Common name: EPRINOMECTIN

Type: pesticide
Chemical class: macrocyclic lactone

CHEMICAL STRUCTURE

Molecular structure of EPRINOMECTIN

 

 

 

 

 

 

 


EFFICACY AGAINST PARASITES

Type of action: Systemic & contact broad-spectrum ectoparasiticide and endoparasiticide.
Main veterinary parasites controlled: Gastrointestinal and pulmonary roundworms, lice, mites, horn flies; myiasis by screwworms, bot flies, warble flies, etc.

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.


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 eprinomectin issued by manufacturers or documented in the scientific literature. They may not be approved in some countries.

Eprinomectin is a macrocyclic lactone with a broad spectrum of activity similar to ivermectin. It is effective against roundworms (gastrointestinal, respiratory, renal, in the skin, etc.) and, depending on the delivery form and the dosage also against a number of external parasites such as lice, mites and various myiasis. However, it is ineffective against tapeworms and flukes, and at the usual use recommendations it doesn't control fleas, stable flies, mosquitoes, horse flies, multi-host ticks (e.g. Amblyomma spp, Dermacentor spp, Haemaphysalis spp, Ixodes spp, Rhipicephalus spp, etc.) and several other external parasites. In the last years it has been increasingly used in some countries against cattle ticks (Boophilus = Rhipicephalus microplus) and horn & buffalo flies (Haematobia irritans). Against cattle ticks, both as an injectable (at 0.2 mg/kg) and as a pour-on (0.5 mg/kg) control is usually sufficient (>90%) but without knock-down effect, i.e. the treated animals need 7-10 days to become more or less tick free. Control of horn & buffalo flies is usually incomplete (<80%).

Eprinomectin is moderately used in ruminants, mainly in pour-ons and injectables. So far it is not used in swine, poultry or horses. Use in cats as a spot-on (in combination with other actives) is still rather scarce. So far it is not used in dogs.

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 injectables and in topical pour-ons and spot-ons. These inert ingredients can significantly affect the pharmacokinetic behavior (e.g. absorption through the skin or from the injection site, 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 EPRINOMECTIN
CATS
Delivery Parasites Dose (against eprinomectin-susceptible parasites)
Topical (spot-on) Ancylostoma spp 0.5-1.6 mg/kg
Topical (spot-on) Toxocara cati 0.5-1.6 mg/kg
Topical (spot-on) Toxascaris leonina 0.5-1.6 mg/kg
Topical (spot-on) Dirofilaria immitis prevention
0.5-1.6 mg/kg once a month
CATTLE
Delivery Parasites Dose (against eprinomectin-susceptible parasites)
Subcutaneous (1-2%) Roundworms 0.2 mg/kg
Subcutaneous (1-2%) Dermatobia hominis 0.2 mg/kg
Subcutaneous (1-2%) Hypoderma spp 0.2 mg/kg
Subcutaneous (1-2%) Mites 0.2 mg/kg
Subcutaneous (1-2%) Lice 0.2 mg/kg
Subcutaneous (5%) Roundworms 1 mg/kg. Protection of up to 150 days against Dictiyocaulus, 120 days against Haemonchus, Oesophagostomum & Ostertagia, and 100 days against Cooperia & Trichostrongylus
Subcutaneous (5%) Hypoderma spp 1 mg/kg; longer protection than at 0.2 mg/kg
Subcutaneous (5%) Mites 1 mg/kg; longer protection than at 0.2 mg/kg
Topical (spot-on) Roundworms 0.5 mg/kg
Topical (spot-on) Dermatobia hominis 0.5 mg/kg
Topical (spot-on) Hypoderma spp 0.5 mg/kg
Topical (spot-on) Mites 0.5 mg/kg
Topical (spot-on) Lice 0.5 mg/kg
Topical (spot-on) Haematobia irritans 0.5 mg/kg; ~4 weeks protections
Topical (spot-on) Boophilus microplus 0.5 mg/kg; no knock-down effect. Control usually incomplete (75-85%). ~7 weeks protection.

DISCLAIMER: Liability is denied for any possible damage or harm to persons, animals or any other goods that could follow the transmission or use of the information, data or recommendations in this site by any site visitor or third parties.


SAFETY

Oral LD50, rat, acute*:  55 mg/kg
Dermal LD50, rat, acute*: not found
* 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

* 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. Eprinomectin is usually allowed for use on dairy cattle.

Learn more about eprinomectin safety.

General safety information for antiparasitics is available in specific articles in this site (click to visit):

WARNING

Never use products for livestock on dogs and cats unless they are explicitly approved for both livestock and pets. Pets may not tolerate livestock formulations.

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: MERCK SHARP & DOHME (→ MERIAL)
Some original brands: EPRINEX, LONGRANGE, BROADLINE
Patent: Expired (particular formulations may be still patent-protected)

Use in LIVESTOCK: Moderate. Only in cattle

Use in HORSES: NO
Use in
DOGS and CATS: YES, rather scarce
Main delivery forms: 

Use in human medicine: No
Use in
public/domestic hygiene: No
Use in
agriculture: No
Generics available: 
Yes, a few


PARASITE RESISTANCE

In livestock: Yes, cross-resistance with ivermectin, very frequent in gastrointestinal roundworms of sheep, goats and cattle. There are a few reports on cattle tick (Boophilus microplus) resistance to ivermectin likely to show cross-resistance to eprinomectin.

Learn more about parasite resistance and how it develops.


SPECIFIC FEATURES

Eprinomectin is the "ivermectin" for dairy, because for years it was the only macrocyclic lactone approved in most countries for use on dairy cows whose milk is intended for human consumption. In the meantime other macrocycli lactones (e.g. moxidectin, doramectin) have been also approved for use on dairy cows in some countries.

During about two decades the 0.5% pour-on (EPRINEX) was the only formulation available with eprinomectin from MERIAL. Only in 2014 MERIAL has introduced LONGRANGE in a few countries (e.g. the USA), a long-acting injectable for cattle containing 5% eprinomectin. Interestingly, for many years MERIAL has marketed a long-acting 3.15% ivermectin injectable (IVOMEC GOLD) for cattle in numerous countries (mainly Latin America), but not in the USA or the EU.

In 2014 MERIAL has also introduced BROADLINE, a spot-on for cats containing a mixture of eprinomectin, fipronil, praziquantel and methoprene., the first eprinomectin-based product approved for cats.

Spectrum of activity and efficacy of eprinomectin are comparable to those of ivermectin. However only the pour-on formulation is approved for dairy cows, not the extended-release injectable.

Efficacy of eprinomectin

In cattle eprinomectin is effective against the major parasitic roundworms: gastrointestinal (e.g. Haemonchus spp, Cooperia spp, Ostertagia spp, Trichostrongylus spp) and pulmonary (e.g. Dictyocaulus spp). It is also effective againts several ectoparasites such as mites and lice species, and against numerous myiases (e.g. those caused by screwworm flies, bot flies and warble flies).

However, at the usual therapeutic dose, eprinomectin products are ineffective against tapeworms and flukes, fleas, mosquitoes, fleas, horse and deer flies and stable flies and several other flying insects. The eprinomectin pour-on provides some control of horn flies and cattle ticks (Boophilus spp). But other ticks (e.g. Amblyomma spp, Hyalomma spp Dermacentor spp, Ixodes spp, Rhipicephalus spp) are not controlled at all by eprinomectin products.

Pharmacokinetics of eprinomectin

After topical administration (pour-on) only about 46% of the administered dose is absorbed through the skin, the rest remains outside and breaks down slowly or is washed away. The halftime for absorption in dairy cows is about 0.95 days. Most of the administered dose is absorbed in the first 7 to 10 days after treatment, but absorption continues until 17 to 21 days. Peak plasma concentrations are reached 2 to 5 days after treatment.

After treatment with the extended-release injectable a polymeric PLGA [poly(lactic-co-glycolic) acid] matrix is formed in the subcutanous tissue. The active ingredient is slowly released from the matrix into the bloodstream maintaing effective parasiticidal blood levels for months.

Once absorbed into blood eprinomectin is poorly metabolized in the bovine's organism. It is well distributed throughout the host's body and the maximum concentrations are found in liver and kidneys. After pour-on administration, eprinomectin does not appear in milk and this is why it was the only macrocyclic lactone approved for use in dairy cows (only the pour-on formulation!). Metabolism after treatment with the extended-release injectable is also scarce.

Eprinomectin is excreted mainly through the feces, only a very small portion through the urine.

Mechanism of action of eprinomectin

As all macrocyclic lactones eprinomectin acts as agonist of the GABA (gamma-aminobutyric acid) neurotransmitter in nerve cells and also binds to glutamate-gated chloride channels in nerve and muscle cells of invertebrates. In both cases it blocks the transmission of neuronal signals of the parasites, which are either paralyzed and expelled out of the body, or they starve. It also affects the reproduction of some parasites by diminishing oviposition or inducing an abnormal oogenesis.

In mammals the GABA receptors occur only in the central nervous system (CNS), i.e. in the brain and the spinal chord. But mammals have a so-called blood-brain barrier that prevents microscopic objects and large molecules to get into the brain. Consequently macrocyclic lactones are much less toxic to mammals than to the parasites that do not have such a barrier, which allows quite high safety margins for use on livestock and pets. A notable exception to this are those dogs that carry the MDR-1 mutation.

Click here to view the list of all technical summaries of antiparasitic active ingredients in this site.

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