PROBAMPACIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROBAMPACIN (PROBAMPACIN).
PROBAMPACIN is a synthetic aminoglycoside antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, causing misreading of mRNA and preventing translocation of peptidyl-tRNA from the A-site to the P-site.
| Metabolism | PROBAMPACin undergoes minimal hepatic metabolism; approximately 90% of the dose is excreted unchanged in the urine via glomerular filtration. No significant cytochrome P450 involvement. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 20% as metabolites; 10% other |
| Half-life | 4.5 hours (prolonged to 12-18 hours in severe renal impairment) |
| Protein binding | 92% (primarily albumin) |
| Volume of Distribution | 0.35 L/kg (reflects moderate tissue penetration, primarily extracellular fluid) |
| Bioavailability | Oral: 85%; IM: 100% |
| Onset of Action | IV: 5-10 minutes; IM: 15-30 minutes; Oral: 45-60 minutes |
| Duration of Action | IV/IM: 6-8 hours; Oral: 4-6 hours |
100 mg IV every 12 hours over 30 minutes.
| Dosage form | FOR SUSPENSION |
| Renal impairment | GFR >60 mL/min: no adjustment; GFR 30-60: 100 mg every 24 hours; GFR 15-29: 50 mg every 24 hours; GFR <15: 50 mg every 48 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg every 12 hours; Child-Pugh C: 50 mg every 24 hours. |
| Pediatric use | 2 mg/kg IV every 12 hours; maximum 100 mg per dose. |
| Geriatric use | Start at 50 mg IV every 12 hours; monitor renal function and adjust per renal dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROBAMPACIN (PROBAMPACIN).
| Breastfeeding | Probampacin is excreted into breast milk in low concentrations (M/P ratio approximately 0.25). The relative infant dose is estimated at less than 5% of maternal weight-adjusted dose. Considered compatible with breastfeeding; monitor infant for potential gastrointestinal disturbances. |
| Teratogenic Risk | Probampacin is an antibiotic with limited human data. In animal studies, no teratogenic effects were observed at therapeutic doses. However, avoid use during first trimester unless essential, as with all medications. Second and third trimester use is generally considered safe based on maternal benefit. |
■ FDA Black Box Warning
WARNING: NEPHROTOXICITY AND OTOTOXICITY. PROBAMPACIN can cause nephrotoxicity, which may progress to renal failure, and irreversible bilateral vestibular and cochlear ototoxicity, especially in patients with renal impairment or those receiving prolonged therapy or high doses. Serial renal function and audiometric tests are recommended. Avoid concurrent use with other nephrotoxic or ototoxic drugs.
| Serious Effects |
Hypersensitivity to PROBAMPACIN or any aminoglycoside antibiotic. Avoid in patients with myasthenia gravis or history of aminoglycoside-induced ototoxicity. Relative contraindication: pre-existing severe renal impairment (CrCl < 30 mL/min) unless on dialysis.
| Precautions | Monitor renal function (serum creatinine, BUN, creatinine clearance) and audiometry at baseline and periodically during therapy. Adjust dose in renal impairment. Risk of neuromuscular blockade, especially in patients with myasthenia gravis or other neuromuscular disorders. May cause electrolyte disturbances (hypocalcemia, hypomagnesemia). Use with caution in elderly patients and those with pre-existing hearing loss or vertigo. |
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| Fetal Monitoring | Monitor maternal renal function, hepatic enzymes, and complete blood count. In fetus, assess for growth and amniotic fluid volume if used for extended periods. No specific fetal monitoring required for short-term use. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at therapeutic doses. |