Gemifloxacin
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| Clinical data | |
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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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| Chemical and physical data | |
| Formula | C18H20FN5O4 |
| Molar mass | 389.387 g·mol−1 |
| 3D model (JSmol) | |
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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]
Indications
[edit]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
[edit]Gemifloxacin has been shown to be active against most strains of the following microorganisms:
- Aerobic gram-positive microorganisms – Streptococcus pneumoniae[2]
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
[edit]Fluoroquinolones are generally well tolerated with most side effects being mild and serious adverse effects being rarely.[3][4] Some of the serious adverse effects which occur more commonly with fluoroquinolones than with other antibiotic drug classes include CNS and tendon toxicity.[3][5] The currently marketed quinolones have safety profiles similar to that of other antimicrobial classes.[3]
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.[6] Events that may occur in acute overdose are rare and include: renal failure and seizure.[6] Children and the elderly are at greater risk.[3][5] Tendon damage may manifest during, as well as up to a year after fluoroquinolone therapy.[7]
The FDA added a boxed warnings on all fluoroquinolones about the possible toxic effects of fluoroquinolones on tendons.[8]
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.[9] 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
[edit]A study showed that gemifloxacin possess anti-metastatic activities against breast cancer in vitro and in vivo (in mice).[10]
References
[edit]- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
- ^ Calvo A, Gimenez MJ (2002). "Ex Vivo Serum Activity (Killing Rates) After Gemifloxacin 320 mg Versus Trovafloxacin 200 mg Single Doses Against Ciprofloxacin-Susceptible and -Resistant Streptococcus pneumoniae". Int. J. Antimicrob. Agents. 20 (2): 144–6. doi:10.1016/S0924-8579(02)00119-X. PMID 12297365.
- ^ a b c d Owens RC, Ambrose PG (July 2005). "Antimicrobial safety: focus on fluoroquinolones". Clinical Infectious Diseases. 41 (Suppl 2): S144 – S157. doi:10.1086/428055. PMID 15942881.
- ^ Ball P, Mandell L, Niki Y, Tillotson G (November 1999). "Comparative tolerability of the newer fluoroquinolone antibacterials". Drug Safety. 21 (5): 407–421. doi:10.2165/00002018-199921050-00005. PMID 10554054. S2CID 26842570.
- ^ a b Iannini PB (June 2007). "The safety profile of moxifloxacin and other fluoroquinolones in special patient populations". Current Medical Research and Opinion. 23 (6): 1403–1413. doi:10.1185/030079907X188099. PMID 17559736. S2CID 34091286.
- ^ a b Nelson LH, Flomenbaum N, Goldfrank LR, Hoffman RL, Howland MD, Lewin NA (2006). Goldfrank's toxicologic emergencies. New York: McGraw-Hill, Medical Pub. Division. ISBN 978-0-07-143763-9.
- ^ Saint F, Gueguen G, Biserte J, Fontaine C, Mazeman E (September 2000). "[Rupture of the patellar ligament one month after treatment with fluoroquinolone]". Rev Chir Orthop Reparatrice Appar mot (in French). 86 (5): 495–7. PMID 10970974.
- ^ "FDA orders 'black box' label on some antibiotics". CNN. 8 July 2008. Retrieved 8 July 2008.
- ^ https://www.fda.gov/downloads/Drugs/DrugSafety/UCM365078.pdf [bare URL PDF]
- ^ Chen TC (January 2014). "Gemifloxacin inhibits migration and invasion and induces mesenchymal-epithelial transition in human breast adenocarcinoma cells". J Mol Med (Berl). 92 (1): 53–64. doi:10.1007/s00109-013-1083-4. PMID 24005829. S2CID 11279701.
