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Anti-Infective Agents
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The pregnancy experience in humans suggests low risk; however, the authors of one study recommended avoid giving Moxifloxacin during pregnancy because safer alternatives are generally available. However, fluoroquinolones are commonly avoided in the perinatal period because of fears from fetal cartilage damage.
Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
Moxifloxacin is a fluoroquinolone antibacterial agent used in a broad number of respiratory infections, which includes bronchitis, chronic sinusitis and pneumonia among others (Scheme 9.10). A key Moxifloxacin precursor has been prepared by hydrolytic resolution of racemic cis-dimethyl-1-acetylpiperidine-2,3-dicarboxylate at 80 g scale using soluble Candida antarctica lipase type B (CAL-B, Ramesh et al., 2015). Thus, after an extraction protocol the starting (–)-diester was isolated in 46% yield and enantiopure form. Due to a migration reaction of the methoxy group between the C-2 and C-3 positions, the hydrolysed resulting monoester was recovered as a mixture of monomethyl esters in 52% yield, which were esterified using thionyl chloride and methanol to measure the optical activity (85% ee) as the corresponding diester. This protocol represents a clear advantage compared with the use of the immobilised CAL-B as only 16 h were required for the completion of the reaction, instead of 140 h. CAL-B catalysed hydrolytic resolution of cis-dimethyl-1-acetylpiperidine-2,3-dicarboxylate, a key precursor in the synthesis of Moxifloxacin.
Moxifloxacin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Moxifloxacin (as moxifloxacin hydrochloride) is available under the brand name Avelox as 400-mg tablets and in parenteral form for intravenous infusion. Moxifloxacin is also sold in an ophthalmic solution 0.5% (eye drops) under the name Vigamox. Moxifloxacin inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, and is bactericidal. Moxifloxacin has a broad spectrum of activity and is approved for use in acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, community-acquired pneumonia, and uncomplicated skin and skin structure infections (Andriole and Andriole, 2001). Moxifloxacin is also used for the treatment of complicated intra-abdominal infections, as a second-line agent in the treatment of tuberculosis, and for bacterial conjunctivitis (ophthalmic solution). While moxifloxacin has a similar spectrum of antibacterial activity to that of gatifloxacin (see Chapter 115, Gatifloaxcin), it does not require dose adjustment in patients with renal impair-ment and it has a much better safety profile; in particular, it is not associated with the same clinical problems of dysglycemia (e.g. hypoglycemia).
Antimicrobial susceptibility and minimum inhibitory concentration distribution of common clinically relevant non-tuberculous mycobacterial isolates from the respiratory tract
Published in Annals of Medicine, 2022
Guiqing He, Lianpeng Wu, Qingyong Zheng, Xiangao Jiang
Although there was no CLSI-recommended resistance breakpoint for tigecycline, a highly sensitive breakpoint was set according to the literature. The key was strong antibacterial activity (MIC50/MIC90 = 0.5/2 μg/mL), which was consistent with recent reports [14,15,21], suggesting that it can be included in regimens as an effective drug. However, in vitro MIC and in vivo efficacy need to be confirmed by further clinical studies. Moxifloxacin was not recommended in the guidelines, but it is widely used in clinical practice. Our study found that moxifloxacin had a high drug resistance rate (95.8%), with MIC50/MIC90 = 8/>8 μg/mL, suggesting weak antibacterial activity, which was consistent with several studies [14,15,21]. Other scholars [22] determined the susceptibility breakpoint of moxifloxacin to be 0.25 μg/mL via PK/PD studies; the effective concentration could not be reached even when the dose was increased to 800 mg qd, suggesting that the efficacy of the conventional dose was limited.
Unilateral Acute Iris Transillumination Syndrome following Uneventful Phacoemulsification Surgery with Intracameral Moxifloxacin
Published in Ocular Immunology and Inflammation, 2022
The exact mechanism of the toxic effect of moxifloxacin on iris tissue remains unclear. Mohanty and associates evaluated the toxicity of topical moxifloxacin by measuring the activity of the melanogenic enzyme tyrosinase in aqueous humor specimens obtained before phacoemulsification surgery and concluded that topical moxifloxacin causes different levels of iris melanocyte toxicity.13 However, none of the patients in their series developed BADI or BAIT. Therefore, they have hypothesized that topical moxifloxacin can cause subclinical toxicity to the iris melanocytes. Perin and associates have shown that moxifloxacin has a significant toxic effect on cultivated iris pigment epithelium in humans.14 The authors have also reported that this toxic effect increased with greater concentrations of moxifloxacin. In accordance with these studies, our patient received a dose of ICM that is higher than the dose that is commonly used, and this may be responsible for the AIT that developed. Therefore, it may indicate that ICM concentration might be a risk factor for the development of AIT after using ICM
Re-assessing Evidence for Adverse Ocular Reactions Associated with Fluoroquinolones: Implications for Intracameral Use
Published in Ocular Immunology and Inflammation, 2022
Moxifloxacin is an 8-methoxyfluoroquinolone bactericidal antibiotic which inhibits DNA gryase and topisomerase IV. Moxifloxacin has broad spectrum activity against Gram-positive and Gram-negative bacteria, anaerobic bacteria and atypical organisms. Fluoroquinolone antibiotics are indicated for the treatment of complicated intra-abdominal infections, community acquired pneumonia, bacterial skin infections, acute bacterial exacerbations of chronic bronchitis, active tuberculosis, plague and conjunctivitis. Adverse events associated with systemic use of fluoroquinolones include tendonitis, tendon rupture, peripheral neuropathy and diplopia. Uveitis was not reported in pre-marketing trials of moxifloxacin, which was approved by the Food and Drug Administration in 1999.1 The first report of uveitis associated with orally administered moxifloxacin occurred in 2004. Subsequent reports expanded our understanding of clinical features of the condition and implicated additional drugs within the fluoroquinolone class.2,3