Delafloxacin

Uses

Delafloxacin is a fluoroquinolone antibiotic used to treat skin and skin structure infections.

Delafloxacin is indicated for the treatment of acute bacterial skin and skin structure infections caused by the Gram-positive organisms Staphylococcus aureus (including methicillin-resistant and methicillin-susceptible isolates), Staphylococcus haemolyticus, Staphylococcus lugdunensis, Streptococcus agalactiae, Streptococcus anginosus Group (including Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), Streptococcus pyogenes, and Enterococcus faecalis as well as the Gram-negative organisms Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, and Pseudomonas aeruginosa .

Delafloxacin is also used to associated treatment for these conditions: Acute Bacterial Skin and Skin Structure Infections caused by Enterobacter cloaecae, Acute Bacterial Skin and Skin Structure Infections caused by Enterococcus faecalis, Acute Bacterial Skin and Skin Structure Infections caused by Escherichia Coli, Acute Bacterial Skin and Skin Structure Infections caused by Klebsiella Pneumoniae, Acute Bacterial Skin and Skin Structure Infections caused by MRSA, Acute Bacterial Skin and Skin Structure Infections caused by MSSA, Acute Bacterial Skin and Skin Structure Infections caused by Pseudomonas Aeruginosa, Acute Bacterial Skin and Skin Structure Infections caused by Staphylococcus Aureus, Acute Bacterial Skin and Skin Structure Infections caused by Staphylococcus Lugdunensis, Acute Bacterial Skin and Skin Structure Infections caused by Staphylococcus haemolyticus, Acute Bacterial Skin and Skin Structure Infections caused by Streptococcus Agalactiae, Acute Bacterial Skin and Skin Structure Infections caused by Streptococcus anginosus, Acute Bacterial Skin and Skin Structure Infections caused by Streptococcus constellatus, Acute Bacterial Skin and Skin Structure Infections caused by Streptococcus intermedius, Acute Bacterial Skin and Skin Structure Infections caused by streptococcus pyogenes

How Delafloxacin works

Delafloxacin inhibits the activity of bacterial DNA topoisomerase IV and DNA gyrase (topoisomerase II) . This interferes with bacterial DNA replication by preventing the relaxation of positive supercoils introduced as part of the elongation process . The resultant strain inhibits further elongation. Delafloxacin exerts concentration-dependent bacteriocidal activity .

Toxicity

The most common adverse reactions noted with Delafloxacin were nausea (8%), diarrhea (8%), headache (3%), transaminase elevations (3%), and vomiting (2%) . Fluoroquinolones are associated with increased frequency of tendon rupture and tendonitis, increased risk of peipheral neuropathy, excacerbation of myasthenia gravis, and development of Clostridium difficile-associated diarrhea. Fluoroquinolones are also associated with an increased risk of central nervous system reactions (CNS), including: convulsions and increased intracranial pressure (including pseudotumor cerebri) and toxic psychosis. Fluoroquinolones may also cause CNS reactions of nervousness, agitation, insomnia, anxiety, nightmares, paranoia, dizziness, confusion, tremors, hallucinations, depression, and suicidal thoughts or acts.

Food Interaction

• Avoid multivalent ions. Separate the administration of multivalent cations from delafloxacin by at least 6 hours before or 2 hours after delafloxacin.
• Take separate from antacids. The administration of antacids should be separated from delafloxacin by at least 6 hours before or 2 hours after delafloxacin.
• Take with or without food.

Delafloxacin multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Oral preparations that contain magnesium, aluminum, or calcium may significantly decrease the gastrointestinal absorption of quinolone antibiotics.

Absorption may also be reduced by sucralfate, which contains aluminum, as well as other polyvalent cations such as iron and zinc.

The mechanism is chelation of quinolones by polyvalent cations, forming a complex that is poorly absorbed from the gastrointestinal tract.

The bioavailability of ciprofloxacin has been reported to decrease by as much as 90% when administered with antacids containing aluminum or magnesium hydroxide.

When coadministration cannot be avoided, quinolone antibiotics should be dosed either 2 to 4 hours before or 4 to 6 hours after polyvalent cation-containing products to minimize the potential for interaction.

When coadministered with Suprep Bowel Prep (magnesium

Please consult individual product labeling for specific recommendations.

Delafloxacin Drug Interaction

Unknown: nitazoxanide, moxifloxacin, tadalafil, duloxetine, torsemide, torsemide, dextromethorphan, amlodipine / valsartan, gemifloxacin, alendronate / cholecalciferol, chondroitin / glucosamine / methylsulfonylmethane, ledipasvir / sofosbuvir, levetiracetam, guaifenesin, bacitracin / neomycin / polymyxin b / pramoxine topical, acetaminophen / oxycodone, itraconazole, budesonide / formoterol, betamethasone / calcipotriene topical, solifenacin

Delafloxacin Disease Interaction

Major: colitis, renal impairment, CNS disorders, myasthenia gravis, peripheral neuropathy, tendonitisModerate: aortic aneurysm, crystalluria, diabetes

Volume of Distribution

The steady sate volume of distrubution of Delafloxacin is 30-48 liters .

Elimination Route

The median time to peak plasma concentration for orally administered Delafloxacin is 0.75 (0.5-4.0) hours after a single dose and 1.00 (0.5-6.0) hours for steady state dosing . The median time to peak plasma concentration for intravenously administered Delafloxacin is 1.00 (1.0-1.2) hours for a single dose and 1.0 (1.0-1.0) hour for steady state dosing. The absolute bioavailability for orally administed Delafloxacin is 58.8%.

Half Life

The mean half life of elimination of Delafloxacin is 3.7 hours after a single intravenous administration . The mean half life of elimination for multple oral administrations is 4.2-8.5 hours.

Clearance

The mean total clearance of Delafloxacin is 16.3 liters per hour . Renal clearance accounts for 35-45% of total clearance.

Elimination Route

After a single intravenous dose, 65% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 28% excreted unchanged in the feces . After a single oral dose, 50% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 48% excreted unchanged in the feces.

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