OPHTHOCORT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OPHTHOCORT (OPHTHOCORT).
OPHTHOCORT contains chloramphenicol, a bacteriostatic antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing peptide bond formation; and hydrocortisone, a corticosteroid that suppresses inflammation by inhibiting phospholipase A2 and reducing prostaglandin and leukotriene synthesis.
| Metabolism | Chloramphenicol is primarily metabolized by hepatic glucuronidation via UDP-glucuronosyltransferase; also partially metabolized to inactive metabolites by bacterial nitroreductases. Hydrocortisone is metabolized in the liver and in peripheral tissues. |
| Excretion | Renal (70-80% as unchanged drug), fecal (15-20% via biliary elimination), with minor metabolic clearance. |
| Half-life | Terminal elimination half-life: 2.5-3.5 hours in adults with normal renal function; prolonged to 12-24 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 30-40% bound to serum albumin; low protein binding limits drug interactions. |
| Volume of Distribution | 0.3-0.5 L/kg, indicating distribution primarily into extracellular fluid; does not penetrate CNS appreciably. |
| Bioavailability | Oral: 60-70% (first-pass metabolism reduces bioavailability); Topical: variable (<10% systemic absorption through intact skin; higher through abraded skin). |
| Onset of Action | Oral: 1-2 hours; Topical: local effect within 30-60 minutes; Intravenous: immediate (within 5-10 minutes). |
| Duration of Action | Oral: 6-8 hours; Topical: 4-6 hours; Intravenous: 8-12 hours (effect related to serum concentrations above MIC). |
| Molecular Weight | Chloramphenicol: 323.13 Da; Hydrocortisone: 362.46 Da; Polymyxin B sulfate: ~1300 Da (variable). |
One drop into the affected eye(s) every 3-4 hours, or more frequently as needed. In severe cases, one drop every hour. Shake well before use.
| Dosage form | OINTMENT |
| Renal impairment | No dosage adjustment required for renal impairment as systemic exposure is minimal. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Same as adult dosing: one drop into the affected eye(s) every 3-4 hours. Safety and efficacy in children have not been established for prolonged use. |
| Geriatric use | Same as adult dosing. No specific geriatric adjustment required; use with caution in patients with glaucoma or cataract history. |
| 1st trimester | Avoid due to potential teratogenicity; contains chloramphenicol (gray baby syndrome risk) and polymyxin B. |
| 2nd trimester | Avoid unless benefit outweighs risk; systemic absorption may affect fetus. |
| 3rd trimester | Avoid near term due to risk of gray baby syndrome from chloramphenicol. |
Clinical note
Comprehensive clinical and safety monograph for OPHTHOCORT (OPHTHOCORT).
| Placental transfer | Chloramphenicol crosses placenta; detectable in fetal serum at 30-80% of maternal levels. |
| Breastfeeding | Chloramphenicol is excreted into breast milk and may cause bone marrow suppression or gray baby syndrome in nursing infants. Avoid breastfeeding during treatment. |
| Lactation Rating |
■ FDA Black Box Warning
Chloramphenicol is associated with serious and fatal blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, granulocytopenia). It should not be used when less potentially toxic agents are effective. Systemic absorption from ocular use may occur.
| Serious Effects |
Hypersensitivity to any componentViral or fungal ocular infectionsUncontrolled glaucomaCorneal epithelial defects
| Precautions | Bone marrow suppression including aplastic anemia; monitoring of blood counts recommended; prolonged use may lead to superinfection; ocular use may result in systemic absorption; avoid use in mild or trivial infections; use with caution in patients with hepatic impairment. |
| Food/Dietary | No known food interactions for ophthalmic OPHTHOCORT. However, systemic absorption is minimal; no dietary restrictions are required. |
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| L4 - Hazardous |
| Teratogenic Risk | Ophthalmologic corticosteroids (e.g., dexamethasone) are classified as FDA Category C. First trimester: No well-controlled human studies; animal studies show increased risk of cleft palate at high systemic doses. Orally administered corticosteroids are associated with a small increased risk of orofacial clefts (absolute risk ~0.1%). Second and third trimesters: Chronic high-dose systemic use may cause fetal adrenal suppression, intrauterine growth restriction, and altered fetal hypothalamic-pituitary-adrenal axis. Ophthalmic use results in minimal systemic absorption, theoretically lower risk, but caution is advised. |
| Fetal Monitoring | Monitor for signs of corticosteroid excess (e.g., weight gain, hyperglycemia, hypertension). Fetal growth ultrasound if prolonged high-dose use. Neonatal assessment for adrenal insufficiency if maternal use continues near term. |
| Fertility Effects | No known adverse effects on fertility with ophthalmic use. Systemic corticosteroids may affect menstrual cycle or sperm parameters, but topical ocular route unlikely to cause significant systemic effects. |
| Clinical Pearls | OPHTHOCORT (hydrocortisone, neomycin, polymyxin B) is a combination ophthalmic suspension. Neomycin carries a risk of sensitization; use with caution in patients with prior aminoglycoside allergy. Prolonged corticosteroid use may elevate intraocular pressure, especially in known glaucoma patients. Do not use in viral (e.g., herpes simplex) or fungal eye infections. Shake vigorously before each use. Apply gentle pressure to the nasolacrimal duct after instillation to minimize systemic absorption. |
| Patient Advice | Shake the bottle well before each use. · Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 15 minutes before reinserting. · Complete the full course even if symptoms improve; do not share medication with others. · Report any signs of allergy (itching, redness, swelling) or worsening vision immediately. · If using other eye drops, separate administration by at least 5 minutes. |