OPHTHOCHLOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OPHTHOCHLOR (OPHTHOCHLOR).
Chloramphenicol inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing peptide bond formation.
| Metabolism | Primarily hepatic via glucuronidation; a small amount is hydrolyzed to inactive metabolites. |
| Excretion | Renal: 70-80% unchanged; biliary/fecal: 20-30% |
| Half-life | 5-6 hours in normal renal function; prolonged up to 24-48 hours in severe renal impairment |
| Protein binding | 50-60% bound to albumin |
| Volume of Distribution | 0.5-1.0 L/kg indicating distribution into total body water |
| Bioavailability | Oral: 80-90%; intravenous: 100% |
| Onset of Action | Oral: 1-2 hours; Intravenous: 10-30 minutes |
| Duration of Action | 6-8 hours after single dose; extended with renal impairment |
Chloramphenicol 0.5% ophthalmic solution: Instill 1-2 drops into the affected eye(s) every 3-4 hours for 7-10 days. For severe infections, every 2 hours initially. Ointment: Apply a small amount (about 0.5 cm) into the conjunctival sac every 3-4 hours.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for ophthalmic use; minimal systemic absorption. |
| Liver impairment | Contraindicated in patients with hepatic impairment due to risk of bone marrow suppression. Child-Pugh Class B or C: avoid use. |
| Pediatric use | Neonates and infants: Avoid systemic use; ophthalmic use with caution. For children >1 year: Same as adult ophthalmic dosing. For systemic infections (uncommon): 12.5-25 mg/kg IV every 6 hours; monitor blood levels. |
| Geriatric use | No specific adjustment needed for ophthalmic use. Monitor for systemic adverse effects in elderly due to potential decreased renal/hepatic function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OPHTHOCHLOR (OPHTHOCHLOR).
| Breastfeeding | Not known if excreted in human milk. Low systemic absorption minimizes risk to breastfed infant. M/P ratio not available. Caution when administered to nursing woman. |
| Teratogenic Risk | No well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Use only if clearly needed and potential benefit justifies risk to fetus. First trimester: theoretical risk based on general principles; second and third trimesters: limited data suggest no known teratogenicity; however, systemic absorption is low. |
■ FDA Black Box Warning
Serious and fatal blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, granulocytopenia) have been reported after systemic use; topical use may also carry risk.
| Serious Effects |
["Hypersensitivity to chloramphenicol or any component","History of drug-related blood dyscrasias","Concurrent use with drugs that suppress bone marrow"]
| Precautions | ["Bone marrow suppression including aplastic anemia","Hypersensitivity reactions","Superinfection with prolonged use","Not for use in viral or fungal infections"] |
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| Fetal Monitoring |
| None specifically required beyond routine prenatal care due to minimal systemic absorption. |
| Fertility Effects | No studies on fertility effects. Based on pharmacological profile, no expected impact on fertility at recommended ophthalmic doses. |