Reference

Relative potencies of anti-herpes compounds

Relative potencies of anti-herpes compounds. Collins, P.; Bauer, D. J. (Wellcome Res. Lab., Beckenham/Kent, Engl.). Ann. N. Y. Acad. Sci., 284, 49-59 (English) 1977. CODEN: ANYAA9. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The relative and abs. potencies of idoxuridine [54-42-2], cytarabine [147-94-4], vidarabine [5536-17-4], trifluorothymidine [70-00-8], and 2,6-diamino-9-.beta.-D-arabinofuranosylpurine (ara-DAP) [34079-68-0] were evaluated by plaque inhibition, plaque redn., and yield redn. tests, the most satisfactory dose-response lines being obtained by plaque redn. The results obtained for 5 strains of type 1 and 5 of type 2 herpesvirus indicated that cytarabine was the most active compd., followed by idoxuridine and trifluorothyrmidine; vidarabine and ara-DAP were found to be the least active compds. From comparisons of ED50 values derived from the dose-response lines it the greater sensitivity of type 1 strains reported in the literature could only be confirmed with idoxuridine, since considerable overlaps in type sensitivity were obsd. with the other compds.

Studies on the toxicity of newly developed drugs for ophthalmic use done on the rabbit cornea by scanning electron microscopy

Studies on the toxicity of newly developed drugs for ophthalmic use done on the rabbit cornea by scanning electron microscopy. Ogawa, Takashi (Sch. Med., Tokushima Univ., Tokushima 770, Japan). Nippon Ganka Gakkai Zasshi, 88(7), 1093-106 (Japanese) 1984. CODEN: NGZAA6. ISSN: 0029-0203. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The cytotoxicity of several drugs was studied on the rabbit cornea using SEM. The antiherpetic drugs, 9-b-D-arabinofuranosyl-2,6-diaminopurine (ara-DAP) [34079-68-0], 9-b-D-arabinofuranosyladenine 5'-monophosphate (ara-AMP) [29984-33-6], 9-b-D-arabinofuranosylthioguanine [32976-84-4] and 9-b-D-arabinofuranosyladenine (ara-A) [5536-17-4] were used. They were applied to the rabbit cornea in the form of 3% ointment, 5 times a day for 2 wks. The antifungal drug, pimaricin [7681-93-8] (1% suspension, 1% ointment and 5% suspension) was applied 5 times a day for 4 wks. The antibiotics, 0.3% soln. of micronomicin [52093-21-7], dibekacin [34493-98-6] and sisomicin [32385-11-8] were instilled 9 times a day for 5 days. One hour after the last instillation, eyes were enucleated and the surface of the corneas were obsd. by SEM. Ara-DAP and ara-A showed almost no cytotoxicity. Therefore, the clin. application of these drugs seems safe. Ara-AMP caused transformation and differences in size of the epithelium, indicating that this drug must be used carefully. One percent suspension of pimaricin showed almost no cytoxocity. One percent ointment of pimaricin caused only mild damage to the microvilli, but 5% suspension induced considerable desquamation. These results suggest the use of 1% suspension or 1% ointment usually and 5% suspension for serious cases in keratomycosis. The antibiotic drops tested showed no damage to the epithelium, promising safety in clin. use.