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PubMed2003

Determination of prednisolone and the most important associated compounds in ocular and cutaneous pharmaceutical preparations by micellar electrokinetic capillary chromatography.

A micellar electrokinetic capillary chromatographic method to separate prednisolone, prednisolone acetate, naphazoline, Zn-bacitracin, sulfacetamide and phenylefrine is described. The separation was carried out by using a fused-silica capillary (57 cmx75 micrometer I.D.) at 25 degrees C and 30 kV, using a 5 mM phosphate-5 mM borate buffer adjusted to pH 8.2, 50 mM sodium dodecyl sulfate (SDS) and 10% methanol-water (v/v) as background electrolyte. Under these conditions, the run time was 8 min and the limits of quantification were about 1.0 mg/l for every component. The method was applied to pharmaceutical preparations and the results provided recoveries close to 100% and the method gave good results when compared with a reference multivariate calibration spectrophotometric method.

Calibration↗
PubMed2006

Broad-specificity immunoassays for sulfonamide detection: immunochemical strategy for generic antibodies and competitors.

Development of antibodies with broad specificity recognition for sulfonamide drugs was found to be surprisingly difficult when conventional immunochemical strategies were applied to hapten design. To improve the cross-reactivity pattern of antibodies for the family of sulfonamide drugs, a novel strategy based on the single-ring (fragment-derived) hapten moieties with different spacer substituent lengths was employed for the preparation of immunogens, coating conjugates, and enzyme competitors. The rabbit antibodies raised against a common (one-ring) p-aminobenzenesulfonamide hapten moiety (attached to a carrier protein through the N-1 position) in combination with a homologous hapten-peroxidase tracer allowed the detection of 15 sulfonamide species at the maximum residue limit level using direct ELISA. The two-ring 6-(4-aminobenzensulfonylamino)hexanoic hapten mimics, previously reported in the literature as a weak generic antigen, generated surprisingly superior immune responses in rabbits. The antibodies raised against this two-ring hapten were capable of detecting at least 19 and 17 sulfonamides in a direct ELISA system at the regulatory level with sensitivities corresponding to 20 and 50% binding inhibition, respectively. A negligible cross-reaction with N4 metabolites makes it possible to measure responses of parent sulfonamides in the presence of their metabolized forms. In skimmed milk, the highest limit of detection (LOD) for sulfacetamide defined as 20% inhibition was 65.2 microg x L(-1) (IC20 value), whereas the additional 18 sulfonamides tested exhibited LODs in the range of 0.2-36.8 microg x L(-1). This sensitivity allows simple multisulfonamide tests to be established for use in the laboratory or on site.

Animals↗
PubMed1983

Microsomal incubation test of potentially hemolytic drugs for glucose-6-phosphate dehydrogenase deficiency.

The in vitro metabolizing method was modified and its ability to correctly identify eight known hemolytic and nine known nonhemolytic drugs of glucose-6-phosphate (G6PD)-deficient erythrocytes was evaluated. The technique is based on inducing in vitro drug metabolism by incubation of red cells and drug with a reduced NADP-generating system in the presence of phenobarbital-induced mouse liver microsomes. Thus, this system provides a model for in vivo metabolic function. The hemolytic potential of tested drugs is indicated by the extent of loss of reduced glutathione of G6PD-deficient erythrocytes during 60-min incubations. Complete agreement between the test and literature for nonhemolytic compounds was observed. The test also correctly identified six of the eight known hemolytic drugs and failed to identify two known hemolytic drugs (acetanilide and sulfacetamide). The test was also applied to 14 drugs about which there is uncertainty regarding hemolytic potential. Of the latter, DL-alpha-methyldopa; alpha-naphthol; beta-naphthol; 2,3, dimercaptopropanol; phenacetin; and menadione were found to react positively. We conclude that this in vitro assay system will be useful in predicting which new drugs will be hemolytic in G6PD-deficient patients.

Animals↗
PubMed1992

Lenticular uptake and distribution of xenobiotics and amino acids.

The objective of this study was to explore the relationship between lipophilicity and the lenticular uptake of radiolabeled xenobiotics. The lenticular uptake of amino acids was also investigated. An organ-culture technique was employed and the partitioning of compounds into the rabbit lens was measured for compounds with log octanol/water partition coefficients (log P o/w) ranging from -1 to 7.3. Drug distribution in the lens was expressed as the concentration ratio of that in the lenticular section (capsule/epithelium, cortex, and nucleus) to that in the incubation medium, (C(lens) section/Cm). The drug partitioning into the lens capsule was facile for all of the compounds tested. The drug concentrations in the lens capsule were higher than those in the cortical and nuclear regions. For compounds with low partition coefficients (such as sulfacetamide and cimetidine), an apparent distribution equilibrium was achieved during a 5-hr period. The C(lens)/Cm value of polar compounds, being less than one, did not further increase by prolonging the incubation period. Only compounds with log Po/w values between 3 and 6 had Cnucleus/Cm values exceeding unity. The maximal values of Ccortex/Cm and Cnucleus/Cm, approximately 15 and 4, respectively, for anthracene (log Po/w = 4.5) and diethylstilbestrol (log Po/w = 5.1), were observed in this study. A bell-shaped relationship was observed between the lenticular uptake rate and drug lipophilicity, of which the maximum occurred around log Po/w of 4. These results indicate the existence of a lipophilicity window for favorable drug distribution into the deeper region of the lens. For several lipophilic compounds, such as padimate-O, values of Cnucleus/Cm increased steadily over a 24-hour incubation period. This suggests that the nucleus behaved as a deep compartment for these compounds. L-Cysteine and L-serine were actively taken up by the lens and the lenticular absorption of L-cysteine was concentration-dependent with Vmax and Km values of 18.3 mumol/gm/hr and 49.8 mM, respectively. In summary, a relationship between lenticular uptake and drug lipophilicity was demonstrated. The optimal log Po/w value for drug uptake into the lens was between 4 and 5. The slowness of reaching significant drug concentrations in the nucleus necessitates a chronic dosing regimen to deliver therapeutic drug levels inside the lens.

Amino Acids↗
PubMed1979

Pseudogonococcal ophthalmia neonatorum. Branhamella (Neisseria) catarrhalis conjunctivitis.

A culture from conjunctivitis occurring in a neonate in association with a recurrent fever yielded a nearly pure growth of Branhamella (Neisseria) catarrhalis. The conjunctivitis was not appreciated and effectively treated until a second hospitalization in the fourth week of life. Partial suppression of symptoms had followed short-term parenteral antibiotic therapy during the first admission. Resolution quickly occurred in response to instillation of sodium sulfacetamide ophthalmic solution. Although B. catarrhalis is considered a non-pathogen, the literature reviewed included a number of diverse infections, but no previous instance of conjunctivitis. The organism's close similarities to Neisseria gonorrhoeae necessitate isolation and correct biochemical differentiation. Misdiagnosis of gonococcal conjunctivitis carries obvious social, psychological and medical impact.

Conjunctivitis↗
PubMed1978

Evidence that glucose starvation-sensitive mutants are altered in the relB locus.

Genetic mapping studies indicate that the relaxed-control mutants isolated on the basis of sensitivity to glucose starvation contain lesions in the relB locus. These mutants, which are sensitive to protein synthesis inhibitors such as sulfacetamide, exhibit relaxed control of both RNA and phospholipid syntheses.

Chromosome Mapping↗
PubMed1984

Prediction of blood levels following oral administration of weakly acidic drug particles such as sulfa drugs in rabbits from the in vitro dissolution behavior.

Prediction of blood levels following oral administration of weakly acidic drug particles such as sulfa drugs from data obtained in in vitro dissolution tests of drug suspensions was studied in the rabbit. The relationship between in vivo and in vitro dissolution rates or between absorption rate and in vitro dissolution rate was investigated. The drug absorption from aqueous solution was suggested to be rate-limited by the gastric emptying rate because the initial absorption rate constant in a biexponential time course of aqueous solution for the amount unabsorbed vs. time plot was almost the same among 9 of the 10 drugs tested, except for sulfacetamide. This indicated that when the in vivo dissolution rate constant is much slower than the initial absorption rate constant of aqueous solution, the time course of blood levels for the solid drug will deviate from that of aqueous solution. Based on the consideration, the critical in vitro dissolution rate constant corresponding to the initial absorption rate constants of aqueous solution was calculated by means of statistical analysis using the relationship between in vivo and in vitro parameters. The validity of this prediction was examined using four high-solubility drugs, and it was found that the prediction could be done whether the in vitro dissolution medium was distilled water or 0.1 N HCl solution. Although in the present study, the experiment was done using an aqueous suspension form in the rabbit, the applicability of this prediction method to other dosage forms and to the case of humans is discussed.

Absorption↗
PubMed1979

Detection of mitotic and meiotic aneuploidy in the yeast Saccharomyces cerevisiae.

A number of genetic systems are described which involve the use of the yeast Saccharomyces cerevisiae. The systems may be used to detect the production of aneuploid cells produced during both mitotic and meiotic cell division in the presence of genetically active chemicals. During mitotic cell division, monosomic colonies (2n - 1) may be detected by plating upon selective medium. Increases in such monosomic colonies are produced by exposure of cells to a number of chemical mutagens such as ethyl methane-sulfonate and mitomycin C. More importantly, monosomic colonies are also induced by nonmutagens such as sulfacetamide and saccharin, which suggests that such chemicals are capable of inducing aneuploidy (aneugenic) in the absence of mutagenic activity. Genetic analysis of aneuploid colonies produced on nonselective medium indicate that at least a proportion of the monosomic colonies were the result of mitotic nondisjunction. During meiotic cell division, disomic cells (n + 1) produced by chromosome nondisjunction may be detected by plating on selective media. The frequency of disomic cells has been shown to increase after exposure to p-fluorophenylalanine.

Aneuploidy↗
PubMedDate not supplied

Corneal ulceration due to Shigella flexneri.

Shigella keratitis with ulceration is a rare occurrence with only four previous reports in the literature. Corneal ulceration appears to be characteristically superficial with a predilection for the inferior cornea. In the case reported here, resolution of ulceration occurred with the use of gentamicin and chloramphenicol, following a poor response to sulfacetamide. Experimental evidence strongly suggests that the course of infection is usually self-limited but that corneal scarring is a common sequelae. In the majority of the clinical cases reported to date, corneal ulceration has responded to appropriate antimicrobials with resolution, but has left residual opacification. To the extent that all of the cases were in young children, assessment of the degree of visual loss has been difficult to ascertain.

Child, Preschool↗
PubMed2003

Trends in ophthalmic antimicrobial utilization pattern in Bahrain between 1993 and 2000: a resurgence of chloramphenicol?

OBJECTIVES: The occurrence of aplastic anemia following topical administration of ophthalmic chloramphenicol is controversial and debated internationally. We have determined the influence of such debate on the utilization of ophthalmic chloramphenicol in Bahrain, through studying the utilization patterns of ophthalmic antimicrobial preparations by the Ministry of Health, with an emphasis on chloramphenicol, between 1993 and 2000. Cost-implications of these patterns are examined. MATERIAL AND METHODS: Information on the annual purchase of ophthalmic antimicrobial drug preparations and their unit price was obtained from the Directorate of Materials Management, Ministry of Health, and analyzed. RESULTS: In 1993, the 3 most commonly purchased ophthalmic antibacterial preparations were oxytetracycline 1% eye ointment (40.1%); sulfacetamide 10% and 20% eye drops (25.3%); and chloramphenicol 0.5% eye drops and 1% eye ointment (10.8%). In 2000, oxytetracycline remained the most frequently purchased preparation (33%), followed by chloramphenicol (21.2%). Between 1993 and 1999, chloramphenicol purchases fluctuated between 10% to 16.4% with a remarkable increase to 21.2%, in 2000. Chloramphenicol accounted for 8.6% and 15.1% of cost of total ophthalmic preparations purchased in 1993 and 2000, respectively. CONCLUSION: Despite continued concerns of potential risks of ophthalmic chloramphenicol, this preparation is extensively utilized in Bahrain. We are of the opinion that for minor infections, chloramphenicol ophthalmic preparations should be replaced by safer alternatives. Further, we recommend that their use be reserved for ocular infections that are resistant to other antimicrobials, and that ophthalmologists, at the secondary care level, should supervise such treatment.

Administration, Topical↗
PubMed1999

Otorrhea after insertion of silver oxide-impregnated silastic tympanostomy tubes.

BACKGROUND: Silver oxide-impregnated tympanostomy tubes have been shown to decrease the incidence of postoperative otorrhea, but without a significant effect in the first postoperative week. OBJECTIVE: To evaluate prospectively our results with silver oxide-impregnated tympanostomy tubes and to identify factors associated with a higher incidence of early postoperative otorrhea. DESIGN: Prospective nonrandomized study. SETTING: University referral center. PATIENTS AND OTHER PARTICIPANTS: Six hundred thirty patients with chronic otitis media with effusion or recurrent otitis media. INTERVENTIONS: Silver oxide-impregnated Silastic tympanostomy tubes were inserted in 1254 ears. Subjects with mucoid or purulent effusions or blood at the myringotomy site at surgery were treated with topical antibiotic prophylaxis (sulfacetamide sodium-prednisolone acetate or neomycin sulfate-polymyxin B sulfate-hydrocortisone) for 5 days after tympanostomy tube placement. MAIN OUTCOME MEASURES: Incidence of otorrhea after tympanostomy tube insertion at 1 week and 1, 3, 6, 9, and 12 months after surgery. RESULTS: The overall incidence of postoperative otorrhea was 1.9%. The incidence of otorrhea in the first postoperative week was 5.6%; the incidence of otorrhea after the first postoperative week was 1.2% (P<.001). Within the first postoperative week, a significantly greater incidence of otorrhea was noted in patients younger than 3 years (7.8%), in patients with mucoid effusions at surgery (8.6%), and in patients younger than 3 years with mucoid effusions at surgery (15.2%). CONCLUSIONS: Silver oxide-impregnated tympanostomy tubes are associated with a low overall incidence of postoperative otorrhea. A significantly higher incidence of otorrhea is seen during the first postoperative week, compared with the incidence after the first week. Patients with thick middle ear effusions and age younger than 3 years have a significantly greater incidence of early otorrhea after tympanostomy tube placement.

Anti-Infective Agents↗
PubMed2000

Treatment of seborrheic dermatitis.

Seborrheic dermatitis is a chronic inflammatory disorder affecting areas of the head and trunk where sebaceous glands are most prominent. Lipophilic yeasts of the Malassezia genus, as well as genetic, environmental and general health factors, contribute to this disorder. Scalp seborrhea varies from mild dandruff to dense, diffuse, adherent scale. Facial and trunk seborrhea is characterized by powdery or greasy scale in skin folds and along hair margins. Treatment options include application of selenium sulfide, pyrithione zinc or ketoconazole-containing shampoos, topical ketoconazole cream or terbinafine solution, topical sodium sulfacetamide and topical corticosteroids.

Dermatitis, Seborrheic↗
PubMed2001

Are 2 combined antimicrobial mechanisms better than 1 for the treatment of acne vulgaris? Clinical and antimicrobial results of a topical combination product containing 1% clindamycin and 5% benzoyl peroxide. Introduction.

Acne vulgaris is the most common chronic skin condition seen by dermatologists. Available topical therapies include comedolytic agents such as tretinoin, adapalene, azelaic acid, tazarotene, and salicylic acid; bactericidal agents such as benzoyl peroxide; antibiotics such as clindamycin, erythromycin, and tetracycline; and anti-inflammatory agents such as sodium sulfacetamide and metronidazole. Therapeutic failure with some antibiotic regimens due to the presence or development of resistant strains is becoming an increasing problem in the treatment of acne. One strategy aimed at limiting the resistant Propionibacterium acnes population is the use of treatment regimens that incorporate agents with complementary but different mechanisms of action. A combination gel consisting of 5% benzoyl peroxide and 1% clindamycin has recently become available. This supplement summarizes the dermatopharmacology, clinical efficacy, and tolerability of this combination gel, along with its potential role in the management of acne vulgaris.

Acne Vulgaris↗
PubMedDate not supplied

A new, sensitive, and rapid spectrophotometric method for the determination of sulfa drugs.

A sensitive, rapid, and simple spectrophotometric method is described for the determination of sulfa drugs. The method is based on the formation of a red-colored product by the diazotization of sulfonamides such as sulfathiazole (SFT), sulfadiazine (SFD), sulfacetamide (SFA), sulfamethoxazole (SFMx), sulfamerazine (SFMr), sulfaguanidine (SFG), and sulfamethazine (SFMt), followed by complexation with dopamine in the presence of molybdate ions in (1 + 1) H2SO4 medium. Absorbance of the resulting red product is measured at 490-510 nm, and the product is stable for 2 days at 27 degrees C. Beer's law is obeyed in the concentration range of 0.04-8.0 microg/mL at the wavelength of maximum absorption. The method was used successfully for the determination of some sulfonamides in tablets and eye drops. Common excipients used as additives in pharmaceuticals do not interfere in the proposed method. The method offers the advantages of simplicity, rapidity, and sensitivity without the need for extraction or heating. The limits of detection and quantitation were calculated for SFT, SFD, SFA, SFMx, SFMr, SFG, and SFMt.

Anti-Infective Agents↗
PubMed1976

Stevens-Johnson syndrome from ophthalmic sulfonamide.

A 71-year-old man, who had a history of a previous bullous drug reaction to a sulfonamide, began receiving an ophthalmic preparation that contained sulfacetamide sodium. The patient received only the ophthalmic sulfonamide, and it was used for one day, but he developed Stevens-Johnson syndrome. This is believed to be the first reported case of Stevens-Johnson syndrome caused by an ophthalmic sulfonamide. The sulfonamides are the best verified drug-trigger for erythema multiforme and Stevens-Johnson syndrome.

Aged↗
PubMed1992

Bilateral dacryocystitis after punctal occlusion with thermal cautery.

A 61-year-old woman developed acute bilateral dacryocystitis secondary to Staphylococcus aureus 3 weeks after undergoing punctal occlusion with thermal cautery for keratoconjunctivitis sicca. The dacryocystitis resolved with intravenous antibiotics, aspiration of the lacrimal sacs, injection of sulfacetamide into the lacrimal sacs, and bilateral dacryocystorhinostomy. Preexisting bilateral nasolacrimal duct obstruction was postulated as the underlying cause. In these cases, irrigation of the lacrimal system is recommended before proceeding with punctal occlusion.

Anti-Bacterial Agents↗
PubMed2004

Diagnosis and treatment of acne.

Acne can cause significant embarrassment and anxiety in affected patients. It is important for family physicians to educate patients about available treatment options and their expected outcomes. Topical retinoids, benzoyl peroxide, sulfacetamide, and azelaic acid are effective in patients with mild or moderate comedones. Topical erythromycin or clindamycin can be added in patients with mild to moderate inflammatory acne or mixed acne. A six-month course of oral erythromycin, doxycycline, tetracycline, or minocycline can be used in patients with moderate to severe inflammatory acne. A low-androgen oral contraceptive pill is effective in women with moderate to severe acne. Isotretinoin is reserved for use in the treatment of the most severe or refractory cases of inflammatory acne. Because of its poor side effect profile and teratogenicity, isotretinoin (Accutane) must by prescribed by a physician who is a registered member of the manufacturer's System to Manage Accutane-Related Teratogenicity program.

Acne Vulgaris↗