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PubMed1966

An intracerebral assay procedure in mice for chemical inactivation of rabies virus.

An intracerebral assay technique in mice is described for testing chemical disinfectants acting on the rabies virus. The assay determines whether more than 99% of 10 000 mouse intracerebral LD(50) of virus are inactivated within 1-2(1/2) minutes. By this test, several substances usually available for the treatment of animal bite wounds were found to be effective. They are: 1%-20% soap solutions; 43%-70% alcohol; 1:1000 (0.1%) or lower dilutions of two quaternary ammonium compounds, benzalkonium chloride and cetrimonium bromide; 1:10 000 or lower dilutions of iodine; acetone; and ether.Several other substances tested for possible use in environmental disinfection were also found to be virucidal. They were: 3% caustic soda and commercial preparations of organic phenols, iodine, and a mixture of trisodium phosphate and sodium hypochlorite. No virucidal effect was exerted by a 2% aqueous solution of mercurochrome, a 1:1000 aqueous solution of thiomersal, or 3% formalin (1% formaldehyde).A number of substances that inactivate rabies virus have thus become available for local treatment of bite wounds and for environmental disinfection. The assay procedure described may be useful in testing other disinfectants and chemical substances.

Animals↗
PubMed1979

Direct spectorphotometric assay of quaternary ammonium compounds using bromthymol blue.

Benzalkonium chloride, benzethonium chloride, and chlorhexidine gluconate were assayed quantitatively by a direct spectrophotometric method with bromthymol blue buffered at pH 7.5. The method shows good results at concentrations of 0--300 microgram/ml and in the presence of epinephrine bitartrate, phenylephrine hydrochloride, pilocarpine hydrochloride, and polyvinyl alcohol.

Benzalkonium Compounds↗
PubMed1971

Inactivation of influenza and other viruses by a mixture of virucidal compounds.

A mixture of benzalkonium chloride, Triton X100, and citric acid (Resiguard F) had a marked virucidal effect on lipid-containing deoxyribonucleic and ribonucleic acid viruses, such as vaccinia virus, herpesvirus, and influenza virus. Adenoviruses and picornaviruses were more resistant to inactivation. Electron microscopy showed that influenza particles became aggregated in the presence of Resiguard F and that the outer fringe of hemagglutinin and neuraminidase spikes seen in control virus preparations became indistinct. The mixture had no detectable antiviral activity in mice infected with influenza AO/PR/8/34 virus, and this was attributed to the reduced virucidal effect of Resiguard F in the presence of serum proteins.

Adenoviridae↗
PubMed1992

A novel microbial sensor using luminous bacteria.

A novel microbial sensor system that uses luminous bacteria was developed for the determination of both glucose and toxic compounds. The sensor system consisted of a membrane with luminous bacteria immobilized upon it and a photomultiplier. Measurements were based on the in vivo intensity of the light emitted by the bacteria, as this is affected by their environment. A linear relationship was observed between increased luminescence and concentrations of glucose between 0.05 mM and 0.55 mM. The relative standard deviation was 10% for 0.55 mM glucose (n = 10). Toxic compounds such as benzalkonium chloride, sodium dodecyl sulphate and chromium(VI) were also detected by measuring the decrease in luminescence in their presence.

Bacteria↗
PubMed1985

The effects of topical drugs and preservatives on the tears and corneal epithelium in dry eye.

Medications used in 'Dry Eye' patients are reviewed for their effects on the corneal surface including the overlying tear film. Preservatives are discussed, since they affect the properties of commercial preparations which may be instilled frequently as a substitute for normal tears. The major beneficial effect which a topically applied agent can have on epithelium is to supplement or stabilise the tear film. Thimerosal sometimes triggers a sensitivity reaction, and other mercurial compounds are unstable. Benzalkonium chloride compromises both corneal epithelium and tear film. Some cationic detergents, including chlorhexidine digluconate and polyquat, cause less disruption at prophylactic concentrations. The use of a small drop size is helpful in preventing toxic effects of preservatives. All preservatives should be avoided when unit doses of a sterile tear replacement, such as saline, can be made available. Topical antibiotics should be used only to control known bacterial infections, avoiding high concentrations of bacitracin, gentamicin, and neomycin. Steroids and antibiotic/steroid combinations must be used with great caution, and only when uncontrolled ocular inflammation justifies the risk of possible corneal ulceration.

Acetylcysteine↗
PubMed1999

Antibiotic and biocide resistance in methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococcus.

Concern has been growing regarding the potential of antibiotic and disinfectant co-resistance in clinically important bacteria. In this study, the susceptibilities of methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA) to chlorhexidine (CHX), the quaternary ammonium compounds cetylpyridinium chloride (CPC) and benzalkonium chloride (BC), triclosan, dibromopropamidine isethionate (DBPI) and triclocarban were compared. MRSA exhibited low-level resistance to CHX and the QACs, with MICs of 1.5 to 3-fold (CHX), and 2 to 4-fold (QACs) higher than MSSA. However, the MIC values for MRSA ranged between 0.025 (the MIC of MSSA) and 1 microg/mL with triclosan, and between <5 (the MIC of MSSA) and 75 microg/mL with DPBI. Nevertheless, these strains remain relatively sensitive to most of these antimicrobial agents. The bactericidal efficacy of CHX, CPC and DBPI (with the exception of one strain) correlated with their MIC value. This was not observed using triclosan; MRSA and MSSA strains were equally susceptible to its killing effect, regardless of MIC. The permeabilizing agent, ethylenediamine tetraacetic acid (EDTA) was unable to potentiate the antibacterial activities of the biocides against any of the strains tested. Attempts to select for staphylococcal strains with increased resistance to triclosan, CPC or CHX, using disc diffusion, step-wise broth, or repeated exposure/recovery technique, were only partially successful, and resistance was found to be unstable. The susceptibilities of vancomycin-resistant enterococcus (VRE) and vancomycin-sensitive enterococcus (VSE) to the biocides were also compared and found to be similar both in terms of MIC testing and time-kill studies.

Anti-Bacterial Agents↗
PubMed2000

Evaluation of the cytotoxic effects of bis-quaternary ammonium antimicrobial reagents on human cells.

The cytotoxic effects of newly synthesized bis-quaternary ammonium compounds (bis-QACs) and benzalkonium chloride were investigated on skin and blood cells, namely normal human epidermal keratinocytes of neonatal foreskin, a normal human skin fibroblast cell line NB1RGB, erythrocytes and a lymphoma cell line JM. The bis-QACs tested were 4, 4'-(1,6-hexamethylenedithio)bis(1-octylpyridinium iodide) (4DTBP-6, 8), N,N'-tetramethylenebis(1-dodecyl-4-carbamoylpyridinium iodide) (4BCAP-4,12), N,N'-hexamethylenebis(1-decyl-4-carbamoylpyridinium iodide) (4BCAP-6,10), 4,4'-(1,4-tetramethylenedicarbonyldiamine) bis (1-decylpyridinium iodide) (4DCABP-4,10), 4,4'-(1, 4-tetramethylenedicarbonyldiamine) bis (1-dodecylpyridinium iodide) (4DCABP-4,12), 4,4'-(1, 4-phenyldicarbonyldiamine)bis(1-dodecylpyridinium iodide) (4DCABP-P, 12), and 4,4'-(1, 6-hexamethylenedioxydicarbonyl)bis(1-dodecylpyridinium iodide) (4DOCBP-6,12). All bis-QACs consisted of two identical alkylpyridinium rings and bridge structure linking rings to each other have a methylene bridge but only 4DCABP-P,12 has a phenyl ring as a bridge. Most of the LD(50) values in acute cytotoxic assays of these bis-QACs tended to be lower than those of benzalkonium chloride. However, the comparison of the antibacterial activity against cytotoxic effects on several human cells revealed that bis-QACs, especially 4DTBP-6,8, have wide concentration ranges showing sufficient antibacterial activity and lower cytotoxic effect on human cells (except for 4DOCBP-6,12), although benzalkonium chloride caused significant human cell damage at the concentrations necessary for antibacterial activity. Moreover, judging from the LD(50) value of 4DTBP-6,8 [67 microM, a 6.7-fold higher concentration than the upper value of MIC] obtained in an artificial human skin model TESTSKIN, 4DTBP-6,8 is thought to be a more effective and safer antiseptic reagent for application to the skin surface than benzalkonium chloride. Taken together, bis-QACs are expected to be a promising new generation of antimicrobial QACs.

Anti-Bacterial Agents↗
PubMed2005

Quantitative determination of benzalkonium chloride in treated wood by solid-phase extraction followed by liquid chromatography with ultraviolet detection.

Ammoniacal copper quat (ACQ) compound wood preservative is comprised of copper and quaternary ammonium compounds with benzalkonium chloride (BAC) as the active ingredient. Solid-phase extraction (SPE) followed by liquid chromatography with ultraviolet detection (LC-UV) was developed for quantitative determination of BAC in treated wood. Five species of wood were used, Japanese cedar (Cryptomeria japonica), Japanese larch (Larix leptolepis), Yezo spruce (Picea jezoensis), Sakhalin fir (Abies sachalinensis), and western hemlock (Tsuga heterophylla). BAC used in the present study was composed of 66% C12, 33% C14 and less than 1% C16. BAC was added to each wood species (500 mg) then extracted with HCl-ethanol (20 ml) and quantitatively determined with LC-UV (262 nm). Wood extractives from the heartwood of each species, except western hemlock, interfered with quantitative determination of BAC, but SPE with an Oasis MCX cartridge was effective in preventing this. Using the present methods, BAC homologue peaks were clearly confirmed without interference. Recoveries from wood ranged from 92 to 101% and the limit of quantitation was approximately 240 microg/g wood for the C12 and C14 homologues.

Abies↗
PubMed1979

Benzalkonium chloride: selective inhibitor of histamine release induced by compound 48/80 and other polyamines.

Benzalkonium chloride (BAC) is a mixture of quaternary benzyldimethylalkylammonium chlorides which was found to inhibit histamine release induced by polyamines (48/80, ATP, bradykinin, curare, guanethidine, polylysine, polymyxin B, poly-THIQ, protamine, stilbamidine or substance P), but not that caused by antigens, concanavalin A, dextran, lonophores (A23187 or X-537A), enzymes (chymotrypsin or phospholipase C), monoamines (dextromethorphan, meperidine or chlorpromazine) or detergents (decylamine, Triton X-100 or a fire ant venom alkylpiperidine). Inhibition by 1.5 and 3 microgram of BAC per ml caused parallel shifts of the 48/80 dose-response curves to the right with no loss of efficacy, indicating that the antagonism was surmountable. Phospholipase C was partially inhibited by BAC, but Triton X-100 also inhibited phospholipase C (but not 48/80), indicating that the inhibition of phospholipase C by BAC was probably a nonspecific, detergent effect. BAC caused histamine release by itself at concentrations over 5 microgram/ml. Heat inactivation (50 degrees C for 15 min) of the mast cells did not prevent this release, suggesting a lytic mechanism for this action. Structure-activity relations studies on various members of the BAC family for their ability to inhibit 48/80-induced histamine release indicated that benzyldimethyltridecylammonium chloride was the most potent.

Animals↗
PubMed1995

Primary interactions of three quaternary ammonium compounds with blastospores of Candida albicans (MEN strain).

The absorption of three quaternary ammonium compounds (QAC), cetylpyridinium chloride, cetrimide and benzalkonium chloride, onto the surface of blastospores of Candida albicans (MEN strain) was examined at room temperature. Equilibrium uptake occurred in less than 30 seconds for cetylpyridinium chloride and cetrimide whereas 5 min contact time was required for benzalkonium chloride. The adsorption of all three agents may be mathematically described as Langmuirian and hence a concentration-dependent formation of drug-monolayer on the surface of the blastospore occurred. From this the number of molecules adsorbed onto the surface of a single blastospore was calculated to be 1.33 x 10(12), 3.17 x 10(12) and 2.32 x 10(12) for cetylpyridinium chloride, cetrimide and benzalkonium chloride, respectively. These dissimilarities are most likely due to differences in the orientations of both the cationic nitrogen atom and the accompanying lipophilic portions of each QAC at the blastospore surface. Relating these observations to the known antiadherence effects of cetylpyridinium chloride and cetrimide, it can be concluded that monolayer coverage of the blastospore surface with QAC does not account for the observed reduced adherence. This suggests that the anti-adherence effects are due to either direct interaction with, or steric blockade of, adhesions on the blastospore surface.

Adsorption↗
PubMed1980

The effects of preservatives on the ciliary beat frequency of chicken embryo tracheas.

The effects of preservatives on the ciliary beat frequency of chicken embryo tracheas are determined, Polar compounds like benzalkonium chloride in commonly used concentrations, decrease the frequency less than 30% after a 20 minutes' exposure. The effect is not reversible after rinsing with Locke-Ringer solution. Lipophilic compounds however, like chlorbutol, cause an arrest of the cilary movement with 10 minutes. The effect, different from the polar compounds, is reversible; but only after a limited exposure-time. Mercuric compounds, like thiomersal, decrease the frequency non-reversibly 30 to 90% after a 20 minutes' exposure. EDTA decreases the frequency 40 to 50%, independent of the exposure-time and in a reversible way. The combination of benzalkonium chloride 0.01% and EDTA 0.05% is recommended to preserve nasal drops.

Animals↗
PubMed1984

Serratia marcescens meningitis associated with a contaminated benzalkonium chloride solution.

Serratia marcescens is recognized as an important and potentially hazardous nosocomial pathogen. The organism has been implicated here as the first reported case of S. marcescens meningitis associated with skin disinfection. A quaternary ammonium compound ( QAC --Benzalkonium Chloride), was used to sterilize the skin prior to injection in a physician's office. Epidemiological studies were initiated. Six spray bottles containing disinfectant, the opened stock bottle of QAC , and an unopened bottle of disinfectant were all cultured. S. marcescens was noted growing in the spray bottles as well as in the opened stock bottle. Antibiograms of the patient and epidemiological isolates are essentially the same. It is our contention as well as that of the Centers for Disease Control that an appropriate skin disinfectant such as Tincture of Chlorhexidine, Iodophors , or Tincture of Iodine should be used, and that physicians performing surgical techniques in the office be aware of the potential hazard of contamination. The consequences of nosocomial infection with resistant organisms warrant every precaution by health care professionals.

Benzalkonium Compounds↗