ZAGAM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZAGAM (ZAGAM).
Sparfloxacin, a fluoroquinolone antibiotic, inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby blocking DNA replication and transcription.
| Metabolism | Sparfloxacin is metabolized primarily via glucuronidation by UGT1A1 and UGT1A9; minor metabolism by CYP3A4. |
| Excretion | Renal: 60-80% unchanged; biliary/fecal: 10-20% |
| Half-life | 10-12 hours; prolonged in renal impairment |
| Protein binding | 25% bound to serum proteins |
| Volume of Distribution | 1.5-2.0 L/kg; indicates extensive tissue penetration |
| Bioavailability | Oral: 95-100% |
| Onset of Action | Oral: 1-2 hours |
| Duration of Action | 12 hours; sustained by post-antibiotic effect |
| Molecular Weight | 416.46 |
600 mg intravenously once daily or 600 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | CrCl 30–49 mL/min: 400 mg IV or oral once daily; CrCl 15–29 mL/min: 300 mg IV or oral once daily; CrCl <15 mL/min or hemodialysis: 200 mg IV or oral once daily. |
| Liver impairment | No dose adjustment required for mild or 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. |
| Geriatric use | No specific dose adjustment required; monitor renal function and adjust dose based on CrCl as per renal adjustment guidelines. |
| 1st trimester | Avoid use in first trimester; animal studies show teratogenic effects (arthropathy). |
| 2nd trimester | Use only if benefit outweighs risk; potential for fetal articular cartilage damage. |
| 3rd trimester | Avoid use in third trimester due to risk of fetal cartilage damage and neonatal joint toxicity. |
Clinical note
Comprehensive clinical and safety monograph for ZAGAM (ZAGAM).
| Placental transfer | Crosses placenta; concentrations in cord blood approximately 50% of maternal serum. |
| Breastfeeding | Excreted into breast milk in small amounts; potential for gastrointestinal disturbance and cartilage toxicity in infant. Use caution, especially in mothers of infants with renal impairment. |
| Lactation Rating |
■ FDA Black Box Warning
Fluoroquinolones, including sparfloxacin, have been associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in older patients (>60 years), patients taking corticosteroids, and patients with kidney, heart, or lung transplants.
| Serious Effects |
Hypersensitivity to sparfloxacin or any fluoroquinoloneHistory of tendon disorders with fluoroquinolone useProlonged QT intervalConcurrent use with drugs that prolong QT interval (e.g., class IA/III antiarrhythmics)Children under 18 years (except specific indications)Epilepsy or history of seizuresG6PD deficiency (increased risk of hemolytic reactions)Pregnancy (contraindicated in all trimesters)
| Precautions | QT prolongation: sparfloxacin prolongs the QT interval; avoid in patients with known QT prolongation, electrolyte disturbances, or those taking other QT-prolonging drugs., Photosensitivity: sparfloxacin is associated with significant phototoxicity; patients should avoid excessive sunlight and UV exposure., Tendon damage: risk of tendinitis and tendon rupture, especially in older patients and those on corticosteroids., Peripheral neuropathy: may cause irreversible neuropathy; discontinue if symptoms occur., CNS effects: may cause dizziness, confusion, and increased risk of seizures; use caution in patients with CNS disorders. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | Fluoroquinolones, including ZAGAM, are generally avoided in pregnancy due to arthropathy risk in immature animals; however, human data are limited. First trimester: no clear evidence of major malformations from limited cohort studies. Second and third trimesters: potential risk of fetal cartilage damage based on animal studies; avoid unless no safer alternative. |
| Fetal Monitoring | Monitor for maternal adverse effects: QT prolongation (ECG monitoring if other risk factors), photosensitivity, tendonitis, and gastrointestinal disturbances. Fetal monitoring: ultrasound for fetal growth and joint development if exposure occurs during second/third trimester. |
| Fertility Effects | Animal studies have not demonstrated impaired fertility. No human data on fertility impact; fluoroquinolones are not known to adversely affect human reproductive function. |
| Food/Dietary | Sparfloxacin absorption is significantly reduced by calcium-containing foods and supplements. Avoid concurrent intake of dairy products (milk, yogurt, cheese), calcium-fortified juices, and antacids containing calcium. Separate administration by at least 2 hours before or 4 hours after these products. Grapefruit juice may increase QT prolongation risk; avoid concurrent use. No significant interaction with caffeine or alcohol, but alcohol may exacerbate CNS effects. |
| Clinical Pearls | ZAGAM (sparfloxacin) is a fluoroquinolone antibiotic with enhanced activity against respiratory pathogens, including Streptococcus pneumoniae and atypical organisms. Due to QT prolongation risk, avoid in patients with hypokalemia, bradycardia, or concurrent use of Class IA/III antiarrhythmics. Photosensitivity is common; avoid sun exposure during therapy and for 5 days after discontinuation. Monitor for tendonitis and Achilles tendon rupture, especially in patients over 60, those on corticosteroids, and renal transplant recipients. |
| Patient Advice | Take this medication exactly as prescribed; do not skip doses or double up on missed doses. · Avoid prolonged sun exposure and use sunblock (SPF 30+) and protective clothing while taking this drug and for 5 days after stopping, as severe sunburn may occur. · Report any tendon pain, swelling, or rupture symptoms (e.g., popping sound, inability to move joint) immediately, especially in the Achilles tendon. · Notify your doctor if you experience palpitations, fainting, or irregular heartbeats; this drug can affect heart rhythm. · Avoid driving or operating heavy machinery if you experience dizziness or vision changes. · Do not take this medication with dairy products (milk, yogurt, cheese) or calcium-fortified juices; take with a full glass of water at least 2 hours before or 4 hours after consuming these. |