Sitafloxacin (Gracevit) 10% granules, 30 g: profile, composition and research

Reference page for Sitafloxacin (Gracevit) 10% granules, 30 g. Active substance: Ситафлоксацин / Sitafloxacin.

Key facts

What sitafloxacin granules are

Sitafloxacin is a synthetic antibacterial substance of the fluoroquinolone class. It was developed in Japan, where it is used in clinical practice under the trade name Gracevit. It belongs to a later generation within the class: the molecule was designed to keep working against bacteria that had stopped responding to earlier fluoroquinolones.

In this pack the substance comes as granules. A 10% concentration means that one gram of granules contains 100 mg of the active substance. The granules are dissolved in water before use, and the pack holds 30 g in total. This form allows the dose to be measured more precisely than with a split tablet and suits patients who find swallowing tablets difficult.

The manufacturer is the Japanese company Daiichi Sankyo.

How it works

The targets

Sitafloxacin blocks two enzymes of the bacterial cell: DNA gyrase and topoisomerase IV. Both are needed to keep the shape of bacterial DNA correct while it is copied and the cell divides.

The result

With both enzymes switched off, the bacterium can no longer multiply and dies. The action is called bactericidal: the drug does not merely stop growth, it breaks the cell.

Resistance

For a bacterium to become insensitive to sitafloxacin, both target genes have to change at the same time. Two mutations coinciding is unlikely, so the substance often keeps its activity where other fluoroquinolones have already failed.

Activity spectrum

The drug covers a wide range of organisms: Gram-positive cocci such as pneumococcus and staphylococci, Gram-negative bacilli including Escherichia coli and other enterobacteria, and anaerobic microorganisms. Activity against anaerobes sets it apart from many other fluoroquinolones.

That is why sitafloxacin is considered for mixed infections in which aerobic and anaerobic bacteria are involved at the same time.

Approved uses

In Japan the substance is registered for bacterial infections of the respiratory tract, including community-acquired pneumonia and flare-ups of chronic bronchopulmonary disease, for complicated urinary tract infections, for infections of the ear, nose, throat and mouth, and for Buruli ulcer, caused by Mycobacterium ulcerans.

The list of indications and the treatment plan are set by a physician after examination. Giving an antibiotic without a confirmed bacterial infection makes no sense: fluoroquinolones do not act on viruses, including those behind the common cold.

Published research

Primary sources, verified against PubMed:

• Antibacterial Mechanisms and Clinical Impact of Sitafloxacin., PubMed 39598446 (Pharmaceuticals (Basel), 2024).
• A randomized, controlled, multicenter clinical trial to evaluate the efficacy and safety of oral sitafloxacin versus moxifloxacin in adult patients with community-acquired pneumonia., PubMed 33534617 (Curr Med Res Opin, 2021).
• The efficacy and safety of sitafloxacin and garenoxacin for the treatment of pneumonia in elderly patients: A randomized, multicenter, open-label trial., PubMed 31113725 (J Infect Chemother, 2019).

Listed for reference. Publication of a study is not a claim about this particular product.

Precautions

• This is a prescription medicine. Prescribing, dosing and monitoring belong to a physician.
• Fluoroquinolones may affect tendons, heart rhythm and the nervous system. Any unusual symptom during treatment should be reported to a doctor.
• Long exposure to the sun should be avoided during treatment: the skin may become more sensitive to ultraviolet light.
• In reduced kidney function the regimen is adjusted by a physician.
• Use during pregnancy or breastfeeding is discussed with a doctor individually.
• Tell your doctor about every other medicine you take: interactions are possible.

Frequently asked