Imidacloprid
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JOURNAL OF PESTICIDE REFORM/ SPRING 2001 • VOL. 21, NO. 1 ● INSECTICIDE FACTSHEET IMIDACLOPRID Imidacloprid is a relatively new, systemic insecticide chemically related to the tobacco toxin nicotine. Like nicotine, it acts on the nervous system. Worldwide, it is considered to be one of the insecticides used in the largest volume. It has a wide diversity of uses: in agriculture, on turf, on pets, and for household pests. Symptoms of exposure to imidacloprid include apathy, labored breathing, incoordination, emaciation, and convulsions. Longer-term exposures cause reduced ability to gain weight and thyroid lesions. In studies of how imidacloprid affects reproduction, exposure of pregnant laboratory animals resulted in more frequent miscarriages and smaller offspring. An agricultural imidacloprid product increased the incidence of a kind of genetic damage called DNA adducts. Imidacloprid is acutely toxic to some bird species, including sparrows, quail, canaries, and pigeons. Partridges have been poisoned and killed by agricultural use of imidacloprid. It has also caused eggshell thinning. The growth and size of shrimp are affected by imidacloprid concentrations of less than one part per billion (ppb). Shrimp and crustaceans are killed by concentration of less than 60 ppb. Imidacloprid is persistent. In a field test in Minnesota, the concentration of imidacloprid did not decrease for a year following treatment. It is also mobile in soil, so is considered by the U.S. Environmental Protection Agency to be a potential water contaminant. The development of resistance to imidacloprid by pest insects is a significant concern. In Michigan potato fields, the Colorado potato beetle developed resistance to imidacloprid after just two years of use. BY CAROLINE COX has a wide variety of uses; it is used in Figure 1 agricultural products for use on cotton Imidacloprid and vegetable crops,3 in turfgrass and or- 2 midacloprid (see Figure 1) is a rela- CH2 N NH namental plant products, in indoor and I = tively new insecticide, first registered for — outdoor cockroach control products,5 and use as a pesticide in the U.S. in 1994, N-NO2 in termite control products.4 It is also Cl — and was the first insecticide in its chemi- N used in products for pets, home, lawn, cal class to be developed for commercial 1-((6-chloro-3-pyridinyl)methyl)-N-nitro-2- and garden use including some, like pot- use.1 Imidacloprid is a systemic insecti- imidazolidinimine ting soil, that may not always be easily cide1; it moves through plants from the recognized as pesticides.6,8-10 place where it was applied and kills in- sects when they feed. Its major manufac- How Does Imidacloprid Figure 2 Kill Insects? turer is Bayer Corporation that markets Nicotine imidacloprid products with the brand Imidacloprid, and other insecticides in names Merit, Admire, Premise, Pre-Empt, the nicotinoid chemical family, are “simi- and Advantage, among others.2-6 N lar to and modeled after the natural nico- 7 N CH3 tine [a tobacco toxin].” (See Figure 2.) Use Because of their molecular shape, size, Although imidacloprid has not been Imidacloprid and nicotine have similar activity and charge, nicotine and nicotinoids fit in use for long relative to other common in the nervous system. into receptor molecules in the nervous pesticides, according to University of system that normally receive the molecule Arizona entomologist George Ware “very acetylcholine. Acetylcholine carries nerve possibly it is used in the greatest volume impulses from one nerve cell to another, Caroline Cox is NCAP’s staff scientist. globally of all insecticides.”7 Imidacloprid or from a nerve cell to the tissue that a NORTHWEST COALITION FOR ALTERNATIVES TO PESTICIDES/NCAP P.O. BOX 1393, EUGENE, OREGON 97440 / (541)344-5044 15 JOURNAL OF PESTICIDE REFORM/ SPRING 2001 • VOL. 21, NO. 1 nerve controls. Imidacloprid and other or “other” ingredients. There is little pub- chromosome damage in laboratory tests.17 nicotinoids irreversibly block acetylcho- licly available information about the iden- Other symptoms of naphthalene expo- line receptors.7 tity of these ingredients. Inerts that have sure include anemia, liver damage, cata- Why is imidacloprid less toxic to mam- been identified in imidacloprid products racts, and skin allergies.18 mals’ nervous systems than to insects’? include the following: Whenever possible, the remaining sec- Both insect and mammal nervous systems Crystalline quartz silica (in Merit 0.5 tions of this article will specify whether have acetylcholine receptors that are G13) is classified by the International tests were conducted with imidacloprid blocked by imidacloprid; most of the sen- Agency for Research on Cancer as “car- alone or with an imidacloprid-contain- sitive receptors are in the central nervous cinogenic to humans”14 and as “known ing product (imidacloprid plus inerts). system of insects, but in nerves associ- to be a human carcinogen”15 by the Na- Toxicity of inerts to cats: An uniden- ated with muscles in mammals.7 How- tional Toxicology Program because it tified inert ingredient in Advantage, an ever, insect acetylcholine receptors are causes lung cancer. It also causes emphy- imidacloprid flea insecticide applied as more sensitive to imidacloprid than are sema and obstructive airway disease and drops on the back of a pet’s neck, can be mammalian receptors,11 although for has also caused genetic damage in exposed toxic to kittens when applied above the some of imidacloprid’s breakdown prod- people and laboratory tests.15 label rate. In laboratory tests, death, coma, ucts this relationship is reversed.12 Naphthalene (in Leverage 2.716) has and incoordination were observed in kit- recently been classified by the National tens receiving five times the recommended Inert Ingredients Toxicology Program as having “clear evi- dose of Advantage.19 Further experiments Commercial imidacloprid insecticides, dence of carcinogenic activity”17 (through showed that the toxicity was probably like nearly all pesticides, contain ingredi- inhalation exposure) because it causes na- caused by the inert present in the largest ents other than imidacloprid called “inert” sal cancers. It also caused two kinds of amount.20 No publicly available studies show the effects of smaller overdoses. Vomiting, salivation, and depression were Figure 3 also observed in cats fed Advantage or its Persistence of Acute Neurological Symptoms Caused by inert ingredients.21 Imidacloprid and a Commercial Imidacloprid Product 12 Acute Toxicity In laboratory animals, symptoms of 10 acute (short-term) oral exposure to imida- cloprid included apathy, labored breath- ing, loss of the ability to move, stagger- 8 ing, trembling, and spasms. Some symp- toms lasted for five days following expo- 6 sure.22 Symptoms following acute expo- sure to an agricultural imidacloprid prod- 4 uct (imidacloprid plus “inerts”) included Days after exposure reduced activity, incoordination, tremors, diarrhea, and emaciation. Some symp- 2 toms lasted 12 days after exposure,23 twice as long as the symptoms of exposure to 0 imidacloprid alone. (See Figure 3.) Symp- Imidacloprid Gaucho toms following acute exposure to an (imidacloprid + “inert” ingredients) imidacloprid flea control product in- Sources: U.S. EPA. Office of Pesticides and Toxic Substances. 1992. Request for experimental use cluded reduced activity, convulsions, and permit 00315-EUP-ENG and 003125 EUP-ENR for NTN 33893 (Imidacloprid-proposed) a labored breathing.24 crystalline end-use formulation containing 0.62% NTN 33893 active ingredient. Memo from M.S. Ottley, Health Effects Div., to D. Edwards, Registration Div. Washington, D.C., Mar. 24. (See Also in laboratory animals, symptoms attached Data Evaluation Report for MRID No. 420553-31.) of breathing imidacloprid (for four hours) U.S. EPA. Office of Prevention, Pesticides and Toxic Substances. 1994. Imidacloprid. included difficult breathing, loss of the Evaluation of toxicity data submitted and identification of outstanding toxicology data requirements. Memo from M.S. Ottley, Health Effects Div., to P. Jenkins and D. Edwards, ability to move, and slight tremors. Symp- Registration Div. Washington, D.C., June 8. (See attached Data Evaluation Report for MRID No. toms of breathing two agricultural imida- 428557-02. cloprid products were similar: incoordi- In laboratory tests, symptoms of exposure to a commercial imidacloprid product lasted over nation, convulsions, reduced activity, twice as long as symptoms of exposure to imidacloprid alone. tremors, and salivation. Some symptoms NORTHWEST COALITION FOR ALTERNATIVES TO PESTICIDES/NCAP 16 P.O. BOX 1393, EUGENE, OREGON 97440 / (541)344-5044 JOURNAL OF PESTICIDE REFORM/ SPRING 2001 • VOL. 21, NO. 1 persisted two days after exposure.25 Eye Irritation: Several imidacloprid Figure 4 products (Merit 0.5 G,26 Merit 75 WP,2 Effects of Imidacloprid Exposure on Successful Pregnancy 4 27 Premise 75, Provado Solupak, and Ad- Weight of Newborn Offspring vantage6) cause eye irritation. Subchronic Toxicity Unexposed Subchronic (medium-term; 10-day) exposure of rats to imidacloprid reduced weight gain at a dose of 10 mg/kg per 28 day. Exposed There are no publicly available sub- chronic studies of commercial imida- cloprid products. 5.0 5.5 6.0 Chronic Toxicity Weight of newborn rats (milligrams) Chronic (long-term; lifetime) feeding Frequency of miscarriages studies with rats showed that the thyroid is especially sensitive to imidacloprid. Thyroid lesions were caused by doses of Unexposed 17 milligrams per kilogram (mg/kg) of body weight per day in males. Slightly higher doses (25 mg/kg per day) reduced 29 weight gain in females. At higher doses Exposed (100 mg/kg per day), effects included at- rophy of the retina in females.30 There are no publicly available chronic 04 812 studies of commercial imidacloprid Miscarriages (% of total rabbit embryos) Source: products. U.S. EPA. Office of Prevention, Pesticides and Toxic Substances. 1993. Imidacloprid. Evaluation of toxicity data submitted and identification of outstanding toxicology data Effects on Reproduction requirements. Memo from M.S. Ottley, Health Effects Div., to P. Jenkins and D. Edwards, Registration Div.