Gemifloxacin

Gemifloxacin

Gemifloxacin mesylate is a synthetic broad spectrum antibacterial for oral administration. Gemifloxacin a compound related to the fluoroquinolone class of antibiotics is available as the mesylate salt in the sesquihydrate form.
Mode of action

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.
Pharmacokinetics

Gemifloxacin is rapidly absorbed from the gastrointestinal tract with absolute bioavailability of about 71%. Peak plasma concentrations occur 0.5 to 2 hours after an oral dose. Gemifloxacin is widely distributed into body tissues including the bronchial mucosa and lungs, and is about 55 to75% bound to plasma proteins. It undergoes limited hepatic metabolism and has an elimination half life of about 7 hours. It excreted as unchanged drug and metabolites in the faeces and urine. Urinary excretion is by active tubular secretion and is reduce by probenecid. Distribution into milk has been found in rats.
Indications
Gemifloxacin is indicated for the treatment of infections caused by susceptible of the designated microorganisms in the condition listed below.
• Acute bacterial exacerbation of chronic bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, or Moraxella catarrhalis.
• Community-acquired pneumonia (of mild to moderate severity) caused by Streptococcus pneumonia (including multi- drug resistant strains [MDRSP]), Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamybia pneumoniae, or Klebsiella pneumoniae.
• Acute sinusitis
• Uncomplicated urinary tract infections
• Acute pyelonephritis

Contraindication

Gemifloxacin is contraindicated in patients with a history of hypersensitivity to gemifloxacin, floroquinolone antibiotic agents, or any of the product components.
Use in pregnancy and Lactation
There are no adequate and well-controlled studies in pregnant women. Reports of arthropathy (observed in immature animals and reported rarely in humans) have limited the use of fluoroquinolones in pregnancy. Reversible fatal growth retardation was observed with gemifloxacin in some animal studies. Based on limited data, quinolones are not expected to be a major human teratogen. Although quinolone antibiotics should not be used as first-line agents during pregnancy, when considering treatment for life-threatening infection and/or prolonged duration of therapy, the potential risk to the fetus must be balanced against the severity of the potential illness. Excretion in breast milk is unknown. So, Gemifloxacin is not recommended in lactating women.
Side Effect
There are many serious side effects of Gemifloxacin:

1. fast or pounding heartbeats
2. feeling light-headed, fainting, drowsiness, dizziness
3. seizure (convulsions)
4. confusion, and feeling restless or anxious
5. a red, blistering, peeling skin rash, vaginal itching or discharge & mild skin itching
6. urinating less than usual or not at all
7. tremors or shaking
8. easy bruising or bleeding, unusual weakness
9. nausea, vomiting, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
10. sudden pain or swelling near your joints (especially in your arm or ankle)
11. numbness, tingling, or weakness in any part of your body
12. diarrhea that is watery or bloody


Drug Interaction

May interact with blood thinners (e.g. warfarin), corticosteroids (e.g. prednisone), diabetes medications (e.g. insulin), probenecid, live vaccines. Report the use of drug which might increase seizure risk (decrease seizure threshold) when combined with Gemifloxacin such as phenothiazines (e.g. thioridazine), tricyclic antidepressants (e.g. amitriptyline), isoniazid (INH) or theophylline.


Except those drugs more over have another drugs which are interact with previous mentions drugs:

• Nonsteroidal anti-inflammatory drugs (NSAIDs)
• Medications for heart arrhythmias
• Erythromycin
• Antipsychotics
• Water pills
• Steroid medications
• Antacids
• Sucralfate

• Didanosine
Gemifloxacin may interact with other medications or substances that are not listed above. In order to avoid potentially hazardous interactions, patients should talk with their doctor about the use of any other medicines, vitamins or supplements before beginning treatment with gemifloxacin.
Precautions
• Before taking Gemifloxacin, caution should be taken if you are allergic or have had a severe reaction to gemifloxacin or any other quinolone or fluoroquinolone antibiotics such as ciprofloxacin, gatifloxacin, levofloxacin, lomefloxacin , moxifloxacin; any other medications.
• You are taking antacids containing aluminum hydroxide or magnesium hydroxide or vitamin or mineral supplements that contain iron, magnesium, or zinc, take these medications 3 hours before or 2 hours after you take gemifloxacin.
• Before using this medication, tells your doctor about rain or nervous system disorder if any (e.g. Cerebral arteriosclerosis, tumors increased intracranial pressure), heart problems (e.g. Cardiomyopathy, slow heart rate, QTc prolongation), history of seizures kidney disease, muscle/joint/tendon problems.
• Gemifloxacin may make your skin sensitive to sunlight or ultraviolet light. So avoid prolong sun exposure.
• This medication should be used only when clearly needed during pregnancy. Consult your doctor before breast feeding.
Overdosage
Any signs or symptoms of overdosage should be treated symptomatically. No specific antidote is known. In the event of acute oral overdosage, the stomach should be emptied by inducing vomiting or by gastric lavage; the patient should be carefully observed and treated symptomatically with appropriate hydration maintained. Hemodialysis removes approximately 20 to 30% of an oral dose of gemifloxacin from plasma.
Mortality occurred at oral gemifloxacin doses of 1600 mg/kg in rats and 320 mg/kg in mice. The minimum lethal intravenous doses in these species were 160 and 80 mg/kg, respectively. Toxic signs after administration of a single high oral dose (400 mg/kg) of gemifloxacin to rodents included ataxia, lethargy, piloerection, tremor, and clonic convulsions.