VIGAMOX™
(moxifloxacin hydrochloride ophthalmic solution) 0.5% as ba
DESCRIPTION: VIGAMOX™ (moxifloxacin HCl ophthalmic solution) 0.5% is a sterile ophthalmic solution. It is an 8-methoxy fluoroquinolone anti-infective for topical ophthalmic u.
C 21H 24FN 3O 4•HCl Mol Wt 437.9
Chemical Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolol[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid, monohydrochloride.
Moxifloxacin hydrochloride is a slightly yellow to yellow crystalline powder. Each mL of
VIGAMOX™ contains 5.45 mg moxifloxacin hydrochloride equivalent to 5 mg moxifloxacin ba.
Contains:
Active: Moxifloxacin 0.5% (5 mg/mL); Inactives: Boric acid, sodium chloride, and purified water. May also contain hydrochloric acid/sodium hydroxide to adjust pH to approximately 6.8.
VIGAMOX™ is an isotonic solution with an osmolality of approximately 290 mOsm/kg.取代英语
CLINICAL PHARMACOLOGY:
一月英文Pharmacokinetics: Plasma concentrations of moxifloxacin were measured in healthy adult male and female subjects who received bilateral topical ocular dos of VIGAMOX™ 3 times a day. The mean steady-state C max (2.7 ng/mL) and estimated daily exposure AUC (45 ng·hr/mL) values were 1,600 and 1,000 times lower than the mean C max and AUC reported after therapeutic 400 mg oral dos of moxifloxacin. The plasma half-life of moxifloxacin was estimated to be 13 hours.
Microbiology:
Moxifloxacin is an 8-methoxy fluoroquinolone with a diazabicyclononyl ring at the C7 position. The antibacterial action of moxifloxacin results from inhibition of the topoisomera II (DNA gyra) and topoisomera IV. DNA gyra is an esntial enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomera IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.
The mechanism of action for quinolones, including moxifloxacin, is different from that of macrolides,
aminoglycosides, or tetracyclines. Therefore, moxifloxacin may be active against pathogens that are resistant to the antibiotics and the antibiotics may be active against pathogens that are resistant to moxifloxacin. There is no cross-resistance between moxifloxacin and the aforementioned class of O O F
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antibiotics. Cross resistance has been obrved between systemic moxifloxacin and some other quinolones.
In vitro resistance to moxifloxacin develops via multiple-step mutations. Resistance to moxifloxacin occurs in vitro at a general frequency of between 1.8 x 10-9 to < 1 x 10-11 for Gram-positive bacteria.
英文翻译中文转换器
Moxifloxacin has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE ction:
Aerobic Gram-positive microorganisms:
Corynebacterium species*
altec lansing
Micrococcus luteus*
Staphylococcus aureus
Staphylococcus epidermidis
Staphylococcus haemolyticus
Staphylococcus hominis
Staphylococcus warneri*
bloom是什么意思Streptococcus pneumoniae
Streptococcus viridans group
Aerobic Gram-negative microorganisms:
Acinetobacter lwoffii*
Haemophilus influenzae再见英文
Haemophilus parainfluenzae*
Other microorganisms:
Chlamydia trachomatis
*Efficacy for this organism was studied in fewer than 10 infections.
The following in vitro data are also available, but their clinical significance in ophthalmic infections is unknown. The safety and effectiveness of VIGAMOX™ in treating ophthalmological infections due to the microorganisms have not been established in adequate and well-controlled trials.
The following organisms are considered susceptible when evaluated using systemic breakpoints. However, a correlation between the in vitro systemic breakpoint and ophthalmological efficacy has n
ot been established. The list of organisms is provided as guidance only in asssing the potential treatment of conjunctival infections. Moxifloxacin exhibits in vitro minimal inhibitory concentrations (MICs) of 2 µg/ml or less (systemic susceptible breakpoint) against most (≥ 90%) of strains of the following ocular pathogens.
Aerobic Gram-positive microorganisms:
Listeria monocytogenes
Staphylococcus saprophyticus
Streptococcus agalactiae
Streptococcus mitis
Streptococcus pyogenes
Streptococcus Group C, G and F
英语童话剧小红帽Aerobic Gram-negative microorganisms:
Acinetobacter baumannii
Acinetobacter calcoaceticus
Citrobacter freundii
Citrobacter kori
dttEnterobacter aerogenes
Enterobacter cloacae
Escherichia coli
Klebsiella oxytoca
Klebsiella pneumoniae
Moraxella catarrhalis
Morganella morganii
Neisria gonorrhoeae
Proteus mirabilis
Proteus vulgaris
Pudomonas stutzeri
Anaerobic microorganisms:
Clostridium perfringens
Fusobacterium species
Prevotella species
Propionibacterium acnes
Other microorganisms:
Chlamydia pneumoniae
Legionella pneumophila
Mycobacterium avium
Mycobacterium marinum
Mycoplasma pneumoniae
Clinical Studies:
In two randomized, double-masked, multicenter, controlled clinical trials in which patients were dod 3 times a day for 4 days, VIGAMOX™ solution produced clinical cures on day 5-6 in 66% to 69% of patients treated for bacterial conjunctivitis. Microbiological success rates for the eradication of the baline pathogens ranged from 84% to 94%. Plea note that microbiologic eradication does not always correlate with clinical outcome in anti-infective trials.
INDICATIONS AND USAGE: VIGAMOX™ solution is indicated for the treatment of bacterial conjunctivitis caud by susceptible strains of the following organisms:
Aerobic Gram-positive microorganisms:
Corynebacterium species*
Micrococcus luteus*
Staphylococcus aureus
Staphylococcus epidermidis
Staphylococcus haemolyticus
Staphylococcus hominis
Staphylococcus warneri*
高级口译官网Streptococcus pneumoniae
Streptococcus viridans group
Aerobic Gram-negative microorganisms:
Acinetobacter lwoffii*
Haemophilus influenzae
Haemophilus parainfluenzae*
Other microorganisms:wow毕业演说
Chlamydia trachomatis
*Efficacy for this organism was studied in fewer than 10 infections. CONTRAINDICATIONS: VIGAMOX™ solution is contraindicated in patients with a history of hypernsitivity to moxifloxacin, to other quinolones, or to any of the components in this medication. WARNINGS:
NOT FOR INJECTION.
VIGAMOX™ solution should not be injected subconjunctivally, nor should it be introduced directly into the anterior chamber of the eye.
In patients receiving systemically administered quinolones, including moxifloxacin, rious and occasionally fatal hypernsitivity (anaphylactic) reactions have been reported, some following the first do. Some reactions were accompanied by cardiovascular collap, loss of consciousness, an
gioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching. If an allergic reaction to moxifloxacin occurs, discontinue u of the drug. Serious acute hypernsitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.
PRECAUTIONS:
General: As with other anti-infectives, prolonged u may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, discontinue u and institute alternative therapy. Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit-lamp biomicroscopy, and, where appropriate, fluorescein staining.
Patients should be advid not to wear contact lens if they have signs and symptoms of bacterial conjunctivitis.
Information for Patients: Avoid contaminating the applicator tip with material from the eye, fingers or other source.
Systemically administered quinolones including moxifloxacin have been associated with hypernsiti
vity reactions, even following a single do. Discontinue u immediately and contact your physician at the first sign of a rash or allergic reaction.
Drug Interactions: Drug-drug interaction studies have not been conducted with VIGAMOX™ solution. In vitro studies indicate that moxifloxacin does not inhibit CYP3A4, CYP2D6, CYP2C9, CYP2C19, or CYP1A2 indicating that moxifloxacin is unlikely to alter the pharmacokinetics of drugs metabolized by the cytochrome P450 isozymes.
Carcinogenesis, Mutagenesis, Impairment of Fertility: Long term studies in animals to determine the carcinogenic potential of moxifloxacin have not been performed. However, in an accelerated study with initiators and promoters, moxifloxacin was not carcinogenic in rats following up to 38 weeks of oral dosing at 500 mg/kg/day (approximately 21,700 times the highest recommended total daily human ophthalmic do for a 50 kg person, on a mg/kg basis).
Moxifloxacin was not mutagenic in four bacterial strains ud in the Ames Salmonella reversion assay. As with other quinolones, the positive respon obrved with moxifloxacin in strain TA 102 using the same assay may be due to the inhibition of DNA gyra. Moxifloxacin was not mutagenic in the CHO/HGPRT mammalian cell gene mutation assay. An equivocal result was obtained in the s
ame assay when v79 cells were ud. Moxifloxacin was clastogenic in the v79 chromosome aberration assay, but it did not induce unscheduled DNA synthesis in cultured rat hepatocytes. There was no evidence of genotoxicity in vivo in a micronucleus test or a dominant lethal test in mice.
Moxifloxacin had no effect on fertility in male and female rats at oral dos as high as 500 mg/kg/day, approximately 21,700 times the highest recommended total daily human ophthalmic do. At 500
mg/kg orally there were slight effects on sperm morphology (head-tail paration) in male rats and on the estrous cycle in female rats.
Pregnancy: Teratogenic Effects.
Pregnancy Category C: Moxifloxacin was not teratogenic when administered to pregnant rats during organogenesis at oral dos as high as 500 mg/kg/day (approximately 21,700 times the highest recommended total daily human ophthalmic do); however, decread fetal body weights and slightly delayed fetal skeletal development were obrved. There was no evidence of teratogenicity when pregnant Cynomolgus monkeys were given oral dos as high as 100 mg/kg/day (approximate
ly 4,300 times the highest recommended total daily human ophthalmic do). An incread incidence of smaller fetus was obrved at 100 mg/kg/day.
Since there are no adequate and well-controlled studies in pregnant women, VIGAMOX™ solution should be ud during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers: Moxifloxacin has not been measured in human milk, although it can be presumed to be excreted in human milk. Caution should be exercid when VIGAMOX™ solution is administered to a nursing mother.
Pediatric U: The safety and effectiveness of VIGAMOX solution in infants below 1 year of age have not been established.
There is no evidence that the ophthalmic administration of VIGAMOX™ has any effect on weight bearing joints, even though oral administration of some quinolones has been shown to cau arthropathy in immature animals.
Geriatric U: No overall differences in safety and effectiveness have been obrved between elderly and younger patients.
