Gemifloxacin
Medication to treat chronic bronchitis
From Wikipedia, the free encyclopedia
Gemifloxacin mesylate, sold under the brand name Factive among others, is a broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. It is taken by mouth. Vansen Pharma Inc. licensed the active ingredient from LG Life Sciences of Korea.[citation needed]
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| Trade names | Factive |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a604014 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | 71% |
| Protein binding | 60–70% |
| Metabolism | Limited metabolism by the liver to minor metabolites |
| Excretion | Feces (61%); urine (36%) |
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| Formula | C18H20FN5O4 |
| Molar mass | 389.387 g·mol−1 |
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Common Uses (Indications)
Gemifloxacin is indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below.
- Acute bacterial exacerbation of chronic bronchitis caused by S. pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, or Moraxella catarrhalis
- Community-acquired pneumonia (of mild to moderate severity) caused by S. pneumoniae (including multi-drug resistant strains, Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamydia pneumoniae, or Klebsiella pneumoniae
Microbiology
Gemifloxacin has been shown to be active against most strains of the following microorganisms:
- Aerobic gram-positive microorganisms – Streptococcus pneumoniae[1]
including multi-drug resistant Streptococcus pneumoniae (MDRSP). MDRSP includes isolates previously known as PRSP (penicillin-resistant Streptococcus pneumoniae), and are strains resistant to two or more of the following antibiotics: penicillin, 2nd generation cephalosporins, e.g., cefuroxime, macrolides, tetracyclines and trimethoprim/sulfamethoxazole.
- Aerobic gram-negative microorganisms – Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae (many strains are moderately susceptible), Moraxella catarrhalis, Acinetobacter lwoffii, Klebsiella oxytoca, Legionella pneumophila, Proteus vulgaris.
- Other microorganisms – Chlamydia pneumoniae, Mycoplasma pneumoniae
Adverse effects
Fluoroquinolones are generally well tolerated with most side effects being mild and serious adverse effects being rarely.[2][3] Some of the serious adverse effects which occur more commonly with fluoroquinolones than with other antibiotic drug classes include CNS and tendon toxicity.[2][4] The currently marketed quinolones have safety profiles similar to that of other antimicrobial classes.[2]
The serious events may occur with therapeutic or with acute overdose. At therapeutic doses they include: central nervous system toxicity, cardiovascular toxicity, tendon / articular toxicity, and rarely hepatic toxicity.[5] Events that may occur in acute overdose are rare and include: renal failure and seizure.[5] Children and the elderly are at greater risk.[2][4] Tendon damage may manifest during, as well as up to a year after fluoroquinolone therapy.[6]
The FDA added a boxed warnings on all fluoroquinolones about the possible toxic effects of fluoroquinolones on tendons.[7]
In August 2013, the FDA issued a Safety Announcement where they described that they are requiring the medication guides and drug labels for all fluoroquinolones to be updated and better describe the risk for peripheral neuropathy.[8] The peripheral neuropathy may occur very quickly, and may be irreversible. This warning applies to fluoroquinolones taken by mouth and injection, but does not apply to fluoroquinolones taken topically.
Research
A study showed that gemifloxacin possess anti-metastatic activities against breast cancer in vitro and in vivo (in mice).[9]