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Avelox

Avelox - General Information

Avelox is a synthetic fluoroquinolone antibiotic agent. Bayer AG developed the drug (initially called BAY 12-8039) and it is marketed worldwide (as the hydrochloride) under the brand name Avelox (in some countries also Avalox) for oral treatment.

 

Pharmacology of Avelox

Avelox is a quinolone/fluoroquinolone antibiotic. Avelox can be used to treat infections caused by the following bacteria: Aerobic Gram-positive microorganisms: Corynebacterium species, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus warneri, Streptococcus pneumoniae, and Streptococcus viridans group. Aerobic Gram-negative microorganisms: Acinetobacter lwoffii, Haemophilus influenzae, and Haemophilus parainfluenzae. Other microorganisms: Chlamydia trachomatis.
Avelox is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Avelox is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

 

Avelox 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 hypersensitivity reactions, even following a single dose. Discontinue use immediately and contact your physician at the first sign of a rash or allergic reaction.

 

Avelox 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 these cytochrome P450 isozymes.

 

Avelox Contraindications

VIGAMOX™ solution is contraindicated in patients with a history of hypersensitivity to moxifloxacin, to other quinolones, or to any of the components in this medication.

 

Additional information about Avelox

Avelox Indication: For the treatment of sinus and lung infections such as sinusitis, pneumonia, and secondary infections in chronic bronchitis. Also for the treatment of bacterial conjunctivitis (pinkeye).
Mechanism Of Action: The bactericidal action of moxifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.
Drug Interactions: Aluminium Formation of non-absorbable complexes
Bismuth Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Iron Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium Formation of non-absorbable complexes
Sucralfate Formation of non-absorbable complexes
Zinc Formation of non-absorbable complexes
Ziprasidone Increased risk of cardiotoxicity and arrhythmias
Sotalol Increased risk of cardiotoxicity and arrhythmias
Quinidine Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Josamycin Increased risk of cardiotoxicity and arrhythmias
Erythromycin Increased risk of cardiotoxicity and arrhythmias
Dihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Disopyramide Increased risk of cardiotoxicity and arrhythmias
Amiodarone Increased risk of cardiotoxicity and arrhythmias
Bretylium Increased risk of cardiotoxicity and arrhythmias
Bepridil Increased risk of cardiotoxicity and arrhythmias
Anisindione Avelox increases the anticoagulant effect
Acenocoumarol Avelox increases the anticoagulant effect
Dicumarol Avelox increases the anticoagulant effect
Warfarin Avelox increases the anticoagulant effect
Quinupristin This combination presents an increased risk of toxicity
Food Interactions: Not Available
Generic Name: Moxifloxacin
Synonyms: Moxifloxacin HCl; Moxifloxacin hydrochloride; BAY 12-8039
Drug Category: Anti-Bacterial Agents; Quinolones
Drug Type: Small Molecule; Approved
Other Brand Names containing Moxifloxacin: Avelox; Avelox I.V.; Vigamox;
Absorption: Well absorbed from the gastrointestinal tract. Absolute oral bioavailability is approximately 90%. Food has little effect on absorption.
Toxicity (Overdose): Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
Protein Binding: 50% bound to serum proteins, independent of drug concentration.
Biotransformation: Approximately 52% or oral or intravenous dose is metabolized via glucuronide and sulphate conjugation. The cytochrome P450 system is not involved in metabolism. The sulphate conjugate accounts for 38% of the dose, and the glucuronide conjugate accounts for 14% of the dose.
Half Life: 11.5-15.6 hours (single dose, oral)
Dosage Forms of Avelox: Solution Intravenous
Tablet Oral
Solution Ophthalmic
Chemical IUPAC Name: 7-[(4aS,7aS)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid
Chemical Formula: C21H24FN3O4
Moxifloxacin on Wikipedia: http://en.wikipedia.org/wiki/Moxifloxacin
Organisms Affected: Enteric bacteria and other eubacteria