5 Must-Have Features in a Eprinomectin for Veterinary Use

What is eprinomectin + praziquantel?

Eprinomectin + praziquantel (brand name Centragard®) is a topical (spot-on) antiparasitic drug used to treat and control hookworm, roundworm, and tapeworm infections, and to prevent heartworm disease in cats and kittens that are at least 7 weeks of age and weigh at least 0.8 kg (1.8 lbs).

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It may be used off label (extra label) in other species. Many drugs are commonly prescribed for off-label use in veterinary medicine. “Off label” means the drug is being used in a way that has not been reviewed or approved by the U.S. Food and Drug Administration (FDA) or Health Canada. In these instances, follow your veterinarian’s directions and cautions carefully, as they may be significantly different from those on the label.

How do I give my pet eprinomectin + praziquantel?

Eprinomectin + praziquantel comes in topical solution form.

• Topical solutions are applied directly onto the skin. Part the fur at the base of the head and apply the product directly to visible skin as per manufacturer instructions.
• Do not apply to broken skin or wet fur.
• Do not allow your pet to contact the application site for at least 5 hours after applying the medication.
• Do not allow this medication to touch the eyes or mouth.

This medication should take effect within 1 to 2 days; however, effects may not be noted outwardly for several days.

What if I miss giving my pet the medication?

If you miss a dose, give it as soon as you remember, and then continue with the regular dosing schedule. However, if it is almost time for the next dose, skip the missed dose and resume the regular dosing schedule. Do not give the pet two doses at once.

Are there any potential side effects from eprinomectin + praziquantel?

Eprinomectin + praziquantel may cause the following side effects:

• scratching or irritation at site of application
• lack of appetite and/or energy
• vomiting
• fur loss

The following reactions are rare, but if they occur, contact your veterinarian immediately:

• an allergic reaction such as irregular breathing, rash, fever, puffiness and swelling around the face
• neurologic toxicity in cats with two copies of the MDR1 mutation:
  • unsteady gait (ataxia)
  • drooling
  • tremors
  • weakness and/or partial paralysis
  • coma
  • seizures
  • death

Drug sensitivities can develop over time with repeated exposure. Your pet may have no reaction after the first few doses but may develop a sensitivity later. It is important to watch for signs of an allergic reaction over the entire course of treatment.

Other side effects may occur. If you notice anything unusual, contact your veterinarian immediately. This moderate-acting medication lasts for several days, although effects can be longer in pets with liver or kidney disease.

Are there any risk factors for this medication?

Eprinomectin + praziquantel should NOT BE USED in cats who:

• are allergic to any component of the medication
• are under 7 weeks of age or under 0.8 kg (1.8 lb)
• are known to have two copies of the MDR1 mutation

Eprinomectin + praziquantel should be USED WITH CAUTION in cats who:

• are pregnant or used for breeding 
• have tested positive for heartworm disease

Are there any drug interactions I should be aware of?

Certain medications should be USED WITH CAUTION when given with eprinomectin + praziquantel, including:

• albendazole
• azole antifungals
• cimetidine
• medications that affect CYP34A (e.g., dexamethasone, phenobarbital, rifampin, fluoxetine)
• medications that affect P-glycoprotein (e.g., amiodarone, cyclosporine, digoxin, spironolactone)
• medications or supplements containing grapefruit juice

Be sure to tell your veterinarian about any medications (including vitamins, supplements, or herbal therapies) that your pet is taking before starting any new treatment.

Is any monitoring needed with this medication?

• Your veterinarian may schedule follow-up visits for monitoring. In this case, follow your veterinarian’s directions.
• At home, monitor for any abnormal changes. If these occur, discontinue the medication and contact your veterinarian.

How do I store eprinomectin + praziquantel?

• Store protected from light at or below 30°C (86°F).
• Keep medication out of reach of children and pets.

What should I do in case of emergency?

If you suspect an overdose or an adverse reaction to the medication, call your veterinary office immediately. If they are not available, follow their directions in contacting an emergency facility.

Eprinomectin is a broad-spectrum antiparasitic active ingredient used in veterinary medicine in cats and livestock against external parasites (lice, mites, etc.) as well as against internal parasites (e.g. roundworms). It is not used against agricultural and household pests. It belongs to the chemical class of the macrocyclic lactones.

Common name: EPRINOMECTIN

Type: veterinary medicine
Chemical class: macrocyclic lactone

CHEMICAL STRUCTURE

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

Click here to view the article in this site with the most common dosing recommendations for eprinomectin used in domestic animals.

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.

Contact us to discuss your requirements of Eprinomectin for Veterinary Use. Our experienced sales team can help you identify the options that best suit your needs.

Learn more about eprinomectin 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

MARKETING & USAGE

Decade of introduction:
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 in cattle, sheep & goats

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

• Pour-on
• Spot-on
• Injectable

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.

Visit also the section in this site about parasite resistance to antiparasitics and more specifically to eprinomectin.

SPECIFIC FEATURES

Eprinomectin is the "ivermectin" for dairy cattle, 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. Eprinomectin has also been approved for use in shee and goats in some countries.

During about two decades the 0.5% pour-on (EPRINEX) for cattle was the only formulation available with eprinomectin. Only in MERIAL introduced LONGRANGE, a long-acting injectable for cattle containing 5% eprinomectin. Interestingly, for many years MERIAL 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. And in MERIAL introduced EPRINEX MULTI, a 0.5% pour-on approved for use in cattle, sheep & goats.

In MERIAL 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 andlice species, and against numerous myiases (e.g. those caused by screwworm flies, bot flies and warble flies).

strong>However, at the usual therapeutic dose, eprinomectin products are ineffective against tapeworms and flukes, fleas, mosquitoes, fleas, horse and deer flies andstable 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. Metabolism after treatment with the extended-release injectable is also scarce.

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!).

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.

For more information, please visit Eprinomectin Api Manufacturers.