ABSTRACT
For the topical employing of nonsteroidal antiinflammatory drugs, some technological problems are to be solved. These were accomplished by the authors by preparing Indosol [indomethacin-TRIS (tromethamine) salt]. pH and osmotic pressure of Indosol eye-drops are similar to that of the tear fluid. The Indosol eye-drops have a great therapeutic efficacy. Indosol eye-drops do not alter tear film break up time (BUT) and do not inhibit reepithelization of the cornea. Indosol eye-drops proved to be useful in the treatment of the anterior segment and the uvea. The most important use is the pre- and post-treatment in intraocular surgery. Indosol eye-drops contribute to the safety of lens-extraction and lens implantation. The great bioavailability was also shown by the high indomethacin level of the aqueous humor after instillation Indosol eye-drops. It does not cause any deleterious side-effects even in long term treatments.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Indomethacin/therapeutic use , Lenses, Intraocular , Biological Availability , Cornea/drug effects , Humans , Indomethacin/adverse effects , Indomethacin/pharmacokinetics , Ophthalmic Solutions , Tears , UveaABSTRACT
The antiviral effect of 5-isopropyl-2'-deoxyuridine (IPDU) on herpes viruses (HSV-1 and HSV-2) is based on the sensitivity of virus DNA to nucleases due to IPDU incorporation into the virus DNA and the resulting change in DNA conformation. Virus selectivity is based on virus induced thymidine kinase activity and on HSV induction of polymerase enzymes catalyzing the incorporation. Hevizos ointment containing IPDU has the following advantageous pharmacokinetic properties: high accumulation in the skin, high resistance to phosphorylases and other metabolizing enzymes.
Subject(s)
Antiviral Agents/toxicity , Antiviral Agents/therapeutic use , DNA, Viral/metabolism , Deoxyuridine/analogs & derivatives , Herpes Simplex/drug therapy , Simplexvirus/drug effects , DNA, Viral/chemistry , DNA, Viral/drug effects , DNA-Directed DNA Polymerase/biosynthesis , Deoxyuridine/metabolism , Deoxyuridine/therapeutic use , Deoxyuridine/toxicity , Humans , Models, Structural , Nucleic Acid Conformation , Ointments , Simplexvirus/enzymology , Simplexvirus/metabolism , Skin/metabolismABSTRACT
The oxidation of the redox indicator Variamine Blue in an aqueous medium has been studied by the ESR method. The optimum conditions for the formation of the radical have been determined. The spectra have in some cases shown hyperfine splitting, from which conclusions could be drawn for the nature of the oxidation reaction and structure of the oxidized product. The coupling constants have also been determined for the radicals. The correctness of the assumptions for the structure of the radicals has been supported by the simulation of spectra and the investigation of deuterated derivatives.