CINOBAC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CINOBAC (CINOBAC).
Cinobufagin, a bufadienolide from toad venom, inhibits Na+/K+-ATPase, leading to increased intracellular calcium, and also induces apoptosis via caspase activation and modulation of signal transduction pathways including PI3K/Akt and MAPK.
| Metabolism | Primarily hepatic, metabolized via cytochrome P450 enzymes (e.g., CYP3A4) and conjugation reactions. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 85-90% of elimination, with 10-15% metabolized hepatically to inactive glucuronide conjugates excreted in urine. Less than 2% is eliminated in feces via biliary excretion. |
| Half-life | Terminal elimination half-life is approximately 1.5-2 hours in patients with normal renal function; may be prolonged up to 8-12 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 15-25% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.2-0.3 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Oral bioavailability is 70-80% when administered on an empty stomach; food reduces bioavailability by approximately 20%. |
| Onset of Action | Oral administration: Onset of action occurs within 30-60 minutes for antibacterial effect; peak serum concentrations achieved in 1-2 hours. |
| Duration of Action | Duration of antibacterial action is approximately 6-8 hours based on serum levels above MIC for susceptible organisms; clinical duration of therapy is 7-14 days depending on infection severity. |
| Molecular Weight | 250.25 |
250 mg orally twice daily for 7-14 days
| Dosage form | CAPSULE |
| Renal impairment | CrCl 30-50 mL/min: 250 mg every 24 hours; CrCl <30 mL/min: contraindicated |
| Liver impairment | No adjustment required for mild to moderate impairment; severe impairment: use with caution, monitor closely |
| Pediatric use | Children ≥12 years: 250 mg orally twice daily; <12 years: safety not established |
| Geriatric use | Consider renal function; may require lower dose due to age-related decline in GFR |
| 1st trimester | Contraindicated due to risk of fetal harm; animal studies show teratogenic effects. |
| 2nd trimester | Contraindicated; no adequate human studies, potential fetal toxicity. |
| 3rd trimester | Contraindicated; risk of neonatal toxicity (e.g., kernicterus due to bilirubin displacement). |
Clinical note
Comprehensive clinical and safety monograph for CINOBAC (CINOBAC).
| Placental transfer | Crosses placenta; documented in human studies. |
| Breastfeeding | Excreted into breast milk; potential for serious adverse reactions in nursing infants (e.g., hemolysis in G6PD deficiency). Not recommended. |
| Lactation Rating |
■ FDA Black Box Warning
Not applicable; not FDA-approved.
| Serious Effects |
Hypersensitivity to cinobac or any quinoloneHistory of tendon disorders with quinolone usePregnancyBreastfeedingChildren and adolescents (<18 years) due to arthropathy riskGlucose-6-phosphate dehydrogenase deficiency
| Precautions | Cardiotoxicity (arrhythmias, digitalis-like effect), Hepatotoxicity, Nephrotoxicity, Electrolyte disturbances (hyperkalemia), Risk of fatal overdose due to narrow therapeutic index |
| Food/Dietary | Do not take with dairy products (milk, yogurt, cheese) or calcium-fortified juices as they chelate and reduce absorption. Separate cinoxacin administration from any calcium-containing foods, antacids, sucralfate, iron or zinc supplements by at least 2 hours. Avoid caffeine; cinoxacin may increase caffeine effects. Grapefruit and grapefruit juice may alter drug metabolism; avoid concurrent use. |
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| L5 - Contraindicated |
| Teratogenic Risk | No data available on teratogenic risk in humans; animal studies insufficient. Avoid in first trimester. |
| Fetal Monitoring | Monitor renal function and fetal growth if used inadvertently. |
| Fertility Effects | No data on human fertility effects. |
| Clinical Pearls | Cinobac (cinoxacin) is a quinolone antibiotic used for urinary tract infections. Avoid in children and pregnant or lactating women due to arthropathy risk. Adjust dose in renal impairment (CrCl <50 mL/min). May prolong QT interval; avoid with other QT-prolonging drugs. Monitor for tendonitis or tendon rupture, especially in patients >60 years, on corticosteroids, or with renal impairment. Administer with food to reduce GI upset, but avoid concurrent dairy products, antacids, or iron supplements as they reduce absorption. |
| Patient Advice | Take this medication exactly as prescribed, even if you feel better. · Finish the entire course of treatment to prevent antibiotic resistance. · Avoid taking with dairy products, antacids, or iron supplements; separate by at least 2 hours. · Drink plenty of fluids to stay hydrated while taking this medication. · Report any tendon pain, swelling, or rupture, especially in the Achilles tendon. · Contact your doctor immediately if you experience signs of an allergic reaction, severe diarrhea, or irregular heartbeat. · This medication may cause dizziness; avoid driving or operating machinery until you know how it affects you. · Avoid excessive sun exposure and use sunscreen; this drug may increase sensitivity to sunlight. |