Moxifloxacin Hydrochloride

(BANM, USAN, rINNM)
Moxifloxacin Hydrochloride Chemical formula
Synonyms: Bay-12-8039; Hidrocloruro de moxifloxacino; Moxifloxacine, chlorhydrate de; Moxifloxacini hydrochloridum. 1-Cyclopropyl6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6Hpyrrolo[3,4b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid hydrochloride.
Cyrillic synonym: Моксифлоксацина Гидрохлорид.

💊 Chemical information

Chemical formula: C21H24FN3O4,HCl = 437.9.
CAS — 151096-09-2 (moxifloxacin); 186826-86-8 ATC — J01MA14; S01AX22.
ATC Vet — QJ01MA14; QS01AX22.

Pharmacopoeias.

In Eur..

Ph. Eur. 6.2

(Moxifloxacin Hydrochloride). Produced using a method validated to demonstrate the satisfactory enantiomeric purity of the final product. A light yellow or yellow powder or crystals, slightly hygroscopic. Sparingly soluble in water; slightly soluble in alcohol; practically insoluble in acetone. A 0.2% solution in water has a pH of 3.9 to 4.6. Store in airtight containers. Protect from light.

💊 Adverse Effects and Precautions

As for Ciprofloxacin.
1. Faich GA, et al. Clinical experience with moxifloxacin in patients with respiratory tract infections. Ann Pharmacother 2004; 38: 749–54
2. Ball P, et al. Safety profile of oral and intravenous moxifloxacin: cumulative data from clinical trials and postmarketing studies. Clin Ther 2004; 26: 940–50
3. Andriole VT, et al. Retrospective analysis of the safety profile of oral moxifloxacin in elderly patients enrolled in clinical trials. Drug Safety 2005; 28: 443–52.

💊 Interactions

As for Ciprofloxacin. Moxifloxacin does not appear to interact significantly with theophylline or probenecid.

💊 Antimicrobial Action

As for Ciprofloxacin. Moxifloxacin is reported to have greater activity against Grampositive bacteria, including pneumococci, than ciprofloxacin.
1. Stein GE, et al. Bactericidal activities of methoxyfluoroquinolones gatifloxacin and moxifloxacin against aerobic and anaerobic respiratory pathogens in serum. Antimicrob Agents Chemother 2003; 47: 1308–12
2. Pletz MWR, et al. Early bactericidal activity of moxifloxacin in treatment of pulmonary tuberculosis: a prospective, randomized study. Antimicrob Agents Chemother 2004; 48: 780–2.

💊 Pharmacokinetics

Moxifloxacin is readily absorbed from the gastrointestinal tract after oral doses with an absolute bioavailability of about 90%. It is widely distributed throughout the body tissues and is about 30 to 50% bound to plasma proteins. Moxifloxacin has an elimination half-life of about 12 hours, allowing once-daily dosing. It is metabolised mainly via sulfate and glucuronide conjugation, and is excreted in the urine and the faeces as unchanged drug and as metabolites, the sulfate conjugate primarily in the faeces and the glucuronide exclusively in the urine. Distribution into milk has been found in animals.

💊 Uses and Administration

Moxifloxacin is a fluoroquinolone antibacterial with actions and uses similar to those of ciprofloxacin. It is given orally, or by intravenous infusion over 60 minutes, for the treatment of susceptible infections including respiratory, skin and skin structure, and intra-abdominal infections. Moxifloxacin is given as the hydrochloride but doses are expressed in terms of the base; moxifloxacin hydrochloride 436.3 mg is equivalent to about 400 mg of moxifloxacin. The usual dose is 400 mg once daily. Moxifloxacin is also used topically as the hydrochloride in eye drops containing the equivalent of 0.5% of moxifloxacin for the treatment of bacterial conjunctivitis.
1. Keating GM, Scott LJ. Moxifloxacin: a review of its use in the management of bacterial infections. Drugs 2004; 64: 2347–77
2. Miravitlles M, et al. Eficacia clínica del moxifloxacino en el tratamiento de las agudizaciones de la bronquitis crónica: revisión sistemática y metaanálisis. Arch Bronconeumol 2007; 43: 22–8
3. Miravitlles M. Moxifloxacin in the management of exacerbations of chronic bronchitis and COPD. Int J Chron Obstruct Pulmon Dis 2007; 2: 191–204
4. O’Brien TP. Evidence-based review of moxifloxacin. Int Ophthalmol Clin 2006; 46: 61–72.

Eye infections.

In order to attain therapeutic concentrations most antibacterials used in the treatment of bacterial endophthalmitis need to be given by the intravitreal route but moxifloxacin given systemically may produce adequate concentrations. An oral dose of moxifloxacin 400 mg daily may be given for 10 days.1
1. Moorfields Eye Hospital NHS Foundation Trust. Pharmacists Handbook 2006. London: Moorfields Pharmaceuticals, 2006.

💊 Preparations

Proprietary Preparations

Arg.: Avelox; Octegra†; Vigamox; Austral.: Avelox; Austria: Actira; Avelox; Octegra; Belg.: Avelox; Proflox; Braz.: Avalox; Vigamox; Canad.: Avelox; Vigamox; Chile: Avelox; Flovacil; Octegra†; Vigamox; Cz.: Avelox; Denm.: Avelox; Fin.: Avelox; Fr.: Izilox; Ger.: Avalox; Gr.: Avelox; Octegra; Proflox; Hong Kong: Avelox; Vigamox; Hung.: Avelox; Octegra; India: Moxicip; Moxif; Indon.: Avelox; Irl.: Avelox; Israel: Megaxin; Vigamox; Ital.: Actira; Avalox; Octegra; Jpn: Avelox; Malaysia: Avelox; Vigamox; Mex.: Avelox; Vigamoxi; Neth.: Actira†; Avelox; Octegra; NZ: Avelox; Philipp.: Avelox; Vigamox; Pol.: Avelox; Port.: Avelox; Proflox; Rus.: Avelox (Авелокс); S.Afr.: Avelon; Singapore: Avelox; Vigamox; Spain: Actira; Octegra; Proflox; Swed.: Avelox; Switz.: Avalox; Thai.: Avelox; Vigamox; Turk.: Avelox; UK: Avelox; USA: Avelox; Vigamox; Venez.: Avelox; Vigamox.
Published May 08, 2019.