Classes
DEA Class; Rx
Common Brand Names; Pentasa, Delzicol, Lialda, Apriso, Asacol HD (DSC)
- 5-Aminosalicylic Acid Derivatives
mesalamine rectal (Rx)
- Classes: 5-Aminosalicylic Acid Derivatives
Description
5-aminosalicylate (5-ASA); available in oral and rectal formulations; clinical response is due to local effect
Used as an anti-inflammatory agent for ulcerative colitis; not considered effective for Crohn’s disease
Also used for ulcerative proctitis (rectal formulations, suppository and enema only)
Indications
Indicated for the treatment of mildly to moderately active ulcerative colitis.
Contraindications
Hypersensitivity to mesalamine or salicylates
Breastfeeding
Rectal suspension: Hypersensitivity to salicylates, aminosalicylates or to any ingredients in the suppository vehicle
Children with chickenpox or flulike symptoms
Adverse Effects
- Abdominal pain (4-8%)
- GI discomfort (4-8%)
- Headache (7%)
- Flatulence (1-6%)
- Nausea (1-6%)
- Fatigue (3%)
- Asthenia (3%)
- Malaise (3%)
- Weakness (3%)
- Fever (3%)
- Exacerbation of colitis (3%)
- Dizziness (2-3%)
- Rash (1-3%)
- Pruritus (1-3%)
- Acne (1-3%)
Warnings
Sulfasalazine hypersensitivity, renal insufficiency, coagulation abnormalities, pyloric stenosis
Use caution in active PUD, severe renal failure
Do not use with lactulose or drugs that lower intestinal pH
Although pericarditis rarely occurs, investigate any chest pain or dyspnea
Oligospermia has been reported in males
Hepatic failure may occur, particularly with preexisting liver impairment
May lead to falsely elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection, because of the similarity in the chromatograms of normetanephrine and mesalamine’s main metabolite, N-acetyl aminosalicylic acid; an alternative, selective assay for normetanephrine should be considered
Worsening of colitis/IBD may occur following initiation of therapy
Renal impairment, including minimal change nephropathy, acute and chronic interstitial nephritis, and renal failure, reported; cases of nephrolithiasis reported; mesalamine-containing stones are radiotransparent and undetectable by standard radiography or computed tomography (CT); ensure adequate fluid intake during treatment; evaluate renal function prior to initiation of therapy and periodically while on therapy
Evaluate renal function in all patients prior to initiation and periodically while on therapy; the risk of adverse reactions to this drug may be greater in patients with impaired renal function; mesalamine is known to be substantially excreted by the kidney; evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function
Acute intolerance syndrome may occur; symptoms include cramping, abdominal pain, bloody diarrhea, and sometimes fever, headache, malaise, pruritis, rash, conjunctivitis, and may be difficult to distinguish from an ulcerative colitis exacerbation; monitor for worsening symptoms; discontinue if acute intolerance syndrome suspected
Hypersensitivity reactions, including myocarditis and pericarditis reported; evaluate patients immediately and discontinue if hypersensitivity reaction suspected
Pregnancy and Lactation
Pregnancy: Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk
Lactation: Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or from underlying maternal conditions
Maximum Dosage
4 grams/day PR for rectal enema; 1 gram/day PR for rectal suppositories. For oral products: 1.5 grams/day PO for extended-release capsules (i.e., Apriso); 2.4 grams/day PO for delayed-release tablets or capsules (i.e, Delzicol); 4 grams/day PO for controlled-release capsules (i.e., Pentasa); 4.8 grams/day PO for delayed-release tablets (i.e., Asacol HD, Lialda).
4 grams/day PR for rectal enema; 1 gram/day PR for rectal suppositories. For oral products: 1.5 grams/day PO for extended-release capsules (i.e., Apriso); 2.4 grams/day PO for delayed-release tablets or capsules (i.e, Delzicol); 4 grams/day PO for controlled-release capsules (i.e., Pentasa); 4.8 grams/day PO for delayed-release tablets (i.e., Asacol HD, Lialda).
Delzicol – Maximum dosage determined by weight:
54 to 90 kg: 44 mg/kg/day PO (Max: 2.4 grams/day)
33 to 53 kg: 61 mg/kg/day PO (Max: 2 grams/day)
17 to 32 kg: 71 mg/kg/day PO (Max: 1.2 grams/day)
Lialda – Maximum dosage determined by weight:
More than 50 kg: 4.8 grams/day PO
More than 35 kg to 50 kg: 3.6 grams/day PO
24 kg to 35 kg: 2.4 grams/day PO
5 to 12 years: Maximum dosage determined by weight and product chosen:
Delzicol
54 to 90 kg: 44 mg/kg/day PO (Max: 2.4 grams/day)
33 to 53 kg: 61 mg/kg/day PO (Max: 2 grams/day)
17 to 32 kg: 71 mg/kg/day PO (Max: 1.2 grams/day)
Lialda
More than 50 kg: 4.8 grams/day PO
More than 35 kg to 50 kg: 3.6 grams/day PO
24 kg to 35 kg: 2.4 grams/day PO
1 to 4 years: Safety and efficacy have not been established; off-label use reported for some formulations in children as young as 4 years of age.
Safety and efficacy have not been established.
How supplied
Mesalamine
capsule, extended-release
- 250mg (Pentasa)
- 375mg (Apriso, generic)
- 500mg (Pentasa, generic)
tablet, delayed-release
- 1.2g (Lialda, generic)
capsule, delayed-release
- 400mg (Delzicol, generic)
rectal suppository
- 1g (Canasa)
rectal suspension enema
- 4g/60mL (Rowasa)