Intravitreal injection of octreotide acetate

Joseph Robertson, Igor Westra, Eugene A. Woltering, Kevin Winthrop, Rosemary Barrie, Thomas M. O'Dorisio, Douglas Holmes

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

This study was conducted to determine the feasibility of injecting the somatostatin analogue, octreotide acetate (OA), into the vitreous cavity. Previous work suggests that octreotide effectively inhibits angiogenesis in vitro, thus its use in vivo may slow the progression of proliferative eye disease. Fifty micrograms of aqueous OA in 50 μl aqueous solution was injected into the mid-vitreous of kitten eyes (n=6), and OA levels were monitored over 4 days. A long-acting release form of octreotide (OA-LAR) was also injected into the mid-vitreous of rabbit eyes at doses of 0.36 (n=16), 1.1 (n=1), 2.1 (n=1), 4.05 (n=1), 8.2 (n=1), and 36 mg (n=3) in solution; and octreotide concentrations were measured at various time points over 42 days. OA concentrations were determined by a highly specific radioimmunoassay. Aqueous octreotide was eliminated rapidly (t 1/2= 16 hours) from the vitreous of the kitten eye, with only negligible amounts recoverable 4 days post- injection. In the long-acting form, OA in the rabbit eye reached peak levels at 28 days. By 42 days, OA levels had declined to the 14-day level. Doses of OA-LAR of 1.1 mg or less produced no gross evidence of clinical toxicity and elicited no grossly visible ocular side effects. Doses greater than 1.1 mg produced significant toxicity, including cataracts and rubeosis. The 28-day peak release for long-acting OA implies that monthly intravitreal injections could provide continual high levels of OA. Intravitreal injection of long- acting OA provides sustained, high concentrations of drug, and deserves further study as a potential treatment of proliferative eye diseases.

Original languageEnglish (US)
Pages (from-to)171-177
Number of pages7
JournalJournal of Ocular Pharmacology and Therapeutics
Volume13
Issue number2
StatePublished - Apr 1997

Fingerprint

Intravitreal Injections
Octreotide
Eye Diseases
Rabbits
Somatostatin
Cataract

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Ophthalmology
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Robertson, J., Westra, I., Woltering, E. A., Winthrop, K., Barrie, R., O'Dorisio, T. M., & Holmes, D. (1997). Intravitreal injection of octreotide acetate. Journal of Ocular Pharmacology and Therapeutics, 13(2), 171-177.

Intravitreal injection of octreotide acetate. / Robertson, Joseph; Westra, Igor; Woltering, Eugene A.; Winthrop, Kevin; Barrie, Rosemary; O'Dorisio, Thomas M.; Holmes, Douglas.

In: Journal of Ocular Pharmacology and Therapeutics, Vol. 13, No. 2, 04.1997, p. 171-177.

Research output: Contribution to journalArticle

Robertson, J, Westra, I, Woltering, EA, Winthrop, K, Barrie, R, O'Dorisio, TM & Holmes, D 1997, 'Intravitreal injection of octreotide acetate', Journal of Ocular Pharmacology and Therapeutics, vol. 13, no. 2, pp. 171-177.
Robertson J, Westra I, Woltering EA, Winthrop K, Barrie R, O'Dorisio TM et al. Intravitreal injection of octreotide acetate. Journal of Ocular Pharmacology and Therapeutics. 1997 Apr;13(2):171-177.
Robertson, Joseph ; Westra, Igor ; Woltering, Eugene A. ; Winthrop, Kevin ; Barrie, Rosemary ; O'Dorisio, Thomas M. ; Holmes, Douglas. / Intravitreal injection of octreotide acetate. In: Journal of Ocular Pharmacology and Therapeutics. 1997 ; Vol. 13, No. 2. pp. 171-177.
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