It is a
nucleoside analogue, a modified form of
deoxyuridine, similar enough to be incorporated into viral
DNA replication, but the
iodine atom added to the
uracil component blocks
base pairing. It is used only topically due to cardiotoxicity. It was synthesized by
William Prusoff in the late 1950s.[1] Initially developed as an anticancer drug, idoxuridine became the first antiviral agent in 1962.[2]
Clinical use
Idoxuridine is mainly used topically to treat
herpes simplexkeratitis.[3] Epithelial lesions, especially initial attacks presenting with a dendritic ulcer, are most responsive to therapy, while infection with stromal involvement are less responsive.[4] Idoxuridine is ineffective against herpes simplex virus type 2 and
varicella-zoster.[3]
Side effects
Common side effects of the eye drops include irritation, blurred vision and
photophobia.[5]Corneal clouding and damage of the corneal epithelium may also occur.[citation needed]
Formulations and dosage
Idoxuridine is available as either a 0.5% ophthalmic
ointment or as a 0.1% ophthalmic
solution.[3] The dosage of the ointment is every 4 hours during day and once before bedtime.[3] The dosage of the solution is 1 drop in the
conjunctival sac hourly during the day and every 2 hours during the night until definitive improvement, then 1 drop every 2 hours during the day and every 4 hours during the night.[3] Therapy is continued for 3–4 days after healing is complete, as demonstrated by
fluorescein staining.[3]
^
abcdefGoodman and Gilman's The Pharmacological Basis of Therapeutics. Edited by Gilman AG, Rall TW, Nies AS, Taylor P. McGraw-Hill. 8th ed. 1990.
^Maxwell E (October 1963). "Treatment of herpes keratitis with 5-iodo-2-deoxyuridine (IDU): a clinical evaluation of 1500 cases". American Journal of Ophthalmology. 56: 571–573.
doi:
10.1016/0002-9394(63)90006-0.
PMID14070708.
^FR 1336866, Gaston A, Vesperto T, "Nouveau procédé de préparation d'un dérivé de l'uridine et produits utilisés dans ce procédé [New process for preparing a derivative of uridine and products used in this process]", published 1963-09-06, assigned to
Roussel-Uclaf
^GB 1024156, "Process for the preparation of 5-iodo-2'-desoxy-uridine", published 1966-03-30, assigned to
Roussel-Uclaf
^Chang PK, Welch AD (July 1963). "Iodination of 2'-Deoxycytidine and Related Substances". Journal of Medicinal Chemistry. 6 (4): 428–430.
doi:
10.1021/jm00340a019.
PMID14184899.
Further reading
Seth AK, Misra A, Umrigar D (August 2004). "Topical liposomal gel of idoxuridine for the treatment of herpes simplex: pharmaceutical and clinical implications". Pharmaceutical Development and Technology. 9 (3): 277–289.
doi:
10.1081/PDT-200031432.
PMID15458233.
S2CID33864681.
Otto SE (1998). "Radiopharmaceuticals (Strontium 89) and radiosensitizers (idoxuridine)". Journal of Intravenous Nursing. 21 (6): 335–337.
PMID10392098.
Fauth E, Zankl H (April 1999). "Comparison of spontaneous and idoxuridine-induced micronuclei by chromosome painting". Mutation Research. 440 (2): 147–156.
doi:
10.1016/s1383-5718(99)00021-2.
PMID10209337.