CIPROFLOXACIN IN DEXTROSE 5% IN PLASTIC CONTAINER
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 inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby interfering with DNA replication, transcription, repair, and recombination.
| Metabolism | Ciprofloxacin is metabolized in the liver: approximately 30-50% of the dose is metabolized via CYP450 (isoenzymes not fully characterized), with four major metabolites (desethylene, sulfonyl, oxo, and N-formyl ciprofloxacin) exhibiting variable antibacterial activity. Approximately 40-50% of the administered dose is excreted unchanged in the urine via glomerular filtration and tubular secretion. |
| Excretion | Renal excretion accounts for approximately 50-70% of the dose as unchanged drug via glomerular filtration and tubular secretion; fecal excretion accounts for 15-25%, with about 20% as unchanged drug; biliary excretion contributes minimally (<5%). |
| Half-life | Terminal elimination half-life is 3.5-5 hours in patients with normal renal function. Clinically, this supports twice-daily dosing. In severe renal impairment (CrCl <30 mL/min), half-life may extend to 6-9 hours, requiring dose adjustment. |
| Protein binding | 20-40% bound to serum proteins, primarily albumin. |
| Volume of Distribution | 2-3 L/kg; high Vd indicates extensive tissue penetration, with concentrations in most tissues exceeding serum levels. |
| Bioavailability | Intravenous: 100% (complete). Ciprofloxacin is not administered orally via this formulation. |
| Onset of Action | IV infusion: Clinical effect typically observed within 1-2 hours after start of infusion, as drug rapidly achieves therapeutic concentrations in plasma and tissues. |
| Duration of Action | Duration of action is approximately 8-12 hours for susceptible organisms, supporting q12h dosing. Post-antibiotic effect (PAE) of 1-3 hours against Gram-negative bacteria may extend suppression. |
400 mg intravenously every 8 to 12 hours for most infections; 400 mg every 8 hours for severe/complicated infections.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 200-400 mg every 12 hours. CrCl <30 mL/min (including hemodialysis): 200-400 mg every 24 hours. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Limited data for severe impairment (Child-Pugh C); use with caution. |
| Pediatric use | For complicated urinary tract infections or pyelonephritis: 6-10 mg/kg IV every 8 hours (max 400 mg/dose). For inhalational anthrax: 10 mg/kg IV every 12 hours (max 400 mg/dose). For other indications per guidelines. |
| Geriatric use | No specific dose adjustment solely based on age; monitor renal function and adjust accordingly based on CrCl. Elderly patients may be at increased risk for tendonitis/tendon rupture and CNS effects. |
| 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 | Ciprofloxacin excreted into breast milk; M/P ratio approximately 0.9-1.3. Avoid breastfeeding due to risk of arthropathy in infant; alternative agents preferred. |
| Teratogenic Risk | Ciprofloxacin is contraindicated in pregnancy. Animal studies show arthropathy in juvenile animals. Human data: limited, but fluoroquinolones may cause cartilage damage in developing joints; risk highest in first trimester, but use is avoided throughout pregnancy. |
■ 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 older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart, or lung transplants. Fluoroquinolones may exacerbate muscle weakness in persons with myasthenia gravis. Avoid use in patients with known history of myasthenia gravis.
| Common Effects | Nausea |
| Serious Effects |
["Hypersensitivity to ciprofloxacin, any fluoroquinolone, or any component of the formulation","Concurrent administration with tizanidine (inhibition of CYP1A2 leading to increased tizanidine effects and toxicity)","Concurrent administration with other medications that prolong QT interval when not manageable"]
| Precautions | ["Tendinitis and tendon rupture","Peripheral neuropathy (irreversible sensorimotor polyneuropathy)","Central nervous system effects (seizures, dizziness, increased intracranial pressure, confusion)","Exacerbation of myasthenia gravis","Hypersensitivity reactions (including anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis)","Clostridioides difficile-associated diarrhea","Phototoxicity (increased risk in UV-exposed skin)","Risk of aortic aneurysm and dissection (reports of aortic rupture or dissection)","Blood glucose disturbances (hypoglycemia and hyperglycemia)","QT interval prolongation (avoid in patients with hypokalemia, known QTc prolongation, or concurrent use with Class IA or III antiarrhythmics)"] |
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| Fetal Monitoring | Monitor maternal renal function, liver function tests, and signs of tendonitis or neuropathy. No specific fetal monitoring required if inadvertent exposure, but document. |
| Fertility Effects | Ciprofloxacin does not appear to impair fertility in humans; animal studies show no significant effects on male or female fertility. |