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Gemifloxacin

Pronunciation

(je mi FLOKS a sin)

Index Terms

  • DW286
  • Gemifloxacin Mesylate
  • LA 20304a
  • SB-265805

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Factive: 320 mg [DSC]

Factive: 320 mg [scored]

Brand Names: U.S.

  • Factive

Pharmacologic Category

  • Antibiotic, Fluoroquinolone
  • Antibiotic, Respiratory Fluoroquinolone

Pharmacology

Gemifloxacin is a DNA gyrase inhibitor and also inhibits topoisomerase IV. DNA gyrase (topoisomerase IV) is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; bactericidal

Absorption

Well absorbed from the GI tract

Distribution

Vdss: 4.2 L/kg

Metabolism

Hepatic (minor); forms metabolites (CYP isoenzymes are not involved)

Excretion

Feces (61%); urine (36%)

Time to Peak

Plasma: 0.5-2 hours

Half-Life Elimination

7 hours (range 4-12 hours)

Protein Binding

~60% to 70%

Special Populations: Renal Function Impairment

Average increase in AUC of approximately 70% in patients with renal insufficiency.

Use: Labeled Indications

Treatment of acute exacerbation of chronic bronchitis (in patients who have no other treatment options); treatment of community-acquired pneumonia (CAP), including pneumonia caused by multidrug-resistant strains of S. pneumoniae (MDRSP)

Use: Unlabeled

Acute sinusitis

Contraindications

Hypersensitivity to gemifloxacin, other fluoroquinolones, or any component of the formulation

Dosing: Adult

Susceptible infections: Oral: 320 mg once daily

Acute exacerbations of chronic bronchitis: Oral: 320 mg once daily for 5 days

Community-acquired pneumonia (mild-to-moderate): Oral: 320 mg once daily for 5 or 7 days (decision to use 5- or 7-day regimen should be guided by initial sputum culture; 7 days are recommended for MDRSP, Klebsiella, or M. catarrhalis infection)

Gonococcal, uncomplicated urogenital infections (alternative therapy in patients with cephalosporin allergy, off-label use): Oral: 320 mg as a single dose in combination with oral azithromycin (CDC [Workowski 2015]; Kirkcaldy 2014)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

CrCl >40 mL/minute: No dosage adjustment necessary.

CrCl ≤40 mL/minute (or patients on hemodialysis/CAPD): 160 mg once daily (administer dose following hemodialysis).

Dosing: Hepatic Impairment

No dosage adjustment necessary.

Administration

May be administered with or without food, milk, or calcium supplements. Do not administer supplements (including multivitamins) containing iron, zinc, or magnesium within 3 hours before or 2 hours after gemifloxacin.

Dietary Considerations

May take tablets with or without food, milk, or calcium supplements. Do not administer supplements (including multivitamins) containing iron, zinc, or magnesium within 3 hours before or 2 hours after gemifloxacin.

Storage

Store at 25°C (77°F). Protect from light.

Drug Interactions

Aminolevulinic Acid: Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid. Monitor therapy

Antacids: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of quinolones. Exceptions: Sodium Bicarbonate. Consider therapy modification

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Blood Glucose Lowering Agents: Quinolone Antibiotics may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Quinolone Antibiotics may diminish the therapeutic effect of Blood Glucose Lowering Agents. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy

Calcium Salts: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of both agents. Exceptions: Calcium Chloride. Consider therapy modification

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Avoid combination

Corticosteroids (Systemic): May enhance the adverse/toxic effect of Quinolone Antibiotics. Specifically, the risk of tendonitis and tendon rupture may be increased. Monitor therapy

Delamanid: Quinolone Antibiotics may enhance the QTc-prolonging effect of Delamanid. Management: Avoid concomitant use of delamanid and quinolone antibiotics if possible. If coadministration is considered to be unavoidable, frequent monitoring of electrocardiograms (ECGs) throughout the full delamanid treatment period should occur. Consider therapy modification

Didanosine: Quinolone Antibiotics may decrease the serum concentration of Didanosine. Didanosine may decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least 2 hours before or 6 hours after didanosine. Monitor for decreased therapeutic effects of quinolones, particularly if doses cannot be separated as recommended. This does not apply to unbuffered enteric coated didanosine. Consider therapy modification

Highest Risk QTc-Prolonging Agents: Moderate Risk QTc-Prolonging Agents may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Iron Salts: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least several hours before (4 h for moxi- and sparfloxacin, 2 h for others) or after (8 h for moxi-, 6 h for cipro-, 4 h for lome-, 3 h for gemi-, and 2 h for levo-, nor-, or ofloxacin or nalidixic acid) oral iron salts. Exceptions: Ferric Carboxymaltose; Ferric Gluconate; Ferric Hydroxide Polymaltose Complex; Ferric Pyrophosphate Citrate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Consider therapy modification

Ivabradine: May enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Avoid combination

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Magnesium Salts: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least several hours before (4 h for moxi- and sparfloxacin, 2 h for others) or after (8 h for moxi-, 6 h for cipro-, 4 h for lome-, 3 h for gemi-, and 2 h for levo-, nor-, or ofloxacin or nalidixic acid) oral magnesium salts. Consider therapy modification

MiFEPRIStone: May enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Avoid combination

Moderate Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of other Moderate Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease the serum concentration of Quinolone Antibiotics. Specifically, polyvalent cations in multivitamin products may decrease the absorption of orally administered quinolone antibiotics. Management: Interactions can be minimized by administering the oral quinolone at least 2 hours before, or 6 hours after, the dose of a multivitamin that contains polyvalent cations (i.e., calcium, iron, magnesium, selenium, zinc). Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): May decrease the serum concentration of Quinolone Antibiotics. Specifically, minerals in the multivitamin/mineral product may impair absorption of quinolone antibiotics. Management: Interactions can be minimized by administering the oral quinolone at least 2 hours before, or 6 hours after, the dose of a multivitamin that contains polyvalent cations (i.e., calcium, iron, magnesium, selenium, zinc). Consider therapy modification

Mycophenolate: Quinolone Antibiotics may decrease the serum concentration of Mycophenolate. Specifically, quinolones may decrease concentrations of the active metabolite of mycophenolate. Monitor therapy

Nadifloxacin: May enhance the adverse/toxic effect of Quinolone Antibiotics. Avoid combination

Nonsteroidal Anti-Inflammatory Agents: May enhance the neuroexcitatory and/or seizure-potentiating effect of Quinolone Antibiotics. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Quinolone Antibiotics. Monitor therapy

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Probenecid: May decrease the excretion of Gemifloxacin. Monitor therapy

QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying): May enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy

Quinapril: May decrease the serum concentration of Quinolone Antibiotics. Management: Separate doses of quinapril and oral quinolones by at least 2 hours in order to reduce the risk of interaction. Monitor for reduced efficacy of the quinolone if these products are used concomitantly. Consider therapy modification

Sevelamer: May decrease the absorption of Quinolone Antibiotics. Management: Administer oral quinolones at least 2 hours before or 6 hours after sevelamer. Consider therapy modification

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

Strontium Ranelate: May decrease the serum concentration of Quinolone Antibiotics. Management: In order to minimize any potential impact of strontium ranelate on quinolone antibiotic concentrations, it is recommended that strontium ranelate treatment be interrupted during quinolone therapy. Avoid combination

Sucralfate: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least 2 hours before or 6 hours after the sucralfate dose. Greater separation of doses may further lessen the risk for a significant interaction. Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification

Varenicline: Quinolone Antibiotics may increase the serum concentration of Varenicline. Management: Monitor for increased varenicline adverse effects with concurrent use of levofloxacin or other quinolone antibiotics, particularly in patients with severe renal impairment. International product labeling recommendations vary. Consult appropriate labeling. Monitor therapy

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Vinflunine: May enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Avoid combination

Vitamin K Antagonists (eg, warfarin): Quinolone Antibiotics may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy

Zinc Salts: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least several hours before (4 h for moxi- and sparfloxacin, 2 h for others) or after (8 h for moxi-, 6 h for cipro-, 4 h for lome-, 3 h for gemi-, and 2 h for levo-, nor-, or ofloxacin or nalidixic acid) oral zinc salts. Exceptions: Zinc Chloride. Consider therapy modification

Adverse Reactions

1% to 10%:

Central nervous system: Headache (4%), dizziness (2%)

Dermatologic: Skin rash (<1% to 5%)

Gastrointestinal: Diarrhea (5%), nausea (4%), abdominal pain (2%), vomiting (2%)

Hematologic: Change in neutrophil count (neutropenia/neutrophilia; 1%), increased platelets (1%), thrombocythemia (1%)

Hepatic: Increased serum transaminases (1% to 4%), increased gamma-glutamyl transferase (1%)

Neuromuscular & skeletal: Increased CPK (1%)

<1% (Limited to important or life-threatening): Acute renal failure, anaphylaxis, anemia, anorexia, antibiotic-associated colitis, dermatitis, dyspepsia, erythema multiforme, exacerbation of myasthenia gravis, fungal infection, gastritis, gastroenteritis, granulocytopenia, hemorrhage, hepatotoxicity (idiosyncratic) (Chalasani, 2014), hot flash, hyperglycemia, increased hematocrit, increased hemoglobin, increased INR, increased intracranial pressure, increased serum alkaline phosphatase, increased serum bilirubin, insomnia, leukopenia, myalgia, pain, peripheral edema, peripheral neuropathy, pharyngitis, pneumonia, prolonged Q-T interval on ECG, pseudotumor cerebri, retinal hemorrhage, rupture of tendon, skin photosensitivity, supraventricular tachycardia, syncope, tendonitis, thrombocytopenia, transient ischemic attacks, uveitis, vaginitis

ALERT: U.S. Boxed Warning

Serious adverse reactions:

Fluoroquinolones have been associated with disabling and potentially irreversible serious adverse reactions that have occurred together, including tendonitis and tendon rupture, peripheral neuropathy, and CNS effects. Discontinue gemifloxacin immediately and avoid use of fluoroquinolones in patients who experience any of these serious adverse reactions. Because fluoroquinolones have been associated with serious adverse reactions, reserve gemifloxacin for use in patients who have no alternative treatment options for acute bacterial exacerbation of chronic bronchitis.

Exacerbation of myasthenia gravis:

Fluoroquinolones may exacerbate muscle weakness in individuals with myasthenia gravis. Avoid gemifloxacin in patients with known history of myasthenia gravis.

Warnings/Precautions

Concerns related to adverse effects:

• Altered cardiac conduction: Fluoroquinolones may prolong QTc interval; avoid use in patients with a history of QTc prolongation, uncorrected hypokalemia, hypomagnesemia, or concurrent administration of other medications known to prolong the QT interval (including Class Ia and Class III antiarrhythmics, cisapride, erythromycin, antipsychotics, and tricyclic antidepressants).

• Glucose regulation: Fluoroquinolones have been associated with the development of serious, and sometimes fatal, hypoglycemia. These events have occurred most often in elderly patients with diabetes, but have also been reported in patients without a prior history of diabetes. Prompt identification and treatment of hypoglycemia is essential. Individual quinolones may differ in their potential to cause this effect. It was most evident with gatifloxacin (no longer marketed as s systemic formulation). Hyperglycemia has also been associated with the use of fluoroquinolones. Patients should be monitored closely for signs/symptoms of disordered glucose regulation.

• Hypersensitivity reactions: Severe hypersensitivity reactions, including anaphylaxis, have occurred with quinolone therapy. The spectrum of these reactions can vary widely; reactions may present as typical allergic symptoms (eg, itching, urticaria, rash, edema) after a single dose, or may manifest as severe idiosyncratic dermatologic (eg, Stevens-Johnson, toxic epidermal necrolysis), vascular (eg, vasculitis), pulmonary (eg, pneumonitis), renal (eg, nephritis), hepatic (eg, hepatic failure or necrosis), and/or hematologic (eg, anemia, cytopenias) events, usually after multiple doses. May cause maculopapular rash, usually 8-10 days after treatment initiation; risk factors may include age <40 years, female gender (including postmenopausal women on HRT), and treatment duration >7 days. Prompt discontinuation of drug should occur if skin rash or other symptoms arise.

• Phototoxicity: Avoid excessive sunlight and take precautions to limit exposure (eg, loose fitting clothing, sunscreen); may cause moderate-to-severe phototoxicity reactions. Discontinue use if photosensitivity occurs.

• Serious adverse reactions:[US Boxed Warning]: Fluoroquinolones are associated with disabling and potentially irreversible serious adverse reactions that may occur together, including tendinitis and tendon rupture, peripheral neuropathy, and CNS effects. Discontinue gemifloxacin immediately and avoid use of fluoroquinolones in patients who experience any of these serious adverse reactions. Patients of any age or without pre-existing risk factors have experienced these reactions; may occur within hours to weeks after initiation.

- CNS effects: Fluoroquinolones have been associated with an increased risk of CNS effects including seizures, increased intracranial pressure (including pseudotumor cerebri), and toxic psychosis; may also cause nervousness, agitation, insomnia, anxiety, nightmares, paranoia, dizziness, confusion, tremors, hallucinations, depression, and suicidal thoughts or actions. May occur following the first dose; discontinue immediately and avoid further use of fluoroquinolones in patients who experience these reactions. Use with caution in patients with known or suspected CNS disorder, or risk factors that may predispose to seizures or lower the seizure threshold.

- Peripheral neuropathy: Fluoroquinolones have been associated with an increased risk of peripheral neuropathy; may occur soon after initiation of therapy and may be irreversible; discontinue if symptoms of sensory or sensorimotor neuropathy occur. Avoid use in patients who have previously experienced peripheral neuropathy.

- Tendinitis/tendon rupture: Fluoroquinolones have been associated with an increased risk of f tendonitis and tendon rupture in all ages; risk may be increased with concurrent corticosteroids, solid organ transplant recipients, and in patients >60 years of age, but has also occurred in patients without these risk factors. Rupture of the Achilles tendon has been reported most frequently; but other tendon sites (eg, rotator cuff, biceps, hand) have also been reported. Inflammation and rupture may occur bilaterally. Cases have been reported within hours or days of initiation, and up to several months after discontinuation of therapy. Strenuous physical activity, renal failure, and previous tendon disorders may be independent risk factor for tendon rupture. Discontinue at first sign of tendon pain, swelling, inflammation or rupture. Avoid use in patients with a history of tendon disorders or who have experienced tendinitis or tendon rupture.

• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with significant bradycardia or acute myocardial ischemia.

• Myasthenia gravis: [US Boxed Warning]: May exacerbate muscle weakness related to myasthenia gravis; avoid use in patients with known history of myasthenia gravis. Cases of severe exacerbations, including the need for ventilatory support and deaths have been reported.

• Renal impairment: Use with caution in renal impairment; dosage adjustment required for CrCl ≤40 mL/minute. May increase risk of tendon rupture.

• Rheumatoid arthritis: Use with caution in patients with rheumatoid arthritis; may increase risk of tendon rupture.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Elderly: Adverse effects (eg, tendon rupture, QT changes) may be increased in the elderly.

• G6PD deficiency: Hemolytic reactions may (rarely) occur with quinolone use in patients with latent or actual G6PD deficiency.

Other warnings/precautions:

• Appropriate use: [US Boxed Warning]: Reserve use of gemifloxacin for treatment of acute bacterial exacerbation of chronic bronchitis for patients who have no alternative treatment options because of the risk of disabling and potentially serious adverse reactions (eg, tendinitis and tendon rupture, peripheral neuropathy, CNS effects).

Monitoring Parameters

WBC, signs/symptoms of infection, renal function

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies. Information specific to gemifloxacin use in pregnancy has not been located.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience diarrhea, nausea, vomiting, or abdominal pain. Have patient report immediately to prescriber signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes), signs of tendon inflammation or rupture (pain, bruising, or swelling in the back of the ankle, shoulder, hand, or other joints), signs of nerve problems (sensitivity to heat or cold; decreased sense of touch; burning, numbness, or tingling; pain, or weakness in the arms, hands, legs, or feet), signs of depression (suicidal ideation, anxiety, emotional instability, or confusion), signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, agitation, flushing, fast breathing, or breath that smells like fruit), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), signs of low blood sugar (dizziness, headache, fatigue, feeling weak, shaking, tachycardia, confusion, increased hunger, or sweating), angina, tachycardia, abnormal heartbeat, dizziness, chills, tinnitus, nightmares, insomnia, seizures, severe headache, shortness of breath, bruising, bleeding, hallucinations, severe loss of strength and energy, tremors, abnormal gait, vaginitis, vision changes, muscle pain, muscle weakness, or signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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