Doramectin

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Structural formula
Structure of Doramectin
General
Non-proprietary name Doramectin
other names

25-Cyclohexyl-5- O- dimethyl-25-de (1-methylpropyl) avermectin A 1a

Molecular formula C 50 H 74 O 14
External identifiers / databases
CAS number 117704-25-3
EC number 601-490-4
ECHA InfoCard 100.123.125
PubChem 6436133
ChemSpider 21258022
Wikidata Q906534
Drug information
ATC code

Q P54AA03

Drug class

Antiparasitic

Mechanism of action

Increase of the membrane permeability for chloride

properties
Molar mass 899.11 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances
06 - Toxic or very toxic 09 - Dangerous for the environment

danger

H and P phrases H: 301-410
P: 273-301 + 310-501
Toxicological data

50–100 mg kg −1 ( LD 50 ,  rat ,  oral )

As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Doramectin is a macrocyclic lactone ( macrolide ) and glycoside . As a medicinal substance, it belongs to the group of avermectins (fermentation product of Streptomyces avermitilis ) and is closely related to ivermectin , but with an additional cyclohexyl group it is longer effective. Doramectin is used in veterinary medicine as an anti-parasitic agent.

Chemical properties and pharmacology

Doramectin is highly lipophilic and good in many organic solvents, but hardly soluble in water.

Like all avermectins increasing the membrane permeability of nerve cells in nematodes and the nerve and muscle cells in arthropods for chloride - ion ( see also ivermectin ). Doramectin therefore acts as a broad-spectrum anti-parasitic agent and has both worm-killing (vermicidal) and insect and mite-killing properties. On the other hand, the drug is not effective against suckers and tapeworms .

Doramectin is mostly administered subcutaneously and is distributed in all tissues, with the highest concentration in adipose tissue. When applied topically , the bioavailability is significantly lower. The plasma half-life is 10 days. It is excreted primarily through the bile and then through the faeces.

Contraindications

Doramectin is well tolerated, not carcinogenic or mutagenic. It can also be used in pregnant and young animals. However , the product must not be used in dogs with MDR1 defects .

Trade names

Dectomax ad us. vet. , Dectomax 0.5% pour-on solution ad us. vet. , Doramec LA , Doraquest LA Oral Gel

Web links

  • Entry on Doramectin at Vetpharm, accessed July 30, 2012.

Individual evidence

  1. ↑ a b c Datasheet Doramectin from Sigma-Aldrich , accessed on May 14, 2017 ( PDF ).