lymphopenia, leucopenia, thrombocytopenia and anemia.

Coumarins, methotrexate, probenecid, spironolactone, furosemide and rifampicin may interact with 5-aminosalicylic acid.

GIT Regulators, Antiflatulents & Anti-Inflammatories

A07EC02 - mesalazine ; Belongs to the class of aminosalicylic acid and similar antiinflammatory. Used in the treatment of intestinal inflammation.

D