FACTIVE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).

How it works

Gemifloxacin inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby interfering with DNA replication, transcription, repair, and recombination.

What the body does with it

Metabolism	Gemifloxacin is partially metabolized in the liver, primarily via glucuronidation and oxidation. The major metabolites are O-desmethyl gemifloxacin and gemifloxacin glucuronide. CYP450 involvement is minimal.
Excretion	Renal excretion of unchanged drug accounts for approximately 61% of the administered dose; fecal elimination accounts for about 35%, with a minor biliary component.
Half-life	12.5 hours (range 10-16 hours), supporting once-daily dosing.
Protein binding	~45% bound to serum proteins (primarily albumin).
Volume of Distribution	3.0 L/kg, indicating extensive tissue penetration.
Bioavailability	75% oral bioavailability (tablet).
Onset of Action	Oral: clinical improvement typically observed within 24-48 hours.
Duration of Action	24 hours, consistent with once-daily dosing interval.

Classification & Brands

Dosing & administration

400 mg orally once daily for 5 days for acute exacerbation of chronic bronchitis; 400 mg orally once daily for 7 days for community-acquired pneumonia; 400 mg orally once daily for 5 days for acute bacterial sinusitis.

Dosage form	TABLET
Renal impairment	For CrCl 40-80 mL/min: no adjustment; CrCl <40 mL/min: not recommended; hemodialysis or peritoneal dialysis: not recommended.
Liver impairment	No adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B); not studied in severe impairment (Child-Pugh C).
Pediatric use	Safety and efficacy not established in pediatric patients (<18 years); not recommended due to increased risk of adverse events.
Geriatric use	No dose adjustment based on age alone; monitor renal function and adjust dose if CrCl <40 mL/min per renal adjustment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).

Breastfeeding	Excreted in breast milk; M/P ratio unknown. Avoid breastfeeding or use alternate drug due to potential arthropathy in infant. Consider discontinuing nursing or drug.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: No adequate studies; potential risk based on animal studies (skeletal malformations). Second and third trimesters: Avoid due to risk of fetal cartilage damage and arthropathy (fluoroquinolone class effect). Use only if benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Fluoroquinolones, including gemifloxacin, have been associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in patients older than 60 years of age, in patients taking corticosteroids, and in patients with kidney, heart, or lung transplants.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to gemifloxacin or any fluoroquinolone","History of tendinopathy or tendon rupture with fluoroquinolone use","Use in children under 18 years of age (except for specific infections)","Use in pregnant or nursing women unless benefit outweighs risk","Concurrent use with class IA or III antiarrhythmics (relative)"]

Clinical Precautions

Precautions

["Tendon effects (tendinitis, tendon rupture)","Exacerbation of myasthenia gravis","QT prolongation and arrhythmias","Peripheral neuropathy","Central nervous system effects including seizures and increased intracranial pressure","Photosensitivity/phototoxicity","Hypersensitivity reactions including anaphylaxis","Clostridioides difficile-associated diarrhea","Blood glucose disturbances","Renal impairment dose adjustment","Avoid use in patients with known aortic aneurysm or at risk"]

Clinical Tips & Counseling

Drug interactions

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FACTIVE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).

How it works

Gemifloxacin inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby interfering with DNA replication, transcription, repair, and recombination.

What the body does with it

Metabolism	Gemifloxacin is partially metabolized in the liver, primarily via glucuronidation and oxidation. The major metabolites are O-desmethyl gemifloxacin and gemifloxacin glucuronide. CYP450 involvement is minimal.
Excretion	Renal excretion of unchanged drug accounts for approximately 61% of the administered dose; fecal elimination accounts for about 35%, with a minor biliary component.
Half-life	12.5 hours (range 10-16 hours), supporting once-daily dosing.
Protein binding	~45% bound to serum proteins (primarily albumin).
Volume of Distribution	3.0 L/kg, indicating extensive tissue penetration.
Bioavailability	75% oral bioavailability (tablet).
Onset of Action	Oral: clinical improvement typically observed within 24-48 hours.
Duration of Action	24 hours, consistent with once-daily dosing interval.

Classification & Brands

Dosing & administration

Dosage form	TABLET
Renal impairment	For CrCl 40-80 mL/min: no adjustment; CrCl <40 mL/min: not recommended; hemodialysis or peritoneal dialysis: not recommended.
Liver impairment	No adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B); not studied in severe impairment (Child-Pugh C).
Pediatric use	Safety and efficacy not established in pediatric patients (<18 years); not recommended due to increased risk of adverse events.
Geriatric use	No dose adjustment based on age alone; monitor renal function and adjust dose if CrCl <40 mL/min per renal adjustment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).

Breastfeeding	Excreted in breast milk; M/P ratio unknown. Avoid breastfeeding or use alternate drug due to potential arthropathy in infant. Consider discontinuing nursing or drug.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: No adequate studies; potential risk based on animal studies (skeletal malformations). Second and third trimesters: Avoid due to risk of fetal cartilage damage and arthropathy (fluoroquinolone class effect). Use only if benefit outweighs risk.
Fetal Monitoring