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PubMed1997

The Guinea Pig Blinking Test: a comparison with human responses.

The Guinea Pig Blinking Test (2) was presented as a model for the selection and development of comfortable ocular formulations. This study compares human nociceptive responses and the blinking response of the guinea pig to different concentrations of a topically applied ophthalmic drug, sulfacetamide. The number of human subjects noting pain upon instillation of various concentrations of sulfacetamide (3) was compared to the blinking responses of guinea pigs treated with 2.5%-17.5% sulfacetamide. The number of blinks was counted over a period of 5 minutes following (1) saline (0.9% NaCl), and (2) 30-60 minutes later a test solution. A Blinking Index (B.I.) = blinks drug/blinks saline was calculated for each animal. The dose/response curves of both humans and guinea pigs were almost identical, showing a threshold at 5% sulfacetamide, followed by a linear increase, reaching a maximum at 12.5%-15% sulfacetamide. A 2.5% solution that elicited pain in 10% of human subjects yielded a B.I. = 1.04 +/- 0.05, whereas a 12.5% solution that elicited pain in 95% of human subjects yielded a B.I. = 1.61 +/- 0.13 (mean +/- S.E., n = 10, P < 0.05). The strong linear relationship between the guinea pig blinking response and the human perception of pain, following identical treatment with a topical ophthalmic drug, demonstrates that this animal test can be useful in predicting the degree of ocular discomfort of human subjects.

Adrenergic Agonists↗
PubMed1996

An ocular bioavailability comparison in rabbits of prednisolone acetate after repeated topical applications formulated as a high-viscosity gel and as an aqueous suspension.

To increase contact time between drug and ocular surface and thus improve the ocular bioavailability, we used the high-viscous, water-soluble polymer carbomer Leogel (carbomer 0.5%). We compared the bioavailability of prednisolone acetate 0.5% given in 1) Leogel using fusidic acid 1% with that obtained using 2) aqueous sulfacetamide sodium 10% as vehicle. We applied the drugs to Copenhagen white rabbits as repeated topical applications (gel preparation: twice daily; aqueous preparation: four times daily) for one week. Dosis regimen was chosen according to earlier investigations (Johansen et al. 1995). Prednisolone concentrations in cornea, conjunctiva and aqueous humour were shown to be higher using the Leogel vehicle than using the aqueous suspension. Fusidic acid and sulfacetamide sodium values were compared with values from a single application (Johansen et al. 1995). Fusidic acid reached higher concentration levels in cornea, conjunctiva and aqueous humour after repeated applications than after a single application. Sulfacetamide sodium concentrations did not rise when applied four times daily for one week. Leogel increases the ocular bioavailability of substance(s) in the gel and allows lower drug concentrations and/or application frequencies.

Administration, Topical↗
PubMed2003

Liquid chromatography-fluorescence detection for simultaneous analysis of sulfonamide residues in honey.

A rapid, accurate LC analytical method has been developed for determination of eight sulfonamides (sulfacetamide, sulfapyridine, sulfamerazine, sulfamethoxypyridazine, sulfameter, sulfachloropyridazine, sulfamethoxazole and sulfadimethoxine) in honey. The sample was dissolved in phosphoric acid solution (pH 2). After filtration, the sample solution was cleaned by use of two solid-phase extraction (SPE) cartridges-an aromatic sulfonic cation-exchange cartridge and an Oasis HLB cartridge. The eight sulfonamides were then derivatized with fluorescamine and the derivatives were determined by LC with fluorescence detection at excitation and emission wavelengths of 405 and 495 nm, respectively. Average recoveries at three fortification levels in the range 0.02-0.50 mg kg(-1) in twelve different kinds of honey were 73.5-94.1% with coefficients of variation of 4.35-16.60%. The limit of detection (LOD) was 0.002 mg kg(-1) for sulfacetamide, sulfapyridine, sulfamerazine, and sulfamethoxypyridazine; that for sulfameter, sulfachloropyridazine, sulfamethoxazole and sulfadimethoxine was 0.005 mg kg(-1). The limit of quantitation (LOQ) was 0.005 mg kg(-1) for sulfacetamide, sulfapyridine, sulfamerazine, and sulfamethoxypyridazine; that for sulfameter, sulfachloropyridazine, sulfamethoxazole, and sulfadimethoxine was 0.010 mg kg(-1). The method is suitable for determination of multiresidue sulfonamides in the various kinds of honey.

Anti-Infective Agents↗
PubMed2005

Monitoring of five sulfonamide antibacterial residues in milk by in-tube solid-phase microextraction coupled to high-performance liquid chromatography.

A simple, rapid, and sensitive method for the quantitative monitoring of five sulfonamide antibacterial residues in milk was developed by coupling in-tube solid-phase microextraction (SPME) to high-performance liquid chromatography with an ultraviolet detector. A poly(methacrylic acid-ethylene glycol dimethacrylate) monolithic capillary column was selected as the extraction medium for this on-line technique. To obtain optimum extraction efficiency, several parameters relating to in-tube SPME were investigated. By simple extraction with ethanol, dilution with phosphate buffer solution, and centrifugation, the sample solution then could be directly injected into the device for extraction. The calculated detection limits for sulfadiazine, sulfamethazine, sulfamethoxazole, sulfamonomethoxine sodium, and sulfacetamide sodium were 2.0, 2.8, 1.7, 2.5, and 22 ng/mL, respectively. The method was linear over the range of 20-5000 ng/mL (100-5000 ng/mL for sulfacetamide sodium) with a correlation coefficient R (2) value >0.9980. Excellent method reproducibility was found by intra- and interbatch precisions, yielding the relative standard deviations of <10.0 and <9.94%, respectively. The proposed method was proved to be robust in monitoring sulfadiazine, sulfamethazine, sulfamethoxazole, sulfamonomethoxine sodium, and sulfacetamide sodium residues in milk.

Animals↗
PubMed2003

Modification of Pseudomonas aeruginosa interactions with corneal epithelial cells by human tear fluid.

Both cytotoxic and invasive strains of Pseudomonas aeruginosa can damage corneal epithelial cells in vitro, but neither can infect healthy corneas in vivo. We tested the hypothesis that whole human tear fluid can protect corneal epithelia against P. aeruginosa virulence mechanisms. Cultured corneal epithelial cells were inoculated with 10(6) CFU of one of 10 strains of P. aeruginosa (five cytotoxic, five invasive)/ml with or without reflex tear fluid collected from the conjunctival sacs of human volunteers. Cytotoxicity was assessed by observation of trypan blue staining and measurement of lactate dehydrogenase release; invasion was quantified by using gentamicin survival assays. Tear fluid retarded growth of only 50% of the P. aeruginosa strains (three of five invasive strains, two of five cytotoxic strains) yet protected corneal cells against invasion by or cytotoxicity of 9 of 10 strains. The only strain resistant to the tear cytoprotective effects was susceptible to tear bacteriostatic activity. Dilution of tear fluid threefold significantly reduced cytoprotection, while bacteriostatic activity prevailed with dilutions beyond 100-fold. Sulfacetamide (1 mg/ml) with bacteriostatic activity matching that of tear fluid was less cytoprotective than tear fluid (80% protection with tear fluid, 48% with sulfacetamide). Video microscopy revealed bacterial chain formation in both tear fluid and sulfacetamide, but tear fluid also blocked bacterial swimming motility. After prolonged tear contact, bacteria regained normal growth rates, swimming motility, and cytotoxic activity, suggesting a breakdown of protective tear factors. Boiled tear fluid lost bacteriostatic activity and effects on bacterial motility but retained cytoprotective function. These results suggest that human tear fluid can protect corneal epithelial cells against P. aeruginosa virulence mechanisms in a manner not dependent upon bacteriostatic activity or effects on bacterial motility. Whether overlapping tear film components are involved in these defense functions is to be determined.

Animals↗
PubMedDate not supplied

Nocardia keratitis in a human immunodeficiency virus patient.

BACKGROUND: The development of Nocardia keratitis in a patient with human immunodeficiency virus infection is rare, and we could find no cases reported in the literature. CASE: A 48-year-old woman who had human immunodeficiency virus infection presented with decreased visual acuity, redness, and irritation in the right eye. OBSERVATIONS: Initially, the diagnosis was fungal keratitis, and she was treated with 0.3% amphotericin B eye drops and oral fluconazole for 1 month without improvement. Then, all former drugs were discontinued, and a corneal scraping was carried out. The culture result disclosed Nocardia asteroides, and after treatment with 10% sulfacetamide eye drops and oral trimethoprim-sulfamethoxazole, the keratitis subsided dramatically. CONCLUSIONS: The treatment result for Nocardia keratitis in a human immunodeficiency virus patient was favorable after intensive use of 10% sulfacetamide eyedrops. Nocardia keratitis should be kept in mind as a possible causative organism when antifungal therapy fails in a keratitis case.

Administration, Oral↗
PubMed1996

A bioavailability comparison in rabbits after a single topical ocular application of prednisolone acetate formulated as a high-viscosity gel and as an aqueous suspension.

To increase contact time between drug and ocular surface and thus improve the bioavailability, we used the high-viscous, water-soluble polymer carbomer Leogel (carbomer 0.5%). The drugs were applied to Copenhagen white rabbits as a single application. We compared the bioavailability of prednisolone acetate 0.5% in Leogel with fusidic acid 1% after 1, 4, 7 and 10 h (n = 3 at each time points) with that obtained when doubling the prednisolone acetate concentration in unchanged Leogel and fusidic acid 1% in 12 rabbits. In addition we compared the bioavailability of prednisolone acetate 0.5% given in 1) Leogel using fusidic acid 1% with that obtained using 2) aqueous sulfacetamide sodium 10% as vehicle after 0.5, 1, 1.5, 2, 3, 6, 8 and 12 h (n = 6 at each time points) in 54 rabbits. When doubling the prednisolone acetate dose an increase in bioavailability was achieved in conjunctiva, cornea and aqueous humour with 1.57, 3.86 and 2.18 times, respectively. Prednisolone concentrations in cornea, conjunctiva and aqueous humour were higher using the Leogel vehicle than using the aqueous suspension. The bioavailability in 0-12 h for prednisolone acetate in Leogel and fusidic acid 1% to conjunctiva was significantly higher (p = 0.003) than for prednisolone acetate in aqueous and sulfacetamide sodium 10%. The bioavailability (0-6 h) for conjunctiva was significantly higher for the Leogel preparation than for the aqueous suspension (p < 0.001). For cornea and aqueous humour, the bioavailability values for the total period (0-12 h) do not differ significantly. However, for the first 6 h the difference is significant (p < 0.001 for cornea and p = 0.003 for aqueous humour).

Administration, Topical↗
PubMed1977

Prophylactic antibiotics in cataract surgery.

The value of preoperative cultures, sensitivity tests and prophylactic preoperative antibiotic treatment was evaluated in a group of senile, uncomplicated lens extractions. Sulfacetamide or a mixture of chloramphenicol and polymixin were applied preoperatively for 1 week and an injection of penicillin and streptomycin was given postoperatively. A control group of 140 cases without treatment was also studied. No postoperative infections developed in either group. The number of pathogenic cultures was significantly smaller in the treated group as compared with the untreated one; the mixture of chloramphenicol and polymixin B sulfate was found to be superior to sulfacetamide, different clinical data was compared in the two groups. No postoperative infections developed in either group.

Aged↗
PubMed1999

Effects of eyelid scrubbing on the lid margin.

PURPOSE: To compare the effects of eyelid scrubbing with an eyelid cleansing solution (ECS) to eyelid scrubbing with ECS and the addition of antibacterial or anti-inflammatory pharmaceuticals on the clinical appearance, microbial status, tissue histology, and the inflammatory cell profile of the normal eyelid margin. METHODS: Eyelid scrubbing was performed twice daily using ECS; ECS with the antibacterial sulfacetamide (ECS+); and ECS with sulfacetamide and prednisolone acetate (ECS++) over a 21 day period on three groups of 16 rabbits with clinically normal eyelids. RESULTS: Significant hyperemia of the margin occurred in all three groups over the 3 week period; however, the degree of hyperemia was less with ECS+ (P<0.05) and ECS++ (P<0.05). Chemosis, tearing, mucus discharge, and the microbial status were not significantly different than controls. There were no marked histologic differences in the tissues, except for increased red blood cell packing in the small vessels near the lid margins in scrubbed eyelids, consistent with hyperemia. The inflammatory cell profile showed minimal changes that were not statistically significant in any of the three groups, except that >50% of mast cells showed evidence of degranulation. CONCLUSIONS: Use of ECS with an antibiotic, or an antibiotic and steroid solution, resulted in less inflammation than scrubbing with ECS alone.

Administration, Topical↗
PubMed2006

Toxicity and biodegradability of sulfonamides and products of their photocatalytic degradation in aqueous solutions.

The photocatalytic degradation of sulfacetamide, sulfathiazole, sulfamethoxazole and sulfadiazine in water solutions during their illumination of UV radiation (lambda(max) 366 nm) with TiO2 catalyst was examined. The growth-inhibition effect of sulfonamides and intermediate products theirs photodegradation was investigated in aqueous solution with the green alga Chlorella vulgaris. The biodegradability of the investigated compounds was determined in the illuminated solutions and is expressed as Biochemical Oxygen Demand. It was found that all of the investigated sulfonamides in the initial solutions were resistant to biodegradation and were toxic relative to C. vulgaris. The toxicity (EC50 values) relative to C. vulgaris increased in the following order sulfacetamide, sulfathiazole, sulfamethoxazole, sulfadiazine. All of the investigated sulfonamides undergo photocatalytic degradation. The toxicity of intermediate products of the sulfonamides degradation was significantly lower than the toxicity of sulfonamides in the initial solutions and was dependent on illumination time and degradation rate. The intermediate products of photocatalysis in contrast to the initial sulfonamides, might be mineralized using biological methods.

Biodegradation, Environmental↗
PubMed2002

Mycobacterium chelonae keratitis associated with soft contact lens wear.

PURPOSE: To report a case of Mycobacterium chelonae keratitis associated with soft contact lens wear. METHODS: A 17-year-old boy who wore frequent replacement soft contact lenses developed keratitis in the right eye. There was no history of trauma to the right eye. The patient was treated initially with topical ciprofloxacin but without improvement. On presentation, visual acuity in his right eye was 20/40. A Gram-stained scraping of the corneal infiltrate revealed beaded filamentous rods, and the organisms were acid-fast positive. The patient's right eye was treated with intensive topical amikacin, 20 mg/mL, and 10 % sulfacetamide. Eventually, Mycobacterium chelonae was cultured on Sabourard's agar, topical sulfacetamide was stopped, and amikacin was continued. RESULTS: The patient's keratitis responded well to amikacin and resolved over a period of 4 weeks. Visual acuity in the right eye improved to 20/25. CONCLUSIONS: Mycobacterium chelonae is a rare cause of keratitis in soft contact lens wearers. We have identified fewer than five cases of Mycobacterium chelonae keratitis associated with soft contact lenses in the literature. Prompt and accurate diagnosis of the organism using comeal scraping can lead to appropriate therapy and resolution of the keratitis.

Adolescent↗
PubMed1979

Conjunctivitis in children. A refresher survey of diagnosis and contemporary treatment.

The management of acute conjunctivitis need not be confusing. In the newborn period the common etiologic agents are chemical, TRIC, and bacterial. The latter two causes are effectively treated with sulfacetamide ophthalmic preparations. Dacryostenosis should be suspected in any child with recurrent conjunctivitis in the first six months of life. With older children the major causes can be classified as viral, allergic, foreign bodies, and bacterial. Bacterial conjunctivitis almost always responds to sulfacetamide ophthalmic preparations.

Anti-Bacterial Agents↗
PubMed2003

Topical acne drugs: review of clinical properties, systemic exposure, and safety.

This review examines the commonly available topical acne agents and factors that determine their percutaneous absorption. Reported and theoretical adverse effects from systemic exposure are detailed. The topical retinoid class, which includes tretinoin, adapalene and tazarotene, and the topical antibacterials, clindamycin and erythromycin, are regulated by prescription in most countries. Used appropriately, the above-mentioned drugs deliver, at most, miniscule amounts of active ingredient into the circulation. Clear-cut links to systemic toxicity in humans are practically nonexistent, except in the case of topical clindamycin, which has been associated with diarrhea rarely, and there have been 2 cases of pseudomembranous colitis reported. Birth defects have occurred in two patients treated with tretinoin and one patient treated with adapalene, but causation was not proven. Another prescription drug, 20% azelaic acid, is associated with relatively high systemic exposure, which is presumed innocuous because it is a normal dietary constituent whose endogenous levels are not altered by topical use. Benzoyl peroxide, salicylic acid, sulfur, and sodium sulfacetamide are available in concentrations of 2% or more in over-the-counter acne treatments and some prescription products. All of these agents are known to exhibit some degree of percutaneous absorption. They remain largely unregulated because, other than skin irritation, only local allergic contact dermatitis from benzoyl peroxide in about 2.5% of patients and rare local and systemic hypersensitivity reactions from sodium sulfacetamide have been reported. Salicylism has occurred using methyl salicylate ointments and high concentrations of salicylic acid on widespread areas of hyperkeratotic skin, but there are no known cases resulting from salicylic acid acne products. Caution is advised in special circumstances, such as during childhood, pregnancy, lactation and concomitant therapy with other drugs, because relevant studies are lacking. Animal data support avoidance of many topical agents, particularly known teratogens such as retinoids and salicylic acid, in pregnant women. Salicylate avoidance is advised during lactation, because aspirin use carries the risk of bleeding disorders in nursing infants.

Acne Vulgaris↗
PubMed1979

Spectrophotometric analysis of binary mixtures of sulfonamides.

Different methods for analyzing binary mixtures by using 2 wavelengths are reviewed. The absorbance ratio calculated at 2 wavelengths, not including the isoabsorptive point, was a quadratic function of relative concentration. The curve-fitting process using orthogonal polynomials was applied to obtain the quadratic equation. An absorbance ratio can be used as a rapid purity index for sulfacetamide sodium in the presence of sulfanilamide. Sulfacetamide sodium has been determined in eye drop preparations.

Ophthalmic Solutions↗
PubMed1979

Meningococcal conjunctivitis.

Meningococcal conjunctivitis is typically described as an acute purulent infection. An atypical case of mild catarrhal conjunctivitis occurred in a 19-year-old college student. The meningococci were identified as Neisseria meningitidis, group A, and were isolated from the throats of the patient and her roommate. The conjunctivitis responded rapidly to treatment with sodium sulfacetamide, and it was not treated systemically. A short review of the literature of meningococcal conjunctivitis is presented, and the current recommendation for prophylaxis is discussed.

Administration, Topical↗
PubMed1988

Ototoxicity of Vasocidin drops applied to the chinchilla middle ear.

Some widely used ototopical preparations are potentially toxic to the middle and inner ear. Vasocidin Ophthalmic Solution (sulfacetamide sodium and prednisolone sodium phosphate) has been advocated as an alternative agent that may have fewer toxic side effects in the treatment of otorrhea. Vasocidin was introduced into the bullae of nine chinchillas to investigate the effects on the middle and inner ear. The organ of Corti and stria vascularis were found to be entirely normal in 17 of the 18 temporal bones studied. Changes observed in the middle ears at one week included inflammation, hemorrhage, and effusion. Examination of specimens at four weeks revealed resolution of most of the inflammatory changes. The results of this experimental study indicate that Vasocidin causes reversible middle ear inflammation with little or no toxic effect on inner ear structures.

Animals↗
PubMed1978

Facile separation of sulfonamides from their degradates by liquid--liquid extraction.

Regulation of acidity for protonation of the free N4-amine can provide for the selective liquid--liquid extraction isolation of a sulfonamide from its degradation products. This principle is applied for the stability-indicating determination of sulfacetamide in the presence of sulfanilamide, sulfaquinoxaline in feed, and sulfabromomethazine in dosage forms. In solution, sulfabromomethazine can exhibit photodecomposition to sulfamethazine. The mean relative errors of the these methods and the precision, represented by relative standard deviations, are each typically less than 2%.

Animal Feed↗
PubMedDate not supplied

Ocular nocardia infections with special emphasis on the cornea.

Nocardia are aerobic, gram-positive, nonmotile and branching filamentous bacteria. Corneal infection by Nocardia is rare. Trauma is the most common predisposing factor. Isolated case reports of nocardial infection associated with contact lens wear and laser in situ keratomileusis (LASIK) have been reported. The clinical picture usually consists of superficial patchy infiltrates, which may be arranged in a wreath pattern. Presence of gram-positive, branching, beaded filaments that stain with 1% acid-fast stain (using 1% sulfuric acid, modified Kinyoun's method) in smears of corneal scrapings is suggestive of nocardial infection. Nocardia grow on commonly used media as tiny, white, dry colonies. Available knowledge and clinical experience suggest that although sulfacetamide eyedrops can be tried as the initial drug, trimethoprim-sulfamethoxazole and amikacin are effective drugs. Once therapy is initiated, the infiltrate responds promptly and resolves, forming a corneal scar with or without vascularization, and good visual recovery can be expected.

Anti-Bacterial Agents↗