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The ability of a supralethal dose of chlorpyrifos to produce delayed neuropathy was examined using assessments of clinical signs, electromyography (EMG), motor nerve conduction velocity (MNCV), lymphocyte neuropathy target esterase activity (LNTE), and histologic changes in nervous system tissues. Cats were exposed to a single, im injection of corn oil (vehicle control), DFP (positive control) at 5.0 mg/kg, or chlorpyrifos at 300 mg/kg and observed for 60 days. Atropine and 2-PAM were administered to chlorpyrifos exposed cats one to two times a day for 14 to 24 days in response to the appearance of cholinergic signs. Anorectic cats during the acute toxicosis were force fed by hand and hydration was maintained by administering fluids sc. Onset of ataxia (mean +/- SD) for the positive control and chlorpyrifos exposed cats were 16.2 +/- 1.8 days (range of 14-19 days) and 19.0 +/- 1.4 days (range of 17-21 days), respectively. Functional deficits for both groups were confined to the hindlimbs and characterized by a crouched-waddling gait, hypermetria, and proprioceptive deficits. Maximal inhibition of LNTE activity was 96% at 24 hr postdosing in the positive control group and 46% at 7 days postdosing in the chlorpyrifos group. No EMG or MNCV abnormalities were detected in any of the treatment groups. Axonal degeneration was similar for the positive control and chlorpyrifos exposed cats. Ascending tracts of the cervical spinal cord and descending tracts of the thoracic and lumbar spinal cord were most severely affected and peripheral nerves were only mildly affected. The clinical and histologic effects produced indicate that chlorpyrifos can cause delayed neuropathy in the domestic cat. The moderate but prolonged inhibition of LNTE produced by chlorpyrifos is atypical of classic organophosphorus delayed neurotoxicants.
The fate of the insecticide Dursban 4E (active ingredient chlorpyrifos) and its effect on crustaceans and insects was studied in indoor experimental freshwater ecosystems that intended to mimick drainage ditches. A single dose (simulating aerial drift) was applied to achieve nominal chlorpyrifos concentrations of 5 or 35 micrograms/L. Two experiments were performed, one in which all model ecosystems were dominated by the macrophyte Elodea nuttallii, and one using systems devoid of macrophytes. In macrophyte-dominated systems, Elodea vegetation adsorbed a large proportion of the dose applied and hampered the mixing of the insecticide in the water (at least up till day 8). Only a small proportion became incorporated in the sediment. In open water systems the insecticide was rapidly mixed in the water, and the sediment played a very significant role as sink for chlorpyrifos. In both Elodea-dominated and open water systems 50% of the dose applied had disappeared on day 8 post-treatment. The rate of disappearance of chlorpyrifos was relatively rapid in water and macrophytes, and relatively slow in the sediment. Of the arthropods in the zooplankton Cladocera were more susceptible than Copepoda. Significant effects (p less than or equal to 0.05) on Cladocera occurred relatively late in Elodea-dominated systems (in week 4 post-application) in contrast to open water systems (week 1), which is in accordance with the observed differences in the fate of chlorpyrifos. Daphnia pulex, D. longispina and Simocephalus vetulus recovered in the model ecosystems when chlorpyrifos concentrations were lower than 0.1-0.2 micrograms/L, which is in agreement with results of laboratory protocol tests performed with these cladocerans. Among the macroscopic Arthropoda the apparent order of susceptibility was amphipods greater than insects greater than isopods. The isopod Asellus aquaticus was more sensitive to the application of the insecticide than the closely related species Proasellus coxalis. In treated open water systems the latter even increased significantly in numbers. Cage experiments in the model ecosystems performed with several species of Arthropoda indicate that laboratory protocol tests may give a reasonable prediction of short-term direct effects of chlorpyrifos for the same species inhabiting more complex aquatic systems.
The bioconcentration kinetics of chlorpyrifos (O,O-diethyl O-3,5,6-trichloro-2-pyridyl phosphorothioate) in guppies (Poecilia reticulata) were investigated. A static exposure was used to study the uptake of the compound. The amount absorbed was calculated from the difference in disappearance rates from the water phase in aquaria with and without fish. The uptake rate was found to be first-order with respect to the exposure concentration, and amounts to ca. 38 ml g-1 (fish) hr-1. The elimination rate was studied in separate experiments. Guppies were first given the opportunity to accumulate chlorpyrifos and, following transfer to clean water, the clearance of the compound was measured by determining the residual chlorpyrifos in the fish. It was found that the elimination rate was first-order with respect to the concentration in fish, but depended slightly on the length of the preexposure period. The half-life of tissue chlorpyrifos varied from 31 to 38 hr. Release of unchanged chlorpyrifos turned out to be negligible relative to the amount eliminated. This indicates that metabolic breakdown is the only pathway for elimination. From the kinetic rate parameters, a bioconcentration factor was calculated of about 1700. This value is very similar to that measured directly after an 8-day semistatic exposure. A two-compartment model is proposed to describe the kinetics of the bioconcentration process. The conditions limiting the applicability of the indirect method for measuring the toxicokinetics of chlorpyrifos are discussed.
Data for louse control are presented chiefly on chlorpyrifos (Dursban) 0, 0-diethyl 0-(3, 5, 6-trichloro-2-pyridyl) phosphorothioate and fenchlorphos in one trial and chlorpyrifos and famphur in three trials. These animal systemics were tested on 168 dairy calves in four herds located in three regions of the North Island, New Zealand. Louse control, following single backline, dermal applications, showed 80%, 87% and 100% with dosages of chlorpyrifos at 5 mg, 13 mg and 20 to 200 mg per kg, respectively, and 100% and 93% with dosages of famphur at 20 mg per kg, respectively. Poor louse control (24 to 58%) with fenchlorphos was expected since this compound requires two applications 14 days apart. Ovicidal effect was demonstrated with chlorpyrifos and famphur. Minor scurfing and hair loss occurred on some calves with all compounds, but hair coats were normal 28 days after treatment. Calves given 100 mg to 200 mg per kg chlorpyrifos showed signs of organophosphate toxicity from 5 mins to 90 mins post-treatment but were normal thereafter.
The mechanism responsible for negative cross-resistance to chlorpyrifos was examined in isogenic dicofol susceptible (Orchard-12) and resistant (Dicofol-IR) two-spotted spider mites, Tetranychus urticae Koch. The acetylcholinesterase of both strains was equally sensitive to inhibition by chlorpyrifos oxon. However, the Dicofol-IR strain showed increased oxidative activation of chlorpyrifos to chlorpyrifos oxon relative to the Orchard-12 strain, suggesting this mechanism is responsible for the observed negative cross-resistance.
Following treatment with a controlled-release formulation of chlorpyrifos, no substantial differences between diversity estimates were evident for 6 post-treatment weeks for both treated and control plots. By post-treatment week 12, significant decreases in diversity estimates occurred in treated plots, suggesting that a directly proportional relationship exists between chlorpyrifos concentrations and reduced diatom colonization through time. Comparatively, diatom colonization progress "normally" and populations proceeded toward "maturity" in the control plots as indicated by the increase in the diversity estimates between post-treatment weeks 6 and 12. Any adverse effects due to the insecticidal treatment, however, were not considered to be environmentally deleterious in light of the restricted type of habitat (rice culture) in which the chlorpyrifos was used.
Of fifteen compounds tested as synergists for chlorpyrifos against susceptible and resistant strains of Blattella germanica, the German cockroach, eleven were active against the resistant strain but only seven were synergistic against the susceptible strain. Overall, the most effective synergist was S,S,S-tributyl phosphorotrithioate (DEF) followed by phenyl saligenin cyclic phosphonate (PSCP) and two substituted N,N-dimethylcarbamates: SK-102 and SK-37. The most effective synergist for overcoming chlorpyrifos resistance was SK-37 which reduced the resistance ratio by 3.2-fold. Four other synergists which reduced chlorpyrifos resistance, in order of their effectiveness, were: SK-102 > PSCP > DEF > tridiphane. The potential usefulness of these synergists for German cockroach control is discussed.
Red-winged blackbird (Agelaius phoeniceus; blackbird) and European starling (Sturnus vulgaris; starling) nestlings were dosed with either 2.0 mg/kg body mass chlorpyrifos, 50.0 mg/kg body mass dimethoate, or a propylene glycol carrier in situ. Four growth measurements (body mass, culmen, tarsus, wing) were recorded from nestlings to determine if these organophosphorus compounds caused perturbations in development at sublethal concentrations. Blackbird nestlings were more sensitive to chlorpyrifos than starling nestlings were more sensitive to dimethoate than blackbird nestlings. This was in contrast to reported adult LD50 values where the reverse was true. Blackbird nestlings were more tolerant of a substantially higher concentration of dimethoate than the adult LD50. The sensitivity of starling nestlings to dimethoate was similar to adults. In contrast, juveniles of both species were more sensitive to chlorpyrifos than adults. After the initial 24 hr, surviving nestlings dosed with either chemical recovered and continued their development. Exposure to dimethoate caused significant depression in starling body mass during the initial 24 hr period. Survivors obtain body mass equal to controls within 48 hr post dosing. The research presented here demonstrates that the simple supposition that passerine nestlings are typically more sensitive to toxins than adults does not always hold true. It also indicates that sensitivity relationships among adults do not necessarily apply to their nestlings.
In urban and sub-urban areas larval populations of Culex pipiens are now resistant to chlorpyrifos. A replacement compound must be found so 31 pesticides were tested against 3 strains: 2 of them were bred in the laboratory (on sensitive and one resistant) and the third one collected in an area treated with agricultural pesticides and chlorpyrifos. The results show that this last compound induces a cross-resistance only to organophosphorus compounds especially to parathion, chlorpyrifos-methyl, pyrimiphos-methyl, diazinon and Abate. Agricultural pesticides made this species resistant to chlorinated hydrocarbon and organophosphorus compounds. Among the latest, trichlorfon, azinphos-methyl, methidathion and malathion are still efficient as are propoxur, Decis (pyrethroid), methoprene and Dimilin.
The urinary excretion rates of diethyl phosphate and diethyl phosphorothioate and changes in blood cholinesterase activities were studied in fifteen persons self-poisoned either by the organophosphorus pesticide quinalphos (twelve persons) or by chlorpyrifos (three persons). The organophosphate poisoning was always indicated by a significant depression of serum and/or red blood cell cholinesterase activities. The return of serum cholinesterase activity in the range of referent values took more than 30 days and had a different course in different persons. The most rapid increase in red blood cell acetylcholinesterase activity was noted within 24 h after the first treatment with oximes Pralidoxime and/or HI-6. None of the spot urine samples, collected daily after admission of persons to hospital, contained measurable quantities of the parent pesticide. There was no correlation between the maximum concentration of total urinary diethylphosphorus metabolites normalized to creatinine and the initial inhibition of blood cholinesterase activities measured in samples collected on the day of admission to hospital. The excretion of metabolites followed the kinetics of a biphasic reaction. The half-time of urinary metabolites concentration decrease in the fast excretion phase in quinalphos poisoned persons was 5.5-14.2 h (eight persons) and 26.8-53.6 h (four persons) and in chlorpyrifos poisoned persons 3.5-5.5 h. The half-time for the slow excretion phase ranged from 66.5 to 127.9 h in all persons and for both compounds. For a given person, the rates of excretion of diethyl phosphate and diethyl phosphorothioate were about the same. However, in quinalphos poisoned persons the proportions of single metabolites in total diethylphosphorus metabolites varied with the initial maximum concentration of total metabolites.(ABSTRACT TRUNCATED AT 250 WORDS)
Exposure of Biomphalaria alexandrina to sublethal concentrations (0.125, 0.25 and 0.05 ppm) of the organophosphorous insecticide, chlorpyrifos (Dursban), induced a reduction in egg production and egg hatchability. Exposure of Schistosoma mansoni miracidia to the insecticide (60 min, 0.50 ppm) prior to infection of B. alexandrina did not affect the subsequent production of cercariae. However, exposure of S. mansoni-infected snails to the insecticide until day 55, from day 20 to day 62 and from day 35 to 62 following infection resulted in blockage of cercarial shedding. Cercarial shedding commenced in some snails when the treatment stopped. Exposure to the insecticide in concentrations of 0.125 and 0.25 ppm during the first 20 days following infection did not affect the subsequent production of cercariae, but exposure to 0.5 ppm during the first 20 days affected markedly the production of cercariae due to a high snail mortality. The findings indicate that the cercaria is the target stage for the activity of chlorpyrifos on the intramolluscan larval development. It is suggested that S. mansoni cercarial production in B. alexandrina may be a useful system for monitoring the effect of low concentrations of pesticides on the aquatic environment, and that the ability by chemical means to interrupt the cercarial production might be a useful tool in further analyses of important aspects of the snail/parasite relationship.
Wheat grain was treated with 14C-chlorpyrifos-methyl to generate bound residues for determining their bioavailability to rats. In a parallel experiment, bound residues were prepared with non-labelled chlorpyrifos-methyl to determine possible adverse effects in rats fed the grain-bound residue for 28 and 90 days. Two dose levels of 10 and 50 ppm were initially used on the grain. The 10 ppm led to the formation of 25.1% bound residues (2.51 ppm) after 6 months as determined by radiomeasurement. The higher dose was assumed to form 12.55 ppm bound residues. When 14C-bound residues were fed to male rats for 24 hours, the animals eliminated 75% of the radioactivity in urine, 7% in expired air and 8% in faeces after 3 days, indicating that the bound residues were highly bioavailable. A further "bioavailable" amount (4%) was found in selected organs.