Gemifloxacin mesylate

Gemifloxacin mesylate
INN
Drug class
Routes of administration	Oral
Pregnancy category
Bioavailability	71%
Metabolism	Hepatic (minimal)
Elimination half-life	7 hours
Excretion	Renal (61%)
Legal status
CAS Number	210353-53-0
PubChem	151164
DrugBank	DB01155
ChemSpider	133224
KEGG	D04066

Gemifloxacin Mesylate is a fluoroquinolone antibiotic used in the treatment of bacterial infections. It is marketed under the brand name Factive.

Pharmacology

Gemifloxacin is a broad-spectrum antibiotic that is effective against a variety of Gram-positive and Gram-negative bacteria. It works by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes critical for DNA replication and transcription.

Mechanism of Action

Gemifloxacin targets the bacterial enzymes DNA gyrase and topoisomerase IV. These enzymes are essential for maintaining the supercoiling of bacterial DNA, which is necessary for DNA replication and transcription. By inhibiting these enzymes, gemifloxacin disrupts DNA processes, leading to bacterial cell death.

Pharmacokinetics

Gemifloxacin is administered orally and has a bioavailability of approximately 71%. It is moderately bound to plasma proteins (60-70%) and has a half-life of about 7 hours. The drug is minimally metabolized in the liver and is primarily excreted via the kidneys.

Clinical Uses

Gemifloxacin is indicated for the treatment of several types of bacterial infections, including:

• Acute bacterial exacerbation of chronic bronchitis
• Community-acquired pneumonia

Adverse Effects

Common adverse effects of gemifloxacin include:

• Nausea
• Diarrhea
• Rash
• Headache

Serious adverse effects may include:

• Tendonitis and tendon rupture
• QT interval prolongation
• Hypersensitivity reactions

Contraindications

Gemifloxacin is contraindicated in patients with a history of hypersensitivity to gemifloxacin or other fluoroquinolones. It should be used with caution in patients with a history of seizures or QT prolongation.

Drug Interactions

Gemifloxacin may interact with:

• Antacids containing magnesium or aluminum
• Sucralfate
• Iron supplements
• Multivitamins containing zinc

These substances can interfere with the absorption of gemifloxacin, reducing its effectiveness.

Special Populations

Pregnancy and Lactation

Gemifloxacin is classified as pregnancy category C in the United States, indicating that risk to the fetus cannot be ruled out. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Pediatric Use

The safety and effectiveness of gemifloxacin in pediatric patients have not been established.

Conclusion

Gemifloxacin Mesylate is a potent fluoroquinolone antibiotic with a broad spectrum of activity against various bacterial pathogens. It is primarily used in the treatment of respiratory tract infections. As with all antibiotics, it is important to use gemifloxacin judiciously to prevent the development of antibiotic resistance.