EFFICACY AGAINST PARASITES
Type of action: Broad spectrum contact, non systemic ectoparasiticide: insecticide, acaricide, tickicide, louisicide, larvicide
Main veterinary parasites controlled: flies, lice, fleas, mosquitoes, ticks, mites, fly maggots (cutaneous myiasis)
Efficacy against a specific parasite depends on the delivery form and on the dose administered. 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.
Click here for general information on features and characteristics of PARASITICIDES.
Oral LD50, rat, acute*: 250-800 mg/kg
Dermal LD50, rat, acute*: >890 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 (equal to or below limit of detection)
- EU: Yes (equal to or below limit of detection)
- USA: No
- AUS: Yes (equal to or below limit of detection)
* This information is an indicator of the acceptance of an active ingredient by the most influential regulatory bodies for use on livestock. MRL's for animal tissues may be set also for agricultural pesticides that are not approved for use on animals but are used on commodities fed to animals. A MRL may be also set 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.
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
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: 1950
Introduced by: SUMITOMO and BAYER
Some original brands: SUMITHION
Patent: Expired (particular formulations may be still patent-protected)
Use in LIVESTOCK: Yes, very scarce and declining as all organophosphates
Use in HORSES: No
Use in DOGS and CATS: Yes, very scarce and declining as all organophosphates
Main delivery forms:
Use in human medicine: No
Use in public/domestic hygiene: Yes
Use in agriculture: Yes
Generics available: Yes
In livestock: Yes, as for all organophosphates: very frequent worldwide in such species as cattle ticks (Boophilus spp), horn flies (Haematobia irritans), sheep lice (Damalinia ovis), poultry mites (Dermanyssus gallinae), houseflies (Musca domestica), mosquitoes
In pets: Yes, quite frequent worldwide in dog and cat fleas (Ctenocephalides spp)
Fenitrothion is a classical, veteran parasiticide belonging to the organophosphates. It has been used scarcely on livestock and pets.
On livestock it is still used in some countries in cattle and pigs in ready-to-use pour-ons, against horn flies. In pets it is used in a few shampoos, soaps, sprays. It is seldom used alone, mostly in combination with a synthetic pyrethroid.
Nevertheless, there is a clear trend to replace all organophosphates, including fenitrothion, with less toxic compounds.
Efficacy of fenitrothion
As most organophosphates fenitrothion is a broad-spectrum insecticide, acaricide and larvicide. Fenitrothion is a "generalist" pesticide, with good average efficacy against most veterinary ectoparasites, but not outstanding against a particular one.
However, resistance of important veterinary parasites to all organophosphates, including chlorpyrifos is widespread, especially in cattle ticks (Boophilus spp), horn flies (Haematobia irritans), sheep lice (Damalinia ovis), poultry mites (Dermanyssus gallinae), mosquitoes, dog and cat fleas (Ctenocephalides spp) and houseflies (Musca domestica). As a consequence, products with this active ingredient may not achieve the expected efficacy in many places. The same applies to all other organophosphates. This is also a reason for their progressive replacement with newer active active ingredients with a different mode of action.
Pharmacokinetics of fenitrothion
Percutaneous absorption (i.e. through the skin) of topically administered fenitrothion depends on the animal species, the administered dose, and the extension of the treated body surface. Animals treated topically can ingest fenitrothion through licking and grooming. Studies on rats suggest a dermal absorption of max 1% of the administered dose.
Ingested fenitrothion is rapidly absorbed into the bloodstream and distributed throughout the body. It is quickly metabolized in the liver and rapidly excreted, mainly through urine. In human volunteers almost the entire dose was excreted within 24 hours after administration. Certain metabolites are significantly more potent inhibitors of acetylcholinesterase than the parent molecule.
Mechanism of action of fenitrothion
As all organophosphates insecticides, fenitrothion acts on the nervous system of the parasites (but also of mammals, birds, fish and many organisms!) as inhibitor of acetylcholinesterase (also known as AchE), an enzyme that hydrolyzes acetylcholine (Ach). Ach is a molecule involved in the transmission of nervous signals from nerves to muscles (so-called neuromuscular junctions) and between neurons in the brain (so-called cholinergic brain synapses).
AchE's role is to terminate the transmission of nervous signals where Ach is the neurotransmitter (there are several other neurotrasmitters). By inhibiting the activity of AchE, carbamates prevent the termination of those nervous signals, i.e. the neurons remain in constant activity and excitation, massively disturbing the normal movements of the parasites. The bottom line for the parasites is that they are paralyzed and die more or less quickly. Organophosphates bind irreversibly to AchE, in contrast with carbamates, another chemical class of parasiticides, which bind reversibly to AchE.
Click here to view the list of all technical summaries of antiparasitic active ingredients in this site.