Moxifloxacin

1-cyclopropyl -6-fluoro -8 -methoxy -7- [( 4aS, 7aS ) - octahydro -6H -pyrrolo [ 3,4-b ] pyridin- 6-yl ] -4-oxo -1 ,4- dihydroquinoline - 3-carboxylic acid

J01MA14, S01AE07

Antibiotic

Gyrase inhibitors

• 203-208 ° C ( decomposition) ( moxifloxacin )
• 324-325 ° C ( decomposition) ( moxifloxacin hydrochloride · )

Hydrochloride

1320 mg · kg -1 ( LD50, Rat, oral, hydrochloride)

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Moxifloxacin is an antibiotic belonging to the fourth generation of fluoroquinolone ( gyrase inhibitors ) group and is subject to medical prescription.

Operation

The mechanism of action of moxifloxacin is identical to that of other fluoroquinolones, but it binds to two topoisomerases and so has two points of attack. Quinolones generally bind to the gyrase, thereby this is inhibited. The binding of fluoroquinolones to the gyrase results in stable complexes that trigger a variety of enzymatic reactions that lead ultimately to death of the bacterial cell.

Application

Moxifloxacin is used therapeutically in a worsening of an already long-standing (chronic) bronchitis, pneumonia and in the case of acute inflammation of the sinuses. In addition, it is approved for complicated skin and soft tissue (about the diabetic foot ).

In one study it was shown that treatment with moxifloxacin the time interval between two attacks ( exacerbations ) extended of chronic bronchitis or acute worsening of COPD compared to standard therapy. After a recommendation from the European Medicines Agency EMEA in July 2008, however, moxifloxacin should be due to unfavorable risk - benefit analysis (see side effects ) for acute sinusitis, chronic bronchitis and community-acquired pneumonia are only used when other antibiotics are not effective or can not be applied.

An application for chlamydia is increasingly recommended and shown to be quite effective. Even in infections with other atypical pathogens such as Mycoplasma and Legionella, it is very effective. The activity against Haemophilus influenzae and Moraxella catarrhalis is very good as with all quinolones against pneumococci excellent.

Side effects

Very common side effects of moxifloxacin are not known. The most common (≥ 1%, < 10%) disorders of the gastrointestinal tract, particularly nausea, diarrhea, vomiting and indigestion, further QT syndrome with known hypokalemia and liver function test abnormalities are observed. Very rare ( < 1/10.000 ), but particularly severe, are fulminant hepatitis to life-threatening liver failure and bullous skin reactions such as Stevens -Johnson syndrome or toxic epidermal necrolysis possibly life-threatening. Also cases of tendinitis after administration of moxifloxacin and other fluoroquinolones have been described.

Trade names

Actira (A), Avelox (D, CH), Avelox (A), Octegra (A), Vigamox (D, CH), Avelon ( South Africa) and generic (D, A)