CIPRO IN SODIUM CHLORIDE 0.9% IN PLASTIC CONTAINER
Clinical safety rating: safe
No significant drug interactions Can cause hypernatremia and fluid overload.
Ciprofloxacin inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby inhibiting DNA replication and transcription.
| Metabolism | Partially metabolized in the liver via CYP1A2 to four metabolites (desethylene-, sulfociprofloxacin, oxociprofloxacin, and formylciprofloxacin). |
| Excretion | Renal excretion accounts for approximately 50-70% of the dose as unchanged drug via glomerular filtration and tubular secretion. Additionally, about 15% is excreted as metabolites (oxo-ciprofloxacin, desethyleneciprofloxacin, sulfociprofloxacin). Biliary/fecal excretion accounts for 20-35%, primarily as unchanged drug and metabolites, with some enterohepatic recirculation. |
| Half-life | 3-5 hours in patients with normal renal function (creatinine clearance > 50 mL/min). In severe renal impairment (CrCl < 20 mL/min), half-life may extend to 6-8 hours. The terminal elimination half-life reflects the prolonged clearance of the drug from peripheral tissues such as skin and bone. |
| Protein binding | 20-40% bound to serum proteins, primarily albumin. Binding is concentration-independent and saturable at high doses ( > 400 mg), but clinically significant displacement interactions are rare due to low affinity. |
| Volume of Distribution | 2.5-3.0 L/kg. This large Vd indicates extensive tissue penetration with concentrations exceeding serum levels in kidney (2-3x), lung (2-3x), prostate (2x), and bone (1-2x). Penetration into cerebrospinal fluid is low (10-40% of serum levels) in non-inflamed meninges, but increases to 50-90% with inflammation. |
| Bioavailability | Intravenous: 100% bioavailability (administered as a 0.9% sodium chloride solution). Oral ciprofloxacin bioavailability is 70-80% but is not relevant for this IV formulation. |
| Onset of Action | Intravenous administration: Onset of action occurs within 1-2 hours post-infusion, with therapeutic serum concentrations achieved by the end of a 60-minute infusion. Time to clinical response varies by infection site (e.g., urinary tract: 12-24 hours; respiratory: 24-72 hours). |
| Duration of Action | Duration of action is 8-12 hours based on the dosing interval of 12 hours for most indications. The antimicrobial effect persists beyond the measured half-life due to post-antibiotic effect (PAE) of 1-2 hours against gram-negative bacteria. Continuous bactericidal activity requires maintaining serum concentrations above MIC throughout the dosing interval. |
400 mg IV every 8 hours for urinary tract infections; 400 mg IV every 12 hours for other infections. Infuse over 60 minutes.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 400 mg IV every 18-24 hours. CrCl 5-29 mL/min: 400 mg IV every 24 hours. CrCl <5 mL/min (on hemodialysis): 400 mg IV every 24 hours (administer after dialysis). |
| Liver impairment | No specific adjustment for hepatic impairment; systemic exposure may be increased but no dose guidelines established. |
| Pediatric use | Neonates (0-7 days): 10 mg/kg IV every 12 hours. Infants (8-28 days): 10 mg/kg IV every 8 hours. Children (1 month - 5 years): 10 mg/kg IV every 8 hours (max 400 mg/dose). Children (5-17 years): 10 mg/kg IV every 8 hours (max 400 mg/dose) for complicated infections; 6-10 mg/kg IV every 8 hours for uncomplicated infections. |
| Geriatric use | Adjust based on renal function (CrCl); no age-specific dose modifications. Monitor for CNS effects and tendon disorders. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Breastfeeding | Ciprofloxacin is excreted into human breast milk. The milk-to-plasma ratio is approximately 0.85. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Teratogenic Risk | Ciprofloxacin is generally avoided during pregnancy, especially in the first trimester, due to potential arthropathy in animal studies. Human data do not demonstrate a significant increase in major malformations, but there is a theoretical risk of fetal cartilage damage. Use only if benefit outweighs risk and no safer alternative exists. |
■ 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 over 60 years of age, those taking corticosteroids, and patients with kidney, heart, or lung transplants.
| Common Effects | fluid replacement |
| Serious Effects |
["Hypersensitivity to ciprofloxacin or any quinolone","Concomitant administration with tizanidine"]
| Precautions | ["Tendon damage, including rupture, can occur within hours or up to several months after therapy","Exacerbation of myasthenia gravis symptoms","Peripheral neuropathy that may be irreversible","Central nervous system effects including seizures, dizziness, and increased intracranial pressure","Clostridium difficile-associated diarrhea","Phototoxicity","QT prolongation","Hypersensitivity reactions, including anaphylaxis","Hepatotoxicity","Blood glucose disturbances, including hypoglycemia and hyperglycemia"] |
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| Fetal Monitoring | Monitor maternal renal function, hepatic function, and complete blood count periodically. In neonates or infants exposed in utero or via breast milk, monitor for signs of arthropathy or other adverse effects. Fetal monitoring includes ultrasonography as clinically indicated. |
| Fertility Effects | Ciprofloxacin has no known direct effects on human fertility. Animal studies have not shown impaired fertility at clinically relevant doses. |