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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↗
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↗
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↗
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↗
PubMed1975

Allergic contact dermatitis caused by idoxuridine. Patterns of cross reactivity with other pyrimidine analogues.

Idoxuridine has been used for many years in the treatment of herpex simplex infections of the eye. Use of the drug for herpes simplex infection of the skin is increasing. Ophthalmologists have noted occasional conjunctival and corneal irritant reactions, but no true delayed cutaneous hypersensitivity has been verified. We report four cases of allergic contact dermatitis from idoxuridine, sensitized by both eye and skin applications. Cross reactivity to brominated and chlorinated, but not fluorinated, pyrimidine analogues is noted. Extensive patch testing indicates the general relationship between the structure of pyrimidine compounds and their antigenic cross reactivity.

Adult↗
PubMed1979

Iontophoretic application of idoxuridine for recurrent herpes labialis: report of preliminary clinical trials.

In clinical trials on six patients the antiviral drug idoxuridine (Stoxil) was applied by anodal (+) iontophoresis to 14 recurrent herpes labialis lesions. Results were characterized by immediate relief of discomfort and swelling, rapid appearance and coalescence of vesicles, minimal or no spread of the lesions, and accelerated healing with minimal or no scab. These encouraging trials indicate that a full-scale, double-blind, controlled clinical study should be carried out to determine whether iontophoresis is the optimal method of applying idoxuridine to the surface lesions caused by herpesvirus.

Adult↗
PubMed1978

Double blind trial in the treatment of herpes simplex and herpes zoster with adenine arabinoside and idoxuridine.

In a double blind trial adenine arabinoside (Vidarabine) and Idoxuridine (IDU) were tested in herpes simplex and herpes zoster infections. Adenine arabinoside covered 19 patients with HSV and 6 with HZ while IDU 19 with HSV and 6 with HZ. From the statistical analysis it was found that Vidarabine acts shorter than IDU in HSV P less than 0.01, while in HZ no significant difference P less than 0.5 was found, possibly due to the small number of patients tested.

Adolescent↗
PubMed1975

Clinical evaluation of adenine arabinoside and idoxuridine in the treatment of ocular herpes simplex.

A Double-blind clinical study comparing idoxuridine (IDU) with adenine arabinoside (ara-A) in treating 54 routine herpetic ulcers, and an open ara-A therapy study of 58 herpetic ulcers in patients intolerant of or resistant to IDU, was carried out over a four-year period. There was no significant difference in healing time between IDU-treated eyes (11.5 days) and ara-A-treated eyes (12.4 days) in the double-blind study but there were four moderate to marked adverse reactions to IDU and only two mild reactions to ara-A. In the open-drug study 21 patients who were intolerant of IDU because of allergy or toxicity and 37 patients who had ulcers resistant to or deteriorating on IDU therapy used ara-A up to 192 days without any adverse reaction. Mean healing time was 10.6 days for 49 of 57 patients in the efficacy analysis. Eight patients developed trophic ulcers that responded to soft lens therapy and one was dropped from the study because his initial disease could not be distinguished from severe IDU-induced keratitis.

Adolescent↗
PubMed1975

Adenine arabinoside in idoxuridine unresponsive and intolerant herpetic keratitis.

Twenty-two patients with active herpes simplex dendritic keratitis, in whom topical idoxuridine was unsuccessful in controlling their disease, were treated with topical adenine arabinoside (ara-A), a purine analogue effective against many DNA viruses. This drug was an effective antiviral agent in these patients. No signs of ocular or adnexal toxicity were noted.

Adenine↗
PubMed1977

Trifluorothymidine and idoxuridine therapy of ocular herpes.

In a coded study, we treated 40 patients who had active herpes simplex corneal ulcers with either 1% trifluorothymidine (F3T) or 0.1% idoxuridine (IDU) drops; we treated 15 similarly afflicted patients, who had failed on IDU or vidarabine, with open 1% F3T drops. All dosages were at therapeutically recommended frequency. In the coded study there was no statistically significant difference between the drugs in rate of healing; mean initial ulcer size in both groups was approximately 7 mm2 and mean healing time was approximately 5.5 days. There was a significant difference, however, in the chances of successful healing; 96% of all F3T treated eyes and only 75% of IDU treated eyes healed completely within 14 days. In the open study, 87% of patients healed completely on F3T eyedrops. Although an insufficient number of patients were on concomitant coricosteroid therapy to provide statistical analysis, F3T-corticosteroid treated eyes (eight masked and open) all healed. The one IDU-corticosteroid treated eye in the masked study failed to heal.

Administration, Topical↗
PubMed1975

Comparison of the treatment of herpes genitalis in men with proflavine photoinactivation, idoxuridine ointment, and normal saline.

36 male patients with genital infection by HSV confirmed by culture were each allocated to one of three treatment groups: (1) Proflavine photoinactivation, (2) 0.5 per cent. idoxuridine ointment (IDU), (3) Normal saline. They were assessed objectively at each attendance by measurement of the lesions with an operating microscope fitted with a measuring grid in one eyepiece. Material for culture for HSV was taken at each visit; the presence of symptoms (pain, discomfort, and irritation) was noted. The areas of lesions in the proflavine photoinactivation group remained larger significantly longer than in the other groups, the healing time was slower, and HSV could be isolated for longer. It is concluded that proflavine photoinactivation is of no greater value than 0.5 per cent. IDU or normal saline in the treatment of genital infection by HSV in the male.

Acridines↗
PubMed1979

Treatment of herpes zoster with idoxuridine ointment, including a multivariate analysis of symptoms and signs.

A double-blind, random selection comparison was made of the therapeutic effects in acute herpes zoster of (A) 40% idoxuridine (IDU) dissolved in dimethyl sulphoxide (DMSO), or one of the following ointments: (B) a basis of polyethylene glycol, (C) a basis with 60% DMSO, (D) a basis with 5% IDU and 60% DMSO, and (E) a basis with 40% IDU and 60% DMSO. Each group comprised 20 patients. The patients were evaluated daily until skin healing and then at 1,3, and 6 months by registering 4 neurological signs, 5 clinical evaluations of skin pathology and 4 photographic evaluations of the skin lesions. A 'profile' of the effect of each treatment was computed by calculating normalized means for each of the 13 variables. A non-random distribution of the clinical and photographic variables indicated a statistically significant, but small therapeutic effect of treatment A on skin healing, whereas no convincing effect on pain or sensitivity disturbances was established. Treatments B-E were without positive effects. The information given by the highly interdependent variables were computed for each variable and for groups of variables after appropriate scoring. It was found that the photographic evaluation contributed evidence independent of the clinical evaluation of skin pathology. A multiple correlation analysis revealed that age was positively correlated to the duration of pain and to delayed healing, that rapid healing was intimately connected to no or short-lived pain, and surprisingly that zoster in the trigeminal area healed faster than in other locations without being correlated to less pain. Treatment A must necessarily be reevaluated taking into account proper controls as well as age and affected dermatomes.

Adolescent↗
PubMed1975

Absence of idoxuridine and persistence of herpes simplex virus in brains of patients being treated for encephalitis.

Thirty-two specimens of brain from five patients with encephalitis suspected to be caused by herpes simplex virus, type 1 (HSV-1) were assayed for antiviral activity. Each patient received 60-80 mg/kg/day of idoxuridine (IDU) by intravenous infusion. The antiviral assay does not measure anti-HSV-1 antibodies. Biopsies of brain in every patient taken before IDU was used, and portions of several regions of the brain at autopsy were available during courses of treatment in four of the five patients. The last patient died 7 days after completing treatment. A significant concentration of IDU (833 mug/ml) was measured transiently in the cerebrospinal fluid of one patient. Meninges and brains showed inflammatory changes. Within the sensitivity of the test (larger than or equal to 6 mug/g) all specimens contained no IDU. As given, IDU does not achieve therapeutic concentrations in human brain. Further clinical use of IDU in therapy of herpes simplex virus encephalitis is not indicated.

Adult↗
PubMed1977

Double--blind clinical trial of adenine arabinoside and idoxuridine in herpetic corneal ulcers.

The results are reported of a fully controlled randomized double-blind clincial trial of adenine arabinoside and idoxuridine ointment in sixty patients with herpetic ulceration of the cornea. Although both antivirals showed a trend towards superiority over placebo, the therapeutic effect did not reach statistical significance in spite of the known efficacy in laboratory animals. Further studies in rabbits are reported; these indicate that systemic immunity may play a role in combating virus proliferation in recurrent disease, and it is considered this disguises the efficacy of topical antiviral therapy in clinical trials, thus necessitating an estimated requirement for approximately fifty patients per treatment group to obtain significant effects. It is concluded that an antiviral is valuable in the treatment of ulcerative herpetic keratitis, particularly in primary disease and in the presence of systemic and local immunosuppression after the use of topical adrenocorticosteroid. In recurrent disease, where a trigger factor is known, experience has shown that therapy can be profitably administered before the onset of clinical disease.

Adolescent↗
PubMed1978

Treatment of herpes simplex keratitis with idoxuridine and vidarabine: a double-blind study.

A double controlled clinical study comparing idoxuridine (IDU) and vidarabine (ara-A) in the treatment of uncomplicated herpes simplex keratitis was carried out with 10 patients. No statistically significant differences occurred in the healing time between IDU (6.8 days) and ara-A (8.0 days). Two moderately adverse reactions to IDU were observed, but no demonstrable ocular toxicity was noted with ara-A.

Adult↗