MESALAMINE- mesalamine

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

MESALAMINE (UNII: 4Q81I59GXC) (MESALAMINE - UNII:4Q81I59GXC)

Available from:

Perrigo New York Inc

INN (International Name):

MESALAMINE

Composition:

MESALAMINE 4 g in 60 mL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Mesalamine Rectal Suspension, USP is indicated for the treatment of active mild to moderate distal ulcerative colitis, proctosigmoiditis or proctitis. Mesalamine Rectal Suspension, USP is contraindicated for patients known to have hypersensitivity to the drug or any component of this medication.

Product summary:

Mesalamine Rectal Suspension, USP, for rectal administration is an off-white to tan colored suspension. Each disposable enema bottle contains 4.0 grams of mesalamine in 60 mL aqueous suspension. Enema bottles are supplied in boxed, foil-wrapped trays as follows: Carton of 7 Bottles - NDC 45802-098 -51 Carton of 28 Bottles - NDC 45802-098 -28 Combo Kit with 7 Bottles and Wipes - NDC 45802-923 -41 Combo Kit with 28 Bottles and Wipes - NDC 45802-923 -49 Mesalamine Rectal Suspension USP, Enemas are for rectal use only. KEEP OUT OF REACH OF CHILDREN Patient instructions are included. Store at 20-25°C (68-77°F). [See USP Controlled Room Temperature]. Once the foil-wrapped unit of seven bottles is opened, all enemas should be used promptly as directed by your physician. Contents of enemas removed from the foil pouch may darken with time. Slight darkening will not affect potency, however, enemas with dark brown contents should be discarded. NOTE: Mesalamine Rectal Suspension, USP will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Take care in choosing a suitable location for administration of this product. Rx Only MADE IN ISRAEL MANUFACTURED BY PERRIGO, YERUHAM 80500, ISRAEL DISTRIBUTED BY PERRIGO® ALLEGAN, MI 49010 Rev. 11/09 2N900 RC J5

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

MESALAMINE- MESALAMINE
PERRIGO NEW YORK INC
----------
MESALAMINE RECTAL SUSPENSION USP, ENEMA
_RECTAL SUSPENSION_
_4 grams/unit (60 mL)_
_RX ONLY_
DESCRIPTION
The active ingredient in Mesalamine Rectal Suspension USP, Enema, a
disposable (60 mL) unit, is
mesalamine, also known as 5-aminosalicylic acid (5-ASA). Chemically,
mesalamine is 5-amino-2-
hydroxybenzoic acid.
The empirical formula is C7H7NO3, representing a molecular weight of
153.14. The structural formula
is:
STRUCTURAL FORMULA
Structural Formula
Each rectal suspension enema unit contains 4 grams of mesalamine. In
addition to mesalamine the
preparation contains the inactive ingredients carbomer 934P, edetate
disodium, potassium acetate,
potassium metabisulfite, purified water and xanthan gum. Sodium
benzoate is added as a preservative.
The disposable unit consists of an applicator tip protected by a
polyethylene cover and lubricated with
USP white petrolatum. The unit has a one-way valve to prevent back
flow of the dispensed product.
CLINICAL PHARMACOLOGY
Sulfasalazine is split by bacterial action in the colon into
sulfapyridine (SP) and mesalamine (5-ASA).
It is thought that the mesalamine component is therapeutically active
in ulcerative colitis [A.K. Azad
Khan et al, LANCET 2:892-895 (1977)]. The usual oral dose of
sulfasalazine for active ulcerative colitis
in adults is two to four grams per day in divided doses. Four grams of
sulfasalazine provide 1.6 g of
free mesalamine to the colon. Each Mesalamine Rectal Suspension, USP
delivers up to 4 g of
mesalamine to the left side of the colon.
The mechanism of action of mesalamine (and sulfasalazine) is unknown,
but appears to be topical rather
than systemic. Mucosal production of arachidonic acid (AA)
metabolites, both through the
cyclooxygenase pathways, i.e., prostanoids, and through the
lipoxygenase pathways, i.e., leukotrienes
(LTs) and hydroxyeicosatetraenoic acids (HETEs) is increased in
patients with chronic inflammatory
bowel disease, and it is possible that mesalamine diminishes
inflammation by