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At least 19 recordsLinked to original sources
PubMed1978

The development of British pharmacopoeia monographs for idoxuridine and idoxuridine eye drops using high-pressure liquid chromatography for assay and for controlling related impurities.

The monograph published in the 1973 edition of the British Pharmacopoeia (BP) for idoxuridine required revision because it contained a non-specific assay and no tests for related impurities. It was also necessary to prepare a new monograph for idoxuridine eye drops. The Japanese Pharmacopoeia contains a thin-layer chromatographic test for impurities but this was not considered ideal. Improved thin-layer chromatographic tests were sought but when this was unsuccessful, methods using high-pressure liquid chromatography were examined. A system using reversed-phase chromatography was selected for inclusion in BP Addendum 1977 since it provided a specific assay method and limit test for related impurities which could be applied to both the drug substance and the eye drops.

Chromatography↗
PubMed1990

Topical idoxuridine for treatment of genital warts in males. A double-blind comparative study of 0.25% and 0.5% cream.

Fifty heterosexual male patients with histologically verified genital warts of short duration (less than 3 months) were randomly allocated to treatment with either 0.25% or 0.5% idoxuridine cream. The application of the cream to the warts was performed twice daily for an initial period of 14 days, whereafter patients with partial improvement or no response were retreated in the same way for another period of 14 days. Patients not completely healed after 28 days were regarded as treatment failures and withdrawn from the study. After the initial treatment period of 14 days, 19 of 25 patients (76%) treated with 0.5% idoxuridine cream, and 9 of 25 patients (36%) treated with 0.25% idoxuridine cream were completely healed. This difference is significant (p less than 0.01). The corresponding figures at the second follow-up examination (28 days after start of the study) were 19 of 25 (76%) and 13 of 25 (52%), respectively. At the last follow-up examination three months after start of treatment, four patients treated with 0.5% idoxuridine cream and five patients treated with 0.25% idoxuridine cream had a relapse. Thus, the overall rate of complete healing was 15 of 25 (60%) for the patients treated with 0.5% idoxuridine cream and 8 of 25 (32%) for those treated with 0.25% idoxuridine cream. The difference is significant (p less than 0.01). No adverse reactions were observed or reported by the patients.

Administration, Topical↗
PubMed1982

Ineffectiveness of topical idoxuridine in dimethyl sulfoxide for therapy for genital herpes.

The efficacy and toxicity of topical applications of 30% idoxuridine in dimethyl sulfoxide, dimethyl sulfoxide alone, or saline in 96 recurrent and 39 first episodes of genital herpes simplex virus (HSV) infection were compared. Drug was applied to lesions four times daily for seven days. In recurrent episodes, the duration of viral shedding after beginning idoxuridine in dimethyl sulfoxide use was significantly shorter (0.6 days) than with dimethyl sulfoxide (1.4 days) or saline (2.0 days) (P less than .05). In primary episodes, viral shedding lasted 2.6 days with idoxuridine in dimethyl sulfoxide and 8.4 days with dimethyl sulfoxide or saline. Idoxuridine in dimethyl sulfoxide had no effect in recurrent or primary HSV on duration of symptoms, new lesion formation, healing time, or risk of subsequent recurrence. Complications in patients given idoxuridine in dimethyl sulfoxide included local burning, generalized contact dermatitis, and vulvar carcinoma in situ. Thirty percent idoxuridine in dimethyl sulfoxide has no effect on clinical manifestations of genital HSV infection and may be hazardous.

Administration, Topical↗
PubMed1987

A trial of topical idoxuridine for vulvar condyloma acuminatum.

The effect of 0.25% idoxuridine ointment on condyloma acuminatum of the vulva was investigated in a randomized, double-blind, placebo-controlled trial in 24 women. Idoxuridine inhibits DNA synthesis in mammalian cells and is a specific inhibitor of DNA viruses. Of the 24 women with vulvar condyloma acuminatum, 14 applied idoxuridine ointment and 10 a placebo ointment to the lesions twice daily for 2 weeks. In 11 out of 14 patients treated with idoxuridine the condylomata regressed completely. The treatment did not cause any side-effects. None of the women in the placebo group showed regression of the condylomata. Topical idoxuridine therapy is effective and non-toxic; it appears to be most effective for new condylomata.

Administration, Topical↗
PubMed2004

In vitro efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyclovir against feline herpesvirus type-1.

OBJECTIVE: To establish the in vitro efficacy of 4 novel drugs (ie, ganciclovir, cidofovir, penciclovir, and foscarnet) against feline herpesvirus type-1 (FHV-1) and compare their antiviral efficacy with that of acyclovir and idoxuridine. SAMPLE POPULATION: Cultured Crandell-Reese feline kidney (CRFK) cells and FHV-1 strain 727 PROCEDURE: For each drug, antiviral effect was estimated by use of conventional plaque-reduction assays, and inhibitory concentration 50 (IC50; drug concentration at which plaque numbers were reduced by 50% relative to the number of plaques for nontreated control wells) was calculated. To determine whether observed antiviral effects were related to alterations in the number or viability of CRFK cells, cytotoxicity assays were performed at 1, 2, and 10 times the median IC50 for each antiviral drug. RESULTS: Median IC50 for each drug was as follows: ganciclovir, 5.2 microM; cidofovir, 11.0 microM; penciclovir, 13.9 microM; foscarnet, 232.9 microM; idoxuridine, 4.3 microM; and acyclovir, 57.9 microM. Obvious changes in morphologic characteristics, confluence, or viability of CRFK cells were not observed at concentrations up to and including 2 times the IC50 for each drug. CONCLUSIONS AND CLINICAL RELEVANCE: In vitro efficacy of idoxuridine and ganciclovir against FHV-1 was approximately equivalent and about twice that of cidofovir and penciclovir. Foscarnet appeared to be comparatively ineffective. Given the reasonable clinical efficacy of idoxuridine in cats infected with FHV-1, clinical trials of ganciclovir, cidofovir, and penciclovir or their prodrug forms appear to be warranted.

Acyclovir↗
PubMed1975

Idoxuridine in the treatment of herpes zoster.

An uncontrolled, double-blind, random-selection study of fifty consecutive patients with attacks of herpes zoster treated with one of two concentrations (5 per cent or 40 per cent) of idoxuridine (IDU) in dimethyl sulphoxide (DMSO) has shown that, over all, the patients fared better than would have been expected had they been treated only symptomatically. There was no apparent difference between the two concentrations of idoxuridine in regard to either side-effects or benefits. In 17 of the fifty patients the skin lesions healed more rapidly than would have been expected without treatment, and pain was relieved more rapidly than expected in 26 of the 47 patients in whom it was a feature of the attack. Side-effects, which included a transient stinging or burning sensation in 29 patients and acute sensitivity to idoxuridine (confirmed by patch-testing) in one, did not lead to withdrawal of any patient from the trial. Three patients complained of an unpleasant, garlicky taste during treatment. No significant abnormalities were noted in liver-function tests and in white-cell or platelet counts in patients in either treatment group. The solutions of idoxuridine in dimethyl sulphoxide were provided by W.B. Pharmaceutical Ltd.

Administration, Topical↗
PubMed1975

Herpes simplex encephalitis in Hodgkins disease. Isolation of drug-sensitive virus from brain following unsuccessful treatment with idoxuridine.

Herpes simplex encephalitis developed in a patient with Hodgkin's disease under therapy. Despite treatment with idoxuridine in a total dose of 280 mg/kg intravenously, he died without showing any clinical response. At autopsy, there was no gross or microscopic evidence of Hodgkin's disease, and virus isolated from the brain postmortem was inhibited in vitro by idoxuridine 0.5 mug/ml. Failure of idoxuridine to affect the course of infection by a drug-sensitive virus may be due to poor tissue penetration, although the role of the Hodgkin's disease cannot be discounted.

Adult↗
PubMed1977

Perfusion and molecular modification of idoxuridine to alter its cerebrospinal fluid metabolism.

Two methods to deter the rapid intrathecal degradation of idoxuridine were investigated: (a) rapid drug perfusion through the ventricular system, and (b) modification of the molecule to its uronic acid derivative, 2'-deoxy-5-iodo-5'-uridinecarboxylic acid, to make it less susceptible to enzymatic digestion. Perfusion of idoxuridine through the ventricular system (ventriculocisternal) of dogs at 0.97 ml/min saturated the metabolic pathway so that the outflow solution yielded a single spot (Rf 0.76) on TLC indicative of the intact molecule. The 125I-labeled uronic acid was synthesized from the 125I-labeled parent compound, and the labeled compounds were compared after their individual intracisternal injection in dogs. Since there was no difference in the disappearance rates, the stability of the uronic acid was, in fact, no greater than that of the parent compound in vivo. Ventricular perfusion of idoxuridine, however, seems a suitable means for increasing the amount of active drug delivered to central nervous system tumors and viral infections.

Animals↗
PubMed1980

Contact allergy to idoxuridine. Sensitization following treatment of herpes zoster.

A total of 45 of 60 patients with herpes zoster previously treated with topical idoxuridine 5-40% in dimethylsulfoxide were patch tested 2 years later with idoxuridine 0.5% and 5% in petrolatum. Three (7%) showed positive reactions. Idoxuridine is considered a weak sensitizer, but in strong concentrations and in active solvents, which increases absorption, there seems to be a risk of sensitization.

Adolescent↗
PubMed1974

Idoxuridine in herpes zoster: further evaluation of intermittent topical therapy.

In a randomized double-blind controlled trial of the value of intermittent topical idoxuridine in treating herpes zoster in 118 patients idoxuridine 5% in 100% dimethyl sulphoxide (DMSO), applied four-hourly for four days, significantly shortened the vesicular phase, healing time, and duration of pain; idoxuridine 25% applied two-hourly produced no greater benefit. The only side effects were transient tender erythema in three patients and "urticarial" oedema in two patients with dermographia.

Administration, Topical↗
PubMed1972

Concentrations of idoxuridine in serum, urine, and cerebrospinal fluid of patients with suspected diagnoses of Herpesvirus hominis encephalitis.

A reproducible microbiologic assay of microgram quantities of idoxuridine (IDU) in serum, urine, or cerebrospinal fluid is presented. The antiviral assay is not interfered with by type-specific antibody or interferon. During slow intravenous infusions of idox-uridine (4 mg/min) in patients with suspected diagnoses of Herpesvirus hominis encephalitis, the rate of inactivation and/or removal of drug exceeded its administration. During several rapid infusions of idoxuridine (50 mg/min) significant quantities of the drug were found in serum, urine, and cerebrospinal fluid. Idoxuridine is not significantly bound to serum proteins and is not deiodinated in fresh serum or urine in vitro to inactive products (iodouracil, uracil, iodide). It is rapidly excreted into the urine. Inactivation of IDU occurs in tissues. This antiviral assay of IDU in body fluids should be applicable to other viruses and potential antiviral agents. Minimal inhibitory concentrations of IDU for fresh isolates of Herpesvirus hominis (type 1 or 2) were determined. Type 1 herpesviruses' microplaques in baby hamster kidney cell (BHK 21) tissue cultures were sensitive to 2.5-10 mug/0.4 ml. Type 2 macroplaques required 25-50 mug/0.4 ml. This latter characteristic may be an additional biologic marker which may be useful in suggesting type-specificity of herpesvirus isolates.

Animals↗
PubMed1989

In vitro susceptibility of feline herpesvirus-1 to vidarabine, idoxuridine, trifluridine, acyclovir, or bromovinyldeoxyuridine.

In vitro activities of 9-[( 2-hydroxyethoxy] methyl) guanine (acyclovir), (E)-5-(2-bromovinyl)-2'deoxyuridine, 9-beta-D-arabinofuranosyladenine (vidarabine), 5-iodo-2'-deoxyuridine (idoxuridine), and 5-trifluoromethyl-2'-deoxyuridine (trifluridine) were studied against 6 strains of feline herpesvirus-1. A significant difference was not detected among viral strains in their susceptibility to these compounds (P = 0.442). The relative potency of these compounds was trifluridine much greater than idoxuridine greater than vidarabine greater than bromovinyldeoxyuridine much greater than acyclovir. Concentrations of trifluridine and idoxuridine (0.67 and 6.8 microM, respectively) required to reduce plaque numbers by 50%, compared with that of controls, were significantly lower (P less than 0.001) than were those of other compounds.

Acyclovir↗
PubMed1975

Idoxuridine ocular insert therapy. Use in treatment of experimental Herpes simplex keratitis.

Therapy of acute Herpes simplex keratitis in rabbits with idoxuridine-releasing ocular inserts showed that an application rate of 30mug/hr gave significantly better results than conventional treatment with idoxuridine drops and ointment while exposing the eye to 40% less drug. Delivery rates lower than this were equal or not as effective as drop and ointment therapy and rates up to 100 mug/hr did not produce significantly better results than rates of 30mug/hr. Serial viral cultures demonstrated the persistence of virus beyond the period of clinical resolution of disease in all treatment groups, indicating that therapy should be continued longer than apparent resolution of disease.

Animals↗
PubMed1983

Idoxuridine-induced conjunctival cicatrization.

Four patients had idoxuridine-induced conjunctival cicatrization similar to ocular cicatricial pemphigoid develop, but in the treated eye only. Three of the four patients had chronic, recurrent herpes simplex epithelial and stromal keratitis. The fourth patient had Sjögren's syndrome. All received idoxuridine (0.1% drops and/or 0.5% ointment) and topical corticosteroids from one to 3 1/2 years. Substantial morbidity resulted that included visual loss, stromal ulceration, corneal scarring, and keratinization. Conjunctival biopsy specimens showed cicatrization with a mixed inflammatory cell reaction and absence of goblet cells. Results of direct immunofluorescent microscopy of the conjunctiva were either negative or nonspecific for autoantibody. No circulating autoantibody was detected in any of the four patients.

Conjunctival Diseases↗
PubMed1979

Idoxuridine and bacterial corneal infection.

Corneas of 20 rabbits were treated with idoxuridine or a bland ointment before and after their inoculation with Staphylococcus aureus. The rabbit corneas treated with idoxuridine had a significantly more severe keratitis and yielded significantly greater numbers of S. aureus on culture than the rabbit corneas treated with the bland ointment.

Animals↗
PubMed1981

Idoxuridine-liposome therapy for herpes simplex keratitis.

In the treatment of acute and chronic herpetic keratitis, an idoxuridine-liposome preparation was more effective than a comparable therapeutic regimen of idoxuridine alone. Both antiviral agents were more effective than a control combination of liposome and saline.

Animals↗
PubMed1982

A double-blind, multicenter clinical trial of acyclovir vs idoxuridine for treatment of epithelial herpes simplex keratitis.

Thirty patients randomized to the Acyclovir (ACV) group (26 with dendritic lesions, 4 geographic lesions) and 34 patients randomized to the idoxuridine (IDU) treatment group (26 dendritic lesions, 8 geographic lesions) with epithelial herpetic keratitis were evaluated for efficacy and adverse reactions in a multi-center, double-masked, randomized, stratified trial. Patients were treated with either 3% acyclovir ophthalmic ointment or 0.5% idoxuridine ophthalmic ointment five times a day for 14 days. The results of the trial indicated no significant difference between ACV and IDU as antiviral agents in the treatment of epithelial herpetic keratitis. The overall healing patterns of ACV and IDU adjusted for lesion type and prognostic factors, including presenting condition (initial or recurrent disease), duration of symptoms, prior ophthalmic steroid use, and positive pretreatment herpesvirus culture, as well as, the healing patterns within each lesion type adjusted for these factors, were not significantly different between the two treatment groups. There was no significant difference between the two groups in the frequency of development of deeper involvement. The only significant difference (P less than 0.01) in the frequency of development of adverse reactions was found in the incidence of development of superficial punctate epitheliopathy (IDU-42%, ACV-11%).

Acyclovir↗
PubMedDate not supplied

Combination of laser-therapy with 0.5% idoxuridine cream in the treatment of therapy-resistant genital warts in male patients: an open study.

Forty heterosexual male patients with therapy resistant penile warts of long duration (mean 12.9 months) were treated with carbon dioxide laser, immediately followed by topical application of 0.5% idoxuridine cream twice daily for 14 days. In case of incomplete or no response to the initial treatment, the treatment procedure was repeated once. All patients had previously been repeatedly treated with podophyllotoxin 0.5% solution and/or carbon dioxide laser surgery. After two weeks of treatment, 32 patients (80%) were completely healed. The remaining eight patients were retreated and four weeks after the start of the study 35 patients (87.5%) showed complete response. Three months after the study had been initiated 34 patients (85%) were still completely healed. No adverse reactions were observed. It was concluded that laser surgery followed by topical application of 0.5% idoxuridine cream for two to four weeks seems to be highly effective in the treatment of longstanding, therapy-resistant genital warts in men. Because of the uncontrolled nature of the present study and the relatively small number of patients treated, it would be important to carry out controlled studies in larger study populations and to carry out a follow-up examination of at least six months after treatment.

Adult↗