CIPROFLOXACIN IN DEXTROSE 5%
Clinical safety rating: caution
Chelates with divalent cations (antacids Ca2+ Fe2+) reducing absorption May enhance effects of warfarin Associated with tendonitis and tendon rupture.
Ciprofloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby interfering with bacterial DNA replication, transcription, repair, and recombination.
| Metabolism | Ciprofloxacin is metabolized in the liver via hepatic CYP1A2 isoenzyme. Approximately 30-50% of an oral dose is metabolized to four metabolites: desethyleneciprofloxacin (M1, major), sulfociprofloxacin (M2), oxociprofloxacin (M3), and formylciprofloxacin (M4). The unchanged drug and metabolites are excreted primarily in urine via glomerular filtration and tubular secretion. |
| Excretion | Renal excretion accounts for approximately 50-70% of an administered dose as unchanged drug; biliary/fecal excretion accounts for about 20-35% (including active drug and metabolites). |
| Half-life | Terminal elimination half-life 3.5-5 hours in healthy adults, prolonged to 6-10 hours in elderly or mild renal impairment, and up to 12-24 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 20-40% bound to serum proteins (primarily albumin). |
| Volume of Distribution | Vd 2.5-3.5 L/kg, indicating extensive tissue penetration including lung, bone, and prostate. |
| Bioavailability | Oral: 70-80% (with minimal food effect); intravenous: 100%. |
| Onset of Action | Intravenous: immediate (upon completion of infusion); oral: 0.5-2 hours to reach therapeutic serum concentrations. |
| Duration of Action | Duration approximately 12 hours based on dosing interval; antibacterial activity persists for 6-12 hours post-dose depending on pathogen susceptibility. |
400 mg IV every 8 hours.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 200-400 mg IV every 12 hours; CrCl 5-29 mL/min: 200-400 mg IV every 18-24 hours; hemodialysis or peritoneal dialysis: 200-400 mg IV every 24 hours (administer after dialysis). |
| Liver impairment | No dose adjustment required for Child-Pugh A or B; severe hepatic impairment (Child-Pugh C): no specific guidelines, use caution and monitor for adverse effects. |
| Pediatric use | 10-20 mg/kg IV every 8 hours; maximum single dose 400 mg; not recommended for children <1 year unless benefit outweighs risk. |
| Geriatric use | No specific dose adjustment based on age alone; adjust according to renal function; monitor for CNS effects (e.g., dizziness, confusion) and tendon disorders. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Chelates with divalent cations (antacids Ca2+ Fe2+) reducing absorption May enhance effects of warfarin Associated with tendonitis and tendon rupture.
| FDA category | Animal |
| Breastfeeding | Excreted into breast milk (M/P ratio ~0.8-2.2). Theoretical risk of arthropathy in infant. Use caution; alternative preferred. The American Academy of Pediatrics considers use compatible with breastfeeding, but avoid in nursing mothers with other options. |
| Teratogenic Risk |
■ FDA Black Box Warning
Fluoroquinolones, including ciprofloxacin, are associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in patients older than 60 years, in those taking corticosteroids, and in patients with kidney, heart, or lung transplants. Additionally, fluoroquinolones may exacerbate muscle weakness in individuals with myasthenia gravis. Avoid use in patients with a history of myasthenia gravis.
| Common Effects | Nausea |
| Serious Effects |
["Hypersensitivity to ciprofloxacin, any fluoroquinolone, or any component of the formulation","Concurrent use with tizanidine (CYP1A2 inhibitor effect)"]
| Precautions | ["Risk of tendinitis and tendon rupture","Exacerbation of myasthenia gravis","Nervous system effects including seizures, dizziness, confusion, tremors, hallucinations, depression, and suicidal thoughts/behaviors","Peripheral neuropathy that may be irreversible","Clostridium difficile-associated diarrhea","Prolongation of QT interval and risk of cardiac arrhythmias","Photosensitivity/phototoxicity reaction","Hypersensitivity reactions including anaphylaxis and Stevens-Johnson syndrome","Superinfection with resistant organisms or fungal overgrowth","Hepatotoxicity including severe liver injury","Renal impairment requiring dose adjustment","Blood glucose disturbances especially in diabetic patients"] |
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| Contraindicated in pregnancy. Fluoroquinolones cause arthropathy in juvenile animals. Human data limited; avoid during first trimester if possible. Second/third trimester: use only if no safer alternative. Risk of fetal cartilage damage, although not confirmed in humans. |
| Fetal Monitoring | Monitor maternal renal function, liver enzymes, and signs of tendonitis/rupture. Monitor neonatal for diarrhea, rash, or signs of C. difficile infection if exposed near term. |
| Fertility Effects | No known adverse effects on fertility in humans. Animal studies show no impairment. |