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Gemifloxacin Mesylate

Class: Quinolones
VA Class: AM900
Chemical Name: (Z-7-[3-(Aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid monomethanesulfonate
Molecular Formula: C18H20FN5O4•CH4O3S
CAS Number: 204519-65-3
Brands: Factive

Warning(s)

    Serious Adverse Reactions
  • Fluoroquinolones, including gemifloxacin, 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 gemifloxacin, in patients who have experienced any of these serious adverse reactions.1 (See Warnings under Cautions.)

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

  • Because of risk of serious adverse reactions, use gemifloxacin for treatment of acute bacterial exacerbations of chronic bronchitis only when no other treatment options available.1

Introduction

Antibacterial; naphthyridine derivative; fluoroquinolone.1 4 12 23

Uses for Gemifloxacin Mesylate

Respiratory Tract Infections

Treatment of acute bacterial exacerbations of chronic bronchitis caused by susceptible Streptococcus pneumoniae, Haemophilus influenzae, H. parainfluenzae, or Moraxella catarrhalis.1 2 3 28

Treatment of mild to moderate community-acquired pneumonia (CAP) caused by susceptible S. pneumoniae (including multidrug-resistant strains), H. influenzae, M. catarrhalis, Mycoplasma pneumoniae, Chlamydophila pneumoniae (formerly Chlamydia pneumoniae), or Klebsiella pneumoniae.1 29 43

Use for treatment of acute bacterial exacerbations of chronic bronchitis only when no other treatment options available.1 140 145 Because systemic fluoroquinolones, including gemifloxacin, have been 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 (see Cautions)1 140 145 and because acute bacterial exacerbations of chronic bronchitis may be self-limiting in some patients,1 risks of serious adverse reactions outweigh benefits of fluoroquinolones for patients with these infections.140 145

Consult current IDSA clinical practice guidelines available at for additional information on management of respiratory tract infections.31

Gemifloxacin Mesylate Dosage and Administration

Administration

Oral Administration

Administer orally once daily without regard to meals.1 14

Take with liberal amounts of fluids.1

Swallow tablets intact;1 do not chew or crush.1

Dosage

Available as gemifloxacin mesylate;1 dosage expressed in terms of gemifloxacin.1

Adults

Respiratory Tract Infections
Acute Exacerbations of Chronic Bronchitis
Oral

320 mg once daily for 5 days.1 (See Respiratory Tract Infections under Uses.)

Mild to Moderate Community-acquired Pneumonia (CAP)
Oral

Known or suspected to be caused by S. pneumoniae, H. influenzae, M. pneumoniae, or C. pneumoniae: 320 mg once daily for 5 days.1

Known or suspected to be caused by multidrug-resistant S. pneumoniae, K. pneumoniae, or M. catarrhalis: 320 mg once daily for 7 days.1

Manufacturer recommends that results of initial sputum cultures be used to guide clinical decisions regarding use of a 5- or 7-day regimen.1

Prescribing Limits

Adults

Do not exceed recommended dosage or duration of therapy.1

Special Populations

Hepatic Impairment

Dosage adjustments not required in adults with mild, moderate, or severe hepatic impairment (Child Pugh class A, B, or C).1

Renal Impairment

Reduce dosage to 160 mg once daily in adults with Clcr ≤40 mL/minute, including those on hemodialysis or CAPD.1

Gemifloxacin partially removed by hemodialysis;1 administer dose after hemodialysis.23

Geriatric Patients

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

Cautions for Gemifloxacin Mesylate

Contraindications

  • Known hypersensitivity to gemifloxacin, other fluoroquinolones, or any ingredient in the formulation.1

Warnings/Precautions

Warnings

Disabling and Potentially Irreversible Serious Adverse Reactions

Systemic fluoroquinolones, including gemifloxacin, 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 gemifloxacin at first signs or symptoms of any serious adverse reactions.1 140 145

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

Tendinitis and Tendon Rupture

Systemic fluoroquinolones, including gemifloxacin, are associated with an increased risk of tendinitis and tendon rupture in all age groups.1 128 129

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 (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 rotator cuff (shoulder), hand, biceps, thumb, and other tendon sites.1

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

Immediately discontinue gemifloxacin if pain, swelling, inflammation, or rupture of a tendon occurs.1 128 129 (See Advice to Patients.)

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

Peripheral Neuropathy

Systemic fluoroquinolones, including gemifloxacin, 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 systemic fluoroquinolones, including gemifloxacin.1 130 Symptoms may occur soon after initiation of the drug and, in some patients, may be irreversible.1 130

Immediately discontinue gemifloxacin 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).1 130 (See Advice to Patients.)

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

CNS Effects

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

Convulsions, increased intracranial pressure (including pseudotumor cerebri), and toxic psychosis reported in patients receiving fluoroquinolones.1 Fluoroquinolones may also cause CNS stimulation, which may lead to tremors, restlessness, anxiety, lightheadedness, confusion, hallucinations, paranoia, depression, insomnia, and rarely, suicidal thoughts or acts.1 These CNS effects may occur after first dose.1

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

Use with caution in patients with a history of convulsions, seizures, or epilepsy or with other risk factors that predispose to convulsions.1

Avoid systemic fluoroquinolones, including gemifloxacin, in patients who have experienced CNS effects associated with fluoroquinolones.1

Exacerbation of Myasthenia Gravis

Fluoroquinolones, including gemifloxacin, 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.)

Prolongation of QT Interval

Prolonged QT interval leading to ventricular arrhythmias, including torsades de pointes, reported with some fluoroquinolones, including gemifloxacin.1

Do not exceed recommended gemifloxacin dosage since this may increase risk of prolonged QT interval, especially in those with renal or hepatic impairment.1

Avoid use in patients with history of prolonged QT interval, in those with uncorrected electrolyte disorders (e.g., hypokalemia, hypomagnesemia), and in those receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents.1

Use with caution in patients receiving other drugs that prolong QT interval (e.g., cisapride [available in US only under limited-access protocol], erythromycin, antipsychotic agents, tricyclic antidepressants) and in those with ongoing proarrhythmic conditions, such as clinically important bradycardia or acute myocardial ischemia.1

Risk of QT interval prolongation may be increased in geriatric patients.1 (See Geriatric Use under Cautions.)

Musculoskeletal Effects

Fluoroquinolones, including gemifloxacin, cause arthropathy and osteochondrosis in immature animals of various species.1 12 45 46 47 48 49 52 53 Degeneration of articular cartilage reported in juvenile dogs, but not in mature dogs.1 (See Pediatric Use under Cautions.)

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

Possible emergence and overgrowth of nonsusceptible organism.1 Institute appropriate therapy if superinfection occurs.1

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 gemifloxacin, and may range in severity from mild diarrhea to fatal colitis.1 37 41 42 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

Outbreaks of severe CDAD caused by fluoroquinolone-resistant C. difficile have been reported with increasing frequency over the past several years.36 37 38 39 41

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

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

Sensitivity Reactions

Hypersensitivity Reactions

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

Some hypersensitivity reactions have been accompanied by cardiovascular collapse, hypotension or shock, seizures, loss of consciousness, tingling, angioedema (e.g., edema or swelling of tongue, larynx, throat, or face), airway obstruction (e.g., bronchospasm, shortness of breath, acute respiratory distress), dyspnea, urticaria, pruritus, and other severe skin reactions.1

Other serious and sometimes fatal adverse reactions reported with fluoroquinolones, including gemifloxacin, that may or may not be related to hypersensitivity reactions include one or more of the following: fever, rash or other severe dermatologic reactions (e.g., toxic epidermal necrolysis, Stevens-Johnson syndrome); vasculitis, arthralgia, myalgia, serum sickness; allergic pneumonitis; interstitial nephritis, acute renal insufficiency or failure; hepatitis, jaundice, acute hepatic necrosis or failure; anemia (including hemolytic and aplastic), thrombocytopenia (including thrombotic thrombocytopenic purpura), leukopenia, agranulocytosis, pancytopenia, and/or other hematologic effects.1

Immediately discontinue gemifloxacin at first appearance of rash, jaundice, or any other sign of hypersensitivity.1 23 Institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).1

Photosensitivity Reactions

Moderate to severe photosensitivity/phototoxicity reactions reported rarely with fluoroquinolones, including gemifloxacin.1

Phototoxicity may manifest as exaggerated sunburn reactions (e.g., burning, erythema, exudation, vesicles, blistering, edema) on areas exposed to sun or artificial ultraviolet (UV) light (usually face, neck, extensor surfaces of forearms, dorsa of hands).1

Relative potential of the various fluoroquinolones to cause photosensitivity/phototoxicity unclear.1 Factors that contribute to susceptibility to this adverse effect during fluoroquinolone therapy include patient’s skin pigmentation, frequency and duration of exposure to sun and UV light, use of protective clothing and sunscreen, concomitant use of other drugs, and dosage and duration of fluoroquinolone therapy.1

Avoid unnecessary or excessive exposure to sunlight or artificial UV light (tanning beds, UVA/UVB treatment) while receiving gemifloxacin.1 If patient needs to be outdoors, they should wear loose-fitting clothing that protects skin from sun exposure and use other sun protection measures (sunscreen).1

Discontinue gemifloxacin if photosensitivity or phototoxicity (sunburn-like reaction, skin eruption) occurs.1

General Precautions

Dermatologic Reactions

Rash (maculopapular, urticarial) reported;1 5 12 7–10% of rash cases were described as severe.1

Rash reported most frequently in patients <40 years of age (especially women), in women receiving hormone replacement therapy, and in patients who received gemifloxacin for >7 days (although this was not evident in men ≥40 years of age).1

Discontinue gemifloxacin at first appearance of rash or urticaria.1 (See Hypersensitivity Reactions under Cautions.)

Selection and Use of Anti-infectives

Use for treatment of acute bacterial exacerbations of chronic bronchitis only when no other treatment options available.1 140 145 Because gemifloxacin, like other systemic fluoroquinolones, has been 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, risks of serious adverse reactions outweigh benefits for patients with these infections.140 145

When prescribing a fluoroquinolone, consider potential benefits and risks for the individual patient.128 129 Most patients tolerate the drugs, but serious adverse reactions (e.g., CNS effects, QT prolongation, C. difficile-associated diarrhea and colitis, damage to liver, kidneys, or bone marrow, alterations in glucose homeostasis) may occur rarely.128 129

To reduce development of drug-resistant bacteria and maintain effectiveness of gemifloxacin and other antibacterials, use only for treatment or prevention 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

Category C.1

Lactation

Distributed into milk in rats.1 Do not use in nursing women unless possible benefits outweigh potential risks.1

Pediatric Use

Safety and efficacy not established in children or adolescents <18 years of age.1 Like other fluoroquinolones, gemifloxacin causes arthropathy and osteochondrosis in juvenile animals.1 12 45 46 47 48 49 52 53 (See Musculoskeletal Effects under Cautions.)

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 risks and benefits for the individual patient.110 292

Geriatric Use

No overall differences in safety or efficacy relative to younger adults.1

Risk of severe tendon disorders, including tendon rupture, is increased in older adults (usually those >60 years of age).1 128 129 This risk is further increased in those receiving concomitant corticosteroids.1 128 129 (See Tendinitis and Tendon Rupture under Cautions.) Use caution in geriatric adults, especially those receiving concomitant corticosteroids.1

Risk of QT interval prolongation may be increased in geriatric patients.1 (See Prolongation of QT Interval under Cautions.)

Consider age-related decreases in renal function when selecting dosage.1 (See Renal Impairment under Dosage and Administration.)

Hepatic Impairment

Serum concentrations and AUC may be increased;1 dosage adjustments not considered necessary.1

Renal Impairment

Decreased renal clearance and prolonged half-life;1 reduce dosage in those with Clcr ≤40 mL/minute.1 (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

GI effects (diarrhea, nausea, abdominal pain, vomiting), rash, headache, dizziness.1

Interactions for Gemifloxacin Mesylate

Does not inhibit and is not metabolized by CYP isoenzymes.1 Pharmacokinetic interactions with drugs metabolized by CYP isoenzymes unlikely.1

Drugs that Prolong QT Interval

Potential pharmacologic interaction (additive effect on QT interval prolongation).1 Avoid use in patients receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents.1 Use with caution in patients receiving other drugs that prolong QT interval (e.g., cisapride [available in US only under limited-access protocol], erythromycin, antipsychotic agents, tricyclic antidepressants).1 (See Prolongation of QT Interval under Cautions.)

Specific Drugs

Drug

Interaction

Comments

Antacids (aluminum- or magnesium-containing)

Decreased absorption of gemifloxacin1

Administer antacids containing aluminum or magnesium at least 3 hours before or 2 hours after gemifloxacin1

Antacids (calcium-containing); calcium supplements

No clinically important pharmacokinetic interactions 1

Anticoagulants, oral (warfarin)

Increased PT, INR, and/or bleeding reported1

Closely monitor PT, INR, or other suitable coagulation tests1

Consider that infectious disease and its accompanying inflammatory process, age, and general patient status also are risk factors for increased anticoagulation activity1

Cimetidine

Slightly increased gemifloxacin concentrations1

Not considered clinically important1

Corticosteroids

Increased risk of tendinitis or tendon rupture, especially in patients >60 years of age1

Use concomitantly with caution1

Didanosine

Decreased absorption of gemifloxacin if used with buffered didanosine preparations1

Administer buffered didanosine (pediatric oral solution admixed with antacid) at least 3 hours before or 2 hours after gemifloxacin1

Digoxin

No evidence of effect on digoxin pharmacokinetics1

Estrogens/progestins

Oral contraceptives containing ethinyl estradiol and levonorgestrel: Possible decreased gemifloxacin concentrations;1 no effect on pharmacokinetics of ethinyl estradiol and levonorgestrel1

Not considered clinically important1

Iron preparations

Decreased absorption of gemifloxacin1 15

Administer ferrous sulfate and dietary supplements containing iron at least 3 hours before or 2 hours after gemifloxacin1 15

Multivitamins and mineral supplements

Decreased absorption of gemifloxacin1

Administer supplements containing iron, magnesium, zinc, or other metal cations at least 3 hours before or 2 hours after gemifloxacin1

Omeprazole

Slightly increased gemifloxacin concentrations1

Not considered clinically important1

Probenecid

Decreased clearance of gemifloxacin resulting in increased gemifloxacin concentrations and half-life1

Sucralfate

Decreased absorption of gemifloxacin1 15

Administer gemifloxacin at least 2 hours before sucralfate1 15

Theophylline

No evidence of effect on theophylline pharmacokinetics 1

Gemifloxacin Mesylate Pharmacokinetics

Absorption

Bioavailability

71%.1

Rapidly absorbed from GI tract;1 21 30 peak plasma concentrations attained within 0.5 –2 hours.1 21 30

Food

Administration of 320-mg dose with a standard high-fat breakfast (2 eggs cooked in butter, 2 strips of bacon, hash brown potatoes, 2 slices of toast with butter, 300 mL whole milk) reduces peak plasma concentration and AUC by 12 and 3%, respectively;14 this reduction in systemic exposure not considered clinically important.1 14

Distribution

Extent

Widely distributed into body tissues and fluids, including lung tissue and fluids.1

Distributed into milk in rats.1

Plasma Protein Binding

60–70%.1

Elimination

Metabolism

Metabolized to a limited extent in liver.1 Not metabolized by CYP isoenzymes.1

Elimination Route

Eliminated by renal and nonrenal mechanisms.1

36% of a dose eliminated in urine and 61% excreted in feces as unchanged drug and metabolites.1

Half-life

7 hours (range 4–12 hours).1 21 30

Special Populations

Pharmacokinetics in geriatric patients similar to that in younger adults.1

Adults with hepatic impairment: Peak plasma concentrations increased 25% in those with mild to moderate hepatic impairment (Child-Pugh class A or B) and increased 41% in those with severe hepatic impairment (Child-Pugh class C); no substantial change in plasma half-life.1 Increased serum concentrations not considered clinically important.1

Adults with renal impairment: Decreased clearance and prolonged half-life.1

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).1 Protect from light.1

Actions and Spectrum

  • Usually bactericidal.1

  • Like other fluoroquinolones, gemifloxacin inhibits bacterial DNA gyrase and topoisomerase IV.1 4 12 Unlike some fluoroquinolones, gemifloxacin targets both enzymes in susceptible S. pneumoniae.1 12

  • Spectrum of activity includes gram-positive aerobic bacteria, some gram-negative aerobic bacteria, and some other organisms (e.g., Chlamydia, Mycoplasma).1 4 12 22

  • More active in vitro than some other fluoroquinolones against S. pneumoniae,4 12 13 22 23 but less active than ciprofloxacin in vitro against many Enterobacteriaceae and Pseudomonas aeruginosa.4 12

  • Gram-positive aerobes: Active in vitro and in clinical infections against S. pneumoniae (including penicillin-resistant and multidrug-resistant strains).1 Also active in vitro against Staphylococcus aureus (oxacillin-susceptible [methicillin-susceptible] strains only) and S. pyogenes (group A β-hemolytic streptococci).1

  • Gram-negative aerobes: Active in vitro and in clinical infections against H. influenzae,1 H. parainfluenzae,1 K. pneumoniae,1 and M. catarrhalis.1 Also active in vitro against some strains of Acinetobacter, K. oxytoca, Legionella pneumophila, and Proteus vulgaris.1

  • Other organisms: Active in vitro and in clinical infections against C. pneumoniae 1 and M. pneumoniae.1 Has some activity against Mycobacterium tuberculosis in vitro, but is considerably less active against mycobacteria than some other fluoroquinolones (e.g., ciprofloxacin, ofloxacin, levofloxacin).27

  • Some cross-resistance occurs between gemifloxacin and other fluoroquinolones.1

Advice to Patients

  • Advise patients to read the manufacturer’s patient information (medication guide) prior to initiating gemifloxacin therapy and each time prescription refilled.1

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

  • May be taken without regard to meals,1 but should be taken with liberal amounts of fluids.1

  • Importance of taking gemifloxacin at least 2 hours before or 3 hours after multivitamins containing iron, magnesium, or zinc; aluminum- or magnesium-containing antacids; or buffered didanosine (pediatric oral solution admixed with antacid).1 Importance of taking gemifloxacin at least 2 hours before sucralfate.1

  • Inform patients that systemic fluoroquinolones, including gemifloxacin, 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 same patient.1 140 145 Advise patients to immediately discontinue gemifloxacin 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, including gemifloxacin, are associated with an increased risk of tendinitis and tendon rupture in all age groups and this risk is increased in adults >60 years of age, individuals receiving corticosteroids, and kidney, heart, or lung transplant recipients.1 Importance of resting and refraining from exercise at 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 with systemic fluoroquinolones, including gemifloxacin, and that symptoms may occur soon after initiation of the drug and may be irreversible.1 Importance of immediately discontinuing gemifloxacin 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, including gemifloxacin, have been associated with CNS effects (e.g., convulsions, dizziness, lightheadedness, increased intracranial pressure, tremors, restlessness, lightheadedness, confusion, hallucinations) that can occur following first dose.1 Importance of informing clinician of any history of convulsions, seizures, or epilepsy before initiating therapy with the drug.1

  • Advise patients that gemifloxacin 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, including gemifloxacin, 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 gemifloxacin may be associated with hypersensitivity reactions (including anaphylactic reactions), even after first dose.1 Importance of immediately discontinuing gemifloxacin and contacting a clinician at first sign of rash, jaundice, or any other sign of hypersensitivity.1

  • Advise patient that gemifloxacin has been associated with rash or hives and that rash occurs most frequently in patients <40 years of age (especially women), in women receiving hormone replacement therapy, and in patients who receive gemifloxacin for >5 days (especially when given for >7 days).1 Importance of discontinuing gemifloxacin and informing a clinician if rash occurs.1

  • Inform patients that photosensitivity/phototoxicity reactions reported following exposure to sun or UV light in patients receiving fluoroquinolones.1 Importance of avoiding or minimizing exposure to sunlight or artificial UV light (e.g., tanning beds, UVA/UVB treatment) and using protective measures (e.g., wearing loose-fitting clothes, sunscreen) if outdoors during gemifloxacin therapy.1 Importance of discontinuing gemifloxacin and contacting a clinician if a sunburn-like reaction or skin eruption occurs.

  • Advise patient that gemifloxacin may prolong QT interval and should be avoided in those receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents and should be used with caution in those receiving other drugs that prolong QT interval (e.g., cisapride [available in US only under limited-access protocol], erythromycin, antipsychotic agents, tricyclic antidepressants).1

  • Importance of informing clinician of personal or family history of QT interval prolongation or proarrhythmic conditions (e.g., hypokalemia, bradycardia, recent myocardial ischemia).1 Importance of informing a clinician if palpitations or fainting spells occur.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 (e.g., drugs that may affect QT interval, warfarin), 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.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Gemifloxacin Mesylate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

320 mg (of gemifloxacin)*

Factive

Merus

Gemifloxacin Mesylate Tablets

AHFS DI Essentials. © Copyright 2017, Selected Revisions September 30, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Merus Labs International Inc. Factive (gemifloxacin mesylate) tablets prescribing information. Toronto, ON M5K 1H1. 2016 May.

2. File T, Schlemmer B, Garau J et al. Gemifloxacin versus amoxicillin/clavulanate in the treatment of acute exacerbations of chronic bronchitis. J Chemother. 2000; 12:314-25. [PubMed 10949981]

3. Wilson R, Schentag JJ, Ball P et al. A comparison of gemifloxacin and clarithromycin in acute exacerbations of chronic bronchitis and long-term clinical outcomes. Clin Ther. 2002; 24:639-52. [PubMed 12017408]

4. Lowe MN, Lamb HM. Gemifloxacin. Drugs. 2000; 59:1137-47. [PubMed 10852645]

5. File TM, Schlemmer B, Garau J et al. Efficacy and safety of gemifloxacin in the treatment of community-acquired pneumonia: a randomized, double-blind comparison with trovafloxacin. J Antimicrob Chemother. 2001; 48:67-74. [PubMed 11474633]

12. Zhanel GG, Ennis K, Vercaigne L et al. A critical review of the fluoroquinolones: focus on respiratory tract infections. Drugs. 2002; 62:13-59. [PubMed 11790155]

13. Ball P. Quinolone generations: natural history or natural selection?. J Antimicrob Chemother. 2000; 46:17-24. [PubMed 10997595]

14. Allen A, Bygate E, Clark D et al. The effect of food on the bioavailability of oral gemifloxacin in healthy volunteers. Int J Antimicrob Agents. 2000; 16:45-50. [PubMed 11185412]

15. Allen A, Bygate E, Faessel H et al. The effect of ferrous sulphate and sucralfate on the bioavailability of oral gemifloxacin in healthy volunteers. Int J Antimicrob Agents. 2000; 16:283-9.

16. Allen A, Vousden M, Porter A et al. Effect of Maalox on the bioavailability of oral gemifloxacin in healthy volunteers. Chemotherapy. 1999; 45:504-11. [PubMed 10567782]

17. Davy M, Allen A, Bird N et al. Lack of effect of gemifloxacin on the steady-state pharmacokinetics of theophylline in healthy volunteers. Chemotherapy. 1999; 45:478-84. [PubMed 10567778]

18. Vousden M, Allen A, Lewis A et al. Lack of pharmacokinetic interaction between gemifloxacin and digoxin in healthy elderly volunteers. Chemotherapy. 1999; 45:485-90. [PubMed 10567779]

19. Davy M, Bird N, Rost KL et al. Lack of effect of gemifloxacin on the steady-state pharmacodynamics of warfarin in healthy volunteers. Chemotherapy. 1999; 45:491-5. [PubMed 10567780]

20. Allen A, Vousden M, Lewis A et al. Effect of omeprazole on the pharmacokinetics of oral gemifloxacin in healthy volunteers. Chemotherapy. 1999; 45:496-503. [PubMed 10567781]

21. Allen A, Bygate E, Vousden M et al. Multiple-dose pharmacokinetics and tolerability of gemifloxacin administered orally to healthy volunteers. Antimicrob Agents Chemother. 2001; 45:540-5. [PubMed 11158752]

22. Boswell FJ, Andrews JM, Jevons G et al. Comparison of the in vitro activities of several new fluoroquinolones against respiratory pathogens and their abilities to select fluoroquinolone resistance. J Antimicrob Chemother. 2002; 50:495-502. [PubMed 12356793]

23. Genesoft, Inc, South San Francisco, CA: Personal communication.

27. Ruiz-Serrano MJ, Alcala L, Martinez L et al. In vitro activities of six fluoroquinolones against 250 clinical isolates of Mycobacterium tuberculosis susceptible or resistant to first-line antituberculosis drugs. Antimicrob Agents Chemother. 2000; 44:2567-8.

28. Sethi S, Fogarty C, Fulambarker A. A randomized, double-blind study comparing 5 days oral gemifloxacin with 7 days of levofloxacin in patients with acute exacerbation of chronic bronchitis. Respir Med. 2004; 98:697-707. [PubMed 15303633]

29. Leophonte P, File T, Feldman C. Gemifloxacin once daily for 7 days compared to amoxicillin/clavulanic acid thrice daily for 10 days for the treatment of community-acquired pneumonia of suspected pneumococcal origin. Respir Med. 2004; 98:708-20. [PubMed 15303634]

30. Allen A, Bygate E, Oliver S et al. Pharmacokinetics and tolerability of gemifloxacin (SB-265805) after administration of single oral doses to healthy volunteers. Antimicrob Agents Chemother. 2000; 44:1604-8. [PubMed 10817716]

31. Mandell LA, Wunderink RG, Anzueto A et al. Infectious Diseases Society of America/American Thoracic Society consensus guidelines on the management of community-acquired pneumonia in adults. Clin Infect Dis. 2007; 44 Suppl 2:S27-72. Updates may be available at IDSA website at www.idsociety.org. [PubMed 17278083]

36. McDonald LC, Killgore GE, Thompson A et al. An epidemic, toxin gene-variant strain of Clostridium difficile. N Engl J Med. 2005; 353:2433-41. [PubMed 16322603]

37. Loo VG, Poirier L, Miller MA et al. A predominantly clonal multi-institutional outbreak of Clostridium difficile-associated diarrhea with high morbidity and mortality. N Engl J Med. 2005; 353:2442-9. [PubMed 16322602]

38. McDonald LC, Owings M, Jernigan DB. Clostridium difficile infection in patients discharged from US short-stay hospitals, 1996-2003. Emerg Infect Dis. 2006; 12:409-15. [PubMed 16704777]

39. Bartlett JG, Peri TM. The new Clostridium difficile–what does it mean? N Engl J Med. 2005; 353:2503-5.

41. Kazakova SV, Ware K, Baughman B et al. A hospital outbreak of diarrhea due to an emerging epidemic strains of Clostridium difficile. Arch Intern Med. 2006; 166:2518-24. [PubMed 17159019]

42. Dhalla IA, Mamdani MM, Simor AE et al. Are broad-spectrum fluoroquinolones more likely to cause Clostridium difficile-associated disease? Antimicrob Agents Chemother. 2006; 50:3216-9.

43. File TM Jr, Mandell LA, Tillotson G et al. Gemifloxacin once daily for 5 days versus 7 days for the treatment of community-acquired pneumonia: a randomized, multicentre, double-blind study. J Antimicrob Chemother. 2007; 60:112-20. [PubMed 17537866]

45. Davis GJ, McKenzie ME. Toxicologic evaluation of ofloxacin. Am J Med. 1989; 87(Suppl 6C):43S-46S. [PubMed 2690619]

46. Mayer DG. Overview of toxicological studies. Drugs. 1987; 34(Suppl 1):150-3. [PubMed 3325258]

47. Kato M, Onodera T. Morphological investigation of cavity formation in articular cartilage induced by ofloxacin in rats. Fund Appl Toxicol. 1988; 11:110-9.

48. Hooper DC, Wolfson JS. Fluoroquinolone antimicrobial agents. N Engl J Med. 1991; 324:384-94. [PubMed 1987461]

49. Paton JH, Reeves DS. Fluoroquinolone antibiotics: microbiology, pharmacokinetics and clinical uses. Drugs. 1988; 36:193-228. [PubMed 3053126]

50. Maggiolo F, Caprioli S, Suter F. Risk/benefit analysis of quinolone use in children: the effect on diarthrodial joints. J Antimicrob Chemother. 1990; 26:469-71. [PubMed 2254219]

51. Pfister K, Mazur D, Vormann J et al. Diminished ciprofloxacin-induced chondrotoxicity by supplementation with magnesium and vitamin E in immature rats. Antimicrob Agents Chemother. 2007; 51:1022-7. [PubMed 17210779]

52. Stahlmann R. Safety profile of the quinolones. J Antimicrob Chemother. 1990; 26(Suppl D):31-44. [PubMed 2286589]

53. Christ W, Lehnert T, Ulbrich B. Specific toxicologic aspects of the quinolones. Rev Infect Dis. 1988; 10(Suppl 1):S141-6. [PubMed 3279489]

96. Cohen SH, Gerding DN, Johnson S et al. Clinical practice guidelines for Clostridium difficile infection in adults: 2010 update by the Society for Healthcare Epidemiology of America (SHEA) and the Infectious Diseases Society of America (IDSA). Infect Control Hosp Epidemiol. 2010; 31:431-55. [PubMed 20307191]

98. Fekety R for the American College of Gastroenterology Practice Parameters Committee. Guidelines for the diagnosis and management of Clostridium difficile-associated diarrhea and colitis. Am J Gastroenterol. 1997; 92:739-50. [PubMed 9149180]

99. American Society of Health-System Pharmacists Commission on Therapeutics. ASHP therapeutic position statement on the preferential use of metronidazole for the treatment of Clostridium difficile-associated disease. Am J Health-Syst Pharm. 1998; 55:1407-11. [PubMed 9659970]

110. Bradley JS, Jackson MA, Committee on Infectious Diseases et al. The use of systemic and topical fluoroquinolones. Pediatrics. 2011; 128:e1034-45.

128. US Food and Drug Administration. FDA news. FDA requests boxed warnings on fluoroquinolone antimicrobial drugs. From the FDA website. Accessed 2008 Sept 8.

129. US Food and Drug Administration. Information for healthcare professionals. FDA alert regarding fluoroquinolone antimicrobial drugs. 2008 Jul 8. From FDA website. Accessed 2008 Sept 8.

130. US Food and Drug Administration. FDA drug safety communication: FDA requires label changes to warn of risk for possibly permanent nerve damage from antibacterial fluoroquinolone drugs taken by mouth or by injection. 2013 Aug 15. From FDA website.

140. US Food and Drug Administration. FDA drug safety communication: FDA advises restricting fluoroquinolone antibiotic use for certain uncomplicated infections; warns about disabling side effects that can occur together. Silver Spring, MD; 2016 May 12. From FDA website.

145. US Food and Drug Administration. FDA drug safety communication: FDA updates warnings for oral and injectable fluoroquinolone antibiotics due to disabling side effects. Silver Sring, MD; 2016 Jul 26. From FDA website.

292. American Academy of Pediatrics. Red Book: 2015 Report of the Committee on Infectious Diseases. 30th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2015.

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