The Qualitative Evaluation of the Pharmacokinetics of Subconjunctivally Injected Antifungal Agents in Rabbits

Klippenstein, K; Dm, O'Day; Rd, Robinson; Te, Williams; Ws, Head

doi:10.1097/00003226-199311000-00009

Cited by 17 publications

(4 citation statements)

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“…The vehicle used to pre- (136). In an experimental animal model, itraconazole (2.5 mg/ml) that had been administered subconjunctivally was found to persist for at least 24 h in normal and debrided corneas, in contrast to amphotericin B, miconazole, fluconazole, and ketoconazole, which did not persist beyond 4 to 8 h (193). However, intravitreal injection of itraconazole appears to cause focal areas of retinal necrosis when doses exceeding 10 g are used (344).…”

Section: Azolesmentioning

confidence: 98%

“…Unused solutions (139); no reports of use in ophthalmic mycoses Peak concn of 0.3 g/ml in serum after single oral dose of 200 mg (401); increased to 3.5 g/ml after 200 mg/day orally for 14 days (51) Concn of 200-250 g/g attained in rabbit corneas after topical application of itraconazole in balanced salt solution polyvinyl alcohol, boric acid, or olive oil (136) Detectable concn found to persist in rabbit corneas after subconjunctival administration (193) Commercially available capsule (100 mg) should be taken with meal; difficult to give in infants and children (124) May be poorly absorbed after oral administration in certain groups of patients (139) should be discarded after 24 h. Amphotericin B is both heat labile and light sensitive; hence, the dry powder should be refrigerated and protected from light (236). The recommended dosage is usually 1 mg/kg of body weight/day; smaller doses may be relatively ineffective (236).…”

Section: Polyenesmentioning

confidence: 99%

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Current Perspectives on Ophthalmic Mycoses

2003

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Fungi may infect the cornea, orbit and other ocular structures. Species of Fusarium, Aspergillus, Candida, dematiaceous fungi, and Scedosporium predominate. Diagnosis is aided by recognition of typical clinical features and by direct microscopic detection of fungi in scrapes, biopsy specimens, and other samples. Culture confirms the diagnosis. Histopathological, immunohistochemical, or DNA-based tests may also be needed. Pathogenesis involves agent (invasiveness, toxigenicity) and host factors. Specific antifungal therapy is instituted as soon as the diagnosis is made. Amphotericin B by various routes is the mainstay of treatment for life-threatening and severe ophthalmic mycoses. Topical natamycin is usually the first choice for filamentous fungal keratitis, and topical amphotericin B is the first choice for yeast keratitis. Increasingly, the triazoles itraconazole and fluconazole are being evaluated as therapeutic options in ophthalmic mycoses. Medical therapy alone does not usually suffice for invasive fungal orbital infections, scleritis, and keratitis due to Fusarium spp., Lasiodiplodia theobromae, and Pythium insidiosum. Surgical debridement is essential in orbital infections, while various surgical procedures may be required for other infections not responding to medical therapy. Corticosteroids are contraindicated in most ophthalmic mycoses; therefore, other methods are being sought to control inflammatory tissue damage. Fungal infections following ophthalmic surgical procedures, in patients with AIDS, and due to use of various ocular biomaterials are unique subsets of ophthalmic mycoses. Future research needs to focus on the development of rapid, species-specific diagnostic aids, broad-spectrum fungicidal compounds that are active by various routes, and therapeutic modalities which curtail the harmful effects of fungus- and host tissue-derived factors

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Section: Azolesmentioning

confidence: 98%

Section: Polyenesmentioning

confidence: 99%

Current Perspectives on Ophthalmic Mycoses

2003

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“…Fluconazole's uptake was shown to be quick, according to the results of fluconazole penetration. Most antifungal drugs cannot penetrate the corneal epithelium, which serves as a significant barrier (16) . Epithelial debridement can lead to significant issues, such as perforation or aggravation of the ulcer, especially in fragile corneas with fungal keratitis, even if the epithelium is intact and removal is desirable.…”

Section: Discussionmentioning

confidence: 99%

Effect of Sub-Conjunctival, Topical and Systemic Fluconazole On Refractory Fungal Keratitis

Elzlitni¹,

Elbarghathi²,

Abdullah³

2022

The Egyptian Journal of Hospital Medicine

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Background: About 40 to 50 percent of all instances of microbial keratitis are caused by fungal keratitis (FK). Untreated FK can lead to corneal damage and endophthalmitis, both of which can lead to irreversible vision loss. Since long-term consequences, including blindness, can be prevented by timely diagnoses and treatment of microbial keratitis, there is no laboratory support for this type of diagnosis. Some experts in the field of ophthalmology have long held that it is possible to discriminate between fungal and bacterial infections of the cornea using clinical indicators. The aim of the study: It was assessment of the efficacy and safety of topical and systemic and sub-conjunctival fluconazole treatment for refractory fungal keratitis. Patients and Methods: Eleven people with refractory fungal keratitis took part in this investigation. All cases were managed with topical fluconazole 2% hourly for 2 days, then tapered 5 times/day for one week, sub-conjunctival fluconazole 2mg/ml once for 14 days and oral fluconazole 150mg per week daily. The diagnosis was based on KOH wet mount and clinical signs of fungal keratitis. Result: The result was eight of patient successfully treated with visual acuity improvement and local nor systemic side effect were observed. Conclusion:Severe fungal keratitis can be treated with topical and systemic, sub-conjunctival fluconazole, which may reduce the need for surgical intervention.

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“…Subconjunctival injections can produce longstanding periocular inflammation and can lead to epithelial ulcerations; also, penetration into the aqueous humor is not adequate. 28 Thus, intracameral injections appear to be a better alternative for adequate drug delivery inside the anterior chamber with minimal intraocular toxicity. Foster et al 29 found that anterior chamber injection of up to 50 Kg amphotericin B did not cause corneal or lenticular toxicity.…”

Section: Discussionmentioning

confidence: 99%