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Intraocular penetration of rifampin after oral administration
K W Wong1, D J D'Amico, B S Oum
1Howe Laboratory of Ophthalmology, Harvard Medical School, Boston, MA.
Abstract:
Rifampin, the most potent anti-staphylococcal drug known, was examined for its penetration into the aqueous and vitreous of rabbits after a single oral dose of 150 mg, 300 mg, or 600 mg. Maximum levels after the 150 mg dose were achieved at 4 h and were 4.2 micrograms/ml in the aqueous and 2.2 micrograms/ml in the vitreous. After the 300 mg dose, maximum levels were also achieved at 4 h, and were 5.0 micrograms/ml in the aqueous and 2.6 micrograms/ml in the vitreous. The 600 mg dose produced maximum levels at 6 h after administration, with 20.0 micrograms/ml in the aqueous and 15.2 micrograms/ml in the vitreous. These levels exceed the minimum inhibitory concentration for many microorganisms and suggest additional investigation into possible applications of systemic rifampin in the prophylaxis and treatment of bacterial endophthalmitis.
Insights
Rifampin, a potent antibiotic, effectively penetrates rabbit eyes after oral administration. Drug concentrations achieved suggest potential for treating bacterial eye infections like endophthalmitis.
Area of Science:
- Ophthalmology
- Pharmacology
- Infectious Diseases
Background:
- Rifampin is a highly effective antibiotic against Staphylococcus bacteria.
- Bacterial endophthalmitis is a serious eye infection requiring effective treatment.
Purpose of the Study:
- To evaluate the penetration of rifampin into the aqueous and vitreous humor of rabbit eyes.
- To determine if achieved drug concentrations are sufficient for treating bacterial endophthalmitis.
Main Methods:
- Rabbits received single oral doses of rifampin (150 mg, 300 mg, or 600 mg).
- Aqueous and vitreous humor samples were collected at various time points post-administration.
- Drug concentrations were quantified using microgram/ml measurements.
Main Results:
- Rifampin achieved significant concentrations in both aqueous and vitreous humor.
- Higher doses resulted in higher and more sustained drug levels.
- Maximum concentrations observed exceeded the minimum inhibitory concentration for many bacteria.
Conclusions:
- Systemic rifampin demonstrates promising ocular penetration.
- Further research is warranted for using rifampin in preventing and treating bacterial endophthalmitis.