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Delafloxacin Meglumine

Class: Quinolones
Chemical Name: 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid
Molecular Formula: C18H12ClF3N4O4
CAS Number: 1256037-58-7
Brands: Baxdela

Medically reviewed on Mar 5, 2018

Warning

    Serious Adverse Reactions
  • Fluoroquinolones have been associated with disabling and potentially irreversible serious adverse reactions (e.g., tendinitis and tendon rupture, peripheral neuropathy, CNS effects) that have occurred together.1 Discontinue immediately and avoid use of fluoroquinolones, including delafloxacin, in patients who have experienced any of these serious adverse reactions.1 (See Warnings under Cautions.)

  • Fluoroquinolones may exacerbate muscle weakness in patients with myasthenia gravis.1 Avoid in patients with known history of myasthenia gravis.1

Introduction

Antibacterial; fluoroquinolone.1 4 5

Uses for Delafloxacin Meglumine

Skin and Skin Structure Infections

Treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible Staphylococcus aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus or ORSA] and methicillin-susceptible S. aureus), S. haemolyticus, S. lugdunensis, Streptococcus pyogenes (group A β-hemolytic streptococci, GAS), S. agalactiae (group B streptococci, GBS), S. anginosus group (includes S. anginosus, S. intermedius, and S. constellatus), Enterococcus faecalis, Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, or Pseudomonas aeruginosa.1

Delafloxacin Meglumine Dosage and Administration

Administration

Administer orally or by slow IV infusion.1

Oral Administration

Administer tablets orally without regard to meals.1 (See Food under Pharmacokinetics.)

Administer orally at least 2 hours before or 6 hours after antacids containing magnesium or aluminum, metal cations (e.g., iron), sucralfate, multivitamins or dietary supplements containing iron or zinc, or buffered didanosine (pediatric powder for oral solution).1 (See Specific Drugs under Interactions.)

IV Infusion

Must be reconstituted and further diluted prior to IV infusion.1 Observe strict aseptic technique when preparing IV solutions.1

Do not infuse simultaneously through same tubing with other drugs.1 Do not administer with any solution containing multivalent cations (e.g., calcium, magnesium).1

If common IV line used to administer other drugs, flush with 0.9% sodium chloride injection or 5% dextrose injection before and after each delafloxacin infusion.1

Vials of lyophilized powder for injection are for single use only.1

For solution and drug compatibility information, see Compatibility under Stability.

Reconstitution

Reconstitute vial containing 300 mg of delafloxacin by adding 10.5 mL of 0.9% sodium chloride injection or 5% dextrose injection to provide a solution containing 25 mg/mL.1

Shake vial vigorously until contents completely dissolved.1 Reconstituted solution should appear clear yellow to amber in color.1

Dilution

To prepare a 300-mg dose of delafloxacin in a 250-mL infusion bag containing 0.9% sodium chloride injection or 5% dextrose injection, remove 12 mL of the diluent from infusion bag, then inject 12 mL of reconstituted delafloxacin solution into the bag.1 20 Concentration of final infusion solution is 1.2 mg/mL.1 20

To prepare a 200-mg dose of delafloxacin in a 250-mL infusion bag containing 0.9% sodium chloride injection or 5% dextrose injection, remove 8 mL of the diluent from infusion bag, then inject 8 mL of reconstituted delafloxacin solution into the bag.1 20 Concentration of final infusion solution is 0.8 mg/mL.1 20

Rate of Administration

Administer by IV infusion over 1 hour.1

Dosage

Available as delafloxacin meglumine;1 dosage expressed in terms of delafloxacin.1

Adults

Skin and Skin Structure Infections
Oral

450 mg every 12 hours for 5–14 days.1

IV

300 mg every 12 hours for 5–14 days.1

IV therapy may be switched to oral therapy at discretion of clinician.1 Total duration of IV and oral therapy is 5–14 days.1

Special Populations

Hepatic Impairment

Mild, moderate, or severe hepatic impairment (Child-Pugh class A, B, or C): Dosage adjustments not needed.1

Renal Impairment

Oral

Mild, moderate, or severe renal impairment (estimated GFR [eGFR] of 15–89 mL/minute per 1.73 m2): Dosage adjustments not needed.1

End-stage renal disease (eGFR <15 mL/minute per 1.73 m2): Not recommended.1

IV

Mild or moderate renal impairment (eGFR of 30–89 mL/minute per 1.73 m2): Dosage adjustments not needed.1

Severe renal impairment (eGFR of 15–29 mL/minute per 1.73 m2): 200 mg every 12 hours.1

End-stage renal disease (eGFR <15 mL/minute per 1.73 m2): Not recommended.1

Geriatric Patients

No dosage adjustments except those related to renal impairment.1 (See Renal Impairment under Dosage and Administration.)

Cautions for Delafloxacin Meglumine

Contraindications

  • Known hypersensitivity to delafloxacin, any component of the preparation, or other quinolones.1

Warnings/Precautions

Warnings

Disabling and Potentially Irreversible Serious Adverse Reactions

Systemic fluoroquinolones are associated with disabling and potentially irreversible serious adverse reactions (e.g., tendinitis and tendon rupture, peripheral neuropathy, CNS effects) that can occur together in the same patient.1 140 145 May occur within hours to weeks after a systemic fluoroquinolone is initiated;1 have occurred in all age groups and in patients without preexisting risk factors for such adverse reactions.1

Immediately discontinue at first signs or symptoms of any serious adverse reactions.1 140 145

Avoid systemic fluoroquinolones, including delafloxacin, in patients who have experienced any serious adverse reactions associated with fluoroquinolones.1 140 145

Tendinitis and Tendon Rupture

Systemic fluoroquinolones are associated with an increased risk of tendinitis and tendon rupture in all age groups.1 129

Risk of developing fluoroquinolone-associated tendinitis and tendon rupture is increased in older adults (usually those >60 years of age), individuals receiving concomitant corticosteroids, and kidney, heart, or lung transplant recipients.1 129 (See Geriatric Use under Cautions.)

Other factors that may independently increase the risk of tendon rupture include strenuous physical activity, renal failure, and previous tendon disorders such as rheumatoid arthritis.1 Tendinitis and tendon rupture have been reported in patients receiving fluoroquinolones who did not have any risk factors for such adverse reactions.1

Fluoroquinolone-associated tendinitis and tendon rupture most frequently involve the Achilles tendon;1 also reported in the rotator cuff (shoulder), hand, biceps, thumb, and other tendon sites.1

Tendinitis and tendon rupture can occur within hours or days after therapy initiated or as long as several months after completion of therapy;1 can occur bilaterally.1

Immediately discontinue delafloxacin if pain, swelling, inflammation, or rupture of a tendon occurs.1 129 (See Advice to Patients.)

Avoid systemic fluoroquinolones, including delafloxacin, in patients who have a history of tendon disorders or have experienced tendinitis or tendon rupture.1

Peripheral Neuropathy

Systemic fluoroquinolones are associated with an increased risk of peripheral neuropathy.1

Sensory or sensorimotor axonal polyneuropathy affecting small and/or large axons resulting in paresthesias, hypoesthesias, dysesthesias, and weakness reported with fluoroquinolones, including delafloxacin.1 130 Symptoms may occur soon after initiation of the drug and, in some patients, may be irreversible.1 130

Immediately discontinue delafloxacin if symptoms of peripheral neuropathy (e.g., pain, burning, tingling, numbness, and/or weakness) occur or if there are other alterations in sensations (e.g., light touch, pain, temperature, position sense, vibratory sensation, and/or motor strength).1 130

Avoid systemic fluoroquinolones, including delafloxacin, in patients who have experienced peripheral neuropathy.1

CNS Effects

Systemic fluoroquinolones are associated with an increased risk of CNS effects.1

Convulsions, increased intracranial pressure (including pseudotumor cerebri), and toxic psychosis reported with fluoroquinolones.1 Fluoroquinolones, including delafloxacin, may also cause nervousness, agitation, insomnia, anxiety, nightmares, paranoia, dizziness, confusion, tremors, hallucinations, depression, and suicidal thoughts or acts.1 CNS effects may occur after first dose.1

If CNS effects occur, immediately discontinue delafloxacin and institute appropriate measures.1 (See Advice to Patients.)

Use in patients with known or suspected CNS disorders (e.g., severe cerebral arteriosclerosis, epilepsy) or with other risk factors that predispose to seizures or lower seizure threshold only if potential benefits of the drug outweigh risks.1

Exacerbation of Myasthenia Gravis

Fluoroquinolones have neuromuscular blocking activity and may exacerbate muscle weakness in myasthenia gravis patients;1 death or need for ventilatory support reported.1

Avoid use in patients with known history of myasthenia gravis.1 (See Advice to Patients.)

Sensitivity Reactions

Hypersensitivity

Serious and occasionally fatal hypersensitivity and/or anaphylactic reactions reported in patients receiving fluoroquinolones.1 These reactions may occur with first or subsequent doses.1

Some hypersensitivity reactions reported with fluoroquinolones have been accompanied by cardiovascular collapse, loss of consciousness, tingling, edema (pharyngeal or facial), dyspnea, urticaria, or pruritus.1

Hypersensitivity and urticaria reported in patients receiving delafloxacin.1

Immediately discontinue delafloxacin at first appearance of rash or any other sign of hypersensitivity.1 (See Advice to Patients.)

Photosensitivity

No evidence of phototoxic potential.1

Other Warnings and Precautions

Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile.1 96 98 99 C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all anti-infectives, including delafloxacin, and may range in severity from mild diarrhea to fatal colitis.1 96 98 99 C. difficile produces toxins A and B which contribute to development of CDAD;1 96 hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.1

Consider CDAD if diarrhea develops during or after therapy and manage accordingly.1 96 98 99 Obtain careful medical history since CDAD may occur as late as ≥2 months after anti-infective therapy is discontinued.1

If CDAD suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible.1 96 Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.1 96 98 99

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of delafloxacin and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria.1

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.1 In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.1

Specific Populations

Pregnancy

Adequate data not available regarding use in pregnant women.1

When administered orally to pregnant rats during organogenesis, no malformations or fetal deaths were observed at delafloxacin concentrations 7 times estimated clinical exposure.1 Maternal toxicity and reduced fetal body weight observed at highest dose (1.6 g/kg per day);1 fetal ossification delays observed at all doses.1 Following IV administration to rats in late pregnancy through lactation, no adverse effects on offspring observed at clinically relevant concentrations.1

Lactation

Distributed into milk in lactating rats;1 not known if distributed into human milk, affects breast-fed infant, or affects milk production.1

Consider developmental and health benefits of breast-feeding along with the mother's clinical need for delafloxacin and potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.1

Pediatric Use

Safety and efficacy not established in children or adolescents <18 years of age.1

Quinolones cause arthropathy in juvenile animals.1

AAP states use of systemic fluoroquinolones may be justified in children <18 years of age in special circumstances when there are no safe and effective alternatives and after careful assessment of the risks and benefits for the individual patient.292 293

Geriatric Use

About 15% of patients receiving delafloxacin in clinical studies were ≥65 years of age.1 Clinical response rate at 48–72 hours was about 76% in patients ≥65 years of age compared with about 82% in those <65 years of age.1

Risk of severe tendon disorders, including tendon rupture, is increased in older adults (usually those >60 years of age).1 129 This risk is further increased in those receiving concomitant corticosteroids.1 129 (See Tendinitis and Tendon Rupture under Cautions.) Use caution in geriatric adults, especially those receiving concomitant corticosteroids.1

Hepatic Impairment

No clinically important differences in pharmacokinetics in adults with mild, moderate, or severe hepatic impairment (Child-Pugh class A, B, or C);1 dosage adjustments not needed in such patients.1

Renal Impairment

Severe renal impairment (eGFR of 15–29 mL/minute per 1.73 m2): Accumulation of the IV delafloxacin vehicle, sulfobutylether-β-cyclodextrin (SBECD), occurs.1 Reduce dosage (see Renal Impairment under Dosage and Administration) and closely monitor Scr and eGFR in patients receiving IV delafloxacin.1 Consider switching to oral delafloxacin if Scr increases during IV delafloxacin treatment.1 If eGFR decreases to <15 mL/minute per 1.73 m2, discontinue delafloxacin.1

End-stage renal disease (eGFR <15 mL/minute per 1.73 m2): Accumulation of IV delafloxacin vehicle (SBECD) occurs.1 Use of delafloxacin (oral or IV) not recommended.1

Common Adverse Effects

GI effects (nausea, diarrhea, vomiting), headache, elevated aminotransferase concentrations.1

Interactions for Delafloxacin Meglumine

Does not inhibit CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4/5 in vitro at clinically relevant concentrations;1 9 shows no potential for induction of CYP1A2, 2B6, 2C19, or 2C8.1 9 Mild induction of CYP2C9 and 3A4 in vitro.1 9

Drugs Affecting or Affected by Membrane Transporters

Substrate of P-glycoprotein (P-gp) transport and breast cancer resistance protein (BCRP) in vitro;1 clinical importance of concomitant use with P-gp inhibitor and/or BCRP inhibitor not known.1

Does not inhibit multidrug-resistance gene (MDR) 1, BCRP, organic anion transporter (OAT) 1, OAT3, organic anion transporting polypeptide (OATP) 1B1, OATP1B3, bile salt export pump (BSEP), or organic cation transporter (OCT) 1 or OCT2 at clinically relevant concentrations.1

Not a substrate of OAT1, OAT3, OCT1, OCT2, OATP1B1, or OATP1B3.1 3

Specific Drugs

Drug

Interaction

Comments

Antacids (aluminum- or magnesium-containing)

Possible decreased oral absorption and decreased systemic concentrations of delafloxacin;1 effect on IV delafloxacin unknown1

Administer oral delafloxacin at least 2 hours before or 6 hours after antacids containing aluminum or magnesium1

Antibacterials

Aztreonam, ceftazidime, colistin (commercially available in US as colistimethate sodium), co-trimoxazole, daptomycin, linezolid, meropenem, tigecycline, or vancomycin: No in vitro evidence of synergistic or antagonistic antibacterial effects1

Didanosine

Possible decreased oral absorption and decreased systemic concentrations of delafloxacin if used concomitantly with buffered didanosine (pediatric powder for oral solution);1 effect on IV delafloxacin unknown1

Administer oral delafloxacin at least 2 hours before or 6 hours after buffered didanosine1

Iron preparations

Possible decreased oral absorption and decreased systemic concentrations of delafloxacin;1 effect on IV delafloxacin unknown1

Administer oral delafloxacin at least 2 hours before or 6 hours after iron preparations1

Midazolam

No substantial effect on peak plasma concentrations or AUC of midazolam or its metabolite (1-hydroxymidazolam)1 9

Multivitamins and dietary supplements

Possible decreased oral absorption and decreased systemic concentrations of delafloxacin;1 effect on IV delafloxacin unknown1

Administer oral delafloxacin at least 2 hours before or 6 hours after multivitamins or dietary supplements containing iron or zinc1

Sucralfate

Possible decreased oral absorption and decreased systemic concentrations of delafloxacin;1 effect on IV delafloxacin unknown1

Administer oral delafloxacin at least 2 hours before or 6 hours after sucralfate1

Delafloxacin Meglumine Pharmacokinetics

Absorption

Bioavailability

Oral: Absolute bioavailability is 58.8%.1 6 Peak plasma concentrations attained 0.75 hours after single dose and 1 hour after a dose at steady state.1

IV: Peak plasma concentrations attained at end of 1-hour infusion after single dose and at steady state.1 6

Steady state achieved within approximately 3 days after oral or IV delafloxacin with accumulation of approximately 36 or 10%, respectively.1

AUC after single 450-mg oral dose is comparable to AUC after single 300-mg IV dose.1 6 Peak plasma concentrations are approximately 55% lower following oral administration;6 not considered clinically important.6

Food

No substantial effect on oral bioavailability.1 8

Distribution

Extent

Volume of distribution at steady state is 30–48 L, which approximates total body water.1 6

Distributed into breast milk in rats;1 not known if distributed into human breast milk.1

Plasma Protein Binding

84%, principally albumin.1

Special Populations

Plasma protein binding not substantially affected in patients with renal impairment.1

Elimination

Metabolism

Metabolized primarily via glucuronidation by UGT1A1, 1A3, and 2B15; 1 6 about 1% of a dose undergoes oxidative metabolism.1

Elimination Route

Oral: 50% of a dose eliminated in urine as unchanged delafloxacin and glucuronide metabolites;1 48% in feces as unchanged drug.1

IV: 65% of a dose eliminated in urine as unchanged delafloxacin and glucuronide metabolites;1 28% in feces as unchanged drug.1 6

Half-life

Oral: 4.2–8.5 hours.1

IV: 3.7 hours.1

Special Populations

Mild, moderate, or severe hepatic impairment (Child-Pugh class A, B, or C): Peak plasma concentrations and AUC not substantially affected.1 7

Mild renal impairment (eGFR of 51–80 mL/minute per 1.73 m2): Oral exposures comparable to those in healthy individuals;1 IV exposures increased 1.3-fold.1

Moderate renal impairment (eGFR of 31–50 mL/minute per 1.73 m2): Oral exposures increased 1.5-fold.1 IV exposures increased 1.6-fold;1 exposures of IV vehicle (SBECD) increased 2-fold.1

Severe renal impairment (eGFR of 15–29 mL/minute per 1.73 m2): Oral exposures increased 1.5-fold.1 IV exposures increased 1.8-fold;1 exposures of IV vehicle (SBECD) increased 5-fold.1

End-stage renal disease (eGFR <15 mL/minute per 1.73 m2) on hemodialysis: When administered IV 1 hour before and 1 hour after hemodialysis, exposures of delafloxacin increased 2.1- and 2.6-fold, respectively, and exposures of IV vehicle (SBECD) increased 7.5- and 27-fold, respectively.1 Approximately 19 and 56% of delafloxacin and SBECD, respectively, recovered in dialysate after 4 hours of hemodialysis.1

Pharmacokinetics not substantially affected by age, gender, race, weight, or body mass index.1 8

Stability

Storage

Oral

Tablets

20–25°C (may be exposed to 15–30°C).1

Parenteral

Powder for Injection, for IV Infusion

20–25°C (may be exposed to 15–30°C).1

Reconstituted or reconstituted and further diluted solutions may be stored under refrigeration or at controlled room temperature for up to 24 hours.1

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility1

Compatible

Dextrose 5%

Sodium chloride 0.9%

Incompatible

Dextrose 5% in Ringer's injection

Dextrose 5% in Ringer's injection, lactated

Ringer's injection

Ringer's injection, lactated

Actions and Spectrum

  • Like other fluoroquinolones, inhibits bacterial topoisomerase IV and DNA gyrase (i.e., topoisomerase II) enzymes.1 4 5 Demonstrates similar affinity for both topoisomerase IV and DNA gyrase.4 5 16

  • Exhibits concentration-dependent bactericidal activity.1 5 16 17

  • Gram-positive aerobes: Active in vitro and in clinical infections against S. aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus or ORSA] and methicillin-susceptible Staphylococcus aureus),1 10 16 17 18 19 S. haemolyticus,1 S. lugdunensis,1 Streptococcus pyogenes (group A β-hemolytic streptococci, GAS),1 16 17 19 S. agalactiae (group B streptococci, GBS),1 19 S. anginosus group (including S. anginosus, S. intermedius, and S. constellatus),1 and Enterococcus faecalis.1 16 17 19

  • Gram-negative aerobes: Active in vitro and in clinical infections against Escherichia coli,1 16 17 18 19 Enterobacter cloacae,1 18 Klebsiella pneumoniae,1 16 17 18 19 and Pseudomonas aeruginosa.1 16 17 19

  • Resistance can occur due to mutations in target regions of topoisomerase IV and DNA gyrase (i.e., quinolone-resistance determining regions [QRDRs]) or through altered efflux.1 4 5 In vitro, resistance develops by multiple step mutations in QRDRs of gram-positive and gram-negative bacteria (e.g., double mutations in gyrA and parC).1 4 10

  • Cross-resistance between delafloxacin and other fluoroquinolones reported; however, some isolates resistant to other fluoroquinolones may be susceptible to delafloxacin.1 5 10 16 17 19

Advice to Patients

  • Advise patients to read manufacturer’s patient information (medication guide).1

  • Advise patients that antibacterials (including delafloxacin) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).1

  • Advise patients that delafloxacin tablets may be taken without regard to food.1

  • Importance of taking delafloxacin tablets at least 2 hours before or 6 hours after magnesium- or aluminum- containing antacids, sucralfate, multivitamins or dietary supplements containing iron or zinc, or buffered didanosine (pediatric powder for oral solution).1

  • Importance of completing full course of therapy, even if feeling better after a few days.1 Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with delafloxacin or other antibacterials in the future.1

  • If a dose of delafloxacin is missed and remembered within 8 hours after the scheduled time, take the dose as soon as possible and take the next dose at the regularly scheduled time.1 If a dose is missed and remembered >8 hours after the scheduled time, skip the dose and take the next dose at the regularly scheduled time.1

  • Inform patients that systemic fluoroquinolones have been associated with disabling and potentially irreversible serious adverse reactions (e.g., tendinitis and tendon rupture, peripheral neuropathy, CNS effects) that may occur together in the same patient.1 140 145 Advise patients to immediately discontinue delafloxacin and contact a clinician if they experience any signs or symptoms of serious adverse effects (e.g., unusual joint or tendon pain, muscle weakness, a “pins and needles” tingling or pricking sensation, numbness of the arms or legs, confusion, hallucinations) while taking the drug.1 140 145 Advise patients to talk with a clinician if they have any questions or concerns.1 140 145

  • Inform patients that systemic fluoroquinolones are associated with an increased risk of tendinitis and tendon rupture in all age groups and that this risk is increased in adults >60 years of age, individuals receiving corticosteroids, and kidney, heart, or lung transplant recipients.1 Symptoms may be irreversible.1 Importance of resting and refraining from exercise at the first sign of tendinitis or tendon rupture (e.g., pain, swelling, or inflammation of a tendon or weakness or inability to use a joint) and importance of immediately discontinuing the drug and contacting a clinician.1 (See Tendinitis and Tendon Rupture under Cautions.)

  • Inform patients that peripheral neuropathies have been reported in patients receiving systemic fluoroquinolones and that symptoms may occur soon after initiation of the drug and may be irreversible.1 Importance of immediately discontinuing delafloxacin and contacting a clinician if symptoms of peripheral neuropathy (e.g., pain, burning, tingling, numbness, and/or weakness) occur.1

  • Inform patients that systemic fluoroquinolones have been associated with CNS effects (e.g., convulsions, dizziness, lightheadedness, increased intracranial pressure).1 Importance of informing clinician of any history of convulsions before initiating therapy with the drug.1 Importance of contacting a clinician if persistent headache with or without blurred vision occurs.1

  • Advise patients that delafloxacin may cause dizziness and lightheadedness;1 caution patients not to engage in activities requiring mental alertness and motor coordination (e.g., driving a vehicle, operating machinery) until effects of the drug on the individual are known.1

  • Advise patients that systemic fluoroquinolones may worsen myasthenia gravis symptoms;1 importance of informing clinician of any history of myasthenia gravis.1 Importance of immediately contacting a clinician if any symptoms of muscle weakness, including respiratory difficulties, occur.1

  • Inform patients that delafloxacin may be associated with hypersensitivity reactions (including anaphylactic reactions), even after the first dose.1 Importance of immediately discontinuing delafloxacin and contacting a clinician at first sign of rash, hives or other skin reaction, rapid heartbeat, difficulty swallowing or breathing, any swelling suggesting angioedema (e.g., swelling of lips, tongue, or face; throat tightness; hoarseness), jaundice, or any other sign of hypersensitivity.1

  • Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued.1 Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.1

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of advising patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Delafloxacin Meglumine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

450 mg (of delafloxacin)

Baxdela

Melinta

Parenteral

For injection, for IV infusion

300 mg (of delafloxacin)

Baxdela

Melinta

AHFS DI Essentials. © Copyright 2018, Selected Revisions March 5, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Melinta. Baxdela (delafloxacin meglumine) tablets and for injection for IV use prescribing information. Lincolnshire, IL; 2017 Jun.

2. Food and Drug Administration. Center for Drug Evaluation and Research. Application number 208610Orig1s000 and 208611Orig1s000: Summary review(s). From FDA website. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000SumR.pdf

3. Food and Drug Administration. Center for Drug Evaluation and Research. Application number 208610Orig1s000 and 208611Orig1s000: Clinical pharmacology and biopharmaceutics review(s). From FDA website. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf

4. Candel FJ, Peñuelas M. Delafloxacin: design, development and potential place in therapy. Drug Des Devel Ther. 2017; 11:881-891. http://www.ncbi.nlm.nih.gov/pubmed/28356714?dopt=AbstractPlus

5. Van Bambeke F. Delafloxacin, a non-zwitterionic fluoroquinolone in Phase III of clinical development: evaluation of its pharmacology, pharmacokinetics, pharmacodynamics and clinical efficacy. Future Microbiol. 2015; 10:1111-23. http://www.ncbi.nlm.nih.gov/pubmed/26119479?dopt=AbstractPlus

6. Hoover R, Hunt T, Benedict M et al. Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers. Clin Ther. 2016; 38:53-65. http://www.ncbi.nlm.nih.gov/pubmed/26718605?dopt=AbstractPlus

7. Hoover R, Marbury TC, Preston RA et al. Clinical Pharmacology of Delafloxacin in Patients With Hepatic Impairment. J Clin Pharmacol. 2017; 57:328-335. http://www.ncbi.nlm.nih.gov/pubmed/27570245?dopt=AbstractPlus

8. Hoover R, Hunt T, Benedict M et al. Single and Multiple Ascending-dose Studies of Oral Delafloxacin: Effects of Food, Sex, and Age. Clin Ther. 2016; 38:39-52. http://www.ncbi.nlm.nih.gov/pubmed/26581327?dopt=AbstractPlus

9. Paulson SK, Wood-Horrall RN, Hoover R et al. The Pharmacokinetics of the CYP3A Substrate Midazolam After Steady-state Dosing of Delafloxacin. Clin Ther. 2017; 39:1182-1190. http://www.ncbi.nlm.nih.gov/pubmed/28495029?dopt=AbstractPlus

10. McCurdy S, Lawrence L, Quintas M et al. In Vitro Activity of Delafloxacin and Microbiological Response against Fluoroquinolone-Susceptible and Nonsusceptible Staphylococcus aureus Isolates from Two Phase 3 Studies of Acute Bacterial Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2017; 61 http://www.ncbi.nlm.nih.gov/pubmed/28630189?dopt=AbstractPlus

11. Soge OO, Salipante SJ, No D et al. In Vitro Activity of Delafloxacin against Clinical Neisseria gonorrhoeae Isolates and Selection of Gonococcal Delafloxacin Resistance. Antimicrob Agents Chemother. 2016; 60:3106-11. http://www.ncbi.nlm.nih.gov/pubmed/26976873?dopt=AbstractPlus

13. Flamm RK, Rhomberg PR, Huband MD et al. In Vitro Activity of Delafloxacin Tested against Isolates of Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Antimicrob Agents Chemother. 2016; 60:6381-5. http://www.ncbi.nlm.nih.gov/pubmed/27458220?dopt=AbstractPlus

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