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). |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OPHTHOCORT (OPHTHOCORT).
| Breastfeeding | Topical ophthalmic corticosteroids have minimal systemic absorption. No specific M/P ratio available. It is considered compatible with breastfeeding; however, apply after nursing to minimize infant exposure. |
| 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. |
■ 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 |
History of hypersensitivity to chloramphenicol, hydrocortisone, or any component; viral diseases of the cornea and conjunctiva (e.g., herpes simplex, vaccinia, varicella); fungal infections; untreated purulent infections; patients with known bone marrow depression.
| 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. |
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| 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. |