MOXIFLOXACIN — moxifloxacin hydrochloride solution
Lupin Pharmaceuticals, Inc.
*Efficacy for this organism was studied in fewer than 10 infections.
Toxic Anterior Segment Syndrome (TASS) has been reported following intraocular administration of moxifloxacin. TASS is typically characterized by anterior chamber inflammatory reactions, such as fibrin, cell or flare and corneal edema, but other events, such as hypopyon, keratic precipitates or vitreous opacities may also occur.
In patients receiving systemically administered quinolones, including moxifloxacin, serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported, some following the first dose. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching. If an allergic reaction to moxifloxacin occurs, discontinue use of the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.
As with other anti-infectives, prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, discontinue use 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.
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 the rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The data described below reflect exposure to moxifloxacin ophthalmic solution in 1263 patients, between 4 months and 92 years of age, with signs and symptoms of bacterial conjunctivitis. The most frequently reported adverse reactions were eye irritation, pyrexia and conjunctivitis, reported in 1% to 2% of patients.
There are no adequate and well-controlled studies with moxifloxacin ophthalmic solution in pregnant women to inform any drug-associated risks.
Oral administration of moxifloxacin to pregnant rats and monkeys and intravenously to pregnant rabbits during the period of organogenesis did not produce adverse maternal or fetal effects at clinically relevant doses. Oral administration of moxifloxacin to pregnant rats during late gestation through lactation did not produce adverse maternal, fetal or neonatal effects at clinically relevant doses (see Data).
Embryo-fetal studies were conducted in pregnant rats administered with 20, 100, or 500 mg/kg/day moxifloxacin by oral gavage on Gestation Days 6 to 17, to target the period of organogenesis. Decreased fetal body weight and delayed skeletal development were observed at 500 mg/kg/day (1420 times the human area under the curve (AUC) at the recommended human ophthalmic dose). The No-Observed-Adverse-Effect-Level (NOAEL) for developmental toxicity was 100 mg/kg/day (152 times the human AUC at the recommended human ophthalmic dose).
Embryo-fetal studies were conducted in pregnant rabbits administered with 2, 6.5, or 20 mg/kg/day moxifloxacin by intravenous administration on Gestation Days 6 to 20, to target the period of organogenesis. Abortions, increased incidence of fetal malformations, delayed fetal skeletal ossification, and reduced placental and fetal body weights were observed at 20 mg/kg/day (5569 times the human AUC at the recommended human ophthalmic dose), a dose that produced maternal body weight loss and death. The NOAEL for developmental toxicity was 6.5 mg/kg/day (1261 times the human AUC at the recommended human ophthalmic dose).
Pregnant cynomolgus monkeys were administered moxifloxacin at doses of 10, 30, or 100 mg/kg/day by intragastric intubation between Gestation Days 20 and 50, targeting the period of organogenesis. At the maternal toxic doses of ≥ 30 mg/kg/day, increased abortion, vomiting and diarrhea were observed. Smaller fetuses/reduced fetal body weights were observed at 100 mg/kg/day (14688 times the human AUC at the recommended human ophthalmic dose). The NOAEL for fetal toxicity was 10 mg/kg/day (894 times the human AUC at the recommended human ophthalmic dose).
In a pre- and postnatal study, rats were administered moxifloxacin by oral gavage at doses of 20, 100, and 500 mg/kg/day from Gestation Day 6 until the end of lactation. Maternal death occurred during gestation at 500 mg/kg/day. Slight increases in the duration of pregnancy, reduced pup birth weight, and decreased prenatal and neonatal survival were observed at 500 mg/kg/day (estimated 1420 times the human AUC at the recommended human ophthalmic dose). The NOAEL for pre- and postnatal development was 100 mg/kg/day (estimated 152 times the human AUC at the recommended human ophthalmic dose).
There are no data regarding the presence of moxifloxacin ophthalmic solution in human milk, the effects on the breastfed infants, or the effects on milk production/excretion to inform risk of moxifloxacin ophthalmic solution to an infant during lactation. A study in lactating rats has shown transfer of moxifloxacin into milk following oral administration. Systemic levels of moxifloxacin following topical ocular administration are low [see Clinical Pharmacology (12.3)] , and it is not known whether measurable levels of moxifloxacin would be present in maternal milk following topical ocular administration. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for moxifloxacin ophthalmic solution and any potential adverse effects on the breastfed child from moxifloxacin ophthalmic solution.
There is no evidence that the ophthalmic administration of moxifloxacin has any effect on weight bearing joints, even though oral administration of some quinolones has been shown to cause arthropathy in immature animals.
Moxifloxacin hydrochloride is an 8-methoxy fluoroquinolone anti-infective, with a diazabicyclononyl ring at the C7 position.
Each mL of moxifloxacin ophthalmic solution USP, 0.5 % contains 5.45 mg moxifloxacin hydrochloride USP, equivalent to 5 mg moxifloxacin base.
Inactives: boric acid, sodium chloride, sorbitol, tyloxapol, xanthan gum, hydrochloric acid and/or sodium hydroxide to adjust pH, and water for injection.
Moxifloxacin ophthalmic solution USP, 0.5% is a greenish-yellow, isotonic solution with an osmolality of 300 to 370 mOsm/kg and a pH of approximately 7.4. Moxifloxacin hydrochloride is a slightly yellow to yellow crystalline powder.
USP pH and Osmolality tests are pending.
All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.