CIPROFLOXACIN EXTENDED RELEASE
Clinical safety rating: caution
Chelates with divalent cations (antacids Ca2+ Fe2+) reducing absorption May enhance effects of warfarin Associated with tendonitis and tendon rupture.
Inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, preventing DNA replication, transcription, repair, and recombination.
| Metabolism | Metabolized in the liver primarily via CYP1A2, with minor routes via CYP3A4 and CYP2D6. Four metabolites identified: desethylene ciprofloxacin (M1), sulfociprofloxacin (M2), oxociprofloxacin (M3), and N-acetylciprofloxacin (M4). |
| Excretion | Primarily renal excretion (50-70% unchanged drug via glomerular filtration and tubular secretion); 15-25% metabolized; 20-35% fecal elimination via biliary secretion and intestinal epithelium. |
| Half-life | Terminal elimination half-life approximately 11 hours, ranging from 10-14 hours in patients with normal renal function. Prolonged in renal impairment; requires dose adjustment. |
| Protein binding | 20-40% bound to serum proteins (primarily albumin); binding is concentration-independent. |
| Volume of Distribution | Apparent Vd 2.0-3.5 L/kg indicating extensive tissue penetration; achieves concentrations in tissues and fluids exceeding serum levels. |
| Bioavailability | Oral extended-release: 70-80% relative to intravenous; food does not significantly affect absorption but delays Tmax. |
| Onset of Action | Oral extended-release: peak plasma concentrations at 1-4 hours; therapeutic effect begins within 2-4 hours post-dose. |
| Duration of Action | Duration approximately 24 hours due to extended-release formulation, allowing once-daily dosing. Clinical effect persists for the dosing interval. |
500-1000 mg orally once daily for 7-14 days; extended-release tablet must be taken whole with a meal.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | For CrCl 30-50 mL/min: 500-1000 mg every 24 hours. For CrCl 5-29 mL/min: 500 mg every 24 hours. For patients on hemodialysis or peritoneal dialysis: 500 mg every 24 hours (administer after dialysis). |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not FDA-approved for extended-release formulation in pediatric patients; use immediate-release formulations if needed. |
| Geriatric use | No specific dose adjustment solely due to age; consider renal function and adjust accordingly; monitor for QT prolongation and tendon adverse 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 is excreted into human breast milk with a milk-to-plasma ratio of approximately 0.9. The estimated infant dose is about 1-2% of the maternal weight-adjusted dose. The American Academy of Pediatrics considers ciprofloxacin compatible with breastfeeding, but caution is advised due to potential effects on the infant's gastrointestinal flora and theoretical risk of arthropathy. Monitoring the infant for diarrhea, rash, or candidiasis is recommended. |
■ FDA Black Box Warning
Fluoroquinolones, including ciprofloxacin, are associated with an increased risk of tendinitis and tendon rupture in all ages. Risk is further increased in patients >60 years, those taking corticosteroids, and those with kidney, heart, or lung transplants. Discontinue at first sign of tendon pain, swelling, or inflammation. Avoid use in patients with a history of tendon disorders related to fluoroquinolones.
| Common Effects | Nausea |
| Serious Effects |
["Hypersensitivity to ciprofloxacin, any other fluoroquinolone, or any component of the formulation","Use in children less than 18 years of age (except for specific approved indications)","Use with tizanidine (CYP1A2 inhibition leading to increased tizanidine levels and risk of hypotension/sedation)","Use in patients with known QT prolongation or concurrent use with QT-prolonging drugs"]
| Precautions | ["Exacerbation of myasthenia gravis","Central nervous system effects including convulsions, dizziness, and increased intracranial pressure","Peripheral neuropathy that may be irreversible","QT interval prolongation","Hypersensitivity reactions","Clostridium difficile-associated diarrhea","Blood glucose disturbances, especially in diabetic patients","Photosensitivity/phototoxicity","Avoid excessive sunlight/UV exposure","Crystalluria (maintain adequate hydration)","Use with caution in patients with known or suspected CNS disorders"] |
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| Teratogenic Risk |
| Fluoroquinolones, including ciprofloxacin, are generally avoided during pregnancy due to animal data showing arthropathy in immature animals. Human studies have not demonstrated a consistent increase in major malformations, but there is a potential risk of musculoskeletal adverse events (e.g., tendon damage) in the fetus. In the first trimester, the risk is low but not zero; in the second and third trimesters, the concern is primarily for fetal cartilage development and tendon integrity. Ciprofloxacin is classified as FDA Pregnancy Category C (prior to 2015) or risk factor based on current labeling: use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor for signs of tendonitis or tendon rupture in both mother and infant (if exposed in utero). Assess for gastrointestinal disturbances, rash, or hypersensitivity reactions. No specific fetal monitoring is required beyond routine prenatal care, but consider ultrasound for assessment of joint development if prolonged exposure occurs. |
| Fertility Effects | In animal studies, ciprofloxacin did not show adverse effects on fertility at clinically relevant doses. No human studies have indicated a significant impact on male or female fertility. However, as with all fluoroquinolones, caution is warranted in patients planning pregnancy due to limited data. |