Emodepside

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Structural formula
Structural formula of emodepside
General
Non-proprietary name Emodepside
other names

Cyclo [ D -2-hydroxypropanoyl- N -methyly- L -leucyl-3- [4- (4-morpholinyl) -phenyl] - D -2-hydroxypropanoyl- N- methyl- L -leucyl- D -2-hydroxypropanoyl- N -methyl- L -leucyl-3- [4- (4-morpholinyl) -phenyl] - D -2-hydroxypropanoyl- N -methyl- L -leucyl] ( IUPAC )

Molecular formula C 60 H 90 N 6 O 14
Brief description

white to yellowish, odorless powder

External identifiers / databases
CAS number 155030-63-0
EC number 604-993-7
ECHA InfoCard 100.123.218
PubChem 6918632
ChemSpider 5293825
DrugBank DB11403
Wikidata Q1339032
Drug information
ATC code

Q P52AA51

Drug class

Anthelmintics

properties
Molar mass 1119.42 g · mol -1
solubility

practically insoluble in water (5.2 mg l −1 at pH 7)

safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances
09 - Dangerous for the environment 08 - Dangerous to health

Caution

H and P phrases H: 372-410
P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Emodepside is an anthelmintic used in veterinary medicine with a broad spectrum of activity against roundworms . It is a semi-synthetic derivative of the fermentation product of the fungus Mycelia sterilia . It is approved in combination with praziquantel under the brand name Profender ( Bayer AG ) for use on the skin ( spot-on ) in cats and in tablet form for oral administration for dogs and under the trade name Procox as an oral solution in combination with toltrazuril for dogs.

The drug blocks the neuromuscular synapses of the pharynx and the body muscles of the nematodes and paralyzes the parasites. After application, the active ingredient accumulates in the fatty tissue and is slowly released from there. The elimination half-life is about 9 days.

Side effects

Occasionally, cats experience whitish residue or hair loss at the site of application. At ten times the recommended daily dose, there is a slight flow of saliva and slight muscle spasms, which disappear again after discontinuing the preparation.

In dogs, the active ingredient should be administered on an empty stomach to ensure slow release. In dogs with MDR1 (- / -) the active ingredient has a narrow therapeutic range : even if the recommended dose is doubled, nausea and unsteadiness can occur in these animals . In all other dogs, these symptoms can very rarely also occur when administered with the food and thus the active substance is released too quickly. The side effects disappear within a day without treatment , and no specific antidote is known.

Individual evidence

  1. ↑ a b Entry on emodepside at Vetpharm, accessed on August 4, 2012.
  2. ↑ Template: CL Inventory / not harmonized There is not yet a harmonized classification for this substance . What is shown is a labeling of (3S, 6R, 9S, 12R, 15S, 18R, 21S, 24R) -3,9,15,21-tetraisobutyl-4,6,10,16,18,22 derived from a self-classification by the distributor -hexamethyl-12,24-bis [4- (4-morpholinyl) benzyl] -1,7,13,19-tetraoxa-4,10,16,22-tetraazacyclotetracosane-2,5,8,11,14,17 , 20.23-octone in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on January 20, 2020.

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