mesalamine (Asacol, Rowasa, Pentasa, Pentasacaps, Lialda, Apriso, Canasa, Delzicol)
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Introduction
Tradenames: Asacol, Rowasa, Pentasa, Apriso.
Indications
* activity minimal in Crohn's disease[8]
Contraindications
Dosage
- Anascol: 800 mg (2 tabs) PO TID
- Pentasa: 1000 mg (4 tabs) PO QID
- Lialda 2-4 tablets QD[5]
- Apriso QD 4 retention enema: 60 mL (4 g) QHS, retained overnight (approximately 8 hours)
- suppository: insert 1 BID
Tabs: 250 mg (Pentasa) & 400 mg (Anascol). Tab (delayed time release): 400 mg. Lialda 1.2 g MMX Multi-Matrix System QD dosing[6]
Suppository: 500 mg. Enema: 4 g/60 mL.
Pharmacokinetics
- mesalamine is poorly absorbed as a rectal enema
- excreted in the feces
- mesalamine tablets release drug in the terminal ileum & distally
- mesalamine capsules release drug throughout the entire GI tract
- acetylated in the mucosal wall of the gut & by the liver
- excreted in the urine & feces
Adverse effects
- common (> 10%)
- headache, abdominal pain, cramps, flatulence, gas
- less common (1-10%)
- uncommon (< 1%)
- anal irritation, acute intolerance syndrome (bloody diarrhea, severe abdominal cramps, severe headache)
- pericarditis
- pancreatitis
- hypersensitivity colitis[8]
- other
- nephrotoxicity, interstitial nephritis[8]
- nausea (common)[8]
Mechanism of action
- effect appears to be topical rather than systemic
- may diminish inflammation by blocking cyclo-oxygenase & inhibiting prostaglandin production in the colon Lialda cost about $275-$550 per month... compared to $236 for Asacol (2007)
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 356
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Jump up to: 5.0 5.1 Prescriber's Letter 14(3): 2007 Drug Therapy for Ulcerative Colitis Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230308&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 6.0 6.1 Kamm MA et al, Once daily, high concentration MMX mesalamine in active ulcerative colitis. Gastroenterology 2007, 132:66 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17241860
- ↑ Jump up to: 7.0 7.1 Deprecated Reference
- ↑ Jump up to: 8.0 8.1 8.2 8.3 8.4 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015