FACTIVE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).
Gemifloxacin inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby interfering with DNA replication, transcription, repair, and recombination.
| 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. |
| Molecular Weight | 417.45 |
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. |
| 1st trimester | Avoid use; fluoroquinolones associated with arthropathy in immature animals and potential risk of tendon damage; limited human data suggest low teratogenic risk, but alternative agents preferred. |
| 2nd trimester | Avoid use; same concerns as first trimester; consider risk-benefit if no alternative. |
| 3rd trimester | Avoid use; potential for infantile musculoskeletal toxicity; avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for FACTIVE (FACTIVE).
| Placental transfer | Crosses placenta; concentrations in cord blood approximately 50-70% of maternal serum levels. |
| Breastfeeding | Drug excreted in breast milk in small amounts; risk of infant joint and tendon toxicity unknown; avoid breastfeeding or use alternative antibiotic. |
■ 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.
| Serious Effects |
History of tendon disorder/tendonitis with fluoroquinolone useMyasthenia gravisHypersensitivity to gemifloxacin or other fluoroquinolonesPediatric patients < 18 years (except in specific approved indications)
| 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 |
| Food/Dietary | Absorption is significantly reduced by concurrent intake of dairy products (milk, yogurt, cheese) or calcium-fortified juices. Also avoid antacids containing magnesium or aluminum, sucralfate, didanosine (chewable/buffered tablets), and multivitamins containing iron or zinc. Take gemifloxacin at least 2 hours before or 4 hours after these products. |
Loading safety data…
| Lactation Rating |
| Avoid |
| 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 | Monitor for maternal adverse effects (CNS, GI, tendonitis). Fetal ultrasound if inadvertent use in first trimester. No specific fetal monitoring required. |
| Fertility Effects | No human data on fertility impairment. Animal studies showed no effect on fertility or reproductive performance. |
| Clinical Pearls | Gemifloxacin (Factive) is a respiratory fluoroquinolone with enhanced activity against Streptococcus pneumoniae, including penicillin-resistant strains. It has a lower potential for phototoxicity compared to other fluoroquinolones but still caution is advised. Avoid use in patients with prolonged QT interval or those on antiarrhythmics. Adjust dose in renal impairment (CrCl <40 mL/min). |
| Patient Advice | Take exactly as prescribed, without missing doses. · Avoid taking with dairy products (milk, yogurt) or mineral supplements (calcium, iron, zinc) as they reduce absorption; separate by at least 2-4 hours. · Drink plenty of fluids to prevent crystalluria. · Report tendon pain or swelling immediately; avoid exercise if pain occurs. · Avoid excessive sunlight or tanning beds; use sunscreen and protective clothing. · May cause dizziness or lightheadedness; avoid driving until you know how you react. · Complete the full course even if you feel better. |