Lialda- Once-daily ulcerative

Company:

Shire

Pharmacologic class:

Aminosalicylate

Active ingredient:

Mesalamine 1.2 g; delayed-release tabs.

Indication:

To induce remission in active, mild-to-moderate ulcerative colitis.

Pharmacology:

Mesalamine is an anti-inflammatory agent that is commonly used as a treatment for the induction of remission in patients with ulcerative colitis. It is available in several formulations, including suppositories, enemas, tablets, and capsules.

Unlike other marketed oral mesalamine products, Lialda is dosed on a once-daily basis. Lialda contains mesalamine in a delayed-release tablet for oral administration. The tablets are coated with a pH-dependent film that resists breakdown until the tablets reach the relatively alkaline environment of the terminal ileum. Here, in the colon, the site of inflammation in ulcerative colitis, mesalamine is released from the tablet core.

The mechanism of action of mesalamine (also known as 5-aminosalicylic acid) appears to be topical rather than systemic. Data suggests that it reduces inflammation by blocking cyclooxygenase and inhibiting the production of prostaglandins in the colon; mechanisms on the nuclear level may contribute to its effects as well.

Taking Lialda with a high-fat meal results in a delay in absorption and an increase in systemic absorption of mesalamine compared to the fasted state.

Clinical trials:

Two randomized, double-blind, placebo-controlled studies were conducted in 517 patients with active, mild-to-moderate ulcerative colitis. Lialda was dosed at 2.4 g/day (as 1.2 g twice daily or 2.4 g once daily) and at 4.8 g/day; treatment was given for eight weeks. Remission was defined as an Ulcerative Colitis Activity Index of ≤1, with scores of zero for rectal bleeding and for stool frequency, and a sigmoidoscopy score reduction of 1 point or more from baseline. In both studies, Lialda dosed at either 2.4 g/day or 4.8 g/day was superior to placebo in the percentage of patients in remission after eight weeks. In Study 1, 34.1% of patients dosed at 2.4 g/day and 29.2% of patients dosed at 4.8 g/day were in remission at week 8, compared with 12.9% of patients given placebo. In Study 2, 40.5% of the patients given 2.4 g/day and 41.2% of patients treated with 4.8 g/day were in remission at week 8, compared with 22.1% for placebo. Lialda treatment also resulted in benefits in clinical improvement, treatment failure, clinical remission, and sigmoidoscopic improvement.

Adults:

≥18 years: Swallow whole with a meal. 2.4-4.8 g once daily for up to eight weeks.

Children:

<18 years: not recommended. Geriatric patients: Evaluate renal function before starting therapy and periodically during treatment.

Precautions:

Sulfasalazine allergy. Pyloric stenosis. Conditions predisposing to myocarditis or pericarditis. Renal or hepatic impairment. Pregnancy (Cat. B). Nursing mothers. Interactions: Increased toxicity with nephrotoxic drugs (e.g., NSAIDs), 6-mercaptopurine, azathioprine.

Adverse reactions:

Headache, flatulence; acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea, fever, headache, rash) (discontinue if suspected), renal impairment, cardiac hypersensitivity reactions, pancreatitis (rare).

How supplied:

Tabs—120.

For more information, call 800.536.7878, or visit www.Lialda.com.

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