Ofloxacin

Ofloxacin is a second-generation fluoroquinolone primarily known for its role in treating mild-to-moderate bacterial infections. While once extensively used in systemic therapies, it has since witnessed a decline due to the advent of more efficacious and safer fluoroquinolones. In contemporary medical settings, ofloxacin finds prominence primarily as a topical agent for ocular and otic applications.

Ofloxacin

Ofloxacin zwitterion ball

Mechanism of Action

The therapeutic efficacy of ofloxacin can be attributed to its potent antimicrobial activity against a wide spectrum of aerobic gram-positive and gram-negative pathogens. Its underlying mechanism centers on the inhibition of type II DNA topoisomerases, specifically DNA gyrase and topoisomerase IV. These enzymes are pivotal for bacterial DNA replication, recombination, and repair. By curbing their function, ofloxacin impedes bacterial DNA synthesis, leading to cell death.

Liver Safety

An important facet of ofloxacin's safety profile is its hepatotoxic potential. While rare, there have been reported instances where ofloxacin intake has precipitated acute hepatocellular injury.

FDA Approval and Availability

In 1990, the U.S. Food and Drug Administration (FDA) greenlit ofloxacin for therapeutic use. However, by 2009, its initial sponsor opted to discontinue its production, driven in part by concerns over its adverse effects. Despite this, several generic versions of the drug, available in 200, 300, and 400 mg tablet formulations, remain in circulation.

Clinical Indications

Ofloxacin has been indicated for a myriad of conditions including:

• Acute bronchitis
• Community-acquired pneumonia
• Skin infections
• Cystitis
• Pelvic inflammatory disease
• Prostatitis
• Urethritis
• Gonorrhea

Dosage and Administration

The drug is typically prescribed in doses ranging from 200 to 400 mg, administered every 12 hours. While a treatment duration of 3 to 10 days is common, more protracted courses may be necessary for intricate or recurrent infections.

Adverse Effects

Ofloxacin's side effect profile encompasses:

• Common Adverse Effects: These can include gastrointestinal disturbances, headaches, skin rashes, and allergic manifestations.
• Severe Adverse Effects: Though infrequent, ofloxacin can elicit significant side effects such as QT interval prolongation, seizures, hallucinatory experiences, tendon ruptures, heightened photosensitivity, and hypersensitivity reactions.

Concluding Remarks

While ofloxacin was once a mainstay in the systemic management of various bacterial infections, its role has evolved, with current applications being predominantly topical. Its use has been curtailed due to concerns regarding its safety and the development of more advanced fluoroquinolones.

List of flouroquinolones

• Ciprofloxacin
• Delafloxacin
• Gemifloxacin
• Levofloxacin
• Moxifloxacin
• Norfloxacin
• Ofloxacin

• Dailymed label info on Ofloxacin
• FDA Ofloxacin

Ofloxacin Resources
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