Methylprednisolone concentrations in the vitreous and the serum after pulse therapy.
OBJECTIVE
Intravenous (i.v.) pulse of corticosteroids has been used to treat severe eye inflammation from different origins. Whether such large doses result in vitreous levels that differ either in magnitude or duration from more conventional corticotherapy remain unsolved issues. The authors therefore determined levels of methylprednisolone hemisuccinate and methylprednisolone in the vitreous and serum of patients at different times after a single i.v. perfusion of methylprednisolone hemisuccinate.


METHODS
Fifty patients scheduled for a first vitrectomy received an i.v. injection of 500 mg hemisuccinate methylprednisolone at different times before surgery (from 15-24 hours). Patients were divided into two groups: those with (n = 21) and without (n = 29) retinal detachment (RD). Pure vitreous samples were analyzed by high-pressure liquid chromatography.


RESULTS
Both the ester and the nonester methylprednisolone forms were sampled in the vitreous, showing a slower rate of hydrolysis compared to the serum. On average, the highest concentration of total methylprednisolone in the vitreous was found at 2.5 hours and rapidly decreased for the group of patients with RD. In the group of patients without RD, the highest concentration was reached at 6 hours and then slowly decreased. The antiinflammatory potency in the nondetached retina eyes was approximately 500 times more than in the physiologic vitreous, but despite the route of administration (i.v. or oral), only 1/10 of the corticosteroid serum concentration was measured in the vitreous.


CONCLUSIONS
High concentration of methylprednisolone is achieved by i.v. pulse therapy without changing the kinetic of entry in the vitreous of nondetached retina eyes when compared to conventional oral corticotherapy. Hydrolysis occurs in the vitreous resulting in high rate of active form. Pulse therapy could be considered in cases of severe ocular inflammation involving the posterior segment of the eye.
Behar-Cohen
F F
FF
Department of Ophthalmology, H tel-Dieu of Paris, France. Beharcohen@aol.com
Gauthier
S
S
El Aouni
A
A
Chapon
P
P
Parel
J M
JM
Renard
G
G
Chauvaud
D
D
D000293:Adolescent; D000328:Adult; D000368:Aged; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D005260:Female; D005938:Glucocorticoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008776:Methylprednisolone Hemisuccinate / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008875:Middle Aged; D020551:Pulse Therapy, Drug; D014018:Tissue Distribution; D014821:Vitrectomy; D014822:Vitreous Body / Q000378:metabolism*
D005938:Glucocorticoids; D008776:Methylprednisolone Hemisuccinate