Doramectin: Avermectin A1a, 25-cyclohexyl-5-O-demethyl-25-de(1-methylpropyl)-; (5'S,6S,6'R,11R,13S,15S,17aR,20R,20aR,20bS)-6'-cyclohexyl-20,20b-dihydroxy-5',6,8,19-tetramethyl-17-oxo-5',6,6',10,11,14,15,17,17a,20,20a,20b-dodecahydro-2H,7H-spiro[11,15-methanofuro[4,3,2-pq][2,6]benzodioxacyclooctadecine-13,2'-pyran]-7-yl (4xi)-2,6-dideoxy-4-O-(2,6-dideoxy-3-O-methyl-α-L-arabino-hexopyranosyl)-3-O-methyl-α-L-threo-hexopyranosideSpecification:Items | Specification | Result |
Appearance | White powder | White powder |
Identification | HPLC:The retention time of major peak of test solution should correspond to that of reference solution | Conforms |
IR:Sample spectrum corresponds to that of standard spectrum | Conforms |
Appearance of solution | The solution is clear and not more intensely colored than reference solution BY6 | Conforms |
Related Substance | Avermectin NMT 2.0% | 0.008 |
Total impurities NMT 5.0% | 0.039 |
Residual Solvents | Ethanol NMT 30000ppm | 360ppm |
Acetone NMT 5000ppm | 140ppm |
BHT | NMT 2000ppm | 316ppm |
Sulphated Ash | NMT 0.1% | 0.0007 |
Heavy Metal | NMT 200ppm | <20ppm |
Water | NMT 3.0% | 0.018 |
Assay(on anhydrous and solvent free basis) | ≥95% | 0.981 |
Doramectin Basic information
Pig antiparasitic Pharmacological effects Precautions
Product Name: Doramectin
Synonyms: DM/CBR15;25-CYCLOHEXYL-5-O-DEMETHYL-25-DE(1-METHYLPROPYL)AVERMECTIN;DORAMECTIN;Doramectin VETRANAL;Doromectin; 25-Cclohexyl-avermectin B1;25-Cyclohexyl-5-O-demethyl-25-de(1-methylpropyl)avermectin A1A;Dectoma
CAS: 117704-25-3
MF: C50H74O14
MW: 899.11
EINECS: 601-490-4
Product Categories: -;Antiparasitic;Intermediates & Fine Chemicals;Pharmaceuticals;IMIPEM;Inhibitors;raw material-
Mol File: 117704-25-3.mol
Pharmacological effects
[Chemical properties] brown powder , very low solubility in water.
Doramectin is used for the treatment of livestock diseases such as nematodes and mites ectoparasitosis,it is fermented by recombinant avermitilis (Streptomyces avermitilis) new strain, and the main difference from ivermectin is that C25 is substituted by cyclohexyl. It is a new, broad-spectrum antiparasitic drug,and is efficient for gastrointestinal nematodes, lung nematodes, Euglena, lice, ticks, mites and wound maggots , also has a good effect on internal and external parasites especially certain nematodes (round worms) and arthropods , but invalid to tapeworms, flukes and protozoa . Its mechanism of action is to increase the release of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) of the worm, thereby blocking the transmission of nerve signals, so that muscle cells lose their ability to contract, resulting in death of the parasites. the neurotransmitter of Peripheral nerves of mammals is acetylcholine,and will not be affected by Doramectin, doramectin cannot go through the blood-brain barrier easily , minimal damage to the central nervous system,safe to cattle. The main feature is that the plasma concentration and half-life are higher or twice than Ivermectin. The United States has approved to use as cattle, pigs and dedicated injection and cattle dedicated pour.
Precautions 1, doramectin is unstable and decomposes rapidly in the sunlight to be inactivated, its remnants of drugs are toxic to fish and aquatic organisms, so pay attention to water protection.
2, pour-on: bovine application, not rain within 6 hours.
3, use with caution in dogs.
4, the goods will be placed out of reach of children, the operator should not eat or smoking, wash hands after handling.
5, withdrawal period, 35 days of cattle, pigs 24 days.
Chemical Properties White Solid
Uses antibacterial
Uses Doramectin is a biosynthetic avermectin derived from a mutant strain of Streptomyces avermitilis, supplemented with a cyclohexylcaboxylic acid starting unit. Doramectin was developed as an anthelmintic for internal parasite control. The presence of the cyclohexyl group replacing the sec-butyl moiety affords greater hydrophobicity and longer biological half-life compared to avermectin. Like the other milbemycin/avermectins, it selectively binds to parasite glutamate-gated chloride ion channels and disrupts neurotransmission leading to paralysis and death of the parasite.
Uses A mutational biosynthetic antiparasitic antibiotic.
Uses Mutational biosynthetic antiparasitic antibiotic structurally related to the avermectins
Veterinary Drugs and Treatments Doramectin injection is indicated for the treatment and control of the following endo- and ectoparasites in cattle: roundworms (adults and some fourth stage larvae)-Ostertagia ostertagi (including inhibited larvae), O. lyrata, Haemonchus placei, Trichostrongylus axei, T. colubriformis, T. longispicularis, Cooperia oncophora, C. pectinata, C. punctata, C. surnabada (syn. mcmasteri), Bunostomum phlebotomum, Strongyloides papillosus, Oesophagostomum radiatum, Trichuris spp.; lungworms (adults and fourth stage larvae)-Dictyocaulus viviparus; eyeworms (adults)-Thelazia spp.; grubs (parasitic stages)-Hypoderma bovis, H. lineatum; lice-Haematopinus eurysternus, Linognathus vituli, Solenopotes capillatus; and mange mites-Psoroptes bovis, Sarcoptes scabiei.
In swine the injection is labeled for the treatment and control gastrointestinal roundworms (adults and 4th stage Ascaris suum, adults and 4th stage Oesophagostomum dentatum, Oesophagostomum quadrispinolatum adults, Strongyloides ransomi adults, and Hydrostrongylus rubidus adults), lungworms (Stephanurus dentatus adults), mange mites (adults and immature stages Sarcoptes scabeii var. suis), and sucking lice (adults and immature stages Haematopinus suis)
The manufacturer states the doramectin protects cattle against infection or reinfection with Ostertagia ostertagi for up to 21 days. Doramectin topical (pour-on) is approved for use in cattle and has a similar spectrum of action against a variety of endo- and ectoparasites, including biting lice.
Injectable doramectin has been used for treating a variety of nematode and arthropod parasites in companion animals, including generalized demodicosis in dogs and cats and spirocercosis in dogs.