Rx Only

The active ingredient in Mesalamine Rectal Suspension 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:

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.

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 Enema 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 blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon.

Mesalamine Rectal Suspension Enema is indicated for the treatment of active mild to moderate distal ulcerative colitis, proctosigmoiditis or proctitis.

Mesalamine Rectal Suspension Enema is contraindicated for patients known to have hypersensitivity to the drug or any component of this medication.

Mesalamine Rectal Suspension Enema contains potassium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown but probably low. Sulfite sensitivity is seen more frequently in asthmatic or in atopic nonasthmatic persons.

Epinephrine is the preferred treatment for serious allergic or emergency situations even though epinephrine injection contains sodium or potassium metabisulfite with the above-mentioned potential liabilities. The alternatives to using epinephrine in a life-threatening situation may not be satisfactory. The presence of a sulfite(s) in epinephrine injection should not deter the administration of the drug for treatment of serious allergic or other emergency situations.

Mesalamine has been implicated in the production of an acute intolerance syndrome characterized by cramping, acute abdominal pain and bloody diarrhea, sometimes fever, headache and a rash; in such cases prompt withdrawal is required. The patient’s history of sulfasalazine intolerance, if any, should be re-evaluated. If a rechallenge is performed later in order to validate the hypersensitivity it should be carried out under close supervision and only if clearly needed, giving consideration to reduced dosage. In the literature one patient previously sensitive to sulfasalazine was rechallenged with 400 mg oral mesalamine; within eight hours she experienced headache, fever, intensive abdominal colic, profuse diarrhea and was readmitted as an emergency. She responded poorly to steroid therapy and two weeks later a pancolectomy was required.

Although renal abnormalities were not noted in the clinical trials with Mesalamine Rectal Suspension Enema, the possibility of increased absorption of mesalamine and concomitant renal tubular damage as noted in the preclinical studies must be kept in mind. Patients on Mesalamine Rectal Suspension Enema, especially those on concurrent oral products which liberate mesalamine and those with preexisting renal disease, should be carefully monitored with urinalysis, BUN (blood urea nitrogen), and creatinine studies.

In a clinical trial most patients who were hypersensitive to sulfasalazine were able to take mesalamine enemas without evidence of any allergic reaction. Nevertheless, caution should be exercised when mesalamine is initially used in patients known to be allergic to sulfasalazine. These patients should be instructed to discontinue therapy if signs of rash or fever become apparent.

While using Mesalamine Rectal Suspension Enema, some patients have developed pancolitis. However, extension of upper disease boundary and/or flare-ups occurred less often in the Mesalamine Rectal Suspension Enema treated group than in the placebo-treated group.

Worsening of colitis or symptoms of inflammatory bowel disease, including melena and hematochezia, may occur after commencing mesalamine.

Rare instances of pericarditis have been reported with mesalamine containing products including sulfasalazine. Cases of pericarditis have also been reported as manifestations of inflammatory bowel disease. In the cases reported with Mesalamine Rectal Suspension Enema, there have been positive rechallenges with mesalamine or mesalamine containing products. In one of these cases, however, a second rechallenge with sulfasalazine was negative throughout a 2-month follow-up. Chest pain or dyspnea in patients treated with Mesalamine Rectal Suspension Enema should be investigated with this information in mind. Discontinuation of Mesalamine Rectal Suspension Enema may be warranted in some cases, but rechallenge with mesalamine can be performed under careful clinical observation should the continued therapeutic need for mesalamine be present.

There have been no documented reports of serious toxicity in man resulting from massive overdosing with mesalamine. Under ordinary circumstances, mesalamine absorption from the colon is limited.

The usual dosage of Mesalamine Rectal Suspension Enema in 60 mL units is one rectal instillation (4 grams) once a day, preferably at bedtime, and retained for approximately eight hours. While the effect of Mesalamine Rectal Suspension Enema may be seen within 3 to 21 days, the usual course of therapy would be from 3 to 6 weeks depending on symptoms and sigmoidoscopic findings. Studies available to date have not assessed if Mesalamine Rectal Suspension Enema will modify relapse rates after the 6-week short-term treatment. Mesalamine Rectal Suspension Enema is for rectal use only.

Patients should be instructed to shake the bottle well to make sure the suspension is homogeneous. The patient should remove the protective sheath from the applicator tip. Holding the bottle at the neck will not cause any of the medication to be discharged. The position most often used is obtained by lying on the left side (to facilitate migration into the sigmoid colon); with the lower leg extended and the upper right leg flexed forward for balance. An alternative is the knee-chest position. The applicator tip should be gently inserted in the rectum pointing toward the umbilicus. A steady squeezing of the bottle will discharge most of the preparation. The preparation should be taken at bedtime with the objective of retaining it all night. Patient instructions are included with every seven units.

Mesalamine Rectal Suspension Enema for rectal administration is an off-white to tan colored suspension. Each disposable enema bottle contains 4 grams of mesalamine in 60 mL aqueous suspension. Enema bottles are supplied in boxed, foil-wrapped trays as follows:

 

Carton of 7 Bottles:           NDC 62559-420-07

Mesalamine Rectal Suspension Enemas are for rectal use only.

KEEP OUT OF REACH OF CHILDREN

Patient instructions are included.

Storage

Store at controlled room temperature 20° to 25°C (68° to 77°F); excursions permitted, please refer to current USP. 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 Enema 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

Distributed by:
ANI Pharmaceuticals, Inc.
Baudette, MN 56623

9819 Rev 07/17

For Medical Inquiries, Call Toll Free: 1-800-308-6755

How to Use this Medication.

Best results are achieved if the bowel is emptied immediately before the medication is given.

NOTE: Mesalamine Rectal Suspension Enema 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.

1. Remove the Bottles

1.

Remove the bottles from the protective foil pouch by tearing or by using scissors as shown, being careful not to squeeze or puncture bottles. Mesalamine Rectal Suspension Enema is an off-white to tan colored suspension. 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.

2. Prepare the Medication for Administration

1.

Shake the bottle well to make sure that the medication is thoroughly mixed.

2.

Remove the protective sheath from the applicator tip. Hold the bottle at the neck so as not to cause any of the medication to be discharged.

3. Assume the Correct Body Position

1.

Best results are obtained by lying on the left side with the left leg extended and the right leg flexed forward for balance.

1.

An alternative to lying on the left side is the “knee-chest” position as shown here.

4. Administer the Medication

1.

Gently insert the lubricated applicator tip into the rectum to prevent damage to the  rectal wall, pointed slightly toward the navel.

2.

Grasp the bottle firmly, then tilt slightly so that the nozzle is aimed toward the back, squeeze slowly to instill the medication. Steady hand pressure will discharge most of the medication. After administering, withdraw and discard the bottle.

1.

Remain in position for at least 30 minutes to allow thorough distribution of the medication internally. Retain the medication all night, if possible.

Rx only

Distributed by:
ANI Pharmaceuticals, Inc.
Baudette, MN 56623

9819 Rev 07/17

For Medical Inquiries, Call Toll Free: 1-800-308-6755

Mesalamine Rectal Suspension Enema, 4 g/60 mL
NDC 62559-420-07
FOR RECTAL USE ONLY
Rx only
7 x 60 mL Unit-Dose Bottles