CIPRO XR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CIPRO XR (CIPRO XR).
Ciprofloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV, thereby preventing DNA replication and transcription.
| Metabolism | Hepatic metabolism via CYP1A2, producing metabolites such as desethylene ciprofloxacin, sulfociprofloxacin, and oxociprofloxacin. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 40-50% of the dose; hepatic metabolism (glucuronidation, sulfation) produces active metabolites, and biliary/fecal elimination (via feces) accounts for 20-35% of the dose. |
| Half-life | Terminal elimination half-life is approximately 10-12 hours in patients with normal renal function, allowing twice-daily dosing; due to extended-release formulation, ciprofloxacin is released over 24 hours. |
| Protein binding | 20-40% bound to serum proteins (mainly albumin). |
| Volume of Distribution | Vd is 2.1-2.7 L/kg, indicating extensive tissue penetration including lung, skin, bone, and urogenital tissues. |
| Bioavailability | Oral (extended-release): 80-90% relative to intravenous ciprofloxacin; food does not significantly affect absorption but may increase time to peak concentration. |
| Onset of Action | Oral (extended-release): 1-2 hours to achieve therapeutic plasma concentrations; clinical effect typically within 24-48 hours. |
| Duration of Action | Duration is approximately 12-24 hours based on dosing interval (once daily for CIPRO XR); clinical effect persists while drug levels remain above MIC for susceptible pathogens. |
| Molecular Weight | 331.34 |
| Action Class | Quinolones/ Fluroquinolones |
| Brand Substitutes | Wocipflo 500mg Tablet, Strox 500mg Tablet, Ciprodac 500 Tablet, Alciflox 500mg Tablet, Cifran OD 500mg Tablet, Cyprine FC 250mg Tablet, Cyprine 250mg Tablet, Ciprokind 250mg Tablet, Floxip 250 Tablet, Ciprodac 250 Tablet |
500 mg to 1000 mg orally once daily for 7 to 14 days; extended-release tablet must be swallowed whole and administered with food.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | CrCl ≥ 30 mL/min: no adjustment; CrCl 5–29 mL/min: 500 mg orally once daily; CrCl < 5 mL/min or on hemodialysis: 500 mg orally once daily (administer after dialysis). |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A and B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not approved for use in pediatric patients under 18 years of age for most indications; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment based solely on age; dose selection should be cautious, reflecting greater frequency of decreased renal function. Monitor renal function and adjust dose accordingly. |
| 1st trimester | Ciprofloxacin is generally avoided in the first trimester due to potential cartilage damage in animal studies and rare cases of arthropathy in children. Use only if benefit outweighs risk and no alternative is available. |
| 2nd trimester | Use with caution; similar concerns as first trimester but some studies suggest lower risk. Reserve for serious infections when alternatives are not available. |
| 3rd trimester | Avoid near term due to potential adverse effects on fetal cartilage; consider alternative antibiotics if possible. If used, monitor infant for possible CNS effects. |
Clinical note
Comprehensive clinical and safety monograph for CIPRO XR (CIPRO XR).
| Placental transfer | Ciprofloxacin crosses the placenta. Studies show fetal concentrations approximately 30-50% of maternal serum levels. There is evidence of transfer in both animal and human studies. |
| Breastfeeding | Ciprofloxacin is excreted into breast milk. The concentration in milk is low, but due to potential for arthropathy and other adverse effects in nursing infants, it is typically avoided in breastfeeding women unless no safe alternative exists. Temporary cessation of breastfeeding during therapy may be considered. |
■ FDA Black Box Warning
CIPRO XR is 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, in patients taking corticosteroids, and in patients with kidney, heart, or lung transplants.
| Serious Effects |
Hypersensitivity to ciprofloxacin or any fluoroquinoloneConcurrent tizanidine administrationHistory of tendon disorders related to fluoroquinolone use
| Precautions | Fluoroquinolones, including Cipro XR, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid use in patients with known myasthenia gravis. May cause central nervous system effects including seizures, dizziness, and increased intracranial pressure. May cause peripheral neuropathy. May cause hypersensitivity reactions, including anaphylaxis. May cause Clostridium difficile-associated diarrhea. May cause phototoxicity. May cause QT prolongation. Avoid use in patients with known QT prolongation or electrolyte disturbances. |
| Food/Dietary | No clinically significant food interactions with CIPRO XR. However, avoid dairy products (milk, yogurt) or calcium-fortified juices when taking CIPRO XR, as these can bind the drug and reduce absorption if taken concurrently. Administer at least 2 hours before or 6 hours after consuming such foods. Caffeine intake should be limited as ciprofloxacin may decrease caffeine clearance, leading to increased nervousness or tachycardia. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) - use with caution; potential for adverse effects in infant. |
| Teratogenic Risk | Ciprofloxacin (CIPRO XR) is contraindicated in pregnancy. Based on human data, fluoroquinolones are associated with an increased risk of musculoskeletal disorders (arthropathy) in the fetus. First trimester exposure may carry a risk of spontaneous abortion. Second and third trimester exposure may lead to fetal cartilage damage and arthropathy. Animal studies show evidence of fetal harm (e.g., skeletal abnormalities) at clinically relevant doses. |
| Fetal Monitoring | Monitor for fetal distress (e.g., nonstress test, biophysical profile) if used near term. Assess for maternal adverse effects: tendinitis, tendon rupture, peripheral neuropathy, CNS effects (dizziness, seizures). Monitor renal function and fluid/electrolyte balance. In the neonate, observe for signs of arthropathy. |
| Fertility Effects | Ciprofloxacin has been associated with reversible reproductive toxicity in animal studies (e.g., decreased spermatogenesis, testicular atrophy). Human data on fertility effects are limited; however, it may transiently impair male fertility. No significant effects on female fertility have been reported. |
| Clinical Pearls | CIPRO XR (ciprofloxacin extended-release) is a fluoroquinolone antibiotic with enhanced activity against Gram-negative aerobes and atypical pathogens, but limited against anaerobes. Use cautiously in patients with known QTc prolongation, electrolyte disturbances, or those on antiarrhythmics due to risk of torsades de pointes. Avoid in tendonitis or tendon rupture history, especially in elderly, renal transplant, or concurrent steroid use. Administer once daily for uncomplicated urinary tract infections (UTIs); distinguish from immediate-release which requires twice-daily dosing. Monitor for signs of Clostridioides difficile infection, peripheral neuropathy, CNS effects (seizures, dizziness), and aortic aneurysm/dissection. May cause significant drug interactions with NSAIDs (increased CNS stimulation), theophylline (increased toxicity), and warfarin (INR elevation). Adjust dose in creatinine clearance <30 mL/min. |
| Patient Advice | Take this medication once daily at the same time each day, with or without food. · Swallow the tablet whole; do not crush, split, or chew the extended-release formulation. · Complete the full course of therapy even if symptoms improve; do not skip doses. · Avoid taking antacids, iron, zinc, calcium, or sucralfate within 2 hours before or 6 hours after CIPRO XR. · Drink plenty of fluids to prevent crystalluria and stay hydrated. · Contact your healthcare provider immediately if you experience tendon pain, swelling, or rupture; numbness or tingling; rapid or irregular heartbeat; severe diarrhea; or allergic reactions. · Avoid driving or operating heavy machinery until you know how this medication affects you, as it may cause dizziness or drowsiness. · Avoid excessive sunlight or UV rays; use sunscreen and protective clothing as this drug may increase sun sensitivity. |