Pentasa - Mesalamine

Pentasa Mesalamine capsules encap- 2-4 g Small bowel... 

Pentasa Mesalamine capsules encapsulated in ethylcellulose microgranules 2 g Small bowel and colon... 

Mesalamine. Rowasa, Asacol, and Pentasa are trade names for mesalamine [89-57-6] (5-ASA, 5-amino-2-hydroxybenzoic acid). It is a white to pinkish crystalline substance that is slightly soluble in cold water and alcohol, more soluble in hot water, and soluble in hydrochloric acid. It may be prepared by the reduction of y -nitrobenzoic acid with zinc dust and HCl. 

Mesalamine derivatives (such as Pentasa or Asacol) that release mesalamine in the small bowel may be more effective than sulfasalazine for ileal involvement. 

Mesalamine (Asacol, Pentasa, Rowasa) Ulcerative colitis Tab 400 mg Cap 250 mg Suppository 500 mg Rectal susp 4000 mg/60 mL... 

Hyoscyamine, Atropine, Scopolamine, Phenobarbital (Donnatal, oth s) Infliximab (Remicade) Lubiprostone (Amitiza) Mesalamine (Asacol, Lialda, Pentasa, Rowasa) Metoclopramide (Reglan, Clopra, Octamide)... 

Mesalamine (Asacol, Lialda, Pentasa, Rowasa) [Anti-inflcinimcifory/Seilicyleite] Uses Mild-mod distal ulcerative colitis, proctosigmoiditis, proctitis Action Unknown may inhibit prostaglandins Dose Rectal 60 mL qhs, retain 8 h (enema), 500 mg bid-tid or 1000 mg qhs (supp) PO Cap 1 g PO qid Tab 1.6-2.4 g/d doses (tid-qid) delayed release 2.4-. 8 g PO daily 8 wk max, do not cut/crush/chew w/ food initial dose in elderly Caution [B, M] Contra Salicylate sensitivity Disp Tabs, caps, supp, rectal susp SE HA, malaise, abd pain, flatulence, rash, pancreatitis, pericarditis Interactions X Effect OF digoxin EMS May turn urine yellow-brown OD May cause NA /D, tinnitus, HA, and drowsiness activated charcoal may be effective... 

To avoid the side effects of sulfapyridine, various preparations to target 5-ASA directly to sites of disease have been formulated. Also known as mesalamine, 5-ASA has been formulated in oral forms (Pentasa, Asacoi). Pentasa is a time-release capsule that releases the drug throughout the GI tract. Asacoi is a pH-dependent-release preparation that delivers drug to the distal small bowel and colon. The response of ulcerative colitis to this formulation appears to be identical to that seen with sulfasalazine. Mesalamine can also be administered as a suppository (Canasa) or enema (Rowasa) for distal colonic disease. 

Sulfasalazine is more effective when Crohn s disease involves the colon. Mesalamine derivatives (such as Pentasa or Asacol) that release mesalamine in the small bowel may be more effective than sulfasalazine for deal involvement. Steroids are frequently used for the treatment of active Crohn s disease, particularly with more severe presentations, or in those patients unresponsive to aminosalicylates. Budesonide is a viable first-line option for patients with mdd to moderate deal or right-sided disease. Systemic steroids induce remission in up to 70% of patients and should be reserved for patients with moderate to severe disease who have faded aminosahcylates or budesonide. Metronidazole (given orally up to 20 mg/kg/day) may be useful in some patients with Crohn s disease, particularly in patients with colonic or deocolonic involvement or those with perineal disease. The combination of metronidazole with ciprofloxacin is efficacious in some patients. 

Asacol, Asacolitin, Canasa, Claversal, Mesalazine, Mesasal, Pentasa, Pentasa SR, Quintasa, Rowasa, Salofalk, Tidocol mesalamine mephenytoin mesalamine Mesnex, Mexan, Uromitexan mesna Mesorin, Serentil mesoridazine minocycline nystatin nimesulide methylphenidate methadone metformin, glipizide cefmetazole... 

Because the mechanism of action of sulfasalazine is not related to the sulfapyridine component, and since sulfapyridine is believed to be responsible for many of the adverse reactions to sulfasalazine, mesalamine alone can be used. Mesalamine can be used topically as an enema for the treatment of proctitis, or given orally in slow-release formulations that deliver mesalamine to the small intestine and colon (Table 34—5 and Fig. 34-1). Slow-release oral formulations of mesalamine such as Pentasa release mesalamine from the duodenum to the ileum, with about 75% of the drug passing into the colon. Olsalazine is a dimer of two 5-aminosalicylate molecules linked by an azo bond. Mesalamine is released in the colon after colonic bacteria cleave olsalazine. Balsalazide is a mesalamine prodrug that is enzymatically cleaved in the colon to produce mesalamine. The recommended daily doses of the oral mesalamine derivatives are intended to approximate the molar equivalent of mesalamine present in 4 g of sulfasalazine. At present, snlfasalazine is nsed in preference to oral mesalamine derivatives, mainly becanse it costs mnch less. However, it is not tolerated as well as the mesalamine altematives. Becanse the oral mesalamine formulations are coated tablets or grannies, they should not be crushed or chewed. 

Mesalamine Rowasa, Salofalk, Claversal, Pentasa Enema g Rectum, terminal colon... 

Mesalamine products such as Pentasa or Asacol, that release mesalamine in the small bowel, are more effective than sulfasalazine for ileal involvement. In a trial of 310 patients with active Crohn s disease, Pentasa alone was more effective than placebo in achieving remission in a 16-week trial (43% vs. 18%, respectively). This beneficial effect was dose dependent and greatest with a dose of 4 g/day. A course of steroids is appropriate in patients who cannot be controlled with mesalamine. However, when a patient is maintained on steroids, there appears to be no benefit from the addition of sulfasalazine. 

Gendre JP, Mary JY, Florent C, et al. Oral mesalamine (Pentasa) as maintenance treatment in Crohn s disease A multicenter placebo-controlled study. Gastroenterology 1993 104 435-439. 

Other Names Salicylic acid, 5-amino- 2-Hydroxy-5-aminobenzoic acid 3-Carboxy-4-hydroxy-aniline 5-ASA 5-Amino-2-hydroxybenzoic acid 5-Aminosalicylic add Asacol Asacolitin Asacolon Canasa Claversal Fisalamine Ipocol Lixacol Mesacol Mesalamine Mesalazine Mesasal NSC 38877 Pentasa Rowasa Salofalk Salozinal m-Aminosalicylic acid CA Index Name Benzoic acid, 5-amino-2-hydroxy-CAS Registry Number 89-57-6 Merck Index Number 5904 Chemical Structure... 

Akbal E, Kofak E, Kbklti S. Mesalamine (Pentasa)-induced painful skin lesions. Inflamm Bowel Dis 2010 16 725-6. 

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