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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CINOBAC (CINOBAC).
| Breastfeeding | Not recommended; no data on excretion or M/P ratio. |
| 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. |
■ FDA Black Box Warning
Not applicable; not FDA-approved.
| Serious Effects |
["Hypersensitivity to bufadienolides","Pre-existing cardiac arrhythmias","Severe renal impairment","Hypokalemia","Pregnancy (teratogenic potential)"]
| Precautions | ["Cardiotoxicity (arrhythmias, digitalis-like effect)","Hepatotoxicity","Nephrotoxicity","Electrolyte disturbances (hyperkalemia)","Risk of fatal overdose due to narrow therapeutic index"] |
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| Fertility Effects |
| No data on human fertility effects. |