PROQUIN XR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROQUIN XR (PROQUIN XR).
Fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV, preventing DNA replication and transcription.
| Metabolism | Hepatic metabolism via glucuronidation and sulfate conjugation; minor CYP450 involvement. |
| Excretion | Primarily renal excretion of unchanged drug (~60-80%) via glomerular filtration and tubular secretion. Biliary/fecal excretion accounts for approximately 20-35%, with a small portion as metabolites. |
| Half-life | Terminal elimination half-life is approximately 10-14 hours in patients with normal renal function (CrCl >80 mL/min). Extended half-life may occur in renal impairment, necessitating dose adjustment. |
| Protein binding | Approximately 30-40% bound to serum proteins (primarily albumin). Low protein binding minimizes displacement interactions. |
| Volume of Distribution | Volume of distribution is 1.7-2.5 L/kg, indicating extensive tissue penetration into lungs, prostate, and urinary tract tissues, exceeding plasma concentrations. |
| Bioavailability | Oral bioavailability is approximately 60-70% for the extended-release formulation, with food slightly increasing peak concentration (Cmax) but not overall AUC. |
| Onset of Action | Following oral administration of PROQUIN XR, therapeutic plasma concentrations are achieved within 1-2 hours. Peak concentrations occur around 6-8 hours due to extended-release formulation. |
| Duration of Action | Duration of antimicrobial activity is approximately 24 hours, allowing once-daily dosing. The extended-release design maintains effective plasma concentrations throughout the dosing interval. |
| Molecular Weight | 331.34 |
500 mg orally once daily with food.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | CrCl 30-50 mL/min: 500 mg every 48 hours; CrCl <30 mL/min: 500 mg every 72 hours; hemodialysis: 500 mg after each dialysis session. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Safety and efficacy not established in patients <18 years. |
| Geriatric use | Increased risk of QT prolongation and tendon rupture. Use lowest effective dose; monitor renal function and electrolytes. |
| 1st trimester | Avoid; risk of arthropathy and cartilage damage in animal studies. |
| 2nd trimester | Avoid; potential fetal cartilage damage. |
| 3rd trimester | Avoid; potential neonatal joint and tendon abnormalities. |
Clinical note
Comprehensive clinical and safety monograph for PROQUIN XR (PROQUIN XR).
| Placental transfer | Crosses placenta; fetal serum levels reach 50-70% of maternal levels. |
| Breastfeeding | Excreted into breast milk; potential for infant joint and tendon toxicity. Use only if benefit outweighs risk. |
| Lactation Rating | L4 (Hazardous) |
■ FDA Black Box Warning
Fluoroquinolones, including PROQUIN XR, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid use in patients with known history of myasthenia gravis.
| Serious Effects |
History of tendinopathy with fluoroquinolonesMyasthenia gravisHypersensitivity to ciprofloxacin or any fluoroquinoloneConcurrent tizanidine use
| Precautions | Tendonitis and tendon rupture; peripheral neuropathy; CNS effects including seizures; Clostridium difficile-associated diarrhea; photosensitivity; QT prolongation; renal impairment dose adjustment. |
| Food/Dietary | Avoid concurrent administration with dairy products (milk, yogurt) or calcium-fortified juices as they may reduce absorption. Take with a meal to minimize GI irritation but separate from calcium-rich foods by at least 2 hours. Avoid excessive caffeine intake as ciprofloxacin may increase caffeine effects. |
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| Teratogenic Risk | Fluoroquinolones including PROQUIN XR are generally avoided in pregnancy due to potential fetal cartilage damage observed in animal studies. First trimester risks include possible skeletal anomalies; second and third trimester risks involve arthropathy and possible CNS effects. Human data is limited but suggests no major malformation risk; however, use is not recommended due to safety concerns. |
| Fetal Monitoring | Monitor maternal renal function and liver enzymes. Fetal monitoring includes ultrasound for skeletal development if exposure occurs. Watch for maternal adverse effects like tendonitis, QT prolongation, and C. difficile infection. Newborn monitoring for joint or neurological symptoms if exposed near term. |
| Fertility Effects | Fluoroquinolones including PROQUIN XR have no established effects on human fertility. Animal studies show no impairment at clinically relevant doses. No specific data on ovarian or testicular function. |
| Clinical Pearls | PROQUIN XR (ciprofloxacin extended-release) is a fluoroquinolone antibiotic that achieves higher Cmax and similar AUC compared to immediate-release ciprofloxacin. Due to QT prolongation risk, avoid use in patients with electrolyte abnormalities, bradycardia, or concurrent QT-prolonging drugs. Monitor for tendinitis and tendon rupture, especially in patients over 60, on corticosteroids, or with renal impairment. Use with caution in myasthenia gravis due to neuromuscular blocking effects. Administer once daily with food to reduce GI upset; do not crush or split tablets. |
| Patient Advice | Take this medication once daily at the same time each day. · Swallow the tablet whole; do not crush, split, or chew it. · Drink plenty of fluids while taking this medication. · Avoid taking with dairy products (milk, yogurt) or calcium-fortified juices alone; take with a meal to minimize interaction. · Stop taking and contact your doctor immediately if you experience tendon pain or swelling, nerve symptoms (tingling, numbness), or rapid heartbeats. · This medication may cause dizziness or lightheadedness; avoid driving until you know how it affects you. · Complete the full course even if you feel better. |