Purpose: The aim of this study is to evaluate the effects and complications of mixed injections of botulinum neurotoxin A (BoNT-A), triamcinolone acetonide, 5-fluorouracil (5-FU) in patients with Graves upper eyelid retraction. Methods: Twenty-four eyes of 17 patients with a mean age of 43.9 years showed symptoms of Grave’s upper eyelid retraction (GUER). They received mixed injections of BoNT-A 4 IU/0.1 mL, triamcinolone acetonide 4 mg/0.1 mL and 5-FU 5 mg/0.1 mL via subconjunctival injection. The response to treatment and the presence of adverse effects were followed up for 9.0 ± 6.0 months and evaluated retrospectively. Results: Margin reflex distance 1 decreased significantly from 5.6 ± 1.2 mm to 4.7 ± 1.1 mm at 1 month after injection. Tarsal platform show increased significantly from 1.4 ± 1.3 mm to 1.8 ± 1.3 mm, and tear break up time increased significantly from 5.2 ± 3.1 seconds to 10.3 ± 7.8 seconds. When success was defined as the correction amount of GUER being larger than 1 mm, the success rate was 66.7%. Kaplan-Meier survival analysis showed that GUER correction effects last longer in patients with a duration of disease longer than 6 months. There were no severe adverse effects such as diplopia, blepharoptosis and intraocular pressure elevation. Conclusions: Mixed injections of BoNT-A, triamcinolone acetonide and 5-FU, which compensate the side effects of solitary injection and enhances the anti-fibrotic effect, improves the eyelid position and tear film stability in the patients with GUER. It is an effective and safe method for treating GUER with long maintenance with less adverse effects. J Korean Ophthalmol Soc 2016;57(5):691-699