Ofloxacin and Levofloxacin
Drug

Difference Between Ofloxacin and Levofloxacin

Overview of Ofloxacin and Levofloxacin

Ofloxacin and Levofloxacin are fluoroquinolone antibiotics commonly prescribed to treat bacterial infections. Though both medications belong to the same class of medication, there may be key distinctions in terms of spectrum of activity, pharmacokinetics, side effects and clinical uses between them.

Ofloxacin has broad spectrum activity and can effectively combat numerous strains of bacteria – both Gram-negative and some Gram-positive strains alike – making it widely used to treat respiratory tract infections, urinary tract infections, gastrointestinal infections and certain sexually transmitted infections.

Levofloxacin offers greater spectrum activity compared to Ofloxacin. This antibiotic can effectively combat Gram-negative and Gram-positive bacteria alike – including rare pathogens like Mycoplasma and Legionella – making Levofloxacin often prescribed to treat respiratory tract infections, urinary tract infections, skin and soft tissue infections as well as certain forms of pneumonia.

Ofloxacin and Levofloxacin differ significantly when it comes to their absorption, distribution, and metabolism in the body. Levofloxacin typically offers better bioavailability; more people respond well to its oral use than its Ofloxacin equivalent and its longer half-life allows once daily dosing in most instances.

Both medications present similar adverse side effects, including gastrointestinal disturbances, central nervous system effects and tendon issues; however, specific side effects and their severity may differ between drugs.

Resistance patterns and susceptibility profiles also differ between Ofloxacin and Levofloxacin, due to longstanding bacteria strains becoming resistant. Prevalence varies based on your region as well as specific species involved; resistance rates will differ for both drugs.

Cost and availability can differ between Ofloxacin and Levofloxacin depending on both healthcare system and country; as their usage, cost, and accessibility affect patients’ decisions to use or access either medicine.

History of Ofloxacin

Ofloxacin is an equivalent of a second-generation fluoroquinolone. It is a broad-spectrum counterpart to norfloxacin. It was created and developed by scientists from Daiichi Seiyaku.

Ofloxacin
Figure 01: Ofloxacin

It first received approval for commercialization within Japan in 1985 for oral administration. Daiichi launched it under the brand trademark Tarvid. Daiichi in collaboration together with Johnson & Johnson, obtained FDA approval in December of 1990 with the brand label Floxin that was approved for adults suffering from respiratory tract infections of the lower part as well as skin and structures infections as well as urinary tract infections prostatitis and sexually transmitted diseases.

As of 1991, it had also been sold by Hoechst as Tarvid in the UK, Germany and Portugal; as Tarvid by Hoechst across the UK, Germany, Belgium and Portugal and as Oflocet across France, Portugal, Tunisia as well as several African countries, by the Roussel-Uclaf company. in the form of Oflocin from Glaxo in Italy as well as Flobacin in Italy by Sigma-Tau in Italy.

Ofloxacin’s market was considered to be difficult since its beginning. It was classified as an “1C” drug, a newly discovered molecular structure that offered very little or no benefit over the existing treatments, and the ciprofloxacin which was of more spectrum of use had already been in the marketplace.

In 1992 the year 1992, an intravenous solution had been authorized for use in marketing 

In 1997, a treatment for pelvic inflammation was accepted from the U.S. Food and Drug Administration (FDA) to use an oral preparation. In this same year an option for ear infection was approved under the name of .

Daiichi and J&J could also have a monopoly on its market when they introduced levofloxacin the levo-enantiomer for ofloxacin in 1996. Johnson & Johnson’s annual revenue from Floxin in 2003 was around $30 million. However, their combined sales of levaquin/floxin topped $1.15 billion that same year. Johnson & Johnson withdrew the marketing license in 2009.

History of Levofloxacin

Levofloxacin belongs to the third-generation fluoroquinolone and is among the isomers ofofloxacin which was a broad-spectrum one that was conformationally locked to norfloxacin. Both ofloxacin and the levofloxaxin derivatives were created and developed by scientists from Daiichi Seiyaku.

The Daiichi scientists were aware ofloxacin’s racemic nature However, they were unable to differentiate the two isomers and in 1985, they were able to synthesize the levo-pure form, and demonstrated that it was not as poisonous and much more potent over the second form. The levo form was more potent and less toxic. It first received approval for commercialization to Japan in 1993 to be administered orally, and Daiichi promoted it using the trade name Cravit.

The company Daiichi in collaboration together with Johnson & Johnson as it was a partner with ofloxacin, received FDA approval in the year 1996 under the name Levaquin for treating bacterial sinusitis and bacterial exacerbations of pneumonia acquired from community sources and skin infections that are not complicated, difficult urinary tract infections as well as acute pyelonephritis.

Levofloxacin is distributed through Sanofi-Aventis in a license agreement by Daiichi in 1993. It is marketed under the brand trademark “Tavanic”. Levofloxacin was a blockbuster at this point; the combined global sales of levofloxacin as well as ofloxacin J&J by themselves was US$1.6 billion in 2009.

Levofloxacin
Figure 02: Levofloxacin

The levofloxacin term in the United States patent was extended by the U.S. Patent and Trademark Office 810 days pursuant to the rules in the Hatch Waxman Amendment so that the patent was due to expire in the year 2010 rather than 2008.The extension was contested by the the generic drug maker Lupin Pharmaceuticals, which did not dispute the legitimacy of the patent.

They did challenge the validity of the extension of patent, saying that the patent didn’t encompass the definition of a “product” and so Hatch-Waxman wasn’t available to extensions.The Federal Patent judge ruled against J&J as well as Daiichi as well as generic versions of levofloxacin were not introduced to into the U.S. market until 2009.

Difference Between Ofloxacin and Levofloxacin

Here are difference between Ofloxacin and Levofloxacin:

1. Spectrum of Activity: Levofloxacin stands out in comparison with Ofloxacin due to its broadened spectrum of action against bacteria. Levofloxacin’s effectiveness against Gram-positive and Gram-negative strains as well as more uncommon pathogens like Mycoplasma and Legionella is greater, while Ofloxacin may still cover many bacterial strains but with limitations in coverage for certain strains.

2. Pharmacokinetics: Levofloxacin typically exhibits greater bioavailability and absorption compared to Ofloxacin. Furthermore, its longer half-life allows for once daily dosing; Ofloxacin may require multiple dosing regimens instead.

3. Clinical Applications: Although both drugs can treat bacterial infections, each has specific indications. Levofloxacin may be effective against respiratory tract Infections, urinary tract Infections, skin and soft tissue Infections as well as certain forms of pneumonia; while Ofloxacin typically treats respiratory tract infections as well as urinary tract infections, gastrointestinal infections as well as certain sexually transmitted infections.

4. Side Effects: Although both drugs share similar adverse reactions, their side effects and severity can differ considerably. Common fluoroquinolone side effects include gastrointestinal disturbances, central nervous system effects and tendon issues – though their frequency and intensity may differ between Ofloxacin and Levofloxacin.

5. Resistance and Susceptibility: Over time, bacteria strains have developed resistance to fluoroquinolone antibiotics like Ofloxacin and Levofloxacin. Their prevalence may differ between drugs as do their susceptibilities against different species; so when selecting an antibiotic it’s essential that local resistance patterns be considered when selecting your chosen treatment option.

6. Cost and Availability: Cost and availability can also differ significantly between Ofloxacin and Levofloxacin depending on factors like healthcare systems and geographic regions, with price/availability issues impacting usage/availability for patients.

Comparison Chart

Topic Ofloxacin Levofloxacin
Spectrum of Activity Effective against a wide range of Gram-negative and some Gram-positive bacteria Broader spectrum of activity, including Gram-negative, Gram-positive, and atypical pathogens
Pharmacokinetics Lower bioavailability and may require more frequent dosing Higher bioavailability, better absorption, and longer half-life, allowing for once-daily dosing
Clinical Uses Commonly used for respiratory tract infections, urinary tract infections, gastrointestinal infections, and certain sexually transmitted infections Prescribed for respiratory tract infections, urinary tract infections, skin and soft tissue infections, and certain types of pneumonia
Side Effects Similar adverse reactions, including gastrointestinal disturbances, central nervous system effects, and potential tendon-related issues Side effects may vary in frequency and severity
Resistance and Susceptibility May have limitations in coverage due to resistance in certain bacterial strains Broader coverage, but resistance patterns may vary
Cost and Availability Cost and availability may vary depending on healthcare systems and regions Cost and availability may vary depending on healthcare systems and regions

Conclusion

Ofloxacin and Levofloxacin are fluoroquinolone antibiotics with similar mechanisms of action, serving to block bacteria’s DNA synthesis by targeting DNA gyrase and topoisomerase IV enzymes, leading to disruptions of DNA replication and cell division for bacteria.

Though similar, both drugs offer differing activities, spectrum of activity, pharmacokinetics, side effects, resistance patterns and availability considerations when choosing an antibiotic treatment for specific infections; taking into account patient condition as well as susceptibilities present for bacteria involved.