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BACTROBAN NASAL (mupirocin calcium ointment, 2%)for intranasal use only | BACTROBAN [Physicians Total Care, Inc.] | BioPortfolio

13:22 EST 27th January 2019 | BioPortfolio

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BACTROBAN NASAL (mupirocin calcium ointment, 2%) contains the dihydrate crystalline calcium hemi-salt of the antibiotic mupirocin. Chemically, it is (αE,2S,3R,4R,5S)-5-[(2S,3S,4S,5S)-2,3-Epoxy-5-hydroxy-4-methylhexyl]tetrahydro-3,4-dihydroxy-β-methyl-2H-pyran-2-crotonic acid, ester with 9-hydroxynonanoic acid, calcium salt (2:1), dihydrate.

The molecular formula of mupirocin calcium is (CHO)Ca•2HO, and the molecular weight is 1075.3. The molecular weight of mupirocin free acid is 500.6. The structural formula of mupirocin calcium is:

BACTROBAN NASAL is a white to off-white ointment that contains 2.15% w/w mupirocin calcium (equivalent to 2.0% pure mupirocin free acid) in a soft white ointment base. The inactive ingredients are paraffin and a mixture of glycerin esters (SOFTISAN 649).

Following single or repeated intranasal applications of 0.2 gram of BACTROBAN NASAL 3 times daily for 3 days to 5 healthy adult male subjects, no evidence of systemic absorption of mupirocin was demonstrated. The dosage regimen used in this study was for pharmacokinetic characterization only. (See DOSAGE AND ADMINISTRATION for proper clinical dosing information.)

In this study, the concentrations of mupirocin in urine and of monic acid in urine and serum were below the limit of determination of the assay for up to 72 hours after the applications. The lowest levels of determination of the assay used were 50 ng/mL of mupirocin in urine, 75 ng/mL of monic acid in urine, and 10 ng/mL of monic acid in serum. Based on the detectable limit of the urine assay for monic acid, one can extrapolate that a mean of 3.3% (range: 1.2 to 5.1%) of the applied dose could be systemically absorbed from the nasal mucosa of adults.

Data from a report of a pharmacokinetic study in neonates and premature infants indicate that, unlike in adults, significant systemic absorption occurred following intranasal administration of BACTROBAN NASAL in this population. At this time, the pharmacokinetic properties of mupirocin following intranasal application of BACTROBAN NASAL have not been adequately characterized in neonates or other children less than 12 years of age, and in addition, the safety of the product in children less than 12 years of age has not been established.

The effect of the concurrent application of intranasal mupirocin calcium ointment, 2% with other intranasal products has not been studied. (See PRECAUTIONS, Drug Interactions.)

Following intravenous or oral administration, mupirocin is rapidly metabolized. The principal metabolite, monic acid, demonstrates no antibacterial activity. In a study conducted in 7 healthy adult male subjects, the elimination half-life after intravenous administration of mupirocin was 20 to 40 minutes for mupirocin and 30 to 80 minutes for monic acid. Monic acid is predominantly eliminated by renal excretion. The pharmacokinetics of mupirocin has not been studied in individuals with renal insufficiency.

Mupirocin is an antibacterial agent produced by fermentation using the organism Pseudomonas fluorescens. Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl transfer-RNA synthetase. Due to this mode of action, mupirocin demonstrates no in vitro cross-resistance with other classes of antimicrobial agents.

When mupirocin resistance does occur, it appears to result from the production of a modified isoleucyl-tRNA synthetase. High-level plasmid-mediated resistance (MIC >1,024 mcg/mL) has been reported in some strains of Staphylococcus aureus and coagulase-negative staphylococci.

Mupirocin is bactericidal at concentrations achieved topically by intranasal administration. However, the minimum bactericidal concentration (MBC) against relevant intranasal pathogens is generally 8-fold to 30-fold higher than the minimum inhibitory concentration (MIC). In addition, mupirocin is highly protein bound (>97%), and the effect of nasal secretions on the MICs of intranasally applied mupirocin has not been determined.

Mupirocin has been shown to be active against most strains of methicillin-resistant S. aureus, both in vitro and in clinical studies of the eradication of nasal colonization. BACTROBAN NASAL only has established clinical utility in nasal eradication as part of a comprehensive program to curtail institutional outbreaks of infections with methicillin-resistant S. aureus. (See INDICATIONS AND USAGE.)

The following in vitro data are available, but their clinical significance is unknown . Mupirocin exhibits in vitro MICs of 1 mcg/mL or less against most (>90%) strains of methicillin-susceptible S. aureus; however, the safety and effectiveness of mupirocin calcium in eradicating nasal colonization of and preventing subsequent infections due to methicillin-susceptible S. aureus have not been established.

BACTROBAN NASAL is indicated for the eradication of nasal colonization with methicillin-resistant S. aureus in adult patients and health care workers as part of a comprehensive infection control program to reduce the risk of infection among patients at high risk of methicillin-resistant S. aureus infection during institutional outbreaks of infections with this pathogen.

NOTE:

All adequate and well-controlled trials of this product were vehicle-controlled; therefore, no data from direct, head-to-head comparisons with other products are available at this time.

BACTROBAN NASAL is contraindicated in patients with known hypersensitivity to any of the constituents of the product.

AVOID CONTACT WITH THE EYES. Application of BACTROBAN NASAL to the eye under testing conditions has caused severe symptoms such as burning and tearing. These symptoms resolved within days to weeks after discontinuation of the ointment.

In the event of a sensitization or severe local irritation from BACTROBAN NASAL, usage should be discontinued.

As with other antibacterial products, prolonged use may result in overgrowth of nonsusceptible microorganisms, including fungi. (See DOSAGE AND ADMINISTRATION.)

Patients should be given the following instructions:

The effect of the concurrent application of intranasal mupirocin calcium and other intranasal products has not been studied. Until further information is known, mupirocin calcium ointment, 2% should not be applied concurrently with any other intranasal products.

Long-term studies in animals to evaluate carcinogenic potential of mupirocin calcium have not been conducted.

Results of the following studies performed with mupirocin calcium or mupirocin sodium in vitro and in vivo did not indicate a potential for mutagenicity: Rat primary hepatocyte unscheduled DNA synthesis, sediment analysis for DNA strand breaks, Salmonella reversion test (Ames), Escherichia coli mutation assay, metaphase analysis of human lymphocytes, mouse lymphoma assay, and bone marrow micronuclei assay in mice.

Reproduction studies were performed in rats with mupirocin administered subcutaneously at doses up to 40 times the human intranasal dose (approximately 20 mg mupirocin per day) on a mg/m basis and revealed no evidence of impaired fertility from mupirocin sodium.

Reproduction studies have been performed in rats and rabbits with mupirocin administered subcutaneously at doses up to 65 and 130 times, respectively, the human intranasal dose (approximately 20 mg mupirocin per day) on a mg/m2 basis and revealed no evidence of harm to the fetus due to mupirocin. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when BACTROBAN NASAL is administered to a nursing woman.

Safety in children under the age of 12 years has not been established. (See CLINICAL PHARMACOLOGY.)

In clinical trials, 210 domestic and 2,130 foreign adult subjects/patients received BACTROBAN NASAL ointment. Less than 1% of domestic or foreign subjects and patients in clinical trials were withdrawn due to adverse events.

The most frequently reported adverse events in foreign clinical trials were as follows: Rhinitis (1.0%), taste perversion (0.8%), pharyngitis (0.5%).

In domestic clinical trials, 17% (36/210) of adults treated with BACTROBAN NASAL ointment reported adverse events thought to be at least possibly drug-related. The incidence of adverse events that were reported in at least 1% of adults enrolled in domestic clinical trials were as follows:

The following events thought possibly drug-related were reported in less than 1% of adults enrolled in domestic clinical trials: Blepharitis, diarrhea, dry mouth, ear pain, epistaxis, nausea, and rash.

All adequate and well-controlled clinical trials have been performed using BACTROBAN NASAL ointment, 2% in 1 arm and the vehicle ointment in the other arm of the study. No adequate and well-controlled safety data are available from direct, head-to-head comparative studies of this product and other products for this indication.

ADVERSE EVENTS (≥1% INCIDENCE)-ADULTS IN US TRIALS
% of Subjects/Patients Experiencing Event BACTROBAN NASAL(n=210)
Headache 9%
Rhinitis 6%
Respiratory disorder, includingupper respiratory tract congestion 5%
Pharyngitis 4%
Taste perversion 3%
Burning/stinging 2%
Cough 2%
Pruritus 1%

Following single or repeated intranasal applications of BACTROBAN NASAL to adults, no evidence for systemic absorption of mupirocin was obtained. Intravenous infusions of 252 mg, as well as single oral doses of 500 mg of mupirocin, have been well tolerated in healthy adult subjects. There is no information regarding local overdose of BACTROBAN NASAL or regarding oral ingestion of the nasal ointment formulation.

(See INDICATIONS AND USAGE.)

Adults (12 years of age and older): Approximately one-half of the ointment from the single-use tube should be applied into 1 nostril and the other half into the other nostril twice daily (morning and evening) for 5 days.

After application, the nostrils should be closed by pressing together and releasing the sides of the nose repetitively for approximately 1 minute. This will spread the ointment throughout the nares.

The single-use 1.0 gram tube will deliver a total of approximately 0.5 grams of the ointment (approximately 0.25 grams/nostril).

The tube should be discarded after usage; it should not be re-used.

The safety and effectiveness of applications of this medication for greater than 5 days have not been established. There are no human clinical or pre-clinical animal data to support the use of this product in a chronic manner or in manners other than those described in this package insert.

Until further information is known, BACTROBAN NASAL should not be applied concurrently with any other intranasal products.

BACTROBAN NASAL is supplied in 1.0-gram tubes.

NDC 54868-4325-0 (package of 10 single-tube cartons).

Store between 20° and 25°C (68° and 77°F); excursions permitted to 15°-30°C (59°-86°F). Do not refrigerate.

BACTROBAN NASAL is a registered trademark of GlaxoSmithKline.

SOFTISAN is a registered trademark of Sasol Olefins & Surfactants GmbH.

GlaxoSmithKline

Research Triangle Park, NC 27709

©2009, GlaxoSmithKline. All rights reserved.

April 2009                    BBN:2PI

Additional barcode labeling by:Physicians Total Care, Inc.Tulsa, Oklahoma        74146

Principal Display Panel

NDC 54868-4325-0

BACTROBAN NASAL

MUPIROCIN CALCIUM OINTMENT 2%

1 x 1.0 gram Single-Use Tube

R only

Store at 20- 25C (68 – 77F); excursions permitted 15 - 30C (59 – 86F).. Do not refrigerate. Each gram contains 21.5 mg mupirocin calcium in a soft white ointment base.

Usual Dosage: For intranasal use only. Apply one-half the contents of a tube in one nostril. Apply other half of tube contents in other nostril. See accompanying prescribing information.

TO OPEN

1. Turn cap counter-clockwise to puncture the seal.

2. Lift off plastic tip cover.

HOW TO APPLY

Apply one-half the contents of the tube in one nostril.

Apply the other half of tube contents in the other nostril.

Press nostrils together. Massage for approximately one minute. Discard tube. Do not reuse.

Avoid contact with eyes. Contact your healthcare professional if you have any questions.

10000000067584

Manufacturer

Physicians Total Care, Inc.

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