Intraocular penetration of tamoxifen.
OBJECTIVE
To document ocular penetration of oral tamoxifen in patients being administered systemic therapy by measuring intraocular and serum levels of the drug in a series of patients undergoing elective ocular surgery.


METHODS
Nonrandomized, prospective, comparative trial.


METHODS
Twenty-one eyes of 21 patients undergoing elective ocular surgery (cataract extraction or vitrectomy). Twenty patients were using the antiestrogen, tamoxifen, and one participant was not. Nine patients were excluded in the final analysis because of inadequate sample size.


METHODS
Preoperative serum samples and perioperative aqueous samples, vitreous samples, or both were obtained for each patient, and these were analyzed for tamoxifen and its metabolites. Dilated fundus examination was performed before surgery on all patients.


METHODS
Evidence of tamoxifen, its metabolites, or both in the samples.


RESULTS
Tamoxifen was detected in all analyzed serum samples (range, 82.4-290.0 ng/ml.) from patients taking the medication and was found to have penetrated into both vitreous (range, 0.5-7.8 ng/ml) and aqueous (range, 0.5-3.9 ng/ml) cavities. No relationship was found between serum and intraocular levels.


CONCLUSIONS
This study shows that tamoxifen penetrates intraocular fluids to varying degrees. The drug levels in aqueous and vitreous do not appear to correlate with serum levels. Evidence of tamoxifen retinopathy or keratopathy was not seen.
Flaxel
C J
CJ
Moorfields Eye Hospital, London, England. flaxelcj@aol.com
Mulholland
B
B
Haynes
B
B
Gregor
Z J
ZJ
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001082:Aqueous Humor / Q000378:metabolism*; D002387:Cataract Extraction; D004965:Estrogen Antagonists / Q000493:pharmacokinetics*; D005260:Female; D005451:Fluorescein Angiography; D005654:Fundus Oculi; D006801:Humans; D008297:Male; D008875:Middle Aged; D011446:Prospective Studies; D012160:Retina / Q000187:drug effects; D013629:Tamoxifen / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014821:Vitrectomy; D014822:Vitreous Body / Q000378:metabolism*
D004965:Estrogen Antagonists; D013629:Tamoxifen