Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2177
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BACTROBAN (Ointment)
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(See INDICATIONS AND USAGE.)<br/>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 NASALshould
not be applied concurrently with any other intranasal products.
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| dailymed-instance:descripti... |
BACTROBAN NASAL (mupirocin calcium ointment,
2%) contains the dihydrate crystalline calcium hemi-salt of the antibiotic
mupirocin. Chemically, it is (��E,2S ,3R,4R ,5S)-5-[(2S ,3S,4S ,5S)-2,3-Epoxy-5-hydroxy-4-methylhexyl]tetrahydro-3,4-dihydroxy-��-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).
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Pharmacokinetics: 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.<br/>Microbiology: 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
NASALonly 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.
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BACTROBAN
NASALis contraindicated in
patients with known hypersensitivity to any of the constituents ofthe product.
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BACTROBAN NASAL is supplied in 1.0-gram tubes
packaged in cartons of 10. NDC 0029-1526-11
(1.0 gram tubes in packages of 10). Store
between 20��and 25��C (68��and 77��F); excursions
permitted to 15��-30��C (59��-86��F). Do not refrigerate.
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General: As with other antibacterial products, prolonged
use may result in overgrowth of nonsusceptible microorganisms, including
fungi. (See DOSAGE AND ADMINISTRATION.)<br/>Information for Patients: Patients should be given the following instructions: ���Apply approximately one-half of the ointment
from the single-use tube directly into 1 nostril and the other half
into the other nostril; ���Avoid contact
of the medication with the eyes; ���Discard
the tube after using, do not re-use; ���Press the sides of the nose together and gently massage after application
to spread the ointment throughout the inside of the nostrils; and ���Discontinue usage of the medication and call
your health care practitioner if sensitization or severe local irritation
occurs.<br/>Drug Interactions: 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.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility: 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/mbasis and revealed no evidence of impaired fertility
from mupirocin sodium.<br/>Pregnancy:<br/>Teratogenic Effects. Pregnancy Category
B: 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.<br/>Nursing Mothers: 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 NASALis administered to a nursing woman.<br/>Pediatric Use: Safety in children under the age of 12 years
has not been established. (See CLINICAL PHARMACOLOGY.)
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Following single or repeated intranasal applications
of BACTROBAN NASALto 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 NASALor regarding oral ingestion of the nasal
ointment formulation.
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mupirocin calcium
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BACTROBAN (Ointment)
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| dailymed-instance:adverseRe... |
Clinical Trials:: In clinical trials, 210 domestic and 2,130 foreign
adult subjects/patients received BACTROBAN NASALointment. 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 NASALointment 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 NASALointment, 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.
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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.
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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.
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BACTROBAN
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