Imidacloprid is an antiparasitic active ingredient used in veterinary medicine in dogs, cats and livestock against external parasites (fleas, flies, lice, etc.). It is also used against agricultural and household pests. It belongs to the chemical class of the neonicotinoids.
Common name: IMIDACLOPRID
Type: pesticide
Chemical class: neonicotinoid
CHEMICAL STRUCTURE
EFFICACY AGAINST PARASITES
Type of action: Broad-spectrum, contact, non-systemic insecticide, lousicide
Main veterinary parasites controlled: fleas, lice
Efficacy against a specific parasite depends on the delivery form and on the dose administered.
Click here for general information on features and characteristics of PARASITICIDES.
DOSING
Dosing recommendations for antiparasitics depend on national regulations. National regulatory authorities determine whether a product is approved for a given indication, i.e. use on a particular host at a specific dose and against a specific parasite. Check the labels of the products available in your country for specific information on approved indications.
The table below indicates some usual dosing recommendations for imidacloprid issued by manufacturers or documented in the scientific literature. They may not be approved in some countries.
Imidacloprid is a contact insecticide without systemic effect that belongs to the chemical class of the neonicotinoids. It is highly effective against fleas and certain lice species, but not against ticks or mites, or any internal parasites. It is often used in combination with a tickicide/acaricide (e.g. cypermethrin, permethrin).
Imidacloprid is abundantly used in dogs and cats, mainly in spot-ons and in a few collars and low-cost sprays, shampoos, soaps, etc. Use in livestock is marginal, with a few pour-ons for cattle (against horn flies) or sheep (against lice).
In most finished products, efficacy and safety depend not only on the amount of active ingredient(s) but also on their formulations (i.e. the type and amount of so-called inert ingredients), particularly in topical pour-ons and spot-ons. These inert ingredients can significantly affect the pharmacokinetic behavior (e.g. absorption through the skin, distribution within the body, spreading throughout the body surface, etc). Generic products usually contain the same amount of active ingredient(s) as the original product, but often in quite different formulations. In many cases, the curative (therapeutic) efficacy of the different formulations is quite comparable, but the protective (prophylactic) efficacy that determines the length of protection against re-infestations may be rather different.
| Dosing recommendations for IMIDACLOPRID |
||
| DOGS | ||
| Delivery | Parasites | Dose (against imidacloprid-susceptible parasites) |
| Spot-on (10%) | Fleas | 10-25 mg/kg; 4-5 weeks protection |
| Spot-on (10%) | Lice (Trichodectes canis, Linognathus setosus) | 10-25 mg/kg |
| CATS | ||
| Delivery | Parasites | Dose (against imidacloprid-susceptible parasites) |
| Spot (10%-on) | Fleas | 10-25 mg/kg; 4-5 weeks protection |
| Spot (10%-on) | Lice (Felicola subrostratus) | 10-25 mg/kg |
| CATTLE | ||
| Delivery | Parasites | Dose (against imidacloprid-susceptible parasites) |
| Pour-on (4%) | Horn flies | 2-5 mg/kg |
| Pour-on (4%) | Lice | 2-5 mg/kg |
| SHEEP | ||
| Pour-on (3.5%) | Lice | 7-9 mg/kg |
| Pour-on (2%) | Lice | 8-20 mg/kg |
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SAFETY
Oral LD50, rat, acute*: 450 mg/kg
Dermal LD50, rat, acute*: >5000 mg/kg
* These values refer to the active ingredient. Toxicity has to be determined for each formulation as well. Formulations are usually significantly less toxic than the active ingredients.
MRL (maximum residue limit) set for animal tissues (e.g. beef, mutton pork or chicken)*:
- CODEX: Yes
- EU: Yes
- USA: Yes
- AUS: Yes
In April 2013 the EU prohibited for two years the use of several nicotinoids on various crops due to suspected detrimental effects on bee colonies. This should have no influence on veterinary uses of neonicotinoids.
* This information is an indicator of the acceptance of an active ingredient by the most influential regulatory bodies for use on livestock. An MRL for meat may be established also for agricultural pesticides that are not approved for use on animals but are used on commodities fed to animals. It may be also established in the form of an IMPORT TOLERANCE for active ingredients not approved in a particular country but approved for imported animal commodities.
Withholding periods for meat, milk, eggs, etc. depend on delivery form, dose and national regulations. Check the product label in your country.
Learn more about imidacloprid safety.
General safety information for antiparasitics is available in specific articles in this site (click to visit):
- General safety of antiparasitics for domestic animals
- General safety of antiparasitics for humans
- General safety of antiparasitics for the environment
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WARNING Never use agricultural or hygiene products with this or any other active ingredient on livestock or pets, even if there are veterinary products with this same active ingredient approved for use on animals. The formulations for agricultural or hygiene use are different and may be toxic for livestock or pets. It is obvious that veterinary products are not intended for and should never be used on humans!!! |
MARKETING & USAGE
Decade of introduction: 1990
Introduced by: BAYER
Some original brands: ADVANTAGE
Patent: Expired (particular formulations may be still patent-protected)
Use in LIVESTOCK: YES, very scarce
Use in HORSES: NO
Use in DOGS and CATS: YES, abundant
Main delivery forms:
Use in human medicine: No
Use in public/domestic hygiene: Yes
Use in agriculture: Yes
Generics available: Yes, numerous but not in all countries
SELECTION OF COMMERCIAL BRANDS WITH IMIDACLOPRID
- ADVANTAGE: for DOGS and CATS - spot-on against FLEAS - BAYER - imidacloprid
- ADVANTIX: for DOGS - spot-on against FLEAS and TICKS - BAYER - imidacloprid + permethrin
- ADVANTAGE II: for DOGS and CATS - spot-on against FLEAS - BAYER - imidacloprid + pyriproxyfen
- ADVANTAGE MULTI: for DOGS and CATS - spot-on against FLEAS, MITES, HEARTWORMS and ROUNDWORMS - BAYER - imidacloprid + moxidectin
- ADVOCATE: for DOGS and CATS - spot-on against FLEAS, MITES, HEARTWORMS and ROUNDWORMS - BAYER - imidacloprid + moxidectin
- K9 ADVANTIX: for DOGS - spot-on against FLEAS and TICKS - BAYER - imidacloprid + permethrin
- K9 ADVANTIX II: for DOGS - spot-on against FLEAS and TICKS - BAYER - imidacloprid + permethrin + pyriproxyfen
- SERESTO: for DOGS and CATS - collar against FLEAS and TICKS - BAYER - imidacloprid + flumethrin
PARASITE RESISTANCE
In pets: No
In livestock: Yes, in houseflies (Musca domestica) in livestock operations.
Learn more about parasite resistance and how it develops.
SPECIFIC FEATURES
Imidacloprid is a modern "classic" insecticide, introduced in the 1990's. It belongs to the neonicotinoids and is BAYER's own flea active ingredient in the ADVANTAGE product range. It is extensively used in agriculture.
Efficacy of imidacloprid
Imidacloprid has a broad spectrum of activity against insects (e.g. fleas and lice), but no efficacy whatsoever against ticks or mites.
In dogs and cats it is used a lot in spot-ons (= pipettes), alone against fleas and certain lice species, or in mixtures with other active ingredients that broaden the spectrum of efficacy to control ticks or other parasites. As most flea spot-ons it controls existing flea infestations in about 1 to 2 days, and provides about 4 weeks protection against re-infestations.
Use of imidacloprid on livestock is very scarce. It is approved for use as a louisicide on sheep in a few countries (e.g. Australia), and there are also a few pour-ons for cattle, mainly against horn flies (in Latin America).
For off-animal use there are also several baits against houseflies and other nuisance flies, and a few formulations for premise and environmental treatments of livestock operations.
Interestingly, BAYER introduced imidacloprid for pets in the 1990's but not for livestock. Only recently it has introduced an off-shears sheep lousicide in Australia and New Zealand. So far BAYER has not introduced it for use in cattle.
Pharmacokinetics of imidacloprid
Imidacloprid is quite lipophilic. When applied topically to animals it quickly goes into the lipids in the hair-coat and the body surface. This allows a rather long residual effect against fleas.
After topical administration to dogs and cats imidacloprid remains mostly on the animal's surface and is not absorbed. However a certain amount can be ingested through licking and grooming. Ingested imidacloprid is vastly absorbed to blood and quickly metabolized in the liver. Excretion runs mainly through urine (~75%) and feces and is completed in about 48 hours.
Mechanism of action of imidacloprid
As all neonicotinoids imidacloprid is an agonist of the nicotinic acetylcholine receptors. It takes the place of the normal neurotransmitter acetylcholine in the receptors, which cannot be deactivated by acetylcholinesterase and remains irreversibly blocked. This leads to an over stimulation of the nerve cells, to paralysis and to death of the affected insect.
These receptors are found in the central and peripheral nervous system of mammals, but only in the central nervous systems of insects. Neonicotinoids bind much more strongly to insect receptors than to mammal receptors, which makes them relatively safe for domestic animals and humans.
Click here to view the list of all technical summaries of antiparasitic active ingredients in this site.
