Emodepside is an antiparasitic active ingredient used in veterinary medicine in dogs and cats against internal parasites (mainly roundworms). It is not used against agricultural and household pests. It belongs to the chemical class of the depsipeptides.
Common name: EMODEPSIDE
Type: veterinary medecine
Chemical class: Depsipeptide
EFFICACY AGAINST PARASITES
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.
Emodepside is a broad-spectrum nematicide used moderately in pets for the control of roundworms, either for oral administration (tablets) to dogs, or for topical administration (spot-on) to cats. It is not used in livestock or horses. Emodepside has no efficacy whatsoever against tapeworms, flukes or any external parasites. It is mostly used in combination with praziquantel to ensure simultaneous tapeworm control.
The table below indicates some usual dosing recommendations for emodepside issued by manufacturers or documented in the scientific literature. They may not be approved in some countries.
|Dosing recommendations for EMODEPSIDE
|Delivery||Parasites||Dose (against emodepside-susceptible parasites)
|Oral (tablets)||Roundworms||>1 mg/kg|
|Topical (spot-on)||Roundworms||3-15 mg/kg, dep. on animal's weight|
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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.
Oral LD50, rat, acute*: >500 mg/kg
Dermal LD50, rat, acute*: >2000 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): Not applicable: not approved for livestock
Withholding periods for meat, milk, eggs: Not applicable: not approved for livestock
WARNING: Dogs of some breeds do not tolerate emodepside or macrocyclic lactones (e.g. ivermectin, milbemycin oxime, moxidectin, selamectin, etc.) that can cross the blood-brain barrier. They can suffer more or less serious adverse effects if treated at dose rates slightly higher than the recommended ones. Consequently dosing must be as accurate as possible. This is the case for Collies and related breeds, which have a mutation in the MDR-1 gene that affects the blood-brain barrier and makes it more permeable to such compounds than in dogs without this mutation. Besides Collies, other dog breeds have shown similar problems, although the MDR-1 mutation has not been confirmed in all of them. The breeds more affected by this mutation are (% frequency): Collie (70%), Long-haired Whippet (65%), Australian Shepherd (50%, also mini), McNab (30%), Silken Windhound (30%), English Shepherd (15%), Shetland Sheepdog (15%), English Shepherd (15%), German Shepherd (10%), Herding Breed Cross (10%). Other less affected breeds are: Old English Sheepdog, Border Collie, Berger Blanc Suisse, Bobtail, Wäller. The only way to be sure that a dog is affected or not is to test for it. As more dogs are tested it is likely that the mutation is discovered in other breeds, or that the frequencies change.
Learn more about emodepside safety.
General information on the safety of veterinary 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
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: PROFENDER
Patent: Expired (particular formulations may be still patent-protected)
Use in LIVESTOCK: No
Use in HORSES: No
Use in DOGS and CATS: Yes, scarce
Main delivery forms:
Use in human medicine: No
Use in public/domestic hygiene: No
Use in agriculture: No
Generics available: Yes, but very few
In dogs and cats: No
Emodepside is a semi-synthetic derivative of fermentation products from Mycelia sterilia, a fungus that grows on leaves of Camellia japonica, the Japanese camellia.
Efficacy of emodepside
Emodepside is a medium-spectrum nematicide, highly effective against several gastrointestinal worms of pets (e.g. Ancylostoma spp, Angiostrongylus vasorum, Crenosoma vulpis, Toxascaris leonina, Toxocara canis, Toxocara cati, Trichuris vulpis, Uncinaria stenocephala). It also inhibits egg production of the worms.
Pharmacokinetics of emodepside
Following topical administration emodepside is absorbed slowly into the bloodstream. Maximum plasma levels are reached 2-3 days after treatment. Absorption after oral administration is higher if administered to fasted animals. Bioavailability after oral administration is ~50%. Emodepside is distributed throughout the whole organism, but highest concentrations are found in fat tissues, where it forms a deposit that is slowly released.
Excretion is slow: halftime after topical administration to cats is ~9 days. In rats, about 45-55% of the administered dose is excreted unchanged, mainly through feces, the rest in the form of numerous metabolites.
Mechanism of action of emodepside
Emodepside has a molecular mode of action that is different from the one of most other anthelmintics. It binds to so-called latrophilin receptors in neuromuscular junctions of the worm muscle cells. There is also evidence that it interferes with the potassium channels in the neuronal membranes. The bottom line for the parasites is that they are paralyzed and die or are expelled.
Click here to view the list of all technical summaries of antiparasitic active ingredients in this site.