Safety evaluation of selenium sulfide antidandruff shampoos.
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Administration, Oral↗
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The effects of ophthalmic preservatives on corneal epithelium of the rabbit: a scanning electron microscopical study.
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Animals↗
Benzalkonium chloride and bronchoconstriction.
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Albuterol↗
Evaluation of ocular hypersensitivity to dipivalyl epinephrine by component eye-drop testing.
Dipivalyl epinephrine (dipivefrin) is a prodrug of epinephrine used for topical glaucoma therapy. Local side effects have been noted in approximately 20% of patients treated and include conjunctival hyperemia, foreign body sensation, and follicular conjunctivitis. We studied five patients with adverse local reactions to dipivefrin (Propine) eye drops. Propine contains the following: dipivefrin, 0.1%; mannitol, 1.89%; sodium metabisulfite, 0.075%; disodium edetate, 0.0127%; and benzalkonium chloride, 0.004%. Since the reactions could conceivably have been caused by an ingredient other than dipivefrin, we first patch tested the patients with the maximum recommended concentration of each ingredient. All patch tests were negative. Sterile ophthalmic solutions of each individual component at the concentrations used in the commercial product were then prepared. In a double-blinded study, the patients applied two drops of each preparation, twice daily for 1 week, with a 1-week, drug-free period between trials. Dipivefrin alone reproduced each patient's initial Propine-induced conjunctivitis; symptoms occurred unilaterally in one patient and bilaterally in the other four patients. This study indicates that testing with single component eye drops can identify the provocative component in ocular drug hypersensitivity and that these reactions can be unilateral.
Adult↗
A combined respiratory and cutaneous hypersensitivity syndrome induced by work exposure to quaternary amines.
The quaternary amine, benzalkonium chloride, has been associated with cutaneous and mucosal delayed hypersensitivity reactions and with paradoxical bronchoconstriction after use of aerosolized asthma medications. Until now, quaternary amines have not been reported to cause occupational asthma. We describe a case of occupational asthma caused by prolonged exposure to a cleaning solution containing benzalkonium chloride in the workplace. Single-blind, placebo-controlled, open-room challenges were performed to determine the specific agent responsible for the patient's symptoms. Pulmonary function and epicutaneous challenge tests were also performed. The patient had positive responses to challenges with a liquid toilet bowl cleaner containing benzalkonium chloride but was unreactive to other agents tested. Removal from the workplace resulted in complete resolution of symptoms. The exact mechanisms responsible for occupational asthma induced by quaternary amines remain unknown; however, this case emphasizes the importance of recognizing reactive chemicals as possible causes.
Adult↗
An improved method for bonding heparin to intravascular cannulae.
The patency of chronically implanted intravascular cannulae is usually limited by thrombus formation at the cannula tip. In the present experiments, methods of improving the antithrombotic properties of the cannulae have been examined using a number of different heparin-bonding treatments. These treatments were evaluated by determining cannula patency in the thoracic aorta of a chronically cannulated rat preparation. Cannulae treated with a heparin-bonding procedure remained patent longer than untreated cannulae. Cannulae treated with tridodecylmethylammonium chloride-heparin-glutaraldehyde remained patent longest (mean patency, 13.3 days compared with 4.0 days in rats with untreated cannulae). This technique provides a simple and effective method of improving the antithrombotic properties of intravascular cannulae by bonding heparin to the lumenal and extralumenal surfaces.
Animals↗
Light-induced genetic toxicity of thimerosal and benzalkonium chloride in commercial contact lens solutions.
Several commercial solutions used for daily care of contact lenses were tested for mutagenicity in 4 strains of Salmonella and for their ability to induce repairable DNA damage in the E. coli DNA polymerase A- assay. 5 of the 13 solutions tested were positive in the polymerase A- assay. These products demonstrated an increased level of genetic toxicity when the assay was conducted under conditions of illumination with visible light. Investigation of the genetic toxicity of some of their components, specifically the preservatives, indicated that thimerosal and benzalkonium chloride were capable of causing repairable DNA damage. Thimerosal was active only when the plates were incubated under conditions of illumination, and thus was light-induced. Benzalkonium chloride was active under conditions of dark incubation, and its genetic toxicity was enhanced when the plates were irradiated with visible light. These results were confirmed in a parallel experiment, in which cells were treated with the test agent and irradiated for a short period in liquid culture and viable cells then determined. None of the commercial products and none of the components tested, were mutagenic in the Salmonella assay.
Baths↗
Neuraminidase- and benzalkonium chloride-dependent inhibition of basic peptide-induced rat mast cell secretion.
Two types of inhibition of basic peptide-induced rat mast cell secretion are reported. Pretreatment of rat peritoneal mast cells with Vibrio comma neuraminidase, an enzyme which cleaves sialic acid from oligosaccharides, led to inhibition of 5-hydroxytryptamine release induced by the basic peptides polylysine, corticotropin 1-24 and a decapeptide sequence of human IgE. Inhibition was similarly observed when mast cells were challenged in the presence of the cationic cell membrane-active substance benzalkonium chloride. It is postulated that both of these experimental procedures inhibit basic peptide-induced secretion by depletion of cell surface negative charge. Sialic acid itself does not act as a specific receptor for basic peptides, since a molar excess of sialic acid in free solution failed to inhibit secretion by binding to basic peptides in the fluid phase.
Animals↗
The mechanism of inhibition of alkylamines on the mast-cell peptidergic pathway.
GTP-binding proteins are known to play an important role in controlling mast-cell exocytosis and are described as the primary targets of peptidic mast-cell histamine releasers. The mechanism of inhibition of the mast-cell peptidergic pathway by alkylamines, which are selective inhibitors of this pathway, was investigated using intact or permeabilized rat peritoneal mast cells. Histamine release induced by GTP gamma S and by mastoparan (a venom peptide activating G proteins) was inhibited by pretreating mast cells with 0.1 to 3 micrograms/ml of a mixture of benzalkonium chloride containing in majority a twelve-carbon-atom aliphatic chain (BAC(C approximately 12)). Pure benzalkonium chloride, with a fourteen-carbon-atom aliphatic chain (BAC (C14)), at 5 to 10 microM also inhibited histamine release induced by GTP gamma S and mastoparan. The dose-response curve of mastoparan-induced histamine release from intact mast cells was shifted to the right by various concentrations of BAC (C14). Similar results were obtained with another alkylamine differing from BAC (C14) by the absence of the benzene ring, tetradecyltrimethylammonium bromide, TAB (C14). This illustrates that the presence of the phenyl radical is not required for the inhibitory effect of benzalkonium chloride. BAC (C approximately 12) and BAC (C14) inhibited the generation of inositol polyphosphates induced by GTP gamma S. BAC (C approximately 12) and TAB (C14) inhibited the mastoparan-stimulated GTPase activity from mast-cell Gi-like proteins. These results suggest that alkylamines exert selectively their inhibitory effect via an interaction with mast-cell Gi-like proteins coupled to phospholipase C, i.e., at an early stage in the stimulus-secretion coupling process.
Benzalkonium Compounds↗
An experimental evaluation of antiseptic wound irrigation.
An experimental wound infection model was used to assess the value of four proprietary antiseptics applied topically in preventing the development of wound sepsis. Irrigation of wounds with either saline or noxytiolin 15 min after contamination with Staphylococcus aureus did not reduce either the incidence or degree of infection. Benzalkonium chloride and, to a lesser degree, povidone-iodine significantly reduced the infection rate, but were inferior to chlorhexidine gluconate which eliminated all overt signs of infection. The rate of healing of the chlorhexidine-treated, contaminated wounds was found to be no different from control non-infected wounds. When irrigation was carried out 45 min before wounds were contaminated, chlorhexidine was the only treatment which reduced the rate of infection (P less than 0.001). It is concluded that the superior activity of chlorhexidine in this model is a good indication that it should be a highly effective agent in the prevention of staphylococcal wound infection, and that this is probably due to a combination of bactericidal and persistent action together with low toxicity.
Animals↗
Enteric neuronal ablation: structure-activity relationship in a series of alkyldimethylbenzylammonium chlorides.
Serosal application of a commercial solution of benzalkonium chloride (BAC) has been shown to selectively ablate myenteric neurons in the rat jejunum. This experimental model has proven useful in the study of the role of the myenteric plexus in intestinal function. The commercial BAC is a mixture of at least three homologous N-alkyldimethylbenzylammonium chlorides (ADBAC). The purpose of this study was to determine neuronal ablative activity in a series of ADBAC homologs when applied on the serosa of rat jejunum. Homologs not commercially available were synthesized and purified. Seven ADBAC homologs with alkyl chain lengths ranging from C6 to C18 were tested. A solution of each homolog (2 mM in saline) was applied directly on the serosa of an exteriorized portion of jejunum from anesthetized rats. Fifteen days after treatment, animals were sacrificed and treated tissues were processed for neuronal cell counts and muscle thickness determinations. All ADBAC homologs, except C18, ablated neurons of the myenteric plexus and produced thickening of intestinal smooth muscle. The number of submucosal neurons was not affected by any of the homologs. The structure-activity relationship observed in this study paralleled that of the reported antimicrobial activity of the ADBAC homologs, and is related to the aqueous solubility and relative surface activities of the homologs. The C14 homolog was found to be the most effective ablative agent, and reduced the number of myenteric neurons in a concentration-dependent manner. Thus, the C14 homolog can be used to produce a selectively denervated jejunal model for use in acute or chronic in vitro or in vivo studies of intestinal function.
Animals↗
Development of an ocular irritation test in the mouse: image analysis of corneal lesions.
An ocular irritation test in the mouse has been developed, in which corneal lesions consecutive to instillation of ophthalmic preparations are assessed by digital image processing. The high sensitivity of this method makes it possible to test very low (i.e. therapeutic) concentrations, which do not produce macroscopic damage to the eye. The relatively low variability of the results allows the determination of irritation potential with a small number of animals. The test permits the establishment of the relationship between instilled concentrations and corneal lesions. The rapidity and simplicity of this approach make the proposed test suitable for the screening of ophthalmic preparations.
Animals↗
Myenteric neuron number after acute and chronic denervation of the proximal jejunum induced by benzalkonium chloride.
The effects of benzalkonium chloride (BAC) on the number of myenteric neurons after acute (until 10 days after BAC application) and chronic (30 and 60 days after BAC application) denervation of the proximal jejunum were determined in rats. There was a significant reduction in the number of myenteric neurons of all segments treated with BAC. The extent of denervation varied with time, and it was reduced in the denervated segments of the chronic group in comparison with the acute group. This may be due to the neuroplasticity phenomenon appearing during the chronic phase.
Animals↗
Action on ileal smooth muscle of synthetic detergents and pardaxin.
Pardaxin (PX), a toxic and repellent substance isolated from the Red Sea flatfish, causes a sharp ball-like profile of drop of saline placed on a hydrophobic film to turn into a flattened one. This effect results with a decrease of the contact angle (theta) from 96 degrees to a maximum of 42 degrees at 10(-4) M of PX. The action of sodium dodecyl sulphate (SDS), a synthetic anionic detergent, benzalkonium chloride (BAC) cationic detergent and pardaxin (PX) a toxic protein with detergent properties, were studied in the ileal guinea-pig longitudinal smooth muscle preparation. SDS (4 X 10(-4) M) and PX (5 X 10(-6) M) diminished the muscle contractile response to field stimulation (0.1 Hz, 1 msec) and to acetylcholine (Ach) and to histamine and elicited a prolonged (4-6 min) TTX-insensitive muscle contraction. The dose dependence of muscle contraction to SDS and PX was found to be sigmoidal and occurred over a narrow range of concentrations. The SDS- but not PX-induced muscle contraction could be reduced by diphenhydramine (H1 antihistamine). BAC (10(-5)-10(-4) M) suppressed the muscle's contractile response to electrical stimulation (0.1 Hz, 1 msec), to Ach, histamine and 5-hydroxytryptamine but did not produce muscle contraction. PX at concentrations higher than 5 X 10(-6) M is a potent detergent and at this concentration shares several pharmacological similarities with SDS.
Animals↗
A permeability test for acute corneal toxicity.
The penetration of sulforhodamine B (SRB) into the two corneas of a freshly killed mouse was measured after one eye was briefly exposed to a solution of a possibly toxic substance. The ratio of the penetrations provides a numerical index of acute toxicity to the corneal epithelium. With a group of 6 animals, a 50% rise in the index can be distinguished at the 95% confidence level; the maximum rise achievable in practice seems to be about 30. NaOH and benzalkonium chloride (BAK) gave graded increases in the value as their concentrations rose; the rise in index corresponded roughly to the injury caused to the living eye.
Animals↗
Determination of benzalkonium chloride in contact lens solutions by positive-ion fast atom bombardment mass spectrometry.
Under positive-ion fast atom bombardment (FAB) mass spectrometric conditions, benzalkonium chloride (BAK) afforded intense peaks at m/z 304 and 332, corresponding to the intact cations [M--Cl]+ of C12 and C14 homologues, respectively. The use of benzethonium chloride as an internal standard and thioglycerol as a FAB matrix allowed the direct and specific determination of the BAK content (0.004-0.020%) in commercial hard contact lens solutions through the individual assay of the two alkyl homologues. A linear relationship between the homologue concentration and the peak-area ratio was observed over the concentration range 3-180 micrograms ml-1.
Benzalkonium Compounds↗
Rapid determination of benzalkonium chloride in pharmaceutical preparations with flow injection liquid-liquid extraction.
Benzalkonium chloride was assayed by on-line extraction of the benzalkonium ion with picrate to chloroform. The absorbance of picrate was measured. The extractions were performed with a home-made flow injection extraction unit. Calibration curves (1.5-180 x 10(-4)% w/v) were straight lines (r = 0.9993) and the relative standard deviation of a series of injections was less than or equal to 2%. Pharmaceutical benzalkonium preparations, containing xylometazoline, timolol, phenylephrine or carbachol could also be assayed. The method was compared with a modified HPLC assay.
Benzalkonium Compounds↗
Determination of benzalkonium chloride in aqueous ophthalmic preparations by high-performance liquid chromatography.
A high-performance liquid chromatographic method is described for the determination of homologues of benzalkonium chloride in aqueous ophthalmic preparations. The technique involves direct injection of the sample on a 5-microns Spherisorb-CN column. The mobile phase is acetonitrile-triethylamine (0.1%, v/v) in water (pH 2.5; 40:60, v/v). Detection is carried out at 215 nm. The method is rapid, specific, reproducible and simple, and is especially useful for the assay of this preservative in stability studies and quality control procedures.
Acetonitriles↗