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| Product NDC Code | 63629-2397 | ||||
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| Drug Name | Mesalamine |
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| Type | Generic | ||||
| Pharm Class | Aminosalicylate [EPC], Aminosalicylic Acids [CS] |
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| Active Ingredients |
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| Route | RECTAL | ||||
| Dosage Form | SUPPOSITORY | ||||
| RxCUI drug identifier | 248420 | ||||
| Application Number | ANDA207448 | ||||
| Labeler Name | Bryant Ranch Prepack | ||||
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Overdosage of Mesalamine
Information about signs, symptoms, and laboratory findings of acute ovedosage and the general principles of overdose treatment.10 OVERDOSAGE There have been no documented reports of serious toxicity in man resulting from massive overdosing with mesalamine suppository. Under ordinary circumstances, mesalamine absorption from the colon is limited.
Adverse reactions
Information about undesirable effects, reasonably associated with use of the drug, that may occur as part of the pharmacological action of the drug or may be unpredictable in its occurrence. Adverse reactions include those that occur with the drug, and if applicable, with drugs in the same pharmacologically active and chemically related class. There is considerable variation in the listing of adverse reactions. They may be categorized by organ system, by severity of reaction, by frequency, by toxicological mechanism, or by a combination of these.6 ADVERSE REACTIONS The most serious adverse reactions seen in mesalamine suppositories clinical trials or with other products that contain or are metabolized to mesalamine are: • Renal Impairment [ see Warnings and Precautions (5.1) ] • Mesalamine-Induced Acute Intolerance Syndrome [ see Warnings and Precautions (5.2) ] • Hypersensitivity Reactions [ see Warnings and Precautions (5.3) ] • Hepatic Failure [ see Warnings and Precautions (5.4) ] The most common adverse reactions (≥ 1%) are: dizziness, rectal pain, fever, rash, acne and colitis. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Rising Pharmaceuticals, Inc. at 1-866-562-4597 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions in adult patients with mildly to moderately active ulcerative proctitis in double-blind, placebo-controlled trials are summarized in the Table 1 below. Table 1: Adverse Reactions Occurring In More Than 1% of Mesalamine Suppository Treated Patients (Comparison to Placebo) Symptom Mesalamine (n = 177) Placebo (n = 84) N % N % Dizziness 5 3 2 2.4 Rectal Pain 3 1.8 0 0 Fever 2 1.2 0 0 Rash 2 1.2 0 0 Acne 2 1.2 0 0 Colitis 2 1.2 0 0 In a multicenter, open-label, randomized, parallel group study in 99 patients comparing the mesalamine 1000 mg suppository administered nightly to that of the mesalamine 500 mg suppository twice daily. The most common adverse reactions in both groups were headache (14%), flatulence (5%), abdominal pain (5%), diarrhea (3%), and nausea (3%). Three (3) patients discontinued medication because of an adverse reaction; one of these adverse reactions (headache) was deemed possibly related to study medication. The recommended dosage of mesalamine suppositories is 1000 mg administered rectally once daily at bedtime [ see Dosage and Administration (2) ] . 6.2 Postmarketing Experience In addition to the adverse reactions reported above in clinical trials involving mesalamine suppositories, the adverse reactions listed below have been identified during post-approval use of mesalamine suppositories and other mesalamine-containing products. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. • Body as a Whole: drug fever, fatigue, lupus-like syndrome, medication residue • Cardiac Disorders : myocarditis, pericarditis, pericardial effusion [ see Warnings and Precautions (5.3) ] • Endocrine: Nephrogenic diabetes insipidus • Eye disorders: eye swelling • Gastrointestinal Disorders: abdominal cramps, abdominal distension, anal pruritus, anorectal discomfort, constipation, feces discolored, flatulence, frequent bowel movements, gastrointestinal bleeding, mucus stools, nausea, painful defecation, pancreatitis, proctalgia, rectal discharge, rectal tenesmus, stomach discomfort, vomiting • Hepatic Disorders : cholestatic jaundice, hepatitis, jaundice, Kawasaki-like syndrome including changes in liver enzymes, liver necrosis, liver failure • Hematologic Disorders: agranulocytosis, aplastic anemia, thrombocytopenia • Neurological/Psychiatric Disorders : Guillain-Barre syndrome, peripheral neuropathy, transverse myelitis, intracranial hypertension • Renal Disorders: interstitial nephritis, renal failure, minimal change nephropathy [ see Warnings and Precautions (5.1) ] • Respiratory, Thoracic and Mediastinal Disorders : hypersensitivity pneumonitis (including allergic alveolitis, eosinophilic pneumonitis, interstitial pneumonitis) • Skin and Subcutaneous Tissue Disorder : alopecia, erythema, erythema nodosum, pruritus, psoriasis, pyoderma gangrenosum, urticaria • Urogenital: reversible oligospermia
| Dizziness | 5 | 3 | 2 | 2.4 |
| Rectal Pain | 3 | 1.8 | 0 | 0 |
| Fever | 2 | 1.2 | 0 | 0 |
| Rash | 2 | 1.2 | 0 | 0 |
| Acne | 2 | 1.2 | 0 | 0 |
| Colitis | 2 | 1.2 | 0 | 0 |
Mesalamine Drug Interactions
Information about and practical guidance on preventing clinically significant drug/drug and drug/food interactions that may occur in people taking the drug.7 DRUG INTERACTIONS • Nephrotoxic Agents including NSAIDs : Increased risk of nephrotoxicity; monitor for changes in renal function and mesalamine-related adverse reactions. ( 7.1 ) • Azathioprine or 6-Mercaptopurine : Increased risk of blood disorders; monitor complete blood cell counts and platelet counts. ( 7.2) 7.1 Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs The concurrent use of mesalamine with known nephrotoxic agents, including nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of nephrotoxicity. Monitor patients taking nephrotoxic drugs for changes in renal function and mesalamine-related adverse reactions [ see Warnings and Precautions (5.1)]. 7.2 Azathioprine or 6-Mercaptopurine The concurrent use of mesalamine with azathioprine or 6-mercaptopurine may increase the risk for blood disorders. If concomitant use of mesalamine suppositories and azathioprine or 6-mercaptopurine cannot be avoided, monitor blood tests, including complete blood cell counts and platelet counts. 7.3 Urinary Normetanephrine Measurements Use of mesalamine may lead to spuriously 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-acetylaminosalicylic acid. Consider an alternative, selective assay for normetanephrine [ see Warnings and Precautions (5.5) ].
Clinical pharmacology
Information about the clinical pharmacology and actions of the drug in humans.12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism of action of mesalamine is not fully understood, but appears to be topical rather than systemic. Although the pathology of inflammatory bowel disease is uncertain, both prostaglandins and leukotrienes have been implicated as mediators of mucosal injury and inflammation. 12.3 Pharmacokinetics Absorption Mesalamine (5-ASA) administered as a rectal suppository is variably absorbed. In patients with ulcerative colitis treated with mesalamine 500 mg rectal suppositories, administered once every eight hours for six days, the mean mesalamine peak plasma concentration (C max ) was 353 ng/mL (CV=55%) following the initial dose and 361 ng/mL (CV=67%) at steady state. The mean minimum steady state plasma concentration (C min ) was 89 ng/mL (CV=89%). Absorbed mesalamine does not accumulate in the plasma. Distribution Mesalamine administered as a rectal suppository distributes in rectal tissue to some extent. Elimination In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, the mean elimination half-life was 5 hours (CV=73%) for 5-ASA and 5 hours (CV=63%) for N-acetyl-5-ASA, the active metabolite, following the initial dose. At steady state, the mean elimination half-life was 7 hours for both 5-ASA and N-acetyl-5-ASA (CV=102% for 5-ASA and 82% for N-acetyl-5-ASA). Metabolism The absorbed mesalamine is extensively metabolized, mainly to N-acetyl-5-ASA in the liver and in the gut mucosal wall. In patients with ulcerative colitis treated with one mesalamine 500 mg rectal suppository every eight hours for six days, the peak concentration (C max ) of N-acetyl-5-ASA ranged from 467 ng/mL to 1399 ng/mL following the initial dose and from 193 ng/mL to 1304 ng/mL at steady state. Excretion Mesalamine is eliminated from plasma mainly by urinary excretion, predominantly as N-acetyl-5-ASA. In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, 12% or less of the dose was eliminated in urine as unchanged 5-ASA and 8% to 77% was eliminated as N-acetyl-5-ASA following the initial dose. At steady state, 11% or less of the dose was eliminated in the urine as unchanged 5-ASA and 3% to 35% was eliminated as N-acetyl-5-ASA.
Mechanism of action
Information about the established mechanism(s) of the drugÕs action in humans at various levels (for example receptor, membrane, tissue, organ, whole body). If the mechanism of action is not known, this field contains a statement about the lack of information.12.1 Mechanism of Action The mechanism of action of mesalamine is not fully understood, but appears to be topical rather than systemic. Although the pathology of inflammatory bowel disease is uncertain, both prostaglandins and leukotrienes have been implicated as mediators of mucosal injury and inflammation.
Pharmacokinetics
Information about the clinically significant pharmacokinetics of a drug or active metabolites, for instance pertinent absorption, distribution, metabolism, and excretion parameters.12.3 Pharmacokinetics Absorption Mesalamine (5-ASA) administered as a rectal suppository is variably absorbed. In patients with ulcerative colitis treated with mesalamine 500 mg rectal suppositories, administered once every eight hours for six days, the mean mesalamine peak plasma concentration (C max ) was 353 ng/mL (CV=55%) following the initial dose and 361 ng/mL (CV=67%) at steady state. The mean minimum steady state plasma concentration (C min ) was 89 ng/mL (CV=89%). Absorbed mesalamine does not accumulate in the plasma. Distribution Mesalamine administered as a rectal suppository distributes in rectal tissue to some extent. Elimination In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, the mean elimination half-life was 5 hours (CV=73%) for 5-ASA and 5 hours (CV=63%) for N-acetyl-5-ASA, the active metabolite, following the initial dose. At steady state, the mean elimination half-life was 7 hours for both 5-ASA and N-acetyl-5-ASA (CV=102% for 5-ASA and 82% for N-acetyl-5-ASA). Metabolism The absorbed mesalamine is extensively metabolized, mainly to N-acetyl-5-ASA in the liver and in the gut mucosal wall. In patients with ulcerative colitis treated with one mesalamine 500 mg rectal suppository every eight hours for six days, the peak concentration (C max ) of N-acetyl-5-ASA ranged from 467 ng/mL to 1399 ng/mL following the initial dose and from 193 ng/mL to 1304 ng/mL at steady state. Excretion Mesalamine is eliminated from plasma mainly by urinary excretion, predominantly as N-acetyl-5-ASA. In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, 12% or less of the dose was eliminated in urine as unchanged 5-ASA and 8% to 77% was eliminated as N-acetyl-5-ASA following the initial dose. At steady state, 11% or less of the dose was eliminated in the urine as unchanged 5-ASA and 3% to 35% was eliminated as N-acetyl-5-ASA.
Contraindications
Information about situations in which the drug product is contraindicated or should not be used because the risk of use clearly outweighs any possible benefit, including the type and nature of reactions that have been reported.4 CONTRAINDICATIONS Mesalamine suppositories are contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any ingredients in the suppository vehicle [ see Warnings and Precautions (5.3), Adverse Reactions (6.2) , and Description (11 )]. Known or suspected hypersensitivity to salicylates or aminosalicylates or to any or to any ingredients in the formulation. ( 4 , 5 .3 )
Description
General information about the drug product, including the proprietary and established name of the drug, the type of dosage form and route of administration to which the label applies, qualitative and quantitative ingredient information, the pharmacologic or therapeutic class of the drug, and the chemical name and structural formula of the drug.11 DESCRIPTION The active ingredient in mesalamine suppositories 1000 mg for rectal use is mesalamine, also known as mesalazine or 5-aminosalicylic acid (5-ASA). Chemically, mesalamine is 5-amino-2-hydroxybenzoic acid, and is classified as an anti-inflammatory drug. Each mesalamine suppository contains 1000 mg of mesalamine (USP) in a base of Hard Fat, NF. The empirical formula is C 7 H 7 NO 3 , representing a molecular weight of 153.14. The structural formula is:
Dosage and administration
Information about the drug product’s dosage and administration recommendations, including starting dose, dose range, titration regimens, and any other clinically sigificant information that affects dosing recommendations.2 DOSAGE AND ADMINISTRATION Dosage The recommended dosage of mesalamine suppositories in adults is 1000 mg administered rectally once daily at bedtime for 3 to 6 weeks depending on symptoms and sigmoidoscopic findings. Safety and effectiveness of mesalamine suppositories beyond 6 weeks have not been established. Administration Instructions : • Evaluate renal function prior to initiation of mesalamine suppositories therapy and periodically while on therapy. • Do not cut or break the suppository. • Retain the suppository for one to three hours or longer, if possible. • If a dose of mesalamine suppositories is missed, administer as soon as possible, unless it is almost time for next dose. Do not use two mesalamine suppositories at the same time to make up for a missed dose. • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Keep mesalamine suppositories away from these surfaces to prevent staining. Dosage The recommended adult dosage is 1000 mg administered rectally once daily at bedtime for 3 to 6 weeks. Safety and effectiveness beyond 6 weeks have not been established.( 2 ) Administration Instructions: • Evaluate renal function prior to initiation of mesalamine suppositories and periodically while on therapy ( 2.1 , 5.1 ) • Do not cut or break the suppository. • Retain the suppository for one to three hours or longer, if possible. • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Keep MESALAMINE SUPPOSITORIES away from these surfaces to prevent staining.
Dosage forms and strengths
Information about all available dosage forms and strengths for the drug product to which the labeling applies. This field may contain descriptions of product appearance.3 DOSAGE FORMS AND STRENGTHS Mesalamine suppositories: 1000 mg mesalamine in a bullet shaped, light tan to grey suppository. Suppository: 1000 mg
Indications and usage
A statement of each of the drug products indications for use, such as for the treatment, prevention, mitigation, cure, or diagnosis of a disease or condition, or of a manifestation of a recognized disease or condition, or for the relief of symptoms associated with a recognized disease or condition. This field may also describe any relevant limitations of use.1 INDICATIONS AND USAGE Mesalamine suppositories are indicated in adults for the treatment of mildly to moderately active ulcerative proctitis. Mesalamine suppositories are an aminosalicylate indicated in adults for the treatment of mildly to moderately active ulcerative proctitis.
Spl product data elements
Usually a list of ingredients in a drug product.Mesalamine Mesalamine MESALAMINE MESALAMINE HARD FAT Light Tan to Grey chemical-structure
Animal pharmacology and or toxicology
Information from studies of the drug in animals, if the data were not relevant to nor included in other parts of the labeling. Most labels do not contain this field.13.2 Animal Toxicology and/or Pharmacology Toxicology studies of mesalamine were conducted in rats, mice, rabbits and dogs, and the kidney was the main target organ of toxicity. In rats, adverse renal effects were observed at a single oral dose of 600 mg/kg (about 3.2 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and at intravenous doses of >214 mg/kg (about 1.2 times the recommended human intra- rectal dose of mesalamine suppositories, based on body surface area). In a 13-week oral gavage toxicity study in rats, papillary necrosis and/or multifocal tubular injury were observed in males receiving 160 mg/kg (about 0.86 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and in both males and females at 640 mg/kg (about 3.5 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area). In a combined 52-week toxicity and 127-week carcinogenicity study in rats, degeneration of the kidneys and hyalinization of basement membranes and Bowman's capsule were observed at oral doses of 100 mg/kg/day (about 0.54 times the recommended human intra- rectal dose of mesalamine suppositories, based on body surface area) and above. In a 14-day rectal toxicity study of mesalamine suppositories in rabbits, intra-rectal doses up to 800 mg/kg (about 8.6 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) was not associated with any adverse effects. In a six-month oral toxicity study in dogs, doses of 80 mg/kg (about 1.4 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and higher caused renal pathology similar to that described for the rat. In a rectal toxicity study of mesalamine suppositories in dogs, a dose of 166.6 mg/kg (about 3 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) produced chronic nephritis and pyelitis. In the 12-month eye toxicity study in dogs, keratoconjunctivitis sicca (KCS) occurred at oral doses of 40 mg/kg (about 0.72 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and above.
Carcinogenesis and mutagenesis and impairment of fertility
Information about carcinogenic, mutagenic, or fertility impairment potential revealed by studies in animals. Information from human data about such potential is part of the warnings field.13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Mesalamine caused no increase in the incidence of neoplastic lesions over controls in a two-year study of Wistar rats fed up to 320 mg/kg/day of mesalamine admixed with diet (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area). Mesalamine was not mutagenic in the Ames test, the mouse lymphoma cell (TK +/- ) forward mutation test, or the mouse micronucleus test. No effects on fertility or reproductive performance of the male and female rats were observed at oral mesalamine doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area).
Nonclinical toxicology
Information about toxicology in non-human subjects.13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Mesalamine caused no increase in the incidence of neoplastic lesions over controls in a two-year study of Wistar rats fed up to 320 mg/kg/day of mesalamine admixed with diet (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area). Mesalamine was not mutagenic in the Ames test, the mouse lymphoma cell (TK +/- ) forward mutation test, or the mouse micronucleus test. No effects on fertility or reproductive performance of the male and female rats were observed at oral mesalamine doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area). 13.2 Animal Toxicology and/or Pharmacology Toxicology studies of mesalamine were conducted in rats, mice, rabbits and dogs, and the kidney was the main target organ of toxicity. In rats, adverse renal effects were observed at a single oral dose of 600 mg/kg (about 3.2 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and at intravenous doses of >214 mg/kg (about 1.2 times the recommended human intra- rectal dose of mesalamine suppositories, based on body surface area). In a 13-week oral gavage toxicity study in rats, papillary necrosis and/or multifocal tubular injury were observed in males receiving 160 mg/kg (about 0.86 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and in both males and females at 640 mg/kg (about 3.5 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area). In a combined 52-week toxicity and 127-week carcinogenicity study in rats, degeneration of the kidneys and hyalinization of basement membranes and Bowman's capsule were observed at oral doses of 100 mg/kg/day (about 0.54 times the recommended human intra- rectal dose of mesalamine suppositories, based on body surface area) and above. In a 14-day rectal toxicity study of mesalamine suppositories in rabbits, intra-rectal doses up to 800 mg/kg (about 8.6 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) was not associated with any adverse effects. In a six-month oral toxicity study in dogs, doses of 80 mg/kg (about 1.4 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and higher caused renal pathology similar to that described for the rat. In a rectal toxicity study of mesalamine suppositories in dogs, a dose of 166.6 mg/kg (about 3 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) produced chronic nephritis and pyelitis. In the 12-month eye toxicity study in dogs, keratoconjunctivitis sicca (KCS) occurred at oral doses of 40 mg/kg (about 0.72 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and above.
Package label principal display panel
The content of the principal display panel of the product package, usually including the product’s name, dosage forms, and other key information about the drug product.Mesalamine 1000 mg Suppository, #30 Label
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Information not classified as belonging to one of the other fields. Approximately 40% of labeling with effective_time between June 2009 and August 2014 have information in this field.17 PATIENT COUNSELING INFORMATION Advise patients to read the FDA-approved patient labeling (Patient Information) Administration Advise patients: • Do not cut or break the suppository. • Retain the suppository for one to three hours or longer, if possible. • If a dose of mesalamine suppositories is missed, administer as soon as possible, unless it is almost time for next dose. Do not use two mesalamine suppositories at the same time to make up for a missed dose. • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Keep mesalamine suppositories away from these surfaces to prevent staining. Renal Impairment Inform patients that mesalamine suppositories may decrease their renal function, especially if they have known renal impairment or are taking nephrotoxic drugs, including NSAIDs, and periodic monitoring of renal function will be performed while they are on therapy. Advise patients to complete all blood tests ordered by their healthcare provider [ see Warnings and Precautions (5.1) , Drug Interactions (7.1) ]. Mesalamine-Induced Acute Intolerance Syndrome and Other Hypersensitivity Reactions Inform patients of the signs and symptoms of hypersensitivity reactions. Instruct patients to stop taking mesalamine suppositories and report to their healthcare provider if they experience new or worsening symptoms Acute Intolerance Syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, and rash) or other symptoms suggestive of mesalamine-induced hypersensitivity [ see Warnings and Precautions (5.2, 5.3) ]. Hepatic Failure Inform patients with known liver disease of the signs and symptoms of worsening liver function and advise them to report to their healthcare provider if they experience such signs or symptoms [ see Warnings and Precautions (5.4) ]. Blood Disorders Inform elderly patients and those taking azathioprine or 6-mercaptopurine of the risk for blood disorders and the need for periodic monitoring of complete blood cell counts and platelet counts while on therapy. Advise patients to complete all blood tests ordered by their healthcare provider [ see Drug Interactions (7.2) , Use in Specific Populations (8.5)]. Distributed by: Rising Pharmaceuticals, Inc. Saddle Brook, NJ 07663 Manufactured by: Halo Pharmaceuticals, Inc. Whippany, NJ 07981 .
PATIENT INFORMATION MESALAMINE (me SAL a meen) suppositories, for rectal use What are mesalamine suppositories? Mesalamine suppositories are a prescription medicine used to treat active ulcerative proctitis (ulcerative rectal colitis). It is not known if mesalamine suppositories are safe and effective in children. Who should not use mesalamine suppositories? Do not use mesalamine suppositories if you are: • allergic to medicines that contain salicylates, including aspirin. • allergic to mesalamine or any of the ingredients in mesalamine. See the end of this leaflet for a complete list of ingredients in mesalamine suppositories. Ask your doctor if you are not sure if your medicine is listed above. Before using mesalamine suppositories, tell your doctor if you: • have a history of allergic reaction to the medicine sulfasalazine (Azulfidine) • have kidney problems • have ever had inflammation of the sac around your heart (pericarditis). • have liver problems • have any other medical conditions • are pregnant or plan to become pregnant. It is not known if mesalamine suppositories can harm your unborn baby. • are breastfeeding or plan to breastfeed. Mesalamine can pass into your breast milk. Talk to your doctor about the best way to feed your baby if you use mesalamine suppositories. Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Using mesalamine suppositories with certain other medicines may affect each other. Using mesalamine suppositories with other medicines can cause serious side effects. Especially tell your doctor if you take nonsteroidal anti-inflammatory drugs (NSAIDS), or medicines that contain azathioprine or 6-mercaptopurine. Taking mesalamine suppositories with NSAIDS may cause kidney problems. Taking mesalamine suppositories with azathioprine or 6-mercaptopurine may cause blood problems. You doctor may do certain tests during treatment with mesalamine suppositories. Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine. How should I use mesalamine suppositories? • Use mesalamine suppositories exactly as prescribed by your doctor. Your doctor will tell you how long to continue using mesalamine suppositories. • Mesalamine suppositories come as a suppository that you insert into your rectum. • Do not cut or break the suppository. • Use mesalamine suppositories 1 time each day at bedtime, for 3 to 6 weeks. It is not known if mesalamine suppositories are safe and effective for use for longer than 6 weeks. • After you insert mesalamine suppositories into your rectum, try to keep (retain) the suppository in your rectum for 1 to 3 hours or longer if possible. • If you miss a dose of mesalamine suppositories, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Take the next dose at your regular time. Do not take 2 doses at the same time. • Mesalamine suppositories can stain surfaces including clothing and other fabrics, flooring, painted surfaces, marble, granite, vinyl and enamel. Keep mesalamine suppositories away from these surfaces to prevent staining. What are the possible side effects of mesalamine suppositories? Mesalamine suppositories may cause serious side effects, including: • Kidney problems. Your doctor will do certain tests before you start using mesalamine suppositories and during your treatment with mesalamine suppositories. • Acute Intolerance Syndrome or Other Allergic Reactions. Some people who use mesalamine suppositories can have allergic type reactions, including “Acute Intolerance Syndrome.” Other allergic reactions can cause heart problems including an inflammation of the sac around the heart (pericarditis), blood problems, and problems with other organs in the body including the kidneys, liver and lungs. These problems usually happen in people who have had an allergic reaction to medicines containing sulfasalazine. Stop using mesalamine suppositories and tell your doctor right away if you get any of these symptoms: o cramps o stomach (abdominal) pain o bloody diarrhea o chest pain o decrease in the amount of urine o fever o headache o rash o shortness of breath o fatigue • Liver problems. This can happen in people who have a history of liver problems and have taken other medicines that contain mesalamine. Tell your doctor right away if you get any of these symptoms while using mesalamine suppositories: o yellowing of your eyes o itchy skin o feeling very tired o flu-like symptoms o nausea or vomiting The most common side effects of mesalamine suppositories include: o dizziness o acne o inflammation of the large intestine (colitis) o rectal pain o fever o rash These are not all of the possible side effects of mesalamine suppositories. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. How should I store mesalamine suppositories? • Store mesalamine suppositories at room temperature below 77°F (25°C). • Mesalamine suppositories may be refrigerated. • Keep mesalamine suppositories away from direct heat, light, or humidity. Keep mesalamine suppositories and all medicines out of the reach of children. General information about the safe and effective use of mesalamine suppositories. Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use mesalamine suppositories for a condition for which it was not prescribed. Do not give mesalamine suppositories to other people, even if they have the same symptoms you have. It may harm them. You can ask your doctor or pharmacist for information about mesalamine suppositories that is written for health professionals. What are the ingredients in mesalamine suppositories? Active ingredients: Mesalamine Inactive ingredients: Hard Fat base Distributed by: Rising Pharmaceuticals, Inc. Saddle Brook, NJ 07663 Manufactured by: Halo Pharmaceuticals, Inc. Whippany, NJ 07981 This Patient Information has been approved by the U.S. Food and Drug Administration Revised: 02/2019
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Information necessary for patients to use the drug safely and effectively..
Clinical studies
This field may contain references to clinical studies in place of detailed discussion in other sections of the labeling.14 CLINICAL STUDIES Two double-blind, placebo-controlled, multicenter trials of mesalamine suppositories were conducted in North America in adult patients with mildly to moderately active ulcerative proctitis. The regimen in Study 1 was a 500 mg mesalamine suppository administered rectally three times daily and in Study 2 was a 500 mg mesalamine suppository administered rectally twice daily. In both trials, patients had an average extent of proctitis (upper disease boundary) of approximately 10 cm and approximately 80% of patients had multiple prior episodes of proctitis. A total of 173 patients were evaluated (Study 1, N=79; Study 2, N=94), of which 89 patients received mesalamine, and 84 patients received placebo. The mean age of patients was 39 years (range 17 to 73 years), 60% were female, and 97% were white. The primary measures of efficacy were clinical disease activity index (DAI) and histologic evaluations in both trials. The DAI is a composite index reflecting rectal bleeding, stool frequency, mucosal appearance at endoscopy, and a physician's global assessment of disease. Patients were evaluated clinically and sigmoidoscopically after 3 and 6 weeks of treatment. Compared to placebo, mesalamine suppositories were statistically (p<0.01) superior to placebo in both trials with respect to improvement in stool frequency, rectal bleeding, mucosal appearance, disease severity, and overall disease activity after 3 and 6 weeks of treatment. The effectiveness of mesalamine suppositories was statistically significant irrespective of sex, extent of proctitis, duration of current episode, or duration of disease. An additional multicenter, open-label, randomized, parallel group study in 99 patients diagnosed with mildly to moderately ulcerative proctitis compared 1000 mg mesalamine suppositories administered rectally once daily at bedtime (N=35) to 500 mg mesalamine suppository administered rectally twice daily, in the morning and at bedtime (N=46), for 6 weeks. The primary measures of efficacy included the clinical disease activity index (DAI) and histologic evaluations. Patients were evaluated clinically and sigmoidoscopically at 3 and 6 weeks of treatment. The efficacy at 6 weeks was not different between the treatment groups. Both were effective in the treatment of ulcerative proctitis and resulted in a significant decrease at 6 weeks in DAI: in the mesalamine 500 mg twice daily group, the mean DAI value decreased from 6.6 to 1.6, and in the 1000 mg at bedtime group, the mean DAI value decreased from 6.2 to 1.3, which represents a decrease of greater than 75% in both groups. After 6 weeks of treatment, a DAI score of less than 3 was achieved in 78% of patients in the mesalamine 500 mg twice daily group and 86% of patients in the mesalamine suppositories 1000 mg once daily group. The recommended dosage of mesalamine suppositories is 1000 mg administered rectally once daily at bedtime [ see Dosage and Administration (2) ].
Geriatric use
Information about any limitations on any geriatric indications, needs for specific monitoring, hazards associated with use of the drug in the geriatric population.8.5 Geriatric Use Clinical trials of mesalamine suppositories did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Systemic exposures are increased in elderly subjects [ See Clinical Pharmacology (12.3) ] . Reports from uncontrolled clinical studies and postmarketing reporting systems suggested a higher incidence of blood dyscrasias (i.e., agranulocytosis, neutropenia and pancytopenia) in patients receiving mesalamine-containing products such as mesalamine suppositories who were 65 years or older compared to younger patients. Monitor complete blood cell counts and platelet counts in elderly patients during treatment with mesalamine suppositories. In general, the greater frequency of decreased hepatic, renal, or cardiac function, and of concurrent disease or other drug therapy in elderly patients should be considered when prescribing mesalamine suppositories [ see Use in Specific Populations (8.6) ].
Pediatric use
Information about any limitations on any pediatric indications, needs for specific monitoring, hazards associated with use of the drug in any subsets of the pediatric population (such as neonates, infants, children, or adolescents), differences between pediatric and adult responses to the drug, and other information related to the safe and effective pediatric use of the drug.8.4 Pediatric Use The safety and effectiveness of mesalamine suppositories in pediatric patients for the treatment of mildly to moderately active ulcerative proctitis have not been established. Information describing a clinical study in which efficacy was not demonstrated in pediatric patients ages 5 to 17 years is approved for Forest Laboratories, LLC’s CANASA (mesalamine) rectal suppositories. However, due to Forest Laboratories, LLC’s marketing exclusivity rights, this drug product is not labeled with that pediatric information.
Pregnancy
Information about effects the drug may have on pregnant women or on a fetus. This field may be ommitted if the drug is not absorbed systemically and the drug is not known to have a potential for indirect harm to the fetus. It may contain information about the established pregnancy category classification for the drug. (That information is nominally listed in the teratogenic_effects field, but may be listed here instead.)8.1 Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No evidence of teratogenicity was observed in rats or rabbits when treated during gestation with orally administered mesalamine at doses greater than the recommended human intra-rectal dose [ see Data ]. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Reproduction studies have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and in rabbits at oral doses up to 495 mg/kg/day (about 5.4 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) following administration during the period of organogenesis, and have revealed no evidence of impaired fertility or harm to the fetus due to mesalamine.
Use in specific populations
Information about use of the drug by patients in specific populations, including pregnant women and nursing mothers, pediatric patients, and geriatric patients.8 USE IN SPECIFIC POPULATIONS • Geriatric Patients: Increased risk of blood dyscrasias; monitor complete blood cell counts and platelet counts. (8.5) 8.1 Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No evidence of teratogenicity was observed in rats or rabbits when treated during gestation with orally administered mesalamine at doses greater than the recommended human intra-rectal dose [ see Data ]. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Reproduction studies have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) and in rabbits at oral doses up to 495 mg/kg/day (about 5.4 times the recommended human intra-rectal dose of mesalamine suppositories, based on body surface area) following administration during the period of organogenesis, and have revealed no evidence of impaired fertility or harm to the fetus due to mesalamine. 8.2 Lactation Risk Summary Mesalamine and its N-acetyl metabolite are present in human milk in undetectable to small amounts [see Data] . There are limited reports of diarrhea in breastfed infants. There is no information on the effects of the drug on milk production. The lack of clinical data during lactation precludes a clear determination of the risk of mesalamine suppositories to an infant during lactation; therefore, the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for mesalamine suppositories and any potential adverse effects on the breastfed child from mesalamine suppositories or from the underlying maternal conditions. Clinical Considerations Monitor breastfed infants for diarrhea. Data In published lactation studies, maternal mesalamine doses from various oral and rectal formulations and products ranged from 500 mg to 3 g daily. The concentration of mesalamine in milk ranged from non-detectable to 0.11 mg/L. The concentration of the N-acetyl-5-aminosalicylic acid metabolite ranged from 5 to 18.1 mg/L. Based on these concentrations, estimated infant daily dosages for an exclusively breastfed infant are 0 to 0.017 mg/kg/day of mesalamine and 0.75 to 2.72 mg/kg/day of N-acetyl-5- aminosalicylic acid. 8.4 Pediatric Use The safety and effectiveness of mesalamine suppositories in pediatric patients for the treatment of mildly to moderately active ulcerative proctitis have not been established. Information describing a clinical study in which efficacy was not demonstrated in pediatric patients ages 5 to 17 years is approved for Forest Laboratories, LLC’s CANASA (mesalamine) rectal suppositories. However, due to Forest Laboratories, LLC’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 8.5 Geriatric Use Clinical trials of mesalamine suppositories did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Systemic exposures are increased in elderly subjects [ See Clinical Pharmacology (12.3) ] . Reports from uncontrolled clinical studies and postmarketing reporting systems suggested a higher incidence of blood dyscrasias (i.e., agranulocytosis, neutropenia and pancytopenia) in patients receiving mesalamine-containing products such as mesalamine suppositories who were 65 years or older compared to younger patients. Monitor complete blood cell counts and platelet counts in elderly patients during treatment with mesalamine suppositories. In general, the greater frequency of decreased hepatic, renal, or cardiac function, and of concurrent disease or other drug therapy in elderly patients should be considered when prescribing mesalamine suppositories [ see Use in Specific Populations (8.6) ]. 8.6 Renal Impairment Mesalamine is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Evaluate renal function in all patients prior to initiation and periodically while on mesalamine suppositories therapy. Monitor patients with known renal impairment or history of renal disease or taking nephrotoxic drugs for decreased renal function and mesalamine-related adverse reactions [ see Warnings and Precautions (5.1) , Drug Interactions (7.1) and Adverse Reactions (6.2) ].
How supplied
Information about the available dosage forms to which the labeling applies, and for which the manufacturer or distributor is responsible. This field ordinarily includes the strength of the dosage form (in metric units), the units in which the dosage form is available for prescribing, appropriate information to facilitate identification of the dosage forms (such as shape, color, coating, scoring, and National Drug Code), and special handling and storage condition information.16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine suppositories 1000 mg for rectal administration are available as bullet shaped, light tan to grey suppositories containing 1000 mg mesalamine supplied in boxes of 30 plastic wrapped suppositories (NDC: 63629-2397-1). Store below 25ºC (77ºF), may be refrigerated. Keep away from direct heat, light or humidity.
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