Gemifloxacin is a fluoroquinolone antibiotic with the antimicrobial property. Gemifloxacin enters bacterial cells by diffusion through integral membrane porin pathway before targeting both DNA gyrase and topoisomerase IV, two enzymes critical for DNA replication and repair. This agent binds to the DNA/DNA-gyrase complex and inhibits the A subunits of the enzyme thereby preventing the bacterial chromosome from rejoining. This interferes with DNA replication and repair processes as well as transcription and ultimately leads to bacterial cell death. Gemifloxacin targets at both Gram-positive, -negative and atypical human pathogens.
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Gemifloxacin is a fourth generation, an oral fluoroquinolone antibiotic used in the therapy of mild-to-moderate respiratory tract infections caused by susceptible organisms. Gemifloxacin has been linked to rare instances of acute liver injury.
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Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth.
Mechanism of Action of Gemifloxacin
Gemifloxacin is a quinolone/fluoroquinolone antibiotic. Gemifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably, the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Like other fluoroquinolone anti-infective agents, gemifloxacin inhibits DNA synthesis in susceptible organisms via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV). However, unlike many other fluoroquinolones, gemifloxacin targets both DNA gyrase and topoisomerase IV in susceptible S. pneumoniae. Although cross-resistance can occur between gemifloxacin and other fluoroquinolones, gemifloxacin may be active against some strains of S. pneumoniae resistant to ciprofloxacin and other fluoroquinolones.
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The fluroquinolone gemifloxacin was examined for its capacity to modulate secretion of cytokines by human monocytes stimulated with lipopolysaccharide (LPS). Monocytes from six male and two female healthy volunteers were stimulated with LPS, exposed to gemifloxacin and the amounts of secreted IL-1 alpha, IL-1 beta, IL-6, IL-10 and TNF-alpha measured at 3, 6 and 24 h. The results revealed that LPS alone increased secretion of each cytokine significantly. Treatment of the LPS-stimulated monocytes with gemifloxacin resulted in a significant inhibition (p < 0.01) of secretion of each of the cytokines from monocytes of the eight volunteers. Nuclear extracts of the human monocyte cell line, THP-1, were used in the electrophoretic mobility shift assay to determine whether gemifloxacin affects nuclear factor-kappa B (NF-kappa B) activation. In addition, RNA from THP-1 cells was used in Northern blots to determine whether inhibition of secretion of IL-1 beta and TNF-alpha by gemifloxacin occurred at the transcription or translation level. Whereas LPS induced a rapid increase in NF-kappa B activation, gemifloxacin alone did not. Gemifloxacin did not affect the kinetics or decrease the extent of activation. Northern blots indicated that the inhibitory activity of gemifloxacin occurred post-transcription. Thus, gemifloxacin may modulate the immune response by altering secretion of cytokines by human monocytes. Although the concentrations of gemifloxacin used were higher than those observed in the serum of human volunteers treated with the dose under clinical development, it should be taken into consideration that concentrations at tissue and intracellular levels may be considerably higher than serum concentrations.
Indications of Gemifloxacin
- Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB)
- Bacterial Infections
- Community-Acquired Pneumonia (CAP)
- Gonorrhea
- Multidrug-resistant Streptococcus pneumoniae infection
- Bacterial rhinosinusitis
- Bronchitis
- Pneumonia
- Strep Throat
Contra Indications of Gemifloxacin
- Acute Bacterial Exacerbation of Chronic Bronchitis
- Bacterial Infections
- Community-Acquired Pneumonia
- Gonorrhea
- Multidrug-resistant Streptococcus pneumoniae infection
- Bacterial rhinosinusitis
- Bronchitis
- Pneumonia
- Strep Throat
- For the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains ), M. pneumoniae, C. pneumoniae, or K. pneumoniae.
Dosage of Gemifloxacin
Strengths: 320 mg
Bronchitis
- 320 mg orally once a day for 5 days
Pneumonia
- 320 mg orally once a day
- Due to known/suspected S pneumoniae, H influenzae, Mycoplasma pneumoniae, or Chlamydophila pneumoniae infection: 5 days
- Due to known/suspected multi-drug resistant S pneumoniae (MDRSP), Klebsiella pneumoniae, or M catarrhalis infection: 7 days
Side Effects of Gemifloxacin
The most common side effects
- allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
- leukopenia/leukemia
- hemolytic anemia
- agranulocytosis
- pain, swelling, irritation where injected
- Abdominal pain
- sweating
- skin color change, mild diarrhea
- mild nausea
- loss of appetite
- vaginal discharge and itching
- swelling of feet or legs
- chest pain
- constipation
- cough
- diarrhea or loose stools
- difficulty with breathing
- dizziness
- heartburn
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- decreased amount of urine
Rare
- Anxiety
- change in vision
- seizures
- tremors
- weight loss
- chest pain or tightness
- confusion
- cough
- Agitation
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
Drug Interactions of Gemifloxacin
Gemifloxacin may interact with following drugs, supplements, & may change the efficacy of drugs
- antacids that contain aluminum, calcium, or magnesium
- birth control medications
- bismuth subsalicylate
- calcium supplements
- digoxin
- Rosuvastatin
- Duloxetine
- Albuterol
- Topiramate
- Carbamazepine
- Vitamin D3 (cholecalciferol)
- Alprazolam
- Cetirizine
- insulin
- iron supplements
- penicillin
- vitamin A derivatives (e.g. isotretinoin)
- warfarin
- zinc sulfate or gluconate
Pregnancy & Lactation of Gemifloxacin
FDA pregnancy category C
Pregnancy
This drug should not be used during pregnancy unless the benefit outweighs the risk to the fetus; safety has not been established during pregnancy.
Lactation
Cartilage erosion and arthropathy have been observed in immature animals giving rise to concern over toxic effects in the developing joints of nursing infants; however, some studies suggest the risk is low. Absorption of the small amounts of fluoroquinolones in milk may be blocked by the calcium in milk; data insufficient to prove or disprove. A nursing mother was administered a single 320 mg oral tablet. A single breast milk sample was collected 3 hours after dosing; milk drug level was about 0.9 mg/L.
References